Protopam Chloride Drug Information
Generic name: PRALIDOXIME CHLORIDE
Uses of Protopam Chloride
Chloride is indicated as an antidote: in the treatment of poisoning due to those pesticides and chemicals (e.g., nerve agents) of the organophosphate class which have anticholinesterase activity and in the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis. The principal indications for the use of PROTOPAM Chloride are muscle weakness and respiratory depression. In severe poisoning, respiratory depression may be due to muscle weakness.
Dosage & Administration of Protopam Chloride
| < 40 kg | 15 mg/kg |
|---|---|
| ≥ 40 kg | Use Adult Dosing Recommendations |
Side Effects of Protopam Chloride
Forty to 60 minutes after intramuscular injection, mild to moderate pain may be experienced at the site of injection. Pralidoxime chloride may cause blurred vision, diplopia and impaired accommodation, dizziness, headache, drowsiness, nausea, tachycardia, increased systolic and diastolic blood pressure, hyperventilation, and muscular weakness when given parenterally to normal volunteers who have not been exposed to anticholinesterase poisons. In patients, it is very difficult to differentiate the toxic effects produced by atropine or the organophosphate compounds from those of the drug.
Elevations in SGOT and/or SGPT enzyme levels were observed in 1 of 6 normal volunteers given 1200 mg of pralidoxime chloride intramuscularly, and in 4 of 6 volunteers given 1800 mg intramuscularly. Levels returned to normal in about 2 weeks. Transient elevations in creatine phosphokinase were observed in all normal volunteers given the drug.
When atropine and pralidoxime chloride are used together, the signs of atropinization may occur earlier than might be expected when atropine is used alone. This is especially true if the total dose of atropine has been large and the administration of pralidoxime chloride has been delayed. Excitement and manic behavior immediately following recovery of consciousness have been reported in several cases.
However, similar behavior has occurred in cases of organophosphate poisoning that were not treated with pralidoxime chloride.
Warnings & Cautions for Protopam Chloride
Chloride is not effective in the treatment of poisoning due to phosphorus, inorganic phosphates, or organophosphates not having anticholinesterase activity. PROTOPAM Chloride is not indicated as an antidote for intoxication by pesticides of the carbamate class since it may increase the toxicity of carbaryl.
Drug Interactions with Protopam Chloride
Drug Interactions When atropine and pralidoxime chloride are used together, the signs of atropinization (flushing, mydriasis, tachycardia, dryness of the mouth and nose) may occur earlier than might be expected when atropine is used alone. This is especially true if the total dose of atropine has been large and the administration of pralidoxime chloride has been delayed. The following precautions should be kept in mind in the treatment of anticholinesterase poisoning, although they do not bear directly on the use of pralidoxime chloride: since barbiturates are potentiated by the anticholinesterases, they should be used cautiously in the treatment of convulsions; morphine, theophylline, aminophylline, reserpine, and phenothiazine-type tranquilizers should be avoided in patients with organophosphate poisoning.
Prolonged paralysis has been reported in patients when succinylcholine is given with drugs having anticholinesterase activity; therefore, it should be used with caution.
Pregnancy Safety for Protopam Chloride
Pregnancy Teratogenic Effects: Animal reproduction studies have not been conducted with pralidoxime chloride. It is also not known whether pralidoxime chloride can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Pralidoxime chloride should be given to a pregnant woman only if clearly needed.
Pediatric Use of Protopam Chloride
Pediatric Use There are no adequate and well-controlled clinical trials that establish the effectiveness of pralidoxime chloride in pediatric patients. Efficacy has been extrapolated from the adult population and is supported by nonclinical studies, pharmacokinetic studies in adults and experience in the pediatric population (see DOSAGE AND ADMINISTRATION ). As in adults, laryngospasm, cardiac arrest, tachycardia, and muscle rigidity or paralysis have been reported following rapid intravenous injection. Muscle fasciculations, apnea, and convulsions have also been reported.
Contraindications for Protopam Chloride
There are no known absolute contraindications for the use of PROTOPAM Chloride (see PRECAUTIONS, Drug Interactions and DOSAGE AND ADMINISTRATION ). Relative contraindications include known hypersensitivity to the drug and other situations in which the risk of its use clearly outweighs possible benefit.
Overdosage Information for Protopam Chloride
Manifestations of Overdosage Observed in normal subjects only: dizziness, blurred vision, diplopia, headache, impaired accommodation, nausea, slight tachycardia. In therapy, it has been difficult to differentiate side effects due to the drug from those due to the effects of the poison.
Clinical Studies of Protopam Chloride
L/kg. Pralidoxime chloride is not bound to plasma protein. Pralidoxime chloride is
relatively short acting and repeated doses may be needed, unless continuous intravenous infusion is selected. Simulations suggest that after a dose of 1000 mg given intravenously, concentrations fall below 4 µg/mL in about 1.5 hours. The short duration of action of pralidoxime chloride and the necessity for repeated doses should be considered especially where there is any evidence of continuing absorption of the poison.
The apparent half-life of pralidoxime chloride is 74 to 77 minutes. The drug is rapidly excreted in the urine by renal tubular secretion, partly unchanged, and partly as a metabolite produced by the liver. After intramuscular administration of 1000 mg of pralidoxime chloride, the renal clearance has been reported to be 7.2 ± 2.9 mL/min/kg in healthy volunteers and 3.6 ± 1.5 mL/min/kg in organophosphate-poisoned patients.
In one study of 11 organophosphate-poisoned pediatric patients (age, 0.8 to 18 years), an intravenous loading dose of 15-50 mg/kg (mean 29 mg/kg) of pralidoxime chloride followed by a continuous infusion of 10-16 mg/kg/hr (mean 14 mg/kg/hr) over 12 to 43 hours (mean 27 ± 8 hours) resulted in an average steady state plasma concentration of 22.2 mg/L (6.9 to 47.4 mg/L) and an average body clearance of 0.88 L/kg/hr (0.28 to 2.20 L/kg/hr). After the continuous infusion was discontinued, determinations of the apparent volume of distribution and half-life ranged from 1.7 to
Drug information sourced from the FDA. This content is for informational purposes only and does not constitute medical advice. Consult a healthcare professional before making any medication decisions.
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