title: [The pharmacokinetics of propranolol and its conjugated metabolites in patients with chronic ischemic heart disease and arterial hypertension with a one-time and course intake of the drug].
abstract: Pharmacokinetics of propranolol (P), 4-hydroxy-propranolol sulfate (4HOP-Sulf), and glucoronides of pharmacologically active S-enantiomer P (S-PG) and ballast R-enantiomer of P (R-PG) in the blood serum of 21 patients with chronic ischemic heart disease and/or arterial hypertension has been studied at a single and course oral P administration. The values od AUC and T1/2 for potentially active 4HOP-Sulf were significantly higher than those for unchanged P at a single and course administration. The values od AUC and T1/2 for for S-PG were approximately three times higher than those for P-PG after both a single and course administration. Thus the results presented show that potentially active 4HOP-Sulf and S-PG (which undergoes a partial deconjugation in an organism at oral administration) may contribute essentially to the value and duration of the P pharmacological effect.
authors.forename: V G
authors.initials: VG
authors.lastname: Belolipetskaia
authors.forename: D S
authors.initials: DS
authors.lastname: Rumiantsev
authors.forename: V K
authors.initials: VK
authors.lastname: Piotrovskiĭ
authors.forename: V I
authors.initials: VI
authors.lastname: Metelitsa
authors.forename: S G
authors.initials: SG
authors.lastname: Duda
authors.forename: T P
authors.initials: TP
authors.lastname: Ostrovskaia
authors.forename: E V
authors.initials: EV
authors.lastname: Kokurina
authors.forename: S Iu
authors.initials: SIu
authors.lastname: Martseva
authors.forename: E V
authors.initials: EV
authors.lastname: Bochkareva
authors.forename: N P
authors.initials: NP
authors.lastname: Filatova
mesh_terms: D000328:Adult; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D002908:Chronic Disease; D006801:Humans; D006973:Hypertension / Q000097:blood / Q000188:drug therapy*; D008875:Middle Aged; D017202:Myocardial Ischemia / Q000097:blood / Q000188:drug therapy*; D011433:Propranolol / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics*; D013237:Stereoisomerism; D013997:Time Factors
chemical_list: D000959:Antihypertensive Agents; C001422:4-hydroxypropranolol; C022056:propranolol glucuronide; D011433:Propranolol
vernacular_title: Farmakokinetika propranolola i ego kon''iugirovannykh metabolitov u bol'nykh khronicheskoĭ ishemicheskoĭ bolezn'iu serdtsa i arterial'noĭ gipertenzieĭ pri odnokratnom i kursovom prieme.