Nafamostat API Manufacturers

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Looking for Nafamostat API 81525-10-2?

Description:
Here you will find a list of producers, manufacturers and distributors of Nafamostat. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
API | Excipient name:
Nafamostat 
Synonyms:
Nafamostatum , p-Guanidinobenzoic acid ester with 6-hydroxy-2-naphthamidine  
Cas Number:
81525-10-2 
DrugBank number:
DB12598 
Unique Ingredient Identifier:
Y25LQ0H97D

General Description:

Nafamostat, identified by CAS number 81525-10-2, is a notable compound with significant therapeutic applications. Nafamostat is a synthetic serine protease inhibitor that is commonly formulated with hydrochloric acid due to its basic properties. It has been used in trials studying the prevention of Liver Transplantation and Postreperfusion Syndrome. The use of nafamostat in Asian countries is approved as an anticoagulant therapy for patients undergoing continuous renal replacement therapy due to acute kidney injury.

Indications:

This drug is primarily indicated for: Used as an anticoagulant in patients with disseminative blood vessel coagulation, hemorrhagic lesions, and hemorrhagic tendencies. It prevents blood clot formation during extracorporeal circulation in patients undergoing continuous renal replacement therapy and extra corporeal membrane oxygenation. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Nafamostat undergoes metabolic processing primarily in: Nafamostat is mainly hydrolyzed by hepatic carboxyesterase and long-chain acyl-CoA hydrolase in human liver cytosol. Main metabolites are p-guanidinobenzoic acid (PGBA) and 6-amidino-2-naphthol (AN) as inactive protease inhibitors. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Half-life:

The half-life of Nafamostat is an important consideration for its dosing schedule: Approximately 8 minutes. This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Nafamostat from the body primarily occurs through: Two metabolites of NM, p-guanidinobenzoic acid (PGBA) and 6-amidino-2-naphthol (AN), are renally excreted. Nafamostat accumulates in the kidneys. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Pharmacodynamics:

Nafamostat exerts its therapeutic effects through: Nafamostat is a fast-acting proteolytic inhibitor used during hemodialysis to prevent the proteolysis of fibrinogen into fibrin by competitively inhibiting several serine proteases including thrombin. It improves acute pancreatitis and prevents blood clot formation during extracorporeal circulation and has an anti-inflammatory effect in vitro. A study suggets that nafamostat has a neuroprotective role during ischemia-induced brain injury from antithrombin activity . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Nafamostat functions by: Nafamostat mesilate inhibits various enzyme systems, such as coagulation and fibrinolytic systems (thrombin, Xa, and XIIa), the kallikrein–kinin system, the complement system, pancreatic proteases and activation of protease-activated receptors (PARs) . Nafamostat inhibits lipopolysaccharide-induced nitric oxide production, apoptosis, and interleukin (IL)-6 and IL-8 levels in cultured human trophoblasts. It is shown to act as an antioxidant in TNF-α-induced ROS production . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Nafamostat belongs to the class of organic compounds known as guanidinobenzoic acids and derivatives. These are aromatic compounds containing a guanidine group linked to the benzene ring of a benzoic acid (or a derivative thereof), classified under the direct parent group Guanidinobenzoic acids and derivatives. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Benzoic acids and derivatives subclass.

Categories:

Nafamostat is categorized under the following therapeutic classes: Amidines, Analgesics, Analgesics, Non-Narcotic, Anti-Inflammatory Agents, Anticoagulants, Antirheumatic Agents, Complement Inactivating Agents, Enzyme Inhibitors, Fibrinolysin, antagonists & inhibitors, Hematologic Agents, Immunologic Factors, Kallikreins, antagonists & inhibitors, OCT1 substrates, OCT2 Substrates, Peripheral Nervous System Agents, Protease Inhibitors, Sensory System Agents, Serine Protease Inhibitors, Trypsin Inhibitors. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Nafamostat 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.