This document discusses several cardiovascular drugs, including their chemistry, mechanisms of action, and therapeutic uses. It describes hydralazine as a vasodilator that acts on resistance arterioles to lower blood pressure. Propranolol is a beta-blocker that competitively blocks beta-1 receptors in the heart to reduce its workload and rate. Procainamide is a sodium channel blocker used to treat arrhythmias by slowing conduction and prolonging the action potential. Prenylamine is a calcium channel blocker and vasodilator formerly used to treat angina by decreasing sympathetic stimulation of the heart.

1. Bangabandhu Sheikh Mujibur Rahman Science and Technology
University
A Presentation on Cardiovascular Drug
Presented By
Md. Shimul Bhuia
Department of Pharmacy
Course Title: Medicinal Chemistry-II
Course Code: PHR303

2. Introduction of Cardiovascular drug
• Cardiovascular drug, any agent that affects
the function of the heart and blood vessels.
Drugs that act on the cardiovascular system
are among the most widely used
in medicine. Examples of disorders in which
such drugs may be useful
include hypertension (high blood
pressure), angina pectoris (chest pain
resulting from inadequate blood flow
through the coronary arteries to the heart
muscle), heart failure(inadequate output of
the heart muscle in relation to the needs of
the rest of the body),
and arrhythmias (disturbances of cardiac
rhythm).

3. Classification of Cardiovascular Drug
Anticoagulants (warfarin and heparin)
ACE Inhibitors (Captopril)
Angiotensin II Receptor Blockers (Losartan)
Beta Blockers (propranolol)
Calcium Channel Blockers (Nifedipine)
Cholesterol-lowering medications (lovastatin)
Digitalis Preparations
Diuretics (hydrochlorothiazide)
Vasodilators (hydralazine)

4. Chemistry of hydralazine
• Hydralazine belongs
to the
hydrazinophthalazine
class of drugs
• Chemical name: 1-
Hydrazinophthalazine

5. Synthesis of Hydralazine

6. Mechanism action of hydralazine
• It is a direct-acting smooth
muscle relaxant and acts as
a vasodilator primarily
in resistance arteriole. By
relaxing vascular smooth muscle,
vasodilators act to
decrease peripheral resistance,
thereby lowering blood
pressure and decreasing afterload.

7. Therapeutic uses of hydralazine
• Used to treat severe essential hypertension
• often used to treat hypertension in pregnancy, with methyldopa
• To prevent heart attacks, stocks and kidney problems
• To treat heart failure (in combination with beta-blockers)
• Used to treat congestive heart failure (in combination with isosorbide
dinitrate)

8. Chemistry of Propranolol
• Generic Name: Propranolol
• IUPAC Name: 1-
naphthalen-1-yloxy-3-
(propan-2-ylamino)propan-
2-ol
• Type: Beta-blocker

9. SYNTHESIS OF PROPRANOLOL

10. Mechanism of action of propranolol
• Propranolol is a competitive antagonist of beta-1-
adrenergic receptors in the heart. It competes
with sympathomimetic neurotransmitters for
binding to receptors, which inhibits sympathetic
stimulation of the heart. Blockage of
neurotransmitter binding to beta 1 receptors on
cardiac myocytes inhibits activation of adenylate
cyclase, which in turn inhibits cAMP synthesis
leading to reduced PKA production. This results in
less calcium influx to cardiac myocytes through
voltage gated L-type calcium channels meaning
there is a decreased sympathetic effect on
cardiac cells

11. THERAPEUTIC USES OF PROPRANOLOL
• Treat high blood pressure
• Control heart rhythm in atrial fibrillation
• Relieve angina
• Prevent migrations
• Reduce essential tremor
• Help with medical conditions involving thyroid and adrenal glands

12. Chemistry of Procainamide
• Procainamide is a medication of the anti
arrhythmic class used for the treatment of cardiac
arrhythmias
• it is a sodium channel blocker of cardiomyocytes.
• Procainamide is structurally similar to procaine,
but in place of an ester group, procainamide
contains an amide group. This susubstitution is
the reason why procainamide exhibits a longer
half-life time than procaine.
• Chemical formula C13-H21-N3-O
• IUPAC Name: 2-(diethylamino)ethyl 4-
aminobenzoate

13. Procainamide: Synthesis

14. Procainamide:
Mechanism
Blocks sodium channels , slows
the upstrok of the action
potential, slows conduction,
prolongs the QRS.
It also prolongs the action
potential duration by blockade
of potassium channels.
 Has direct depressant action
on SA and AV nodes.
Extracardiac effect: It has
ganglion-blocking properties..

15. Procainamide: Therapeutic Uses
Used for treating ventricular arrhythmias;
Ventricular ectopy;
Tachycardia;
Supraventricular tachycardia;
Atrial fibrillation (abnormal heart rhythm
characterized by rapid and irregular beating);
SVT with aberrancy;
Pre-excitation syndromes.

16. Chemistry of Prenylamine
• Prenylamine (Segontin) is
a calcium channel blocker of
the amphetamine chemical
class which was used as
a vasodilator in the treatment
of angina pectoris
• IUPAC Name: 3,3-diphenyl-N-(1-
phenylpropan-2-yl)propan-1-
amine

18. Mechanism action of prenylamine
Prenylamine has two primary molecular target in
human, Calmodulin and Myosin light-chain kinase 2 found in skeletal
and cardiac muscle. Pharmacologically, it decreases the sympathetic
stimulation on cardiac muscle predominantly through partial depletion
of catecholamine via competitive inhibition of reuptake by storage
granule, which lead to further depletion due to spontaneous leakage as
a result of disturbance of equilibrium
Resulting- CO, HT, Vasodilation

20. Thank you