sulindac (Clinoril)
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Introduction
Tradename Clinoril.
Indications
- temporary relief of minor aches, pains, fever & inflammation
- rheumatoid arthritis
- gout
Dosage
150-200 mg PO BID with food; max 400 mg/day
Tabs: 150, 200 mg.
Pharmacokinetics
- reversible metabolized to active sulindac sulfide which reaches peak concentration in 2 hours
- 1/2life of parent molecule is 7 hours; t1/2 of sulfide is 15-16 hours
- sulfide oxidizes irreversible to sulindac sulfone
elimination via liver
1/2life = 7 hours
1/2life = 16 hours active sulfide
protein binding = 93 %
elimination by hemodialysis = -
elimination by peritoneal dialysis = -
Monitor
- liver function tests periodically[7]
Adverse effects
- common (> 10%)
- less common (1-10%)
- 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
- may be less nephrotoxic than other NSAIDs because it is inactivated by enzymes in the kidney[6]
Drug interactions
- corticosteroids:
- increase clearance of salicylates
- increase GI & nephrotoxicity
- ACE inhibitors: decreased antihypertensive effect
- coumadin: prolonged bleeding time
- sulindac may increase plasma levels of:
- drug interaction(s) of direct oral anticoagulants (DOAC) with NSAIDs
- drug interaction(s) of cholinesterase inhibitors with NSAIDs
- drug interaction(s) of lithium carbonate with NSAIDs
- drug interaction(s) of NSAIDs with oral contraceptive
- drug interaction(s) of NSAIDs with SSRIs
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of aspirin with NSAIDs
- drug interaction(s) of apixaban with NSAIDs
- drug interaction(s) of warfarin with NSAIDs
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs with ARBs
- drug interaction(s) of NSAIDs with aldosterone antagonis
- drug interaction(s) of NSAIDs with glucocorticoid
- drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
- drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
- drug interaction(s) of NSAIDs with ACE inhibitors
- drug interaction(s) of NSAIDs & antihypertensives
- drug interaction(s) of NSAIDs & loop diuretics
- drug interaction(s) of NSAIDs & aspirin
Laboratory
Mechanism of action
- acetic acid class NSAID
- analgesia, antipyretic, anti-inflammatory agent
- non-selective cyclooxygenase inhibitor
More general terms
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
- ↑ 6.0 6.1 Prescriber's Letter 10(5):29 2003
- ↑ 7.0 7.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com