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Ultram: profile and news
Biovail Reports First-Quarter 2006 Financial Results; Company ... May 11, 2006 Biovail 1st-Qtr Profit Rises Sixfold on Wellbutrin (Update3) May 11, 2006 Biovail Faces Generic Competition May 12, 2006 APS: For Migraine and Cluster Headaches, Most Anything Is Worth a ... May 15, 2006 Biovail Q1 Earnings Surge On Strong Sales Of Antidepressant ... May 11, 2006 Biovail to Promote AstraZeneca's Zoladex(R) 3.6mg (Goserelin ... May 2, 2006 Ask the Clinician: Answers to Readers' Questions May 8, 2006 PORK IS A SAFE, HEALTHY, DELICIOUS FOOD Apr 18, 2006 Biovail seeks acquisitions after US$64.5M Q1 profit driven by ... May 11, 2006 Analysis: Botox for Headaches? May 6, 2006 Neuropathic Pain: An Update on Effective Management Strategies May 5, 2006 TheraQuest's Tramadol ER gets fast tracked Apr 18, 2006 Exploring Phantom Limb Pain Apr 17, 2006 FDA Fast Track Designation For Tramadol ER In Painful HIV ... Apr 19, 2006 Other information Indication Indicated in the treatment of moderate to severe pain. Pharmacology Tramadol, a centrally-acting analgesic, exists as a racemic mixture of the trans isomer, with important differences in binding, activity, and metabolism associated with the two enantiomers. Although Tramadol is a synthetic analog of codeine, it has a significantly lower affinity for opioid receptors than codeine. Tramadol is used to treat postoperative, dental, cancer, and acute musculosketetal pain and as an adjuvant to NSAID therapy in patients with osteoarthritis. Mechanism Of Action Tramadol and its O-desmethyl metabolite (M1) are selective, weak OP3-receptor agonists. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. The analgesic properties of Tramadol can be attributed to norepinephrine and serotonin reuptake blockade in the CNS, which inhibits pain transmission in the spinal cord. The (+) enantiomer has higher affinity for the OP3 receptor and preferentially inhibits serotonin uptake and enhances serotonin release. The (-) enantiomer preferentially inhibits norepinephrine reuptake by stimulating alpha(2)-adrenergic receptors. Drug Category Narcotics; Analgesics; ATC:N02AX02 Brand Names/Synonyms Crispin; Ralivia Er; Ralivia Flashtab; TRAMADOL/HCL; Tramadol; Tramadol Hcl; Tramadol Hcl Bp/Ep; Tramadol Hydrochloride; Tramadolum [Inn-Latin]; Tramal; Tramodol Hcl; Ultram; Zydol Dosage Forms TABLET Absorption Racemic tramadol is rapidly and almost completely absorbed after oral administration. The mean absolute bioavailability of a 100 mg oral dose is approximately 75%.The mean peak plasma concentration of racemic tramadol and M1 occurs at two and three hours, respectively, after administration in healthy adults. Interactions -->Interactions for Tramadol: In vitro studies indicate that tramadol is unlikely to inhibit the CYP3A4-mediated metabolism of other drugs when tramadol is administered concomitantly at therapeutic doses. Tramadol 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 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 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 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 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. Use With Cimetidine Concomitant administration of ULTRAM with cimetidine does not result in clinically significant changes in tramadol 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. 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. Chemical IUPAC Name 2-(dimethylaminomethyl)-1-(3-methoxyphenyl)-cyclohexan-1-ol Chemical Formula C16H25NO2 Half Life 23 +/- 10 minutes Drug Type Approved Drug # Accession No APRD00028 CAS Registry Number 27203-92-5 |
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