Active metabolite information

An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental...

biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions...

Due to opening of the thiophene ring, the chemical structure of the active metabolite has three sites that are stereochemically relevant, making a total...

pharmacologically active metabolites. The main active metabolite of diazepam is desmethyldiazepam (also known as nordazepam or nordiazepam). Its other active metabolites...

and 1,100 nM. Trazodone has a minor active metabolite known as meta-chlorophenylpiperazine (mCPP), and this metabolite may contribute to some degree to the...

sold under the tradename Hidrasec, among others. Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on...

derivatives with antiparasitic and antiviral activity. Tizoxanide, an active metabolite of nitazoxanide in humans, is also an antiparasitic drug of the thiazolide...

metabolized in the liver to the active metabolite, 6-methoxy-2-naphthyl acetic acid. Nabumetone's active metabolite inhibits the cyclooxygenase enzyme...

O-desmethyltramadol (O-DSMT), is an opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 to...

only active metabolite, norfluoxetine. Both drugs are also potent inhibitors of CYP2D6. The extremely slow elimination of fluoxetine and its active metabolite...

in critically ill patients, as accumulation of midazolam and its active metabolites may occur. Kidney or liver impairments may slow down the elimination...

of protein binding with amitriptyline. Since amitriptyline and its active metabolite nortriptyline are primarily metabolized by cytochromes CYP2D6 and...

approval in other countries, however. Paliperidone (Invega) – Primary, active metabolite of risperidone that was approved in 2006. Perospirone † – Has a higher...

(September 1997). "Actions of tramadol, its enantiomers and principal metabolite, O-desmethyltramadol, on serotonin (5-HT) efflux and uptake in the rat...

is absorbed and extensively conjugated to a phenolic glucuronide (active metabolite). Mean Cmax (45–71 ng/ml) of ezetimibe-glucuronide is attained within...

other drugs. Chlordiazepoxide has a medium to long half-life but its active metabolite has a very long half-life. The drug has amnesic, anticonvulsant, anxiolytic...

volume. As a prodrug, perindopril is hydrolyzed in the liver to its active metabolite, perindoprilat. It was patented in 1980 and approved for medical use...

Norcocaine is a minor metabolite of cocaine. It is the only confirmed pharmacologically active metabolite of cocaine, although salicylmethylecgonine is...

variants of CYP2D6 enzymes may not produce adequate amounts of the active metabolite (desmetramadol) for effective pain control. Sleep medicine physicians...

effects associated with terfenadine, and so both loratadine and its active metabolite, desloratadine, are currently marketed. Approximately 10% of all marketed...

is active in both stationary and growth phases of bacterial replication. Enrofloxacin is partially deethylated by CYP450 into the active metabolite ciprofloxacin...

certain cardiovascular disorders. Gidazepam is a prodrug for its active metabolite 7-bromo-2,3-dihydro-5-phenyl-1H-1,4-benzodiazepin-2-one (desalkylgidazepam...

netarsudil is cleaved by esterases in the cornea to AR-13503, which is the active metabolite. Concentrations reached in the blood plasma are so low that they are...

Inactive lisdexamfetamine is completely (>98%) converted to its active metabolite D-amphetamine in the circulation (Pennick, 2010; Sharman and Pennick...

receptor. They are all prodrugs which need to be converted to an active metabolite in-vivo to inhibit the P2Y12 receptor. On the other hand, novel drugs...

an active metabolite of the anticonvulsant drug primidone, although it is produced in a much lower concentration than phenobarbital, the other active metabolite...

to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects...