NCM 106: PHARMACOLOGY

LECTURE
MODULE 5: RESPIRATORY AND DRUGS FOR UPPER RESPIRATORY
GASTROINTESTINAL DRUGS DISORDERS

Outline: UPPER RESPIRATORY DISORDERS

A. Respiratory System
• Drugs for Upper Respiratory Disorders
• Drugs for Lower Respiratory Disorders
B. Gastrointestinal System
• Drugs for Gastrointestinal Tract Disorder
• Antiulcer Drugs
RESPIRATORY SYSTEM
The Respiratory tract is divided into two major parts:
1. Upper Respiratory Tract
2. Lower Respiratory Tract
Respiration and ventilation are distinct terms and
should not be used interchangeably
Respiration
- process of gas exchange in the alveolar
capillary membrane
PHASES OF RESPIRATION
1. Ventilation
- phase in which oxygen passes through the
airways (Inspiration and Expiration)
- movement of air from the atmosphere and
should not be used interchangeably
2. Perfusion
- involves blood flow at the alveolar capillary
bed
- influenced by alveolar pressure
- perfusion of each of the alveolus must be
matched by adequate ventilation
3. Diffusion
- movement of molecules from higher to lower
concentration
- takes place when oxygen passes through the
capillary bed to be circulated and carbon
dioxide leaves the capillary bed and diffuses
into the alveoli for ventilator excretion
Common colds (most prevalent)
- Caused by rhinovirus and affects
primarily the nasopharyngeal tract.
- Most contagious 1 to 4 days before the
onset of symptoms (incubation period)
and during the last 3 days of the colds.
- Symptoms include: rhinorrhea (watery
nasal discharge); nasal congestion,
cough and increased mucosal
secretions.
Acute rhinitis
- Acute inflammation of the mucus
membranes of the nose, usually
accompanies the common cold.
Sinusitis
- inflammation of the mucous membranes of
one or more of the maxillary, frontal,
ethmoid, or sphenoid sinuses
• Systemic or nasal decongestant
may be indicated
• Acetaminophen, fluids and rest may
be helpful
• Antibiotic may be prescribed for
acute or severe sinusitis
Acute Pharyngitis
- inflammation of the throat/sore throat
- can be caused by a virus, bacteria, beta-
hemolytic streptococci
- can occur alone or with the common cold
and rhinitis or acute sinusitis
• Saline gargles, lozenges, increased
fluid intake are usually indicated
• Acetaminophen may be taken to
decrease elevated temperature
• Antibiotics are not effective for viral
pharyngitis
Drugs used to manage cold symptoms includes:
• Antihistamines (H1 blockers)
• Decongestants (sympathomimetic amines)
• Antitussives
• Expectorants
ü These drugs can be used singly or in
combination preparations.
ANTIHISTAMINES (H1 blockers or H1 antagonist)
- suppress the histamine-induced wheal
response (swelling) and flare response
(vasodilation) by blocking the binding of
histamine to its receptors or reducing
histamine receptor activity on nerves,
vascular smooth muscle, glandular cells,
endothelium, and mast cells.

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First Generation Antihistamines
- can cause drowsiness, dry mouth and other
anticholinergic symptoms
- patients should be alerted not to drive or
operate dangerous machinery when taking
Diphenhydramine
- Blocks the effects of histamine by competing
for and occupying H1 receptor sites.
- Has anticholinergic effects and should and
should not be used by patient with narrow-
angle glaucoma.
- Can cause CNS depression if taken with
alcohol, narcotics hypnotics and barbiturates.
- Side effects: drowsiness, dizziness, fatigue,
disturbed coordination, skin rash, dry mouth,
urine retention, blurred vision and wheezing.
- Onset of action: 15 minutes (Oral and IM),
Immediate (IV)
- Duration of action: 4 to 6 hours
Benadryl
- frequently combined with other ingredients in
cold remedy preparations
- primary use is to treat rhinitis
Second Generation Antihistamines
- fewer anticholinergic effects and a lower
incidence of drowsiness
- frequently called nonsedating antihistamines
because they have little to no effect on
sedation
• Cetirizine (Zyrtec)
• Fexofenadine (Allegra)
• Loratidine (Claritin)
Cholinergic substance
- capable of producing, altering, or releasing
acetylcholine, or butyrylcholine
("indirectacting"), or mimicking their
behaviors at one or more of the body's
acetylcholine receptor ("direct-acting") or
butyrylcholine receptor types ("direct-
acting").
Cholinergic crisis
- an episode of excessive stimulation at one of
the body’s neuromuscular junction points
- results from a buildup of acetylcholine (Ach)
stemming from acetylcholinesterase
inactivity or insufficiency
- common cause is the unintended overdose
of treatment drugs in myasthenia gravis
patients
o Signs of cholinergic crisis
• Diarrhea
• Urination
• Miosis
• Bradycardia
• Emesis
• Lacrimation
• Lethargy
• Salivation
o Side effects of anticholinergics
• Blurred vision
• Urinary retention
• Dry mouth
• Constipation
• Dry eyes
• Dizziness due to drop in blood
pressure on standing up
(Postural hypotension)
• Cognitive problems (confusion)
• Heart rhythm disturbance
NASAL AND SYSTEMIC DECONGESTANTS
Nasal decongestants
- stimulates the alpha adrenergic receptors,
producing vascular constriction
(vasoconstriction) of the capillaries within the
nasal mucosa.
- The result is shrinking of the nasal mucous
membranes and a reduction in fluid
secretion.
- Administered by nasal spray or drops or in
tablet, capsule or liquid form.
- Frequent use of decongestants, especially
nasal spray or drops, can result in tolerance
and rebound nasal congestion.
Systemic Decongestants
- alpha-adrenergic agonists
- available in tablet, capsule, and liquid form
- used primarily for allergic rhinitis, hay fever,
acute coryza
• Ephedrine
• Phenylephrine
• Oxymetazoline
• Pseudoephedrine
o Side effects:
• Jittery, nervous, or restless
(decrease or disappear as the
body adjusts to the drug)
• Rebound nasal congestion
• Increase blood pressure and
glucose level
Note: use in extreme caution in patient with
hypertension, cardiac disease, hyperthyroidism and
diabetes mellitus.
Drug interactions:
• Pseudoephedrine may decrease the effect of
beta blockers.
• Hypertension or cardiac dysrhythmias if
taken with MAOI’s (monoamine oxidase
inhibitors)
• Coffee and tea can increase restlessness
and palpitations.
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INTRANASAL GLUCOCORTICOIDS
- Effective for treating allergic rhinitis because
they have an inflammatory action, thus
decreasing the allergic rhinitis symptoms of
rhinorrhea, sneezing and congestion
- Undergo rapid deactivation after absorption.
Most allergic rhinitis is seasonal; therefore
the drugs are for short-term use unless
otherwise indicated by the health care
provider
• Beclomethasone
• Budesonide
• Dexamethasone
• Flunisolide
• Fluticasone
• Mometasone
• Triamcinolone
ANTITUSSIVES
- Act on the cough-control center in the
medulla to suppress the cough reflex.
- The cough is a naturally protective way to
clear the airway of secretions or any
collected material. Sore throat may cause
coughing that increases throat irritation.
- If the cough is non-productive and irritating,
an antitussive may be taken.
- Usually used in combination with other
agents
3 types of antitussives:
1. Nonopioid
2. Opioid
3. Combination
Codeine
- opioid antitussive
- usually mixed with antihistamine,
decongestant, and/or expectorant
- can cause drowsiness, dizziness, nausea,
constipation, and respiratory depression
Dextromethrophan (Robittusin, Sucrets)
- nonnarcotic antitussive/an expectorant
- reduces the viscosity of tenacious secretions
- also acts as a nonopioid antitussive by
changing non-productive cough to a less
frequent productive cough
- Onset of action:
• 15 to 30 minutes
• Duration 3 to 6 hours
- Side effects: Dizziness, drowsiness,
confusion, fatigue, ataxia, GI distress,
nervousness
- Adverse reaction:
• Respiratory depression (life threatening)
• Serotonin syndrome
EXPECTORANT
- loosen bronchial secretions so they can be
- eliminated by coughing
- can be used with or without other
pharmacologic agents
- found in many OTC cold remedies along with
analgesics, antihistamines, decongestants,
and antitussives
- hydration – best natural expectorant
Guaifenesin
- most common expectorant
- for dry, unproductive cough
- may be combined with other cold remedies,
take water to loosen mucus
- can cause nausea and vomiting
DRUGS FOR LOWER RESPIRATORY
DISORDERS
LOWER RESPIRATORY DISORDERS
• Chronic obstructive pulmonary disease (COPD)
- caused by airway obstruction with increased
airway resistance of airflow to lung tissues.
Medications prescribed for COPD include:
• Bronchodilators – to assist in opening
narrowed airways.
• Glucocorticoids (steroids) – to decrease
inflammation.
• Leukotriene modifiers – to reduce
inflammation in the lung tissue
• Cromolyn – acts as an inflammatory agent
by suppressing the release of histamine and
other mediators from the mast cells.
• Expectorants – to assist in loosening mucus
from the airways.
• Antibiotics – to prevent serious
complications, from bacterial infections
• Restrictive lung disease
- decrease in total lung capacity as a result of
fluid accumulation or loss of elasticity of the
lung
Cyclic adenosine monophosphate (cAMP)
- cellular signaling molecule, that is involved in
many cellular activities and maintains
bronchodilation.
SYMPATHOMIMETIC DRUGS
- also known as adrenergic drugs and
adrenergic amines)
- stimulant compounds which mimic the
effects of endogenous agonists of the
sympathetic nervous system
- are able to directly activate adrenergic
receptors or to indirectly activate them by
increasing norepinephrine and epinephrine
- The primary endogenous agonists which
function as both neurotransmitters and
hormones, of the sympathetic nervous
system are the:
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o catecholamine (epinephrine –
adrenaline)
o norepinephrine (noradrenaline)
o dopamine
- Used to treat cardiac arrest and low blood
pressure, or even delay premature labor,
among other things
- Long-acting sympathomimetics are used for
maintenance
ALPHA AND BETA2 ADRENERGIC AGENTS
- First line of defense in an acute asthma
attack
- Promote cAMP production and promotes
bronchodilation
- Can be administered orally or by inhalation
with a metered-dose inhaler
- For long-term asthma treatment, beta2-
adrenergic agonists are frequently
administered by inhalation (delivers more of
the drug directly to the constricted bronchial
site)
- Onset of action: 1 minute (oral inhalation), 5-
30 minutes (nebulization), 15-30 minutes
(orally)
- Note: Excessive use of the aerosol drug can
lead to tolerance and loss of drug
effectiveness.
- Side effects: tremors, headaches,
nervousness, increased pulse rate,
palpitations (high dosage)
ANTICHOLINERGICS
Tiotropium
- Used for maintenance treatment of
bronchospasms
- Administered by inhalation only with the
HandiHaler device (dry-powder capsule
inhaler)
- HandiHalers should be washed with warm
water and dried.
- Side effects: dry mouth, constipation,
vomiting, dyspepsia, abdominal pain,
depression, insomnia, headache, joint pain,
and peripheral edema.
Ipratropium bromide
- For bronchospasm associated with COPD,
including asthma.
- Used to treat asthmatic conditions by dilating
the bronchioles.
- Fewer systemic effects.
- Administered by MDI
- Ipratropium with albuterol sulfate is used to
treat COPD

Albuterol
- For acute and chronic asthma, bronchitis,
and exercise induced bronchospasm.
- selective beta2 drug that is effective for
treatment and control of asthma by causing
bronchodilation with long duration of action

Metaproterenol
- has some beta1 effect but is primarily used
as a beta2 agent

Isoproterenol
- For acute bronchospasm
- stimulates both beta1 and beta2 receptors
- administered by inhalation, using an aerosol
inhaler or nebulizer, or intravenously (IV) for
severe asthmatic attacks.

Levalbuterol
- For acute bronchospasm and prevention of
exercise-induced asthma. Product from
albuterol derivative.

