salsalate

Action and Spectrum

Actions and Spectrum: 

salsalate is a non-steroidal anti-inflammatory drug (NSAID) that is used to relieve pain and inflammation. It works by blocking the production of certain chemicals in the body that cause inflammation. 

Drug Interaction

Adverse Reaction

Frequency undefined: 

GI bleeding 

Hearing impairment  

Nausea 

Vertigo 

Abdominal effects 

Tinnitus 

Black Box Warning

Black Box Warning: 

It is essential to follow the dosage and administration instructions for the medication carefully.

Contraindication / Caution

Contraindication/Caution: 

salsalate should not be used in people hypersensitive to the drug itself. 

Pregnancy / Lactation

Pregnancy consideration:  

Category C 

Breastfeeding warnings:  

Use the drug with caution as its metabolite, salicylate, is secreted in breast milk. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology 

salsalate is commonly used to relieve pain, swelling, and stiffness caused by conditions such as osteoarthritis, rheumatoid arthritis, and gout. It is also used to reduce fever. 

The drug is taken orally, usually 3-4 times a day, with or without food. The recommended dosage is based on the condition being treated, the patient’s age, and other medications they may be taking. 

Pharmacodynamics: 

salsalate selectively inhibits COX-2 enzymes, which are primarily responsible for the synthesis of prostaglandins involved in inflammation and pain. This is why it is classified as a COX-2 selective inhibitor. 

Pharmacokinetics:  

The pharmacokinetics of salsalate describes how the drug is absorbed, distributed, metabolized, and eliminated by the body. 

Absorption 

salsalate is rapidly and completely absorbed from the gastrointestinal tract following oral administration. The peak plasma concentrations are reached within 1-2 hours, and the bioavailability is about 60-70%. 

Distribution 

salsalate is widely distributed in the body, with high concentrations found in the plasma, liver, kidney, and synovial fluid. It is highly protein-bound, primarily to albumin. 

Metabolism 

salsalate is extensively metabolized in the liver, primarily by glucuronidation, a process in which the drug is conjugated with glucuronic acid to form a water-soluble metabolite. This metabolite is then excreted in the urine. 

Elimination and excretion 

The elimination half-life of salsalate is about 2-3 hours, which means that it takes about 2-3 hours for the plasma concentration of the drug to be reduced by half. The drug is eliminated mainly through the urine (about 85-90% of the dose), with a small amount excreted in the feces. 

Adminstartion

Administration: 

salsalate is administered orally in the form of tablets. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: salsalate  

Pronounced: SAL-sa-late 

Why do we use salsalate? 

salsalate is used to treat osteoarthritis and rheumatoid arthritis.