PHARMACOLOGY

PHARMACODYNAMICS = drug's mechanism of action

■ Drug Actions maybe through;
1. RECEPTORS
2. ENZYMES and PUMPS
3. ION CHANNELS
4. ALTERING METABOLIC PROCESS
■ AGONISTS
= binds to a receptor and stimulates the action
■ ANTAGONISTS
1. Competitive Antagonist
= binds to a same RECEPTOR = potency of an agonist is reduced
2. Non Competitive Antagonist
= binds to a DIFFERENT RECEPTOR = prevents potency of an agonist
PHARMACOKINETICS
■ = body's response to the drug
■ Liberation
■ drug enters body and releases the active ingredient
■ Absorption
■ drug in blood
■ Distribution
■ drug in tissue and cells
■ Metabolism ( Biotransformation )
■ drug in liver
■ drug changed to a form easily excreted
■ Excretion ( Elimination )
■ drug changed into inactive form eliminated by the body
• Dose
^ amount of drug to be administered to the patient
• Schedule
^ frequency, how many dose/s per day
• Recommended dose
^ RIGHT amount + RIGHT schedule
• Critical concentration
^ level of drug in the blood which produces a therapeutic effect
• Therapeutic effect
^ favorable response after a treatment of any kind
• Loading dose
^ initial dose, immediate response
• Half Life
^ time it takes for a drug to become half of its previously peaked level
Rights of Drug Administration
1. Right DRUG
2. Right PATIENT
3. Right DOSE
4. Right ROUTE
5. Right TIME
Considerations to the 5 rights:
1. Right DOCUMENTATION
2. Right CLIENT EDUCATION
3. Right to REFUSE
4. Right ASSESSMENT
5. Right EVALUATION
TOXICOLOGY:
1. PRIMARY ADVERSE EFFECTS = simple overdose
2. SECONDARY ADVERSE EFFECTS = the OTHER effect of the drugs
3. HYPERSENSITIVITY
= exaggerated response of the immune response
DOSAGE FORMS OF DRUG:
A. SOLID
■ TABLET
a. Scored
b. Layered
c. Enteric-coated
d. Chewable
e. Sustained-release
■ CAPSULE
a. Hard Gel
b. Soft Gel
■ LOZENGES
o antiseptic action
 o analgesic action
■ SUPPOSITORY
B. LIQUID
■ Syrup
■ Suspension
■ Elixir
C. TOPICAL
■ Ointment
■ Cream
■ Lotion
■ Patch

AUTONOMIC NERVOUS SYSTEM DRUGS

NEUROTRANSMITTERS
= chemicals in the body acting as "messengers"

■ Acetylcholine ( ACh )
■ Norepinephrine and Epinephrine ( NE / E )
■ Dopamine ( Dopa )
■ Serotonin ( 5HT )
■ Gamma Amino Butyric Acid ( GABA )

■ Includes two neurotransmitters

■ Norepinephrine and acetylcholine
■ Two branches :
■ Sympathetic
■ Adrenergic nervous system
■ Parasympathetic
■ Cholinergic
 Constrict pupils Dilate pupils

Inhibit salivation

Stimulate activity
of stomach

Inhibit r of Stimulate release of glucose;

glucose; stimulate inhibit gallbladder
gallbladder Inhibit activity of intestines

Stimulate activity
of intestines

Secrete
epinephrine and
norepinephrine
Relax bladder
Contract bladder
Promote erection •
of genitals

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 Autonomic Nervous SYMPATHETIC PARASYMPATHETIC
System

