Ballicules.com

Phentolamine

REGITINE

What it isShort-acting reversible nonselective alpha-1/alpha-2 antagonist used for acute catecholamine excess and vasopressor extravasation.

Why this oneRapid IV alpha blockade can reverse a catecholamine-driven hypertensive crisis or local ischemia without prolonged postoperative hypotension.

What limits itMarked hypotension and reflex tachycardia can provoke myocardial or cerebral ischemia; avoid when coronary perfusion is tenuous.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Reversal of pharmacologically-induced mydriasisAdult & Pediatric >=12 yr1-2 drops per dilated eye after exam
Reversal of pharmacologically-induced mydriasisPediatric 3-11 yr1 drop per dilated eye after exam

Renal Undefined

Hepatic Undefined

Second drop, if used, is given 5 minutes after the first.

Instructions

Cautions

Adverse reactions

Pregnancy No human data; use only if benefit justifies potential fetal risk.

Lactation No data; weigh benefits of breastfeeding against clinical need.

NO BOXED WARNINGS

Principal riskmarked hypotension with reflex tachycardia and ischemia

Cost, est. cash$20–$1,500/dose or month

Generic entry1998

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

Mechanism of action: Phentolamine ballicule

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

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