Pralidoxime Chloride

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Overview

What is Pralidoxime Chloride?

Pralidoxime Chloride Injection (auto-injector) provides pralidoxime chloride in a sterile solution for intramuscular injection.

Each prefilled auto-injector provides a dose of the antidote, pralidoxime chloride in a self-contained unit, specially designed for automatic self- or buddy-administration by military personnel. Pralidoxime in the auto-injector may also be administered by qualified civilian emergency responders The recommended procedure (see ) is to inject the contents of the auto-injector into the muscles of an outer thigh.

After an auto-injector has been activated, the empty container should be disposed of properly (see ), it cannot be refilled nor can the protruding needle be retracted.

When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH range is 2.0-3.0. The product is pyrogen free.

Pralidoxime chloride is a cholinesterase reactivator.

Chemical Name:

Structural Formula:

Pralidoxime chloride occurs as an odorless, white, nonhygroscopic, crystalline powder which is soluble in water to the extent of 1 g in less than 1 mL. Stable in air, it melts between 215°C and 225°C, with decomposition.

The specific activity of the drug resides in the 2-formyl-1 methylpyridinium ion and is independent of the particular salt employed. The chloride is preferred because of physiologic compatibility, excellent water solubility at all temperatures, and high potency per gram, due to its low (173) molecular weight.

What does Pralidoxime Chloride look like?

What are the available doses of Pralidoxime Chloride?

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What should I talk to my health care provider before I take Pralidoxime Chloride?

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How should I use Pralidoxime Chloride?

This auto-injector for pralidoxime chloride is specifically indicated for intramuscular use as an adjunct to atropine in the treatment of poisoning by nerve agents having anticholinesterase activity.

Exposure to nerve agents possessing anticholinesterase activity (organophosphate type)

MILD CASE—headache, blurred vision, mild muscarinic signs

MODERATELY SEVERE CASE—excessive sweating, lacrimation, salivation, diarrhea, tightness in the chest

For optimal reactivation of organophosphate-inhibited cholinesterase, atropine and pralidoxime should be administered as soon as possible after exposure. Depending on the severity of symptoms, immediately administer one atropine-containing auto-injector, followed by one pralidoxime-containing auto-injector. Atropine must be given first until its effects become apparent and only then should pralidoxime be administered. If nerve agent symptoms are still present after 15 minutes, repeat injections. If symptoms still exist after an additional 15 minutes, repeat injections for a third time. If after the third set of injections, symptoms remain, do not give any more antidotes but seek medical help.

What interacts with Pralidoxime Chloride?

The pralidoxime chloride auto-injector is contraindicated in patients who are hypersensitive to any component of the product.

What are the warnings of Pralidoxime Chloride?

The occurrence of hypersensitivity reactions to allopurinol may be increased in patients with decreased renal function receiving thiazides and allopurinol concurrently. For this reason, in this clinical setting, such combinations should be administered with caution and patients should be observed closely.

What are the precautions of Pralidoxime Chloride?

General:

Pralidoxime has been very well tolerated in most cases, but it must be remembered that the desperate condition of the organophosphate-poisoned patient will generally mask such minor signs and symptoms as have been noted in normal subjects.

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 pralidoxime should be reduced in the presence of renal insufficiency.

Information for Patients:

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The pralidoxime chloride auto-injector should be self- or buddy-administered by military personnel or administered by qualified civilian emergency responders only after the following events have occurred:

Appropriate steps must be taken to insure that personnel equipped with auto-injectors understand their indications and use including review of symptoms of poisoning and operation of the auto-injector.

Laboratory Tests:

Treatment of organophosphate poisoning should be instituted without waiting for the results of laboratory tests. Red blood cell, plasma cholinesterase, and urinary paranitrophenol measurements (in the case of parathion exposure) may be helpful in confirming the diagnosis and following the course of the illness. A reduction in red blood cell cholinesterase concentration to below 50% of normal has been seen only with organophosphate ester poisoning.

Drug Interactions:

When atropine and pralidoxime 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 has been delayed.

