 Calcium channel blockers

 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. vmay 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.
 Mechanism of action..
 Calcium channels are of 5 subtypes- L, N, T, P, and R. o L-type in cardiac and smooth
muscle cells.
 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.
10. Ø Increase the time that Ca2+ channels are closed. Ø Relaxation of the arterial
smooth muscle. Ø Significant reduction in afterload. Ø Coronary vasodilatation.

PHARMACOLOGICAL ACTIONS..
11. 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.
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.