• Beta1 stimulation causes heart rate increases

and tachycardia
• Beta2 stimulation promotes bronchodilation

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LECTURE
METHYLXANTHINE (XANTHINE) DERIVATIVES
- second major group of bronchodilators used
to treat asthma
- includes: aminophylline, caffeine,
theophylline
Theophylline
- Relaxes the smooth muscles of the bronchi,
bronchioles and pulmonary blood vessels by
inhibiting the enzyme phosphodiesterase,
resulting in an increase in cAMP, which
promotes bronchodilation.
- Toxicity to occur when the serum level is
greater than 20 mcg/ml.
- Side effects and adverse effects: anorexia,
nausea and vomiting, gastric pain caused by
increased gastric acid secretion, intestinal
bleeding, nervousness, dizziness, headache,
irritability, cardiac dysrythmias, tachycardia,
palpitations, marked hypotension,
hyperreflexia and seizures
- Rapid IV administration of aminophylline, can
cause dizziness, flushing, hypotension,
severe bradycardia, and palpitations.
- To avoid severe adverse effects, IV
Theophylline preparations must be
administered slowly via infusion pump.
Drug Interactions
- Beta-blockers, cimetidine, propanolol and
erythromycin decrease the liver metabolism
rate and increase the half-life and effects of
theophylline.
- Barbiturates and carbamazepine decrease
its effects.
- Increases the risk of digitalis toxicity and
decrease the effects of lithium.
• Bronchodilators if given together with beta-
adrenergic agonist can result to a synergistic
effect that can lead to cardiac dysrhythmias
• To decrease the potential for side effects,
patients should not take other xanthenes while
taking theophylline
Half-life
- refers to how long it takes for half of the dose
to be metabolized and eliminated from the
bloodstream
- time it takes for it to be reduced by half
Synergistic effect
- seen when two or more substances combine
to create an effect that is greater than either
one of them could have manifested by itself
LEUKOTRIENE (LT) INHIBITORS
- chemical mediator that can cause
inflammatory changes in the lungs
- Cysteinyl leukotrienes promote an increase
in eosinophil migration, mucous production
and airway wall edema that results in
bronchoconstriction
- LT modifiers are effective in reducing
inflammatory symptoms of asthma triggered
by allergic and environmental stimuli.
- Should not be used during the acute
asthmatic attack
- They are only for prophylactic and
maintenance drug therapy for chronic
asthma
Zafirlukast
- Reduce the inflammatory process and
- decrease bronchoconstriction.
- Administered orally
- Moderately long half-life
Zileuton
- Short half-life of 1 to 2.3 hours
Montelukast
- Short half-life of 2.7 to 5.5 hours
- Safe for children 2 years and old
GLUCOCORTECOIDS (STEROIDS)
- Has anti-inflammatory action and are
indicated if asthma is unresponsive to
bronchodilator therapy or if the patient has
an asthmatic attack while on maximum
doses of theophylline or an adrenergic drug.
- Can be given using the following methods:
• MDI inhaler – Beclomethasone
• Tablet – Dexamethasone,
prednisone, prednisolone,
• methylprednisolone
• Intravenous – Dexamethasone
- Inhaled glucocorticoids are more effective for
controlling symptoms of asthma than are
bete2 agonist, particularly in reduction of
bronchial hyperresponsiveness.
- Inhaled glucocortecoids are preferred over
oral preparations unless they fail to control
the asthma.
- Oral glucocorticoids may be prescribed to
young child to control a moderate sever
asthmatic state
Recommended Glucocortecoids by National
Asthma Education and Prevention Program
- For management of moderate to severe
asthma exacerbations.
• Prednisone
• Prednisolone
• Dexamethasone
• Methylprednisolone
• A combination inhalation drug containing the
glucocorticoid fluticasone propionate and
salmeterol is effective in controlling asthma
symptoms by alleviating airway constriction
and inflammation.
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• Side effects: Throat irritation, hoarseness,
dry mouth, coughing, headache, euphoria,
confusion, sweating, hyperglycemia,
insomnia, nausea, vomiting, weakness and
menstrual irregularities.
• Adverse effects: Depression, peptic ulcer,
loss of bone density, and development of
osteoporosis and psychosis.
Important Information
• Glucocorticoids can irritate the gastric
mucosa and should be taken with food to
avoid ulceration.
• When oral and IV steroids are used in
prolonged periods, electrolyte imbalance,
fluid retention (puffy eyelids, edema in the
lower extremities, moon face, weight gain),
hypertension, thinning of the skin, purpura,
abnormal subcutaneous fat distribution,
hyperglycemia, and impaired immune
response, are likely to occur.
CROMOLYN AND NEDOCROMIL
- used to treat the inflammatory effects of
asthma in children
Cromolyn Sodium
- Is used for prophylactic treatment of
bronchial asthma, and it must be taken daily.
- It is not used for acute asthmatic attack.
- Cromolyn does not have bronchodilator
properties but instead act by inhibiting
release of histamine and other inflammatory
mediators from mast cells to prevent asthma
attack.
- Administered by inhalation and can be used
with beta-adrenergic and xanthine
derivatives
- The drug should not be discontinued abruptly
because a rebound asthmatic attack can
result.
- Side effects: postnasal drip, irritation of the
nose and throat, cough (can be decreased
by drinking water before and after using the
drug)
- Adverse effects: rebound bronchospasm
Nedocromil Sodium
- has an antiinflammatory effect and
- suppresses the release of histamine,
leukotrienes, and other
- mediators from the mast cell
- used to prevent bronchospasm and acute
asthmatic attack
- believed to be more effective than cromolyn
MUCOLYTICS
- Act as detergents to liquefy and loosen thick,
mucous secretions so that they can be
expectorated
Acetylcysteine
- Adjunct to bronchodilator, but these are not
mixed together. (bronchodilator should be
given 5 to 15 minutes before the mucolytic)
- Side effects: nausea and vomiting, stomatitis
(oral ulcers), runny nose.
- Note: Acetylcysteine should be diluted in
- water to minimize the risk of vomiting.
ANTIMICROBIALS
- Are used only if a bacterial infection results
from retained mucous secretions.
Trimethoprim-sulfamethoxazole
- effective for the treatment of mild to
moderate acute exacerbation of chronic
bronchitis (AECB’s) from infection cases.
DRUGS FOR GASTROINTESTINAL TRACT
DISORDERS
Gastrointestinal tract disorders:
• Vomiting
• Diarrhea
• Constipation
VOMITING
- the expulsion of gastric contents
- has a multitude of causes, including motion
sickness, viral and bacterial infection, food
intolerance, surgery, pregnancy, pain, shock,
effects of selected drugs (e.g.,
antineoplastics, antibiotics) radiation,
disturbance of the middle ear that affect
equilibrium
- The two cerebral centers - the
chemoreceptor trigger zone (CTZ), which lies
near the medulla, and the vomiting center in
the medulla – cause vomiting when
stimulated.
- Antiemetics can mask the underlying cause
of vomiting and should not be used until the
cause has been determined, unless the
vomiting is so severe as to cause
dehydration and electrolyte imbalance
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• The CTZ receives most of the impulses from the
drugs, toxins, and the vestibular center in the ear
and transmits them to the vomiting center
• The neurotransmitter dopamine stimulates the
CTZ, which in turn stimulates the vomiting center
• When the vomiting center is stimulated, the motor
neuron responds by causing contraction of the
diaphragm, the anterior abdominal muscles, and
the stomach. The glottis closes, the abdominal
wall moves upward, and vomiting occurs.
Nausea
- a queasy sensation, may or may not precede
the expulsion
NONPHARMACOLOGIC MEASURES
- Non-pharmacologic measures should be
used first when nausea and vomiting occur.
- Includes: administration of weak tea, flat
soda, gelatin, Gatorade, Pedialyte (for use in
children), crackers and dry toast
• If non-pharmacologic measures are not effective,
antiemetics are combined with nonpharmacologic
measures.
• IV fluids are needed to restore body fluid balance
when dehydration becomes severe.
Drugs groups used to correct or control vomiting,
diarrhea, and constipation are classified as:
• Antiemetics
• Emetics
• Antidiarrheals
• Laxatives.
TWO MAJOR GROUPS OF ANTIEMETICS
1. Nonprescription (antihistamines, bismuth
subsalicylate, phosphorated carbohydrate
solution)
2. Prescription (antihistamines, dopamine
antagonist, benzodiazepines, serotonin
antagonist, glucocorticoids, cannabinoids
and miscellaneous antiemetics)
NONPRESCRIPTION ANTIEMETICS
- antivomiting agents
- can be purchased as over-the-counter drugs
- frequently used to prevent nausea, vomiting,
and dizziness (vertigo), motion sickness
- have minimal effect on controlling severe
vomiting resulting from an anticancer agents
(antineoplastics), radiation, and toxins
- not effective in relieving motion sickness if
taken after vomiting has occurred
- inhibit vestibular stimulation in the middle ear
Diphenhydramine hydrochloride (Benadryl)
- used to prevent or alleviate allergic reactions
to drugs, insects, and food by acting as an
antagonist to histamine1 (H1) receptors.
- Side effects: Drowsiness, dryness of mouth
and constipation
Dimenhydrinate (Dramamine)
- primarily used to prevent motion sickness
- Side effects: drowsiness, dizziness, dry
mouth, and hypotension
Cyclizine hydrochloride (Marezine)
- used for prevention and treatment of nausea,
vomiting, and motion sickness
Meclizine hydrochloride (Antivert)
- prevention of nausea, vomiting, and
dizziness
- Side effects: drowsiness and dry mouth
Bismuth subsalicylate (Pepto-Bismol)
- act directly on the gastric mucosa to
suppress vomiting
- marketed in liquid and chewable tablet forms
and can be taken for gastric discomfort or
diarrhea.
Phosphorated carbohydrate solution (Emetrol)
- A hyperosmolar carbohydrate
- Decreases nausea and vomiting by changing
the gastric pH and may also decrease
smooth muscle contraction of the stomach
- Its effectiveness as an antiemetic has not
been verified.
- Patients with diabetes mellitus should avoid
this drug because of its high sugar content.
PRESCRIPTION ANTIEMETICS
1. antihistamines
2. anticholinergics
3. dopamine antagonists
4. benzodiazepines
5. serotonin antagonists
6. glucocorticoids
7. cannabinoids (for patients with cancer)
8. miscellaneous
Antihistamines and Anticholinergics
- act primarily on the vomiting center; they also
act by decreasing stimulation of the CTZ and
vestibular pathways.
Hydroxyzine (Vistaril)
- Antihistamine
- For post-operative nausea, vomiting, vertigo
- Given preoperatively with narcotics to
decrease nausea
- Give hydroxyzine deep IM
Scopolamine (Transderm-Scop)
- Anticholinergic
- For motion sickness
- Side effects: dizziness, drowsiness, dry
mouth, constipation
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Dopamine Antagonist
- Suppresses emesis by blocking dopamine
(D2) receptors in the CTZ
- Common side effects: extrapyramidal
symptoms (EPS) caused by blocking
dopamine receptors and hypotension
- Categories:
o Phenothiazines
o Butyrophenones
o Benzodiazepines
Phenothiazines Antiemetics
- Used to treat nausea and vomiting resulting
from surgery, anesthetics, chemotherapy,
and radiation sickness.
- They act by inhibiting the CTZ
- Have antihistamines and anticholinergic
properties
- Mainly used as antipsychotic
- Side effects: moderate sedation;
hypotension; extrapyramidal symptoms, CNS
effects (restlessness, weakness, dystonic
reactions, agitation)
- Because the dose is lower for vomiting than
for psychosis, the side effects are not so
severe.
Chlorpromaine (Thorazine) and Prochlorperazine
edisylate (Compazine)
- the first phenothiazines used for both
psychosis and vomiting
Promethazine (Phenergan)
- high-alert medication
- has a sedative effect and can also be used
for motion sickness and management of
nausea and vomiting
- most frequently prescribed antiemetic drug.
- readily absorbed in the gastrointestinal (GI)
tract
- has 93% protein-binding capacity
- metabolized by the liver and excreted in
urine and feces.
Butyrophenones
Haloperidol (Haldol) and Droperidol (Inapsine)
- Block the D2 receptors in the CTZ.
- They are used to treat postoperative nausea
and vomiting and emesis associated with
toxins, cancer chemotherapy and radiation
therapy
- Mainly used as antipsychotic
Benzodiazepines
- indirectly control nausea and vomiting that
may occur with cancer chemotherapy
Lorazepam (Ativan)
- drug of choice
- effectively provides emesis control, sedation,
anxiety reduction, and amnesia when used in
combination with a glucocorticoid and
serotonin 5-HT3 receptor antagonist.
Serotonin Receptor Antagonists
- suppress nausea and vomiting by blocking
the serotonin receptors (5-HT3) in the CTZ
and the afferent vagal nerve terminals in the
upper GI tract.
- most effective of all antiemetics in
suppressing nausea and vomiting caused by
cancer chemotherapy-induced emesis or
emetogenic anticancer drugs:
• ondansetron (Zofran)
• granisetron (Kytril)
• dolasetron (Anzemet)
• palonosetron (Aloxi)
Glucocorticoids (Corticosteroids)
Dexamethasone (Decadron) and methylprednisolone
(SoluMedrol)
- effective in suppressing emesis associated
with cancer chemotherapy
Cannabinoids
- Alleviate nausea and vomiting resulting from
cancer treatment
- May be prescribed for patients receiving
chemotherapy who do not respond to or are
unable to take other antiemetics
- Contraindicated for patients with psychiatric
disorders.
- Can be used as an appetite stimulant for
patients with acquired immunodeficiency
syndrome (AIDS)
Dronabinol (Marinol)
- For nausea and vomiting caused by cancer
chemotherapy.
- Taken before and for 24 hours after
chemotherapy. Can be an appetite stimulant
for patients with AIDS.
Miscellaneous Antiemetics
Diphenidol (Vontrol) and trimethobenzamide (Tigan)
- do not act strictly as antihistamines,
anticholinergics, or phenothiazines
- suppress impulses to the CTZ
- Diphenidol also prevents vertigo by inhibiting
impulses to the vestibular area.
Metoclopramide
Metoclopramide (Reglan)
- suppresses emesis by blocking the
dopamine receptors in the CTZ
- used in the treatment of postoperative
emesis, cancer chemotherapy, and radiation
therapy
- High doses can cause sedation and diarrhea
- should not be given if the patient has GI
obstruction, hemorrhage, or perforation.
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• The cannabinoids act on the cerebral cortex.
Phenothiazines, miscellaneous antiemetics (e.g.,
metoclopramide), and trimethobenzamide act on
the CTZ center.
• Drug combination therapy is commonly used to
manage chemotherapy-induced nausea and
vomiting.
• Lorazepam (Ativan), glucocorticoids, and
serotonin (5-HT3) receptor antagonists are quite
effective in combination therapy.
• Lorazepam, haloperidol, and glucocorticoids are
not approved by the U.S. Food and Drug
Administration (FDA) as antiemetics but are
extremely effective when combined for this
unlabeled use.
EMETICS
- Used to induce vomiting
- When an individual has consumed certain
toxic substances, induced vomiting (emesis)
may be indicated to expel the substance
before absorption occurs. Vomiting can be
induced in a number of ways without using
drugs, such as putting finger in the back of
the throat.
- Vomiting should not be induced if caustic
substances, such as ammonia, chlorine
bleach, lye, toilet cleaners, or battery acid,
have been ingested. Regurgitating these
substances can cause additional injury to the
esophagus.
- To prevent aspiration, vomiting should also
be avoided if petroleum distillates are
ingested; these include gasoline, kerosene,
paint thinners, and lighter fluid.
- Activated charcoal is given when emesis is
contraindicated.
Ipecac syrup
- induces vomiting after poisoning
- administer within 60 minutes of poisoning to
an alert and conscious individual
- should be taken with a glass of water
Charcoal (CharcoAid)
- an adsorbent, to be used when vomiting is
not induced
- promotes absorption of poison/toxic
substances
DIARRHEA
- frequent liquid stool
- a symptom of an intestinal disorder
- Causes
1. spicy or spoiled food
2. fecal impaction
3. bacteria or viruses
4. toxins
5. drug reactions
6. laxative abuse
7. malabsorption syndrome caused by
lack of digestive enzymes
8. stress and anxiety
9. bowel tumor
10. inflammatory bowel disease such a
ulcerative colitis or Crohn disease.
- Antidiarrheals should not be used for more
than 2 days and should not be used if fever
is present.
NONPHAMACOLOGIC MEASURES
- Nonpharmacologic treatment for diarrhea is
- recommended until the underlying cause can
be determined
- Includes: use of clear liquids and oral
solutions such as Gatorade (for adults) and
Pedialyte or Rehydralyte (for children) and IV
electrolyte solutions.
- Anti-diarrheal drugs are frequently used in
combination with nonpharmacologic
treatment
TRAVELERS’ DIARRHEA
- also called acute diarrhea
- usually caused by E.coli
- ordinarily lasts less than 2 days; however, if
it becomes severe, fluoroquinolone
antibiotics are usually prescribed.
- Loperamide may be used to slow peristalsis
and decrease the frequency of defecation,
but it can also slow the exit of organism from
the GI tract.
- Travelers’ diarrhea can be reduced by
drinking bottled water, washing fruit, and
eating cooked vegetables
ANTIDIARRHEALS
1. Opiates and opiate-related agents
2. Somatostatin analogue
3. Adsorbents
4. Miscellaneous antidiarrheals
Opiates and Opiate-Relate Agents
- Opiates decrease intestinal motility thereby
decreasing peristalsis.
- Frequently combined with other antidiarrheal
agents
- Opium antidiarrheals can cause CNS
depression when taken with alcohol,
sedatives and tranquilizers
Diphenoxylate with atropine (Lomotil)
- frequently prescribed with travellers’ diarrhea
- an opiate that has less potential for causing
drug dependence than other opiates such as
codeine
Difenoxin with atropine (Motofen)
- For acute nonspecific and chronic diarrhea
- an active metabolite of diphenoxylate and
more potent
- Combination of a synthetic narcotic and
atropine
NCM 106: PHARMACOLOGY
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- Avoid use in patients with narrow-angle
glaucoma.
Loperamide (Imodium)
- structurally related to diphenoxylate but
causes less CNS depression than
diphenoxylate and difenoxin
- can be purchased as an OTC drug
- protects against diarrhea, reduces fecal
volume, and decreases intestinal fluid and
electrolyte losses
Deodorized Opium Tincture
- For acute, nonspecific diarrhea
- To treat withdrawal symptoms in neonates of
mothers who are addicted to opiates
- Not recommended for diarrhea caused by
poison.
• Patients with severe hepatic impairment should
not take products that contain dyphenoxilate,
difenoxin, and loperamide.
Adsorbents
- Act by coating the wall of the GI tract and
adsorbing bacteria or toxins that cause
diarrhea.
Kaolin and Pectin
- combined as a mild or moderate
antidiarrheal that can be purchased OTC and
used in combination with other antidiarrheals
Bismuth subsalicylate (Pepto-Bismol)
- considered an adsorbent because it adsorbs
bacterial toxins
- can also be used as an antacid for gastric
discomfort. an OTC drug commonly used to
treat traveler’s diarrhea
Colestipol and cholestyramine
- prescription drugs that have been used to
treat diarrhea due to excess bile acids in the
colon
Miscellaneous Antidiarrheals
- prescribed to control diarrhea
Rifaximin (Xifaxan)
- For treatment of travelers’ diarrhea caused
by noninvasive strains of E. coli.
CONSTIPATION
- the accumulation of hard fecal material in the
large intestine
- a relatively common complaint and a major
problem for older adults
- insufficient water intake and poor dietary
habits are contributing factors
Causes include:
• fecal impaction
• bowel obstruction
• chronic laxative use
• neurologic disorders (paraplegia)
• ignoring the urge to defecate
• lack of exercise
• select drugs such as anticholinergics,
narcotics, and certain antacids.
NONPHARMACOLOGIC MEASURES
Nonpharmacologic management includes: diet (high
fiber), water, exercise, and routine bowel habits.
A ‘’normal’’ number of bowel movements ranges
between one and three per day to three per week.
LAXATIVES AND CATHARTICS
- Are used to eliminate fecal matter
- Laxatives promote a soft stool.
- Cathartics result in a soft to watery stool with
some cramping.
- Purgatives are harsh cathartics that cause a
watery stool with abdominal cramping
- 4 types of laxatives:
1. Osmotics (saline)
2. Stimulants (contact or irritation)
3. Bulk-forming
4. Emollients (stool softeners)
• Laxatives should be avoided if there is any
question that the patient may have intestinal
obstruction; if abdominal pain is severe; or if
symptoms of appendicitis, ulcerative colitis, or
diverticulitis are present.
• Most laxatives stimulate peristalsis.
• Laxative abuse from chronic use is a common
problem, especially in older adults.
• Laxative dependence can become a problem, so
patient teaching is an important nursing
responsibility.
Osmotic (Saline/Hyperosmolar) Laxatives
- Include salt, lactulose, glycerin or saline
products that consist of sodium or
magnesium.
- Hyperosmolar salts pull water into the colon
and increase water in the feces to increase
bulk, which stimulates peristalsis.
- Good renal function is needed to excrete any
excess salts.
- Saline cathartics cause a semiformed to
watery stool according to low or high doses.
- Saline cathartics are contraindicated for
patients with heart failure.
Sodium salts
- sodium phosphate or Phospho-Soda, sodium
biphosphate
Magnesium salts
- magnesium hydroxide or Milk of magnesia,
magnesium citrate
- Patients who have renal insufficiency should
avoid magnesium salts.
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- Hypermagnesemia can result from
continuous use of magnesium salts, causing
symptoms such as drowsiness, weakness,
paralysis, complete heart block, hypotension,
flush, and respiratory depression.
Polyethylene glycol (PEG)
- marketed as GoLYTELY
- used for bowel preparation for diagnostics
and surgical procedure
- a large volume of solution (approx. 3-4 liters
over 3 hours) must be ingested
- Patients may be advised to keep GoLYTELY
refrigerated to make it more palatable.
Lactulose
- not absorbed, draws water into the intestines
to form a soft stool
- decreases the serum ammonia level and is
useful in liver diseases, such as cirrhosis
- Side effects: flatulence, diarrhea, abdominal
cramps, nausea, vomitting
- Patients who have diabetes mellitus should
avoid lactulose, because it contains glucose
and fructose.
Glycerin
- increases water in the feces in the large
intestine
- stimulates peristalsis and defecation
- Use with caution in patients with cardiac,
renal, or liver disease and for older adults or
dehydrated patients
Stimulant (Contact) Laxatives
- Increase peristalsis by irritating sensory
nerve endings in the intestinal mucosa.
Bisacodyl (Dulcolax)
- used to empty the bowel before diagnostic
test
- most frequently used and abused laxative
and can be purchased OTC
- irritates the colon, causing defecation, and
psyllium compounds increase fecal bulk and
peristalsis
Senna (Senokot)
- Prolonged use of senna can damage nerves,
which may result in loss of intestinal
muscular tone
Castor oil
- harsh laxative (purgative) that acts on the
small bowel and produces a watery stool
- Not FDA approved to correct constipation but
rather it is used mainly for bowel
preparations.
- should not be used in early pregnancy,
because it stimulates uterine contraction
- Side effects: nausea, abdominal cramps,
weakness, and reddish brown urine caused
by excretion of phenolphthalein, senna, or
cascara
Bulk-forming laxatives
- Are natural fibrous substances that promote
large, soft stools by absorbing water into the
intestines, increasing the fecal bulk and
peristalsis.
- Non-absorbable
- Defacation usually occurs 8 to 24 hours
- Powdered bulk-forming laxatives should be
mixed in a glass of water or juice, stirred,
drunk immediately, and followed by a half to
a full glass of water
- Insufficient fluid intake can cause the drug to
solidify in the GI tract, which can result in
intestinal obstruction.
- This group of laxatives does not cause
laxative dependence and may be used by
patients with diverticulosis, irritable bowel
syndrome, and ileostomy and colostomy.
- Examples:
• Polycarbophil
• Polyethylene glycol
• Methylcellulose
• Psyllium
Side effects: nausea, vomiting, flatus or diarrhea may
occur if taken excessively.
Chloride Channel Activators
- New category of laxatives used to treat
idiopathic constipation in adults.
Lubiprostone
- activates calcium channel in the small
intestines, leading to an increase in intestinal
fluid secretion and motility
- relieves constipation, as well as
accompanying symptoms of abdominal
discomfort, pain, and bloating
- Contraindicated for patients with a history of
mechanical GI obstruction, Crohn’s disease,
diverticulitis, and severe diarrhea
- Adverse effect: nausea that seems to be
dose dependent; diarrhea; headache;
abdominal distention and flatulence.
Emollients
- Are lubricants and stool softener (surface-
acting or wetting drugs)
- Used to prevent constipation
- Decrease straining during defecation
Mineral oil
- increases water retention in the stool
- Absorbs fat-soluble vitamins, ADEK
Stool softeners
- work by lowering surface tension and
promoting water accumulation in the
intestine and stool
NCM 106: PHARMACOLOGY
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- frequently prescribed for patients after
myocardial infarction or surgery
- Examples
• docusate calcium (Surfak)
• dosusate sodium (Colace)
• docusate sodium with senna (Peri-
Colace)
ANTIULCER DRUGS
Peptic Ulcer
- Broad term for an ulcer that occurs in the
esophagus, stomach, or duodenum within
the upper GI tract
- The classic symptom of peptic ulcers is
gnawing, aching abdominal pain.
Esophageal ulcer
- results from reflux of acidic gastric secretions
into the esophagus as a result of a defective
or incompetent cardiac sphincter
Gastric ulcer
- frequently occurs because of a breakdown of
the gastric mucosal barrier
Duodenal ulcer
- caused by hypersecretion of acid from the
stomach passing into the duodenum
because of (1) insufficient buffers to
neutralize gastric acid in the stomach, (2) a
defective or incompetent pyloric sphincter, or
(3) hypermotility of the stomach
Gastroesophageal reflux disease (GERD)
- inflammation or erosion of the esophageal
mucosa caused by a reflux of gastric acid
content from the stomach into the
esophagus.
- Drugs used in treatment include H2 blockers
such as ranitidine (Zantac), and PPIs such
as omeprazole (Prilosec), lansoprazole
(Prevacid), rabeprazole (Aciphex),
pantoprazole (Protonix), or esomeprazole
(Nexium)
ANTIULCER DRUGS
1. Tranquilizers – decrease vagal activity
2. Anticholinergics – decrease acetylcholine by
blocking the cholinergic receptors
3. Antacids – neutralize gastric acid
4. H2 blockers – block the H2 receptors
5. PPI’s – inhibit gastric acid secretion
6. Pepsin – inhibitor sucralfate
7. Prostaglandin E1 analogue misoprostol -
inhibits gastric acid secretion and protects
mucosa.
TRANQUILIZERS
- Have minimal effect in preventing and
treating ulcers; however, they reduce vagal
stimulation and decrease anxiety.
- A combination of anxiolytic and
anticholinergic may be used in treating
ulcers:
• Chlordiazepoxide (anxiolytic)
• Clidinium bromide (anticholinergic)
- Side effects: Edema, ataxia, confusion, EPS,
and agranulocytosis
ANTICHOLINERGICS (ANTIMUSCARINICS,
PARASYMPATHOLYTICS)
- These drugs relieve pain by decreasing GI
motility and secretion.
- They act by inhibiting acetylcholine and
blocking histamine and hydrochloric acid.
- Delay gastric emptying time, so they are
used more frequently in duodenal ulcers than
for gastric ulcers.
- Anticholinergics should be taken before
meals to decrease the acid secretion that
occurs with eating.
- Antacids can slow the absorption of
anticholinergics and therefore should be
taken 2 hours after anticholinergic
administration.
Propantheline bromide
- inhibits gastric acid secretions in the
treatment of peptic ulcers.
Glycopyrrolate
- for duodenal ulcer
- should be taken before meals to decrease
acid secretion that occurs with eating.
ANTACIDS
- Promotes ulcer healing by neutralizing
hydrochloric acid and reducing pepsin
activity; they do not coat the ulcer.
- 2 types of antacids:
1. Systemic effect
2. Non-systemic effect
Systemic Antacids
Sodium bicarbonate
- seldom used to treat peptic ulcers because it
has many side effects:
• Sodium excess (causing
hypernatremia and water retention)
• Metabolic alkalosis caused by
excess bicarbonate
• Acid rebound (excess acid
secretion)
Calcium carbonate
- most effective in neutralizing acid
- can cause rebound acid
- excessive use of calcium carbonate results
to hypercalcemia and Burnett’s syndrome
Non-systemic Antacids
Aluminium hydroxide
NCM 106: PHARMACOLOGY
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- To alleviate heartburn, acid indigestion,
esophagitis, and hiatal hernia caused by
hyperacidity
- used to neutralize hydrochloric acid
- frequently used to lower high serum
phosphate (hyperphosphatemia)
- can cause constipation
Magnesium hydroxide and magnesium trisilicate
- To alleviate heartburn, gastritis, esophagitis,
and peptic ulcers caused by hyperacidity.
- can cause diarrhea
- contraindicated in patients with impaired
renal function because of the risk for
hypermagnesemia
Side effects:
• Magnesium compounds – diarrhea
• Aluminum and calcium – constipation
HISTAMINE2 BLOCKERS
- Are popular drugs used in the treatment of
gastric and duodenal ulcers.
- These drugs block the H2 receptors of the
parietal cells in the stomach thus reducing
gastric acid secretion and concentration
Cimetidine
- For peptic ulcers (gastric and duodenal)
- Has a short half-life and a short duration of
action; blocks about 70% of acid secretion
for 4 hours
- 50% to 80% of Cimetidine is excreted
unchanged in the urine. It can also cause an
increase in BUN, serum creatinine, and
serum alkaline phosphatise.
• Three H2 blockers, ranitidine (Zantac), famotidine
(Pepcid), and nizatidine (Axid), are more potent
than cimetidine.
• In addition to blocking gastric acid secretions,
they promote healing of the ulcer by eliminating
its cause.
• Their duration of action is longer, decreasing the
frequency of dosing, and they have fewer side
effects and fewer drug interactions than
cimetidine.
Ranitidine
- Has longer duration of action (up to 12
hours) than cimetidine.
- Inhibits histamine at the H2 receptor site
- Large doses of ranitidine are effective for
controlling Zollinger-Ellison syndrome
- Effective in treating gastric and duodenal
ulcers and can be used prophylactically
- also useful in relieving symptoms of reflux
esophagitis, preventing stress ulcers that can
occur following major surgery, and
preventing aspiration pneumonitis that can
result from aspiration of gastric acid
secretions.
Famotidine
- Is 50% to 80% more potent than cimetidine
and is to five to eight times more potent than
ranitidine
- It is indicated for short-term use (4 to 8
weeks) for duodenal ulcer and for Zollinger-
Ellison syndrome.
Nizatidine
- is an H2 blocker that can relieve nocturnal
gastric acid secretion for 12 hours.
- To prevent recurrence of duodenal ulcers,
administer nizatidine 150 mg twice a day at
bedtime or famotidine 20 mg twice a day at
bedtime.
PROTON-PUMP INHIBITORS (PPI)
- Gastric acid secretion inhibitors, gastric acid
PUPM inhibitors
- PPIs suppress gastric acid secretion by
inhibiting the hydrogen/potassium
- ATPase enzyme system located in the
gastric parietal cells.
- They tend to inhibit gastric acid secretion up
to 90% more than H2 blockers (histamine
antagonists).
- These agents block the final step of acid
production.
- Effective in suppressing gastric acid
secretions and are used to treat peptic ulcers
and GERD (gastroesophageal reflux
disease)
- Recognized long-term side effects of PPIs:
osteoporosis, fractures, pneumonia,
clostridium difficile infection, kidney disease,
low Iron and vitamin B12 levels causing
anemia
- Should usually be taken before meals
- Drug Interactions: can enhance the action of
digoxin, oral anticoagulants, certain
benzodiazepines, and phenytoin, because
they interfere with liver metabolism of these
drugs
Omeprazole
- first PPI marketed
- promotes irreversible hydrogen or potassium
ATPase inhibition until new enzyme is
synthesized.
Omeprazole with sodium bicarbonate (Zegerid)
- combination medication
- only drug given to prevent stress ulcers in
critically ill patients
- also used to treat GERD, erosive
esophagitis, and gastric or duodenal ulcers
Esomemprazole with Naproxen (Vimovo)
- combination medication
NCM 106: PHARMACOLOGY
LECTURE
- immediate-release PPI layered over an Outline:
entericcoated NSAID in one tablet used to A. Endocrine System
prevent NSAID-associated gastric ulcers • Hypothalamic and pituitary agents
• Adrenocortical agents
Lansoprazole • Thyroid and parathyroid agents
- ulcer relief usually occurs in 1 week. • Antidiabetic agents

Rabeprazole
- is more effective in treating duodenal ulcer THE ENDOCRINE SYSTEM
than gastric ulcers, but it is most effective in
treating GERD and hypersecretory disease
(Zollinger-Ellison Syndrome).

Pantoprazole
- is prescribed to treat short-term erosive
GERD.

Esomeprazole
- has the highest success rate in treating
erosive GERD, more than omeprazole.

Dexlansoprazole
- is prescribed to treat erosive esophagitis and
symptomatic non-erosive GERD.

PEPSIN INHIBITORS (MUCOSAL PROTECTIVE

DRUGS)
Sucralfate
- a complex of sulfated sucrose and aluminum
hydroxide, is classified as a pepsin inhibitor,
or mucosal protective drug.
- It is nonabsorbable and combines with
protein to form a viscous substance that
covers the ulcer and protects it from acid and
pepsin.
- promotes healing by adhering to the ulcer
surface
- This drug does not neutralize acid or
decrease acid secretions.
- Side effects: constipation
PROSTAGLANDIN ANALOGUE ANTIULCER DRUG
Misoprostol
- Used to prevent and treat peptic ulcer
- It appears to suppress gastric acid secretion,
increase cytoprotective mucus in the GI tract,
and causes a moderate decrease in pepsin
secretion.
- Patients who complain of gastric distress
from NSAIDs such as aspirin or
indomethacin prescribed for long-term
therapy can benefit from misoprostol
- Contraindicated during pregnancy and for
women of childbearing age
MODULE 6: ENDOCRINE DRUGS
PITUITARY GLAND AGENTS
ANTERIOR LOBE
- called the adenohypophysis
- secretes hormone that target glands and tissues,
including:
1. Growth Hormone (GH)
- stimulates growth in tissue and bone.
2. Thyroid-stimulating hormone (TSH)
- acts on the thyroid gland.
3. Adrenocorticotropic hormone (ACTH) -
stimulates the adrenal gland.
4. Gonadotropins (Follicle-stimulating hormone
(FSH) and Luteinizing hormone (LH))
- affects the ovaries and testes.
5. Prolactin (PRL)
- primarily affects the breast tissues.
Growth Hormone
• 2 hypothalamic hormones regulate GH:
1. GH-releasing hormone (GH-RH; somatropin)
2. GH-inhibiting hormone (GH-IH; somatostatin)
• GH does not have a specific target gland.
• It affects body tissues and bone
• GH replacement stimulates linear growth when
there are GH deficiencies.
• GH drugs cannot be given orally because they
are inactivated by GI enzymes.
• Subcutaneous (subcut) or intramuscular (IM)
administration is necessary.

