Dosing and uses of Salsalate
Adult dosage forms and strengths
tablet
- 500mg
- 750mg
Osteoarthritis
3 g PO divided q8-12hr
Use lowest effective dose for shortest possible duration
Rheumatoid Arthritis
3 g PO divided q8-12hr
Use lowest effective dose for shortest possible duration
Pediatric dosage forms and strengths
Safety & efficacy not established
Geriatric dosage forms and strengths
Osteoarthritis
3 g PO divided q8-12hr
Use lowest effective dose for shortest possible duration
Rheumatoid arthritis
3 g PO divided q8-12hr
Use lowest effective dose for shortest possible duration
Salsalate adverse (side) effects
Frequency not defined
Abdominal effects
Anaphylactic reactions
GI bleed
Hearing impairment
Nausea
Tinnitus
Vertigo
Warnings
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
Contraindications
Hypersensitivity to aspirin or NSAIDs
CABg
Late pregnancy (may cause premature closure of ductus arteriosus)
Relative: Advanced renal disease, viral infections
Cautions
Bleeding disorders, CHF, fluid retention, GI ulcers, concomitant anticoagulants
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
- High dose salicylates should be avoided or withdrawn whenever possible
- AHA/ACC Heart Failure Guidelines; Circulation. 2016; 134
Pregnancy and lactation
Pregnancy category: C
Lactation: metabolite salicylate crosses into breast milk, use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Salsalate
Mechanism of action
Inhibits synthesis of prostaglandins in body tissues by inhibiting at least 2 cyclooxygenase isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2)
May inhibit chemotaxis, may alter lymphocyte activity, decrease proinflammatory cytokine activity, and may inhibit neutrophil aggregation. These effects may contribute to its anti-inflammatory activity
Pharmacokinetics
Half-life eliination: 7-8 hr
Absorption: Complete from intestine; slowed by food
Metabolism: Liver
Metabolites: Salicylic acid (active form)
Excretion: Urine
Dialyzable: yes
