[Pharmacokinetic behaviour of gliquidone (AR-DF 26), a new sulfonyl urea. Summary of the studies so far (author's transl)].
Pharmacokinetic studies of the new antidiabetic agent gliquidone, AR-DF 26, 1-cyclohexyl-3-((p-[2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2 (1H)-isoquinolyl)-ethyl]-phenyl)-sulfonyl)-urea (Glurenorm) in healthy volunteers and patients with several diseases related to diabetes are reported. Plasma levels and excreta were monitored using the 14C-labelled compound and/or a specific radioimmunoassay. Following oral administration of a 30 mg tablet a maximal plasma level of approximately 600 ng/ml was attained after 2 to 3 h. The compound was eliminated mainly with the bile. Urinary excretion amounted to about 5% only. Comparison of diabetic patients with or without concomitant renal insufficiency did not reveal significant differences with respect to the pharmacokinetic behaviour of the drug. This holds true also for administration following a multiple dosage regimen where even three doses of 60 mg each a day, did not result in elevated blood levels in either group. AR-DF 16 is metabolized mainly to four products, which were identified besides unchanged drug in bile, stool and urine. All excreta showed quite a similar pattern of distribution. In plasma, however, unchanged drug accounted for at least 80% of total radioactivity up to 8 h besides some biotransformed products, mainly AR-DF 33.
D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000032:analysis; D002250:Carbon Radioisotopes; D003920:Diabetes Mellitus / Q000188:drug therapy* / Q000378:metabolism; D004341:Drug Evaluation; D005243:Feces / Q000032:analysis; D006801:Humans; D007004:Hypoglycemic Agents; D007275:Injections, Intravenous; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D007413:Intestinal Mucosa / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D007674:Kidney Diseases / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D009206:Myocardium / Q000378:metabolism; D011863:Radioimmunoassay; D051381:Rats; D013154:Spleen / Q000378:metabolism; D013453:Sulfonylurea Compounds / Q000032:analysis / Q000378:metabolism / Q000494:pharmacology*
D002250:Carbon Radioisotopes; D007004:Hypoglycemic Agents; D007328:Insulin; D013453:Sulfonylurea Compounds
Pharmakokinetisches Verhalten von Gliquidone (AR-DF 26), einem neuen Sulfonylharnstoff (Zusammenfassung der bisherigen Untersuchungen)