Chemical: Drug
salsalate

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Overview

Generic Names
  • Salsalatum [inn-latin]
  • Sasapyrine
  • salicylsalicylic acid
Trade Names
  • Disalcid
Brand Mixture Names

PharmGKB Accession Id

PA164745462

Type(s):

Drug

Description

Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo. 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. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours.

Source: Drug Bank

Indication

For relief of the signs and symptoms of rheumatoid arthritis, osteoarthritis and related rheumatic disorders.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The mode of anti-inflammatory action of salsalate and other nonsteroidal anti-inflammatory drugs is not fully defined, but appears to be primarily associated with inhibition of prostaglandin synthesis. This inhibition of prostaglandin synthesis is done through the inactivation of cyclooxygenase-1 (COX-1) and COX-2, which are reponsible 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.

Source: Drug Bank

Pharmacology

Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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.

Source: Drug Bank

Protein Binding

Salicylate: 90-95% bound at plasma salicylate concentrations <100 mcg/mL; 70-85% bound at concentrations of 100-400 mcg/mL; 25-60% bound at concentrations >400 mcg/mL.

Source: Drug Bank

Absorption

Salsalate is insoluble in acid gastric fluids (< 0.1 mg/ml at pH 1.0), 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. The amount of salicylic acid available from salsalate is about 15% less than from aspirin, when the two drugs are administered on a salicylic acid molar equivalent basis (3.6 g salsalate/5 g aspirin). Food slows the absorption of all salicylates including salsalate.

Source: Drug Bank

Half-Life

The parent compound has an elimination half-life of about 1 hour. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours.

Source: Drug Bank

Toxicity

Death has followed ingestion of 10 to 30 g of salicylates in adults, but much larger amounts have been ingested without fatal outcome.

Source: Drug Bank

Chemical Properties

Chemical Formula

C14H10O5

Source: Drug Bank

Isomeric SMILES

c1ccc(c(c1)C(=O)Oc2ccccc2C(=O)O)O

Source: OpenEye

Canonical SMILES

OC(=O)C1=CC=CC=C1OC(=O)C1=CC=CC=C1O

Source: Drug Bank

Average Molecular Weight

258.2262

Source: Drug Bank

Monoisotopic Molecular Weight

258.05282343

Source: Drug Bank

SMILES

OC(=O)C1=CC=CC=C1OC(=O)C1=CC=CC=C1O

Source: Drug Bank

InChI String

InChI=1S/C14H10O5/c15-11-7-3-1-5-9(11)14(18)19-12-8-4-2-6-10(12)13(16)17/h1-8,15H,(H,16,17)

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
PTGS1 (source: Drug Bank )
PTGS2 (source: Drug Bank )

Drug Interactions

Interaction Description
betamethasone - salsalate The corticosteroid, betamethasone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
chlorpropamide - salsalate The salicylate, salsalate, increases the effect of the sulfonylurea, chlorpropamide. (source: Drug Bank )
dexamethasone - salsalate The corticosteroid, dexamethasone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
divalproex sodium - salsalate The salicylate, salsalate, increases the effect of divalproex sodium. (source: Drug Bank )
fludrocortisone - salsalate The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
glibenclamide - salsalate The salicylate increases the effect of sulfonylurea (source: Drug Bank )
glibenclamide - salsalate The salicylate, salsalate, increases the effect of the sulfonylurea, glibenclamide. (source: Drug Bank )
gliclazide - salsalate The salicylate, salsalate, increases the effect of the sulfonylurea, gliclazide. (source: Drug Bank )
hydrocortisone - salsalate The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
methazolamide - salsalate The salicylate, salsalate, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide. (source: Drug Bank )
methotrexate - salsalate The salicylate, salsalate, increases the effect and toxicity of methotrexate. (source: Drug Bank )
prednisolone - salsalate The corticosteroid, prednisolone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
prednisone - salsalate The corticosteroid, prednisone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
probenecid - salsalate The salicylate, salsalate, decreases the uricosuric effect of probenecid. (source: Drug Bank )
sulindac - salsalate Risk of additive toxicity (e.g. bleed risk). Salsalate may decrease the serum concentration of sulindac. Consider alternate therapy or monitor for changes in the therapeutic effects of sulindac and adverse effects of both agents if the interacting agent is initiated, discontinued or dose changed. (source: Drug Bank )
tiaprofenic acid - salsalate Increased risk of gastrointestinal bleeding. (source: Drug Bank )
tolmetin - salsalate Additive effects increase the risk of GI bleeding. Monitor for increased bleeding risk during concomitant therapy. (source: Drug Bank )
trandolapril - salsalate The salicylate, Salsalate, may reduce the efficacy of Trandolapril. Monitor for changes in Trandolapril efficacy if Salsalate is initiated, discontinued or dose changed. (source: Drug Bank )
treprostinil - salsalate The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Salsalate. Monitor for increased bleeding during concomitant thearpy. (source: Drug Bank )
triamcinolone - salsalate The corticosteroid, triamcinolone, may decrease the effect of the salicylate, salsalate. (source: Drug Bank )
No related diseases are available

LinkOuts

DrugBank:
DB01399
KEGG Drug:
D00428
PubChem Compound:
5161
PubChem Substance:
46506882
7847494
ChemSpider:
4977
Therapeutic Targets Database:
DAP000734

Clinical Trials

These are trials that mention salsalate and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.