Isradipine
Indications
Isradipine is indicated in the management of hypertension. It may be used alone or concurrently with thiazide-type diuretics.
Pharmacology
Isradipine is a dihydropyridine Calcium channel blocker. It prevents Ca++ ions from entering the slow channels or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarisation, producing a relaxation of coronary vascular smooth muscle and coronary vasodilation.
Dosage & Administration
Adult: Initially, 2.5 mg bid, increase if necessary after 3-4 wk to 5 mg bid, or 10 mg bid as required.
Elderly: Initially, 1.25 mg bid. Maintenance: 2.5 or 5 mg once daily.
Hepatic Impairment: Initially 1.25 mg bid. Maintenance: 2.5 or 5 mg once daily.
May be taken with or without food.
Elderly: Initially, 1.25 mg bid. Maintenance: 2.5 or 5 mg once daily.
Hepatic Impairment: Initially 1.25 mg bid. Maintenance: 2.5 or 5 mg once daily.
May be taken with or without food.
Interaction
Concurrent admin with enzyme-inducing drugs (e.g. rifampicin, phenobarbital, carbamazepine) reduced plasma concentrations of isradipine. Increased bioavailability with cimetidine. May increase serum levels with CYP3A4 inhibitors (e.g. macrolides, HIV protease inhibitors, azole antifungals, delavirdine).
Contraindications
Cardiogenic shock, within 1 mth of MI, unstable angina, treatment of hypertensive crisis.
Side Effects
Headache, dizziness, palpitations, tachycardia, peripheral oedema, flushing, dyspnoea, abdominal discomfort, rash, pruritus, polyuria, fatigue, malaise.
Pregnancy & Lactation
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus
Precautions & Warnings
Patients with CHF, severe aortic stenosis, hypertrophic cardiomyopathy with outflow tract obstruction. Hepatic impairment. Pregnancy and lactation.
Overdose Effects
Symptoms: Excessive peripheral vasodilation with subsequent marked and prolonged systemic hypotension and tachycardia.
Management: Symptomatic and supportive treatment. Emesis, gastric lavage, admin of activated charcoal followed in 30 min by a saline cathartic. A vasoconstrictor (e.g. epinephrine) may be useful in restoring normotensive state. Refractory hypotension or AV conduction disturbances may be treated with IV Ca salts or glucagon.
Management: Symptomatic and supportive treatment. Emesis, gastric lavage, admin of activated charcoal followed in 30 min by a saline cathartic. A vasoconstrictor (e.g. epinephrine) may be useful in restoring normotensive state. Refractory hypotension or AV conduction disturbances may be treated with IV Ca salts or glucagon.
Therapeutic Class
Calcium-channel blockers
Storage Conditions
Store below 30° C.