Response to: HEART

LUINGS,
BRONCHUS
PUPILS

GIT
( blood flow, motility,
secretions )
KIDNEY
- blood flow
URINARY BLADDER
- sphincter
- detrusor muscle
BLOOD VESSELS
( smooth muscle )
ADRENERGIC AGONISTS
1. ADRENERGIC AGONISTS
a. Epinephrine = CPR, Shock
a. Dobutamine = CHF
a. Dopamine
= CHF, Cardiogenic Shock
a. Norepinephrine = cardiac arrest
2. ALPHA 1 ADRENERGIC AGONISTS
a. Phenylephrine
= vasoconstriction ^ decongestion = allergy
3. ALPHA 2 ADRENERGIC AGONISTS
a. Clonidine ( Catapres )
= found in CNS neurons ^ dec Epinephrine flow =
Hypertension
4. BETA 1 ADRENERGIC AGONIST
a. Dobutamine
 = CHF
5. BETA 2 ADRENERGIC AGONISTS
a. Albuterol / Salbutamol
b. Isoproterenol
c. Terbutaline
d. Isosuxprine
Nursing Considerations:
1. Avoid sudden withdrawal of the drug
2. Monitor vital signs
3. Provide comfort measures
4. Provide adequate health teaching on the name of drug,
prescribed
dosage, effects and adverse effects to increase patient's
knowledge and subsequent compliance.
ADRENERGIC ANTAGONISTS

1. ALPHA and BETA ADRENERGIC ANTAGONISTS

a. Carvediol
b. Labetalol
2. ALPHA ADRENERGIC ANTAGONISTS
a. Phentolamine
3. ALPHA 1 ADRENERGIC ANTAGONISTS
a. Prazosin
b. Doxazosin
c. Terazosin
d. Alfuzosin
e. Tamsulosin
4. BETA ADRENERGIC ANTAGONISTS " olol "
a. Propranolol
b. Pindolol
5. BETA 1 SPECIFIC ADRENERGIC ANTAGONISTS
a. Betaxolol. Bisoprolol
b. Esmolol
c. Atenolol Acebutolol
d. Metoprolol

MYASTHENIA GRAVIS

• in Women, 20 - 40 y/o, unknown cause or idiopathic

• Autoimmune
• Descending muscle weakness

CHOLINERGIC AGONISTS
 1. NEOSTIGMINE = treatment
2. PYRIDOSTIGMINE = treatment
3. PHYSOSTIGMINE = treatment
4. EDROPHONIUM CHLORIDE = diagnostic

Diagnostic Test: Tensilon Test Myasthenic Crisis :

■ Signs and symptoms : Weakness, paralysis
■ Cause : underdose
■ Treatment : Cholinergic drugs Cholinergic Crisis :
■ Signs and symptoms : Weakness, paralysis
■ Cause : overdose
■ Treatment : Anticholinergic drugs:

ALZHEIMER'S DISEASE

DESCRIPTION:
= degeneration of cholinergic nerves

• Signs & Symptoms :

• A - amnesia
• A - agnosiak
• A - apraxia
• A - aphasia
- Expressive
- brocca's aphasia
- Receptive
- wernickes aphasia
CHOLINERGIC DRUGS:
1. RIVASTIGMINE
2. TACRINE
3. DONEPEZIL

PARKINSON'S DISEASE

Classes of Anti-Parkinson Agents I.

Anticholinergic DRugs
 a. Benztropine (Cogentin)
b. Biperiden (Akineton)
c. Diphenhydramine (Benadryl)
d. Trihexyphenidyl (Artane)
II. Dopaminergic Drugs
a. Dopamine precursors
b. Dopamine receptor agonists
c. MAO Inhibitors
d. Catechol-O-methyltransferase
inhibitors

DRUGS AFFECTING THE RESPIRATORY

SYSTEM

Upper Respiratory Tract Drugs

• ANTIHISTAMINE

DECONGESTANTS

• EXPECTORANTS

• MUCOLYTIC

• ANTITUSSIVES
I. BRONCHODILATORS:
A. SYMPATHOMIMETICS ( Beta 2 Adrenergic Agonist )
o Albuterol o Ephedrine o Epinephrine
B. PARASYMPATHOLYTICS
o Ipratropium
C. M ETHYLXANTHINES
o Caffeine o Aminophylline o Theophylline

