Tramadol

Name: Tramadol the generic form of Ultram, is an analgesic used to treat or prevent pain

Chemical Name: hydrochloride is (±)cis-2- [(dimethylamino)methyl]-1-(3-methoxyphenyl) cyclohexanol hydrochloride

Chemical Structure



Chemical Information

The molecular weight of tramadol hydrochloride is 299.8. Tramadol hydrochloride is a white, bitter, crystalline and odorless powder. It is readily soluble in water and ethanol and has a pKa of 9.41. The n-octanol/water log partition coefficient (logP) is 1.35 at pH 7. ULTRAM tablets contain 50 mg of tramadol hydrochloride and are white in color. Inactive ingredients in the tablet are corn starch, hypromellose, lactose,magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, sodium starch glycolate, titanium dioxide and wax.

Drug Interactions

In vitro studies indicate that Tramadol (Ultram) is unlikely to inhibit the CYP3A4-mediated metabolism of other drugs when Tramadol (Ultram) is administered concomitantly at therapeutic doses.Tramadol (Ultram) does not appear to induce its own metabolism in humans, since observed maximal plasma concentrations after multiple oral doses are higher than expected based on single-dose data. Tramadol (Ultram) is a mild inducer of selected drug metabolism pathways measured in animals.

Use With Carbamazepine

Patients taking carbamazepine may have a significantly reduced analgesic effect of ULTRAM. Because carbamazepine increases tramadol metabolism and because of the seizure risk associated with tramadol, concomitant administration of ULTRAM and carbamazepine is not recommended.

Use With Quinidine

Tramadol (Ultram) is metabolized to M1 by CYP2D6. Quinidine is a selective inhibitor of that isoenzyme, so that concomitant administration of quinidine and ULTRAM results in increased concentrations of Tramadol (Ultram) and reduced concentrations of M1.The clinical consequences of these findings are unknown. In vitro drug interaction studies in human liver microsomes indicate that Tramadol (Ultram) has no effect on quinidine metabolism.

Use With Inhibitors of CYP2D6

In vitro drug interaction studies in human liver microsomes indicate that concomitant administration with inhibitors of CYP2D6 such as fluoxetine, paroxetine, and amitriptyline could result in some inhibition of the metabolism of Tramadol (Ultram)..

Use With Cimetidine

Concomitant administration of ULTRAM with cimetidine does not result in clinically significant changes in Tramadol (Ultram) pharmacokinetics. Therefore, no alteration of the ULTRAM dosage regimen is recommended.

Use With MAO Inhibitors

Interactions with MAO Inhibitors, due to interference with detoxification mechanisms, have been reported for some centrally acting drugs (see WARNINGS, Use With MAO Inhibitors).

Use With Digoxin and Warfarin

Post-marketing surveillance has revealed rare reports of digoxin toxicity and alteration of warfarin effect, including elevation of prothrombin times.

Children

There is no specific information on the relationship of age to the effects of Tramadol (Ultram) in patients less than 16 years of age.