- It is located in the postganglionic
Pharmacology Review.
AUTONOMOUS NERVOUS SYSTEM (ANS) DRUGS
Autonomous Nervous System
 It is a division of PNS that acts on smooth muscles
and glands.
 Also known as visceral system.
 It controls and regulates the heart, respiratory system,
GI, bladder, eyes and glands.
 It is involuntary system, which solely means that it
has “little or no control”.
 It has two sets of neurons:
1. Afferent (Sensory) Neurons – sends signals
towards the CNS
2. Efferent (Motor) Neurons – receives the
information and then makes the response
 It has two branches (efferent [motor] neurons):
1. Sympathetic Nervous System
(Sympathomimetic)
- Also known as adrenergic system
- NEUROTRANSMITTER:
Norepinephrine (It is released from the
terminal nerve ending and stimulates the
cell receptors to produce a response).
9 The receptors being “stimulated”
are the adrenergic receptor organ
cells
 Beta 1
 Beta 2
 Alpha 1
 Alpha 2
2. Parasympathetic Nervous System
(Parasympathomimetic)
- Also known as cholinergic system.
- NEUROTRANSMITTER: Acetylcholine
(It stimulates the receptor cells (muscarine
and nicotine) to produce a response but
ACETYLCHOLINESTERASE
inactivate AchE before it reaches the
receptors).
NOTE. The sympathetic and parasympathetic nervous system
may act as stimulants or depressants.
Adrenergic Agonists
 They mimic the neurotransmitter norepinephrine and
the epinephrine of the SNS.
 Adrenergic Receptors
o ALPHA-ADRENERGIC – located in the blood
vessels, eyes, bladder and prostate.
a) Alpha 1
- It is located into the vascular tissues
- Vasoconstriction, increases BP
b) Alpha 2
sympathetic nerve endings
- Inhibits the release of norepinephrine
- Vasodilation; decreases central
sympathetic outflow
c) Beta 1
- Found in the heart and some in the
kidney
- Increases heart rate
d) Beta 2
- Located in the smooth muscles of lungs,
GI tract, liver and uterine muscles.
- Bronchodilation
e) D1
- Vasodilation in splanchnic (abdomen)
and renal vessels
NOTE. Other are dopaminergic such as located in the renal,
mesenteric, coronary and cerebral arteries. ONLY
DOPAMINE CAN ACTIVATE THESE.
Inactivation of Neurotransmitters
1. Reuptake of the neurotransmitter back into the neuron
2. Enzymatic transformation/degradation
3. Diffusion away from the receptor
 These 2 enzymes inactivate norepinephrine.
1. Monoamine Oxidase
2. Catechol-O-Methyltransferase
Classification of Sympathomimetics
1. Direct-Acting Sympathomimetics
- Stimulate adrenergic receptors
- Ex. Norepinephrine, Epinephrine
-
2. Indirect-Acting Sympathomimetics
- Stimulate the release of norepinephrine from the
terminal nerve endings.
- Ex. Amphetamine
may -
3. Mixed-Acting Sympathomimetics
- Stimulate the adrenergic receptors and the releases
of norepinephrine from the terminal nerve
endings.
- Ex. Ephedrine, Pseudoephedrine
CATHECOLAMINES
 Chemical structures that can produce a
sympathomimetic response.
 Ex. Epinephrine, Norepinephrine, Dopamine
Side Effects of Sympathomimetics
 Hypertension  Dizziness
 Tachycardia  Urinary difficulty
 Palpitation  N/V
 Dysrhythmia
 Tremors
Direct-Acting Adrenergic Agonists  Many are non-selective.
Epinephrine
 Stimulates alpha 1, beta 1 and 2 Direct-Acting Cholinergic Agonists
 Not given orally - Activates a tissue response
 Administered by SQ, IVa (vastus lateralis), IV,
topical, inhalation, IC. Betanechol
 Metabolized in the liver  Used for urinary distension
 It is used to treat anaphylaxis, cardiac arrest, asthma,
COPD and hemostasis Policarpine
 It is a potent inotropic (myocardial contraction  To prevent symptoms of xeropthalmia.
strengthening)
Nicotine
Albuterol  For smoking cessation
 Stimulates beta-2 (beta-2 selective)
 It is used for relaxation of bronchial smooth muscle Indirect-Acting Cholinergic Agonists
and bronchodilation - Inhibit the action of the cholinesterase.
