Definition
Description
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Route of Elimination: Indomethacin is eliminated via renal excretion, metabolism, and biliary excretion. Half Life: 4.5 hours
- Uses/Sources: For moderate to severe rheumatoid arthritis including acute flares of chronic disease, ankylosing spondylitis, osteoarthritis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis.
- Symptoms: The following symptoms may be observed following overdosage: nausea, vomiting, intense headache, dizziness, mental confusion, disorientation, or lethargy. There have been reports of paresthesias, numbness, and convulsions.
- Treatment: Treatment is symptomatic and supportive. The stomach should be emptied as quickly as possible if the ingestion is recent. If vomiting has not occurred spontaneously, the patient should be induced to vomit with syrup of ipecac. If the patient is unable to vomit, gastric lavage should be performed. Once the stomach has been emptied, 25 or 50 g of activated charcoal may be given. Depending on the condition of the patient, close medical observation and nursing care may be required. The patient should be followed for several days because gastrointestinal ulceration and hemorrhage have been reported as adverse reactions of indomethacin. Use of antacids may be helpful. (L1712)
- Route of Exposure: Parenteral(intravenous); enteral(rectal); oral. Bioavailability is approximately 100% following oral administration and 80-90% following rectal administration.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 50 mg/kg (oral, mice) (based on 14 day mortality response) LD50: 12 mg/kg (oral, rat) (based on 14 day mortality response)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Peroxisome proliferator-activated receptor alpha Peroxisome proliferator-activated receptor gamma Serum paraoxonase/arylesterase 1 Arachidonate 5-lipoxygenase Sodium-dependent dopamine transporter Multidrug resistance-associated protein 1 Aldo-keto reductase family 1 member C3 Solute carrier organic anion transporter family member 1B1 Aldose reductase Solute carrier family 22 member 8 Solute carrier family 22 member 6 Multidrug and toxin extrusion protein 1 Interleukin-8 Prostaglandin E2 receptor EP2 subtype Phospholipase A2, membrane associated Prostaglandin reductase 2 Lactoylglutathione lyase Prostaglandin D2 receptor 2 Aldo-keto reductase family 1 member C1 Canalicular multispecific organic anion transporter 1 Aldo-keto reductase family 1 member C4 Aldo-keto reductase family 1 member C2 Solute carrier organic anion transporter family member 2B1 Solute carrier organic anion transporter family member 1B3 Prostaglandin E synthase Bifunctional epoxide hydrolase 2 Dehydrogenase/reductase SDR family member 9 |
21689932 10411562 14996743 15870392 12130730 23611293 18707884 17346963 21434686 15563582 10991954 22877157 17243824 3097317 9057869 12689521 16030019 21237663 22992107 19000823 19548782 16256979 9013583 22506594 19560921 22541068 11160644 23432095 23241029 |
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Prostaglandin G/H synthase 1 Prostaglandin G/H synthase 2 |
Antiinflammatory effects of Indomethacin are believed to be due to inhibition of cylooxygenase in platelets which leads to the blockage of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. |
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