Search results
Results From The WOW.Com Content Network
An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects.
Drug metabolism is the metabolic breakdown of drugs by living organisms, usually through specialized enzymatic systems. More generally, xenobiotic metabolism (from the Greek xenos "stranger" and biotic "related to living beings") is the set of metabolic pathways that modify the chemical structure of xenobiotics, which are compounds foreign to an organism's normal biochemistry, such as any drug ...
Some benzodiazepines produce active metabolites. Active metabolites are produced when a person's body metabolizes the drug into compounds that share a similar pharmacological profile to the parent compound and thus are relevant when calculating how long the pharmacological effects of a drug will last.
These metabolites are conjugated with glucuronide and are excreted primarily in the urine. Because of these active metabolites, the serum values of diazepam alone are not useful in predicting the effects of the drug. Diazepam has a biphasic half-life of about one to three days and two to seven days for the active metabolite desmethyldiazepam. [20]
It is used to treat anxiety, insomnia and symptoms of withdrawal from alcohol, benzodiazepines, and other drugs. Chlordiazepoxide has a medium to long half-life, while its active metabolite has a very long half-life. The drug has amnesic, anticonvulsant, anxiolytic, hypnotic, sedative, and skeletal muscle relaxant properties. [4]
Clorazepate is a long-acting benzodiazepine drug. [10] Clorazepate produces the active metabolite desmethyl-diazepam, which is a partial agonist of the GABA A receptor and has a half life of 20–179 hours; a small amount of desmethyldiazepam is further metabolised into oxazepam.
Levoamphetamine is a major active metabolite of selegiline (L-deprenyl; N-propargyl-L-methamphetamine). [7] [86] Selegiline is a monoamine oxidase inhibitor (MAOI), specifically a selective inhibitor of monoamine oxidase B (MAO-B) at lower doses and a dual inhibitor of both monoamine oxidase A (MAO-A) and MAO-B at higher doses.
Nordazepam is among the longest lasting (longest half-life) benzodiazepines, and its occurrence as a metabolite is responsible for most cumulative side-effects of its myriad of pro-drugs when they are used repeatedly at moderate-high doses; the nordazepam metabolite oxazepam is also active (and is a more potent, full BZD-site agonist), which ...