Pharmacokinetics of prethcamide following rapid intravenous injection and oral administration in rabbits. 1985

P Bryła, and T Szumiło

A simple gas chromatographic method for the quantitative determination of ethyl butamide and propyl butamide, the active constituents of the analeptic drug "Prethcamide", in whole blood and tissues has been developed. The method was used to study the disposition of the compounds after iv and po administration to rabbits. The course of changes of ethyl butamide and propyl butamide concentration following rapid intravenous injection and oral administration was described by the two-compartment and one-compartment open models, respectively. The mean half-life (t1/2 beta, min), the body clearance (Clb, 1/min), the mean absorption rate constant (ka, min1-) and tmax (min) values were, respectively: 43.07 +/- 10.54, 0.05 +/- 0.0125, 0.033 +/- 0.0073 and 30.0 +/- 5.0 for ethyl butamide and 30.0 +/- 4.13, 0.0962 +/- 0.0269, 0.0512 +/- 0.0328 and 30.0 +/- 5.0 for propyl butamide. The low bioavailability (F) of the compounds, in the range 24-32%, may be attributed to low absorption of the drugs from the gastro-intestinal tract, or the first-pass effect, or both. The drugs accumulate predominantly in the liver. The faster metabolism and elimination of propyl butamide is postulated.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D003437 Crotonates Derivatives of BUTYRIC ACID that include a double bond between carbon 2 and 3 of the aliphatic structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobutryrate structure. 2-Butenoic Acids,Crotonic Acids,2 Butenoic Acids,Acids, 2-Butenoic,Acids, Crotonic
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000613 Aminobutyrates Derivatives of BUTYRIC ACID that contain one or more amino groups attached to the aliphatic structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobutryrate structure. Aminobutyric Acids,Aminobutyric Acid,Acid, Aminobutyric,Acids, Aminobutyric
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
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.

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