The absorption and excretion of the peripheral vasodilator 14C-mecinarone, (14C-6809 MD) in rat, dog and man. 1980

D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly

Oral doses of the peripheral vasodilator mecinarone (6809 MD), administered as the 14C-compound, were well absorbed from the gastrointestinal tract of rats, dogs and humans. Much of the dose was excreted in 24 by rats and dogs, but more slowly by humans. In 5 days, rats, dogs and humans excreted in the urine and faeces respectively means of 3.3 and 95.9%, 13.2 and 80.3%, and 22.0 and 60.8%. The proportions of radioactivity excreted in urine and faeces after intravenous doses were similar to those after oral doses, means of 3.1 and 85.0% respectively by rats and 16.8 and 78.3% by dogs. Radioactivity present in the faeces was probably mainly excreted in bile; rats (n = 2) excreted a mean of 52.3, 19.8 and 3.9% in bile, faeces and urine after oral doses. Plasma concentrations of radioactivity after oral doses reached a maximum at 1 h in rats (mean 126 ng equiv/ml), at 1 to 2 h in dogs (mean 784 ng equiv/ml) and at 1.5 to 2 h in humans (mean 547 ng equiv/ml. Only a small proportion of this radioactivity (10-30%) represented unchanged drug. When "normalised" for dose/bodyweight differences, those levels were in the ratio 1 : 7 : 32 (rat less than dog less than man). Areas under plasma radioactivity concentration-time curves after oral doses to rats and dogs were about 25% and 53% respectively of those after corresponding intravenous doses. Only about 20% of the radioactivity in the plasma of dogs at 2 min after an intravenous dose represented unchanged drug. These data suggest that 6890 MD was probably rapidly biotransformed in rat, dog and man.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D002250 Carbon Radioisotopes Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes. Radioisotopes, Carbon
D002599 Chalcone An aromatic KETONE that forms the core molecule of CHALCONES. Benzalacetophenone,Benzylideneacetophenone,1,3-Diphenyl-2-Propen-1-One,Chalkone,1,3 Diphenyl 2 Propen 1 One
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
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

Related Publications

D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
January 1977, Arzneimittel-Forschung,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
January 1983, European journal of drug metabolism and pharmacokinetics,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
January 1978, Drug metabolism and disposition: the biological fate of chemicals,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
January 1992, European journal of drug metabolism and pharmacokinetics,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
October 1974, Acta pharmacologica et toxicologica,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
June 1977, Archives internationales de pharmacodynamie et de therapie,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
November 1973, The Journal of pharmacology and experimental therapeutics,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
January 1982, Arzneimittel-Forschung,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
November 1971, The Biochemical journal,
D R Hawkins, and K T Weston, and L F Chasseaud, and A Darragh, and A O'Kelly
June 1965, British journal of pharmacology and chemotherapy,
Copied contents to your clipboard!