SLT INSTITUTE OF PHARMACEUTICAL SCIENCES

GURU GHASIDAS VISHWAVIDYALAYA

DEPARTMENT OF PHARMACY

SEMINAR ON
ANTI-HYPERTENSIVE DRUGS

SUBJECT: ADVANCED MEDICINAL CHEMISTRY

SUBMITTED TO : Dr HARISH RAJAK SIR

SUBMITTED BY : PRIYA TIWARI

M.PHARMA 1ST SEMESTER
ROLL NO: 20703007
ENROLLMENT NO : 06332
 HYPERTENSION
• HYPERTENSION IS A COMMON CVS DISEASE AFFECTING WORLDWIDE POPULATION. A PERSISTENT
AND SUSTAINED HIGH BLOOD PRESSURE HAS DAMAGING EFFECTS ON THE HEART , BRAIN ,
KIDNEYS AND EYES.
• 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.(normal BP
• 120/80
PRIMARY HYPERTENSION
It is other wise known as essential hypertension. It is
characterized by the following:
Primary • Elevation of diastolic BP.
• Normal cardiac output.
Types of • An increase in peripheral resistance.
Hypertension SECONDARY HYPERTENSION
Factors causing secondary hypertension are as follows:
Secondary • Acute or chronic renal disease.
• Hyperaldosteronism.
• Cushing’s syndrome.
• Acromegaly.
• Pheochromocytoma.
• Oral contraceptives, steroids, estrogen, and
sympathomimetics.
CAUSES OF HYPERTENSION RISKS OF HYPERTENTION
 ANTIHYPERTENSIVE
CLASSIFICATION
1. Angiotensin converting enzyme (ACE) inhibitors
Captopril, enalapril , ramipril , lisinopril ,
2. Angiotensin II receptor blockers ACE Inhibitors
Losartan , candesartan , telmisartan
3. Direct renin inhibitors
Aliskiren Angiotensin II
4. Calcium channel blockers Sympatholytics Receptor
blockers
Diltiazem, verapamil , nifedipine , amlodipine ,
5. Diuretics
a) Thiazides – hydrochlorothiazide Antihypertensive On
b) Loop Diuretics – furosemide , bumetanide The basis of
c) Potassium Sparing Diuretics – amiloride , therapeutic action
triamterene
spironolactone
6. Sympatholytics Diuretics
d) Centrally acting – Clonidine , α-methyldopa Direct renin
e) Βeta-Adrenergic blockers- atenolol, metoprolol , esmolol, inhibitors
betaxolol, timolol, propranolol.
Calcium channel
f) Β-Adrenergic blockers with α blocking activity blockers
Labetalol , Carvedilol
d) α adrenergic blockers : prazocin , terazocin

7. Vasodilators – Minoxidil , Hydralazine , Glyceryl trinitrate

 ACE INHIBITORS AND
HYPERTENSION

ACE inhibitors work by interfering with the body's

renin-angiotensin-aldosterone system (RAAS). RAAS is
a complex system responsible for regulating the body's
blood pressure. The kidneys release an enzyme called
renin in response to low blood volume, low salt
(sodium) levels or high potassium levels
1st choice of drug in all grades of hypertension except in bilateral
renal stenosis
Advantages:
1. No electrolyte imbalance (no fatigue or weakness) or postural
hypotension
2. No hyperuricemia or deleterious effect on plasma lipid profile
3. Safe in diabetics and asthmatics
4. performance etc.
 ANGIOTENSIN RECEPTOR
BLOCKERS
Angiotensin II receptor blockers (ARBs) are medications
that block the action of angiotensin II by
preventing angiotensin I from binding
to angiotensin II receptors on the muscles surrounding
blood vessels. As a result, blood vessels enlarge (dilate)
and blood pressure is reduced
But, combination therapy: Total suppression of RAS
1. A-II generate by non ACEW mechanisms – ARBs block
2. ACEIs produce bradykinin related vasodilatation –
CALCIUM CHANNEL
BLOCKERS
Calcium channel blockers lower your blood pressure by
preventing calcium from entering the cells of your heart
and arteries. Calcium causes the heart and arteries to
contract more strongly. By blocking calcium, calcium
channel blockers allow blood vessels to relax and open.

• Verapamil, diltiazem, nifedipine and amlodipine etc.

• advantages:
• No hemodynamic effect – physical work capacity
• No effect on lid profile, uric acid
• They lower BP by decreasing peripheral resistance
without compromising cardiac output
 DIURETICS – MOA
Mechanism of antihypertensive action:
Diuretics help rid your body of sodium and
water. Most work by making your kidneys
release more sodium into the urine. The sodium
then takes water with it from your blood
decreasing the amount of fluid flowing through
your blood vessels hence lowering blood
pressure.
Initially: diuresis- depletion of Na+ and body fluid volume
_decrease in cardiac output
Drugs causing net loss of Na+ and water in urine .
MECHANISM
STRUCTURES
BETA –ADRENERGIC BLOCKERS

• Non selective: Propranolol (others: nadolol timolol, pindolol and

labetolol ) and Cardio selective: Metoprolol (others: atenolol,
acebutalol, esmolol, betaxolol)
• All beta-blockers similar antihypertensive effects:
• Reduction in CO but no change in BP initially but slowly- adaptation
• Beta blockers work by blocking the effects of the
hormone epinephrine, also known as adrenaline. Beta
blockers cause your heart to beat more slowly and with
less force, which lowers blood pressure. Beta
blockers also help open up your veins and arteries to
improve blood flow.
CENTRALLY ACTING ANTIHYPERTENSIVES 
The classic centrally acting antihypertensives such as
clonidine, guanfacine and alpha-methyl-DOPA (via its active
metabolite alpha-methyl-noradrenaline) induce peripheral
sympathoinhibition and a fall in blood pressure as a result of
alpha2-adrenoceptor stimulation in the brain stem

Renin inhibitors
Renin inhibitors are pharmaceutical drugs inhibiting the
activity of renin that is responsible for hydrolyzing
angiotensinogen to angiotensin I, which in turn reducing the
formation of angiotensin II that facilitates blood pressure. ALISKIREN

VASODILATORS
Vasodilators. As the name implies, vasodilator drugs relax
the smooth muscle in blood vessels, which causes the
vessels to dilate. Dilation of arterial (resistance) vessels
leads to a reduction in systemic vascular resistance, which
leads to a fall in arterial blood pressure.
CLASS MECHANISM
ANTIHYPERTENSIVES AVOIDED DURING PREGNANCY

Ace inhibitors
Diuretics
Nonselective beta blockers
Sod nitoprusside

ANTIHYPERTENSIVES SAFE DURING PREGNANCY

Methyldopa
Calcium channel blocker-(not in labour)
Cardiselective beta blocker- atenolol, metoprolol,pindolol
Prazocin and clonidine
THANK YOU