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QuickView for tramadol (compound)


PubChem
Name: Tramadol
PubChem Compound ID: 10017651
Description: A narcotic analgesic proposed for severe pain. It may be habituating.
Molecular formula: C16H26ClNO2
Molecular weight: 299.836 g/mol
DrugBank
Identification
Name: Tramadol
Name (isomeric): DB00193
Drug Type: small molecule
Description: A narcotic analgesic proposed for severe pain. It may be habituating.
Synonyms:
Tramadol hydrochloride; Tramodol Hcl; Tramadolum [INN-Latin]; Tramadol HCl
Brand: Ultram, Tramadol HCl BP/EP, Ultram ER, Crispin, Ralivia Flashtab, Tridural, Tramal, Ralivia ER, Zydol
Category: Narcotics, Analgesics, Analgesics, Opioid
CAS number: 27203-92-5
Pharmacology
Indication: Indicated in the treatment of moderate to severe pain. Consider for those prone to constipation or respiratory depression. Tramadol is used to treat postoperative, dental, cancer, and acute musculosketetal pain and as an adjuvant to NSAID therapy in patients with osteoarthritis.
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.
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...
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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.
Protein binding: 20%
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.
Route of elimination: Tramadol is eliminated primarily through metabolism by the liver and the metabolites are eliminated primarily by the kidneys. Tramadol and its metabolites are excreted primarily in the urine with observed plasma half-lives of 6.3 and 7.4 hours for tramadol and M1, respectively. Approximately 30% of the dose is excreted in the urine as unchanged drug, whereas 60% of the dose is excreted as metabolites.
Half Life: 23 +/- 10 minutes
Clearance: 5.9 mL/min/Kg [Healthy Adults, 100 mg qid, MD p.o] 8.5 mL/min/Kg [Healthy Adults, 100 mg SD p.o] 6.89 mL/min/Kg [Geriatric, (<75 yr), 50 mg SD p.o.] 4.23 mL/min/Kg [Hepatic Impaired, 50 mg SD p.o.] 4.23 mL/min/Kg [Renal Impaired, Clcr10-3mL/min, 100 mg SD i.v.] 3.73 mL/min/Kg [Renal Impaired, CLcr<5 mL/min, 100 mg SD i.v.] 6.4 mL/min/Kg [Male following a 100 mg IV dose] 5.7 mL/min/Kg [Female following a 100 mg IV dose]
Toxicity: LD50=350mg/kg (orally in mice)
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
RanolazineRanolazine may decrease the effect of Tramadol by decreasing active metabolite production.
ImipramineTramadol increases the risk of serotonin syndrome and seizures. Imipramine may decrease the effect of Tramadol by decreasing active metabolite production.
IsoniazidIsoniazid may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Isoniazid may decrease the effect of Tramadol by decreasing active metabolite production.
TrimipramineTramadol may increase the risk of serotonin syndrome and seizures.
PrimidonePrimidone may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
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