Drug Therapy: Growth Hormone Deficiency

Somatropin (Genotropin)
- a growth hormone used to treat growth
failure in children because of GH deficiency

NCM 106: PHARMACOLOGY
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- a product that has the identical amino acid
sequence as human growth hormone (HGH)
- contraindicated in pediatric patients who
have growth deficiency due to Prader-Willi
syndrome and in those who are severely
obese or who have severe respiratory
impairment because fatalities associated
with these factors can occur
Drug Interactions:
• Corticosteroids can inhibit the effects of
somatropin.
• Can enhance the effects of antidiabetics nd
can cause hypoglycaemia.
• Side effects: Paresthesia (burning or prickling
sensation), arthralgia (joint pain), myalgia
(muscle pain), peripheral edema, weakness, and
cephalgia (cluster headache)
• Adverse reaction: Seizures; intracranial
hypertension, and secondary malignancy (e.g.
leukemia)
Drug Therapy: Growth Hormone Excess
- Disorders that can occur with GH
hypersecretion and are frequently caused by
a pituitary tumor.
- If the tumor cannot be destroyed by
radiation, the prolactin-release inhibitor
bromocriptine can inhibit the release of GH
from the pituitary gland.
Gigantism
- excessive growth during childhood
Acromegaly
- excessive growth after puberty
Octreotide (Sandostatin)
- For acromegaly
- potent synthetic somatostatin used to
suppress GH release
- can be used alone or with surgery or
radiation and can also be used for severe
diarrhea resulting from carcinoid tumors
Pegvisomant
- GH receptor antagonist
- Blocks GH receptor sites, preventing
abnormal growth by normalizing Insulin-like
- growth factor 1 (IGH-1) level.
- Given injection
- Side effects: hyperhidrosis (abnormally
excessive sweating); cephalgia and fatigue.
- Adverse reaction: chest pain, hypertension,
and elevated hepatic transaminases.
Lanreotide
- Somatostatin analogues
- Has a duration of 28 days after a single
injection, therefore injections are given every
4 weeks
- Administered deep subcutaneous.
- Side effects: diarrhea, abdominal pain,
nausea, vomiting, constipation, weight loss,
flatulence
Bromocriptine
- Dopamine agonist
- Inhibits the secretion of GH caused by
pituitary adenomas.
- Available in oral forms and has fewer side
effects.
- Adverse reaction:
• Cardiac toxicity (hypertension,
myocardial infarction, and angina)
- Cerebrovascular toxicity (stroke and
seizure)
- Should be discontinued if hypertension
occurs due to pregnancy (preeclampsia,
eclampsia or PIH)
Thyroid-Stimulation Hormone
- Stimulates the Thyroid gland to release
thyroxine (T3) and triiodothyronine (T4).
- HYPERthyroidism – excess TSH secretion
- HYPOthyroidism – TSH deficit, may be
caused by a thyroid gland disorder or a
decrease in TSH secretion
Thyrotropin (Thyrogen)
- A purified extract of TSH
- For thyroid cancer
- Used as a diagnostic agent to differentiate
between primary and secondary
hypothyroidism
- Symptoms of hyperthyroidism (nervousness,
anxiety and irritability, sensitivity to heat,
palpitations, Urticaria (Hives), rash, pruritus,
and flushing
Adrenocorticotropic hormone (ACTH)
- stimulates the release of glucocorticoids
(cortisol), mineralocorticoids (aldosterone),
and androgen from the adrenal cortex
Cosyntropin
- A synthetic ACTH, is only approved for
diagnostic purposes and is less potent and
less allergenic than corticotrophin.
- Stimulates the production and release of
cortisol, corticosterone, and androgens from
the adrenal cortex.
- For diagnostic testing to differentiate
between pituitary and adrenal cause of
adrenal insufficiency
- Administered via IM or IV
- Caution is advised when administering in
patients receiving diuretics; can increase
electrolyte loss.
- Side effects: bradycardia, hypertension,
sinus tachycardia, and peripheral edema.
Corticotropin
- Used to diagnose adrenal gland disorders
NCM 106: PHARMACOLOGY
LECTURE
- Used to treat adrenal gland insufficiency,
anti-inflammatory drug in the treatment of
allergic response, multiple sclerosis and
infantile spasms
- Available as Repository Corticotropin
Injection (RCI), administered via IM or subcut
- RCI controls the synthesis of ACTH from
cholesterol, which stimulates adrenal glands
in releasing its hormones
Prolactin
- Primary function of prolactin (PRL) is
stimulation of breast tissue for milk
production
- Hypoprolactinemia – deficiency PRL
- Hyperprolactinemia – excess PRL
o Males – excess breast tissue
(gynecomastia), may lactate
(galactorrhea), decrease sperm
production
o Females – can experience lactation
not pregnancy related, amenorrhea.
- Excess PRL can be treated with dopamine
agonist:
o Bromocriptine
o Cabergoline – better tolerated, has
a longer half-life.
POSTERIOR LOBE
- also known as neurohypophysis
- secretes ADH (antidiuretic hormone) and
Oxytocin
Antidiuretic hormone (ADH)
- promotes water reabsorption from the renal
tubules to maintain water balance in the
body fluids.
- ADH preparations, vasopressin and
desmopressin acetate can be administered
intranasal or by injections.
- Contraindicated in patients with moderate to
severe renal disease and in patients with
hyponatremia or a history of such.
- Side effects: hyponatemia, cephalgia (A
distinctive syndrome of headaches, also
known as cluster headache or migrainous
neuralgia). Dyspepsia, diarrhea, nausea and
vomiting.
Diabetes insipidus
- condition where large amounts of water is
excreted by the kidneys due to deficiency of
ADH; can lead to severe fluid volume deficit
and electrolyte imbalances.
Vasopressin
- For diabetes insipidus, relief of intestinal
distention
- Decreases GI bleeding from esophageal
varices
Desmopressin acetate
- For diabetes insipidus, hemophilia A, and
von Willebrand disease
- Can have a long duration of action (5-21 h)
SIADH
- Syndrome of inappropriate antidiuretic
hormone
- When secretion of ADH from the posterior
pituitary gland is excessive
- Most common cause is small cell carcinoma
of the lung
- Medications, other malignancies, and
stressors (pain, infection, anxiety, trauma)
may also be causative factors
- These conditions lead to an excessive
amount of water retention expanding the
intracellular and intravascular volume
- This increased fluid volume causes
enhanced glomerular filtration and
decreased tubular sodium reabsorption
- SIADH can be treated by fluid restrictions, by
hypertonic saline or by drugs such as:
demeclocycline, conivaptan, tolvaptan
Demeclocycline
- For treatment of SIADH
- Is a tetracycline antibiotic.
- Adverse effect: photosensitivity, dental
discoloration, enamel hypoplasia.
- Fluid and electrolytes must be monitored
closely.
Vaptans (conivaptan and tolvaptan)
- Vasopressin receptor antagonists and are
indicated for the treatment of euvolemic
hyponatremia in SIADH.
- Tolvaptan is given orally. It has black-box
warnings for patients with alcoholism,
hepatic disease and malnutrition; should be
avoided in these patients.
- Vaptans are contraindicated in patients with
hypovolemia.
- Fluid restrictions should be avoided during
therapy to prevent too rapid an increase in
serum sodium.
THYROID GLAND
Thyroxine (T4) and Triiodothyronine (T3)
- secreted by the thyroid gland
- regulate protein synthesis and enzyme
activity and to stimulate mitochondrial
oxidation
- feedback mechanisms regulate T4 and T3
secretion from the thyroid gland
Thyrotropin-releasing hormone (TRH)
- released from the hypothalamus
- stimulates the release of TSH from the
pituitary gland
NCM 106: PHARMACOLOGY
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HYPOTHYROIDISM
- decrease in thyroid hormone secretion
- thyroid deficiency
- synthetic T4 and T3 may be prescribed
Drug Therapy: Hypothyroidism
Levothyroxine sodium
- Drug of choice for the treatment of primary
hypothyroidism.
- It increases the levels of T4 and
metabolically is deiodinated to T3.
- Also used to treat simple goiter and chronic
lymphocytic thyroiditis (Hashimoto’s
disease).
Liothyronine sodium
- Is a synthetic T3 with a biologic half-life of
2.5 days with rapid onset of action.
- It is not recommended for maintenance
therapy
- Is indicated for use as replacement or
supplemental treatment for hypothyroidism of
any aetiology.
- Does not need to be deionated which
increases the availability for use by the body
tissues.
- Initial therapy for treating myxedema
Desiccated thyroid
- Is a naturally occurring thyroid hormone from
porcine thyroid glands.
- It contains both levothyroxine sodium and
liothyronine sodium
- Used to treat hypothyroidism due to thyroid
atrophy, thyroid hormone deficiency and
goiter.
Liotrix
- mixture of levothyroxine sodium and
liothyronine sodium in a 4:1 ratio
ANTITHYROID DRUGS
• Reduce the excessive secretion of thyroid
hormones by inhibiting thyroid secretions.
Thiourea derivatives (thiomides)
- decreases thyroid hormone production.
HYPERTHYROIDISM
- an increase in circulating T4 and T3 levels,
which usually results from an overactive
thyroid gland or excessive output of thyroid
hormones from one or more thyroid nodules.
- can be treated by surgical removal of a
portion of the thyroid gland (subtotal
thyroidectomy), radioactive iodine therapy, or
antithyroid drugs, which inhibit either
synthesis or release of thyroid hormone
Graves’ disease (thyrotoxicosis)
- most common type of hyperthyroidism
caused by hyperfunction of the thyroid gland
- characterized by a rapid pulse (tachycardia),
palpitations, excessive perspiration, heat
intolerance, nervousness, irritability,
exophthalmos (bulging eyes), and weight
loss
Propranolol (Inderal)
- control cardiac symptoms like palpitations
and tachycardia that result from
hyperthyroidism
- does not lower T4 and T3
Propylthiouracil (PTU) and methimazole
- Used to control overactive thyroid due to
Graves disease, toxic nodular goiter.
- Methimazole is 10 times potent than PTU
and has a longer half-life and the euthyroid
state is achieved in 2 to 4 months.
Drug interactions:
• Oral anticoagulants (warfarin) – can cause
increase in anticoagulation effect.
• Thyroid drugs decreased the effects of
insulin and oral antidiabetics.
Nursing Responsibilities:
• Teach patient to take drug with meals to
decrease gastrointestinal symptoms.
• Advise patient about effects of iodine and its
presence in iodized salt, shellfish, and OTC
cough medicines.
• Emphasize importance of drug compliance;
abruptly stopping antithyroid drug could bring
on thyroid crisis.
• Teach patient signs and symptoms of
hypothyroidism: lethargy, puffy eyelids and
face, thick tongue, slow speech with
hoarseness, lack of perspiration, and slow
pulse. Hypothyroidism can result from
treatment of hyperthyroidism.
• Advise patient to avoid antithyroid drugs if
pregnant or breastfeeding. Antithyroid drugs
taken during pregnancy can cause
hypothyroidism in fetus or infant.
PARATHYROID GLANDS
• secrete parathyroid hormone (PTH), which
regulates calcium levels in the blood.
• A decrease in serum calcium stimulates the
release of PTH.
• Calcitonin decreases serum calcium levels
by promoting renal excretion of calcium
HYPOPARATHYROIDISM
• Parathyroid hormone agents treat
hypoparathyroidism.
• Hypocalcemia (serum calcium deficit) can be
caused by PTH deficiency, vitamin D
NCM 106: PHARMACOLOGY
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deficiency, renal impairment, or diuretic
therapy, and PTH replacement helps correct
the calcium deficit.
• The action of PTH is to promote calcium
absorption from the GI tract, promote
reabsorption of calcium from the renal
tubules, and activate vitamin D.
Calcitriol
- a vitamin D analogue that promotes calcium
absorption from the GI tract and secretion of
calcium from bone to the bloodstream
- For hypoparathyroidism and rickets
- Enhances calcium and phosphorus
absorption
HYPERPARATHYROIDISM
- can be caused by malignancies of the
parathyroid glands or ectopic PTH hormone
secretion from lung cancer, hyperthyroidism,
or prolonged immobility, during which
calcium is lost from bone
- Synthetic calcitonin treats
hyperparathyroidism
Calcitonin-salmon
- For Paget’s disease (osteitis deformans),
hyperparathyroidism, and hypercalcemia
- Calcitonin decreases serum calcium by
binding at receptor sites on osteoclast
Etridronate
- For Paget’s disease; for hypercalcemia
caused by antineoplastic therapy
ADRENAL GLANDS
- The adrenal cortex produces two types of
hormones, or corticosteroids:
1. glucocorticoids (cortisol)
2. mineralocorticoids (aldosterone)
Cortisol
- secreted by the adrenal glands in response
to the hypothalamus-pituitaryadrenal (HPA)
axis as a result of the feedback mechanism
- the main glucocorticoid, has antiallergic, anti-
inflammatory, and andantistress effects.
- A decrease in serum cortisol levels increases
CRF and ACTH secretions, which stimulate
the adrenal glands to secrete and release
cortisol.
- An increased serum cortisol level exerts the
negative feedback mechanism, which inhibits
the HPA axis, resulting in less cortisol being
released.
Corticosteroids
- promote sodium retention and potassium
excretion
- Because of their influence on electrolytes
and carbohydrate, protein, and fat
metabolism, a deficiency of corticosteroids
can result in serious illness or death.
Addison’s disease
- Adrenal hyposecretion or adrenal
insufficiency
- A decrease in corticosteroid secretion
Cushing’s syndrome
- adrenal hypersecretion
- increase in corticosteroid secretion
GLUCOCORTICOIDS
- influenced by ACTH, which is released from
the anterior pituitary gland.
- They affect carbohydrate, protein, and fat
metabolism and muscle and blood cell
activity.
- Because of their many mineralocorticoid
effects, glucocorticoids can cause sodium
absorption from the kidney, resulting in water
retention, potassium loss, and increased
blood pressure.
- Indications: trauma, surgery, inflammation,
emotional upsets, and anxiety.
- Cortisone drugs have several routes of
administration:
o oral
o parenteral (IM or IV)
o topical (creams, ointments, lotions)
o aerosol (inhaler).
Dexamethasone (Decadrone)
- used to treat severe inflammatory response
resulting from head trauma or allergic
reactions
- Potent antiinflammatory drug
- For acute allergic disorders, asthma attack,
cerebral edema, and unresponsive shock
- For diagnosis of Cushing’s syndrome and
depression. Can be administered IV push or
in IV fluids. Give oral dose with food.
- Long acting
Prednisone
- inexpensive glucocorticoid frequently
prescribed
- For antiinflammatory or immunosuppressive
effect
- Intermediate acting
Cortisone acetate / Hydrocortisone
- For adrenocortical insufficiency.
- Short acting
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Side effects and Adverse Reactions
• Increased blood sugar
• Abnormal fat deposits in the face and trunk
(so-called moon face and buffalo hump)
• Decreased extremity size
• Muscle wasting
• Edema
• Sodium and water retention
• Hypertension
• Euphoria or psychosis
• Thinned skin with purpura
• Increased intraocular pressure (glaucoma)
• Peptic ulcers
• Growth retardation
• Long-term use: Adrenal atrophy (loss of
adrenal gland function)
Nursing Responsibilities:
• Determine vital signs. Glucocorticoids such
as prednisone can increase blood pressure
and sodium and water retention.
• Administer glucocorticoids only as ordered.
Routes of administration include oral, IM (not
in deltoid muscle), IV, aerosol, and topical.
Apply topical glucocorticoids in thin layers.
Rashes, infection, and purpura should be
noted and reported.
• Record weight. Report weight gain of 5 lb in
several days; this would most likely be
caused by water retention.
• Monitor laboratory values, especially serum
electrolytes and blood sugar. Serum
potassium level could decrease to < 3.5
mEq/L, and blood sugar level would probably
increase.
• Watch carefully for signs and symptoms of
hypokalemia: nausea, vomiting, muscular
weakness, abdominal distention, paralytic
ileus, and irregular heart rate.
• Assess for side effects from glucocorticoid
drugs when therapy has lasted more than 10
days and drug is taken in high dosages.
Cortisone preparation should not be abruptly
stopped, because adrenal crisis
• can result.
• Monitor older adults for signs and symptoms
of increased osteoporosis. Glucocorticoids
promote calcium loss from bone.
• Report changes in muscle strength. High
doses of glucocorticoids promote loss of
muscle tone.
Health Teaching
• Advise patient to take drug as prescribed.
Caution patient not to abruptly stop drug.
When drug is discontinued, dose is tapered
over 1 to 2 weeks.
• Prepare schedule for patient to decrease
dose over 4 to 5 days. For short-term use
(<10 days) of glucocorticoids such as
prednisone or other cortisone preparations,
drug dose still needs to be tapered. For
example, day 1: 1 tab four times a day; day
2: 1 tab three times a day; day 3: 1 tab twice
a day; day 4: 1 tab once a day.
• Direct patient not to take cortisone
preparations (oral or topical) during
pregnancy unless necessary and prescribed
by health care provider. Drugs may be
harmful to fetus.
• Inform patient that certain herbal laxatives
and diuretics may interact with glucocorticoid
drug and may increase severity of
hypokalemia.
• Teach patient to avoid persons with
respiratory infections, because these drugs
suppress immune system. This is especially
important if patient is receiving high dose of
glucocorticoids.
• Teach patient receiving glucocorticoids to
inform other health care providers of all
drugs taken, especially before surgery.
• Encourage patient to carry MedicAlert
identification card, tag, or bracelet stating
glucocorticoid taken.
• Counsel patient to take cortisone
preparations at mealtime or with food.
Glucocorticoid drugs can irritate gastric
mucosa and cause peptic ulcer.
• Advise patient to eat foods rich in potassium,
such as fresh and dried fruits, vegetables,
meats, and nuts. Prednisone promotes
potassium loss and hypokalemia.
MINERALOCORTICOIDS
• Second type of corticosteroid
• secrete aldosterone
• Aldosterone is controlled by the
reninangiotensin system, not by ACTH.
• These hormones maintain fluid balance by
promoting the reabsorption of sodium from
the renal tubules.
• Mineralocorticoid deficiency usually occurs
with glucocorticoid deficiency, frequently
called corticosteroid deficiency.
Fludrocortisone (Florinef)
- an oral mineralocorticoid that can be given
with a glucocorticoid
- the serum potassium level should be
monitored because potassium excretion
occurs with the use of mineralocorticoids and
glucocorticoids
ANTIDIABETIC DRUGS
- Used primarily to control diabetes mellitus, a
chronic disease that affects carbohydrate
metabolism.
- Two groups of antidiabetic agents:
1. Insulin
NCM 106: PHARMACOLOGY
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2. Oral hypoglycemic (antidiabetic) drugs
DIABETES MELLITUS
- chronic disease resulting from deficient glucose
metabolism
- caused by insufficient insulin secretion from the
beta cells and results in high blood glucose
(hyperglycemia)
- Characterized by the three p’s:
1. Polyuria (increased urine output)
2. Polydipsia (increased thirst)
3. Polyphagia (increased hunger)
- Type 1 diabetes mellitus: viral infections,
environmental conditions, genetic factors
- Type 2 diabetes mellitus: most common type
Insulin
- protein secreted from the beta cells of the
pancreas
- necessary for carbohydrate metabolism and
plays an important role in protein and fat
metabolism
- promotes the uptake of glucose, amino
acids, and fatty acids and converts them to
substances that are stored in body cells
Commercially Prepared Insulin
Human insulin (Humulin)
- duplicates insulin produced by the pancreas
of the human body
- has a low incidence of allergic effects and
insulin resistance
- Examples: Humulin R and Novolin N
Human insulin analogues
- modifications of human insulin with
alterations in onset and duration of action
- Examples: Insulin lispro (Humalog) and
insulin aspart
- (Novolog)
• To prevent dosage errors, the nurse must be
certain that there is a match of the insulin
concentration with the calibration of units on the
insulin syringe.
• Before use, the patient or nurse must roll, not
shake, cloudy insulin bottles to ensure that the
insulin and its ingredients are well mixed.
• Shaking a bottle of insulin can cause bubbles and
an inaccurate dose
Administration of Insulin
• cannot be administered orally because
gastrointestinal secretions destroy the insulin
structure.
• administered subQ, at a 45- to 90-degree angle.
• Regular insulin is the only type that can be
administered IV
• Insulin absorption is greater when given in the
abdominal areas than when given in the thigh
and buttock areas.
• Heat and massage could increase subQ
absorption. Cooling the subQ area can decrease
absorption.
• Usually given in the morning before breakfast
• Insulin injection sites should be rotated to prevent
lipodystrophy (tissue atrophy or hypertrophy),
which can interfere with insulin absorption.
Lipoatrophy (tissue atrophy) is a depression
under the skin surface that primarily occurs in
women and children. Lipohypertrophy (tissue
hypertrophy) is a raised lump or knot on the skin
surface that is more common in men.
Types of Insulin
1. Rapid acting
2. Short acting
3. Intermediate acting
4. Long acting
5. Combinations
• Rapid- and short-acting insulins are in a clear
solution without any added substance to prolong
insulin action.
• Intermediate-acting insulins are cloudy and may
contain protamine, a protein that prolongs the
action of insulin, or zinc, which also slows the
onset of action and prolongs the duration of
activity
• Rapid acting: Insulin lispro, human insulin aspart
• Short acting: Regular Humulin R
• Intermediate acting: neutral-protamine-
Hagedorn, Lente, Humullin N
• Long acting: Insulin glargine, insulin detmir
• Combination: Humulin 70/30, Novolin 70/30,
Humulin 50/50, and Humalog Mix 75/25
Storage of Insulin
• Unopened insulin vials are refrigerated until
needed, and should not be placed in direct
sunlight or in high-temperature area
• Once an insulin vial has been opened, it may be
kept (1) at room temperature for 1 month or (2) in
the refrigerator for 3 months
NCM 106: PHARMACOLOGY
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Sliding-Scale Insulin Coverage
• Insulin may be administered in adjusted
doses that depend on individual blood
glucose test results.
• When the diabetic patient has extreme
variances in insulin requirements (e.g.,
stress from hospitalization, surgery, illness,
or infection), adjusted dosing or sliding-scale
insulin coverage provides a more constant
blood glucose level.
• Blood glucose testing is performed several
times a day at specified intervals (usually
before meals). A preset scale usually
involves directions for the administration of
rapid- or short-acting insulin.
Drug Interactions
• Drugs such as thiazide diuretics,
glucocorticoids (cortisone preparations),
thyroid agents, and estrogen increase the
blood sugar; therefore the insulin dosage
may need adjustment.
• Drugs that decrease insulin needs are
tricyclic antidepressants, monoamine
oxidase inhibitors (MAOIs), aspirin products,
and oral anticoagulants.
Side Effects and Adverse Reactions: Hypoglycemic
Reactions And Ketoacidosis
• When more insulin is administered than needed
for glucose metabolism, a hypoglycemic reaction,
or insulin shock, occurs.
• The person may exhibit:
o Nervousness
o Trembling
o Lack of coordination
o Cold and clammy skin
o Complain of a headache
o Some patients become combative and
incoherent
Somogyi effect
- may develop in response to an excessive
dose of insulin
- this hypoglycemic condition usually occurs in
the predawn hours of 2:00 am to 4:00 am
- a rapid decrease in blood glucose during the
nighttime hours stimulates a release of
hormones to increase blood glucose by
lipolysis, gluconeogenesis, and
glycogenolysis
- Management: monitoring blood glucose
between 2:00 am and 4:00 am and reducing
the bedtime insulin dosage.
Dawn phenomenon
- Hyperglycemia on awakening
- The patient usually awakens with a
headache and reports night sweats and
nightmares
- Management: increasing the bedtime dose of
insulin
Insulin Pen Injectors
- Resembles a fountain pen
- Contains a disposable needle and a
disposable insulin-filled cartridge
- They come in two types: prefilled and
reusable.
- These are considered to deliver a more
accurate dose than the traditional 100-unit
syringe and vial
Insulin Pumps
- Alternative to daily insulin injections used in
association with blood glucose monitoring
and carbohydrate counting.
- These computerized devices have an insulin
reservoir and programming capacity to
deliver continuous rapid-acting insulin in
varying amounts at different times
throughout a 24-hour period.
- These pumps are smaller than most mobile
phones.
- Types of insulin pumps:
1. Implantable
2. Portable
Implantable insulin pump
- Surgically implanted in the abdomen
- Delivers both basal infusion (continuous
release of a small amount of insulin) and
bolus (additional)
- Administered intraperitoneally
- Fewer hypoglycemic reactions occur and
blood glucose levels are controlled
Portable or external insulin pumps
- Also called continuous subq insulin infusion
(CSII), may have a tube (or infusion set)
placed under the skin
- The needle is inserted into the abdomen,
upper thigh, or upper arm. This type of pump
NCM 106: PHARMACOLOGY
LECTURE
is worn outside the body and placed in a
pocket or bra
- A battery-operated device that uses rapid-
acting insulin, which is stored in a reservoir
syringe placed inside the device
Insulin Jet Injectors
- They shoot insulin, without a needle, directly
through the skin into the fatty tissue
- Because the insulin is delivered under high
pressure, stinging, pain, burning, and
bruising may occur.
- This method of insulin insertion is not
indicated for children or older adults.
- This type of device is also expensive, costing
approximately 2 to 10 times as much as the
subQ dose
• Advise patient to carry a MedicAlert card,
tag, or bracelet indicating the health problem
and insulin dosage.
• Instruct patient on how to check blood
glucose with a glucometer (Sure Touch, One
Step, Accu-Chek).
• Teach patient about care of insulin container
and syringes. Inform patient taking NPH
insulin with regular insulin that regular insulin
is drawn up before NPH insulin.
• Advise patient taking insulin to eat
prescribed diet on a consistent schedule.
Diet information may be obtained from ADA
or a nutritionist.

Nursing Responsibilities
• Monitor vital signs. Tachycardia can occur
during insulin reaction.
• Determine blood glucose levels, and report
changes. The reference value is 60 to 100
mg/dL for blood glucose and 70 to 110
mg/dL for serum glucose.
• Monitor the patient’s HbA1c to provide
feedback of diabetic control.
• Prepare a teaching plan based on patient’s
knowledge of health problem, diet, and drug
therapy.

