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Dihydropyridine Calcium Channel Blockers

Calcium channel blockers inhibit the influx of calcium ions responsible for maintaining the plateau phase of the action potential in cells like vascular smooth muscle, heart muscle, and sinus and atrioventricular nodes. They cause dilation of coronary and peripheral arteries with little effect on veins, reduce heart rate and conduction velocity, and have a negative inotropic effect. Individual drugs have different selectivities and uses depending on their effects in tissues and on baroreceptor reflexes. Dihydropyridines like nifedipine selectively dilate blood vessels with little effect on heart rate or contractility, while diltiazem and verapamil also slow conduction and are used to treat arrhythmias as well as angina and hypertension.

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76 views4 pages

Dihydropyridine Calcium Channel Blockers

Calcium channel blockers inhibit the influx of calcium ions responsible for maintaining the plateau phase of the action potential in cells like vascular smooth muscle, heart muscle, and sinus and atrioventricular nodes. They cause dilation of coronary and peripheral arteries with little effect on veins, reduce heart rate and conduction velocity, and have a negative inotropic effect. Individual drugs have different selectivities and uses depending on their effects in tissues and on baroreceptor reflexes. Dihydropyridines like nifedipine selectively dilate blood vessels with little effect on heart rate or contractility, while diltiazem and verapamil also slow conduction and are used to treat arrhythmias as well as angina and hypertension.

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Calcium channel blockers

Calcium-channel blockers, (calcium antagonists, calcium-entry blockers, or slowchannel blockers) inhibit the cellular influx of calcium that is responsible for maintenance of the plateau phase of the action potential. Thus calcium-channel blockers mainly affect tissues in which depolarisation is dependent upon calcium rather than sodium influx, such as vascular smooth muscle, myocardial cells, and cells within the sino-atrial (SA) and atrioventricular (AV) nodes. The main actions of the calcium-channel blockers include dilatation of coronary and peripheral arteries and arterioles with little or no effect on venous tone, a negative inotropic action, reduction of heart rate, and slowing of AV conduction. However, the effects of individual drugs, and therefore their uses, are modified by their selectivity of action at different tissue sites and by baroreceptor reflexes. Dihydropyridine calcium-channel blockers (such as nifedipine) act on slow, L-type (long) channels. They have a greater selectivity for vascular smooth muscle than for myocardium and therefore their main effect is vasodilatation. They are non-ratelimiting, with little or no action at the SA or AV nodes, and negative inotropic activity is rarely seen at therapeutic doses. They are used for their antihypertensive and antianginal properties. Some dihydropyridine derivatives, for example nimodipine, cross the blood-brain barrier and are used in cerebral ischaemia. Benzothiazepine calcium-channel blockers (such as diltiazem) and phenylalkylamine calcium-channel blockers (such as verapamil) also act on L-type channels, but they have less selective vasodilator activity than dihydropyridine derivatives. They are classed as rate-limiting and have a direct effect on myocardium, causing depression of SA and AV nodal conduction. They are used for supraventricular arrhythmias as well as angina and hypertension.

NIFEDIPINE

United Kingdom: Adalat; Adipine; Coracten

AMLODIPINE

United Kingdom: Amlostin;

VERAPAMIL

United Kingdom: Half Securon; Securon; Univer;

DILTIAZEM (Benzothiazepine)

United Kingdom: Adizem; Angitil; Tildiem; Viazem;

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