Pralidoxime chloride

What is Pralidoxime chloride?

• Pralidoxime chloride (PROTOPAM Chloride) is a cholinesterase reactivator used to treat organophosphate poisoning in conjunction with atropine and either diazepam or midazolam.

Pralidoxime-3D-vdW

Pralidoxime Mechanism

What are the uses of this medicine?

PROTOPAM Chloride is used as an antidote:

• For 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.

How does this medicine work?

• The principal action of pralidoxime chloride is to reactivate cholinesterase (mainly outside of the central nervous system) which has been inactivated by phosphorylation due to an organophosphate pesticide or related compound.
• The destruction of accumulated acetylcholine can then proceed, and neuromuscular junctions will again function normally.
• The drug has its most critical effect in relieving paralysis of the muscles of respiration.
• Because pralidoxime chloride is less effective in relieving depression of the respiratory center, atropine is always required concomitantly to block the effect of accumulated acetylcholine at this site.

Who Should Not Use this medicine ?

• There are no known absolute contraindications for the use of PROTOPAM Chloride.
• Relative contraindications include known hypersensitivity to the drug.

What drug interactions can this medicine cause?

• No formal drug interaction studies have been conducted with PROTOPAM.

Is this medicine FDA approved?

• Initial U.S. Approval: 2010

How should this medicine be used?

Recommended dosage:

• Adult dosing:
• Inject an initial dose of 1000 to 2000 mg of PROTOPAM Chloride, preferably as an infusion in 100 mL of normal saline, over a 15- to 30-minute period.
• A second dose of 1000 to 2000 mg may be indicated after about one hour if muscle weakness has not been relieved.
• Additional doses may be given every 10-12 hours if muscle weakness persists.

Intramuscular dosing in adults should be based on the severity of clinical symptoms. MILD SYMPTOMS

• For treatment of mild symptoms, administer a 600 mg (2 mL) intramuscular dose of PROTOPAM Chloride. Wait 15 minutes for PROTOPAM Chloride to take effect.
• If, after 15 minutes, mild symptoms persist, then administer a second 600 mg (2 mL) intramuscular dose of PROTOPAM Chloride.
• If, after an additional 15 minutes, mild symptoms continue to persist, a third 600 mg (2 mL) dose of PROTOPAM Chloride may be administered for a total cumulative dose of 1800 mg.
• If at any time after the first dose, the patient develops severe symptoms, administer two additional 600 mg intramuscular doses in rapid succession for a total cumulative dose of 1800 mg of PROTOPAM Chloride.

SEVERE SYMPTOMS

• For treatment of severe symptoms, administer three 600 mg intramuscular doses (3 doses of 2 mL each) in rapid succession for a total dose of 1800 mg of PROTOPAM Chloride.
• PERSISTENT SYMPTOMS
• If symptoms persist after administering the complete 1800 mg regimen (3 injections of 600 mg each), the series may be repeated beginning approximately 1 hour after administration of the last injection.

• PEDIATRIC DOSING (FOR PATIENTS 16 YEARS AND UNDER)

PEDIATRIC INTRAVENOUS DOSING:

• Administer a loading dose of 20-50 mg/kg (not to exceed 2000 mg/dose) over 15-30 minutes followed by a continuous infusion of 10-20 mg/kg/hour.
• Administer an initial intermittent infusion of 20-50 mg/kg (not to exceed 2000 mg/dose) over 15-30 minutes.
• A second dose of 20-50 mg/kg may be indicated after about one hour if muscle weakness has not been relieved.
• Repeat dosing is permissible every 10-12 hours as needed.

PEDIATRIC INTRAMUSCULAR DOSING: MILD SYMPTOMS:

• For the treatment of mild symptoms, administer a weight-appropriate intramuscular dose of PROTOPAM Chloride. Wait 15 minutes for PROTOPAM Chloride to take effect.
• If, after 15 minutes, mild symptoms persist, then administer a second weight-appropriate intramuscular dose of PROTOPAM Chloride.
• If after an additional 15 minutes, mild symptoms continue to persist, a third weight-appropriate intramuscular dose of PROTOPAM Chloride may be administered.

SEVERE SYMPTOMS:

• For treatment of severe symptoms, administer the weight-appropriate intramuscular dose of PROTOPAM Chloride Injection as three injections, in rapid succession, into the patient’s anterolateral thigh.

PERSISTENT SYMPTOMS

• If symptoms persist after administering a complete course (3 injections of the weight-appropriate dose each), the series may be repeated beginning approximately 1 hour after administration of the last injection.

Anticholinesterase Overdosage:

• PROTOPAM Chloride may be given in a dosage of 1000 to 2000 mg intravenously followed by increments of 250 mg every five minutes.

Administration: PROTOPAM Chloride is supplied as 1000 mg single-dose vials for injection. For INTRAVENOUS infusion:

• Reconstitute a single PROTOPAM Chloride 1000 mg vial by adding 20 mL of Sterile Water for Injection, USP, which results in a 50 mg/mL concentration.
• The solution should further be diluted with Normal Saline for Injection, USP to achieve a concentration of 10 to 20 mg/mL (e.g. 1000 mg in 100 mL or 2000 mg in 100 mL).
• For fluid restricted patients or for rapid administration (over at least 5 min), a maximum concentration of 50 mg/mL may be used.

For INTRAMUSCULAR injection:

• Reconstitute a single PROTOPAM Chloride 1000 mg vial by adding 3.3 mL of Sterile Water for Injection, USP for an approximate concentration of 300 mg/mL.
• Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
• Discard unused solution after a dose has been withdrawn.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As PROTOPAM Chloride (pralidoxime chloride) for Injection

This medicine is available in fallowing brand namesː

• PROTOPAM Chloride

What side effects can this medication cause?

The most common side effects of this medicine include:

• blurred vision
• diplopia
• impaired accommodation
• dizziness
• headache
• drowsiness
• nausea
• tachycardia
• increased systolic and diastolic blood pressure
• hyperventilation
• muscular weakness

What special precautions should I follow?

• Intravenous administration of PROTOPAM Chloride should be carried out slowly and, preferably, by continuous or intermittent infusion, since temporary worsening of cholinergic manifestations (i.e. tachycardia, cardiac arrest, laryngospasm, and muscle rigidity or paralysis) may occur if PROTOPAM Chloride is infused too rapidly.
• Because pralidoxime is excreted in the urine, a decrease in renal function will result in increased blood levels of the drug. Thus, the dosage of PROTOPAM Chloride should be reduced in the presence of renal insufficiency.
• Treatment of organophosphate poisoning should be instituted without waiting for the results of laboratory tests
• PROTOPAM 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.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• dizziness
• blurred vision
• diplopia
• headache
• impaired accommodation
• nausea
• slight tachycardia

Can this medicine be used in pregnancy?

• 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.

Can this medicine be used in children?

• There are no adequate and well-controlled clinical trials that establish the effectiveness of pralidoxime chloride in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active Ingredients:

• PRALIDOXIME CHLORIDE

Inactive ingredients:

• SODIUM HYDROXIDE

Who manufactures and distributes this medicine?

Manufactured for

• Baxter Healthcare Corporation
• Deerfield, IL USA
• By: Baxter Pharmaceutical Solutions LLC Bloomington, IN

What should I know about storage and disposal of this medication?

• Store at 20°-25°C (68°-77°F), excursions permitted to 15°-30°C (59°-86°F).

• Dailymed label info on Pralidoxime chloride
• FDA Pralidoxime chloride

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