Pralidoxime

Indications
 Parenteral
Organophosphorus poisoning
Adult: Used in combination with atropine. Admin atropine via IM/IV inj and repeat as needed until patient shows signs of atropine toxicity. Maintain atropinisation for at least 48 hr. As soon as the effects of atropine are observed, 1-2 g of pralidoxime (chloride, iodide or mesilate) may be given via IM/IV inj. Repeat dose after 1 hr, then every 8-12 hr, if necessary. In severe poisoning, continuous infusion of 200-500 mg/hr may be given, titrated according to response. Alternatively, pralidoxime chloride may be given at an initial dose of 30 mg/kg via IV infusion over 20 minutes or IV inj over 5 minutes, followed by IV infusion at 8 mg/kg/hr. Max: 12 g/24 hr.
Child: As mesilate: 20-60 mg/kg.
Renal impairment: Dose adjustment may be required.

Special Populations: In both adults and children, atropine might have to be injected frequently to relieve resp depression. Full resuscitative measures should be always utilized.
Contraindications
 Carbamate pesticide poisoning, hypersensitivity.
Warnings / Precautions
 Renal dysfunction, myasthenia gravis. Atropinisation may occur faster when atropine and pralidoxime are used together. Pregnancy, lactation.
Adverse Reactions
 Drowsiness, dizziness, visual disturbances, nausea, tachycardia, headache, hyperventilation and muscle weakness.
Potentially Fatal: Rapid admin causes tachycardia, laryngospasm and rigidity. Large doses cause neuromuscular blockade.
Drug Interactions
 Potentially Fatal: Potentiates toxicity by carbamate pesticides.
See Below for More pralidoxime Drug Interactions
Lab Interactions
 May interfere with estimation of acetylcholinesterase activity using acetylcholine reagent.
Mechanism of Actions
 Pralidoxime reactivates cholinesterase outside the CNS which has been inactivated by phosphorylation due to organophosphate pesticide exposure-resulting. This leads to the destruction of acetylcholine at the neuromuscular junction thus relieving muscle paralysis. It also removes the phosphyl group from the active site of inactivated enzyme which is dependent on the nature of the phosphyl group.
Distribution: Not bound and does not readily penetrate the CNS.
Excretion: Via urine (rapid; as unchanged and partly as metabolites); 1-3 hr (elimination half-life).
Storage Conditions
 Parenteral: Store at 20-25°C.
ATC Classification
 V03AB04 - pralidoxime ; Belongs to the class of antidotes. Used in the management of organo-phosphate poisoning.
Storage
 Parenteral: Store at 20-25°C.
Available As
  • Pralidoxime 1000 mg
  • Pralidoxime Iodide 25 mg
  • Pralidoxime 500 mg

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