Lacibloc

Lacidipine.

Each Film-coated Tablet contains: Lacidipine 4 mg, 6 mg.
The main use of calcium-channel blockers is in the management of angina pectoris and hypertension; some are also employed in cardiac arrhythmias.
Calcium-channel blockers, also known as calcium antagonists, calcium-entry blockers, and slow-channel blockers inhibit the cellular influx of calcium which is responsible for maintenance of the plateau phase of the action potential. Thus calcium-channel blockers primarily affect tissues in which depolarization is dependent upon calcium rather than sodium influx, and these include 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.

Pharmacology: Pharmacokinetics: Lacidipine is rapidly but poorly absorbed from the gastrointestinal tract following oral administration and undergoes extensive first-pass metabolism; the bioavailability has been reported to be 2 to 9%, or 18.5% (range 4 to 52%) using a more sensitive assay method. It is more than 95% bound to plasma proteins. Lacidipine is eliminated by metabolism in the liver and metabolites are excreted mainly by the biliary route. About 70% of an oral dose is eliminated in the faeces, the remainder in the urine. The average steady-state terminal elimination half-life of lacidipine is 13 to 19 hours.

It is used in the treatment of hypertension, particularly essential or primary hypertension is widespread and although usually asymptomatic, is a major risk factor for stroke and to some extent ischaemic heart disease.

The usual initial dose is 2 mg daily by mouth increased if necessary after 3 to 4 weeks or more to 4 mg daily; a further increase in dose to 6 mg daily may be necessary in some patients or as prescribed by the physician.

Lacidipine should be used with caution in patients with hypotension, in patients whose cardiac reserve is poor, and in those with heart failure since deterioration of heart failure has been noted. Lacidipine should not be used in cardiogenic shock, in patients who have recently suffered a myocardial infarction, or in acute unstable angina. Lacidipine should not be used to treat an anginal attack in chronic stable angina. In patients with severe aortic stenosis lacidipine may increase the risk of developing heart failure. Sudden withdrawal of lacidipine might be associated with an exacerbation of angina. The dose may need to be reduced in patients with hepatic impairment.

The most common adverse effects of lacidipine are associated with its vasodilator action and often diminish on continued therapy. They include dizziness, flushing, headache, hypotension, peripheral edema, tachycardia, and palpitations. Nausea and other gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain, and mental depression have also occurred. A paradoxical increase in ischaemic chest pain may occur at the start of treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness.

Lacidipine may enhance the antihypertensive effects of other antihypertensive drugs such as beta blockers although the combination is generally well tolerated. Enhanced antihypertensive effects may also be seen with concomitant used of drugs such as aldesleukin and antipsychotics that cause hypotension. Lacidipine may modify insulin and glucose responses and therefore diabetic patients may need to adjust their antidiabetic treatment when receiving Lacidipine. Lacidipine is extensively metabolized in the liver by the cytochrome P450 enzyme system, and interactions may occur other drugs, such as quinidine, sharing the same metabolic pathway, and with enzyme inducers, such as carbamazepine, phenytoin, and rifampicin, and enzyme inhibitors, such as cimetidine and erythromycin.

Store at temperatures not exceeding 30°C.

Calcium Antagonists

C08CA09 - lacidipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.

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