 Better than isoproterenol 1. Reversible – bind the ChE for several minutes
 High doses may affect beta-1 receptor 2. Irreversible – bind the enzyme permanently
 Half-life: 2.7 – 6 hours
Endrophonium Chloride (Tensilon)
 Side effects:
o Tremors  Indirect-acting
 5-20 minutes increases muscle strength
o Restlessness
 If ptosis, then it may indicated MG.
o Nervousness
 It is used to distinguish myasthenia crisis or
o Hypertension (MAOI)
cholinergic crisis.
o Myasthenia Crisis – if given to patient, muscle
Dopamine
weakness will be alleviated
 Stimulates alpha 1, beta 1 and D1
o Cholinergic Crisis – if given to patient, muscle
 Used during cardiogenic shock and heart failure
weakness will be severe
Alpha-Adrenergic Blockers/Alpha Blockers
 Side Effects:
o Miosis
Beta-Adrenergic Blockers/Beta Blockers o Salivation
Propanolol (Inderal) o N/V
 NON-SELECTIVE o Diarrhea
 First beta-blocker to treat angina, cardiac o Bradycardia
dysrhythmia and HTN.
 Many side effects due to it being non-selective. Neostigmine (Pro-Stigmin)
 It is used to treat angina prophylaxis, HTN,  Indirect acting
arrythmias, migraine, performance anxiety and  It is used to manage/treat myasthenia gravis.
hyperthyroidism  It is used in treatment for myotonia gravis and non-
 May reduce renin levels reversal, non-depolarizing neuromuscular blockade
 Found In breastmilk  Side Effects:
o Miosis
Carvedilol and Labetalol o Salivation
 It is used for pheochromocytoma o N/V
 Combined both alpha and beta blockade. o Diarrhea
o Bradycardia
Atenolol  Muscarinic effects are blocked by atropine.
 BETA-1 SELECTIVE  Half-life: 0.5 – 1 hour
 Used to treat angina, HTN and heart failure  Given every 2-4 hours

Cholinergic Drugs NOTE. The antidote for myasthenia gravis medication

 There are two (2) types of cholinergic receptors toxicity is atropine sulfate. Muscarinic receptor antagonist is
1. Muscarinic – stimulate smooth muscles; slow the a competitive antagonist for Ach.
HR
2. Nicotinic (Neuromuscular) – stimulates/ affects the Atropine
skeletal muscles  Muscarinic
  Blocks all muscarinic receptors  HALF-LIFE: 9-13 hours
 Antidote for betanechol.  Amphetamines and dextroamphetamine are
 Increases heart rate when bradycardia is present. prescribed for narcolepsy and ADHD when
 Well absorbed orally and parentally amphetamine-like drugs are ineffective.
 Toxicity: (DUMBBELSS)
o Increase temperature Amphetamine-Like Drugs
o Delusion, confusion Methylphenidate and Dexmethylphenidate
o Temp. blindness; blurred vision  These are amphetamine-like drugs
o Flush of the face  Given to increase a child’s attention span and
o Dryness cognitive performance and to decrease
impulsiveness, hyperactivity, and restlessness.
 It is classified as a Controlled Substance Schedule
CNS and PNS DRUGS (CSS) ll drug.
 The CNS drugs has limited use of it which are the  Administer to children for atleast 30-45 minutes
following: before breakfast and lunch.
o Treatment for ADHD for children.  Should be taken 6 hours before sleeping.
o Narcolepsy  Transdermal patches may be worn for 9 hours.
o Reversal respiratory distress  It inhibits metabolism of barbiturates, which leads
to increased blood vessels.
 The major groups are the following:
1. Amphetamine and Caffeine  Educate pt. to avoid foods that contain caffeine.
- Stimulates the cerebral cortex of the brain  Report for tachycardia and palpitations.
- Abused and is only used for short-term (up  Monitor for children onset of Tourette Syndrome.
to 12 weeks)
2. Analeptics and Caffeine Modafinil
- Acts on the brainstem and medulla to  Increases wakefulness of the pt.
stimulate respiration
3. Anorexiants Anorexiants
- Suppress appetite by stimulating satiety  Suppress appetite
center in the hypothalamic and limbic areas  For wt. loss
of the brain.  Children younger than 12 years should not be given
anorexiants, and self-medication with anorexiants
Illnesses in Relation to CNS and PNS Drugs should be discouraged.
