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    Pralidoxime

    Table of Contents > Drugs > Pralidoxime     Print

    Pronunciation
    U.S. Brand Names
    Synonyms
    Generic Available
    Canadian Brand Names
    Use
    Use - Unlabeled/Investigational
    Pregnancy Risk Factor
    Lactation
    Contraindications
    Warnings/Precautions
    Adverse Reactions
    Overdosage/Toxicology
    Drug Interactions
    Stability
    Mechanism of Action
    Pharmacodynamics/Kinetics
    Dosage
    Administration
    Monitoring Parameters
    Reference Range
    Patient Education
    Nursing Implications
    Additional Information
    Anesthesia and Critical Care Concerns/Other Considerations
    Cardiovascular Considerations
    Dental Health: Effects on Dental Treatment
    Dental Health: Vasoconstrictor/Local Anesthetic Precautions
    Mental Health: Effects on Mental Status
    Mental Health: Effects on Psychiatric Treatment
    Dosage Forms
    References
    International Brand Names

    Pronunciation

    (pra li DOKS eem)

    U.S. Brand Names

    Protopam®

    Synonyms

    2-PAM; Pralidoxime Chloride; 2-Pyridine Aldoxime Methochloride

    Generic Available

    No

    Canadian Brand Names

    Protopam®

    Use

    Reverse muscle paralysis caused by toxic exposure to organophosphate anticholinesterase pesticides and chemicals; control of overdose of anticholinesterase medications used to treat myasthenia gravis (ambenonium, neostigmine, pyridostigmine)

    Use - Unlabeled/Investigational

    Treatment of nerve agent toxicity (chemical warfare) in combination with atropine

    Pregnancy Risk Factor

    C

    Lactation

    Excretion in breast milk unknown/not recommended

    Contraindications

    Hypersensitivity to pralidoxime or any component of the formulation; poisonings due to phosphorus, inorganic phosphates, or organic phosphates without anticholinesterase activity; poisonings due to pesticides or carbamate class (may increase toxicity of carbaryl)

    Warnings/Precautions

    Use with caution in patients with myasthenia gravis; dosage modification required in patients with impaired renal function; use with caution in patients receiving theophylline, succinylcholine, phenothiazines, respiratory depressants (eg, narcotics, barbiturates).

    Adverse Reactions

    Frequency not defined.

    Cardiovascular: Tachycardia, hypertension

    Central nervous system: Dizziness, headache, drowsiness

    Dermatologic: Rash

    Gastrointestinal: Nausea

    Hepatic: Transient increases in ALT, AST

    Local: Pain at injection site after I.M. administration

    Neuromuscular & skeletal: Muscle rigidity, weakness

    Ocular: Accommodation impaired, blurred vision, diplopia

    Renal: Renal function decreased

    Respiratory: Hyperventilation, laryngospasm

    Overdosage/Toxicology

    Symptoms of overdose include blurred vision, nausea, tachycardia, and dizziness. Treatment is supportive.

    Drug Interactions

    Decreased effect: Atropine, although often used concurrently with pralidoxime to offset muscarinic stimulation, these effects can occur earlier than anticipated

    Increased effect: Barbiturates (potentiated)

    Increased toxicity: Use with aminophylline, morphine, theophylline, and succinylcholine is contraindicated; use with reserpine and phenothiazines should be avoided in patients with organophosphate poisoning

    Stability

    Store at controlled room temperature of 20°C to 25°C (68°F to 77°F). For I.V. administration, dilute 1 g with 20 mL SWI; solution should be further diluted and administered as 1-2 g in 100 mL NS. If not practical or in cases of fluid overload, may prepare as a 5% solution.

    Mechanism of Action

    Reactivates cholinesterase that had been inactivated by phosphorylation due to exposure to organophosphate pesticides by displacing the enzyme from its receptor sites; removes the phosphoryl group from the active site of the inactivated enzyme

    Pharmacodynamics/Kinetics

    Protein binding: None

    Metabolism: Hepatic

    Half-life elimination: 74-77 minutes

    Time to peak, serum: I.V.: 5-15 minutes

    Excretion: Urine (80% to 90% as metabolites and unchanged drug)

    Dosage

    Organic phosphorus poisoning (use in conjunction with atropine; atropine effects should be established before pralidoxime is administered): I.V. (may be given I.M. or SubQ if I.V. is not feasible):

    Children: 20-50 mg/kg/dose; repeat in 1-2 hours if muscle weakness has not been relieved, then at 8- to 12-hour intervals if cholinergic signs recur

    Adults: 1-2 g; repeat in 1 hour if muscle weakness has not been relieved, then at 8- to 12-hour intervals if cholinergic signs recur. When the poison has been ingested, continued absorption from the lower bowel may require additional doses; patients should be titrated as long as signs of poisoning recur; dosing may need repeated every 3-8 hours.

