Hypertension, or high blood pressure, is a common cardiovascular disease defined by elevated blood pressure in the arteries. It is categorized based on systolic and diastolic blood pressure readings into prehypertension, stage 1 hypertension, stage 2 hypertension, and stage 3 hypertension. There are many risk factors that can contribute to hypertension, and it is classified as either essential or secondary hypertension. Treatment involves use of several classes of antihypertensive drugs, including diuretics, sympatholytics, beta blockers, calcium channel blockers, ACE inhibitors, and others. These drugs work to lower blood pressure through various mechanisms like reducing fluid volume, decreasing sympathetic nervous system activity, blocking adrenoreceptor sites, and inhibiting the renin

1. ANTIHYPERTENSIVE
DRUGS
Presentation by-
Diksha Kumari
B.pharm 6th sem
22
Gurunanak institute of
pharmaceutical science
and technology

2. Definition-Hypertension is common cardiovascular disease
determined by increase blood pressure (pressure exerted by
blood against the wall of a blood vessel )in arteries.
Normal blood pressure-
120/80 mmHg systolic/diastolic
Symptoms that may occur
include:
•Confusion
•Ear noise or buzzing
•Fatigue
•Headache
•Irregular heartbeat
•Nosebleed
•Vision changes
BP= CO X SVR
BP = Blood pressure
CO =Cardiac output
SVR=Systemic vascular
resistance

3. Category Systolic Blood
Pressure(mmHg)
Diastolic Blood
Pressure(mmHg)
Pre-hypertension 120-139 80
Hypertension – Stage 1 140-159 90-99
Hypertension – Stage 2 160-179 100-109
Hypertension – Stage 3 >180 >110
CATEGORIES OF HYPERTENSION
ACCORDING TO EUROPEAN SOCIETY
OF CARDIOLOGY.

4. Types of
Hypertension
Essential Secondary
A disorder of unknown origin affecting the
Blood Pressure regulating mechanisms
Secondary to other disease processes
RISK FACTORS-
•Hyperlipidaemia –more LDL content
•Tension and stress
•Smoking-more nicotine intake
•Diabetes mellitus
•Imbalance between vasoconstrictor and
vasodilators peptides

5. Treatment-Why???

6. Global Mortality 2000:
Impact of hypertension and other health risk
factors
Adapted from Ezzati et al. Lancet 2002;360:1347–60
Attributable mortality (in millions (total: 55,861,000)
Developing region
Developed region
0 87654321

7. Antihypertensive Drug Therapy

8. DIURETICS :
EXAMPLES:Thiazides: chlorthalidone
High ceiling:Furosemide
K+ sparing:Spironolactone,
MOA: Act on V-2 receptor in kidneys (vasopressin
receptor) having an antediuretic function---- leads
to diuresis----increased secretion of Na & H2O
decrease in blood volume ----decreased CO----
decreased BP.Adverse Reactions
•dizziness,
•electrolyte
imbalance/depletion,
•hypokalemia,
•hyperlipidemia,
•hyperglycemia
(Thiazides)
Contraindications
•hypersensitivity,
•compromised kidney
function
•hyponatremia

9. Central Sympatholytics (a-2
Agonists)Drugs: clonidine, methyldopa
Site of Action:CNS medullary ,cardiovascular
centers
MOA: CNS a-2 adrenergic stimulation----
autoinhibitory feed back mechanism----
decreased sympathetic outflow----decreased
norepinephrine release----vasodilatation----
decreased PR---- decreased BP.Adverse Effect:dry mouth; sedation; drowsiness;nasal
congestion
SYMPATHOLYTIC DRUGS
a-1 Adrenergic blockers (Antagonists)
Drugs:Prazocin,Terazocin
Site of Action: peripheral arterioles, smooth muscle
MOA:Blocks a-1 receptor(in post synaptic neurone as
well as in vascular smooth muscles)---- cause
vasodialatation due to relaxation of vascular smooth
muscles---- decreased PR----also reduces preload by
pooling of blood----decreased CO ---- decreased BP.
Adverse Effects:nausea; drowsiness; postural

10. b -ADRNERGIC BLOCKERS(ANTAGONISTS)
Drugs: Non Selective– Propranolol,Timolol, Pindolol
Cardioselective –Atenolol, Metoprolol(acts only on
beta-1 receptor )
Site of Action: heart,kidney.
MOA: 1.heart:blocks b -1receptor---reduce heart rate ----
decreased CO---- decreased BP
2.kidney:decreased renin production(mediated by b- 1
receptor)----depresses RAS system---- decreased PR----
decreased BP
Advantages:No postural hypotension;No salt and water
retention
Low incidence of side effects
Adverse Effects:impotence; bradycardia; fatigue; exercise
intolerance
Contraindication: asthma;bradycardia;hypersensitivity
b-1
DUAL ALPHA & BETA RECEPTOR ANTAGONISTS
Drugs: Labetalol (3:1 ratio of beta:alpha blocking activity),Carvedilol
IT IS USEFUL IN HYPERTENSIVE EMERGENCIES
VASODIALATOR
Drugs: Arteriolar – Hydralazine
Arterio-venular: Sodium Nitroprusside (USED IN EMERGENCY
SITUATION)
MOA: Releases NO ----stimulation of guanylyl cyclase---- more conversion of
GTP to cGMP-----activate
protein kinase----inhibit MLCK phosphorylation---- myosin
phosphorylation & combination with
actin inhibited----relaxation of vascular smooth muscles----

11. CALCIUM CHANNEL BLOCKERS
(CCBs)Drugs: verapamil ; nifedipine ; diltiazem ;
amlodipine:felodipine
Site of Action- Vascular
smooth muscle
KCaN
a
MOA:Blocks long acting
voltage sensitive calcinm
channels
Advantages:
No sedation or other CNS effects
Can be given to asthma patients &
angina patients
No impairment of renal perfusion
No deleterious effect on uric acid
level& electrolyte
balance
Side effects:
flushing; headache; tachycardia;
peripheral oedema
gastroesophageal reflux
Contraindications:
Congestive heart failure;
Pregnancy and lactation

12. DRUGS ACTING ON RENIN
ANGIOTENSIN SYSTEM
(RAS)1ACE inhibitors: captopril;enalapril;
lisinopril
2 renin inhibitors: Aliskiren; remikinen
3 AT1 receptor antagonists:losartan
;candesartan
1st line of Drug:
No postural hypotension or electrolyte
imbalance (no fatigue or weakness)
Safe in asthmatics and diabetics
Prevention of secondary
hyperaldosteronism and K+ loss
Reverse the ventricular hypertrophy
and increase in lumen size of vessel
No hyperuraecemia or deleterious
effect on plasma lipid profile
Side effects:
Dry cough;
Steep fall in BP with 1st dose
Skin rash
Angioneurotic oedema

14. Reference-
1)Essentials of medical pharmacology sixth edition K.D Tripathi MD
2010. Jaypee brothers medical publishers. Page no-539 to 554.
2)Introduction to pharmacology by S.K kulkarni updated seventh
edition. Page no-286 to 302