The following precautions should be kept in mind in the treatment of anticholesterinase poisoning, although they do not bear directly on the use of pralidoxime; since barbiturates are potentiated by the anticholinesterases, they should be used cautiously in the treatment of convulsions; morphine, theophylline, aminophylline, succinylcholine, reser-pine, and phenothiazine-type tranquilizers should be avoided in patients with organophosphate poisoning.

Carcinogenesis, Mutagensis, Impairment of Fertility:

Since the pralidoxime chloride auto-injector is indicated for short-term emergency use only, no investigations of its potential for carcinogenesis, mutagenesis, or impairment of fertility have been conducted by the manufacturer, or reported in the literature.

Pregnancy

Animal reproduction studies have not been conducted with pralidoxime. It is also not known whether pralidoxime can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Pralidoxime should be given to a pregnant woman only if clearly needed.

Nursing Mother:

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when pralidoxime is administered to a nursing woman.

Pediatric Use:

Safety and effectiveness in children have not been established.

What are the side effects of Pralidoxime Chloride?

Forty to 60 minutes after intramuscular injection, mild to moderate pain may be experienced at the site of injection.

Pralidoxime 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. A single intramuscular injection of 330 mg in 1 mL in rabbits caused myonecrosis, inflammation and hemorrhage.

When atropine and pralidoxime 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 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.

What should I look out for while using Pralidoxime Chloride?

The pralidoxime chloride auto-injector is contraindicated in patients who are hypersensitive to any component of the product.

Pralidoxime is not effective in the treatment of poisoning due to phosphorus, inorganic phosphates or organophosphates not having anticholinesterase activity.

What might happen if I take too much Pralidoxime Chloride?

How should I store and handle Pralidoxime Chloride?

Store at 20 to 25C (68 to 77F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Keep tightly closed (protect from moisture). Protect from light.Pralidoxime chloride is supplied in aqueous solution prefilled in the auto-injector (600 mg, 2 mL) for military use and for use by qualified civilian emergency responders. Auto-injectors are supplied through the Directorate of Medical Materiel, Defense Supply Center Philadelphia or other analogous local, state or federal agency.When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH is 2.0-3.0 The product is pyrogen free.Store at 25°C (77°F); Excursions permitted to 15-30°C (59-86°F).[See USP Controlled Room Temperature] Keep from freezing.Meridian Medical Technologies, Inc.Columbia, MD 21046A Pfizer Company0000197608/16Printed in U.S.A.Pralidoxime chloride is supplied in aqueous solution prefilled in the auto-injector (600 mg, 2 mL) for military use and for use by qualified civilian emergency responders. Auto-injectors are supplied through the Directorate of Medical Materiel, Defense Supply Center Philadelphia or other analogous local, state or federal agency.When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH is 2.0-3.0 The product is pyrogen free.Store at 25°C (77°F); Excursions permitted to 15-30°C (59-86°F).[See USP Controlled Room Temperature] Keep from freezing.Meridian Medical Technologies, Inc.Columbia, MD 21046A Pfizer Company0000197608/16Printed in U.S.A.Pralidoxime chloride is supplied in aqueous solution prefilled in the auto-injector (600 mg, 2 mL) for military use and for use by qualified civilian emergency responders. Auto-injectors are supplied through the Directorate of Medical Materiel, Defense Supply Center Philadelphia or other analogous local, state or federal agency.When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH is 2.0-3.0 The product is pyrogen free.Store at 25°C (77°F); Excursions permitted to 15-30°C (59-86°F).[See USP Controlled Room Temperature] Keep from freezing.Meridian Medical Technologies, Inc.Columbia, MD 21046A Pfizer Company0000197608/16Printed in U.S.A.Pralidoxime chloride is supplied in aqueous solution prefilled in the auto-injector (600 mg, 2 mL) for military use and for use by qualified civilian emergency responders. Auto-injectors are supplied through the Directorate of Medical Materiel, Defense Supply Center Philadelphia or other analogous local, state or federal agency.When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH is 2.0-3.0 The product is pyrogen free.Store at 25°C (77°F); Excursions permitted to 15-30°C (59-86°F).[See USP Controlled Room Temperature] Keep from freezing.Meridian Medical Technologies, Inc.Columbia, MD 21046A Pfizer Company0000197608/16Printed in U.S.A.Pralidoxime chloride is supplied in aqueous solution prefilled in the auto-injector (600 mg, 2 mL) for military use and for use by qualified civilian emergency responders. Auto-injectors are supplied through the Directorate of Medical Materiel, Defense Supply Center Philadelphia or other analogous local, state or federal agency.When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH is 2.0-3.0 The product is pyrogen free.Store at 25°C (77°F); Excursions permitted to 15-30°C (59-86°F).[See USP Controlled Room Temperature] Keep from freezing.Meridian Medical Technologies, Inc.Columbia, MD 21046A Pfizer Company0000197608/16Printed in U.S.A.Pralidoxime chloride is supplied in aqueous solution prefilled in the auto-injector (600 mg, 2 mL) for military use and for use by qualified civilian emergency responders. Auto-injectors are supplied through the Directorate of Medical Materiel, Defense Supply Center Philadelphia or other analogous local, state or federal agency.When activated, each auto-injector dispenses 600 mg of pralidoxime chloride in 2 mL of a sterile solution containing 20 mg/mL benzyl alcohol, 11.26 mg/mL glycine in Water for Injection, USP. The pH is adjusted with hydrochloric acid. The pH is 2.0-3.0 The product is pyrogen free.Store at 25°C (77°F); Excursions permitted to 15-30°C (59-86°F).[See USP Controlled Room Temperature] Keep from freezing.Meridian Medical Technologies, Inc.Columbia, MD 21046A Pfizer Company0000197608/16Printed in U.S.A.

