Isradipine

Indications

Isradipine is used for: Hypertension

Adult Dose

Oral Hypertension 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.

Child Dose

Renal Dose

Administration

May be taken with or without food.

Contra Indications

Cardiogenic shock; recent MI or acute unstable angina; severe aortic stenosis; lactation; porphyria.

Precautions

Hypotension, poor cardiac reserve, heart failure. Pregnancy. Lactation: not known if excreted into breast milk

Pregnancy-Lactation

Pregnancy Category: C Lactation: not known if excreted into breast milk

Interactions

Concurrent admin w/ enzyme-inducing drugs (e.g. rifampicin, phenobarbital, carbamazepine) reduced plasma concentrations of isradipine. Increased bioavailability w/ cimetidine. May increase serum levels w/ CYP3A4 inhibitors (e.g. macrolides, HIV protease inhibitors, azole antifungals, delavirdine).

Adverse Effects

Side effects of Isradipine : >10% Headache (2-22%) 1-10% Edema (1-9%), Dizziness (2-8%), Palpitation (1-5%), Flushing (1-5%), Tachycardia (1-3%), Chest pain (2-3%), Rash (2%), Nausea (1-5%), Vomiting (<1%), Diarrhea (≤ 3%), Weakness (<1%), Dyspnea (1-3%), Urinary frequency (1-3%) <1% Drug-induced gingival hyperplasia, Angioedema, Drowsiness, Hyperhidrosis, Leg pain, Nasal congestion.Drug fever, Dysuria.Impotence, Pruritus, Urticaria, Weight gain, Myocardial infarction

Mechanism of Action

Isradipine is a dihydropyridine Ca 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.