Sulindac

Sulindac (sul-in’-dak) is a NSAID from the arylalkanoic acid class of drugs used to help manage a range of musculoskeletal problems, especially osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, tendinitis and shoulder bursitis. It takes it name from sul(finyl)-ind(ene)-ac(etic acid). Sulindac has been in use since 1976.

Also used to reduce growth of polyps and precancerous lesions in the colon in those with familial adenomatous polyposis.

Mechanism of action:
Sulindac is a prodrug derived from sulfinylindene, that is converted in the liver to an active sulfide compound whose mechanism is not totally clear, but probably that acts on the COX-1 and COX-2 enzymes to inhibit prostaglandin synthesis. .

Pharmacokinetics:
Bioavailability is about 90% after oral ingestion.
Initially metabolised by a reversible reduction to the sulphide metabolite and then irreversible oxidation to the sulfone metabolite.
The mean elimination half-life of sulindac is 7.8 hours and for its metabolites, it is 16.4 hours.
Excretion is mainly via the renal (50%) and faecal (25%) routes.

Adverse effects:
Common side effects include stomach pain, diarrhea, constipation, indigestion, nausea, dizziness.
Increased risk for cardiovascular events.

Contraindications:
Known hypersensitivity; Severe hepatic, renal or cardiac failure; last trimester of pregnancy.

Dosage:
Typically, 150-200 mg twice per day taken with food.

Overdose:
Clinical features: disorientation, loss of consciousness, a diminished urine output, hypotension, blurred vision.
Management: symptomatic; airway management; activated charcoal or gastric lavage within one hour of ingestion if life-threatening; monitor renal and liver function.
Recovery is usual outcome but may have kidney damage requiring long-term dialysis.

Precautions:
Used with caution if have peptic ulcer disease.
Sulindac has not been established as being safe for use in pregnant or lactating women.

Interactions:
May reduce the effect of antihypertensives.
Decreased elimination of lithium.
Reduces effects of diuretics.
May exacerbate cardiac failure in those on cardiac glycosides.
Decreases elimination of methotrexate.
Increased risk of GI ulceration or bleeding if on corticosteroids.
May increase the effects of anti-coagulants (eg warfarin)
Use with probenecid leads to increased levels in plasma of sulindac.

Brand names: Clinoril (Merck), Imbaral
Chemical formula: C₂₀H₁₇FO₃S
Systematic chemical name: 2-[(1Z)-5-fluoro-1-[(4-methanesulfinylphenyl)methylidene]-2-methyl-1H-inden-3-yl]acetic acid
Availability: Prescription only

Patient education:
Take with food.
Avoid alcohol or maybe an increased risk of gatrointestinal bleeding.
Advice on how to be alert for the symptoms of cardiovascular thrombotic events.

In Australia, Sulindac is on the National Podiatry Scheduled Medicines List for use by authorised podiatrists.

Other nonsteroidial anti-inflammatory drugs (NSAID’s):

Preferential COX-2 Inhibitors
Diclofenac	Nimesulide	Aceclofenac	Meloxicam	Etodolac

Selective COX-2 Inhibitors
Celecoxib	Etoricoxib	Parecoxib	Rofecoxib

Nonselective COX-2 Inhibitors
Salicylates:	Aspirin
Propionic acid derivatives:	Ibuprofen	Naproxen	Ketoprofen	Flurbiprofen
Enolic Acid derivatives:	Prioxicam	Tenoxicam
Acetic Acid derivatives:	Ketorolac	Indomethacin	Nabumetone
Pyrazolane derivatives:	Phenylbutazone	Oxyphenbutazone
Indeneacetic acid derivatives:	Sulindac
Fenamate:	Mephenamic acid

Analgesic & Antipyretics with a weak anti-inflammatory action
Para aminophenol derivatives:	Paracetamol (Acetaminophen)
Benzoxazocine derivatives:	Nefopam
Pyrazolone derivatives:	Propiphenazone	Metamizol

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