Health Teachings
• Teach patient to recognize and immediately
report symptoms of hypoglycemic (insulin)
reaction, such as headache, nervousness,
sweating, tremors, rapid pulse, and
hyperglycemic reaction (diabetic acidosis),
such as thirst, increased urine output, and
sweet, fruity breath odor.
• Advise patient that hypoglycemic reactions
are more likely to occur during peak action
time. Most diabetic patients know whether
they are having a hypoglycemic reaction, but
some have higher tolerance to low blood
glucose and can have a severe reaction
without realizing it.
• Explain that orange juice, sugar-containing
drinks, and hard candy may be used when a
hypoglycemic reaction begins.
• Teach family members to administer
glucagon by injection if patient has a
hypoglycemic reaction and cannot drink
sugar-containing fluid.
• Inform patient that certain herbs may interact
with insulin and oral antidiabetic drugs. A
hypoglycemic or hyperglycemic effect might
occur.
• Teach patient about necessity for
compliance with prescribed insulin therapy
and diet. HbA1c provides most accurate
picture of optimal diabetic control.
ORAL HYPOGLYCEMIC DRUGS
- oral antidiabetic drugs
- synthetic preparations that stimulate insulin
release or otherwise alter the metabolic
response to hyperglycemia
- should be used by those with type 2 diabetes
Sulfonylureas
- group of antidiabetics chemically related to
sulfonamides but lacking antibacterial activity
- stimulate pancreatic beta cells to secrete
more insulin which increases the insulin cell
receptors, increasing the ability of the cells to
bind insulin for glucose metabolism
First- Generation Sulfonylureas
• Tolbutamide (Orinase) is a first-generation
shortacting sulfonylurea.
• Tolazamide (Tolinase) is a first-generation
intermediate-acting sulfonylurea.
• Chlorpropamide (Diabinese) is a first-
generation long-acting sulfonylurea.
Second-Generation Sulfonylureas
- increase the tissue response to insulin and
decrease glucose production by the liver
- have greater hypoglycemic potency than the
first-generation sulfonylureas
- have a longer duration of action and cause
fewer side effects

NCM 106: PHARMACOLOGY
LECTURE
- should not be used when liver or kidney
dysfunction is present
• Glimepiride (Amaryl) and glipizide (Glucotrol,
Glucotrol XL), which directly stimulate the
beta cells to secrete insulin, thus decreasing
the blood glucose level.
• Glimepiride improves postprandial glucose
levels.
Side Effects, Adverse Reactions, Contraindications
• The side effects of most oral antidiabetic
drugs are similar to those of insulin. Taking
antidiabetic drugs without adequate food can
lead to an insulin reaction with signs and
symptoms such as nervousness, tremors,
and confusion.
• Adverse reactions include hematologic
disorders, such as aplastic anemia,
leukopenia, and thrombocytopenia. Weight
gain, seizures, and coma may also occur.
• Sulfonylureas are contraindicated in type 1
diabetes (no functioning beta cells), diabetic
ketoacidosis, pregnancy, and lactation and
during stress, surgery, or severe infection.
• The major side effect of sulfonylureas is
hypoglycemia. Acarbose does not cause
hypoglycemia unless it is taken with a
sulfonylurea or insulin. It can cause
increased flatulence (gas), diarrhea, and
abdominal distention.
Nonsulfonylureas
- these drugs affect the hepatic and GI
production of glucose
Biguanides: Metformin (Glucophage)
Metformin
- A biguanide compound that acts by
decreasing hepatic production of glucose
from stored glycogen.
- Diminishes the increase in serum glucose
following a meal and blunts the degree of
postprandial hyperglycemia
- Decreases the absorption of glucose from
the small intestine, and there is evidence that
it increases insulin receptor sensitivity as
well as peripheral glucose uptake at the
cellular level
- Not recommended for patients with renal
impairment
Alpha-Glucosidase Inhibitors: Acarbose (Precose)
and Miglitol (Glyset)
Acarbose
- Acts by inhibiting the digestive enzyme in the
small intestine that is responsible for the
release of glucose from complex
carbohydrates(CHO) in the diet.
- By inhibiting alpha glucosidase, absorption of
complex CHO is delayed.
- Has no demonstrated systemic effects and is
not absorbed into the body in significant
amounts. It does not cause hypoglycemic
reaction.
Miglitol
- inhibits alpha glucosides and is absorbed
from the GI tract
- hypoglycemia could occur if taken with a
sulfonylurea or insulin
Thiazolidinediones
Pioglitazone (Actos)
- Can be taken in combination with
sulfonylurea or insulin, and rosiglitazone may
be combined with metformin.
- These drugs do not induce hypoglycemic
reactions if taken alone.
- They decrease insulin resistance and
improve blood glucose control.
Meglitinides
Repaglinide (Prandin) and nateglinide (Starlix)
- oral antidiabetic agents
- Stimulate the beta cells to release insulin.
- The action of repaglinide and nateglinide is
similar to that of sulfonylureas.
Incretin Modifier
• Also called dipeptidyl peptidase-4 [DPP-4]
inhibitors and gliptins
• The action of DPP-4 inhibitors is to increase
the level of incretin hormones, increase
insulin secretion, and decrease glucagon
secretion to reduce glucose production.
Sitagliptin phosphate and saxagliptin
- oral antidiabetics
- classified as incretin modifiers for treatment
of type 2 diabetes mellitus
- used as adjunct treatment with exercise and
diet to reduce both fasting and postprandial
plasma glucose levels.
Guidelines for Oral Antidiabetic (Hypoglycemic)
Therapy For Type 2 Diabetes
• Onset of diabetes mellitus at age 40 years or
older
• Diagnosis of diabetes for < 5 years
• Normal weight or overweight
• Fasting blood glucose ≤200 mg/dL
• <40 units of insulin required per day
• Normal renal and hepatic function
Nursing Responsibilities
• Determine vital signs. Oral antidiabetics
increase cardiac function and oxygen
consumption, which can lead to cardiac
dysrhythmias.
• Administer oral antidiabetics with food to
minimize gastric upset.
NCM 106: PHARMACOLOGY
LECTURE
• Monitor blood glucose levels, and report
changes. Reference value is 60 to 100
mg/dL for blood glucose and 70 to 110
mg/dL for serum glucose.
• Prepare a teaching plan based on patient’s
knowledge of health problems, diet, and drug
therapy.
Health Teaching
• Advise patient that hypoglycemic (insulin)
reaction can occur when taking an oral
hypoglycemic drug, especially sulfonylureas.
This drug stimulates the release of insulin
from beta cells of the pancreas. Oral
antidiabetics are not insulin. Normally,
patients with diabetes mellitus type 1 do not
have functioning beta cells and should not
take oral antidiabetics, only insulin.
Sulfonylureas are prescribed for patients with
diabetes mellitus type 2.
• Teach patient to recognize symptoms of
hypoglycemic reaction (headache,
nervousness, sweating, tremors, and rapid
pulse) and hyperglycemic reaction (thirst,
increased urine output, sweet, fruity breath
odor).
• Explain that insulin might be needed instead
of oral antidiabetic drug during stress,
surgery, or serious infection. Blood glucose
levels are usually elevated during stressful
times.
• Tell patient about necessity for compliance to
diet and drug.
• Advise patient to carry MedicAlert card, tag,
or bracelet indicating health problem and
antidiabetic dosage.
• Teach patient how to check blood glucose
level with a glucometer. Patient should
record and report abnormal results.
• Advise patient to report side effects such as
vomiting, diarrhea, and rash.
• Caution patient not to ingest alcohol with
antidiabetic drugs to avoid hypoglycemic
reaction.
• Advise patient taking oral antidiabetics to eat
prescribed diet on schedule. Delaying or
missing a meal can cause hypoglycemia.
• Explain use of orange juice, sugar-containing
drinks, or hard candy when hypoglycemic
reaction begins. Explain importance of
reporting such problems to health care
provider.
• Direct patient to take oral antidiabetics with
food to decrease gastric irritation.
HYPERGLYCEMIC DRUGS
Glucagon
- It is a hyperglycemic hormone secreted by
alpha cells of the islets of Langerhans in the
pancreas.
- It increases blood sugar by stimulating
glycogenolysis (glycogen breakdown) in the
liver.
- It protects the body cells, especially those in
the brain and retina, by providing the
nutrients and energy needed to maintain
body function.
- Glucagon is available for parenteral use
(subQ, IM, and IV). It is used to treat insulin-
induced hypoglycemia when other methods
of providing glucose are not available.
Diazoxide
Oral diazoxide (Proglycem)
- which is chemically related to thiazide
diuretics, increases blood sugar by inhibiting
insulin release from the beta cells and
stimulating release of epinephrine
(Adrenalin) from the adrenal medulla.
- This drug is not indicated for hypoglycemic
reaction; rather, it is used to treat chronic
hypoglycemia caused by hyperinsulinism
due to islet cell cancer or hyperplasia.
- The parenteral form of diazoxide (Hyperstat)
is prescribed for malignant hypertension.
- Hypotension does not usually occur with oral
diazoxide.
MODULE 7: RENAL DRUGS
DIURETICS
- Drugs inducing a state of increased urine
flow
- Most diuretics act directly on the kidney with
few exceptions on tubular
- All diuretics except spironolactone exert their
effects from the luminal side of the nephron
- It is necessary for diuretics to get into the
tubule fluid in order to be effective
Drugs that modify salt excretion
• Carbonic anhydrase inhibitors
• Loop diuretics
• Thiazides
• K+ sparing diuretics
• Osmotic diuretics
Drugs that modify water excretion
• Osmotic diuretics
• ADH agonists
• ADH antagonists
Potassium Sparing Diuretics
• Prevent K+ secretion by antagonizing the
effects of aldosterone in collecting tubule
they produce a modest increase in urine
production
• spironolactone, eplerenone--inhibition may
occur by direct pharmacologic antagonism of
mineralocorticoid receptors
NCM 106: PHARMACOLOGY
LECTURE
• amiloride, triamterene-- inhibition of Na+
influx through ion channels in the luminal
membrane nesiritide
• Adverse reaction: hyperkalemia,
hyperchloremic metabolic acidosis,
gynecomastia, acute renal failure, kidney
stones
Baseline data:
• Obtain baseline values for serum potassium,
along with baseline values for weight, blood
pressure (sitting and supine), pulse,
respiration, sodium, and chloride.
• For patients with edema, record sites and
extent of edema
• Use with caution in patients taking ACE
inhibitors, angiotensin receptor blockers, and
direct renin inhibitors
Loop Diuretics
• These drugs produce more loss of fluid and
electrolytes than any other diuretics. They
are known as loop diuretics because their
site of action is in the loop of Henle.
• Loop diuretics inhibit the cotransport of Na +
/K+ /2Cl− in the luminal membrane in the
ascending limb of the loop of Henle.
• Therefore, reabsorption of these ions into the
renal medulla is decreased. By lowering the
osmotic pressure in the medulla, less water
is reabsorbed from water permeable
segments, like the descending loop of Henle,
causing diuresis.
Drugs:
Bumetanide, Ethacrynic acid, Furosemide, Torsemide
• Indication: edema, hypercalcemia, hyperkalemia
• Adverse effects: Ototoxicity, Hyperuricemia,
Hypotension, Hypokalemia, Hypomagnesemia
Identifying High Risk Patients
• Use with caution in patients with
cardiovascular disease, renal impairment,
diabetes mellitus, or a history of gout, and in
patients who are pregnant or taking digoxin,
lithium, ototoxic drugs, NSAIDs, or
antihypertensive drugs.
• Hypotension. Monitor blood pressure. If it
falls precipitously, withhold medication and
notify the prescribed physician
Carbonic Anhydrase Inhibitors
• Pharmacokinetics: well absorbed orally or
topically for glaucoma – applied topically 2-4x
daily
• Adverse effects: hyperchloremic metabolic
acidosis - due to reduction of body bicarbonate
stores potassium depletion, drowsiness and
paresthesia
Preparation
• Oral - Acetazolamide(Diamox) tablet 250 mg
1-4x/d Dichlorphenamide 50 mg 1-3x/d;
Methazolamide 50-100 mg 2-3x/d
• Topical - Dorzolamide ophthalmic drops 2%,
brinzolamide ophthalmic drops
Uricosuric agents
- Drugs which alter excretion of organic
molecules
1. Probenecid
- lipid soluble derivative of benzoic
acid
- inhibits reabsorption of urate in the
proximal convoluted tubule –
increasing its excretion
- effect on Penicillin: inhibits its
excretion thus increasing plasma
concentration
- 90% bound to protein
- given orally, well absorbed in GIT,
peak concentration – 3h
2. Sulfinpyrazone
- congener of phenylbutazone
- powerful inhibitory effects on uric
acid reabsorption in the PCT
- absorbed in GIT
- highly protein bound
- Indacinone – diuretic with uricosuric
properties
- Main effect of uricosuric drugs:
block blood urate reabsorption and
lower plasma urate concentration
TYPES OF INTRAVENOUS FLUIDS
CRYSTALLOIDS
- contain fluids and electrolytes and are
- able to freely cross capillary walls
- used to treat dehydration and electrolyte
imbalances and as short-term maintenance
fluids
- balanced salt/electrolyte solutions which may
be isotonic, hypertonic, or hypotonic
Major Classifications of Crystalloid
Isotonic Solution
- primarily used for hydration and to expand
ECF volume, because the fluid remains in
the intravascular space
- have the same approximate osmolality as
ECF or plasma
- water does not enter/leave the cell because
of the osmotic equilibrium; therefore, there is
no effect on red blood cells
- Examples: Lactated Ringer’s solution,
Ringer’s solution, Normal saline, 5%
Dextrose and water, Plasma-Lyte
NCM 106: PHARMACOLOGY
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Hypotonic Solution
- exert less osmotic pressure than ECF, which
allows water to move into the cell
- used to provide free water and treat cellular
dehydration
- promote waste elimination by the kidneys
- do not administer to clients at risk for IICP or
third-space fluid shift
- Example: 0.45% Normal Saline, 0.33% NaCl,
2.5% Dextrose and water
Hypertonic Solution
- exert greater osmotic pressure than ECF,
resulting in a higher solute concentration
than the serum
- draw fluid out of the intracellular and
interstitial compartments into the vascular
compartment, expanding vascular volume
- do not administer to clients with kidney or
heart disease or clients who are dehydrated
- Example: 3% Sodium chloride, 5% Dextrose
and 0.45% normal saline, 5% Dextrose and
normal saline, 5% Dextrose in Lactated
Ringer’s, 10% Dextrose and water, 50%
Dextrose and water
COLLOIDS
- Also known as plasma expanders
- Contain protein or other large molecular
substances that increase osmolarity without
dissolving in the solution.
- Because of their size, the particles are
unable to pass through the semipermeable
membranes of the capillary walls and stay
within the intravascular compartment
- Act by increasing the colloidal oncotic
pressure and pulling fluids from the
interstitial space into the plasma, increasing
blood volume.
- Composition: proteins, carbohydrates, and
lipids.
- Examples: Albumin, hetastarch, pentastarch,
plasma and dextran
FREE H2O SOLUTIONS
- provide water that is not bound by
macromolecules or organelles, thus is free to
pass through membranes
- Examples: D5W, D10W, D20W, D50W, D50-
50, dextrose/crystalloid mixes
BLOOD PRODUCTS
- include whole blood and the components
that can be processed through centrifugation
methods
- essentially are also considered colloids
- Include whole blood, packed RBCs (PRBCs),
FFP, plasma, platelets, and cryoprecipitate
ELECTROLYTES
SODIUM
- Most abundant cation in ECF and a major
contributor to serum osmolality
- Normal serum sodium levels: 135-145 mEq/L
- Found in many foods like bacon, ham,
processed cheese, and table salt
- Reabsorption:
o 2/3 Proximal Convoluted Tubule
o 25-30% Thick Ascending Loop of
Henle
o 5-10% Distal Convoluted Tubule
Functions of Sodium
- Plays a major role in fluid volume balance,
and is the primary determinant of plasma
osmolality.
- Combines readily with chloride (Cl−) or
bicarbonate (HCO3− ) to promote acid-base
balance
- Promotes the transmission and conduction of
nerve impulses and is part of the
sodium/potassium pump
HYPONATREMIA
- Caused by sodium loss, deficient intake, or
water gain
- Sodium loss can result from vomiting,
diarrhea, nasogastric suctioning, burns,
wound drainage, trauma,r enal failure, heart
failure, third-spacing, syndrome of
inappropriate antidiuretic hormone secretion,
excessive hypertonic or sodium-free IVF,
surgery, and thiazide diuretics
- Oral sodium replacement is the preferred
treatment if the patient is able or if the deficit
is mild. Sodium may also be replaced via
enteral feeding tubes.
Clinical features:
• Cellular swelling
• Primarily neurologic: cerebral edema
• Early symptoms: nausea, headache, and
vomiting
• Severe complications: seizures, brainstem
herniation, normocapneic, respiratory failure,
coma, and death
HYPERNATREMIA
- caused by sodium gain, sodium retention, or
water loss
NCM 106: PHARMACOLOGY
LECTURE
- Causes include excessive oral sodium
intake, deficient water intake, hypertonic tube
feedings, hypertonic IVF,
hyperaldosteronism, Cushing’s syndrome,
corticosteroid use, and acute kidney failure
- Treatments include administration of IVF and
diuretics.
Clinical features:
• Cellular shrinkage
• Predominantly neurologic
• Altered mental status
• Vascular complications (pediatric/neonates)
• Rhabdomyolysis
• Patients with chronic hypernatremia are less
likely to develop severe neurologic
compromise
• Cellular response to chronic hypernatremia
predisposes these patients to the
development of cerebral edema and seizures
during overly rapid hydration
POTASSIUM
- The major intracellular cation; 98% of the
body’s potassium is found within the cells
- Essential for neuromuscular activity and
cellular metabolism
- Moves in and out of the cells under the
influence of the potassium-sodium pump
- Recommended potassium intake is about 40
to 60 mE1 daily; must be ingested daily
because the body cannot conserve it.
Functions of Potassium
- Necessary for transmission and conduction
of nerve impulses and for contraction of
skeletal, cardiac, and smooth muscles
- Necessary for normal kidney function and for
the enzyme action used to change
carbohydrates to energy and amino acids to
protein
- Promotes glycogen storage in hepatic cells,
regulates the osmolality of cellular fluids, and
plays a role in acid-base balance.
HYPOKALEMIA
- Potassium deficit, occurs with serum levels
<3.5 mEq/L
- Caused by excessive loss rather than
deficient intake
- Early clinical manifestations include fatigue,
muscle weakness, anorexia, nausea, and
vomiting.
- Patients with low normal serum potassium
levels may be advised to consume additional
foods high in potassium.
- Clinical features:
• Skeletal muscle weakness and paralysis
• Ileus
• Cardiac
o Arrhythmias
o Hypertension and heart failure
o ECG changes:
§ Broad flat T waves
§ ST depression
§ QT prolongation
• Kidneys
o NaCl and HCO3 retention
o Polyuria, phosphaturia
o Structural changes
Potassium Replacement
• Oral replacement (KCl) – mainstay of
therapy
• Potassium phosphate (oral/IV) – combined
hypokalemia and hypophosphatemia
• Potassium bicarbonate or potassium citrate –
concomitant metabolic acidosis
• IV KCl – reserved use; administered in saline
Oral Potassium Preparations
• Potassium bicarbonate: Indicated for use in
patients with hypokalemia and metabolic
acidosis. (Potassium acetate available for IV
administration.)
• Potassium phosphate: Found primarily in
food. Indicated for patients with hypokalemia
and hypophosphatemia.
• Potassium gluconate: available as elixir or
tablet
• Potassium chloride: All other indications,
including hypokalemic alkalosis. Raises
serum K+ level faster than potassium
bicarbonate.
HYPERKALEMIA
- serum potassium level >5.3 mEq/L; causes
include excessive intake, decreased
NCM 106: PHARMACOLOGY
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excretion, or shift from intracellular to
extracellular space
- Clinical features:
• Cardiac arrhythmias
o Sinus bradycardia, sinus arrest
o Ventricular tachycardia, Vfib,
asystole
• Secondary hyperkalemic paralysis
• Familial hyperkalemic periodic paralysis
• Metabolic acidosis
Treatments
• Potassium Restriction
• Intravenous Sodium Bicarbonate
• 10% Calcium Gluconate
• Insulin and Glucose (10%-50%)
• Kayexalate (Sodium Polystyrene) and
Sorbitol 70%: may be administered orally or
rectally
Effects of Drugs on Potassium Balance
Diuretics are divided into two categories:
1. potassium wasting (kaliuretic)
2. potassium-sparing (antikaliuretic)
Potassium-wasting diuretics
- excrete potassium and other electrolytes
Clinical Manifestations
such as sodium and chloride in the urine
- major cause of hypokalemia, along with
laxatives, corticosteroids, and antibiotics
Potassium-sparing diuretics
- retain potassium but excrete sodium and
chloride in the urine
- cause hyperkalemia, along with oral and IV
potassium salts, central nervous system
(CNS) agents
CALCIUM
- found in approximately equal proportions in
ICF and ECF
- The serum calcium range is 4.5 to 5.5
mEq/L, or 8.5 to 10.5 mg/dL
Physical Examination
Effect of Drugs on Calcium Balance
Functions of Calcium
- Promotes normal nerve and muscle
contraction and plays a role in cardiac
excitability
- Maintains normal cellular permeability and
promotes blood clotting by converting
prothrombin into thrombin
- Also needed for formation of bone and teeth
- Regulated by parathyroid hormone and
calcitonin.
- Calcium and phosphorus have an inverse
relationship; increased calcium levels result
in decreased phosphorus levels.
HYPOCALCEMIA
- Calcium deficit (<4.5 mEq/L)
- Common causes: hyperphosphatemia, acute
pancreatitis, widespread bony metastases,
hypoparathyroidism, alkalosis, diarrhea,
alcoholism, malnutrition, use of loop
diuretics, vitamin D deficiency, and multiple
blood transfusions
HYPERCALCEMIA
- Calcium excess (>5.5 mEq/L)
- May be a result of hyperparathyroidism,
malignancy, hypophosphatemia, excessive
calcium intake, prolonged immobilization,
multiple fractures, and drugs such as
thiazide diuretics and steroids
• Mild hypercalcemia (11-11.5 mg/dL)
o Usually asymptomatic
o Vague neuropsychiatric symptoms
o Peptic ulcer disease
o Nephrolithiasis
o Increased fracture risk
• Severe hypercalcemia (>12-13 mg/dL)
o Lethargy, stupor and coma
o GI symptoms (nausea, anorexia,
constipation)
o Polyuria and polydipsia
o ECG changes
o Bradycardia, AV block and short QT
interval
• Band keratopathy
• Nervous system
o Hypotonia, hyporeflexia, paresis
o Coma, confusion
• Renal
o Signs of renal failure
• Gastrointestinal
o Signs of malignancy
• Cardiovascular
o Arrhythmias, hypotension
• Phosphate preparations, corticosteroids,
loop diuretics, aspirin, anticonvulsants,
magnesium sulfate, and mithramycin are
some of the drug groups that can lower
serum calcium levels.
NCM 106: PHARMACOLOGY
LECTURE
• Excess calcium salt ingestion or infusion and
thiazide and chlorthalidone diuretics can all
contribute to an increased serum calcium
level.
MAGNESIUM
- Most plentiful in the ICF
- Normal serum magnesium level is 1.5 to 2.5
mEq/L or 1.8 to 3 mg/dL
- Daily magnesium requirement is 8 to 20 mEq
Functions of Magnesium
- Promotes transmission of neuromuscular
activity; an important mediator of neural
transmission in the CNS.
- Promotes contraction of the myocardium
- Activates many enzymes for metabolism of
carbohydrates and protein and is responsible
for transportation of sodium and potassium
across cell membranes
HYPOMAGNESEMIA
- Magnesium deficit
- Probably the most undiagnosed electrolyte
deficiency
- To correct severe hypomagnesemia, IV
magnesium sulfate is usually given.
- Cardiac (ventricular) dysrhythmias,
hypotension, and heart block can occur as a
result
HYPERMAGNESEMIA
- Magnesium excess
- Calcium gluconate may be given to decrease
the serum magnesium level.
Effect of Drugs on Magnesium Balance
• Sodium inhibits tubular absorption of magnesium
and calcium. Long-term administration of saline
infusions may result in losses of magnesium and
calcium.
• Diuretics, certain antibiotics, laxatives, and
steroids are drug groups that promote
magnesium loss.
• Hypomagnesemia, enhances the action of
digitalis and causes digitalis toxicity.
• Magnesium sulfate corrects hypomagnesemia
and symptoms of digitalis toxicity. It is common
practice after bypass surgery or myocardial
infarction for patients to be given magnesium
sulfate orally to prevent ventricular arrhythmias in
the perioperative period.
• Excess intake of magnesium salts is the major
cause of serum magnesium excess. Commonly
used medications that may cause
hypermagnesemia include laxatives and
antacids.
CHLORIDE
- Principal anion of ECF
- Major contributor to acid-base balance,
gastric juice acidity, the osmolality of ECF
- Normal serum chloride level is 95-108 mEq/L
HYPOCHLOREMIA
- Decreased serum chloride level
- Clinical manifestations: tremors, twitching,
and slow, shallow breathing
HYPERCHLOREMIA
- Dlevated serum chloride level
- Clinical manifestations: weakness; lethargy;
deep, rapid breathing; and eventual
unconsciousness
PHOSPHORUS
- Found in both ICF and ECF; but is the
primary anion in ICF
- Regulated by PTH and need vitamin D for
absorption from the GI tract
- Normal phosphorus level: 1.7-2.6 mEq/L
- Essential in bone and teeth formation and for
neuromuscular activity
- Important component of nucleic acids (DNA
and RNA) and assists in energy transfer in
cells, helps maintain cellular osmotic
pressure, and supports the acid-base
balance of body fluids
HYPOPHOSPHATEMIA
- May lead to hemolytic anemia, platelet
dysfunction, and reduced oxygen transport.
- Increased intake in the form of laxatives may
also increase serum levels
- Clinical manifestations: muscle weakness,
tremors, paresthesia, bone pain,
hyporeflexia, seizures, hyperventilation,
anorexia, and dysphagia
HYPERPHOSPHATEMIA
- Most often related to chronic kidney disease
- Symptoms: hyperreflexia, tetany, positive
Chvostek’s and Trousseau’s signs, flaccid
paralysis, muscular weakness, tachycardia,
nausea, diarrhea, and abdominal cramps
- Hyperphosphatemia in patients with chronic
kidney disease is treated with restriction of
dietary phosphorus, phosphorus-binding
medications such as calcium acetate
(Phoslo), or dialysis
NCM 106: PHARMACOLOGY
LECTURE
MODULE 8: CENTRAL NERVOUS SYSTEM
DRUGS
Outline:
1. Central Nervous System
• Anxiolytic and hypnotic agents
• Antidepressant agents
• Psychotherapeutic
• Antiepileptic agents
• Antiparkinsonism agents
• Muscle relaxants
• Narcotics and anti-migraine drugs
• General and local anesthetics
• Neuromuscular blocking agents
2. Autonomic Nervous System
• Adrenergic agents
• Adrenergic blocking agents
• Cholinergic agents
• Cholinergic blocking agents
ANXIOLYTIC AND HYPNOTIC AGENTS
ANXIOLYTICS
- Also known antianxiety drugs.
- They are primarily used to treat anxiety and
insomnia.
• Primary anxiety is not caused by a medical
condition or by drug use.
• Secondary anxiety is related to selected drug use
or medical or psychiatric disorders.
• Clinical Manifestations:
o Dyspnea
o Choking sensation
o Chest pain
o Heart palpitations
o Dizziness
o Faintness
o Sweating
o Trembling and shaking
o Fear of losing control
NON PHARMACOLOGIC MEASURES
• Using of relaxation technique
• Psychotherapy
• Support groups
PHARMACOLOGIC MEASURES
Benzodiazepines
- Used as anticonvulsants, sedative-hypnotics,
preoperative drugs, substance abuse
withdrawal agents, and anxiolytics.
- Used mainly for severe or prolonged anxiety.
- Examples: chlordiazepoxide (Librium),
diazepam (Valium), clorazepate dipotassium
(Tranxene), lorazepam (Ativan), and
alprazolam (Xanax).
Lorazepam (Ativan)
- To control anxiety, treat status epilepticus
- For preoperative sedation
- For substance withdrawal
- Potentiate gammaaminobutyric (GABA)
effects by binding to specific benzodiazepine
receptors and inhibiting GABA
neurotransmission
• Side effects: Drowsiness, dizziness, weakness,
confusion, blurred vision, nausea, vomiting,
anorexia, restlessness, hallucinations,
anterograde amnesia, sleep-related behaviors
• Adverse reactions: hypertension, hypotension,
bradycardia, respiratory depression
• Contraindications: Hypersensitivity, CNS
depression, shock, coma, narrow-angle
glaucoma, seizures, alcohol intoxication, liver
impairment, pregnancy, lactation
Nursing Responsibilities
• Observe patient for side effects of anxiolytics.
Recognize that drug tolerance and physical and
psychological dependency can occur with most
anxiolytics.
• Recognize that anxiolytic dosages should be
lower for older adults, children, and debilitated
persons than for middle-aged adults.
• Monitor vital signs, especially blood pressure and
pulse; orthostatic hypotension may occur.
• Encourage family to be supportive of patient.
Health Teachings
• Encourage patient to rise slowly from sitting to
standing position to avoid dizziness from
orthostatic hypotension.
• Advise patient not to drive a motor vehicle or
operate dangerous equipment when taking
anxiolytics, because sedation is a common side
effect.
• Warn patient not to consume alcohol or CNS
depressants such as narcotics while taking an
anxiolytic.
• Teach patient ways to control excess stress and
anxiety (relaxation techniques, long walks).
• Inform patient that effective response may take 1
to 2 weeks.
• Encourage patient to follow drug regimen and not
to abruptly stop taking the drug after prolonged
use because withdrawal symptoms can occur.
Drug dose is usually tapered when drug is
discontinued.
NCM 106: PHARMACOLOGY
LECTURE
SEDATIVE-HYPNOTICS
- For treatment of sleep disorders.
Short-acting hypnotics
- useful in achieving sleep
- allow patient to awaken early in the morning
without experiencing lingering side effects
Intermediate-acting hypnotics
- useful for sustaining sleep
- however, after using one, the patient may
experience residual drowsiness, or
hangover, in the morning.
NONPHARMACOLOGIC METHODS
• Arise at a specific hour in the morning.
• Take few or no daytime naps.
• Avoid drinks that contain caffeine and alcohol 6
hours before bedtime. Also avoid smoking
nicotine 6 hours before bedtime.
• Avoid heavy meals or strenuous exercise before
bedtime.
• Take a warm bath, listen to quiet music, or
perform other soothing activities before bed.
• Decrease exposure to loud noises.
• Avoid drinking copious amounts of fluids before
sleep.
• Drink warm milk before bedtime.
PHARMACOLOGIC MEASURES
Barbiturates
Long-acting barbiturates
- Used to control seizures in epilepsy.
- Phenobarbital and Mephobarbital
Intermediate-acting barbiturates
- Used as sleep sustainers for maintaining
long periods of sleep.
- Butabarbital (Butisol)
Short-acting barbiturates
- Used primarily for sedation preoperatively.
- Secobarbital (Seconal) and pentobarbital
(Nembutal)
Ultrashort-acting barbiturates
- Used as a general anesthetic.
- Thiopental sodium (Pentothal)
Nonbenzodiazepines
- It is used for short term treatment (less than
10 days) of insomnia.
Zolpidem Tartate (Ambien)
- To treat insomnia
- Mode of action: CNS depression,
neurotransmitter inhibition
• Side effects: Drowsiness, lethargy, headache, hot
flashes, hangover (residual sedation), irritability,
dizziness, ataxia, visual disturbances, anxiety,
mental depression, nausea and vomiting, erectile
dysfunction
• Adverse reactions: tolerance, psychological or
physical dependence; sleep-related behaviors,
hypotension, angioedema, dysrhythmias, suicidal
ideation
• Contraindications: Hypersensitivity to
benzodiazepine, respiratory depression, lactation
Nursing Responsibilities: Hypnotics
• Monitor vital signs. Check for signs of respiratory
depression (slow, irregular breathing patterns)
• Use bed alarm for older adults or patients
receiving nonbenzodiazepines for the first time
• Confusion may occur, and injury may result.
• Observe patient for side effects of
nonbenzodiazepines (e.g., hangover [residual
sedation], lightheadedness, dizziness, confusion)
Health Teachings
• Teach patient to use nonpharmacologic ways to
induce sleep
• Encourage patient to avoid alcohol,
antidepressant, antipsychotic, and narcotic drugs
while taking nonbenzodiazepines. Severe
respiratory depression may occur when these
drugs are combined.
• Advise patient to take nonbenzodiazepine before
bed time. Alprazolam takes effect within 15 to 30
minutes.
• Suggest that patient urinate before taking
nonbenzodiazepine to prevent sleep disruption
• Encourage patient to check with health care
provider about OTC sleeping aids
• Drowsiness may result from taking these drugs,
so caution while driving is advised.
• Advise patient to report adverse reactions such
as hangover to health care provider.
• Drug selection or dosage may need to be
changed if hangover occurs.
Melatonin Agonists
Ramelteon (Rozerem)
- Is in the newest category of
sedative/hypnotics.
- Acts by selectively targeting melatonin
receptors to regulate circadian rhythm in the
treatment of insomnia
- Has not been shown to decrease REM sleep
- Also used as an antianxiety drug
• Adverse effects: drowsiness, dizziness, fatigue,
headache, nausea, and suicidal ideation
ANTIDEPRESSANT AGENTS AND
MOOD STABILIZERS
ANTIDEPRESSANTS
NCM 106: PHARMACOLOGY
LECTURE
- used for depressive episodes that are
accompanied by feelings of hopelessness
and helplessness
- can be prescribed for 1-12 months or longer
DEPRESSION
- Characterized primarily by mood changes
and loss of interest in normal activities
- Contributing causes of depression
o Genetic predisposition
o Social and environmental factors
o Biologic conditions.
- Signs of major depression
o Loss of interest in most activities
o Depressed mood
o Weight loss or gain
o Insomnia or hypersomnia
o Loss of energy
o Fatigue
o Feelings of despair
o Decreased ability to think or
concentrate
o Suicidal thoughts
- Three types of depression:
1. Reactive
2. Major
3. Bipolar Affective
Reactive depression
- Usually has a sudden onset after a
precipitating event (e.g., depression resulting
from a loss, such as death of a loved one).
- The patient knows why he or she is
depressed and may call this “the blues.”
- This type of depression lasts for months
- A benzodiazepine agent may be prescribed.
Major depression
- Characterized by loss of interest in work and
home, inability to complete tasks, and deep
depression (dysphoria)
- Antidepressants have been effective in
treating major depression
o Primary is not related to other
health problems.
o Secondary to a health problem
(e.g., physical or psychiatric
disorder or drug use)
Bipolar affective disorder
- Involves swings between two moods, the
manic (euphoric) and the depressive
(dysphoria).
- Lithium (Lithobid) was originally the drug of
choice for treating this type of disorder.
- Other mood stabilizers, such as
carbamazepine (Tegretol), valproic acid or
divalproex (Depakote, Valproate), and
lamotrigine (Lamictal) are also currently first-
line drugs of choice for bipolar disorder.
Antidepressant Agents:
1. Tricyclic Antidepressants (TCAs), or
Tricyclics
2. Selective Serotonin Reuptake Inhibitors
(SSRIs)
3. Serotonin Norepinephrine Reuptake
Inhibitors (SNRIs)
4. Atypical Antidepressants that affect
various neurotransmitters
5. Monoamine Oxidase Inhibitors (MAOIs)
TRICYCLIC ANTIDEPRESSANTS (TCAs)
- Block the uptake of the neurotransmitters
norepinephrine and serotonin in the brain.
- Clinical response of TCAs occurs after 2 to 4
weeks of drug therapy.
- Elevate mood, increase interest in daily living
and activity, and decrease insomnia.
List of Tricyclic Antidepressants
• amitriptyline (Elavil)
• clomipramine HCl (Anafranil)
• desipramine HCl (Norpramin)
• doxepin (Silenor)
• imipramine (Tofranil)
• nortriptyline (Pamelor/ Aventyl)
• protriptyline (Vivactil)
• trimipramine (Surmontil)
SIDE EFFECTS
• Orthostatic hypotension
• Sedation
• Anticholinergic effects
• Allergic reactions (skin rash, pruritus, and
petechiae) and sexual dysfunction
(impotence and amenorrhea)
ADVERSE REACTIONS
• Blood dyscrasias (leukopenia,
thrombocytopenia, and agranulocytosis)
requiring close monitoring of blood cell
counts.
• Extrapyramidal symptoms (EPS)
• Neuroleptic malignant syndrome (NMS)
• Seizure
• Cardiotoxicity, such as dysrhythmias that
may result from high doses of the drug.
• Note: The therapeutic serum range is 100 to
200 ng/mL
WARNING!
• Alcohol, hypnotics, sedatives, and
barbiturates potentiate central nervous
system (CNS) depression when taken with
TCAs.
• Concurrent use of MAOIs with amitriptyline
may lead to cardiovascular instability and
toxic psychosis.
• Antithyroid medications taken with
amitriptyline may increase the risk of
dysrhythmias.
NCM 106: PHARMACOLOGY
LECTURE
SELECTIVE SEROTONIN REUPTAKE INHIBITORS Adverse Effects
(SSRIs) • Hyponatremia • Blood dyscrasias
- Block the reuptake of serotonin into the • Bleeding • Suicidal ideation
nerve terminal of the CNS, thereby • Hypertension • Stevens Johnson
enhancing its transmission at the • Angioedema syndrome
serotonergic synapse.
- Do not block the uptake of dopamine or ATYPICAL ANTIDEPRESSANTS
norepinephrine, and they do not block - Also known as Second-generation
cholinergic and alpha1-adrenergic receptors. antidepressants
- Commonly used to treat depression than are - Used for major depression, reactive
TCAs. They have fewer side effects than depression, and anxiety.
TCAs - They affect one or two of the three
neurotransmitters: serotonin, norepinephrine,
List of Selective Serotonin Reuptake Inhibitors and dopamine.
(SSRIs) • Note: Atypical antidepressants should not be
• fluoxetine (Prozac) taken with MAOIs and should not be used within
• fluvoxamine (Luvox) 14 days after discontinuing MAOIs.
• sertraline (Zoloft)
• paroxetine (Paxil) List of Atypical Antidepressants
• citalopram (Celexa) • amitriptyline (Elavil)
• escitalopram (Lexapro) • clomipramine (Anafranil)
• desipramine (Norpramin)
Side Effects • doxepin (Sinequan)
• Dry mouth • Tremors • imipramine (Tofranil)
• Blurred vision • Anorexia • nortriptyline (Aventyl)
• Insomnia • Nausea • protriptyline (Vivactil)
• Headache • Diarrhea • trimipramine (Surmontil)
• Nervousness • Sexual Dysfunction
Side Effects
Adverse Reactions • Drowsiness
• Seizures • Bleeding • Dizziness
• Hyponatremia • Osteopenia • Orthostatic hypotension
• Dehydration • Suicidal ideation • Dry mouth
• Constipation
• Note: Many SSRIs have an interaction with • Urinary retention
grapefruit juice that can lead to possible toxicity
• It is recommended that daily intake be limited to 8 Adverse Reaction
ounces of grapefruit juice or ½ of a grapefruit. • Suicidal ideation

