title: [The role of changes in the functional activity and the amount of p-glycoprotein in drug pharmacokinetics].
abstract: Data on the structure of P-glycoprotein, the mechanisms of interaction with drugs, the general properties of substrates, the role in the distribution of drugs, and the modulation of their interactions are summarized. Being an ATP-dependent transport agent in the reverse yield, P-glycoprotein participates in the intestinal secretion, limitation of the permeability of histohematic barriers, and the renal and bile excretion of exogenous substrates, thus protecting the organism against xenobiotics. The interactions of drugs on the level of P-glycoprotein either leads to a decrease in these effects, when this transporter is activated by one of the drugs, or causes undesired reactions if P-glycoprotein is inhibited. Poly- or mononucleotide polymorphism of MDRI gene encoding P-glycoprotein can lead to a change in the pharmacokinetics of related substrates. Pharmacotherapy must take into account both the substrate specificity of drugs with respect to P-glycoprotein and the individual features of patients, in particular, race and sex (allele homozygotes versus heterozygotes).
authors.forename: G V
authors.initials: GV
authors.lastname: Ramenskaia
authors.forename: S L
authors.initials: SL
authors.lastname: Faĭnshteĭn
authors.forename: D A
authors.initials: DA
authors.lastname: Sychev
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D000818:Animals; D006224:Cricetinae; D006801:Humans; D051379:Mice; D010599:Pharmacokinetics; D051381:Rats
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1