ADHD  Long-term use of these drugs frequently results in
 Characteristics behaviors of the various types of such severe side effects such as nervousness,
ADHD include inattentiveness, inability to restlessness, irritability, insomnia, heart
concentrate, restlessness (fidgety), hyperactivity palpitations, and hypertension.
(excessive and purposeless activity), inability to
complete tasks, and impulsivity.
 Abnormal electroencephalograph (EEG) findings Analeptics
 Learning disability  It has 2 subgroups:
1. Xanthines (Methylxanthines)
Narcolepsy 2. Theophylline
 Falling asleep during normal waking activities - It is used to relax bronchioles
 SLEEP PARALYSIS – muscle paralysis during - Used to increase respiration for NB.
sleep; accompanied by narcolepsy Caffeine
 With the help of caffeine, it stimulates the CNS,
Amphetamines while larger doses of analeptics may lead to
 Stimulate the release of dopamine and stimulation of respiration.
norepinephrine.  Side effects are similar to anorexiants.
 It normally causes euphoria and increase alertness.  Other side effects:
 It may also cause: o Diuresis (increased urination)
o Insomnia o GI irritation (e.g. nausea, diarrhea)
o Restlessness o Tinnitus [RARE]
o Tremors  Half-life: 5 hours
o Irritability
o Weight loss CNS Depressants
 Continuous use may cause cardiovascular problems  Causes varying degrees of depression
  These include: [SGAOAAA] 9 It may cause anterograde
o Sedative-Hypnotic amnesia/memory impairment.
o General anesthetics - Small doses only!
o Analgesics
o Opioid and non-opioid analgesics NOTE. Antidote for overdose is FLUMAZENIL.
o Anticonvulsants
o Antipsychotics 3. Nonbenzodiazepines
- Ex. Zolpidem
o Antidepressants
9 A nonbenzodiazepines that differs
in chemical structure from
Sedative Hypnotics
benzodiazepines.
 It is ordered for treatment of sleep disorders 9 It is used for short-term treatment
 It diminishes physical and mental responses at lower (<10 days) of insomnia.
dosages of certain CNS depressants but does not - Advise patients to take nonbenzodiazepines
affect consciousness. before bedtime.
 Mostly used during daytime. - Alprazolam takes effect within 15 to 30
 Hypnotics maybe short or intermediate acting: minutes
o Short Acting – achieving sleep
o Intermediate Acting – sustaining sleep. Anesthetics
 The ideal hypnotic promotes natural sleep without A. Balance Anesthesia
disrupting normal patterns of sleep and produces no - Combination of drugs used in GA.
hangover or undesirable effect. - May include the following:
 A hypnotic given the night before
NOTE. Ramelteon the only major sedative-hypnotic  Premedication with an opioid analgesic or
approved for long-term use. benzodiazepine (e.g. midazolam) plus an
anticholinergic (e.g. atropine) given about
 The following are categories of sedative-hypnotics: 1 hour before surgery to decrease
1. Barbiturates (-barbital) secretions.
 Long-Acting Group  A short-acting nonbarbiturate such as
- For seizures and epilepsy propofol
- Ex. Phenobarbital Mephobarbital  An inhaled gas, often a combination of an
 Intermediate-Acting Group inhalation anesthetic, nitrous oxide, and
- For maintaining long periods of sleep. oxygen.
- Ex. Butabarbital  A muscle relaxant given as needed
 Slow-Acting Group
- For procedure sedation B. General Anesthesia
- Ex. Secobarbital - Used for surgical procedures.
- Stage 4. Medullary Paralysis might cause loss
Pentobarbital or respiration
 Increases hepatic enzyme action, causing an
increased metabolism and decreased effects of drugs C. Inhalation Anesthesia (-lanes)
such as oral anticoagulants, glucocorticoids, tricyclic - Used during surgery
antidepressants, and quinidine. - Example.
 Pentobarbital may cause hepatoxicity if taken with o Halothane, isoflurane, and enflurane,
large dose of acetaminophen. recovery of consciousness usually occurs
 Together with secobarbital they are used for t(x) of in approximately 1 hour.
insomnia. o Desflurane and sevoflurane is within
minutes.
