Sulindac

Trade Names:
Clinoril
- Tablets 200 mg

Trade Names:
Sulindac
- Tablets 150 mg

Pharmacology

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Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

Pharmacokinetics

Absorption

T _max is 3 to 4 h. Approximately 90% of the drug is absorbed after oral administration.

Distribution

93% bound to plasma proteins. Sulindac penetrates the blood-brain and placental barriers.

Metabolism

Recirculation of sulindac and its sulfone metabolite is more extensive than that of the active sulfide metabolite.

Elimination

The t _½ is 7.8 h. The main route of excretion is via the urine. Approximately 25% is found in feces, primarily as the sulfone and sulfide metabolites. Renal Cl is 68 to 74 mL/min.

Special Populations

Use a lower daily dose to avoid excessive drug accumulation.

Plasma concentrations have been reported to be higher in patients with alcoholic liver disease; patients with acute and chronic hepatic disease may require reduced doses.

Pharmacokinetics have not been studied.

Pharmacokinetic differences have not been identified.

Indications and Usage

Treatment of acute and chronic rheumatoid (class I to III) and osteoarthritis, ankylosing spondylitis, acute gouty arthritis, and acute painful shoulder (tendonitis, bursitis).

Unlabeled Uses

Juvenile rheumatoid arthritis.

Contraindications

Patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; treatment of perioperative pain in setting of coronary artery bypass graft (CABG) surgery; hypersensitivity to any component of the product.

Dosage and Administration

PO 200 mg twice daily; therapy for 7 days is usually sufficient.

PO 200 mg twice daily; therapy for 7 to 14 days is usually sufficient.

PO 150 mg twice daily. Adjust dose as needed.

General Advice

• Max dosage is 400 mg/day
• Administer dose with food.

Storage/Stability

Store at 59° to 86° F.

Store at 68° to 77°F.

Drug Interactions

The antihypertensive effect may be decreased by sulindac.

Plasma levels may be elevated by sulindac.

May increase effect of anticoagulants because of decreased plasma protein binding. May increase risk of gastric erosion and bleeding.

Risk of GI adverse reactions may be increased; plasma levels of active sulindac metabolite may be reduced.

Plasma levels of sulindac may be reduced.

Sulindac has increased cimetidine bioavailability.

Risk of cyclosporine toxicity may be increased.

Plasma level of active sulindac metabolite may be reduced.

Dimethyl sulfoxide may decrease formation of active metabolite of sulindac, possibly resulting in decreased therapeutic effect. Also, topical dimethyl sulfoxide with sulindac has resulted in severe peripheral neuropathy.

Decreased diuresis may result.

Risk of hemorrhage may be increased.

May decrease lithium Cl.

May increase methotrexate levels.

Coadministration with other NSAIDs may increase the risk of GI toxicity.

Sulindac plasma levels may be elevated.

Risk of GI bleeding may be increased.

Laboratory Test Interactions

May prolong bleeding time.

Adverse Reactions

Cardiovascular

CHF (less than 1%).

CNS

Dizziness, headache (3% to 9%); nervousness (1% to 3%).

Dermatologic

Rash (3% to 9%); pruritus (1% to 3%).

EENT

Tinnitus (1% to 3%); erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis (less than 1%).

GI

GI pain (10%); constipation, diarrhea, dyspepsia, nausea with or without vomiting (3% to 9%); anorexia, flatulence, GI cramps (1% to 3%).

Hepatic

Elevated LFTs (15%).

Miscellaneous

Edema (1% to 3%).

Precautions

Pregnancy

Category C . Avoid in late pregnancy. Premature closure of ductus arteriosus may occur if sulindac is used in late pregnancy.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Increased risk of adverse reactions.

Hypersensitivity

May occur; use caution in aspirin-sensitive individuals because of possible cross-sensitivity. The reaction may be fatal. Fever and other evidence of hypersensitivity, including LFT abnormalities, skin reactions, and death, have occurred.

Renal Function

Not recommended in patients with advanced renal disease.

Hepatic Function

Delayed, elevated, and prolonged levels of sulindac metabolites may occur.

Anaphylactic/Anaphylactoid reactions

May occur in patients without known prior exposure to sulindac.

Asthma

Do not use in patients with aspirin-sensitive asthma. Use with caution in patients with preexisting asthma.

CHF

Fluid retention and edema may occur.

Hematologic effects

Inhibition of platelet aggregation and prolongation of bleeding time may occur. Anemia, resulting from fluid retention, or occult or gross GI blood loss may occur.

Hypertension

New-onset hypertension or worsening of preexisting hypertension may occur.

Pancreatitis

Has been reported. If pancreatitis is suspected, discontinue and do not restart the drug.

Renal effects

Long-term administration has resulted in renal papillary necrosis and other renal injury.

Renal lithiasis

Use with caution in patients with a history of renal lithiasis.

SLE and mixed connective tissue disease

Risk of aseptic meningitis may be increased in patients with SLE or mixed connective tissue disease.

Overdosage

Symptoms

Coma, death, diminished urine output, hypotension, stupor.

Patient Information

• Advise patient who becomes pregnant to avoid use in late pregnancy because of possible premature closure of the ductus arteriosus.
• Instruct patient to promptly report signs or symptoms of unexplained weight gain or edema to health care provider.
• Advise patient to take medication with food or after meals.
• Tell patient to take medication with full glass of water to prevent medication from lodging in esophagus.
• Emphasize importance of regular medical follow-up, even in absence of adverse reactions or problems related to drug therapy.
• Instruct patient to report the following symptoms of toxicity to health care provider immediately: blurred vision, change in urine (pattern, blood in urine), ringing in ears.
• Tell patient to avoid intake of alcoholic beverages, other NSAIDs, or aspirin during therapy (increases risk of GI irritation/bleeding), especially during long-term therapy.
• Advise patient that drowsiness or dizziness may occur and to use caution while driving or performing other activities requiring mental alertness.

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