Amidopyrine

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Product Name :	Amidopyrine
Specs :	USP/BP/EP
Cas No.：	58-15-1
Product Serie：	Antipyretics Series
Product  Details ：	Molecular Formula: C13H17N3O    Molecular Weight: 231.29

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Overview

Initially developed in the early 20th century as a antipyretic-analgesic, it exhibits potent fever-reducing and pain-relieving properties by inhibiting cyclooxygenase (COX) enzymes, though its use has evolved due to historical hematological safety concerns. This yellowish crystalline powder is soluble in ethanol and chloroform, slightly soluble in water, and stable when stored in airtight containers away from light. Despite reduced use in some regions, it remains a key component in fixed-dose combinations in certain markets, particularly for musculoskeletal and post-surgical pain.

Features

Pharmacological Profile:

COX Inhibition: Non-selectively inhibits COX-1 and COX-2, reducing prostaglandin synthesis in the hypothalamus (antipyretic) and peripheral tissues (analgesic), with moderate anti-inflammatory effects.

Rapid Onset: Oral administration achieves peak plasma concentrations in 1-2 hours, with a half-life of 1-4 hours, though metabolism via N-demethylation to noramidopyrine (a hepatotoxin) necessitates cautious dosing.

Formulation Adaptability:

Combination Products: Frequently paired with caffeine (enhances absorption), phenacetin (historical use, now replaced by paracetamol), or codeine (for opioid-sparing analgesia), improving efficacy in migraine and tension headache.

Veterinary Use: Used in livestock as an antipyretic, particularly in bovine respiratory disease, with intramuscular injection providing rapid fever reduction.

Safety and Toxicity:

Hematological Risks: Associated with agranulocytosis (incidence ~1:10,000), leading to restricted use in many countries; however, in regions where it is approved, strict blood count monitoring is mandated.

Drug Interactions: Enhances anticoagulant effects of warfarin via CYP2C9 inhibition, requiring INR monitoring in co-administered patients.

Applications

Therapeutic Uses:

Pain Management:

Acute Pain: Effective for post-operative pain, dental procedures, and musculoskeletal disorders (arthritis, myalgia), often in combination with muscle relaxants.

Headache Disorders: Used in migraine prophylaxis (with ergotamine) and tension headache, leveraging its rapid CNS penetration (lipid solubility log P = 1.8).

Fever Reduction: Targets febrile illnesses (viral/bacterial infections), particularly when acetaminophen/ibuprofen are contraindicated (e.g., hepatic impairment).

Research and Historical Context:

Pharmacology Studies: Serves as a model for pyrazolone drug design, inspiring the development of safer analogs like metamizole (dipyrone), which lacks the N-demethylation pathway.

Toxicology Reference: Its historical use highlights the balance between efficacy and safety in COX inhibitor development, informing modern risk-benefit assessments.

Quality Control

Manufactured to BP/USP standards, our Amidopyrine features a melting point of 107-113°C and low impurity profiles (related compounds ≤0.5%). It undergoes rigorous microbial testing (Total Plate Count <1000 CFU/g, E. coli absent), ensuring safety for oral and parenteral formulations where approved.