2. Benzodiazepines (-am)
- Induce sleeping D. Intravenous Anesthetics
- Benzodiazepines (except temazepam) can - Used for the induction stage of anesthesia.
suppress stage 4 of NREM sleep, which - Ex. Propofol and Midazolam
may result in vivid dreams or nightmares - It may cause adverse reactions such as:
and can delay REM sleep. o Respiratory and cardiovascular
- Ex. Triazolam depression
9 A short-acting hypnotic with a half-
life of 2 to 5 hours. It does not E. Topical Anesthesia
produce any active metabolites.
F. Local Anesthesia
 - Block pain at the site where the drug is  Most commonly ordered as sustained-release (SR)
administered by preventing conduction of capsule
nerve impulses  For IV:
o 50mg/min – adults
G. Spinal Anesthesia o 25 mg/min – older adults
- Requires that a local anesthetic be injected into  It displaces anticoagulants and aspirin
the subarachnoid space.  Barbiturates, rifampin, and chronic ingestion of
o Spinal Block - penetration of the ethanol increase hydantoin metabolism
anesthetic into the subarachnoid space o Drugs like sulfonamides and cimetidine can
o Epidural Block – epidural space increase the action of hydantoins by inhibiting
o Caudal Block – sacral hiatus liver metabolism.
 Antacids, calcium preparations, sucralfate, and
NOTE. Blood pressure should be monitored during antineoplastic drugs also decrease the absorption of
administration of these types of anesthesia because a decrease hydantoins
in blood pressure resulting from the drug and procedure might  Ex. Phenytoin
occur.
Barbiturates
Antiseizure Drugs  Prescribed to treat tonic-clonic, partial, and
 Used for epileptic seizures myoclonic seizures and status epilepticus, a rapid
 Stabilize never cell membranes and suppress the succession of epileptic seizures
abnormal electric impulses in the cerebral cortex  Reduce seizures by enhancing the activity of GABA.
 Prevent seizures but do not eliminate the cause or  THERAPEUTIC RANGE: 20-40 mcg/ml
provide a cure.
 Stop medication of after 3-5 years there is no Benzodiazepines
occurrence of seizure.  CLONAZEPAM - effective in controlling absence
 Types of anticovulsants: and myoclonic seizures, but tolerance may occur 6
o Hydantoins (Phenytoin) months after drug therapy starts.
o Long-acting Barbiturates  CLORAZEPATE DIPOTASSIUM - treating
o Benzodiazepines partial seizures.
o Succinimides  DIAZEPAM - treat status epilepticus
o Carbamazepine  Ex. Clonazepam, clorazepate dipotassium,
o Valproate lorazepam, and diazepam
 Physiology of anticonvulsants:
1. Suppressing sodium influx Succinimides
o Phenytoin, fosphenytoin,  Used to treat absent seizures
carbamazepine, oxcarbazepine,  Decrease calcium influx
valproic acid, topiramate,  Ex. Ethosuximide
zonisamide, and lamotrigine. 9 THERAPEUTIC RANGE: 40- 100
2. Suppressing calcium influx mcg/ml.
o Valproic acid and ethosuximide.
3. Increase the action of gamma-aminobutyric Carbamazepine
acid (GABA)  It is used to control tonic-clonic and partial seizures.
o Barbiturates, benzodiazepines, and  THERAPEUTIC RANGE: 4-12 mcg/ml.
tiagabine.
Valproate
Hydantoins  For mixed-type of seizures.
 Suppressing sodium influx
 Stabilize cell membranes Drugs for Parkinson’s Disease
 Reduce receptive neural firing  PARKINSON’S D(X): It is a chronic, progressive,
 Limit seizures and neurologic disorder that affects the
 Newborns, persons with liver disease, and older extrapyramidal motor tract, which controls posture,
adults require a lower dose because of a decrease in balance, and locomotion.
metabolism that results in more available drug  Pseudoparkinsonism – adverse reaction from:
 THERAPEUTIC RANGE: 10-20 mcg/ml o Chloropromazine
 ONSET OF ACTION: 30 minutes – 2 hours o Haloperidol
 PEAK CONCENTRATION: 1.5 – 6 hours o Lithium
o Methyldopa
 o Metoclopramide
o Reserpine
Anticholinergics
 Reduce the rigidity and some of the tremors
characteristic of Parkinson’s disease but have a
minimal effect on bradykinesia.
