[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].
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.
Belolipetskaia
V G
VG
Rumiantsev
D S
DS
Piotrovskiĭ
V K
VK
Metelitsa
V I
VI
Duda
S G
SG
Ostrovskaia
T P
TP
Kokurina
E V
EV
Martseva
S Iu
SIu
Bochkareva
E V
EV
Filatova
N P
NP
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
D000959:Antihypertensive Agents; C001422:4-hydroxypropranolol; C022056:propranolol glucuronide; D011433:Propranolol
Farmakokinetika propranolola i ego kon''iugirovannykh metabolitov u bol'nykh khronicheskoĭ ishemicheskoĭ bolezn'iu serdtsa i arterial'noĭ gipertenzieĭ pri odnokratnom i kursovom prieme.