Pharmacology Book

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Indomethacin

Aka: Indomethacin, Indocin
  1. Mechanism
    1. NSAID in the acetic acid class (indole)
  2. Pharmacokinetics
    1. Half life: 2 hours
  3. Advantages
    1. Only NSAID in suppository form
    2. Most potent NSAID (however this carries renal and GI risks)
  4. Indications
    1. Acute Gouty Arthritis
    2. Ankylosing Spondylitis
    3. Pericarditis
    4. Bartter's Syndrome
    5. Preterm Labor (Tocolysis)
    6. Patent Ductus Arteriosus in the newborn
  5. Contraindications
    1. Peptic Ulcer Disease
    2. Aspirin Sensitivity
    3. Renal Disease
    4. Coagulopathy
    5. Pregnancy beyond 30 weeks
    6. Childhood (except Patent Ductus Arteriosus)
    7. Dementia (consider avoiding in elderly)
  6. Dosing: General Analgesic use
    1. Regular: 25-50 mg PO tid with food or milk
    2. Sustained Release: 75 mg PO qd to bid
    3. Maximum: 200 mg/day
  7. Dosing Protocol: Preterm Labor
    1. Protocol 1
      1. Loading dose: 100 mg suppository rectally
      2. Maintenance: 25 mg PO every 6 hours for 24 hours
      3. Repeat for an additional 24 hours maximum
    2. Protocol 2
      1. Loading dose: 50 mg PO
      2. Maintenance: 25 mg PO every 4 hours for 24 hours
      3. Repeat for an additional 24 hours maximum
    3. Monitoring
      1. Amniotic Fluid Index biweekly for use >48 hours
  8. Adverse Effects (more than other NSAIDs)
    1. Headache
    2. Peptic ulcer
    3. Gastrointestinal upset
    4. Fluid retention
    5. Prolonged Bleeding Time
    6. Nausea or Vomiting
    7. Pruritus
    8. Bowel changes
    9. Fetal effects
      1. Early ductus arteriosus closure
      2. Oligohydramnios
      3. Not linked to Intraventricular Hemorrhage
        1. Suarez (2001) Obstet Gynecol 97:921-5
    10. Nephrotoxic
      1. See Nephrotoxicity due to NSAIDs
  9. Drug Interactions
    1. Lithium

Indomethacin (C0021246)

Definition (CHV) a kind of nonsteroidal anti-inflammatory drug
Definition (NCI) A drug that reduces pain, fever, swelling, and redness. It is also being used to reduce tumor-induced suppression of the immune system and to increase the effectiveness of anticancer drugs. It is a type of nonsteroidal anti-inflammatory drug (NSAID).
Definition (MSH) A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes.
Definition (NCI) A synthetic nonsteroidal indole derivative with anti-inflammatory activity and chemopreventive properties. As a nonsteroidal anti-inflammatory drug (NSAID), indomethacin inhibits the enzyme cyclooxygenase, thereby preventing cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines. This agent also may inhibit the expression of multidrug-resistant protein type 1, resulting in increased efficacies of some antineoplastic agents in treating multi-drug resistant tumors. In addition, indomethacin activates phosphatases that inhibit the migration and proliferation of cancer cells and downregulates survivin, which may result in tumor cell apoptosis. (NCI04)
Definition (CSP) non-steroidal anti-inflammatory agent that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids; also inhibits the motility of polymorphonuclear leukocytes.
Definition (PDQ) A synthetic nonsteroidal indole derivative with anti-inflammatory activity and chemopreventive properties. As a nonsteroidal anti-inflammatory drug (NSAID), indomethacin inhibits the enzyme cyclooxygenase, thereby preventing cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines. This agent also may inhibit the expression of multidrug-resistant protein type 1, resulting in increased efficacies of some antineoplastic agents in treating multi-drug resistant tumors. In addition, indomethacin activates phosphatases that inhibit the migration and proliferation of cancer cells and downregulates survivin, which may result in tumor cell apoptosis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39489&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39489&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C576" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D007213
SnomedCT 363607008, 373513008, 60149003
English 1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, Indometacin, 1-(4-chlorobenzoyl)-5-methoxy- 2-methyl-1-H-indole-3-acetic acid, indomethacin, Indomethacin, Indomethacin product, indomethacin (medication), INDOMETHACIN, Indomethacin [Chemical/Ingredient], Indomethacin (product), Indomethacin (substance), INDO, Indomethacin product (substance), Indometacin product
Swedish Indometacin
Czech indomethacin
Spanish Indometacin product, Indomethacin product (substance), Indomethacin product, indometacina (producto), indometacina (sustancia), indometacina, Indometacina
Finnish Indometasiini
Russian METINDOL, INDOMETATSIN, ИНДОМЕТАЦИН, МЕТИНДОЛ
Croatian INDOMETACIN
Polish Metindol, Indometacyna
Japanese インドメサシン, インドメタシン
French Indométacine
German Indometacin
Italian Indometacina
Portuguese Indometacina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Indocin (C0700798)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D007213
English indocin, Indocin
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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