Calcium channel

blockers
Symposium on :
Antihypertensive drugs..
Presented by :
AASHNA DHINGRA
Roll no. 03
Batch 2010
INTRODUCTION

CLASSIFICATION

MECHANISM OF ACTION

PHARMACOLOGICAL
ACTIONS

PHARMACOKINETICS

USES

ADVERSE EFECTS

CONTRAINDICATIONS

SUMMARY

Layout of the presentation :
INTRODUCTION..

also known as calcium antagonists.

prevent calcium from infiltrating the cells of the
heart and blood vessel walls.

relaxes and widens blood vessels of the heart
within the arterial walls, promoting lowered blood
pressure.

may also slow the heart rate, relieve chest
pressure and control an irregular heartbeat.


they are first line antihypertensive drugs.

the onset of antihypertensive action is quick.

monotherapy with CCBs is effective in about
50% of the hypertensives.

can also be used for treating angina.
PHENYLAKYLAMINES
Verapamil
Very

1,4-DIHYDROPYRIDINES
Nifedipine
Nice

BENZOTHIAZEPINES
Diltiazem
Drugs

1,4 dihydopyrimidines are selective for the
arteriolar beds.

The phenylalkylamines and
benzothiazepines are selective
for the atrioventricular node.
Short-acting
nifedipine, dilatiazem, verapamil


Long-acting
amlodipine, felodipine, isradipine,
nicardipine, nisoldipine,
Mechanism of action..
o Calcium channels are of 5 subtypes- L, N, T,
P, and R.

o L-type in cardiac and smooth muscle cells.
Moa :
CCBs block voltage sensitive
L- type Ca channels by binding
to specific site on the -1
subunit.


Prevent entry of Ca into cell.


No excitation-coupling
reaction in heart and vascular
smooth muscles.
Increase the time that Ca
2+
channels
are closed.
Relaxation of the arterial smooth
muscle.
Significant reduction in afterload.
Coronary vasodilatation.
PHARMACOLOGICAL ACTIONS..
PHARMACOKINECTICS..
well absorbed through Git.

first pass metabolism.

highly bound to plasma proteins.

metabolised in liver.

excreted through urine.
USES OF CCBs..
1. angina pectoris - Due to decrease in myocardial oxygen
consumption, and dilatation of coronary arteries.

2. supraventicular arrhythmias - because of its
depressant action on S-A and A-V nodes.

3. hypertension - they control blood pressure by their
vasodilatory effect.

4. Migraine

5. raynauds phenomenon - due to their vasodilatory
property.
ADVERSE EFFECTS..
Postural hypotension
palpitation
reflex tachycardia
edema
dizziness
constipation
sedation
A-V block
headache
fatigue
lowered B.P.
CONTRAINDICATIONS
o Heart failure

o Bradycardia

o Atrioventricular block.

o Dihydropyridine calcium-channel blockers
should not be used in people with uncontrolled
heart failure.
SUMMARY..