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Icatibant

FIRAZYR

What it isSelective bradykinin B2 receptor antagonist; acute attacks of hereditary angioedema.

Why this oneIt blocks the mediator directly, so it works in the bradykinin-mediated angioedema that antihistamines, steroids and epinephrine do not touch.

What limits it⚑ That distinction is the teaching point: ACE-inhibitor and hereditary angioedema are bradykinin-mediated, and the usual anaphylaxis drugs fail. Self-injected subcutaneously; injection-site reactions are near-universal.

FDA label

FDA dosingPopulationStartTargetMax
Acute attacks of hereditary angioedema (HAE)Adults (≥18 yr)30 mg SC (abdominal area) at attack onset30 mg SC; may repeat if response inadequate or symptoms recur (≥6 h apart)3 doses (90 mg) SC per 24 h

Renal No adjustment needed

Hepatic No adjustment needed

Repeat doses at intervals of at least 6 h; no more than 3 doses in any 24-h period

Instructions

Cautions

Adverse reactions

Pregnancy Human data have not identified drug-associated risk of birth defects or miscarriage; animal studies showed premature birth/abortion (rabbits) and delayed parturition/fetal death (rats) at low multiples of MRHD

Lactation No human data; present in rat milk, but systemic absorption in infant via breast milk not expected — weigh benefits against risk

NO BOXED WARNINGS

Principal riskInjection-site reactions; it does not treat histaminergic angioedema

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: Icatibant ballicule

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

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