Absorption kinetics of oral and rectal flecainide in healthy subjects. 1990

L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
Department of Clinical Pharmacy, St. Antonius Hospital, Nieuwegein, The Netherlands.

The absorption kinetics of different pharmaceutical formulations of orally and rectally administered flecainide have been assessed in a cross-over study in 7 healthy volunteers. The subjects received single doses of flecainide after a washout period of at least one week. A tablet, an oral solution, a rectal solution and a 10 min i.v. infusion during 10 min each containing 100 mg flecainide were administered to the subjects in a randomized order. The mean absolute bioavailability was 98%, 78% and 81% for the rectal and oral solutions and the tablet. The lag time after administration of the oral solution was 0.33 h and it was 0.86 h after the tablet and 0.18 h after the rectal solution. The mean time to the peak serum concentration (tmax) after the rectal solution (0.67 h) was shorter than after either the tablet (4 h) or oral solution (1 h). The maximum serum concentration (Cmax) was 0.29 mg.l-1 after the rectal solution, 0.14 mg.l-1 after the tablet and 0.17 mg.l-1 after the oral solution. All the volunteers showed significantly higher serum flecainide concentrations during the first 20 min of the absorption phase after rectal administration of 100 mg flecainide as a solution compared to its oral administration. CONCLUSIONS based on the absolute bioavailability, Cmax, tmax, and lag times, rectal administration of flecainide solution gave a better absorption profile than after oral tablet or solution.

UI MeSH Term Description Entries
D008297 Male Males
D005260 Female Females
D005424 Flecainide A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS. Flecainide Acetate,Apocard,Flecadura,Flecainid-Isis,Flecainide Monoacetate,Flecainide Monoacetate, (+-)-Isomer,Flecainide Monoacetate, (R)-Isomer,Flecainide Monoacetate, (S)-Isomer,Flecainide, (R)-Isomer,Flecainide, (S)-Isomer,Flecainide, 5-HO-N-(6-oxo)-Derivative,Flecainide, 5-HO-N-(6-oxo)-Derivative, (+-)-Isomer,Flecatab,Flécaïne,R818,Tambocor,Flecainid Isis
D005502 Food Substances taken in by the body to provide nourishment. Foods
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
D000285 Administration, Rectal The insertion of drugs into the rectum, usually for confused or incompetent patients, like children, infants, and the very old or comatose. Anal Drug Administration,Drug Administration, Rectal,Instillation, Rectal,Rectal Drug Administration,Drug Administration, Anal,Rectal Administration,Administration, Anal Drug,Administration, Rectal Drug,Administrations, Anal Drug,Administrations, Rectal,Administrations, Rectal Drug,Anal Drug Administrations,Drug Administrations, Anal,Drug Administrations, Rectal,Instillations, Rectal,Rectal Administrations,Rectal Drug Administrations,Rectal Instillation,Rectal Instillations
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities

Related Publications

L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
January 1988, European journal of clinical pharmacology,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
August 2004, British journal of clinical pharmacology,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
January 1985, Clinical pharmacology and therapeutics,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
January 1989, European journal of clinical pharmacology,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
June 1997, Journal of clinical pharmacy and therapeutics,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
April 1987, Journal of cardiovascular pharmacology,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
May 1999, Clinical therapeutics,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
February 1975, Computers in biology and medicine,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
May 1985, Clinical pharmacology and therapeutics,
L Lie-A-Huen, and J H Proost, and J H Kingma, and D K Meijer
October 1997, World journal of surgery,
Copied contents to your clipboard!