Biomaterial Database

[Pharmacokinetics of second generation antidepressants]. 2000

M Grzesiak, and J A Beszłej, and A Kiejna

Katedry i Kliniki Psychiatrii AM we Wrocławiu.

This paper presents the pharmacokinetic properties of newer second generation antidepressants, with an emphasis on the main metabolic pathways of drugs and metabolites as well as their effects on the cytochrome P450 enzymes. Except for Milnacipran all newer antidepressants are biotransformed in the presence of at least one cytochrome P450 izoenzyme. Drugs and their metabolites may be the substrates or inhibitors of cytochromes P450. The knowledge of drugs' metabolic pathways as well as the knowledge of substrates and inhibitors of izoenzymes assists in choice of a proper drug and its dose. It is particularly important in case of polypharmacotherapy when there is a high risk of adverse events. It is also important to remember about genetic polymorphism of some cytochrome P450 izoenzymes (CYP2D6, CYP2C19) that underlies the marked inpatient variability in drug metabolism.

UI	MeSH Term	Description	Entries
D003577	Cytochrome P-450 Enzyme System	A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.	Cytochrome P-450,Cytochrome P-450 Enzyme,Cytochrome P-450-Dependent Monooxygenase,P-450 Enzyme,P450 Enzyme,CYP450 Family,CYP450 Superfamily,Cytochrome P-450 Enzymes,Cytochrome P-450 Families,Cytochrome P-450 Monooxygenase,Cytochrome P-450 Oxygenase,Cytochrome P-450 Superfamily,Cytochrome P450,Cytochrome P450 Superfamily,Cytochrome p450 Families,P-450 Enzymes,P450 Enzymes,Cytochrome P 450,Cytochrome P 450 Dependent Monooxygenase,Cytochrome P 450 Enzyme,Cytochrome P 450 Enzyme System,Cytochrome P 450 Enzymes,Cytochrome P 450 Families,Cytochrome P 450 Monooxygenase,Cytochrome P 450 Oxygenase,Cytochrome P 450 Superfamily,Enzyme, Cytochrome P-450,Enzyme, P-450,Enzyme, P450,Enzymes, Cytochrome P-450,Enzymes, P-450,Enzymes, P450,Monooxygenase, Cytochrome P-450,Monooxygenase, Cytochrome P-450-Dependent,P 450 Enzyme,P 450 Enzymes,P-450 Enzyme, Cytochrome,P-450 Enzymes, Cytochrome,Superfamily, CYP450,Superfamily, Cytochrome P-450,Superfamily, Cytochrome P450
D003866	Depressive Disorder	An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.	Depression, Endogenous,Depression, Neurotic,Depression, Unipolar,Depressive Syndrome,Melancholia,Neurosis, Depressive,Unipolar Depression,Depressions, Endogenous,Depressions, Neurotic,Depressions, Unipolar,Depressive Disorders,Depressive Neuroses,Depressive Neurosis,Depressive Syndromes,Disorder, Depressive,Disorders, Depressive,Endogenous Depression,Endogenous Depressions,Melancholias,Neuroses, Depressive,Neurotic Depression,Neurotic Depressions,Syndrome, Depressive,Syndromes, Depressive,Unipolar Depressions
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001711	Biotransformation	The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
D018687	Antidepressive Agents, Second-Generation	A structurally and mechanistically diverse group of drugs that are not tricyclics or monoamine oxidase inhibitors. The most clinically important appear to act selectively on serotonergic systems, especially by inhibiting serotonin reuptake.	Antidepressants, Atypical,Atypical Antidepressants,Second-Generation Antidepressive Agents,Antidepressive Drugs, Second-Generation,Agents, Second-Generation Antidepressive,Antidepressive Agents, Second Generation,Antidepressive Drugs, Second Generation,Drugs, Second-Generation Antidepressive,Second Generation Antidepressive Agents,Second-Generation Antidepressive Drugs