SEROTONIN NOREPINEPHRINE REUPTAKE

INHIBITORS (SNRIs) MONOAMINE OXIDASE INHIBITORS
- Inhibit the reuptake of serotonin and - The enzyme monoamine oxidase (MAO)
norepinephrine, increasing availability in the inactivates norepinephrine, dopamine,
synapse. epinephrine, and serotonin. By inhibiting
- Used for major depression MAO, the levels of these neurotransmitters
- Other approved uses are for generalized rise.
anxiety disorder and social anxiety disorders - There are two forms of MAO enzyme: MAO-
A and MAO-B. These enzymes are found
List of Serotonin Norepinephrine Reuptake primarily in the liver and brain. MAO-A
Inhibitors (SNRIs) inactivates dopamine in the brain, whereas
• duloxetine (Cymbalta) MAO-B inactivates norepinephrine and
• desvenlafaxine (Pristiq) serotonin.
• venlafaxine (Effexor) - The MAOIs are nonselective, inhibiting both
MAO-A and MAO-B.
Side Effects
• Drowsiness • Euphoria List of Monoamine Oxidase Inhibitors
• Dizziness • Amnesia • tranylcypromine sulfate (Parnate)
• Insomnia • Photosensitivity • isocarboxazid (Marplan)
• Headache • Ejaculation • selegiline HCl (Emsam, Eldepryl)
• Blurred vision dysfunction • phenelzine sulfate (Nardil)

NCM 106: PHARMACOLOGY
LECTURE
Side Effects
• CNS stimulation (agitation, restlessness, and
insomnia)
• Orthostatic hypotension
• Anticholinergic effects.
• Note: Any drugs that are CNS stimulants or
sympathomimetics (e.g., vasoconstrictors and
cold medications containing phenylephrine and
pseudoephedrine) can cause a hypertensive
crisis when taken with an MAOI.
• Foods that contain tyramine (cheese [cheddar,
Swiss, bleu], cream yogurt, coffee, chocolate,
bananas, raisins, Italian green beans, liver,
pickled foods, sausage, soy sauce, yeast, bear,
and red wines) have sympathomimetic-like
effects and cause a hypertensive crisis
Nursing Responsibilities: ANTIDEPRESSANTS
- Observe patient for signs and symptoms of
depression: mood changes, insomnia,
apathy, or lack of interest in activities.
- Monitor patient’s vital signs. Orthostatic
hypotension is common. Check for
anticholinergic-like symptoms: dry mouth,
increased heart rate, urinary retention, or
constipation. Check weight two to three
times per week.
- Monitor patient for suicidal tendencies when
marked depression is present.
- Observe patient for seizures when patient is
taking an anticonvulsant; antidepressants
lower the seizure threshold. The
anticonvulsant dose might need to be
increased.
- Monitor for drug-drug and food-drug
interactions. Sympathomimetic-like drugs
and foods containing tyramine may cause a
hypertensive crisis if taken with MAOIs.
- Check patient for extremely high blood
pressure when taking MAOIs.
- Provide patient with a list of foods to avoid
when taking MAOIs to avoid hypertensive
crisis.
- These foods include cheese, red wine, beer,
liver, bananas, yogurt, and sausage.
Health Teachings
- Teach patient to take the medication as
prescribed. Compliance is important.
- Inform patient that full effectiveness of drug
may not be evident until 1 to 2 weeks after
start of therapy.
- Encourage patient to keep medical
appointments.
- Caution patient not to consume alcohol or
any CNS depressants because of their
addictive effect.
- Inform patient that many herbal products
interact with antidepressants, especially
MAOIs and SSRIs. Herbs may need to be
discontinued, or the antidepressant drug
dosage may need to be modifie
- Warn patient not to drive or be involved in
potentially dangerous mechanical activity
until stabilization of drug dose has been
established.
- Advise patient not to abruptly stop taking the
drug. Drug dose should be gradually
decreased by health care provider.
- Encourage patient who is planning
pregnancy to consult with health care
provider about possible teratogenic effects of
the drug on the fetus.
- Take with food if gastrointestinal (GI) distress
occurs.
- Advise patient that antidepressants may be
taken at bedtime to decrease dangers from
the sedative effect. Have patient check with
health care provider.
- Transient side effects include nausea,
drowsiness, headaches, and nervousness.
MOOD STABILIZERS
- Used to treat bipolar affective disorder.
- First-line drugs for bipolar disorder
o Lithium (Lithobid)
o carbamazepine (Tegretol)
o valproic acid or divalproex
(Depakote, Valproate)
o lamotrigine (Lamictal)
Lithium (Lithobid)
- To treat bipolar psychosis, manic episodes
- Mode of Action: Alteration of ion transport in
muscle and nerve cells; increased receptor
sensitivity to serotonin
• Side Effects: Headache, memory impairment,
blurred vision, metallic taste, dental caries,
lethargy, drowsiness, dizziness, tremors, slurred
speech, dry mouth, anorexia, vomiting, diarrhea,
polyuria, dehydration, hypotension, abdominal
pain, muscle weakness, restlessness
• Adverse Reactions Urinary and fecal
incontinence, hyperglycemia, hyponatremia,
proteinurea, polyurea, leukocytosis,
nephrotoxicity Lifethreatening: Cardiac
dysrhythmias, seizures, cardiac arrest, serotonin
syndrome, neuroleptic malignant syndrome
• Contraindications: Liver and renal disease,
pregnancy, lactation, severe cardiovascular
disease, severe dehydration, hyponatremia,
children <12 y
Nursing Responsibilities
- Observe patient for signs and symptoms of
depression: mood changes, insomnia,
apathy, or lack of interest in activities.
- Monitor patient’s vital signs. Orthostatic
hypotension is common.
NCM 106: PHARMACOLOGY
LECTURE
- Draw blood samples for lithium levels
immediately before the next dose (8 to 12
hours after the previous dose).
- Monitor for signs of lithium toxicity. Report
high (greater than 1.5 mEq/L) and toxic
(greater than 2.0 mEq/L) serum lithium levels
immediately to health care provider.
- Monitor patient for suicidal tendencies when
marked depression is present.
- Evaluate patient’s urine output and body
weight. Fluid volume deficit may occur as a
result of polyuria.
- Observe patient for fine- and gross-motor
tremors and presence of slurred speech,
which are signs of adverse reaction.
- Check patient’s cardiac status. Loss of fluids
and electrolytes may cause cardiac
dysrhythmias.
- Monitor patient’s serum electrolytes. Report
abnormal findings.
Health Teachings
- Teach patient to take lithium as prescribed.
- Emphasize importance of adherence to the
therapy, laboratory tests, and follow-up visits
with health care provider. If lithium is
stopped, manic symptoms will reappear.
- Encourage patient to keep medical
appointments. Have patient check with
health care provider before taking OTC
preparations.
- Warn patient not to drive a motor vehicle or
be involved in potentially dangerous
mechanical activity until stable lithium level is
established.
- Advise patient to maintain adequate fluid
intake: 2 to 3 L/d initially and 1 to 2 L/d
maintenance. Fluid intake should increase in
hot weather.
- Teach patient to take lithium with meals to
decrease gastric irritation.
- Inform patient that effectiveness of drug may
not be evident until 1 to 2 weeks after the
start of therapy. Compliance in taking the
prescribed lithium doses on a daily basis is a
major problem with bipolar patients. When
patient has a period of emotional stability, he
- or she does not believe that the drug is
needed; thus, patient stops taking the
lithium.
- Advise patient who is planning pregnancy to
consult with health care provider about
possible teratogenic effects of the drug on
the fetus, especially during the first 3
months.
- Encourage patient to wear or carry an
identification tag or bracelet indicating the
drug taken.
- Inform patient to avoid caffeine products
(coffee, tea, cola), because they can
aggravate the manic phase of bipolar
disorder.
- Advise patient to maintain adequate sodium
intake and to avoid crash diets that affect
physical and mental health.
- Advise patient to contact health care provider
if experiencing symptoms of toxicity. Early
symptoms include diarrhea, drowsiness, loss
of appetite, muscle weakness, nausea,
vomiting, slurred speech, trembling. Late
symptoms include blurred vision, confusion,
increased urination, convulsions, severe
trembling, and unsteadiness.
ANTIPSYCHOTICS
- These drugs improve the thought processes
and behavior of patients with psychotic
symptoms, especially those with
schizophrenia and other psychotic disorders.
- Sometimes these antipsychotics are called
dopamine antagonists. Antipsychotics block
D2 dopamine receptors in the brain, reducing
psychotic symptoms.
- Many antipsychotics block the
chemoreceptor trigger zone and vomiting
(emetic) center in the brain, producing an
antiemetic (prevents or relieves nausea and
vomiting) effect.
- When dopamine is blocked, however,
extrapyramidal symptoms (EPS) of
Parkinsonism such as tremors, masklike
facies, rigidity, and shuffling gait may
develop. Many patients who take high
potency antipsychotic drugs may require
long-term medication for parkinsonian
symptoms
PSYCHOSIS
- Losing contact with reality
- Manifested in a variety of mental or
psychiatric disorders
- Usually characterized by more than one
symptom, but these may include difficulty in
processing information and coming to a
conclusion, delusions, hallucinations,
incoherence, catatonia, and aggressive or
violent behavior.
SCHIZOPHRENIA
- A chronic psychotic disorder
- Major category of psychosis in which many
of these symptoms are manifested (divided
into two groups)
o Positive symptoms
§ Exaggeration of normal
function (e.g., agitation)
§ Incoherent speech
§ Hallucinations
§ Delusions
§ Paranoia
o Negative symptoms
§ Decrease or loss in
function and motivation
§ Poverty of speech content
NCM 106: PHARMACOLOGY
LECTURE
§ Poor self-care - Remain with patient while medication is
§ Social withdrawal taken and swallowed; some patients hide
antipsychotics in the mouth to avoid taking
Note: The typical or traditional group of antipsychotics them.
is more helpful for managing positive symptoms than - Avoid skin contact with liquid concentrates to
negative symptoms. While atypical have been found prevent contact dermatitis. Liquid must be
to be more useful in treating both the positive and protected from light and should be diluted
negative symptoms of schizophrenia. with fruit juice.
- Administer oral doses with food or milk to
Typical Antipsychotic Agents decrease gastric irritation.
Nonphenothiazines - Dilute oral solution of fluphenazine in fruit
- block only the neurotransmitter dopamine juice, water, or milk. Avoid apple juice and
o butyrophenones caffeinated drinks.
o dibenzoxazepines - Administer by IM route deep into muscle,
o dihydroindolones because drug irritates fatty tissue. Do not
administer intravenously.
Phenothiazines - Check blood pressure for marked decrease
- block norepinephrine, causing sedative and or increase 30 minutes after drug is injected.
hypotensive effects early in treatment - Do not mix in same syringe with heparin,
o thioxanthenes pentobarbital, cimetidine, or dimenhydrinate.
- Chill suppository in refrigerator for 30
Atypical Antipsychotic Agents minutes before removing foil wrapper.
- They are effective for treating schizophrenia - Observe for EPS: acute dystonia, akathisia,
and other psychotic disorders in patients who pseudoparkinsonism, and tardive dyskinesia.
do not respond to or are intolerant of typical - Report these promptly to the health care
antipsychotics. provider.
- They are often used instead of traditional - Assess for symptoms of NMS: increased
typical antipsychotics as first-line therapy fever, pulse, and blood pressure; muscle
because of their decreased side effects, rigidity; increased creatine phosphokinase
atypical antipsychotics. and WBC count; altered mental status; acute
renal failure; varying levels of
Adverse Reactions consciousness; pallor; diaphoresis;
1. Extrapyramidal Syndrome tachycardia; and dysrhythmias.
- Record urine output as urinary retention may
result.
- Monitor serum glucose level.

