Biomaterial Database

Pharmacokinetics of rectal diclofenac and its hydroxy metabolites in man. 1990

D Landsdorp, and T B Vree, and T J Janssen, and P J Guelen

Department of Clinical Pharmacy, Sint Radboud University Hospital, Nijmegen, The Netherlands.

Diclofenac 100 mg suppository is well absorbed from the gastrointestinal tract of six human volunteers. Plasma concentrations of 4'-hydroxydiclofenac and diclofenac could be measured; the concentrations of the three other metabolites were below the detection limit of the HPLC analysis. The apparent half-lives of diclofenac and 4'-OH-diclofenac are, respectively 1.3 +/- 0.3 h and 4.3 +/- 1.0 h. When the t 1/2 values are derived from the renal excretion rate-time profiles, they are as follows: diclofenac 1.8 +/- 0.9 h, 3'-OH-, and 5-OH-diclofenac 2.3 +/- 1.0 h and 2.5 +/- 0.4 h, respectively, while those of 4'-OH- and 4',5-diOH-diclofenac are, respectively 3.6 +/- 0.5 h and 3.1 +/- 1.3 h. Diclofenac is excreted for 13.6 +/- 6.5%, its renal clearance (Clr) = 3.23 +/- 1.03 ml/min. The main metabolite excreted in the urine is 4'-OH-diclofenac (27.2 +/- 12% dose; Clr = 6.14 +/- 4.04 ml/min). The total body clearance of the parent drug and the apparent total body clearance of the main metabolite are similar, 28.0 +/- 11.9 l/h and 27.5 +/- 10.9 l/h.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D004008	Diclofenac	A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.	Diclophenac,Dichlofenal,Diclofenac Potassium,Diclofenac Sodium,Diclonate P,Dicrofenac,Feloran,GP-45,840,Novapirina,Orthofen,Orthophen,Ortofen,SR-38,Sodium Diclofenac,Voltaren,Voltarol,Diclofenac, Sodium,GP 45,840,GP45,840,SR 38,SR38
D005260	Female		Females
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
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
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
D013997	Time Factors	Elements of limited time intervals, contributing to particular results or situations.	Time Series,Factor, Time,Time Factor