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Theophylline is metabolized extensively in the liver. [2] It undergoes N-demethylation via cytochrome P450 1A2. It is metabolized by parallel first order and Michaelis-Menten pathways. Metabolism may become saturated (non-linear), even within the therapeutic range. Small dose increases may result in disproportionately large increases in serum ...
The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. CYP1A2 localizes to the endoplasmic reticulum and its expression is induced by some polycyclic aromatic hydrocarbons (PAHs), some of which are found in cigarette smoke.
CYP3A4 is a member of the cytochrome P450 superfamily of enzymes.The cytochrome P450 proteins are monooxygenases that catalyze many reactions involved in drug metabolism and synthesis of steroids (including cholesterol), and other lipids.
CYP1A1 is involved in phase I xenobiotic and drug metabolism (one substrate of it is theophylline). It is inhibited by hesperetin (a flavonoid found in lime, sweet orange), [8] fluoroquinolones and macrolides and induced by aromatic hydrocarbons. [9] CYP1A1 is also known as AHH (aryl hydrocarbon hydroxylase).
Cytochrome P450 2E1 (abbreviated CYP2E1, EC 1.14.13.n7) is a member of the cytochrome P450 mixed-function oxidase system, which is involved in the metabolism of xenobiotics in the body. This class of enzymes is divided up into a number of subcategories, including CYP1, CYP2, and CYP3, which as a group are largely responsible for the breakdown ...
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Theophylline has also been marketed in combination with other ephedrine-like sympathomimetics like racephedrine and pseudoephedrine and with other barbiturates such as amobarbital and butabarbital, among other drugs. [15] A combination of theophylline, ephedrine, and hydroxyzine has been marketed under the brand name Marax among others as well.
By definition, when a medication is administered intravenously, its bioavailability is 100%. [ 2 ] [ 3 ] However, when a medication is administered via routes other than intravenous, its bioavailability is lower due to intestinal epithelium absorption and first-pass metabolism .