Sulindac

BRANDS OF SULINDAC IN KENYA

No brands Available


Sulindac Structure: in Kenya
Sulindac Chemical Structure

SULINDAC MODE OF ACTION

Sulindac is a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition.

INDICATIONS:

Sulindac is a non-steroidal anti-inflammatory drug with analgesic and antipyretic activity and is indicated in rheumatoid arthritis, osteoarthritis, acute gouty arthritis, ankylosing spondylitis and musculoskeletal and periarticular disorders such as tendinitis, tenosynovitis, and bursitis.

DOSAGE AND ADMINISTRATION:

Sulindac should be administered orally twice a day with food. The maximum dosage is 400 mg per day. Dosages above 400 mg per day are not recommended.
In osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis, the recommended starting dosage is 150 mg twice a day. The dosage may be lowered or raised depending on the response.
A prompt response (within one week) can be expected in about one-half of patients with osteoarthritis, ankylosing spondylitis, and rheumatoid arthritis. Others may require longer to respond.
In acute painful shoulder (acute subacromial bursitis/supraspinatus tendinitis) and acute gouty arthritis, the recommended dosage is 200 mg twice a day. After a satisfactory response has been achieved, the dosage may be reduced according to the response. In the acute painful shoulder, therapy for 7 to 14 days is usually adequate. In acute gouty arthritis, therapy for 7 days is usually adequate.

CONTRAINDICATIONS:

Hypersensitivity to the active substance or any of the excipients NSAIDs are contraindicated in patients who have previously shown hypersensitivity reactions (e.g. asthma, rhinitis, angioedema or urticaria) in response to ibuprofen, aspirin, or other non-steroidal anti-inflammatory drugs.
Severe hepatic, renal, and cardiac failure.
During the last trimester of pregnancy.
Active or history of recurrent peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
History of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
Use with concomitant NSAIDs including cyclooxygenase 2 specific inhibitors.

DRUG INTERACTIONS:

Other analgesics including cyclooxygenase-2 selective inhibitors: Avoid concomitant use of two or more NSAIDs (including aspirin) as this may increase the risk of adverse effects.
Anti-hypertensives:  reduced anti-hypertensive effect.
Diuretics: Reduced diuretic effect. Diuretics can increase the risk of nephrotoxicity of NSAIDs.
Cardiac glycosides: NSAIDs may exacerbate cardiac failure, reduce GFR and increase plasma glycoside levels.
Lithium: Decreased elimination of lithium.
Methotrexate: Decreased elimination of methotrexate.
Ciclosporin: Increased risk of nephrotoxicity. Renal function should be carefully monitored.
Mifepristone: NSAIDs should not be used for 8-12 days after mifepristone administration as NSAIDs can reduce the effect of mifepristone.
Corticosteroids: Increased risk of GI ulceration or bleeding.
Anti-coagulants: NSAIDs may enhance the effects of anti-coagulants, such as warfarin. Patients should be carefully monitored to ascertain that no change in their anticoagulant dosage is necessary.
Quinolone antibiotics: Animal data indicate that NSAIDs can increase the risk of convulsions associated with quinolone antibiotics. Patients taking NSAIDs and quinolones may have an increased risk of developing convulsions.
Anti-platelet agents and selective serotonin reuptake inhibitors (SSRIs): Increased risk of gastrointestinal bleeding.
Tacrolimus: Possible increased risk of nephrotoxicity when NSAIDs are given with tacrolimus.
Probenecid: Use of probenecid with sulindac leads to increased levels in the plasma of sulindac and the inactive sulphone metabolite.
Diflunisal: Concurrent administration with diflunisal may lead to a reduction in the plasma level of the active metabolite of sulindac.
Dimethyl sulfoxide: Concurrent use of dimethyl sulfoxide and sulindac is not recommended since this has been shown to lead to both a reduction in plasma levels of the active sulfide metabolite and to causing peripheral neuropathy.
Zidovudine: Increased risk of hematological toxicity when NSAIDs are given with zidovudine. There is evidence of an increased risk of haemarthroses and hematoma in HIV(+) hemophiliacs receiving concurrent treatment with zidovudine and ibuprofen.

ADVERSE REACTIONS:

Gastrointestinal: The most commonly observed adverse events are gastrointestinal. Peptic ulcers, perforation or GI bleeding, sometimes fatal, particularly in older people, may occur Nausea, vomiting, anorexia, diarrhea, flatulence, constipation, gastrointestinal cramps, dyspepsia, abdominal pain, melaena, haematemesis, pancreatitis, ulcerative stomatitis, exacerbation of colitis and Crohn’s disease  have been reported following administration. Less frequently, gastritis and gastroenteritis have been observed. Pancreatitis has been reported very rarely.
Hypersensitivity: Hypersensitivity reactions have been reported following treatment with NSAIDs. These may consist of (a) non-specific allergic reactions and anaphylaxis (hypersensitivity vasculitis) (b) respiratory tract reactivity comprising asthma, aggravated asthma, bronchospasm, dyspnoea or epistaxis or (c) assorted skin disorders, including rashes of various types, sore or dry mucous membranes, pruritus, urticaria, purpura, angioedema, alopecia and, more rarely exfoliative and bullous dermatoses (including toxic epidermal necrolysis, erythema multiforme and Stevens-Johnson syndrome).
Cardiovascular: Oedema, hypertension and cardiac failure have been reported in association with NSAID treatment. Less frequently, congestive heart failure, especially in patients with marginal cardiac function, palpitation, hypertension and arrhythmia, has been reported with sulindac. Clinical trial and epidemiological data suggest that use of some NSAIDs (particularly at high doses and in long term treatment) may be associated with an increased risk of arterial thrombotic events (for example myocardial infarction or stroke) ).
Other adverse events reported less commonly include:
Genito-urinary: urine discoloration, vaginal bleeding, haematuria, proteinuria, crystalluria, gynaecomastia
Renal: Nephrotoxicity in various forms, including interstitial nephritis, nephrotic syndrome and renal failure.
Hepatic: Abnormal liver function, hepatitis, cholestasis, and jaundice.
Neurological and special senses: Visual disturbance including blurred vision, optic neuritis, decreased hearing, metallic or bitter taste, headaches, paraesthesia, reports of aseptic meningitis (especially in patients with existing auto-immune disorders, such as systemic lupus erythematosus, mixed connective tissue disease), with symptoms such as the stiff neck, headache, nausea, vomiting, fever or disorientation, depression, nervousness, confusion, hallucinations, convulsions, syncope, psychic disturbances including acute psychosis, tinnitus, vertigo, somnolence, insomnia, sweating, asthenia, dizziness, malaise, fatigue, and drowsiness.
Haematological: Thrombocytopenia, neutropenia, agranulocytosis, leucopenia, bone marrow depression including aplastic anemia, hemolytic anemia, increased prothrombin time in patients on oral anticoagulants
Metabolic: hyperkalemia, hyperglycemia
Dermatological: photosensitivity, ecchymosis, purpura.

Reporting of suspected adverse reactions

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:

Clinical | Pharmacokinetic data


Pregnancy Category: C
Routes of Administration: Oral
Bioavailability: Approximately 90% (Oral)
Protein Binding: Not Available
Metabolosim: Not Available
Onset of Action: Not Available
Elimination Half life: 7.8 hours, metabolites up to 16.4 hours
Excretion: Renal (50%) and fecal (25%)

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This Drug is not Subject to DDA drugs Act
Dosage Forms | Strengths:
Tablets

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References/ Citation:




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