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indomethacin (Indocin)
Tradename: Indocin.
Indications:
- temporary relief of minor pains, fevers & inflammation
- bursitis
- treatment of acute flairs of gout
- treatment of pericarditis
- alternative to surgery for closure of patent ductus arteriosus in neonates
- Bartter syndrome [5]
- nephrogenic diabetes insipidus
- premature labor [5]
Contraindications:
1) other NSAIDs
2) active GI bleeding
3) peptic ulcer disease
4) impaired renal function
5) platelet count < 60,000/mm3
6) may excerbate asthma [6]
Dosage: 25-50 mg TID, max 200 mg/day
Tabs: 25 & 50 mg tabs
Suppository: 50 mg
Suspension: 25 mg/5 mL.
Indocin SR: 75 mg PO BID/QD. 75 mg.
Pharmacokinetics:
1) rapid absorption from the GI tract
2) onset of action: within 30 minutes to several hours
3) extensive enterohepatic recirculation
4) duration of action 4-12 hours
5) 1/2life is 2.4 hours
Adverse effects:
1) common (> 10%)
a) skin rash
b) dizziness
c) abdominal cramps
d) heartburn
e) indigestion
f) nausea
2) less common (1-10%)
- itching, tinnitus, fluid retention, headache, nervousness, vomiting
3) uncommon (< 10%)
- congestive heart failure, hypertension, arrhythmias,epistaxis, confusion, hallucinations, aseptic meningitis, mental depression, peripheral neuropathy, hives, erythema multiforme, epidermal necrolysis, Stevens-Johnson syndrome, gastritis, GI ulceration, cystitis, agranulocytosis, anemia, bone marrow suppression, leukopenia, thrombocytopenia, hepatitis, angioedema, allergic rhinitis, toxic amblyopia, blurred vision, conjunctivitis, dry eyes, hearing loss, polyuria, shortness of breath, polydipsia, tachycardia, hot flashes, drowsiness, insomnia, acute renal failure
Drug interactions:
1) corticosteroids
a) increase the clearance of salicylates
b) increased renal toxicity when used in combination
2) decreased antihypertensive effect of ACE inhibitor
3) increased anticoagulant effect of warfarin
4) aluminum & magnesium hydroxide may decrease rate but not extent of indomethacin absorption
5) bicarbonate increases rate of indomethacin absorption
6) probenecid increases indomethacin concentrations
7) indomethacin may decrease renal elimination of:
a) Li+
b) digoxin
c) methotrexate
8) indomethacin may inhibit diuretic effect of furosemide
Laboratory:
1) specimen:
a) serum, plasma (EDTA), urine, gastric fluid
b) stable for at least 14 days at -20 degrees C
2) methods:
a) serum/plasma: HPLC, GC, GC-MS, TLC, RIA, EIA
b) urine: GC, HPLC, TLC, RIA
3) labs with Loincs
- indomethacin in specimen
- indomethacin in gastric fluid
- indomethacin in serum/plasma
- indomethacin in urine
Mechanism of action:
1) acetic acid class NSAID
2) analgesic
3) antipyretic
4) anti-inflammatory agent
Interactions
drug interactions
drug adverse effects of NSAIDs
monitor with non steroidal anti-inflammatory agents (NSIADs)
General
indole
non-steroidal anti-inflammatory agent (NSAID)
peroxisome proliferator; PPAR agonist; PPAR gamma agonist
Properties
INHIBITS: cyclooxygenase
MISC-INFO: elimination route LIVER
1/2life 1-16 HOURS
therapeutic-range 0.5-3.0 UG/ML
protein-binding >90%
elimination by hemodialysis -
peritoneal dialysis -
pregnancy-category ?
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed,
WB Saunders, Philadelpha 1995
- Deprecated Reference
- NEJM Knowledge+ Allergy/Immunology