Indications
Diltiazem is indicated in the prophylaxis and treatment of angina pectoris. It is used in the management of classical and vasospastic angina pectoris. It has also been used in the treatment of essential hypertension. It is used for prophylaxis of some selected supraventricular tachyarrhythmias.
Therapeutic Class
Calcium-channel blockers
Pharmacology
Diltiazem hydrochloride is a calcium channel antagonist. It is a peripheral and coronary vasodilator with some negative inotropic activity. Diltiazem inhibits cardiac conduction particularly at the sino-atrial and atrioventricular nodes. Diltiazem has the following actions:Antianginal: A direct dilatation of coronary arteries and arterioles proved oxygen supply to myocardial tissues. In addition dilatation of the peripheral vasculature reduces systemic pressure of cardiac “after load” which results in lessened stress and reduced oxygen requirements of the myocardial tissues.
Antiarrhythmic: The inhibited influx of calcium ions in cardiac tissues result in slowed electrophysiological activity through the S-A and A-V nodes without affecting accessory bypass conduction or altering normal atrial action potential or intraventricular conduction.
Antihypertensive: Reduces peripheral vascular resistance as a result of vasodilatation.
Dosage & Administration
Hypertension: Dosage needs to be adjusted by titration to individual patient needs. When used as monotherapy, usual starting doses are 120 to 240 mg once daily. Maximum antihypertensive effect is usually observed by 14 days of chronic therapy; therefore, dosage adjustments should be scheduled accordingly. The usual dosage range studied in clinical trials was 120 to 540 mg once daily. Current clinical experience with 540 mg dose is limited; however, the dose may be increased to 540 mg once daily.Angina: Dosages for the treatment of angina should be adjusted to each patient’s needs, starting with a dose of 120 mg to 180 mg once daily. Individual patients may respond to higher doses of up to 540 mg once daily. When necessary, titration should be carried out over 7 to 14 days.
Interaction
Diltiazem Hydrochloride should be carefully administered in case of concomitant use with the following drugs.
- Anti-hypertensive agents : effects of anti-hypertensive agents are enhanced
- Propranolol : concentration of propranolol may be increased
- Carbamazepine : plasma level of Carbamazepine may be increased and it may cause Carbamazepine induced toxic symptoms such as sleepiness, nausea, vomiting, vertigo etc.
- Digoxin preparations : plasma level of Digoxin is increased
- Cyclosporin : may increase serum cyclosporin concentration by 75% or more.
Contraindications
Diltiazem Hydrochloride is contraindicated in pregnant women or those of child bearing potential, patients with Sick Sinus syndromes, patients with second or third degree AV block, patients with severe bradycardia and patients who demonstrated hypersensitivity to the drug.
Side Effects
Diltiazem Hydrochloride produces few side effects and these are usually mild. Oedema, nausea, headache, finger swelling, skin rash, dizziness and asthenia have been reported. Other adverse effects include bradycardia, AV block, hypotension, gastrointestinal symptom, hyperactivity with associated psychiatric symptoms and mild elevation of liver function tests.
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