Health Teachings
- Encourage patient to take the drug exactly
as ordered. In schizophrenia and other
psychotic disorders, antipsychotics do not
cure the mental illness but do alleviate
symptoms. Many patients on medication can
function outside of the institution setting.
Adherence to drug regimen is extremely
2. Neuroleptic Malignant Syndrome
important.
- Inform patient that medication may take 6
List of Antipsychotics
weeks or longer to achieve full clinical effect.
- Caution patient not to consume alcohol or
other CNS depressants such as narcotics;
these drugs intensify the depressant effect
on the body.
- Recommend patient not to abruptly
discontinue the drug. Seek advice from
health care provider before making any
changes in dosage.
- Encourage patient to read labels on OTC
preparations. Some are contraindicated
when taking antipsychotics.
- Teach smoking cessation, because smoking
Nursing Responsibilities: Antipsychotics
increases metabolism of some
- Monitor vital signs. Orthostatic hypotension
antipsychotics.
is likely to occur.

NCM 106: PHARMACOLOGY
LECTURE
- Guide patient to maintain good oral hygiene
by frequently brushing and flossing teeth.
- Encourage patient to talk with health care
provider regarding family planning. The
effect of antipsychotics on the fetus is not
fully known; however, there may be
teratogenic effects.
- Explain to the breastfeeding patient that
phenothiazine passes into breast milk,
possibly causing drowsiness and unusual
muscle movement in the infant.
- Warn patient about importance of routine
follow-up examinations.
- Encourage patient to obtain laboratory tests
on schedule. WBCs are monitored for 3
months, especially during the start of drug
therapy. Leukopenia, or decreased WBCs,
may occur. Be alert to symptoms of malaise,
fever, and sore throat, which may be an
indication of agranulocytosis, a serious blood
dyscrasia.
- Teach patient to report symptoms of infection
promptly to the health care provider,
especially when patient is taking clozapine.
- Advise patient to wear an identification
bracelet indicating the medication taken.
- Inform patient that tolerance to sedative
effect develops over a period of days or
weeks.
- Direct patient to avoid potentially dangerous
situations, such as driving, until drug dosing
has been stabilized.
- Inform patient about EPS; instruct patient to
promptly report symptoms to health care
provider.
- Encourage patient to wear sunglasses for
photosensitivity, to limit exposure to direct
sunlight, and to use sunscreen and
protective clothing to prevent a skin rash.
- Warn patient about orthostatic hypotension
and possible dizziness.
- Teach patient who is taking aliphatic
phenothiazines such as chlorpromazine that
the urine might be pink or red-brown; this
discoloration is harmless.
- Inform patient that changes may occur
related to sexual functioning and
menstruating. Women could have irregular
menstrual periods or amenorrhea, and men
might experience impotence
andgynecomastia (enlargement of breast
tissue).
- Suggest lozenges or hard candy if mouth
dryness occurs. Advise patient to consult
health care provider if dry mouth persists for
more than 2 weeks.
- Encourage patient to avoid extremes in
environmental temperatures and exercise.
- Advise patient to rise slowly from sitting or
lying to standing to prevent a sudden
decrease in blood pressure.
ANTIEPILEPTIC AGENTS
- Drugs used for epileptic seizures
- Also known as anticonvulsants
- Stabilize nerve cell membranes and
suppress the abnormal electric impulses in
the cerebral cortex.
Anticonvulsant Drugs Work in One of Three Ways
1. By suppressing sodium influx through the
drug binding to the sodium channel when it is
inactivated, prolonging the channel
inactivation and thereby preventing neuron
firing.
2. By suppressing the calcium influx, preventing
the electric current generated by the calcium
ions to the T-type calcium channel.
3. By increasing the action of gamma-
aminobutyric acid (GABA), which inhibits
neurotransmitter throughout the brain
Hydantoins
- Act by inhibiting sodium influx, stabilizing cell
membranes, reducing repetitive neuronal
firing, and limiting seizures.
- By increasing the electrical stimulation
threshold in cardiac tissue, it also acts as an
antidysrhythmic.
- It has a small effect on general sedation, and
it is nonaddicting.
Phenytoin (Hydantin)
- To prevent tonicclonic (grand mal) and
complex partial seizures
- Mode of Action: Reduces motor cortex
activity by altering ion transport
• Side effects: Headache, diplopia, confusion,
dizziness, sluggish, decreased coordination,
ataxia, slurred speech, rash, anorexia, nausea,
vomiting, hypotension (after IV administration),
pink-red/brown discoloration of urine
• Adverse reactions: Leukopenia, hepatitis,
depression, gingival hyperplasia, nystagmus,
hirsutism, osteoporosis Life-threatening Aplastic
anemia, thrombocytopenia, agranulocytosis,
Stevens-Johnson syndrome, hypotension,
ventricular fibrillation, encephalopathy, suicidal
ideation
• Contraindications: hypersensitivity, heart block,
bradycardia, psychiatric disorders, pregnancy
Succinimides
Ethosuximide (Zarontin)
- To treat absence or petit mal seizures, and it
may be used in combination with other
anticonvulsants to treat such seizures
- Mode of action: act by decreasing calcium
influx through the T-type calcium channels
• Side effects: Gastric irritation; may take with food
NCM 106: PHARMACOLOGY
LECTURE
• Adverse reactions: Blood dyscrasias, renal and
liver impairment, and systemic lupus
erythematosus
Benzodiazepines
Clonazepam (Klonopin) CSS IV
- Effective in controlling petit mal (absence)
seizures, myoclonus, and status epilepticus.
Iminostilbene
Carbamazepine (Tegretol)
- Effective in treating refractory seizure
disorders that have not responded to other
anticonvulsant therapies
- Used to control grand mal and partial
seizures and a combination of these seizures
- Also used for psychiatric disorders (e.g.,
bipolar disease), trigeminal neuralgia (as an
analgesic), and alcohol withdrawal
Valproate
Valproate (Depakote)
- For psychomotor, myoclonic, absence, and
tonic-clonic seizures
- Also approved for bipolar disorder and
migraine prophylaxis
Nursing Responsibilities
- Monitor serum drug levels of anticonvulsant
to determine therapeutic range (10 to 20
mcg/mL).
- Encourage patient’s compliance to
medication regimen.
- Monitor patient’s CBC levels for early
detection of blood dyscrasias.
- Use seizure precautions (environmental
protection from sharp objects, such as table
corners) for patients at risk for seizures.
- Determine whether patient is receiving
adequate nutrients; phenytoin may cause
anorexia, nausea, and vomiting.
- Advise female patients who are taking oral
contraceptives and anticonvulsants to use an
- additional contraceptive method.
Health Teaching
• Teach patient to shake suspension form
thoroughly before use to adequately mix
medication and assure accurate dosage.
• Advise patient not to drive or perform other
hazardous activities when initiating
anticonvulsant therapy as drowsiness may occur.
• Counsel female patients contemplating
pregnancy to consult with health care provider,
because phenytoin and valproic acid may have a
teratogenic effect.
• Monitor serum phenytoin levels closely during
pregnancy, because seizures tend to become
more frequent due to increased metabolic rates.
• Warn patient to avoid alcohol and other CNS
depressants, because they can cause an added
depressive effect on the body.
• Explain to patient that certain herbs can interact
with an anticonvulsant drug and dose adjustment
may be required.
• Encourage patient to obtain medical alert
identification card, medical alert bracelet, or tag
that indicates health diagnosis and drug regimen.
• Teach patient not to abruptly stop drug therapy,
but rather to withdraw the prescribed drug
gradually under medical supervision to prevent
seizure rebound (recurrence of seizures) and
status epilepticus (continuous seizure state).
• Counsel patient about the need for preventive
dental checkups.
• Warn patient to take prescribed anticonvulsant,
get laboratory tests as ordered, and keep follow-
up visits with health care provider.
• Teach patient not to self-medicate with over-the-
counter (OTC) drugs without first consulting
health care provider.
• Advise patient with diabetes to monitor serum
glucose levels more closely than usual because
phenytoin may inhibit insulin release, causing an
increase in glucose level. Inform patient of the
existence of national, state, and local
associations that provide resources, current
information, and support for persons with
epilepsy.
• Coach patient to take anticonvulsant at the same
time every day with food or milk.
• Tell patient that urine may be a harmless pinkish
red or reddish brown.
• Advise patient to maintain good oral hygiene and
to use a soft toothbrush to prevent gum
• irritation and bleeding.
• Teach patient to report symptoms of sore throat,
bruising, and nosebleeds, which may indicate a
blood dyscrasia.
• Encourage patient to inform health care provider
of adverse reactions such as gingivitis,
nystagmus, slurred speech, rash, and dizziness.
Stevens-Johnson syndrome begins with a rash.
ANTIPARKINSONISM AGENTS
Parkinsonism (Parkinson’s disease)
- A chronic neurologic disorder that affects the
extrapyramidal motor tract (which controls
posture, balance, and locomotion).
- It is caused by an imbalance of the
neurotransmitters dopamine (DA) and
acetylcholine (ACh).
- It is marked by degeneration of neurons of
the extrapyramidal motor tract. The reason
for the degeneration of neurons is unknown.
Pathophysiology of Parkinsonism
- There are two neurotransmitters within
neurons of the striatum of the brain:
dopamine, an inhibitory neurotransmitter,
NCM 106: PHARMACOLOGY
LECTURE
and acetylcholine, an excitatory
neurotransmitter.
- Dopamine is released from the dopaminergic
neurons; acetylcholine is released from the
cholinergic neurons.
- Dopamine normally maintains control of
acetylcholine and inhibits its excitatory
response.
- In parkinsonism, there is an unexplained
degeneration of the dopaminergic neurons,
and an imbalance between dopamine and
acetylcholine occurs.
- With less dopamine production, the
excitatory response of acetylcholine exceeds
the inhibitory response of dopamine. An
excessive amount of acetylcholine stimulates
neurons that release GABA. With increased
stimulation of GABA, the symptomatic
movement disorders of parkinsonism occur.
Three symptoms were described by Parkinson
1. Involuntary tremors of the limbs
2. Rigidity of muscles
3. Slowness of movement (bradykinesia)
Pseudoparkinsonism
- frequently occurs as an adverse reaction to
antipsychotic drugs, especially the
phenothiazines.
NONPHARMACOLOGIC MEASURES
• Patient teaching
• Exercise (Therapeutic exercise program)
• Nutrition (Balanced diet with fiber and fluids)
• Group support
Drugs used to treat parkinsonism reduce the
symptoms or replace the dopamine deficit.
These drugs fall into five categories:
1. Anticholinergics - block cholinergic
receptors
2. Dopamine replacements - stimulate
dopamine receptors
3. Dopamine agonists - stimulate dopamine
receptors
4. MAO-B inhibitors - inhibit the monoamine
oxidase-B (MAO-B) enzyme that interferes
with dopamine
5. COMT inhibitors - inhibit the catechol O-
methyltransferase enzyme that inactivates
dopamine.
Anticholinergic Drugs
- They reduce the rigidity and some of the
tremors characteristic of parkinsonism but
have minimal effect on bradykinesia.
- These are parasympatholytics that inhibit the
release of acetylcholine.
- They are still used to treat drug-induced
parkinsonism, or pseudoparkinsonism, a side
effect of the antipsychotic drug group
phenothiazines.
- Examples of anticholinergics used for
parkinsonism include trihexyphenidyl
(Artane), benztropine (Cogentin), and
biperiden (Akineton).
Side Effects
• Dry mouth, blurred vision, drowsiness,
muscle weakness, constipation
Contraindications:
• Patients with glaucoma
• GI obstruction
• Severe ulcerative colitis
• Prostatic hypertrophy
• Myasthenia gravis
Nursing Responsibilities
- Monitor vital signs, urine output, and bowel
sounds. Increased pulse rate, urinary
retention, and constipation are side effects of
anticholinergics.
- Observe for involuntary movements.
Health Teachings
- Advise patient to avoid alcohol, cigarettes,
caffeine, and aspirin to decrease gastric
acidity.
- Encourage patient to relieve dry mouth with
hard candy, ice chips, or sugarless chewing
gum. Anticholinergics decrease salivation.
- Suggest that patient use sunglasses in direct
sunlight because of possible photophobia.
- Advise patient to void before taking the drug
to minimize urinary retention.
- Counsel patient who takes an anticholinergic
for control of symptoms of parkinsonism to
have routine eye examinations because
patients who have glaucoma should not take
anticholinergics.
- Encourage patient to ingest foods high in
fiber and increase fluid intake to prevent
constipation.
Dopaminergics
Levodopa
- effective in diminishing symptoms of
Parkinson’s disease and increasing mobility,
because the blood-brain barrier admits
levodopa but not dopamine.
Dopa decarboxylase
- The enzyme that converts levodopa to
dopamine in the brain, but this enzyme is
also found in the peripheral nervous system
and allows 99% of levodopa to be converted
to dopamine before it reaches the brain.
- Therefore only about 1% of levodopa taken
is available to be converted to dopamine
once it reaches the brain, and large doses
are needed to achieve a pharmacologic
response.
NCM 106: PHARMACOLOGY
LECTURE
Carbidopa • Administer carbidopa-levodopa (Sinemet) with
- developed to inhibit the enzyme dopa lowprotein foods. High-protein diets
decarboxylase. By inhibiting the enzyme in • interfere with drug transport to the CNS.
the peripheral nervous system, more • Observe for symptoms of parkinsonism.
levodopa reaches the brain.
- The carbidopa is combined with levodopa in Health Teachings
a ratio of 1 part carbidopa to 10 parts • Urge patient not to abruptly discontinue the
levodopa. medication. Rebound parkinsonism
• (increased symptoms of parkinsonism) can occur.
Carbidopa-Levodopa (Sinemet) • Inform patient that urine may be discolored and
- To treat parkinsonism; to relieve tremors and will darken with exposure to
rigidity • air. Perspiration also may be dark. Explain that
both are harmless but clothes
Mode of Action: Transmission of levodopa to brain
• may be stained.
cells for conversion to dopamine; carbidopa blocks
• Advise patient to avoid chewing or crushing
the conversion of levodopa to dopamine in the
extended release tablets.
intestine and peripheral tissues
• Encourage patient to report side effects and
Advantages of the carbidopa-levodopa combination symptoms of dyskinesia. Explain to
- More dopamine reaches the basal ganglia. • patient that it may take weeks or months before
- Smaller doses of levodopa are required to symptoms are controlled.
achieve the desired effect. • Suggest to patient that taking levodopa with food
may decrease GI upset, but
Disadvantage of the carbidopa-levodopa combination • food will slow the drug absorption rate.
- With more available levodopa, more side • Urge patient who takes high doses of selegiline to
effects may be noted. avoid foods high in tyramine
• (e.g., aged cheese, red wine, cream, yogurt,
Side Effects chocolate, bananas, raisins) to
• Anorexia • Dry mouth • prevent hypertensive crisis.
• Nausea • Bitter taste
• Vomiting • Twitching Dopamine Agonists
• Dysphagia • Blurred vision - Stimulate the dopamine receptors.
• Fatigue • Insomnia
• Dizziness • Dark urine
Amantadine hydrochloride (Symmetrel)
• Headache
- an antiviral drug that acts on the dopamine
receptors.
Adverse Reactions
- May be taken alone or in combination with
• Involuntary • Priapism
carbidopa-levodopa or an anticholinergic
movements • Psychosis drug.
• Palpitations • Severe depression - Initially, amantadine produces improvement
• Orthostatic with suicidal ideation in symptoms of parkinsonism in
hypotension • Hallucinations approximately two thirds of patients, but this
• Urinary retention improvement is usually not sustained,
because drug tolerance develops.
Contraindications: - Can also be used to treat drug induced
• Narrow-angle glaucoma parkinsonism.
• Severe cardiac, renal, hepatic disease
• Suspicious skin lesions (activates malignant Bromocriptine mesylate (Parlodel)
melanoma) - acts directly on dopamine receptors in the
central nervous system (CNS),
Nursing Responsibilities cardiovascular system, and gastrointestinal
• Monitor patient’s vital signs and tract.
electrocardiogram. Orthostatic hypotension may - More effective than amantadine and the
occur anticholinergics; however, it is not as
• during early use of levodopa and bromocriptine. effective as carbidopa-levodopa in alleviating
Instruct patient to rise slowly to avoid parkinsonism symptoms.
• faintness. - Patients who do not tolerate carbidopa-
• Observe for weakness, dizziness, or syncope, levodopa are frequently given bromocriptine
which are symptoms of orthostatic
• hypotension. Side Effects

NCM 106: PHARMACOLOGY
LECTURE
• Hypotension, lightheadedness, syncope,
nausea, fatigue, somnolence
Mao-B Inhibitors
- Monoamine oxidase-B
- Causes catabolism of dopamine
Selegiline
- Inhibits MAO-B, thus prolonging the action of
levodopa
- May be ordered for newly diagnosed patients
with parkinsonism
- Could delay carbidopa-levodopa therapy by
1 year
- Decreases “on-off” fluctuations
Rasagiline (Azilect)
- a MAO-B inhibitor used for the treatment of
parkinsonism
- Large doses of selegiline may inhibit MAO-A,
an enzyme that promotes metabolism of
tyramine in the GI tract. If they are not
metabolized by MAO-A, ingestion of foods
high in tyramine (aged cheese, red wine, and
bananas) can cause a hypertensive crisis.
- Severe adverse drug interactions can occur
between selegiline and various tricyclic
antidepressants (TCA) or selective serotonin
reuptake inhibitors (SSRIs).
COMT Inhibitors
- Catechol O-methyltransferase (COMT)
- Inactivates dopamine
- Increase the amount of levodopa
concentration in the brain when taken with a
- levodopa preparation
Tolcapone (Tasmar)
- First COMT inhibitor taken with levodopa for
advanced parkinsonism.
- May cause severe liver damage. Patients
with liver dysfunction should not take this
drug.
- The urine can be bright yellow
Entacapone (Comtan)
- not known to affect liver function.
- the urine can be dark yellow to orange
Adverse Reactions
• Both tolcapone and entacapone can intensify
the adverse reactions of levodopa (e.g.,
hallucinations, orthostatic hypotension,
constipation, dizziness) because these drugs
prolong the effect of levodopa.
Comparison of Drugs Used to Treat Parkinson’s
Disease
Anticholinergics; Antiparkinson
- First group of drugs used to treat Parkinson’s
disease before levodopa and dopamine
agonists were introduced.
- Useful in decreasing tremors related to
Parkinson’s disease.
- The major use of these agents currently is to
treat drug-induced parkinsonism.
- Treatment starts with low dosages, and then
dose is gradually increased.
- Older adults are more susceptible to the
many side effects of anticholinergics
- Patients with memory loss or dementia
should not be on anticholinergic therapy
Dopaminergics
- Carbidopa-levodopa
- Decreases symptoms of parkinsonism.
- Carbidopa, a decarboxylase inhibitor,
permits more levodopa to reach the striatum
nerve terminals (where levodopa is
converted to dopamine). With the use of
carbidopa, less levodopa is needed
Dopamine Agonist
Amantadine
- First used as an antiviral drug for influenza A
- Decreases symptoms of parkinsonism
- Can be used for early treatment of
Parkinson’s disease, which could delay the
necessity
- Is effective in treating drug-induced
parkinsonism, and has fewer side effects
than anticholinergics
Bromocriptine
- A D2-dopamine receptor agonist
- Can be used for early treatment of
Parkinson’s disease
- With increasing motor symptoms, can be
used for early treatment of Parkinson’s
disease. With increasing motor symptoms,
can be given levodopa therapy
Pramipexole
- D2- and D3-dopamine receptor agonists
- Can be used in combination with levodopa
- Fewer side effects than older dopamine
agonists
MAO-B Inhibitors
Selegiline HCl (Eldepryl)
- Inhibits catabolic enzymes of dopamine.
Extends action of dopamine.
- Can be used for early treatment of
Parkinson’s disease.
- If given with levodopa, dosage of levodopa is
usually decreased
Rasagline (Azilect)
- Inhibits breakdown of dopamine at synapses
in the brain.
NCM 106: PHARMACOLOGY
LECTURE
- Allows neurons to reabsorb more dopamine Alzheimer’s disease is galantamine
for use later (Razadyne).

COMT Inhibitors Side Effects

Entacapone (Comtan) • Anorexia • Dizziness
- Inhibits COMT enzyme, increasing • Nausea • Depression
concentration of levodopa. • Vomiting • Peripheral edema
- Used in combination with levodopa • Diarrhea • Dry mouth
carbidopa (Sinemet). • Constipation • Dehydration
- With COMT inhibitors, smaller dose of • Abdominal pain • Restless legs
levodopa is needed • Gastrointestinal syndrome
bleeding • Nystagmus
ALZHEIMER’S DISEASE
- It is an incurable dementia illness
characterized by chronic, progressive Adverse Reactions
neurodegenerative conditions with marked
• Seizures • Cataracts
cognitive dysfunction.
• Bradycardia • Myocardial
- Onset usually occurs between 45 and 65
years of age. • Orthostatic infarction
hypotension • Heart failure
Theories related to the changes that cause Alzheimer’s
disease
Contraindications
• Degeneration of the cholinergic neuron and
deficiency in acetylcholine • Liver and renal diseases
• Neuritic plaques that form mainly outside of • Urinary tract obstruction
the neurons and in the cerebral cortex. • Orthostatic hypotension
• Apolipoprotein E4 (apo E4) that promotes • Bradycardia
formation of neuritic plaques, which binds
betaamyloid in the plaques Nursing Responsibilities
• Beta-amyloid protein accumulation in high • Maintain consistency in care.
levels that may contribute to neuronal injury • Assist patient in ambulation and activity.
• Presence of neurofibrillary tangles with twists • Monitor for side effects related to continuous
inside the neurons use of AChE inhibitors.
• Record vital signs periodically. Note signs of
Histologic changes in Alzheimer’s disease bradycardia and hypotension.
A. Healthy neuron. • Observe patient’s behavioral changes, and
B. Neuron affected by Alzheimer’s disease record improvement or decline Patient
showing characteristic neuritic plaques and
cellular neurofibrillary tangles. Health Teachings
• Explain to patient and family the purpose for
• Factors thought to influence the occurrence of prescribed drug therapy.
Alzheimer’s disease are genetic predisposition, • Clarify time for drug dosing and schedule for
virus, infection, or inflammation that attacks brain increasing drug dosing to family member
cells, as well as nutritional, environmental, and • responsible for patient’s medications.
immunologic. • Teach family member about safety
techniques (e.g., removing obstacles from
Acetylcholinesterase Inhibitors/Cholinesterase patient’s path so that patient can avoid injury
Inhibitors when wandering).
- AChE is an enzyme responsible for breaking • Inform family member of available support
down ACh and is also known as groups such as the Alzheimer’s Disease and
cholinesterase • Related Disorders Association.
- tacrine (Cognex); donepezil (Aricept); and • Inform patient and family member that
rivastigmine (Exelon), drug that permits more patient should rise slowly to avoid dizziness
acetylcholine in the neuron receptors. and loss of balance.
- Rivastigmine has effective penetration into • Monitor routine liver function tests, as
the CNS; thus, cholinergic transmission is hepatotoxicity is an adverse effect.
increased. • Inform family member about foods that may
- These AChE inhibitors increase cognitive be prepared for patient’s consumption and
function for patients with mild to moderate tolerance
- Alzheimer’s disease. A reversible AChE
inhibitor used to treat mild to moderate MUSCLE RELAXANTS