II. ANTIINFLAMMATORY DRUGS:

A. INHALED STEROIDS
o Budesonide o Fluticasone o Triamcinolone
 ANGINA
" chest
pain

DRUGS AFFECTING BLOOD COAGULATION

• Antiplatelets
= blocks the formation of platelet plug
• Aspirin
• Clopidogrel
• Anticoagulants
= blocks thrombin production
• Warfarin
= blocks the Vit. K dependent clotting factors = Route:
oral
= Therapeutic test: PT/INR
= Therapeutic margin: 1.5 - 2.0 times the normal =
Side effect: bleeding
• Heparin
= blocks the formation of thrombin = Route: IV / SQ
= Therapeutic test: aPTT = Therapeutic margin: 1.5
- 2.5 times the normal = Side effect: bleeding
• Thrombolytics
= dissolve the clot by activating the plasminogen ^
plasmin = goal: restore the blood flow
• Alteplase
• Streptokinase
• Reteplase
• Urokinase
= Side effect: bleeding
• Antifibrinolytic
• Aminocaproic acid
• Tranexamic acid
 Drugs Affecting Blood Coagulation
INJURY Plasminogen {liver 1

vasoconstriction

formation of platelet plug

Plasmin

intrinsic pathwa extrinsic

exrnrj: pathway
Vlt. K
liver Prothrombin Thrombi
Fibrinolysis

Fibrinogen

COAGULAT ON CASCADE

HYPERTENSION

■ Mean Arterial Pressure (MAP)

■ average pressure through out each cycle of the heartbeat
■ Normal : 70-100 mmHg
MAP = SBP + 2 (DBP)
3
□ Clinical significance
> perfusion pressure seen by organs in the body
 Angiotensin I

Converting
Enzyme

ANGIOTENSIN 1

Osmolarttv f

Ai RECEPTORS

vasoconstriction

Blood vessel

-s
| blood flow back to • BP
kidney

RENIN ANGIOTENSION ALDOSTERONE SYSTEM

ANTIHYPERTENSIVE DRUGS AFFECTING THE RAAS:

• ACE Inhibitors "pril"

• Angiotensin 2 Receptor Blockers (ARB) "sartan "
• Renin Antagonists
• Selective Aldosterone Antagonist

ANTIHYPERTENSIVE DRUGS AFFECTING THE ANS RECEPTORS:

• Alpha 1 Adrenergic Antagonists "zosin"

• Alpha 2 Adrenergic Agonist
• Beta Adrenergic Blockers "olol"
VASODILATORS :

• Indirect-Acting Vasodilator
= Calcium Channel Blocker
• Direct-Acting Vasodilator
 = Vasodilators
OTHERS:
• DIURETICS

ARRHYTHMIA

• CLASS I: blocks the sodium channel

■ Class Ia: QUINIDINE, PROCAINAMIDE
■ Class Ib: LIDOCAINE, PHENYTOIN
• CLASS II: blocks the beta receptor
■ PROPRANOLOL
■ ESMOLOL
• CLASS III: blocks the potassium channel
• AMIODARONE
• CLASS IV: blocks the calcium channel
• VERAPAMIL
• DILTIAZEM

ELECTRICAL IMPULSE
 CONGESTIVE HEART FAILURE
= "PUMP FAILURE"

DRUGS FOR CONGESTIVE HEART FAILURE:

• CARDIOTONIC DRUGS
■ Cardiac Glycosides : Digoxin ( Lanoxin )
■ Phosphodiesterase Inhibitors : Inamrinone
■ Sympathomimetic : Dobutamine
■ Diuretics : Furosemide
■ Vasodilators
■ ACE Inhibitors : Captopril, Enalapril
■ Vasodilators : Nitroglycerine

DRUGS USED FOR PEPTIC ULCER DISEASE (PUD)

PEPTIC ULCER
= an erosion in the mucosal lining

• ANTACIDS
= neutralize the hydrochloric acid in the stomach
■ Al (OH)
■ Mg (OH)
■ Mg + Al (OH)2
• HISTAMINE 2 RECEPTOR BLOCKERS
= blocks the histamine 2 receptors ^ decreasing the HCl- secretion
■ CIMETIDINE
■ RANITIDINE
■ FAMOTIDINE
• PROTON PUMP INHIBITORS
= blocks the proton pump ^ decreasing the HCl- secretion
■ OMEPRAZOLE
■ PANTOPRAZOLE
• CYTOPROTECTIVES = coats the ulcer
■ SUCRALFATE
• PROSTAGLANDIN AGONIST = stimulates prostaglandin ^
■ MISOPROSTOL ( CYTOTEC )
 DRUGS USED TO CONTROL BLOOD GLUCOSE LEVEL

