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Sometimes drugs are formulated in an inactive form that is designed to break down inside the body to form the active drug. These are called prodrugs.The reasons for this type of formulation may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better absorbed by the body or has superior pharmacokinetics (e.g., lisdexamphetamine).
Oxazepam is an active metabolite formed during the breakdown of diazepam, nordazepam, and certain similar drugs. It may be safer than many other benzodiazepines in patients with impaired liver function because it does not require hepatic oxidation, but rather, it is simply metabolized by glucuronidation , so oxazepam is less likely to ...
Metabolism of ticlopidine, clopidogrel and prasugrel to an active metabolite. Clopidogrel is a prodrug that is metabolized by two pathways. In one of the pathway most of the dose of clopidogrel (85%) is hydrolyzed by esterases to an inactive carboxylic acid derivate and rapidly cleared via glucoridination followed by renal excretion .
Drugs altering hepatic microsomal enzyme activity (e.g., alcohol, barbiturates, rifampicin, or phenytoin) may result in accelerated metabolism of cyclophosphamide into its active metabolites, increasing both pharmacologic and toxic effects of the drug; alternatively, drugs that inhibit hepatic microsomal enzymes (e.g. corticosteroids, tricyclic ...
Treatment is discontinued in up to 30% of patients due these effects but therapeutic drug monitoring of the biologically active metabolites, i.e. thiopurine nucleotides can help to optimize the efficacy and safety. Clinically, most hospitals resort to ion-exchange LC-MS (liquid chromotography – mass spectrometry) but the newly developed ...
Teriflunomide is the active metabolite of leflunomide, responsible for its therapeutic actions. It results from the reaction of isoxazole ring opening, which occurs in vivo . Teriflunomide then can interconvert between the E and Z enolic forms (and the corresponding keto-amide), with the Z -enol being the most stable and therefore most ...
Treatment is discontinued in up to 30% of patients due these effects but therapeutic drug monitoring of the biologically active metabolites, i.e. thiopurine nucleotides can help to optimize the efficacy and safety. Clinically, most hospitals resort to on-exchange LC-MS (liquid chromatography - mass spectrometry) but the newly developed approach ...
As with other benzodiazepines, in case of abrupt discontinuation following prolonged use, severe withdrawal symptoms may occur including restlessness, anxiety, insomnia, seizures, convulsions and death, though because of its intermediate half-life [17] [18] [19] as well as that of its active metabolites, these withdrawal symptoms may take two ...