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cholinesterase

V03AB29

Forms & Strengths

Injectable solution 0.5% (5 mg/mL)
Lyophilized powder for reconstitution 1 mg vials
Intramuscular suspension 1 mg/mL
Available as sterile ampoules 2 mL
Stored at 2‑8°C, protected from light

Adult Dosing

Organophosphate poisoning: 2–4 mg/kg IV over 30 min, repeat every 6‑8 h as needed
Severe carbamate toxicity: 1–2 mg/kg IM once, may repeat after 12 h
Maximum single dose 500 mg IV
Do not exceed 1 g per 24 h
Dose adjustment for renal impairment not required

Pediatric Dosing

Mild to moderate poisoning: 0.5–1 mg/kg IV over 30 min
Severe poisoning: up to 2 mg/kg IV, repeat q6‑8 h
Maximum total daily dose 50 mg in children <12 kg
Weight‑based dosing recommended; round to nearest 0.5 mg
Use with caution in infants <6 months

Indications

Acute organophosphate poisoning
Carbamate insecticide toxicity
Pre‑exposure prophylaxis for high‑risk occupational exposure
Adjunct in reversal of neuromuscular blockade (rare)
Diagnostic assay for plasma cholinesterase activity

Mechanism of Action

Provides exogenous cholinesterase that hydrolyzes acetylcholine and organophosphate agents
Acts as a bioscavenger, binding and detoxifying phosphorylated cholinesterase inhibitors
Restores normal cholinergic neurotransmission by decreasing acetylcholine excess
Rapidly reduces systemic organophosphate concentration

Contraindications

Known hypersensitivity to cholinesterase preparation
Active cholinergic crisis with severe bradycardia or asystole
Uncontrolled asthma or severe bronchospasm
Pregnancy only if benefit outweighs risk
Concurrent use of high‑dose anticholinergic agents

Adverse Reactions

Bradycardia and hypotension
Excess salivation, lacrimation, and rhinorrhea
Bronchospasm and increased airway resistance
Abdominal cramps, nausea, diarrhea
Local irritation at IM injection site

Drug Interactions

Additive cholinergic effects with other cholinesterase inhibitors (e.g., pyridostigmine, physostigmine)
May blunt effects of anticholinergic drugs (e.g., atropine, scopolamine)
Beta‑blockers can exacerbate bradycardia
Concurrent use with succinylcholine may prolong neuromuscular blockade
CYP450 substrates generally unaffected; monitor clinical response

Curated Content: Needs Vetting Before Put to Clinical Use