Indomethacin


Description

Indometacin, or indomethacin, is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic properties. NSAIDs consist of agents that are structurally unrelated; the NSAID chemical classification of indometacin...

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Pharmacology

Indication

Oral indometacin is indicated for symptomatic management of moderate to severe rheumatoid arthritis... Read more

Pharmacodynamic

Indometacin is an NSAID with analgesic and antipyretic properties that exerts its pharmacological ef... Read more

Mechanism of action

Indometacin is a nonspecific and reversible inhibitor of the cyclo-oxygenase (COX) enzyme, or prosta... Read more

Absorption

Indometacin displays a linear pharmacokinetics profile where the plasma concentrations and area unde... Read more

Protein binding

Indometacin is a weak organic acid that is 90-99% bound to protein in plasma over the expected range... Read more

Volume of distribution

The volume of distribution ranged from 0.34 to 1.57 L/kg following oral, intravenous, or rectal admi... Read more

Clearance

In a clinical pharmacokinetic study, the plasma clearance of indometacin was reported to range from... Read more

Half life

Indometacin disposition from the plasma is reported to be biphasic, with a half-life of 1 hour durin... Read more

Route of elimination

Indometacin is eliminated via renal excretion, metabolism, and biliary excretion. It is also subject... Read more

Toxicity

Acute oral LD50 is 2.42 mg/kg in rats and 13 mg/kg in mice.[MSDS] The oral LD50 of indomethacin in m... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 11.7%
  • Varying Reports
    Gastrointestinal bleeding, perforation, and ulceration US
  • Kind: experimental
    • Percent: 1-4%
  • Varying Reports
    Peptic Ulcer US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Flatulence US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Bloating US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Anorexia US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Ulcerative stomatitis US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Ileitis US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Colitis US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Gastrointestinal Bleeding US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Rectal Bleeding US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Gastroenteritis US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Ulceration US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Intestinal structures US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Proctitis US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Jaundice US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Toxic heptitis US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Muzziness US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Insomnia US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Muscle Weakness US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Involuntary muscle movement US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Anxiety US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Drowsiness US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Syncope US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Light-headedness US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Psychotic episodes US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Psychic dirsturbancess US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Mental confusion US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Depersonalization US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Aggravation of parkinsonism US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Coma US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Paraesthesia US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Aggravation of epilepsy US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Corneal deposits US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Retinal disturbances US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Peripheral nephropathy US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Convulsion US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Dysarthria US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Hypertension US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Hypotension US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Tachycardia US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Blurred vision US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Diplopia US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Hearing disturbances US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Congestive Heart Failure US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Chest Pain US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Edema US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Palpitations US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Arrhythmia US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports
    Flushing or sweating US
  • Kind: experimental
    • Percent: <1%
  • Varying Reports

    Contraindications

    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Patent Ductus Arteriosus
        • Drugbank Id: DBCOND0031877
        • Name: Neonatal Congenital Heart Disease
        • Drugbank Id: DBCOND0043939
    • Patient Conditions Associated With:
        • Name: Aortic Coarctation
        • Drugbank Id: DBCOND0000541
        • Name: Tetralogy Of Fallot
        • Drugbank Id: DBCOND0065153
        • Name: Pulmonary Atresia
        • Drugbank Id: DBCOND0000569
        • Name: Reduction of Blood Flow
        • Drugbank Id: DBCOND0077897
    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Renal Impairment
        • Drugbank Id: DBCOND0031781
    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Suspected necrotizing enterocolitis
        • Drugbank Id: DBCOND0107642
    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Coagulation Defects
        • Drugbank Id: DBCOND0057558
    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Thrombocytopenia
        • Drugbank Id: DBCOND0006608
    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Intracranial Haemorrhage
        • Drugbank Id: DBCOND0086527
        • Name: Bleeding
        • Drugbank Id: DBCOND0020313
        • Name: Gastrointestinal haemorrhage
        • Drugbank Id: DBCOND0011340
    • Route:
      • Intravenous
    • Regions: US
    • Age Groups:
      • neonatal
      • premature infants
    • Patient Conditions:
        • Name: Proven or suspected untreated infection
        • Drugbank Id: DBCOND0107641
    • Hypersensitivity:
      • true
    • Sex Group: all
    • Regions: US
    • Route:
      • Oral
      • Rectal
    • Regions: US
    • Patient Conditions:
        • Name: History of allergic reaction caused by Anti-Inflammatory Agents, Non-Steroidal
        • Drugbank Id: DBCOND0107640
        • Combination Of:
          • Caused By:
              • Name: Anti-Inflammatory Agents, Non-Steroidal
              • Drugbank Id: DBCOND0052889
          • Included Conditions:
              • Name: History of allergic reaction
              • Drugbank Id: DBCOND0107639
    • Route:
      • Oral
      • Rectal
    • Regions: US
    • Patient Conditions:
        • Name: History of urticaria caused by Anti-Inflammatory Agents, Non-Steroidal
        • Drugbank Id: DBCOND0107638
        • Combination Of:
          • Caused By:
              • Name: Anti-Inflammatory Agents, Non-Steroidal
              • Drugbank Id: DBCOND0052889
          • Included Conditions:
              • Name: History of urticaria
              • Drugbank Id: DBCOND0107637
    • Route:
      • Oral
      • Rectal
    • Regions: US
    • Patient Conditions:
        • Name: History of asthma caused by Anti-Inflammatory Agents, Non-Steroidal
        • Drugbank Id: DBCOND0107636
        • Combination Of:
          • Caused By:
              • Name: Anti-Inflammatory Agents, Non-Steroidal
              • Drugbank Id: DBCOND0052889
          • Included Conditions:
              • Name: History of asthma
              • Drugbank Id: DBCOND0107635
    • Route:
      • Oral
      • Rectal
    • Regions: US
    • With Therapies:
        • Name: Coronary Artery Bypass Graft Surgery
        • Drugbank Id: DBCOND0032060