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Pralidoxime chloride is a cholinesterase reactivator.

The principal action of pralidoxime 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. Pralidoxime also slows the process of "aging" of phosphorylated cholinesterase to a non-reactivatable form, and detoxifies certain organophosphates by direct chemical reaction. The drug has its most critical effect in relieving paralysis of the muscles of respiration. Because pralidoxime 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. Pralidoxime relieves muscarinic signs and symptoms, salivation, bronchospasm, etc., but this action is relatively unimportant since atropine is adequate for this purpose.

Pralidoxime is distributed throughout the extracellular water, it is not bound to plasma protein. The drug is rapidly excreted in the urine partly unchanged, and partly as a metabolite produced by the liver. Consequently, pralidoxime is relatively short acting and repeated doses may be needed, especially where there is any evidence of continuing absorption of the poison.

The minimum therapeutic concentration of pralidoxime in plasma is 4 g/mL, this level is reached in about 16 minutes after a single injection of 600 mg pralidoxime chloride. The apparent half-life of pralidoxime chloride is 74-77 minutes.

It has been reported that the supplemental use of oxime cholinesterase reactivators (such as pralidoxime) reduces the incidence and severity of developmental defects in chick embryos exposed to such known teratogens as parathion, bidrin, carbachol and neostigmine. This protective effect of the oximes was shown to be dose related.

Non-Clinical Toxicology

The pralidoxime chloride auto-injector is contraindicated in patients who are hypersensitive to any component of the product.

Pralidoxime is not effective in the treatment of poisoning due to phosphorus, inorganic phosphates or organophosphates not having anticholinesterase activity.

When atropine and pralidoxime 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 has been delayed.

The following precautions should be kept in mind in the treatment of anticholesterinase poisoning, although they do not bear directly on the use of pralidoxime; since barbiturates are potentiated by the anticholinesterases, they should be used cautiously in the treatment of convulsions; morphine, theophylline, aminophylline, succinylcholine, reser-pine, and phenothiazine-type tranquilizers should be avoided in patients with organophosphate poisoning.

Pralidoxime has been very well tolerated in most cases, but it must be remembered that the desperate condition of the organophosphate-poisoned patient will generally mask such minor signs and symptoms as have been noted in normal subjects.

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 pralidoxime should be reduced in the presence of renal insufficiency.

Forty to 60 minutes after intramuscular injection, mild to moderate pain may be experienced at the site of injection.

Pralidoxime 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. A single intramuscular injection of 330 mg in 1 mL in rabbits caused myonecrosis, inflammation and hemorrhage.

When atropine and pralidoxime 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 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.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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Interactions

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