NCM 106: PHARMACOLOGY
LECTURE
- Relieve muscular spasms and pain - (Adjunct to Anesthesia)
associated with traumatic injuries and - Used in surgery for relaxation of skeletal
spasticity from chronic debilitating disorders muscle
(e.g., MS, stroke [cerebrovascular accident],
cerebral palsy, head and spinal cord Side Effects:
injuries). • Anticholinergic • Headache
- Spasticity results from increased muscle effects (blurred • Fever
tone from hyperexcitable neurons caused by vision, constipation, • Abdominal pain
increased stimulation from the cerebral dry mouth, • Vomiting
neurons or lack of inhibition in the spinal cord tachycardia, urinary • Diarrhea
or at the skeletal muscles. retention) • Flatulence
- The centrally acting muscle relaxants • Drowsiness • Erectile dysfunction
depress neuron activity in the spinal cord or • Dizziness
brain or enhance neuronal inhibition on the
skeletal muscles. Adverse Reactions:
• Allergic reactions • Seizures
Centrally Acting Muscle Relaxants • Angioedema • Ileus
- The mechanism of action is not fully known. • Myocardial
- They are used in cases of spasticity to infarction
suppress hyperactive reflex and for muscle
spasms that do not respond to Contraindications:
antiinflammatory agents, physical therapy, or • Acute myocardial infarction
other forms of therapy.
• AV blocks, bundle-branch block
- cyclobenzaprine (Flexeril), carisoprodol
• Cardiac arrhythmias
(Soma), chlorzoxazone (Parafon forte DSC),
- methocarbamol (Robaxin), metaxalone • Heart failure
(Skelaxin) and orphenadrine citrate (Norflex). • Hyperthyroidism
• Paralytic ileus
Anxiolytics • Concurrent use of monoamine oxidase inhibitors
Diazepam (Valium) or within 14 days after discontinuation
- To relieve muscle spasms associated with
paraplegia and cerebral palsy Nursing Responsibilities
• Monitor serum liver enzyme levels of patients
Spasticity (Centrally Acting) taking dantrolene and carisoprodol.
- For muscle spasms caused by MS and • Report elevated levels of liver enzymes such as
spinal cord injury. Overdose may cause CNS alkaline phosphatase (ALP), alanine
depression. aminotransferase (ALT), and gamma-glutamyl
- Baclofen (Lioresal), Tizanidine (Zanaflex) transferase (GGT).
• Record vital signs. Report abnormal results.
Spasticity (Direct Acting) • Observe for CNS side effects (e.g., dizziness).
Dantrolene sodium (Dantrium)
- For chronic neurologic disorders causing Health Teaching
spasms: spinal cord injuries, stroke, MS • Teach patient that the muscle relaxant
should not be abruptly stopped. Drug should
Centrally Acting Muscle Relaxants be tapered over 1 week to avoid rebound
- For relaxation of skeletal muscles spasms.
• Advise patient not to drive or operate
carisoprodol (Soma) dangerous machinery when taking muscle
chlorzoxazone (Parafon forte DSC) relaxants. These drugs have a sedative
methocarbamol (Robaxin) effect and can cause drowsiness.
metaxalone (Skelaxin) • Inform patient that most of the centrally
orphenadrine citrate (Norflex) acting muscle relaxants for acute spasms
are usually taken for no longer than 3 weeks.
Depolarizing Muscle Relaxants • Teach patient to avoid alcohol and CNS
succinylcholine (Anectine) depressants. If muscle relaxants are taken
- (Adjunct to Anesthesia) with these drugs, CNS depression may be
- For surgical skeletal muscle relaxation. Also intensified.
used in endoscopy and intubation • Advise patient that these drugs must be used
cautiously for pregnant or nursing patients.
Nondepolarizing Muscle Relaxants Check with health care provider.
pancuronium bromide (Pavulon) • Encourage patient to report side effects of
vecuronium (Norcuron) the muscle relaxant: nausea, vomiting,

NCM 106: PHARMACOLOGY
LECTURE
dizziness, fainting, headache, and diplopia. Scheduled combination of
Dizziness and fainting are most likely caused nonopioid and opioid (oxycodone 5
by orthostatic (postural) hypotension. mg and acetaminophen 325 mg
• Advise patient to take muscle relaxants with q4h)
food to decrease gastrointestinal upset. o Severe pain:
Scheduled potent opioid (morphine
NONOPIOID AND OPIOID AGENTS 15 mg q4h)
• Pain is an unpleasant sensory and emotional
experience related to tissue injury. Due to the Chronic
subjective nature of pain, the nurse must be - Pain persists for greater than 6 months and
knowledgeable and skillful in the assessment and is difficult to treat or control
measurement of pain to achieve optimal pain - Drug treatment:
management. o Nonopioid drugs are suggested.
• Nociceptors (sensory pain receptors) are o Opioids, if used, should meet these
activated by noxious stimuli (mechanical, thermal, criteria:
and chemical) in peripheral tissues. When tissue § Oral or transdermal
damage occurs, injured cells release chemical § Long duration of action
mediators that affect the exposed nerve endings § Include adjunct therapy
of the nociceptors. Pain that originates from § Cause minimal respiratory
tissue injury is nociceptor pain, which includes depression
somatic (structural tissues: bones, muscles) and
visceral (organ) pain.
• Neuropathic pain is an unusual sensory
disturbance often involving neural Cancer
supersensitivity. This pain is due to injury or - Pain from pressure on nerves and organs,
disease of the peripheral or central nervous blockage to blood supply, or metastasis to
system (CNS). Patients with neuropathic pain bone
usually complains of burning, tingling, or electrical - Drug treatment:
shocks in the affected area, often triggered by o NSAIDs and opioid drugs
light touch. administered PO, transdermal, IM,
IV, or PCA
PATHOPHYSIOLOGY OF PAIN
According to the gate theory proposed by Melzack Somatic
and Wall in 1965, tissue injury activates nociceptors - Pain of skeletal muscle, ligaments, and joints
and causes the release of chemical mediators such - Drug treatment:
as substance P, prostaglandins, bradykinin, o Nonopioids: NSAIDs; also act as
histamine, serotonin, acetylcholine, glutamate, anti-inflammatories and muscle
adenosine triphosphate, leukotrienes, and potassium. relaxants
These substances initiate an action potential along a
sensory nerve fiber and sensitize pain receptors. Superficial
Nociceptive action potentials are transmitted via - Pain from surface areas such as skin and
afferent nerve fibers. One type of pain fiber that mucous membranes
primarily transmits impulses from the periphery is the - Drug treatment:
A delta (δ) fiber. Because A δ pain fibers are wrapped o Mild pain: Nonopioid
in a myelin sheath, they transmit impulses rapidly in o Moderate pain: Combination of
acute pain. The C fiber is a type of pain fiber that is opioid and nonopioid analgesic drug
small and unmyelinated, and because C fibers are
unmyelinated, they transmit impulses slowly. C fibers Vascular
are more often associated with chronic, dull pain. - Pain from vascular or perivascular tissues
contributing to headaches or migraines
TYPES OF PAIN AND ITS DRUG TREATMENT - Drug treatment:
o Nonopioid drugs
Acute
- Pain occurs suddenly and responds to Visceral
treatment; can result from trauma, tissue - Pain from smooth muscle and organs
injury, inflammation, or surgery - Drug treatment:
- Drug treatment: o Opioid drugs
o Mild pain:
Scheduled nonopioid NONOPIOID ANALGESICS
(acetaminophen, NSAIDs q6h) • Nonopioid analgesics (aspirin,
o Moderate pain: acetaminophen, ibuprofen, naproxen) are
less potent than opioid analgesics.

NCM 106: PHARMACOLOGY
LECTURE
• They are used to treat mild to moderate pain.
• They are usually purchased over-the-counter
(OTC), but COX-2 inhibitors require a
prescription.
• Nonopioids are effective for the dull,
throbbing pain of headaches, dysmenorrhea
(menstrual pain), inflammation, minor
abrasions, muscular aches and pain, and
mild to moderate arthritis.
• Most analgesics also have an antipyretic
effect and will lower an elevated body
temperature.
• Some, such as aspirin, have anti-
inflammatory and antiplatelet effects as well.
Nonsteroidal Anti-inflammatory Drugs
- All NSAIDs have an analgesic effect as well
as an antipyretic and anti-inflammatory
action.
- NSAIDs such as aspirin (ASA), ibuprofen
(Motrin, Advil), and naproxen (Aleve) can be
purchased as OTC drugs.
- Aspirin, a salicylate NSAID, is the oldest
nonopioid analgesic drug still in use. In
addition to its analgesic, antipyretic, and
antiinflammatory properties, aspirin
decreases platelet aggregation (clotting).
- Aspirin and other NSAIDs relieve pain by
inhibiting biosynthesis of prostaglandin by
different forms of the enzyme
cyclooxygenase (COX).
- Inhibition of COX-2 decreases inflammation
and pain, but inhibition of COX-1 decreases
protection of the stomach lining.
There are seven groups of NSAIDs:
1. Salicylates
2. Para-chlorobenzoic acid derivatives, or
indoles
3. Phenylacetic acids
4. Propionic acid derivatives
5. Fenamates
6. Oxicams
7. Selective COX-2 inhibitors
Salicylates
Aspirin
- comes from the family of salicylates derived
from salicylic acid.
- also called acetylsalicylic acid (ASA) after
the acetyl group used in the composition of
aspirin.
- a prostaglandin inhibitor that decreases the
inflammatory process.
- It is also considered an antiplatelet drug for
patients with cardiac or cerebrovascular
disorders; aspirin decreases platelet
aggregation, and thus blood clotting is
decreased.
- should not be taken with other NSAIDs
because it decreases the blood level and
effectiveness of NSAIDs.
- Others: Aspirin (ASA, Bayer, Ecotrin),
diflunisal (Dolobid), olsalazine sodium
(Dipentum), and sulfasalazine (Azulfidine)
Side Effects
• Anorexia • Hearing loss
• Nausea • Heartburn
• Vomiting • Rash
• Diarrhea • Abdominal
• Dizziness pain
• Confusion • Drowsiness
Adverse Reactions
• Tinnitus • Ulceration
• Urticaria • GI bleeding
Contraindications
• Hypersensitivity to salicylates or NSAIDs
• Flu or virus symptoms in children
• Anticoagulant therapy
• GI bleeding
• Bone marrow suppression
• Third trimester of pregnancy
Nursing Responsibilities
• Monitor serum salicylate (aspirin) level when
patient takes high doses of aspirin for chronic
conditions such as arthritis. Normal therapeutic
range is 15 to 30 mg/ dL. Mild toxicity occurs at
serum level of >30 mg/dL, and severe toxicity
occurs at >50 mg/dL.
• Observe patient for signs of bleeding such as
dark (tarry) stools, bleeding gums, petechiae
(round red spots), ecchymosis (excessive
bruising), and purpura (large red spots) when
patient takes high doses of aspirin.
Health Teachings
• Advise patient not to take aspirin with alcohol or
with drugs that are highly protein-bound, such as
the anticoagulant warfarin (Coumadin). Aspirin
displaces drugs like warfarin from the protein-
binding site, causing increased anticoagulant
levels.
• Suggest that patient inform the dentist before a
dental visit if taking high doses of aspirin.
• Instruct patient to discontinue aspirin 3 to 7 days
before surgery to reduce risk of bleeding (with the
health care provider’s approval).
• Keep aspirin bottle out of reach of children.
• Educate parent to call poison control center
immediately if a child has taken a large or
unknown amount of aspirin (or acetaminophen).
• Warn patient not to administer aspirin for virus or
flu symptoms in children. Reye’s syndrome
(vomiting, lethargy, delirium, and coma) has been
linked with aspirin and viral infections.
Acetaminophen is usually prescribed for cold and
flu symptoms.
NCM 106: PHARMACOLOGY
LECTURE
• Inform patient that aspirin tablets can cause GI • Nausea • Dizziness
distress. • Vomiting • Lightheadedness
• Inform patient with dysmenorrhea to take • Diarrhea • Anxiety
acetaminophen instead of aspirin 2 days before • Edema • Confusion
and during the first 2 days of the menstrual • Rash • Fluid retention with
period. • Purpura edema
• Direct patient to report side effects such as • Tinnitus
drowsiness, tinnitus (ringing in the ears),
headaches, flushing, dizziness, GI symptoms Adverse Reactions
(bleeding, heartburn), visual changes, and • GI bleeding
seizures.
• Instruct patient to take aspirin (also ibuprofen) Contraindications
with food, at mealtime, or with plenty of fluids. EC • Severe renal or hepatic disease
aspirin helps prevent GI disturbance. • Asthma
• Peptic ulcer
• Anticoagulant therapy
Para-chlorobenzoic Acid
- This group may cause sodium and water
Fenamates
retention and increased blood pressure.
- Includes potent NSAIDs used for acute and
chronic arthritic conditions.
Indomethacin (Indocin)
- Like most NSAIDs, gastric irritation is a
• One of the first NSAIDs introduced common side effect of fenamates, and
• a para-chlorobenzoic acid patients
• It is used for rheumatoid arthritis, gouty arthritis, - with a history of peptic ulcer should avoid
and osteoarthritis and is a potent prostaglandin taking this group of drugs.
inhibitor. - Other side effects include edema, dizziness,
tinnitus, and pruritus.
• Two other para-chlorobenzoic acid - Example: meclofenamate sodium
derivatives: sulindac (Clinoril) and tolmetin monohydrate (Meclomen) and mefenamic
(Tolectin) produce less severe adverse acid (Ponstel)
reactions than indomethacin.
Oxicams
Phenylacetic Acid Derivatives Piroxicam (Feldene)
Diclofenac sodium (Voltaren-XR) - indicated for long-term arthritic conditions
• a phenylacetic acid derivative. such as rheumatoid arthritis and
• Its analgesic and antiinflammatory effects are osteoarthritis.
similar to those of aspirin, but it has minimal to no - It too can cause gastric problems such as
antipyretic effects. ulceration and epigastric distress, but the
• It is indicated for rheumatoid arthritis, incidence is lower than for some other
osteoarthritis, and ankylosing spondylitis. NSAIDs.
- It is well tolerated, and its major advantage
• Others: diclofenac sodium (Voltaren XR), over other NSAIDs is its long half-life, which
etodolac (Lodine) and ketorolac tromethamine allows it to be taken only once daily.
(Toradol)
• Others: Meloxicam (Mobic)
Propionic Acid Derivatives
- They are relatively new group of NSAIDs. Selective Cox-2 Inhibitors (Second-Generation
- These drugs are aspirin-like but have NSAIDs)
stronger effects and create less GI irritation. - Became available in the last several years to
decrease inflammation and pain.
Ibuprofen (Motrin) - Most NSAIDs are nonselective inhibitors that
- most widely used propionic acid NSAID and inhibit COX-1 and COX-2.
may be purchased OTC in lower doses (200 - By inhibiting COX-1, protection of the
mg) stomach lining is decreased and clotting time
is also decreased, which may benefit the
• Others: fenoprofen calcium (Nalfon), naproxen patient with cardiovascular or coronary artery
(Naprosyn), ketoprofen (Orudis), flurbiprofen disease (CAD).
(Ansaid), and oxaprozin (Daypro). - Selective COX-2 inhibitors are drugs of
choice for patients with severe arthritic
Side Effects conditions who need high doses of an anti-
• Anorexia • Fatigue inflammatory drug, because large doses of

NCM 106: PHARMACOLOGY
LECTURE
NSAIDs may cause peptic ulcer and gastric
bleeding.
- Example: celecoxib (Celebrex)
Nursing Responsibilities: NSAIDs
• Observe patient for bleeding gums, petechiae,
ecchy moses, or black (tarry) stools.
• Bleeding time can be prolonged when NSAIDs
are taken, especially with a highly protein-bound
drug such as warfarin (anticoagulant).
• Report if patient has GI discomfort. Administer
NSAIDs at mealtime or with food to prevent GI
upset.
• Monitor vital signs and check for peripheral
edema, especially in the morning.
• Do not give directions such as “take one blue pill”
at a specified time. Instead, provide name and
dosage of medication.
Health Teaching
• Inform patient not to take aspirin and
acetaminophen with NSAIDs. Taking an NSAID
with aspirin could cause GI upset and possible GI
bleeding.
• Inform patient to avoid alcohol when taking
NSAIDs. GI upset or gastric ulcer may result.
• Alert patient that many herbal products may
interact with NSAIDs and could cause bleeding.
Doses of NSAIDs and/or herbs may need to be
modified to avoid possible bleeding occurrence.
• Direct patient to inform the dentist or surgeon
before a procedure when taking ibuprofen or
other NSAIDs for a continuous period.
• Warn female patients not to take NSAIDs 1 to 2
days before menstruation to avoid heavy
menstrual flow. If discomfort occurs,
acetaminophen is usually prescribed.
• Advise pregnant patients to avoid NSAIDs.
Congenital abnormalities may occur when
NSAIDS are taken during early pregnancy, and
excess bleeding might occur during delivery.
• Inform patient that it may take several weeks to
experience desired drug effect of some NSAIDs
and disease modifying antirheumatic drugs
(DMARDs).
• Educate patient of the common side effects of
NSAIDs. Nausea, vomiting, peripheral edema, GI
upset, purpura or petechiae, or dizziness might
occur. Report occurrences of side effects.
• Advise patient to take NSAIDs with meals or
snacks to reduce GI upset.
Acetaminophen
- analgesic (paraaminophenol derivative)
- a popular nonprescription drug for the relief
of pain, discomfort, and fever in infants,
children, adults, and older adults.
- It is a nonopioid drug, but it is not an NSAID.
- It does not have the antiinflammatory
properties of aspirin, so it is not the drug of
choice for any inflammatory process.
- It constitutes 25% of all OTC drugs sold
- Examples of OTC products that contain
acetaminophen include Anacin; Excedrin;
Midol: Maximum Strength Menstrual
Formula; and Vicks: Cold & Flu Relief.
Acetaminophen (Tylenol)
- an analgesic and antipyretic drug used for
muscular aches and pains and for fever
caused by viral infections.
- It is a safe, effective drug when used at
therapeutic doses.
- Causes little to no gastric distress and does
not interfere with platelet aggregation.
- An IV formulation was FDA approved in 2010
for treating pain and fever.
- There is no link between acetaminophen and
Reye’s syndrome, and it does not increase
the potential for excessive bleeding if taken
for dysmenorrhea, as do aspirin and
NSAIDs.
Side Effects
• Anorexia • Rash
• Nausea • Insomnia
• Vomiting
Adverse Reactions
• Oliguria
• Urticaria
• Elevated liver enzymes
Contraindications
• Acetaminophen hypersensitivity
• Severe hepatic or renal disease
• Alcoholism
Nursing Responsibilities
• Check liver enzyme tests such as alanine
aminotransferase, alkaline phosphatase, gamma-
glutamyl transferase, 5′ nucleotidase, and
bilirubin for elevations in patients taking high
doses or overdoses of acetaminophen.
Health Teachings
• Teach patient to keep acetaminophen out of
children’s reach. Acetaminophen for children is
available in flavored tablets and liquid. High
doses can cause hepatotoxicity.
• Advise patient not to self-medicate with
acetaminophen longer than 10 days.
• Teach adult caregiver not to medicate child
longer than 5 days without health care provider’s
approval.
• Direct parent to call poison control center
immediately if a child has taken a large or
unknown amount of acetaminophen.
• Teach patient to check acetaminophen dosage
on package label of OTC drugs.
• Do not exceed the recommended dosage.
Suggested safe adult acetaminophen dose is
NCM 106: PHARMACOLOGY
LECTURE
2000 mg/d (2 g/day), not to exceed 4 g/day to
avoid liver damage
• Encourage patient to report side effects.
Overdosing can cause severe liver damage and
death.
• Inform patient that liver damage may occur with
excess use of acetaminophen.
• Check serum acetaminophen level if toxicity is
suspected. Normal serum level is 5 to 20
mcg/mL; toxic level is >50 mcg/mL. Levels of
>200 mcg/mL could indicate hepatotoxicity.
• The antidote for acetaminophen is acetylcysteine
(Mucomyst). Dosage is based on serum
acetaminophen level.
OPIOID ANALGESICS
- Also called opioid agonists.
- Are prescribed for moderate and severe pain
Morphine
- prototype opioid
- obtained from the sap of seed pods of the
opium poppy plant
Codeine
- Another drug obtained from opium.
- They act mostly on the CNS.
- They act primarily by activating the µ
receptors, while also exerting a weak
activation of the kappa (κ) receptors.
- Analgesia, respiratory depression, euphoria,
and sedation are effects of µ activation.
Activation of κ receptors leads to analgesia
and sedation, having no effect on respiratory
depression and euphoria.
- They not only suppress pain impulses but
also respiration and coughing by acting on
the respiratory and cough centers in the
medulla of the brainstem.
- Codeine is not as potent as morphine (1/15
to 1/20 as potent), but it also relieves mild to
moderate pain and suppresses cough, which
allows it also to be classified as an
antitussive.
• Most opioids, with the exception of meperidine
(Demerol), have an antitussive (cough
suppression) effect.
• Hydromorphone (Dilaudid) is a semisynthetic
opioid similar to morphine.
Side Effects
• Anorexia • Urinary retention
• Nausea • Rash
• Vomiting • Blurred vision
• Constipation • Bradycardia
• Drowsiness • Flushing
• Dizziness • Euphoria
• Sedation • Pruritus
• Confusion
Adverse Reactions
• Hypotension, Urticaria, Seizures, Ileus
Contraindication
• Hypersensitivity
• CNS or respiratory depression
• tatus asthmaticus
• Increased intracranial pressure
• Shock
• Alcoholism
• Ileus
• Hypovolemia
Nursing Responsibilities
• Administer morphine before pain reaches its peak
to maximize effectiveness of the drug.
• Monitor vital signs at frequent intervals to detect
respiratory changes. Respirations of < 10/ min
can indicate respiratory distress.
• Record patient’s urine output because urinary
retention is a side effect of morphine. Urine
output should be at least 600 mL/day.
• Check bowel sounds for decreased peristalsis;
constipation is a side effect of morphine.
• Dietary change or mild laxative might be needed.
• Check for pupil changes and reaction. Pinpoint
pupils can indicate morphine overdose.
• Have naloxone (Narcan) available as an antidote
to reverse respiratory depression if morphine
overdose occurs.
• Validate dose of morphine before its
administration. Check older adults for alertness
and orientation because confusion is a side effect
of morphine. Use side rails, and take other safety
precautions as necessary.
Health Teaching
• Encourage patient not to use alcohol or CNS
depressants with any opioid analgesics such
as morphine. Respiratory depression can
result.
• Suggest nonpharmacologic measures to
relieve pain as patient recuperates from
surgery. As recovery progresses, a
nonopioid analgesic may be prescribed.
• Alert patient that with continuous use,
opioids such as morphine can become
addicting. If addiction occurs, inform patient
about methadone treatment programs and
other resources in the area.
• Encourage patient to report dizziness while
taking morphine. Dizziness could be due to
orthostatic hypotension. Advise patient to
ambulate with caution or only with
assistance.
• Teach patient to report difficulty in breathing,
blurred vision, and headaches.
OPIOID AGONIST-ANTAGONISTS
- They are medications in which an opioid
antagonist (e.g., naloxone [Narcan]) is added
NCM 106: PHARMACOLOGY
LECTURE
to an opioid agonist, were developed in depression are adverse reactions that might
hopes of decreasing opioid abuse. occur.