    Treatment of acetylcholinesterase inhibitor toxicity: Adults: I.V.: Initial: 1-2 g followed by increments of 250 mg every 5 minutes until response is observed

    Nerve agent toxicity management (unlabeled use): Note: Atropine is a component of the management of nerve agent toxicity; consult atropine monograph for specific route and dose. To be effective, pralidoxime must be administered within minutes to a few hours following exposure (depending on the nerve agent).

    Infants and Children:

    Prehospital ("in the field"): Mild-to-moderate symptoms: I.M.: 15 mg/kg; severe symptoms: 25 mg/kg

    Hospital/emergency department: Mild-to-severe symptoms: I.V.: 15 mg/kg (up to 1 g)

    Adults:

    Prehospital ("in the field"): Mild-to-moderate symptoms: I.M.: 600 mg; severe symptoms: 1800 mg

    Hospital/emergency department: Mild-to-severe symptoms: I.V.: 15 mg/kg (up to 1 g)

    Frail patients, elderly:

    Prehospital ("in the field"): Mild-to-moderate symptoms: I.M.: 10 mg/kg; severe symptoms: 25 mg/kg

    Hospital/emergency department: Mild-to-severe symptoms: I.V.: 5-10 mg/kg

    Elderly: Refer to Adults dosing; dosing should be cautious, considering possibility of decreased hepatic, renal, or cardiac function

    Dosing adjustment in renal impairment: Dose should be reduced

    Administration

    I.V.: Infuse over 15-30 minutes at a rate not to exceed 200 mg/minute; may administer I.M. or SubQ if I.V. is not accessible. If a more concentrated 5% solution is used, infuse over at least 5 minutes.

    Monitoring Parameters

    Heart rate, respiratory rate, blood pressure, continuous ECG; cardiac monitor and blood pressure monitor required for I.V. administration

    Reference Range

    Minimum therapeutic concentration: 4 mcg/mL

    Patient Education

    When administered in emergency situation, patient education and instruction should be appropriate to patient condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Breast-feeding is not recommended.

    Nursing Implications

    Monitor heart rate, respiratory rate, blood pressure, continuous ECG

    Additional Information

    Pralidoxime is most effective when given immediately after poisoning. If the poison has been ingested, exposure may continue due to slow absorption from the lower bowel; relapses may occur after initial improvement and treatment may need continued for several days in these patients. In cases of dermal exposure to organophosphate poisoning, clothing should be removed and hair and skin washed with sodium bicarbonate or alcohol as soon as possible.

    Anesthesia and Critical Care Concerns/Other Considerations

    Use I.V. phentolamine for treatment of pralidoxime-induced hypertension (children: 1 mg; adults: 5 mg).

    Cardiovascular Considerations

    Use I.V. phentolamine for treatment of pralidoxime-induced hypertension (children: 1 mg; adults: 5 mg).

    Dental Health: Effects on Dental Treatment

    No significant effects or complications reported

    Dental Health: Vasoconstrictor/Local Anesthetic Precautions

    No information available to require special precautions

    Mental Health: Effects on Mental Status

    May cause dizziness or drowsiness

    Mental Health: Effects on Psychiatric Treatment

    Avoid with phenothiazines; effects of barbiturates may be increased

    Dosage Forms

    Injection, powder for reconstitution, as chloride: 1 g

    References

    de Kort WL, Kiestra SH, and Sangster B, "The Use of Atropine and Oximes in Organophosphate Poisoning: A Modified Approach,"J Toxicol Clin Toxicol, 1988, 26(3-4):199-208.

    Ekins BR and Geller RJ, "Methomyl-Induced Carbamate Poisoning Treated With Pralidoxime Chloride,"West J Med, 1994, 161(1):68-70.

    Farrar HC, Wells TG, and Kearns GL, "Use of Continuous Infusion of Pralidoxime for Treatment of Organophosphate Poisoning in Children,"J Pediatr, 1990, 116(4):658-61.

    Jovanovic D, "Pharmacokinetics of Pralidoxime Chloride. A Comparative Study in Healthy Volunteers and in Organophosphorus Poisoning,"Arch Toxicol, 1989, 63(5):416-8.

    Kurtz PH, "Pralidoxime in the Treatment of Carbamate Intoxication,"Am J Emerg Med, 1990, 8(1):68-70.

    "Medical Management Guidelines (MMGs) for Nerve Agents: Tabun (GA); Sarin (GB); Soman (GD); and VX." Available at: www.atsdr.cdc.gov/MHMI/mmg166.html. Accessed January 8, 2003.

    Medicis JJ, Stork CM, Hoffman RS, et al, "Improved 2-PAM Dosing Regimen in Human Volunteers: A Pharmacokinetic Study,"Vet Hum Toxicol, 1994, 36:377.

    Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings,"Chest, 2003, 123(3):897-922.

    Murphy M and Desai H, "Pralidoxime-Induced Laryngospasm,"Vet Hum Toxicol, 1994, 36:375.

    International Brand Names

    Pralidoxime Chloride® (TH); Protopam® (CA)

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