Pralidoxime
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Pralidoxime
Brand names: Protopam®
Chemical formula:
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- Inyección de pralidoxima
Pralidoxime injection
What is pralidoxime injection?
PRALIDOXIME (Protopam®) treats poisoning by some insecticides (called organophosphates) and nerve agents, and overdoses of some medicines that treat myasthenia gravis. Generic pralidoxime injection is available. Emergency kits for injection are also available.What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:• kidney disease
• myasthenia gravis
• an unusual or allergic reaction to pralidoxime, other medicines, foods, dyes, o preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I use this medicine?
Pralidoxime is for injection into a muscle, under the skin, or into a vein. It is given by a health-care professional in a hospital or clinic setting. Pralidoxime is not for self-medication, except in emergency situations when it is possible that workers may be exposed to nerve agents or organophosphate insecticides. Injection kits are available for self-injection in case of emergency. Learn how and when to use the autoinjector before an emergency arises. If organophosphate poisoning occurs, atropine and pralidoxime are given as soon as possible. An atropine injection is given first and after the effects become apparent pralidoxime is given. Repeat the injections of atropine and pralidoxime after 15 minutes if symptoms continue, and again after an additional 15 minutes if symptoms persist. If symptoms of nerve agent exposure continue after the third set of injections, obtain medical help.What if I miss a dose?
This does not apply.What drug(s) may interact with pralidoxime?
• atropine• barbiturate medicines for inducing sleep or treating seizures (convulsions)
• medicines that improve muscle strength or tone for conditions like myasthenia gravis
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking pralidoxime?
Pralidoxime is not intended for long-term use. Contact your prescriber or health care professional immediately after an organophosphate or nerve agent poisoning occurs for instructions regarding treatment.Remove contaminated clothing and wash the poison from the skin and hair.
What side effects may I notice from receiving pralidoxime?
Side effects may be difficult to distinguish from those caused by the poison.Side effects that you should report to your prescriber or health care professional as soon as possible:
• hyperventilation (over breathing)
• muscle rigidity
• rapid heartbeat
• spasm of the larynx (voice box)
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• blurred or double vision
• dizziness, drowsiness
• excitement, agitation, or manic behavior
• headache
• muscle weakness
• nausea, vomiting
• skin rash
Where can I keep my medicine?
Keep out of the reach of children.Store at room temperature, approximately 25 degrees C (77 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Saunders Veterinary Dictionary:
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pralidoxime
A cholinesterase reactivator, effective against the nicotinic cholinergic effects of organophosphorus compounds; it also has limited value in counteracting carbamate-type cholinesterase inhibitors; abbreviated 2-PAM.
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Pralidoxime
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This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (June 2010) |
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| Systematic (IUPAC) name | |
| 2-[(hydroxyimino)methyl]-1-methylpyridin-1-ium | |
| Clinical data | |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Pregnancy cat. | C |
| Legal status | RX-only |
| Identifiers | |
| CAS number | 6735-59-7  |
| ATC code | V03AB04 |
| PubChem | CID 6789253 |
| DrugBank | DB00733 |
| ChemSpider | 5193737 |
| UNII | P7MU9UTP52 |
| KEGG | C07400 |
| ChEBI | CHEBI:8354 |
| ChEMBL | CHEMBL1420 |
| Synonyms | 1-methylpyridine-6-carbaldehyde oxime |
| Chemical data | |
| Formula | C7H9N2O+ |
| Mol. mass | 137.159 g/mol |
| SMILES | eMolecules & PubChem |
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Pralidoxime (2-pyridine aldoxime methyl chloride,) or 2-PAM, usually as the chloride or methiodide salts, belongs to a family of compounds called oximes that bind to organophosphate-inactivated acetylcholinesterase. It is used to combat poisoning by organophosphates[1] or acetylcholinesterase inhibitors (nerve agents), in conjunction with atropine and diazepam. In India, it is marketed by Nucleus Inc. with the brand names LyoPAM and PurePAM.
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Contents
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Mechanism of action
Pralidoxime, typically used in cases of organophosphate poisoning (which causes AChase inhibition), attaches to the site where a cholinesterase inhibitor has attached, then attaches to the inhibitor, removing the organophosphate from cholinesterase, allowing it to work normally again. This is known as "regenerating" or "reactivating" acetylcholinesterase allowing the breakdown of Ach at the synapse. After some time though, some inhibitors can develop a permanent bond with cholinesterase, known as aging, where oximes such as pralidoxime can not reverse the bond.[citation needed] Pralidoxime is often used with atropine (a muscarinic antagonist) to help reduce the parasympathetic effects of organophosphate poisoning. Pralidoxime can also be used to treat neostigmine or pyridostigmine (both ACHase inhibitors) overdoses due to its ACHase regenerating capacities.
Pralidoxime has an important role in reversing paralysis of the respiratory muscles but due to its poor blood–brain barrier penetration, it has little effect on centrally-mediated respiratory depression. This is why atropine which has excellent blood–brain barrier penetration, is concomitantly administered with pralidoxime during the treatment of organophosphate poisoning.
Dosage
- Adults: 30 mg/kg (typically 1-2 g), administered by intravenous therapy over 15–30 minutes or intramuscular injection or subcutaneous injection, repeated 60 minutes later. It can also be given as a 500 mg/hr continuous IV infusion.
- Children: 20–50 mg/kg followed by a maintenance infusion at 5–10 mg/kg/hr.
Intravenous infusions can lead to respiratory or cardiac arrest if given too quickly.[2]
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 anticholinesterase 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, reserpine, and phenothiazine-type tranquilizers should be avoided in patients with organophosphate poisoning.
Contraindications
There are no known absolute contraindications for the use of pralidoxime. Relative contraindications include known hypersensitivity to the drug and other situations in which the risk of its use clearly outweighs possible benefit.
Chemistry
Pralidoxime, 2-pyridinaldoxime methylchloride, is synthesized by reacting picolinaldehyde (2-formyl pyridine) with hydroxylamine, giving pyridine-2-aldoxime, which is further reacted with methyl iodide, giving the desired pralidoxime.
- D. Nachmansonn, S. Ginsburg, U.S. Patent 2,816,113 (1957).
- L.P. Black, U.S. Patent 3,123,613 (1964).
- D.E. Easterday, A.A. Kondritzer, U.S. Patent 3,140,289 (1964).
- W.B. McDowell, U.S. Patent 3,155,674 (1964).
See also
References
- ^ Jokanović M, Prostran M (2009). "Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and efficacy in the treatment of poisoning with organophosphorus compounds". Curr. Med. Chem. 16 (17): 2177–88. doi:10.2174/092986709788612729. PMID 19519385. http://www.bentham-direct.org/pages/content.php?CMC/2009/00000016/00000017/0004C.SGM.
- ^ Baxter Healthcare Corporation 2006, Protopam Prescribing Information
External links
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Copyrights:
Saunders Veterinary Dictionary
Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.
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