Pentazocine (Talwin) OPIOID ANTAGONISTS

- the first opioid analgesic - Antidotes for overdoses of natural and
- can be given orally (tablet) and by injection synthetic opioid analgesics.
(subQ, IM, and IV). - They have a higher affinity to the opiate
receptor site than the opioid being taken.
Butorphanol tartrate (Stadol), buprenorphine - They block the receptor and displaces any
(Buprenex), nalbuphine hydrochlorid (Nubain) opioid that would normally be at the receptor,
- These drugs are not given for cancer pain, - inhibiting the opioid action.
because of the risk of potential CNS toxicity - They are indicated for reversal of
from the high doses required. postoperative opioid depression and opioid
- These analgesics are considered safe for overdose.
use during labor, but their safety during early
pregnancy has not been established. • Examples: Naloxone (Narcan), administered IM
or IV; naltrexone hydrochloride (ReVia),
Side Effects administered orally by tablet or liquid; nalmefene
• Dizziness • Crying - These drugs are perfect examples of
• Confusion • Dysphoria pharmacologic antagonists because they
• Hallucinations • Unusual dreams reverse the respiratory and CNS depression
• Blurred vision • Dry mouth (sedation and hypotension) caused by
• Headache • Bitter taste opioids
• Flushing • Nausea
• Sedation • Vomiting HEADACHES: MIGRAINE AND CLUSTER
• Nervousness • Abdominal cramps - It is characterized by a unilateral throbbing
head pain accompanied by nausea,
• Restlessness • Clammy skin
vomiting, and photophobia which frequently
• Euphoria • Urinary urgency
persist for 4 to 24 hours and for several days
• Depression in some cases.
- Symptoms usually decrease or are absent
Adverse Reactions during pregnancy and menopause.
• Bradycardia • Hypertension - The intensity of migraine pain can disrupt
• Tachycardia • Dyspnea daily activities.
• Hypotension
PATHOPHYSIOLOGY
Contraindications Migraine headaches are caused by inflammation and
• Hypersensitivity dilation of the blood vessels in the cranium. The
etiology is unknown, but some theories suggest an
Nursing Responsibilities imbalance in the neurotransmitter serotonin (5-
• Monitor vital signs. Note any changes in hydroxytryptamine [5-HT]) that causes
respirations. vasoconstriction and suppresses migraine
• Check bowel sounds and date of last bowel headaches. The tendency of calcitonin gene-related
movement to identify constipation. peptide (CGRP) is to promote a migraine attack.
• Decreased peristalsis may result in constipation. PREVENTIVE TREATMENT FOR MIGRAINES
A mild laxative may be necessary. • Beta-adrenergic blockers:
• Determine urine output. Report if urine output is o propranolol (Inderal)
<30 ml/hr or <600 ml/day. o atenolol (Tenormin)
• Administer IV nalbuphine undiluted. Do not mix • Anticonvulsants:
with barbiturates. o valproic acid (Depakote)
o gabapentin (Neurontin)
Health Teaching • Tricyclic antidepressants:
• Warn patient not to use alcohol or CNS o amitriptyline (Elavil)
depressants while taking nalbuphine. o imipramine (Tofranil)
Respiratory depression can occur.
• Suggest nonpharmacologic methods for Antimigraine Medication
lessening pain like changing position or - It should be taken early during a migraine
ambulation. attack.
• Advise patient to report side effects of - The triptans (5-HT1 receptor agonists) are
nalbuphine: dizziness, headaches, the most recently developed group of drugs
constipation, dysuria,rash, or blurred vision. for the treatment of migraine headaches.
Hallucinations, tachycardia, and respiratory

NCM 106: PHARMACOLOGY
LECTURE
Sumatriptan (Imitrex) 3. The ascending reticular activating
- A selective serotonin receptor agonist with a system is altered, and the neurons
short duration of action, was the first triptan cease to transmit information (stimuli) to
drug. the brain.
- It is considered more effective than ergot
alkaloids in treating acute migraine attacks. Stages of Anesthesia
- Mode of Action: Causes vasoconstriction of
cranial arteries to relieve migraine attacks Stage 1 (Analgesia)
- This stage may be called the induction stage
Side Effects - Begins with consciousness and ends with
• Dizziness • Muscle cramps loss of consciousness.
• Fainting • Nausea - Speech is difficult; sensations of smell and
• Tingling • Vomiting pain are lost.
• Numbness • Dry mouth - Dreams and auditory and visual
• Warm sensation • Diarrhea hallucinations may occur.
• Drowsiness • Abdominal
cramping Stage 2 (Excitement or Delirium)
- Produces a loss of consciousness caused by
Adverse Reactions depression of the cerebral cortex.
• Hypotension • Thromboembolism - Confusion, excitement, or delirium occur.
- Short induction time.
• Hypertension • Seizures
• Heart block • Central nervous
Stage 3 (Surgical)
• Angina system
- Surgical procedure is performed during this
• Dysrhythmias hemorrhage
stage
• Stroke - There are four phases
- The surgery is usually performed in phase 2
Contraindications and upper phase 3
• Hypersensitivity • Diabetes mellitus - As anesthesia deepens, respirations become
• Coronary artery • Smoking more shallow and respiratory rate is
disease • Hepatic disease increased
• Peripheral vascular • Cerebrovascular
disease disease Stage 4 (Medullary Paralysis)
• Hypertension • Older adults - Toxic stage of anesthesia
• Obesity - Respirations are lost, and circulatory
collapse occurs
- Ventilatory assistance is necessary
ANESTHETICS
- Classified as general and local Inhalation Anesthetics
- General anesthetics depress the CNS, - During the third stage of anesthesia,
alleviate pain, cause a loss of consciousness inhalation anesthetics (i.e., gas or volatile
liquids administered as gas) are used to
Nitrous oxide (“laughing gas”) deliver general anesthesia.
- first anesthetic, was used for surgery in the - Certain gases, notably nitrous oxide, are
early 1800s absorbed quickly, have a rapid action, and
- It is still an effective anesthetic and is are eliminated rapidly.
frequently used in dental procedures and - Inhalation anesthetics typically provide
surgery smooth induction. Upon discontinuing
administration of halothane, isoflurane, and
Pathophysiology enflurane, recovery of consciousness usually
- Several theories exist regarding how occurs in approximately 1 hour. Recovery
inhalation anesthetics cause CNS from desflurane and sevoflurane is within
depression and a loss of consciousness. minutes.
1. The lipid structure of cell membranes is - Inhalation anesthetics are usually combined
altered, resulting in impaired physiologic with a barbiturate (e.g., thiopental), a strong
functions. analgesic (e.g., morphine), and a muscle
2. The inhibitory neurotransmitter gamma- relaxant (e.g., pancuronium) for surgical
aminobutyric acid (GABA)is activated to procedures.
the GABA receptor that pushes chloride
ions into the neurons. This greatly • Adverse effects: respiratory depression,
decreases the fire action potentials of hypotension, dysrhythmias, and hepatic
the neurons.

NCM 106: PHARMACOLOGY
LECTURE
dysfunction. In patients at risk, these drugs may
trigger malignant hyperthermia
Intravenous Anesthetics
- IV anesthetics may be used for general
anesthesia or for the induction stage of
anesthesia.
- For outpatient surgery of short duration, an
intravenous anesthetic might be the
preferred form of anesthesia
thiopental sodium (Pentothal)
- an ultrashort-acting barbiturate
- was the general anesthetic used for short-
term surgery
- used for the rapid induction stage of
anesthesia and in dental procedures
droperidol (Innovar), etomidate (Amidate), and
ketamine hydrochloride (Ketalar)
- also used intravenously as general
anesthetics
Midazolam (Versed) and propofol (Diprivan)
- are commonly administered for the induction
and maintenance of anesthesia or conscious
sedation for minor surgery or procedures like
mechanical ventilation or intubation.
- Patients are sedated and relaxed but
responsive to commands.
Adverse effects from IV anesthetics
• respiratory and cardiovascular depression
Topical Anesthetics
- Use of topical anesthetic agents is limited to
mucous membranes, broken or unbroken
skin surfaces, and burns.
- Topical anesthetics come in different forms:
solution, liquid spray, ointment, cream, gel,
and powder.
- Topical anesthetics decrease the sensitivity
of nerve endings in the affected area.
Local Anesthetics
- Local anesthetics block pain at the site
where the drug is administered, allowing
consciousness to be maintained.
- Local anesthetics are useful in dental
procedures, suturing skin lacerations, short-
term (minor) surgery at a localized area,
blocking nerve impulses (nerve block) below
the insertion of a spinal anesthetic, and
diagnostic procedures such as lumbar
puncture and thoracentesis.
Procaine hydrochloride (Novocain)
- a synthetic of cocaine, was discovered in the
early 1900s.
Lidocaine hydrochloride (Xylocaine)
- a rapid onset and a long duration of action, is
more stable in solution, and causes fewer
hypersensitivity reactions than procaine.
Bupivacaine (Marcaine)
- delivered via a Y-connector to both sides at a
flow rate of approximately 2 mL/h. By
controlling pain with this delivery method, the
patient is allowed increased mobility,
reduced opioid use (which reduces
associated drowsiness and nausea), and
reduced hospital stay.
Spinal Anesthesia
- Spinal anesthesia requires that a local
anesthetic be injected in the subarachnoid
space at the third or fourth lumbar space.
- If the local anesthetic is given too high in the
spinal column, the respiratory muscles could
be affected, and respiratory distress or
failure could result.
- Headaches might result following spinal
anesthesia (a “spinal”), possibly because of
a decrease cerebrospinal fluid pressure
caused by a leak of fluid at the needle
insertion point.
- Encouraging the patient to remain flat
following surgery with spinal anesthesia and
to take increased fluids usually decreases
the likelihood of leaking spinal fluid.
- Hypotension also can result following spinal
anesthesia due to predisposing factors
including sensory block location, history of
hypertension, and chronic alcohol intake.
• Spinal block is the penetration of the anesthetic
into the subarachnoid membrane, the second
layer of the spinal cord.
• Epidural block is the placement of the local
anesthetic in the outer covering of the spinal
cord, or the dura mater.
• Caudal block is placed near the sacrum.
• Saddle block is given at the lower end of the
spinal column to block the perineal area.
Nursing Interventions
• Monitor patient’s postoperative state of
sensorium. Report if patient remains excessively
nonresponsive or confused.
• Observe preoperative and postoperative urine
output. Report deficit of hourly or 8-hour urine
output.
• Monitor vital signs following general and local
anesthesia; hypotension and respiratory
depression may result.
• Administer an analgesic or a narcotic-analgesic
with caution until patient fully recovers from
anesthetic. To prevent adverse reactions, dosage
might need to be adjusted if patient is under the
influence of anesthetic.
NCM 106: PHARMACOLOGY
LECTURE
• Explain to patient the preoperative preparation
and postoperative nursing assessment and
interventions.
ADRENERGIC AGONISTS AND ADRENERGIC
BLOCKERS
Adrenergic Agonists
- Drugs that stimulate the sympathetic nervous
system are called adrenergics, adrenergic
agonists, or sympathomimetics, because
they mimic the sympathetic
neurotransmitters norepinephrine and
epinephrine.
- They act on one or more adrenergic receptor
sites located in the effector cells of muscles,
such as the heart, bronchiole walls,
gastrointestinal (GI) tract, urinary bladder,
and ciliary
Effects of Adrenergic Agonist and Receptors
Alpha1 Increases force of heart contraction;
vasoconstriction increases blood
pressure; mydriasis (dilation of pupils)
occurs; decreases secretion in salivary
glands; increases urinary bladder
relaxation and urinary sphincter
contraction
Alpha2 Inhibits release of norepinephrine; dilates
blood vessels; produces hypotension;
decreases gastrointestinal motility and
tone
Beta1 Increases heart rate and force of
contraction; increases renin secretion,
which increases blood pressure
Beta2 Dilates bronchioles; promotes
gastrointestinal and uterine relaxation;
promotes increase
in blood sugar through glycogenolysis in
liver; increases blood flow in skeletal
muscles
Classification of Sympathomimetics
The sympathomimetic drugs that stimulate adrenergic
receptors are classified into three categories
according to their effects on organ cells.
1. Direct-acting Sympathomimetics
- directly stimulate the adrenergic receptor
(e.g. epinephrine or norepinephrine).
2. Indirect Acting Sympathomimetics
- stimulate the release of norepinephrine
from the terminal nerve endings
(e.g. amphetamine)
3. Mixed-acting Sympathomimetics
- both direct and indirect acting
- stimulate the adrenergic receptor sites and
stimulate the release of norepinephrine from
the terminal nerve endings
(e.g., ephedrine)
Epinephrine
- It is frequently used in emergencies to treat
anaphylaxis, which is a life-threatening
allergic response.
- Epinephrine is a potent inotropic
(strengthens myocardial contraction) drug
that increases cardiac output, promotes
vasoconstriction and systolic blood pressure
elevation, increases heart rate, and produces
bronchodilation.
- High doses can result in cardiac
dysrhythmias necessitating
electrocardiogram (ECG) monitoring
- Epinephrine can also cause renal
vasoconstriction, thereby decreasing renal
perfusion and urinary output.
Albuterol
Albuterol sulfate (Proventil)
- a beta2-adrenergic agonist, is selective for
beta2-adrenergic receptors, so the response
is relaxation of bronchial smooth muscle and
bronchodilation.
Central-Acting Alpha Agonists
Clonidine and Methyldopa Clonidine (Catapres)
- a selective alpha2-adrenergic agonist
(sympathomimetic)
- used primarily to treat hypertension.
- Alpha2 drugs act by decreasing the release
of norepinephrine from sympathetic nerves
and decreasing peripheral adrenergic
receptor activation.
- Alpha2 drugs also produce vasodilation by
stimulating alpha2 receptors in the central
nervous system (CNS), leading to a
decrease in blood pressure.
Nursing Responsibilities: Adrenergic Agonist
• Administer epinephrine 1 mg (10 mL of a 1
:10,000 concentration per AHA guidelines) IV for
cardiac resuscitation; may repeat q3-5 min.
Follow each dose with 20-mL saline flush to
ensure proper delivery. Normally, epinephrine is
administered 1 mg IV over 1 minute or more;
however, in cardiac arrest, it may be given more
rapidly.
• Monitor IV site frequently when administering
norepinephrine bitartrate (Levarterenol) or
dopamine (Intropin) because extravasation of
these drugs causes tissue necrosis. These drugs
should be diluted sufficiently in IV fluids.
• Administer antidote, phentolamine mesylate
(Regitine) 5 to 10 mg, diluted in 10 to 15 mL of
saline infiltrated into the area for IV extravasation
of norepinephrine (Levophed) and dopamine.
• Record patient’s vital signs. Report signs of
increasing blood pressure and increasing heart
rate. If patient receives an alpha-adrenergic
agonist intravenously for shock, check the blood
pressure q3-5min or as indicated to avoid severe
hypertension.
• Monitor ECG for dysrhythmias when given IV.
NCM 106: PHARMACOLOGY
LECTURE
• Report side effects of adrenergic drugs:
tachycardia, palpitations, tremors, dizziness, and
increased blood pressure.
• Check patient’s urinary output, and assess for
bladder distention. Urinary retention can result
from high drug dose or continuous use of
adrenergic agonists.
• Offer food to patient when giving adrenergic
agonists to avoid nausea and vomiting.
• Evaluate blood glucose levels in patients with
diabetes mellitus because they may be
increased.
Health Teachings:
• Advise patient to read labels on all over-the-
counter (OTC) drugs for cold symptoms and diet
pills. Many of these have properties of
sympathetic (adrenergic agonists,
sympathomimetics) drugs and should not be
taken if patient is hypertensive or has diabetes
mellitus, cardiac dysrhythmias, or coronary artery
disease.
• Explain to patient that continuous use of nasal
sprays or drops that contain adrenergic agonists
may result in rebound (inflamed and congested
tissue) nasal congestion.
• Encourage patient to report side effects (e.g.,
rapid heart rate, palpitations, rash, itching,
flushing, chest pain, irregular heartbeat, vomiting,
numbness of fingers and toes) to a health care
provider as dose may require adjustment.
Self-Administration
• Encourage patient to take medication as
prescribed.
• Advise patient and family on proper
administration of drug and allow return
demonstration. Cold medications by spray or
drops in the nostrils should be used with the head
in an upright position. Use of nasal spray while
lying down can cause systemic absorption.
Coloration of nasal spray or drops might indicate
deterioration.
• Notify health care provider if EpiPen is needed
more than twice a week.
• Encourage patient to have EpiPen readily
available at all times and to store additional
medication in a cool, dark place (refrigeration is
not recommended).
• Teach patient and family that EpiPen must be
taken immediately upon the initial occurrence of
difficulty breathing, wheezing, hoarseness, hives,
itching, or swelling of lips and tongue.
• Teach patient to administer EpiPen properly.
Inspect solution for particles or discoloration prior
to administration. Do not use if particles are pink
to brown in color.
• Take care to inject subcutaneously and not
intradermally, and to apply sufficient pressure to
activate EpiPen while holding device in place for
5 to 10 seconds.
• The EpiPen should be inserted into outer thigh.
After administration, massage injection site for 10
seconds to promote absorption and reduce
vasoconstriction and tissue irritation.
Adrenergic Blockers (Antagonists)
- Drugs that block the effects of adrenergic
neurotransmitters are called adrenergic
blockers, adrenergic antagonists, or
sympatholytics.
- They act as antagonists to adrenergic
agonists by blocking the alpha and beta
receptor sites.
- Most adrenergic blockers block either the
alpha receptor or the beta receptor.
- They block the effects of the
neurotransmitter either directly by occupying
the receptors or indirectly by inhibiting the
release of the neurotransmitters
norepinephrine and epinephrine.
Alpha-Adrenergic Blockers
- Drugs that block or inhibit a response at the
alpha-adrenergic receptor site are called
alpha-adrenergic blockers or alpha blockers
- Alpha-blocking agents are divided into two
groups:
• selective alpha blockers block alpha1
• nonselective alpha blockers block alpha1
and alpha2
Beta-Adrenergic Blockers
- Beta-adrenergic blockers, commonly called
beta blockers, decrease heart rate, and a
decrease in blood pressure usually follows.
- Some beta blockers are nonselective,
blocking both beta1 and beta2 receptors.
Adrenergic Neuron Blockers
- Drugs that block the release of
norepinephrine from the sympathetic
terminal neurons
- Classified as a subdivision of the adrenergic
blockers.
Nursing Responsibilities: Adrenergic Neuron Blockers
• Monitor patient’s vital signs. Report marked
changes such as marked decrease in blood
pressure and heart rate.
• Report any complaints of excessive dizziness,
lightheadedness, early morning insomnia, mental
depression, or chest pain.
• Assist patient with ambulation to avoid falls from
orthostatic hypotension, which is more common
with high doses.
• Note any complaint of stuffy nose, because
vasodilation may result and nasal congestion can
occur.
Health Teachings
• Encourage patient to adhere to the drug regimen.
NCM 106: PHARMACOLOGY
LECTURE
• Advise patient that therapeutic effects of
reserpine may not occur for 2 to 3 weeks after
initiation of therapy.
• Teach patient and family how to take pulse and
blood pressure.
• Encourage patient to take reserpine at the same
time every day and not to discontinue without
permission of health care provider.
• Encourage patient to avoid orthostatic (postural)
hypotension by slowly rising from supine or sitting
positions to standing.
• Inform patient and family of possible mood
changes when taking reserpine due to
catecholamine depletion. Mood changes can
include depression, detachment, inability to
concentrate, nightmares, and suicidal tendencies.
• Warn patient that reserpine may cause
impotence or decreased libido, which is usually
dose related.
• Advise patient not to drive or engage in operation
of dangerous equipment until the drug response
is known.
CHOLINERGIC AGONISTS AND
ANTICHOLINERGICS
Cholinergic Agonists
- Drugs that stimulate the parasympathetic
nervous system (parasympathomimetics)
- They mimic the parasympathetic
neurotransmitter acetylcholine.
- Also called cholinomimetics or cholinergic
stimulants. Acetylcholine (ACh) is the
neurotransmitter located at the ganglions
and the parasympathetic terminal nerve
endings. It innervates cholinergic receptors
in organs, tissues, and glands.
The two types of cholinergic receptors are:
1. Muscarinic Receptors - stimulate smooth muscle
and slow the heart rate.
2. Nicotinic Receptors (neuromuscular) - which
affect the skeletal muscles.
• Direct-acting cholinergic agonists act on
receptors to activate a tissue response.
• Indirect-acting cholinergic agonists inhibit the
action of the enzyme cholinesterase (ChE)
(acetylcholinesterase) by forming a chemical
complex, thus permitting acetylcholine to persist
and attach to the receptor.
Direct-Acting Cholinergic Agonists
- Many drugs classified as direct-acting
cholinergic agonists are primarily selective to
the muscarinic receptors but are nonspecific
because the muscarinic receptors are
located in the smooth muscle of the GI and
genitourinary tracts, glands, and heart.
Bethanechol chloride (Urecholine)
- acts on the muscarinic (cholinergic) receptor
- used primarily to increase micturition
(urination) in the treatment of urinary
retention and neurogenic bladder.
Metoclopramide HCl (Reglan)
- usually prescribed to treat gastroesophageal
reflux disease (GERD).
Pilocarpine
- constricts the pupils of the eyes, thus
opening the canal of Schlemm to promote
drainage of aqueous humor (fluid).
Indirect-Acting Cholinergic Agonists
- The indirect-acting cholinergic agonists do
not act on receptors; instead they inhibit or
inactivate the enzyme cholinesterase,
permitting acetylcholine to accumulate at the
receptor sites.
- This action gives them the name
cholinesterase (ChE) inhibitors,
acetylcholinesterase (AChE) inhibitors, or
anticholinesterases, of which there are two
types: reversible and irreversible.
Nursing Responsibilities: Cholinergic Agonist, Direct
Acting
• Monitor patient’s vital signs. Heart rate and blood
pressure decrease when large doses of
cholinergics are taken. Orthostatic hypotension is
a side effect of a cholinergic agonist such as
bethanechol.
• Record fluid intake and output. Decreased urinary
output should be reported because it may be
related to urinary obstruction.
• Give cholinergic agonists 1 hour before or 2
hours after meals. If patient complains of gastric
pain, the drug may be given with meals.
• Check serum amylase, lipase, aspartate
aminotransferase, and bilirubin levels. These
laboratory values may increase slightly when
taking cholinergic agonists.
• Observe patient for side effects such as gastric
pain or cramping, diarrhea, increased salivary or
bronchial secretions, bradycardia, and orthostatic
hypotension.
• Auscultate breath sounds for rales (cracking
sounds from fluid congestion in lungs) or rhonchi
(rough sounds resulting from mucous secretions
in lungs). Cholinergic agonists can increase
bronchial secretions.
• Have IV atropine sulfate (0.6 mg to 1.2 mg)
available as an antidote for cholinergic overdose.
• Early signs of overdosing include flushing,
salivation, sweating, nausea, and abdominal
cramps.
• Increase bathing frequency and linen change
when needed. Diaphoresis (excessive
perspiration) may occur.
• Monitor for possible cholinergic crisis (overdose)
including symptoms of muscular weakness and
increased salivation.
NCM 106: PHARMACOLOGY
LECTURE
Health Teaching
• Teach patient to take the cholinergic agonist as
prescribed. Compliance with the drug regimen is
essential.
• Direct patient to report severe side effects, such
as profound dizziness or a decrease in heart rate
below 60 beats/min.
• Teach patient to arise from a lying position slowly
to avoid dizziness. This is most likely a result of
orthostatic hypotension.
• Encourage patient to maintain effective oral
hygiene if excess salivation occurs.
• Advise patient to report any difficulty in breathing
as a result of respiratory distress.
Anticholinergics
- Drugs that inhibit the actions of acetylcholine
by occupying the acetylcholine receptors
(parasympatholytics).
- Other names used for anticholinergics are
cholinergic blocking agents, cholinergic or
muscarinic antagonists, antiparasympathetic
agents, antimuscarinic agents, and
antispasmodics.
- The major body tissues and organs affected
by the anticholinergic group of drugs are the
heart, respiratory tract, GI tract, urinary
bladder, eyes, and exocrine glands.
- By blocking the parasympathetic nerves, the
sympathetic (adrenergic) nervous system
dominates.
- Anticholinergics and adrenergic agonists
produce many of the same responses.
- Muscarinic receptors are a type of
cholinergic receptor involved in tissue and
organ responses to anticholinergics,
because anticholinergics inhibit the actions
of acetylcholine by occupying these receptor
sites.
Atropine
- A classic anticholinergic
- Muscarinic antagonist drug
- Scopolamine was the second belladonna
alkaloid produced. Atropine and scopolamine
act on muscarinic receptors, but they have
little effect on nicotinic receptors.
Atropine is useful primarily:
1. As a preoperative medication to decrease
salivary secretions.
2. As an agent to increase heart rate when
bradycardia is present.
Nursing Responsibilities
• Monitor patient’s vital signs. Report if tachycardia
occurs.
• Determine fluid intake and output. Encourage
patient to void before taking the medication.
• Report decreased urine output. Anticholinergics
can cause urinary retention. Maintain adequate
• fluid intake.
• Assess bowel sounds. Absence of bowel sounds
may indicate paralytic ileus resulting from a
• decrease in GI motility (peristalsis).
• Examine for constipation caused by decrease in
GI motility. Encourage patient to ingest foods
• that are high in fiber, to drink adequate amounts
of fluids, and to exercise if able.
• Use bed alarms for patients who are confused
and debilitated. Atropine could cause central
• nervous system stimulation (excitement,
confusion) or drowsiness.
• Provide mouth care. Atropine decreases oral
secretions and can cause dryness.
• Administer IV atropine undiluted or prefer diluted
in 10 mL of sterile water. Rate of
• administration is 1 mg or fraction thereof/min.
Health Teaching
• Direct patient to avoid hot environments and
excess physical exertion. Elevations in
• body temperature can result from diminished
sweat gland activity.
• Teach patient with narrow-angle glaucoma to
avoid atropine-like drugs.
• Anticholinergics cause mydriasis and increase
intraocular pressure. Instruct patient to check
labels on over-the-counter (OTC) drugs to
determine whether they are contraindicated for
glaucoma.
• Instruct patient not to drive a motor vehicle or
participate in activities that require alertness.
Drowsiness is common.
• Tell patient with mydriasis following an eye
examination to use sunglasses in bright light
because of photophobia.
• Advise patient of common side effects such as
dry mouth, decrease in urination, and
constipation that occur as a result of
anticholinergic use.
• Direct patient to increase fluid intake and
consumption of high-fiber foods to prevent
constipation when taking anticholinergics for a
prolonged period.
• Instruct patient to urinate before taking the
anticholinergic. Urinary retention can be a
problem.
• Advise patient to report a marked decrease in
urine output.
• Suggest that patient use hard candy, ice chips, or
chewing gum. Maintain effective
• oral hygiene if patient’s mouth is dry.
Anticholinergics decrease salivation.
• Encourage patient to use eye drops to moisten
dry eyes that result from decreased lacrimation
(tearing).