    Food Interactions

    • Avoid alcohol.
    • Take with food or antacids to reduce irritation.

    Interactions

    Type in a drug name to check for interaction with Indomethacin

    The risk or severity of bleeding and hemorrhage can be increased when Indometacin is combined with (R)-warfarin.
    The risk or severity of bleeding and hemorrhage can be increased when Indometacin is combined with (S)-Warfarin.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 1-benzylimidazole.
    The risk or severity of adverse effects can be increased when Indomethacin is combined with 2-Methoxyethanol.
    The risk or severity of hypoglycemia can be increased when Indometacin is combined with 2,4-thiazolidinedione.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 2,5-Dimethoxy-4-ethylamphetamine.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of bleeding and hemorrhage can be increased when Indometacin is combined with 4-hydroxycoumarin.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 4-Methoxyamphetamine.
    The risk or severity of hypertension can be increased when Indomethacin is combined with 5-methoxy-N,N-dimethyltryptamine.
    The risk or severity of adverse effects can be increased when Indomethacin is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
    Indomethacin may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The metabolism of Indomethacin can be increased when combined with Abatacept.
    The risk or severity of bleeding and hemorrhage can be increased when Indometacin is combined with Abciximab.
    The risk or severity of hypertension can be increased when Indomethacin is combined with Abediterol.
    The serum concentration of Abemaciclib can be increased when it is combined with Indomethacin.
    The risk or severity of adverse effects can be increased when Indomethacin is combined with Abetimus.
    The metabolism of Indomethacin can be decreased when combined with Abiraterone.

    References

    • 1 . Lucas S: The Pharmacology of Indomethacin. Headache. 2016 Feb;56(2):436-46. doi: 10.1111/head.12769. Epub 2016 Feb 11. [PubMed: 26865183]
    • 2 . Helleberg L: Clinical Pharmacokinetics of indomethacin. Clin Pharmacokinet. 1981 Jul-Aug;6(4):245-58. doi: 10.2165/00003088-198106040-00001. [PubMed: 7249487]
    • 3 . Nalamachu S, Wortmann R: Role of indomethacin in acute pain and inflammation management: a review of the literature. Postgrad Med. 2014 Jul;126(4):92-7. doi: 10.3810/pgm.2014.07.2787. [PubMed: 25141247]
    • 4 . Pacifici GM: Clinical pharmacology of indomethacin in preterm infants: implications in patent ductus arteriosus closure. Paediatr Drugs. 2013 Oct;15(5):363-76. doi: 10.1007/s40272-013-0031-7. [PubMed: 23754139]
    • 5 . Jensen KM, Grenabo L: Bioavailability of indomethacin after intramuscular injection and rectal administration of solution and suppositories. Acta Pharmacol Toxicol (Copenh). 1985 Nov;57(5):322-7. [PubMed: 4090993]
    • 6 . Weber M, Kodjikian L, Kruse FE, Zagorski Z, Allaire CM: Efficacy and safety of indomethacin 0.1% eye drops compared with ketorolac 0.5% eye drops in the management of ocular inflammation after cataract surgery. Acta Ophthalmol. 2013 Feb;91(1):e15-21. doi: 10.1111/j.1755-3768.2012.02520.x. Epub 2012 Sep 12. [PubMed: 22970738]
    • 7 . Alvan G, Orme M, Bertilsson L, Ekstrand R, Palmer L: Pharmacokinetics of indomethacin. Clin Pharmacol Ther. 1975 Sep;18(3):364-73. [PubMed: 1100305]
    • 8 . Ricciotti E, FitzGerald GA: Prostaglandins and inflammation. Arterioscler Thromb Vasc Biol. 2011 May;31(5):986-1000. doi: 10.1161/ATVBAHA.110.207449. [PubMed: 21508345]
    • 9 . Rouzer CA, Marnett LJ: Cyclooxygenases: structural and functional insights. J Lipid Res. 2009 Apr;50 Suppl:S29-34. doi: 10.1194/jlr.R800042-JLR200. Epub 2008 Oct 23. [PubMed: 18952571]
    • 10 . HART FD, BOARDMAN PL: INDOMETHACIN: A NEW NON-STEROID ANTI-INFLAMMATORY AGENT. Br Med J. 1963 Oct 19;2(5363):965-70. [PubMed: 14056924]
    • 11 . Indomethacin Capsules (25 mg) - FDA Label [Link]
    • 12 . INDOCIN® (indomethacin) (INDOMETHACIN FOR INJECTION) Drug Label - Merck & Co., Inc. [File]

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