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Pentamidine

PENTAM

What it isMacromolecular-biosynthesis inhibitor used IV for Pneumocystis treatment or inhaled for prophylaxis when preferred drugs fail.

Why this oneInhalation offers non-sulfonamide prophylaxis with less systemic exposure, while IV treatment reaches established disease.

What limits itParenteral use can cause fatal hypotension, dysglycemia, pancreatitis, renal injury, and arrhythmia; inhaled drug misses extrapulmonary sites.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Prevention of Pneumocystis jiroveci pneumoniaadult300 mg once every 4 weeks (nebulized)

Renal Undefined

Hepatic Undefined

Single 300 mg dose repeated every 4 weeks.

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Pregnancy Category C - no adequate human studies; use only if clearly needed.

Lactation Undefined

⚠ BOXED WARNING

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

Generic entry1992

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades3 / 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: Pentamidine ballicule

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

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