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Antihypertensive:- PPT / PDF

▪ Antihypertensive drugs are defined as the drugs that are used to decrease
 the elevated blood pressure (hypertension).
▪ It is one of the common cardiovascular disorders and it is a state of the
 body in which the systolic blood pressure (BP) is 150 mm Hg or more and
 diastolic BP is 95 mm Hg or more.
(A) Adrenoceptor Blocking Agents:
1) α – Adrenergic Antagonist
a) Piperazinylquinazoline derivatives e.g. Prazosin, Terazosin
b) Imidazoline derivatives e.g. Tolazoline, Phentolamine
2) β – adrenoceptor antagonists e.g. Propranolol, Atenolol, Metoprolol
3) α, β – adrenoceptor antagonists e.g. Labetalol
4) Centrally Acting Agents e.g. Methyldopa, Clonidine, Guanabenz,
5) Agents Depleting Neurotransmitter Stores e.g. Reserpine, Guanethidine,
Guandrel Sulfate
6) Gaglionic Blocking Agents e.g. Pentolinium, Trimethaphan,
Mecamylamine HCl
(B) Agents Acting on Renin-angiotensin system:
1) Angiotensin Converting Enzyme (ACE) Inhibitors e.g. Captopril,
Lisinopril, Enalapril, Benazepril, Quinapril
2) Angiotensin Receptor Antagonist e.g. Losartan, Saralasin
(C) Vasodilators
1) Directly Acting Vasodilators
a) Arterial dilators: e.g. Hydralazine, Dihydralazine, Sodium nitroprusside
b) Potassium Channel agonist: e.g. Minoxidil, Diazoxide
2) Calcium Channel Blockers
a) Alkylamines: e.g. Verapamil
b) Benzothiazepines: e.g. Diltiazem
c) Dihydropyrimidines: e.g. Nifedipine, Felodipine, Amlodipine, Nimodipine
(D) Diuretics
1) Thiazides: e.g Hydrochlorothiazide
2) Loop Diuretics: e.g. Furosemide
3) Potassium Sparing Diuretics: e.g. Triamterene, Spironolactone
(E) 5HT Antagonists e.g. Ketanserine

Benazepril hydrochloride
Methyl dopate Clonidine

Guanethidine monosulphate
Sodium Nitroprusside Diazoxide



Hydralazine hydrochloride
a. The N-ring must contain a carboxylic acid to mimic the C-terminal
carboxylate of ACE substrates.
b. Large hydrophobic heterocyclic rings in the ~N-ring increase potency and
alter pharmacokinetic parameters.
C. Groups A, B, or C can serve as zinc binding groups.
d. The sulfhydryl group shows superior binding to zinc (Phe in carboxylate
and phosphinic acid side chain compensates for sulfhydryl group).
e. Sulfhydryl-containing compounds produce high incidence of skin rash and
taste disturbances.
f. Sulfhydryl-containing compounds can form disulfides, which may shorten
duration of action.
g. Binding to zinc through either a carboxylate or phosphinate mimics the
peptide hydrolysis transition state.
h. Esterification of the carboxylate or phosphinate produces an orally
bioavailable prodrug.
i. X is usually methyl to mimic the side chain of alanine. Within the
dicarboxylate series, when X equals n-butylamine (lysine side chain) this
produces a compound, which is orally active without being a prodrug.
j. Optimum activity occurs when stereochemistry of inhibitor is consistent with
L-amino acid stereochemistry.