Dosing and uses of Clinoril, Sulin (sulindac)
Adult dosage forms and strengths
tablet
- 150mg
- 200mg
Ankylosing Spondylitis, Osteoarthritis, Rheumatoid Arthritis
150-200 mg PO q12hr
No more than 400 mg
Use lowest effective dose for shortest possible duration
Shoulder Pain
200 mg PO q12hr for 7-14 days
Gout
200 mg PO q12hr for 7 days
Familial Adenomatous Polyposis (Off-label)
150-200 mg PO q12hr
Renal Impairment
Severe renal impairment: Not recommended; administer lower dose and monitor closely if administration necessary
Hepatic Impairment
Administer lower dose; discontinue if toxicity occurs
Administration
Take with food or 8-12 oz water to avoid GI effects
Other Indications & Uses
Bursitis/bursitis (shoulder), synovitis, tendonitis/tendonitis (shoulder), tenosynovitis
Pediatric dosage forms and strengths
Safety & efficacy not established
Geriatric dosage forms and strengths
Ankylosing spondylitis, osteoarthritis, rheumatoid arthritis
150-200 mg PO q12hr
No more than 400 mg
Use lowest effective dose for shortest possible duration
Shoulder Pain
200 mg PO q12hr for 7-14 days
Gout
200 mg PO q12hr for 7 days
Familial Adenomatous Polyposis (Off-label)
150-200 mg PO q12hr
Clinoril, Sulin (sulindac) adverse (side) effects
1-10%
GI pain (10%)
Constipation (3-9%)
Diarrhea (3-9%)
Dizziness (3-9%)
Dyspepsia (3-9%)
Headache (3-9%)
Nausea (3-9%)
Rash (3-9%)
Abdominal cramps (1-3%)
Anorexia (1-3%)
Edema (1-3%)
Nervousness (1-3%)
Pruritus (1-3%)
Tinnitus (1-3%)
Vomiting (1-3%)
<1%
Hypersensitivity reactions (including anaphylaxis, angioedema, bronchospasm, dyspnea) Sulindac therapy should be discontinued & not reinstituted if unexplained fever or other evidence of hypersensitivity occurs
Thrombocytopenia
Ecchymosis
Purpura
Leukopenia
Agranulocytosis
Neutropenia
Bone marrow depression
CHF (<1%)
Hematuria (<1%)
Renal impairment (including renal failure)
Interstitial nephritis
Nephrotic syndrome
Warnings
Black box warnings
Cardiovascular Risk
- NSAIDs may increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), & stroke, which can be fatal
- Risk may increase with duration of use
- Patients with risk factors for or existing cardiovascular disease may be at greater risk
- NSAIDs are contraindicated for perioperative pain in the setting of coronary artery bypass graft (CABG) surgery (increased risk of MI & stroke)
Gastrointestinal Risk
- NSAIDs increase risk of serious GI adverse events including bleeding, ulceration, & perforation of the stomach or intestines, which can be fatal
- GI adverse events may occur at any time during use & without warning symptoms
- Elderly patients are at greater risk for serious GI events
Contraindications
Absolute: ASA allergy, nursing mother, hypersensitivity
Relative: Bleeding disorder, duodenal/gastric/peptic ulcer, renal calculus, stomatitis, SLE, ulcerative colitis, upper GI disease, late pregnancy (may cause premature closure of ductus arteriosus)
Cautions
Use caution in asthma (bronchial), cardiac disease, CHF, hepatic impairment, hypertension, renal impairment
Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include the elderly, or those with impaired renal function, hypovolemia, heart failure, liver dysfunction, salt depletion, and individuals taking diuretics, ACE inhibitors, or ARBs
Heart Failure(HF) risk
- NSAIDS have the potential to trigger HF by prostaglandin inhibition that leads to sodium and water retention, increased systemic vascular resistance, and blunted response to diuretics
- NSAIDS should be avoided or withdrawn whenever possible
- AHA/ACC Heart Failure Guidelines; Circulation. 2016; 134
Pregnancy and lactation
Pregnancy category: B; D if used for prolonged periods, or near term (may cause premature closure of ductus arteriosus)
The Quebec Pregnancy Registry identified 4705 women who had spontaneous abortions by 20 weeks' gestation; each case was matched to 10 control subjects (n=47,050) who had not had spontaneous abortions; exposure to nonaspirin NSAIDs during pregnancy was documented in approximately 7.5% of cases of spontaneous abortions and in approximately 2.6% of controls. (CMAJ, September 6, 2011; DOI:10.1503/cmaj.110454)
Lactation: not known if distributed in milk
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Clinoril, Sulin (sulindac)
Mechanism of action
Inhibits synthesis of prostaglandins in body tissues by inhibiting at least 2 cyclooxygenase isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2)
May inhibit chemotaxis, may alter lymphocyte activity, decrease proinflammatory cytokine activity, and may inhibit neutrophil aggregation. These effects may contribute to its anti-inflammatory activity
Pharmacokinetics
Half-life: Sulindac (8 hr); sulfide metabolite (16.4 hr)
Peak Plasma Time: 2 hr (sulindac); 5-6 hr (sulfide metabolites)
Concentration: 3-6 mcg/mL
Excretion: Urine (50%); feces (25%)
Bioavailability: 90%
Protein Bound: Approx 93% (sulindac); approx 98% (sulfide metabolite)
Metabolism: Hepatic reduction; significant enterohepatic circulation
Metabolites: Sulfide and sulfone metabolites
Dialyzable: Unknown
Enzymes inhibited: Cyclooxygenase
