Detail of "7206-76-0"

Reference

Kinetics of penetration of common antiepileptic drugs into cerebrospinal fluid

Kinetics of penetration of common antiepileptic drugs into cerebrospinal fluid. Loescher, Wolfgang; Frey, Hans Hasso (Sch. Vet. Med., Free Univ. Berlin, Berlin 1000/33, Fed. Rep. Ger.). Epilepsia (N. Y.), 25(3), 346-52 (English) 1984. CODEN: EPILAK. ISSN: 0013-9580. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The rate of entry of common antiepileptic drugs and some active metabolites into cerebrospinal fluid (CSF) was studied in anesthetized dogs. Diazepam [439-14-5], its active metabolites desmethyldiazepam [1088-11-5] and oxazepam [604-75-1], clonazepam [1622-61-3], and ethosuximide [77-67-8] entered the CSF very rapidly with mean half-times to equil. between 3 and 7 min. Valproic acid [99-66-1], phenytoin [57-41-0], phenobarbital [50-06-6], and carbamazepine [298-46-4] when in more slowly, but mean penetration half-times were still only 12-18 min. Primidone [125-33-7], its metabolite phenylethylmalondiamide [7206-76-0], and the active metabolite of carbamazepine, i.e., carbamazepine-10,11-epoxide [36507-30-9], passed into CSF considerably slower, with half-times of 40-50 min. No correlation was found between penetration rates and plasma protein binding, but at equil., the ratio between CSF and total plasma concns. was almost equal to the free fraction of drug in plasma. A significant correlation was found between penetration rate and the benzene-buffer distribution ratio of antiepileptic drugs, which indicates that the lipid-soly., rather than the protein binding or the degree of ionization, plays the major role in detg. the differences in rate of entry of these drugs. Valproic acid differed from other drugs studied because it was almost completely ionized at physiol. pH and its lipid-soly. at this pH was very low. The rapid penetration of valproic acid into CSF may therefore suggest an active transport process.

Economical HPTLC method for the simultaneous determination of antiepileptics in small series

Economical HPTLC method for the simultaneous determination of antiepileptics in small series. Mueller, T.; Steinbach, I.; Kapp, S. (Lab. Dr. Kapp und Dr. Breuer, Mainz D-6500, Fed. Rep. Ger.). Fresenius' Z. Anal. Chem., 318(3-4), 261-3 (German) 1984. CODEN: ZACFAU. ISSN: 0016-1152. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The simultaneous detn. of antiepileptics such as carbamazepine [298-46-4], primidone [125-33-7], phenobarbital [50-06-6], hexobarbital [56-29-1], clonazepam [1622-61-3], sultiam [61-56-3] methoin [50-12-4], mesuximide [77-41-8], phenytoin [57-41-0], ethosuximide [77-67-8] as well as phenylethylmalonamide [7206-76-0] and N-desmethylmesuximide [1497-17-2] in human serum by high-performance thin-layer chromatog. (HPTLC) is described. Serum extn. was performed on an Extrelut column washed with dichloromethane:2-propanol (). Chromatog. was performed on Kieselgel 60 F254 HPTLC plates with a mobile phase of CHCl3-2-propanol-ammonia, 25% (80 + 20 + 1). Complete anal. of a single serum sample can be achieved in approx. 1 h.