 Decrease salivation
 Ex. Trihexyphenidyl and Benztropine
Dopaminergics (-dopa)
 LEVODOPA – first dopaminergic drug
9 Effective in diminishing symptoms of
Parkinson’s disease and increasing mobility.
 Combined with CARBIDOPA
9 Inhibit the enzyme dopa decarboxylase
 Urge patients who take high doses of selegiline to
avoid foods high in tyramine such as aged cheese, red
wine, cream, yogurt, chocolate, bananas, and raisins
to prevent crisis
 Urge patients taking amantadine to report any signs
of skin lesions, seizures, or depression
 Advise patients taking bromocriptine to report
symptoms of lightheadedness
 Pt. who does not respond to AchE inhibitors may
use prednisone instead, if lower dose, add
azathioprine.
9 WBC count and liver enzymes should be
closely monitored to avoid leukopenia and
hepatoxicity.
Skeletal Muscle Relaxant
 Relieve muscular spasms and pain associated with
traumatic injuries and spasticity form chronic
debilitating disorders (e.g. MS, stroke, cerebral palsy,
head and spinal cord injuries).
o SPASTICITY - increased muscle tone from
hyperexcitable neurons. It is caused by
increase stimulation from the cerebral
neurons or lack of inhibition in the spinal
cord or at the skeletal muscles
Spasticity
 Drugs used to treat spasticity are:
o Baclofen
o Dantrolene
o Tizanidine
o Diazepam
o Benzodiazepine

Monoamine Oxidase B Inhibitor (-gilines) Muscle Spasm

 MAO-B causes catabolism of dopamine
 SELEGILINE
9 Inhibits MAO-B and thus prolongs the action
of levodopa.
9 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- such as aged cheese, red
wine, and bananas- can cause a hypertensive
crisis.
 RASAGILINE
9 MAO-B inhibitor used for the treatment of
Parkinson’s disease
Cathecol-O-Methyltransferase Inhibitors (-capone)
 Increase the amount of levodopa concentration in the
brain.
 A great expection for cyclobenzaprine.
 Drugs used to treat muscle spasm are carisoprodol,
chlorzoxazone, cyclobenzaprine, metaxalone,
methocarbamol, and orphenadrine citrate.
NOTE. The side effects from centrally acting muscle
relaxants include drowsiness, dizziness, lightheadedness,
headaches, and occasional GI sensitivity (e.g. nausea,
vomiting, abdominal distress).
Psychiatric Agent
 These include:
o Antipsychotics
- Also known as neuroleptics
- Drug that modifies psychotic behavior and
exerts an antipsychotic effect
o Anxiolytics
- To treat anxiety and sometimes insomnia

Drugs for Alzheimer’s Diseases Antipsychotics

Acetylcholinesterase Inhibitors  It has two main categories namely:
 RIVASTIGMINE 1. Typical Antipsychotics
9 Has effective penetration into the CNS, thus - These are divided into 2:
cholinergic transmission is increased I. Phenothiazines
 Ex. Donepezil, memantine, galantamine, and  Blocks norepinephrine
rivastigmine  Ex. Thioxanthines
II. Nonphenothiazines
Drugs for Myasthenia Gravis  Ex. Butyrophenones
Acetylcholinesterase Inhibitors (block dopamine)
 Ex. Neostigmine and pyridostigmine  Other examples.
 PYRIDOSTIGMINE -given every 4-6 hours and 9 Dibenzoxazepines,
has an intermediate action 9 Dihydroindolones
 9 Thioxanthenes
2. Atypical Antipsychotics
- Ex. Clozapine
- Effective in treating schizophrenia and
other psychotic disorders in patients
who do not respond to or are
intolerant of atypical antipsychotic
 AR: EPS and NMS
 Most common side effect is drowsiness.
NONPHENOTHIAZINES
 Frequently prescribed nonphenothiazines is
haloperidol.
 Administration precautions should be taken to
prevent soreness and inflammation at the injection
site.
 Medication is a viscous liquid, a large-gauge needle
(e.g. 21 gauge) should be used with the Z-track
method for administration in a deep muscle.
 Use to control psychosis and to decrease agitation in
adults and children
Anxiolytics
 It is used to treat anxiety and insomnia
 BENZODIAZEPINE.
