|
|
|
|
|
Tramadol
drug data and news
Tramadol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
|
| Generic name | Tramadol | ||
| 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 | ||
| Indication | Indicated in the treatment of moderate to severe pain. | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Tramadol News (When available) |
Grunenthal to market Labopharm's tramadol in Belgium May 11, 2006 TheraQuest's Tramadol ER gets fast tracked Apr 18, 2006 FDA Fast Track Designation For Tramadol ER In Painful HIV ... Apr 19, 2006 Labopharm In Belgian Distrib Pact For Tramadol May 9, 2006 Labopharm to Present at Bank of America Healthcare Conference May 15, 2006 TheraQuest's Tramadol gets fast tracked Apr 19, 2006 Labopharm Enters Into Distribution Agreement with Grunenthal for ... May 9, 2006 Labopharm Enters Into Distribution Agreement with Grunenthal for ... May 9, 2006 APS: For Migraine and Cluster Headaches, Most Anything Is Worth a ... May 15, 2006 Cipher reports first quarter results May 2, 2006 Biovail Reports First-Quarter 2006 Financial Results; Company ... May 11, 2006 Labopharm reports results for first quarter fiscal 2006 Apr 25, 2006 Neuropathic Pain: An Update on Effective Management Strategies May 5, 2006 Labopharm reports results for first quarter fiscal 2006 Apr 25, 2006 Biotech financing up 25 per cent in 2005 May 14, 2006 Biovail Q1 Earnings Surge On Strong Sales Of Antidepressant ... May 11, 2006 Meda AB (publ.) Interim Report January - March 2006 May 3, 2006 Zentiva NV 1st Quarter Results 2006 May 2, 2006 Painkillers label was misread Apr 20, 2006 Man died after drug overdose Apr 21, 2006 FDA fast tracks drug for HIV-related condition Apr 19, 2006 Bulls becoming annoying guests for Heat May 3, 2006 Reaction to drugs putting 250,000 in hospital a year May 11, 2006 PORK IS A SAFE, HEALTHY, DELICIOUS FOOD Apr 18, 2006 Labopharm Enters Into Distribution Agreement With Grunenthal ... May 9, 2006 Shingles pain costs up to $9,000 May 5, 2006 Labopharm prices US$80M public offering: $8 US each for 11M shares Apr 28, 2006 Par Pharmaceutical Reports First-Quarter Sales and Earnings May 1, 2006 Biovail to Promote AstraZeneca's Zoladex(R) 3.6mg (Goserelin ... May 2, 2006 Analysis: Botox for Headaches? May 6, 2006 Exploring Phantom Limb Pain Apr 17, 2006 Labopharm completes public offering for estimated net proceeds of ... May 3, 2006 Cipher receives FDA response to CIP-ISOTRETINOIN NDA submission May 2, 2006 Labopharm completes public offering for estimated net proceeds of ... May 3, 2006 Drugmaker Labopharm to raise $80.9 mln in offering Apr 28, 2006 Biotechs showing a healthy pulse Apr 21, 2006 Body found after police raid home for underage drinking Apr 19, 2006 Suspect may have swallowed evidence Apr 18, 2006 Labopharm's Q1 loss increases to $6.8M Apr 26, 2006 Labopharm to offer stock Apr 19, 2006 Police Log for April 20, 2006 Apr 20, 2006 Labopharm Goes Public On Nasdaq, Raises $88M Gross Apr 28, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Narcotics; Analgesics; ATC:N02AX02 | ||
| 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. | ||
| Toxicity | LD50=350mg/kg (orally in mice) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 2-(dimethylaminomethyl)-1-(3-methoxyphenyl)-cyclohexan-1-ol | ||
| Chemical Formula | C16H25NO2 | ||
| Molecular Weight | 263.375 g/mol | ||
| Smiles String | CN(C)CC1CCCCC1(C2=CC(=CC=C2)OC)O | ||
| Melting Point | 180-181°C | ||
| Water Solubility | Soluble in water. | ||
| State | Solid | ||
| LogP/Hphobicity | 2.951 | ||
| Isoelectric Point | 9.41 | ||
| Biotransformation | The major metabolic pathways appear to be N- and O- demethylation and glucuronidation or sulfation in the liver. One metabolite (O-desmethyltramadol, denoted M1) is pharmacologically active in animal models. | ||
| Half Life | 23 +/- 10 minutes | ||
| Protein Binding [%] | 20% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Tramadol.html http://www.rxlist.com/cgi/generic/tramadol.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00028 | ||
| CAS Registry Number | 27203-92-5 | ||
| KEGG Compound ID | C07153 | ||
| PubChem ID | SID:175579 | ||
| PharmGKB ID | PA451735 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
|
Home | About | Cancers | Treatment | Medications Copyright onconews.org 2005. All Rights Reserved. |