Dimercaprol

BAL

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Dimercaprol ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Dimercaprol ballicule

What it isDithiol chelator; arsenic, mercury, gold and lead poisoning.

Why this oneIt is the chelator for arsenic and inorganic mercury, where oral agents fail.

What limits itPainful intramuscular injection in peanut oil, and it redistributes some metals to the brain. Hypertension and fever.

Dimercaprol molecular structure (skeletal formula) — Molecular structure: Dimercaprol

FDA label

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FDA dosing	Population	Start
Mild arsenic or gold poisoning	All	2.5 mg/kg IM QID ×2 days, then BID on day 3, then QD ×10 days
Severe arsenic or gold poisoning	All	3 mg/kg IM q4h ×2 days, QID on day 3, then BID ×10 days
Mercury poisoning	All	5 mg/kg IM initially, then 2.5 mg/kg QD–BID ×10 days
Acute lead encephalopathy	All	4 mg/kg IM first dose alone, then q4h with edetate calcium disodium at a separate site (3 mg/kg after first dose if less severe)

Renal Discontinue or use only with extreme caution if acute renal insufficiency develops during therapy.

Hepatic Contraindicated in most instances of hepatic insufficiency (exception: post-arsenical jaundice).

Instructions

By deep intramuscular injection only
Begin injections at the earliest possible moment; use adequate amounts at frequent intervals
Inspect visually for particulate matter and discoloration before administration
Use with other supportive measures
Treatment maintained for 2 to 7 days for acute lead encephalopathy depending on clinical response

Available strengths

inj 10 %

Contraindications

Hepatic insufficiency, in most instances (exception: post-arsenical jaundice)
Discontinue or use with extreme caution if acute renal insufficiency develops during therapy

Cautions

Dose-related rise in blood pressure accompanied by tachycardia
Febrile reactions and other dose-dependent symptoms with higher doses
Discontinue/use extreme caution if acute renal insufficiency develops

Adverse reactions

Rise in blood pressure with tachycardia
Nausea and vomiting
Headache
Burning sensation in lips/mouth/throat
Feeling of constriction or pain in throat/chest/hands
Conjunctivitis, lacrimation, rhinorrhea, salivation
Tingling of hands, sweating
Painful sterile abscesses; anxiety/weakness

Pregnancy Pregnancy Category C; use only if clearly needed.

Lactation Unknown whether excreted in human milk; exercise caution in nursing women.

Cost

Dimercaprol (BAL)

Strength		#/mo	generic $/unit	CostPlus
10 %	inj	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Dimercaprol is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskPainful injection; it can redistribute metal to the brain

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Legacy pregnancy categoryC

Defining liabilityNephrotoxicity, painful injections, hypertension and G6PD-related hemolysis

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