 Benzodiazepine are considered more effective than
barbiturates because they enhance the action of
gamma aminobutyric acid (GABA), an inhibitory
neurotransmitter within the CNS.
Antidepressant Drugs
1. Tricyclic antidepressants (TCAs)
2. Selective serotonin reuptake inhibitors (SSRIs)
3. Serotonin-norepinephrine reuptake inhibitors
(SNRIs)
4. Atypical antidepressants that affect the
neurotransmitters
5. Monoamine oxidase inhibitors
Tricyclic Antidepressants
 Used to treat major depression because they are
effective and are less expensive.
 Block the uptake of the neurotransmitters,
norepinephrine and serotonin in the brain
 Ex. Imipramine [t(x) for enuresis].
 POLYDRUG THERAPY - The practice of giving
several antidepressants or antipsychotics together,
should be avoided if possible because of potential
side effects.
 It elevates mood, increases interest in daily living and
activity, and decreases insomnia.
 For agitated persons:
o Amitriptyline – can cause EPS
o Doxepin
o Trimipramine
 Often given at night.
 CLOMIPRAMINE – cause NMS.
 Most common AR: cardiotoxicity
Selective Serotonin Reuptake Inhibitors
 Block the reuptake of serotonin into the nerve
terminal of the CNS, thereby enhancing its
transmission of the serotonergic synapse
 Commonly used to treat depression than are TCAs
 Ex. Fluoxetine, Fluvoxamine, Sertraline, Paroxetine,
Citalopram and Escitalopram
 Interaction with grapefruit juice that can lead to
possible toxicity
Fluoxetine
 S/E:
o Dry mouth, blurred vision, insomnia, headache,
nervousness, anorexia, nausea, diarrhea, and
suicidal ideation.
Monoamine Oxidase Inhibitors
 Inactivates norepinephrine, dopamine, epinephrine,
and serotonin.
 MAO-A and MAO-B are found in the liver and the
brain.
o MAO-A: Inactivates dopamine in the brain
o MAO-B: Inactivates norepinephrine and
serotonin.
 Ex. Tranylcypromine Sulfate, Isocarboxazid,
Selegiline HCl, Phenelzine Sulfate.
Mood Stabilizers
 It is used to treat bipolar affective disorder
 Ex. Lithium (Antimania), Carbamazepine, Valproic
acid or Divalproex, and Lamotrigine.
 Patient may not achieve the desired effect for 5 to 6
days
NOTE. The antipsychotic drugs olanzapine, ziprasidone, and
aripiprazole are approved to treat acute mania and mixed
episodes of bipolar disorder.
RESPIRATORY DRUGS
Lower Respiratory Disorders
 Common Colds
 Acute Rhinitis
 Allergic Rhinitis
Antihistamines
 Blocks the release of histamine (the chemical
mediator for inflammation which causes increase of
secretions and bronchoconstriction.
 For acute rhinitis (ig?)
H1 Blocker/Antagonist
 It competes with histamine receptors
  Relieve respiratory symptoms and allergic conditions - Lack of the alpha-1 antitrypsin protein that
 It has 5 classifications: inhibits proteolytic enzymes that destroy
1. Ethanolamines alveoli.
2. Piperazine o Asthma
3. Alkylamines - Inflammatory disorder of the airway walls
4. Phenothiazines associated with a varying amount of airway
5. 1st and 2nd Generation H1 Blockers obstruction.
o 1st Generation - BRONCHIAL ASTHMA. Bronchospasm.
- It causes drowsiness  A decrease in forced expiratory volume in 1 second
- It causes sedation and anticholinergic as measured by pulmonary function test.
effects
- Ex. Diphenhydramine Restrictive Lung Disease
o 2nd Generation  It is a decrease in total lung capacity as a result of
- Opposite of 1st generation for it fluid accumulation or loss of elasticity of the lung.
doesn’t cause sedation (little) or any  It is usually caused by the following:
anticholinergic effects. o Pulmonary edema
- Ex. Cetirizine, Fexofenadine, o Pulmonary fibrosis
Loratadine, Azelastine o Pneumonitis
o Lung tumor
Nasal Decongestant o Thoracic deformities (scoliosis)
 Stimulate the alpha-adrenergic receptors which o Myasthenia gravis
leads to vascular constrictions of nasal mucosa.
