INTRODUCTION
CLASSIFICATION
MECHANISM OF ACTION
PHARMACOLOGICAL ACTIONS
PHARMACOKINETICS
USES
ADVERSE EFECTS
CONTRAINDICATIONS
SUMMARY
Layout of the presentation :
3.
INTRODUCTION..
also known ascalcium 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.
4.
Indications of CalciumChannel
Blockers
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.
5.
Classification of CCBs
PHENYLAKYLAMINES
• Verapamil Very
1,4-DIHYDROPYRIDINES
• Nifedipine , Amlodipine etc… Nice
BENZOTHIAZEPINES
• Diltiazem Drugs
6.
1,4 dihydopyrimidinesare
selective for the arteriolar
beds.
The phenylalkylamines and
benzothiazepines are
selective for the
atrioventricular node.
Mechanism of action..
oCalcium channels are of 5 subtypes- L, N, T, P, and R.
o L-type in cardiac and smooth muscle cells.
9.
Moa :
CCBs blockvoltage sensitive L- type Ca channels by binding to
specific site on the α-1 subunit.
Prevent entry of Ca into cell.
No excitation-coupling reaction in heart and vascular smooth
muscles.
11.
1,4 dihydopyrimidines
areselective for the
arteriolar beds.
Phenylalkylamines
and
benzothiazepines are
selective for the
atrioventricular node.
12.
Increase thetime that Ca2+
channels are closed.
Relaxation of the arterial smooth muscle.
Significant reduction in afterload.
Coronary vasodilatation.
PHARMACOLOGICAL ACTIONS..
13.
PHARMACOKINECTICS..
well absorbedthrough GIT.
first pass metabolism.
highly bound to plasma proteins.
metabolized in liver.
excreted through urine.
14.
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. raynaud’s phenomenon - due to their vasodilatory property.
CONTRAINDICATIONS
o Heart failure
oBradycardia
o Atrioventricular block.
o Dihydropyridine calcium-channel blockers should not
be used in people with uncontrolled heart failure.