This document discusses hypertension and antihypertensive drugs. It defines hypertension as a blood pressure higher than 140/90 mmHg. Lifestyle factors like smoking, alcohol, diet and stress can cause primary hypertension. Common antihypertensive drug classes include diuretics, beta blockers, ACE inhibitors, calcium channel blockers, and angiotensin receptor blockers. Propranolol is provided as an example beta blocker drug, and its mechanism and structure-activity relationships are described.

1. Pratiksha Mishra
Pharmaceutical
Chemistry Department
M.J.B.Govt.Girl’s
P.G.College,Indore

2.  Anti-hypertensive are class of drugs that are
used to treat hypertension. Anti-hypertensive
therapy seeks to prevent the complication of
high blood pressure, such as stroke and
myocardial infarction.
 Hypertension is known as silent killer.
 Hypertension is defined as either a sustained
systolic blood pressure of greater than 140mmHg
or sustained diastolic blood pressure of greater
than 90mm Hg.
 Normal blood pressure—120/80mm Hg
 Where, 120 is systolic blood pressure
80 is diastolic blood pressure

3. The arterial blood pressure
fluctuates with each contraction of
heart. The maximum arterial
pressure resulting from ventricular
contraction is called as SYSTOLIC
BLOOD PRESSURE. During the
relaxation of cardiac cycle, the
pressure falls. This lower is called
DIASTOLIC BLOOD PRESSURE.

4. Systolic/Diastolic
Pressure
(mm Hg)
Category
<120/80 Normal
120-135/80-89 Pre-hypertension
≥140/90 Hypertension
140-159/90-99 Stage 1
≥160/100 Stage 2

5. When there is no specific reason for high blood
pressure it is referred as primary
hypertension or essential hypertension.
 Age
 Smoking
 Drinking large amount of alcohol
 High amount of salt in diet
 Overweight
 Lack of exercise
 Stress
 Family history of blood pressure

6.  Kidney disease
 Narrowing of arteries
 Hormonal imbalance like Cushing’s disease
and primary aldosteronism
(Hyperaldosternoism)
 Recreational drugs(cocaine etc)
 Oral contraceptives, steroids, estrogen and
sympathomimetics

7.  In patients with mild elevation in blood
pressure, non pharmacological treatment
methods may be applicable. These treatment
method may include.
 Stop smoking
 Lose weight
 Moderate alcohol consumption
 Exercise
 Reduce salt intake
 Reduce stress

8.  Diuretics
 Thiazides and related agents Ex. Hydrochlorthiazide
 Loop diuretics Ex. Ethacrynic acid & Frusemide
 Potassium sparing diuretics Ex. Spiranolactone
 Sympatholytics drugs
 Centrally acting agents Ex. Methyl dopa
 Ganglion blocking agent Ex. Hexamethonium bromide
 Adrenergic neuron blocking agent Ex. Guanthidine
 β-adrenoreceptor blocker Ex.Atenolol,Propanolol
 α-adrenoreceptor blocker Ex. Prazosin
 α+β blocker Ex.Labetalol

9.  Vasodilators
 Arterial Ex.Hydrazaline
 Arterial and Venous Ex Nitroprusside
 Calcium channel blocker Ex. Amlodipne &
Verapamil
 Angiotensin converting enzyme inhibitor
Ex. Captopril
 Angiotensin II receptor blocker Ex.Lostran
 Potassium channel opener Ex. Pinacidil

10. It is used as anti-hypertensive
agent.
It suppresses ventricular
tachycarrrdia.
It is used as anti-arrhythmic
agent.
It is also used to treat essential
hypertension

12.  It is an β adrenoreceptor blocker or
antagonist. It usually inhibit action of
catecholamine.
 Propanolol also has an anti-renin effect.

13.  The O-CH2 group between aromatic ring and
ethylamino side chain is responsible for the
antagonistic activity.
 Converting the aromatic portion to phenathrene
or anthracene decreases activity.
 Nitrogen atom should be secondary amine for
optimum activity.
 Replacement of ethereal oxygen in
aryloxypropanolamines with –S,-CH2 or –NCH3
decreases β activity.
 Alpha methyl group at side chain decreases
activity.

14.  Cyclic alkyl substituent are better than
corresponding open chain substituent at
nitrogen atom of amine.
 The two carbon side chain is essential for the
activity.
 The most effective substituent at amino
group is isopropyl and tert-butyl group.
 The aryloxypropanolamines are more potent
than arylethanolamines
 The carbon side having hydroxyl group must
be S-configuration for optimum affinity to β
receptor.

16. ANGIOTENSINOGEN
RENIN
ANGIOTENSIN I VASOCONSTRICTION
ACE
SYMPATHETIC ACTIVITY
ANGIOTENSIN II
ADRENAL GLAND
ALDOSTERONE
KIDNEY

17.  The N- ring portion must contain a carboxyl
group.
 Large heterocyclic ring in N- ring increases
potency.
 Sulfhydryl, carboxylate or phosphinate group
can serve as Zn binding group.
 –SH group shows superior binding to Zn ion.
 Duration of action of such compound is
shorter.
 Instead of methyl substituted with n-butyl
produces an orally active drug.

18. It is used as Anti-hypertensive
Agent.
It is used in the treatment of
Congestive Heart Failure.
It is used in diabetic neuropathy.