Oral Antidiabetic Medication Families

| Medication name
How it works Side effects

Sulfonylureas Glipizide Stimulates release of insulin from pancreas Hypoglycemia

(Gl'jcotm) May also increase cellular sensitivity to
insulin

Meglitinides Promotes insulin secretion by the Hypoglycemia Repogiinide pancreas [Prand in}

Biguanides Decreases glucose pro duct on by the liver Gl disturbances: cecreased appetite,
Metformin and Increased glucose uptake by muscle nausea, and diarrhea: rare: metabolic
(Glucophage) acidos s (rema! Impairment)

Oral Antidiabetic Medication Families

Medication name How it works Side effects

Thiazo idinediones [glita Increases insulin sensitivity in patients with Promotes water retention [weight
zones) type 2 diabetes (increases insulin uptake gain and edema)
by muscle and decreases glucose
production by the liver)

Al p ha -g luc osi da se I nhlblts cartjohyd rate GI symptom s: fl atu lenee, cram ps.
inhibitors dlg&Stion/absorptkJrt distention. brnborygmus
Acarbose [Precose) Dccrcasc-S postprandial
blood glucose :ise
Gliptins Enhances the activity of in cretins None yet
SFtiaglipcin (Januv'ia) (Inhibits Ihelr breakdown}
Increases nsulin re ease Reduces glucagon
release Decreases heps Me glucose
production

INSULIN
Action: liver, muscle & adipose to facilitate passage of glucose, K+, and Mg
Indications : DM type 1, DM type 2
■ onset, peak & duration • Storage:
1. avoid extremes of temperature
2. before injection : should be room temp
3. if vial will be used in 1 month: room temp
4. Otherwise : refrigerate

Type Example Onset Peak Duration

Very short Aspart, Lispro 15 min 30 to 60 min 2-4 hours

Short Regular] 30 - 60 min 2-4 hours 4-6 hours

Intermediate NPH 2-4 hours 6-8 hours 16-20 hours

Long acting Ultralente 6-8 hours 12-16 hours 20 - 30 hours

Very long Glargine, 1 hour No peak 24 hours

acting Lantus

• Dawn phenomenon
• reduced tissue sensitivity to insulin
• develops between 5 - 8 am
• prebreakfast hyperglycemia
• caused by nocturnal release of GH
• tx: inc intermediate-acting insulin at 10 pm
• Somogyi phenomenon
• normal or elevated blood glucose levels at bedtime
• hypoglycemia occurs 2-3 am causing inc of counterregulatory hormones
• 7 am as a response ^ rebound hyperglycemia
• Tx: dec pm production of glucagon after meals, slows gastric emptying ( w/c limits
the rise in the blood glucose level pc ) reduces fasting and postprandial blood glucose
levels and reduces caloric intake ^ weight loss
■ Glucose-Elevating Agents
- diazoxide
- glucagon
 THYROID AGENTS

■ AntiThyroid Agents
- Levothyroxine
- Liothyronine
- Liotrix
- thyroid desiccated

■ Thyroid Replacement Agents

Antithyroid Agents Thiomides
- methimazole
- propylthiouracil Iodine solutions
- sodium iodide L131
- strong iodine solutions
- potassium iodide

ANTIMICROBIALS

□ BLOCKS CELL WALL SYNTHESIS

■ BETA LACTAMS
■ PENICILLINS
■ CEPHALOSPORINS
■ CARBAPENEMS
■ MONOBACTAM
■ VANCOMYCIN
□ BLOCKS PROTEIN SYNTHESIS
■ MACROLIDES
■ CHLORAMPHENICOL
■ LINCOSAMINES
■ AMINOGLYCOSIDES
■ TETRACYCLINES
□ FOLIC ACID SYNTHESIS INHIBITOR
■ SULFONAMIDES
■ TRIMETHOPRIM
□ NUCLEIC ACID SYNTHESIS INHIBITOR
■ FLUOROQUINOLONES
Classification of some antimicrobial agents by their sites of action. (THFA = tetrahydrofolic acid; PABA
= p-aminobenzoic acid.)
Source : Lippincott Illustrated Reviews, Pharmacology - Whalen, Karen