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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 ...
Paraxanthine, also known as 1,7-dimethylxanthine, is a metabolite of theophylline and theobromine, two well-known stimulants found in coffee, tea, and chocolate mainly in the form of caffeine. It is a member of the xanthine family of alkaloids , which includes theophylline, theobromine and caffeine .
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.
CYP1A2 is a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
TH: One of the few exceptions where a drug shows F of over 100% is theophylline. If administered as an oral solution F is 111%, since the drug is completely absorbed and first-pass metabolism in the lung after intravenous administration is bypassed. [22]
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.
The gene is located on chromosome 22q13.1. near two cytochrome P450 pseudogenes (CYP2D7P and CYP2D8P). [16] Among them, CYP2D7P originated from CYP2D6 in a stem lineage of great apes and humans, [17] the CYP2D8P originated from CYP2D6 in a stem lineage of Catarrhine and New World monkeys' stem lineage. [18]
Caffeine is metabolized in the liver into three primary metabolites: paraxanthine (84%), theobromine (12%), and theophylline (4%) Reference: # ^ Caffeine. The Pharmacogenetics and Pharmacogenomics Knowledge Base. Retrieved on 2006-08-14. This reference is somewhat out of date.
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