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Isradipine

DYNACIRC

What it isVascular L-type calcium-channel blocker; hypertension.

Why this oneParkinson trials were negative, and as an antihypertensive it offers no advantage over longer-acting dihydropyridines.

What limits itPeripheral edema and reflex tachycardia limit use; CYP3A4 interactions can alter exposure.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
HypertensionAdult2.5 mg BIDup to 10 mg/day20 mg/day

Titration Adjust in 5 mg/day increments at 2- to 4-week intervals.

Renal Mild impairment: usual 2.5 mg BID starting dose (AUC increased).

Hepatic Hepatic impairment: usual 2.5 mg BID starting dose (AUC increased).

Little added benefit above 10 mg/day; adverse effects increase above 10 mg/day.

Instructions

Cautions

Adverse reactions

Pregnancy Category C; use only if potential benefit outweighs risk.

Lactation Undefined

NO BOXED WARNINGS

Principal riskPeripheral edema and reflex tachycardia

Cost, est. cash$10–$300/month

Generic entry2006

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger4 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades2 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityHypotension and edema therapeutically; overdose can cause prolonged vasodilatory or cardiogenic shock.

Mechanism of action: Isradipine ballicule

Isradipine ballicule: receptor binding, kinetics and half-life diagram

Open Isradipine in the interactive console ↗

Memory aids: mascots and interaction avatars

Isradipine DYNACIRC mascot mnemonic cartoon
“Is radish dipping Dino circuit?”
Isradipine CYP3A4 substrate avatar
CYP3A4 substrate

Open Isradipine in the interactive console ↗