Sulindac

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Contents 1 Introduction 2 Indications 3 Dosage 4 Pharmacokinetics 5 Monitor 6 Adverse-effects 7 Drug-interactions 8 Laboratory 9 Mechanism-of-action 10 More General Terms 11 Internet Database 12 References

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]
  
• monitor with non steroidal anti-inflammatory agents (NSIADs)

Adverse-effects

• common (> 10%)

• rash, dizziness, abdominal cramps, heartburn, indigestion, nausea

• less common (1-10%)

• itching, ringing in ears, fluid retention, headache, nervousness, vomiting

• 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 adverse effects of NSAIDs

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:

• digoxin
• Li+
• methotrexate
  

• drug interaction(s) of lithium carbonate with NSAIDs
• drug interaction(s) of NSAIDs with SSRIs
• drug interaction(s) of aspirin with NSAIDs
• drug interaction(s) of NSAIDs with beta blockers
• drug interaction(s) of NSAIDs with ARBs
• drug interaction(s) of NSAIDs with ACE inhibitors
• drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
• drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
• drug interaction(s) of NSAIDs & loop diuretics
• drug interaction(s) of NSAIDs & aspirin

Laboratory

• specimen:

• serum, plasma ( EDTA)
• stable for at least 14 days at -20 degrees C

• methods: HPLC, EIA

Mechanism-of-action

• acetic acid class NSAID
• analgesia, antipyretic, anti-inflammatory agent
• non-selective cyclooxygenase inhibitor

More General Terms

• non-steroidal anti-inflammatory agent (NSAID)

Internet Database

PubChem: 5352
PubChem: 1548887
PubChem: 1548885

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 792
3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
5. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
6. Prescriber's Letter 10(5):29 2003
7. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: [1] (subscription needed) [2]

sulindac (Clinoril)