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Antipyrine | CAS No: 60-80-0 | GMP-certified suppliers
A medication that provides analgesic relief and is used in combination otic solutions for symptomatic treatment of acute otitis media and as a probe in hepatic enzyme function studies.
Therapeutic categories
Primary indications
- Antipyrine is an analgesic often used to test effects of other drugs on liver enzymes
- In combination with benzocaine in otic solutions, antipyrine is indicated for the symptomatic relief of acute otitis media arising from various etiologies
Product Snapshot
- Antipyrine is available primarily as oral and otic liquid and solution formulations
- It is used mainly as an analgesic and as a component in otic solutions for symptomatic relief of acute otitis media
- Antipyrine is approved and marketed in the US and Canada, with status ranging from approved to investigational
Clinical Overview
Clinically, antipyrine is utilized both as an analgesic for pain mitigation and as an experimental probe to assess hepatic drug-metabolizing enzyme function. It is notably involved in in vivo studies evaluating the effects of concomitant drugs or disease states on cytochrome P450 enzymatic activity, reflecting its role as a substrate and inhibitor across multiple CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C19, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.
Pharmacodynamically, antipyrine exerts analgesic and antipyretic effects through central nervous system mechanisms. Its primary mode of action involves inhibition of cyclooxygenase isoenzymes (COX-1, COX-2, and COX-3), leading to reduced prostaglandin synthesis and an elevated pain threshold.
Key absorption, distribution, metabolism, and excretion (ADME) characteristics include its extensive hepatic metabolism mediated by multiple CYP enzymes and subsequent elimination via renal pathways. This metabolic profile underpins its sensitivity to drug-drug interactions and necessitates careful consideration when co-administered with other agents affecting cytochrome P450 activity.
Safety considerations include the potential for nephrotoxicity and methemoglobinemia, albeit reported infrequently. Given its involvement in CYP-mediated pathways, monitoring for adverse effects related to altered hepatic metabolism is advisable during clinical use.
Notable pharmaceutical contexts focus on antipyrine’s inclusion in otic preparations combined with benzocaine for ear pain relief and its application as a probe substrate in pharmacokinetic investigations.
From a sourcing and quality standpoint, antipyrine API procurement demands stringent adherence to purity specifications and verification of the synthetic route, considering its extensive clinical and investigational use. Suppliers should provide comprehensive certificates of analysis verifying identity, purity, residual solvents, and absence of contaminants to ensure compliance with regulatory standards.
Identification & chemistry
| Generic name | Antipyrine |
|---|---|
| Molecule type | Small molecule |
| CAS | 60-80-0 |
| UNII | T3CHA1B51H |
| DrugBank ID | DB01435 |
Pharmacology
| Summary | Antipyrine acts centrally to elevate pain threshold by inhibiting cyclooxygenase isoforms COX-1, COX-2, and COX-3, thereby reducing prostaglandin synthesis. It functions as an analgesic and antipyretic and is used both systemically and topically, including in otic formulations combined with benzocaine for symptomatic relief in acute otitis media. Additionally, antipyrine serves as a probe substrate in assessing hepatic drug-metabolizing enzyme activity. |
|---|---|
| Mechanism of action | Antipyrine is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. |
| Pharmacodynamics | Antipyrine is an analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29) |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin G/H synthase 2 | Humans | inhibitor |
| Prostaglandin G/H synthase 1 | Humans | inhibitor |
Formulation & handling
- Antipyrine is a small molecule suitable for oral, topical, auricular, buccal, and ophthalmic formulations.
- This compound demonstrates moderate water solubility and logP, supporting aqueous solution and suspension dosage forms.
- Oral administration can be with or without food, as food intake does not significantly affect overall bioavailability.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has patent protection expiring in the US and Canada within the next two years, transitioning the product toward a mature market phase with increasing generic availability. Market activity is expected to shift from exclusive brand presence to broader competition following patent expiry. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Antipyrine includes multiple originator companies producing branded formulations primarily in the US and Canadian markets. Several branded products such as Acella and Rezall indicate an established presence in North America. Given the availability of multiple branded versions and no mention of recent patent protections, generic competition is likely existing or imminent in these regions. |
|---|
Antipyrine is a type of Analgesics
Analgesics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are commonly used to relieve pain. They are designed to alleviate discomfort by targeting the body's pain receptors or by reducing inflammation. Analgesics are widely utilized in the medical field to manage various types of pain, ranging from mild to severe.
One of the primary classes of analgesics is nonsteroidal anti-inflammatory drugs (NSAIDs). NSAIDs work by inhibiting the production of prostaglandins, substances that contribute to pain and inflammation. This class includes well-known drugs like ibuprofen and naproxen. Another class of analgesics is opioids, which are derived from opium or synthetic compounds that mimic the effects of opium. Opioids act on the central nervous system to reduce pain perception and provide potent pain relief. Examples of opioids include morphine, codeine, and oxycodone.
Analgesics are available in various forms, such as tablets, capsules, creams, and injections, allowing for different routes of administration based on the patient's needs. They are commonly used to manage pain associated with conditions like arthritis, headaches, dental procedures, and post-operative recovery.
It is important to note that analgesics should be used under medical supervision, as improper use or overuse can lead to adverse effects, including gastrointestinal complications, addiction, and respiratory depression in the case of opioids. Therefore, it is crucial for healthcare professionals to assess each patient's individual needs and prescribe the appropriate analgesic and dosage.
In summary, analgesics are a vital category of pharmaceutical APIs used to alleviate pain by targeting pain receptors or reducing inflammation. With various classes and forms available, they provide valuable options for pain management when used responsibly and under medical guidance.
Antipyrine API manufacturers & distributors
Compare qualified Antipyrine API suppliers worldwide. We currently have 7 companies offering Antipyrine API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Caesar & Loretz GmbH (CAE... | Distributor | Germany | Unknown | BSE/TSE, CoA, GMP, ISO9001, MSDS | 211 products |
| Duchefa Farma B.V. | Distributor | Netherlands | Unknown | CoA, GMP, ISO9001, MSDS | 170 products |
| Shandong Xinhua | Producer | China | China | CoA, WC | 21 products |
| Vani Pharma Labs | Producer | India | India | CoA, WC | 2 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 133 products |
| Xellia (Taizhou) | Producer | China | China | CoA, WC | 8 products |
| Zhejiang Haisen Pharma | Producer | China | China | CoA, WC | 7 products |
When sending a request, specify which Antipyrine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Antipyrine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
