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Calcium channel
blockers
Presented by :
KAWALAY STEVEN
 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.
Indications of Calcium Channel
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.
Classification of CCBs
 PHENYLAKYLAMINES
• Verapamil Very
 1,4-DIHYDROPYRIDINES
• Nifedipine , Amlodipine etc… 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 α-1 subunit.
Prevent entry of Ca into cell.
No excitation-coupling reaction in heart and vascular smooth
muscles.
 1,4 dihydopyrimidines
are selective for the
arteriolar beds.
 Phenylalkylamines
and
 benzothiazepines are
selective for the
atrioventricular node.
 Increase the time that Ca2+
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.
 metabolized 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. raynaud’s 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..
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