Medications
Systemic Decongestant  Bronchodilators – assist in opening narrow airways
 Ex. Pseudoephedrine, Phenyleprine, Ephenperine o Sympathomimetics (adrenergics)
o Parasympatholytics (anticholinergic drugs,
Intranasal Glucocorticoids
ipratropium bromide)
 T(x) for allergic rhinitis o Methylxanthines (caffeine, theophylline)
 Ex. Beclomethason, Budesonide, Dexamethasone,
 Glucocorticoids (steroids) – used to decrease
Flunisolide
inflammation
 Leukotriene modifiers – reduce inflammation of the
Antitussives
lung tissue
 Suppresses cough reflex of the medulla oblongata
 Cromolyn (anti-inflammatory agent) – suppressing
the release of histamine and other mediators from the
LOWER RESPIRATORY DRUGS (book_pharma.exe)
mast cells
Lower Respiratory Disorders  Expectorants – loosening mucus from the airways
1. Chronic Obstructive Pulmonary Disease  Antibiotics – prevent serious complications from
2. Restrictive Pulmonary/Lung Disease bacterial infections.
IRREVERSIBL
Chronic Obstructive Pulmonary Disease E Bronchodilators
REVERSIBLE
 It is caused by airway obstruction with increased Sympathomimetics (Alpha- and Beta-Adrenergic Agonists)
airway resistance of airflow to lung tissues.  Increases cAMP (Cyclic Adenosine Monophosphate),
 It is usually caused by the following: causing dilation of the bronchioles
o Chronic Bronchitis  NON-SELECTIVE SYMPATHOMIMETICS
- A progressive lung disease caused by (Epinephrine) – given subcutaneously to promote
smoking or chronic lung infections. bronchodilation and elevate BP. Administered during
- Productive coughing (excess mucous emergency situation to restore circulation and
secretions result in airway obstruction) increase airway patency.
o Bronchiectasis  Beta-2 Adrenergics are given by means of
- Dilation of the bronchi and bronchioles inhalation/oral for people exp. Bronchospasm
- Abnormal frequent infection and (associated with chronic asthma/COPD)
inflammation.
- Breakdown of the epithelium of the Albuterol
bronchial mucosa.  A beta-2 adrenergic drug for asthma.
o Emphysema  High dose and overuse of this may lead response to
beta-1 receptor
  It’s effective for the control of asthma by causing  Used for the maintenance t(x) of bronchospasms
bronchodilation with a long duration of action associated with COPD.
 Inhalation only with HandiHaler device (dry-powder
Metaproterenol capsule inhaler)
 It has some beta-1 effects but it is primarily used as a  Side Effects and Adverse Rxn.:
beta-2 agent o Dry mouth
 Administered orally or by inhalation o Constipation
o Vomiting
NOTE. o Dyspepsia (pain in upper chest)
Onset of Action o Abdominal pain
 INHALATION – 1 minute o Depression
 NEBULIZATION – 5-30 minutes o Insomnia
 ORAL – 15-30 minutes o Headache
o Joint pain
If pt. is using inhalers and effectivity is not evident, o Peripheral edema
advice the pt. to attach a space device in the inhaler to o Chest pain (during administration)
improve drug delivery to the lung with less disposition
in the mouth. Ipratropium Bromide
 It is used to treat asthmatic conditions by dilating the
bronchioles.
Side Effects and Adverse Rxn.
 Administered by MDI.
 Epinephrine
o Tremors Other Examples of Anticholinergics
o Dizziness  Ipratropium bromide
o Hypertension  Aclidinium
o Tachycardia  Tiotropium
o Heart palpitations  Umeclidinium
o Cardiac dysrhythmias
o Angina NOTE. Ipratropium Bromide + Albuterol Sulfate = T(x) for
 Beta-2 Adrenergic Drugs (Albuterol) COPD.
o Tremors
o Headaches Methylxanthine Derivatives
o Nervousness  Stimulate the CNS and respiration, dilate coronary
o Increased Pulse Rate and pulmonary vessels and cause diuresis.
