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sulindac (Clinoril)
Tradename Clinoril.
Indications:
1) temporary relief of minor aches, pains, fever & inflammation
- bursitis
2) rheumatoid arthritis
3) gout
Dosage: 150-200 mg PO BID with food; max 400 mg/day
Tabs: 150, 200 mg.
Pharmacokinetics:
1) reversible metabolized to active sulindac sulfide which reaches peak concentration in 2 hours
2) 1/2life of parent molecule is 7 hours; t1/2 of sulfide is 15-16 hours
3) sulfide oxidizes irreversible to sulindac sulfone
Monitor:
- liver function tests periodically [7]
Adverse effects:
1) common (> 10%)
- rash, dizziness, abdominal cramps, heartburn, indigestion, nausea
2) less common (1-10%)
- itching, ringing in ears, fluid retention, headache, nervousness, vomiting
3) uncommon (< 1%)
- congestive heart failure, hypertension, arrhythmia, epistaxis, confusion, hallucinations, aseptic meningitis, depression, peripheral neuropathy, urticaria, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, gastritis, GI ulceration, cystitis, agranulocytosis, anemia, hemolytic anemia, bone marrow suppression, leukopenia, thrombocytopenia, hepatitis, angioedema, allergic rhinitis, toxic amblyopia, blurred vision, conjunctivitis, dry eyes, decreased hearing, polyuria, shortness of breath, polydipsia, tachycardia, hot flashes, drowsiness, insomnia, acute renal failure
4) may be less nephrotoxic than other NSAIDs because it is inactivated by enzymes in the kidney [6]
Drug interactions:
1) corticosteroids:
a) increase clearance of salicylates
b) increase GI & nephrotoxicity
2) ACE inhibitors: decreased antihypertensive effect
3) coumadin: prolonged bleeding time
4) sulindac may increase plasma levels of:
a) digoxin
b) Li+
c) methotrexate
Laboratory:
1) specimen:
a) serum, plasma (EDTA)
b) stable for at least 14 days at -20 degrees C
2) methods: HPLC, EIA
Mechanism of action:
1) acetic acid class NSAID
2) analgesia, antipyretic, anti-inflammatory agent
3) non-selective cyclooxygenase inhibitor
Interactions
drug interactions
drug adverse effects of NSAIDs
monitor with non steroidal anti-inflammatory agents (NSIADs)
General
non-steroidal anti-inflammatory agent (NSAID)
Properties
INHIBITS: cyclooxygenase
MISC-INFO: elimination route LIVER
1/2life 7 HOURS
16 HOURS
protein-binding 93%
elimination by hemodialysis -
peritoneal dialysis -
pregnancy-category D <3rd trimester>
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Saunders Manual of Medical Practice, Rakel (ed),
WB Saunders, Philadelphia, 1996, pg 792
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Prescriber's Letter 10(5):29 2003
- Prescriber's Letter 17(7): 2010
Recommended Lab Monitoring for Common Medications
Liver Function Test Scheduling
Detail-Document#: 260704
(subscription needed) http://www.prescribersletter.com