SALSALATE

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DRUGS
SALSALATE

Salsalate is a nonsteroidal anti-inflammatory drug (NSAID). It is mainly used for treating pain and inflammation caused due to arthritis and rheumatoid arthritis. It works by blocking several different chemical processes within the body that cause pain and inflammation.

Introduction

Salsalate is a nonsteroidal anti-inflammatory drug (NSAID). It is mainly used for treating pain and inflammation caused due to arthritis and rheumatoid arthritis. It works by blocking several different chemical processes within the body that cause pain and inflammation.

Pharmacological class: NSAID

Indications

  • Osteoarthritis

  • Rheumatoid Arthritis

Pharamcological Action

Salsalate is believed to act primarily through the inhibition of prostaglandin synthesis. This prostaglandin synthesis inhibition is done through the inactivation of cyclooxygenase-1 (COX-1) and COX-2, which are responsible for catalyzing the formation of prostaglandins in the arachidonic acid pathway. Although salicylic acid (the primary metabolite of salsalate) is a weak inhibitor of prostaglandin synthesis in vitro, salsalate appears to selectively inhibit prostaglandin synthesis in vivo, providing anti-inflammatory activity equivalent to aspirin and indomethacin. Unlike aspirin, salsalate does not inhibit platelet aggregation.

Dosage

  • Osteoarthritis: 3000 mg orally, daily in divided doses

  • Rheumatoid Arthritis: 3000 mg orally, daily in divided doses

Pharmacokinetics

Salsalate is insoluble in acid gastric fluids, but readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged. Food slows the absorption of all salicylates including salsalate. Salsalate is readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged and undergoes rapid esterase hydrolysis in the body. The parent compound has an elimination half-life of about 1 hour.

Contraindications

  • Contraindicated in patients hypersensitive to salsalate.

  • Contraindicated in patients with increased cardiovascular event risk and disease of heart and blood vessels.

  • Contraindicated in patients with severe liver disease, bleeding of the stomach or intestines and kidney disease.

  • Contraindicated in pregnant and breast feeding women.

Drug Interactions

  • Concomitant administration of salsalate with anti-platelet drugs such as clopidogrel, "blood thinners" such as dabigatran/enoxaparin/warfarin, may increase the risk of bleeding

  • Aspirin and other salicylate drugs may increase plasma concentrations of salsalate to toxic levels

  • Salicylates may enhance the hypoglycemic effect of oral antidiabetic drugs of the sulfonylurea class

  • Salicylate competes with a number of drugs for protein binding sites, notably penicillin, thiopental, thyroxine, triiodothyronine, phenytoin, sulfinpyrazone, naproxen, warfarin, methotrexate, and possibly corticosteroids.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Stomach upset

  • Heartburn

  • Mild dizziness

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Sudden numbness or weakness

  • Easy bruising or bleeding

  • Fever and chills

  • Urinating more or less than usual

  • Severe stomach pain

  • Nausea or vomiting

  • Dark urine

  • Jaundice (yellowing of the skin or eyes)

Very rare (affecting less than 1 in 10,000)

  • Feeling like passing out

  • Chest pain

  • Severe dizziness

  • Shortness of breath

  • Slurred speech

  • Problems with vision or balance

  • Black, bloody, or tarry stools

  • Coughing up blood or vomit that looks like coffee grounds

  • Hearing problems, ringing in ears

  • Fast or pounding heartbeats

Precautions

  • Avoid in patients with less than 18 years of age

  • Avoid long term use of salsalate

  • Avoid bruising and injury, as it may reduce platelet counts

  • Avoid consumption of alcohol

Clinic Evidence

  • Total 301 patients meeting the ACR criteria for RA were drawn from 16 centers. After withdrawal of NSAIDs and subsequent flare, patients were randomized to receive either salsalate or diclofenac for 8 weeks, according to a double blind, double dummy protocol. Initial doses of salsalate 3.0 g/day and diclofenac 75 mg/day were titrated for the first 5 weeks. The primary outcome measure was a multivariate analysis at 8 weeks of tender joint count, pain, visual analog scale score, and physician's global assessment. A 190 patients completed the study. All outcomes showed a tendency for more improvement with salsalate. Salsalate is as efficacious as diclofenac. It may be considered an alternative to other NSAID as the first line treatment of patients with RA.1

References

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