Disalcid (Salsalate) Drug Information: Clinical Pharmacology

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May 27, 2012

Disalcid

Osteoarthritis »

Osteoarthritis facts

Osteoarthritis is a joint inflammation that results from cartilage degeneration.
Osteoarthritis can be caused by aging, heredity, and injury from trauma or disease.
The most common symptom of osteoarthritis is pain in the affected joint(s) after repetitive use.
There is no blood test for the diagnosis of osteoarthritis.
The goal of treatment in osteoarthritis is to reduce joint pain and inflammation while improving and maintaining joint function.

What is osteoarthritis?

Osteoarthritis is a form of arthritis that features the breakdown and eventual loss of the cartilage of one or more joints. Cartilage is a protein substance that serves as a "cushion" between the bones of the joints. Among the over 100 different types of arthritis conditions, osteoarthritis is the most common, affecting over 25 million people in the United Stat...

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Disalcid

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Please Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

CLINICAL PHARMACOLOGY

DISALCID (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 and undergoes rapid esterase hydrolysis in the body; its half-life is about one hour. About 13% is excreted through the kidneys as a glucuronide conjugate of the parent compound, the remainder as salicylic acid and its metabolites. Thus, the amount of salicylic acid available from DISALCID (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).

Salicylic acid biotransformation is saturated at anti-inflammatory doses of DISALCID (salsalate) . Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours. Thus, dosing with DISALCID (salsalate) twice a day will satisfactorily maintain blood levels within the desired therapeutic range (10 to 30 mg/100 ml) throughout the 12-hour intervals. Therapeutic blood levels continue for up to 16 hours after the last dose. The parent compound does not show capacity-limited biotransformation, nor does it accumulate in the plasma on multiple dosing. Food slows the absorption of all salicylates including DISALCID (salsalate) .

The mode of anti-inflammatory action of DISALCID (salsalate) and other nonsteroidal anti-inflammatory drugs is not fully defined. Although salicylic acid (the primary metabolite of DISALCID (salsalate) ) is a weak inhibitor of prostaglandin synthesis in vitro, DISALCID (salsalate) appears to selectively inhibit prostaglandin synthesis in vivo, providing anti-inflammatory activity equivalent to aspirin and indomethacin. Unlike aspirin, DISALCID (salsalate) does not inhibit platelet aggregation.

The usefulness of salicylic acid, the active in vivo product of DISALCID (salsalate) , in the treatment of arthritic disorders has been established. In contrast to aspirin, DISALCID (salsalate) causes no greater fecal gastrointestinal blood loss than placebo.

Last reviewed on RxList: 12/8/2004
This monograph has been modified to include the generic and brand name in many instances.