Drug information of Sulindac

Sulindac

فارسی

Sulindac is a nonsteroidal anti-inflammatory agent (NSAID) of the arylalkanoic acid class.Sulindac is a prodrug, derived from sulfinylindene, that is converted in vivo to an active sulfide compound by liver enzymes.

Mechanism of effect

Its anti inflammatory effects are believed to be due to inhibition of both COX-1 and COX-2 which leads to the inhibition of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

Pharmacodynamic

Sulindac is a non-steroidal anti-inflammatory indene derivative, also possessing analgesic and antipyretic activities.

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

Drug indications

artirit rhomatoid

Dosage

Adult

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

Pediatric

Safety & efficacy not established

Alerts

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  • NSAIDS should be avoided or withdrawn whenever possible

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

Points of recommendation

  • High blood pressure has happened with drugs like this one. Have your blood pressure checked as you have been told by your doctor.
  • Talk with your doctor before you drink alcohol.
  • If you smoke, talk with your doctor.
  • If you have asthma, talk with your doctor. You may be more sensitive to sulindac.
  • You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.
  • If you are taking aspirin to help prevent a heart attack, talk with your doctor.
  • This medicine may affect how much of some other drugs are in your body. If you are taking other drugs, talk with your doctor. You may need to have your blood work checked more closely while taking sulindac with your other drugs.
  • Liver problems have happened with drugs like this one. Sometimes, this has been deadly. Call your doctor right away if you have signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
  • This medicine may raise the chance of a very bad brain problem called aseptic meningitis. Call your doctor right away if you have a headache, fever, chills, very upset stomach or throwing up, stiff neck, rash, bright lights bother your eyes, feeling sleepy, or feeling confused.
  • NSAIDs like sulindac may affect egg release (ovulation) in women. This may cause you to not be able to get pregnant. This goes back to normal when sulindac is stopped. Talk with your doctor.
  • Take with food to prevent an upset stomach.
  • Take with a full glass of water.
  • Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.
  • Do not take more than what your doctor told you to take. Taking more than you are told may raise your chance of very bad side effects.
  • Do not take sulindac for longer than you were told by your doctor.
  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

Pregnancy level

B

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