Pramipexole

Allopathic
Indications
  • Organophosphate poisoning: Treatment of poisoning due to organophosphate insecticides and nerve agents by reactivating inhibited acetylcholinesterase.
  • Adjunct to atropine: Used alongside atropine to reverse muscarinic and nicotinic symptoms of organophosphate toxicity.
  • Carbamate poisoning: Occasionally indicated, though efficacy varies.
  • Chemical warfare exposure: Emergency antidote for nerve agent poisoning.
Dosage & Administration
  • Adults:
    Initial dose of 1–2 grams intravenously over 15 to 30 minutes. Repeat doses of 0.5–1 gram every 1–2 hours if necessary or continuous infusion of 500 mg/hour for 24–48 hours based on clinical response.
  • Pediatrics:
    20–50 mg/kg IV over 15–30 minutes, repeated as needed.
  • Elderly:
    Standard dosing with close monitoring.
  • Route: Intravenous preferred; intramuscular if IV access unavailable.
  • Duration: Until symptoms resolve and acetylcholinesterase activity is restored.
  • Dose adjustment: No specific recommendations for renal/hepatic impairment; monitor clinically.
Mechanism of Action (MOA)

Pralidoxime chloride reactivates acetylcholinesterase by cleaving the phosphate bond formed between the enzyme and the organophosphate toxin. This restores enzymatic function, allowing acetylcholine breakdown at synapses. The resulting decrease in acetylcholine reverses muscle weakness, respiratory paralysis, and other cholinergic toxic effects.

Pharmacokinetics
  • Absorption: Rapid following IV or IM administration.
  • Distribution: Widely distributed in extracellular fluid; poor penetration of blood-brain barrier.
  • Metabolism: Minimal.
  • Elimination: Primarily renal excretion unchanged.
  • Onset: Within minutes after IV administration.
  • Half-life: Approximately 1–2 hours.
Pregnancy Category & Lactation
  • Pregnancy: FDA Category C. Use only if benefits outweigh risks.
  • Lactation: Unknown excretion; use with caution.
Therapeutic Class
  • Cholinesterase reactivator
  • Antidote for organophosphate poisoning
Contraindications
  • Hypersensitivity to pralidoxime chloride or components.
  • Caution in myasthenia gravis.
  • Severe renal impairment (use with caution).
Warnings & Precautions
  • May cause muscle weakness or respiratory distress if administered rapidly.
  • Monitor cardiovascular status (hypertension, tachycardia).
  • Early administration critical; ineffective after aging of enzyme-toxin complex.
  • Monitor renal function during therapy.
Side Effects
  • Common: Dizziness, headache, blurred vision, nausea, flushing, tachycardia.
  • Rare but serious: Hypertension, laryngospasm, muscle rigidity, respiratory failure.
  • Side effects may be dose and infusion rate dependent.
Drug Interactions
  • Synergistic with atropine.
  • Additive muscle weakness with neuromuscular blockers.
  • No known CYP450 interactions.
Recent Updates or Guidelines
  • Early administration emphasized in organophosphate poisoning management.
  • Continuous infusion suggested for severe cases.
Storage Conditions
  • Store at 20°C to 25°C (68°F to 77°F).
  • Protect from light and moisture.
  • Keep vial tightly closed.
  • Do not freeze.