o Palpation (high doses)  It includes the following:
o Increase blood glucose o Aminophylline
o Theophylline
Other Examples of Sympathomimetics o Caffeine
 Alpha- and Beta-Adrenergics
o Ephedrine Sulfate Theophylline
o Epinephrine  It relaxes the smooth muscles of the bronchi,
 Beta-2 Adrenergics bronchioles and pulmonary blood vessels by
o Albuterol inhibiting the enzyme phosphodiesterase, resulting in
o Formoterol an increase in cAMP, which promotes
o Levalbuterol bronchodilation.
o Metaproterenol sulfate  THERAPEUTIC RANGE: 5-15 mcg/mL
o Salmeterol  TOXICITY: 20 mcg/mL
o Terbutaline sulfate  It is well-absorbed by oral administration; absorbed
o Arformoterol tartrate from oral liquids and uncoated plain tablets.
o Indacaterol  Food and antacids may decrease the rate but not the
extent of absorption; large volume fluids and high-
o Olodaterol
protein meals may increase the rate of absorption.
 It can also be administered by IV.
 Side Effects and Adverse Rxn.:
o Anorexia
Anticholinergics
Tiotropium o N/V
o Gastric pain increased by gastric acid secretion
 o Intestinal bleeding o IV: Dexamethasone
o Nervousness  More effective than beta-2 agonist (reduction of
o Dizziness bronchial hyperresponsiveness)
o Headache  It includes the following:
o Irritability o Prednisone
o Cardiac dysrhythmias o Prednisolone
o Tachycardia o Methylprednisolone
o Palpitations o Dexamethasone
o Marked hypotension  It can irritate the gastric mucosa and should be taken
o Hyperreflexia with food to avoid ulceration.
o Seizures  One inhalation in the morning and night.
o Hyperglycemia  Side Effects
o Decreased clotting time o Headache
o Leukocytosis o Euphoria
o Confusion
Leukotriene Receptor Antagonists and Synthesis Inhibitors o Sweating
 LEUKOTRIENE – a chemical mediator that can o Hyperglycemia
cause inflammatory changes in the lung. o Insomnia
 CYSTEINYL LEUKOTRIENE – promote an o N/V
increase in eosinophil migration, mucous production o Weakness
and aiway wall edema that results in o Menstrual irregularities
bronchoconstriction.  Adverse Rxn.:
 Effective in reducing the inflammatory symptoms of o Depression
asthma triggered by allergic and environmental o Peptic ulcer
stimuli. o Loss of bone density
 NOT RECOMMENDED FOR ASTHMATIC o Development of osteoporosis
ATTACKS o Psychosis
 It includes the following drugs:
o Zafirlukast NOTE. Fluticasone propionate + Salmeterol = Controlling
o Zileuton asthma symptoms.
o Montelukast
Cromolyn
Leukotriene Receptor Antagonist  T(x) for bronchial asthma
Zafirlukast  Inhibits release of histamine and other chemical
 First drug in the class of leukotriene modifiers. mediators for inflammation
 Reduce the inflammatory process and decreasing  Common side effects:
bronchoconstriction. o Postnasal drip
 Administered orally. o Irritation of the nose and throat
o Cough
Montelukast
 Effectivity will decrease if taken with water
 Administered to children (2 years of age)
 Can be used with xanthine and beta-adrenergics
 SERIOUS SIDE EFFECTS: Rebound
Leukotriene Synthesis Inhibitors
bronchospasm
Zileuton
 Decrease the inflammatory process and decreasing
Mucolytics
bronchoconstriction.
 Detergents to liquify and loosen mucous secretions so
they can be expectorated.
Glucocorticoids
 Ex. Acetylcysteine
 It is used to treat respiratory disorders (asthma).
9 Nebulization, bronchopulmonary disorders
 Have an anti-inflammatory action and are indicated if
 SHOULD NOT BE MIXED WITH OTHER DRUGS
asthma is unresponsive to bronchodilator therapy or
if the pt. has an asthmatic attack while on maximum  Bronchodilator should be given 5 minutes before
doses of theophylline. giving mucolytics
 Synergistic effect with beta-2 agonist  Maybe diluted in softdrinks.
 Can be given with the following methods:
Antimicrobial
o MDI Inhaler: Beclomethasone
 Ex. Trimethoprim-sulfamethoxazole
o Tablet: Dexamethasone, Prednisone
9 Effective for t(x) of mild to moderate acute
exacerbations of chronic bronchitis (AECBs)
from infectious causes.