The in vitro metabolism of desglymidodrine, an active metabolite of prodrug midodrine by human liver microsomes

European Journal of Drug Metabolism and Pharmacokinetics

Volumn 29, Issue 3, 2004, Pages 179-186

  Akimoto, Masayuki ^a,b   Iida, Izumi ^a   Itoga, Hiroki ^a   Miyata, Atsunori ^a   Kawahara, Shizuko ^a   Kohno, Yoshiro ^a  

^a TAISHO PHARMACEUTICAL CO LTD   (Japan)

^b JOSAI INTERNATIONAL UNIVERSITY   (Japan)

Author keywords

5' O demethylation; CYP1A2; CYP2D6; Desglymidodrine (DMAE); Human liver microsomes; Midodrine hydrochloride

Indexed keywords

ANTIBODY; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2D6; CYTOCHROME P450 INHIBITOR; CYTOCHROME P450 ISOENZYME; DESGLYMIDODRINE; DRUG METABOLITE; FURAFYLLINE; MIDODRINE; O DEMETHYLASE; PRODRUG; QUINIDINE; RECOMBINANT ENZYME; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CATALYSIS; CONTROLLED STUDY; DEMETHYLATION; DRUG METABOLISM; DRUG OXIDATION; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IN VITRO STUDY; LIVER MICROSOME; NONHUMAN;

EID: 7444234331     PISSN: 03787966     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF03190595     Document Type: Article

References (18)

1. Wright RA, Kaufmann HC, Perera R, Opfer-Gehrking TL, McElligott MA, Sheng KN, and Low PA (1998): A double-blind, dose-response study of midodrine in neurogenic orthostatic hypotension. Neurology, 51, 120-124.
2. Kolossa N, Shutzenberger WG, Wiener H and Krivnek P (1979): Plasma levels of the prodrug midodrine and its active metabolite in comparison with the alpha-mimetic action in dogs. Arch. Int. Pharmacodyn., 96, 120-124.
3. Grobecker Von H, Kees F, Linden M, Schrader E and Welte S (1987): Untersuchungen zur Bioverfugbarkeit von Midodrin und ÉΩ-2,5- Dimethoxyphenyl-Éά-aminoethanol-hydrochlorid. Arzneim.-Forsch./Drug Res., 37, 447-450.
4. Tsutsui S, Suwa T, Masuda N, Minagawa T, Sano M, Tamaya R and Tsuchida K (1987): Midodrine-no-Tainaidotai. Kiso-to-Rinsho, 21, 549-561.
5. Posch W and Lindner W (1989): Quantification of Midodrine and its Active Metabolite in Plasma using a High Performance Liquid Chromatography Column Switching Technique. Biomed., Chromatogr., 3, 153-156.
6. Newton DJ, Wang RW and Lu AYH (1995): Cytochrome P450 inhibitors. Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab. Dispos., 23, 154-158.
7. Rodrigues AD (1999): Integrated cytochrome P-450 reaction phenotyping. Attempting to bridge the gap between cDNA-expressed cytochromes p450 and native human liver microsomes. Biochem. Pharmaacol., 57, 465-461.
8. Rodrigues AD, Roben EF, Mulford DJ, Yao Y and Ouellet D (1997): Oxidation metabolism of clarithromycin in the presence of human liver microsomes. Major role for the cytochrome P4503A (CYP3A) subfamily. Drug Metab. Dispos., 25, 623-630.
9. Suzuki A, Iida I, Tanaka F, Akimoto M, Fukushima K, Tani M, Ishizaki T and Chiba K (1999): Identification of human cytochrome P-450 isoforms involved in metabolism of R(+)- and S(-)-gallopamil: Utility of in vitro disappearance rate. Drug Metab. Dispos., 27, 1254-1259.
10. Bourie M, Meunier V, Berger Y and Fabre G (1996): Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes. J. Pharmacol. Exp. Ther., 277, 321-332.
11. Yoshimoto K, Echizen H, Chiba K, Tani M and Ishizaki T (1995): Identification of human CYP isoforms involved in the metabolism of propranolol enantionmers_N-desisopropylation is mediated mainly by CYP1A2. Br. J. Clin. Pharmacol., 39, 421-431.
12. Nakajima M, Kobayashi K, Shimada N, Tokudome S and Yamamoto T and Kuroiwa K (1998): Involvement of CYP1A2 in mexiletine metabolism. Br. J. Clin. Pharmacol., 46, 55-62.
13. Yamazaki H, Guo Z, Persmark M, Mimura M, Inoue K, Guengerich FP and Shimada T (1994): Bufuralol hydroxylation by cytochrome P450 2D6 and 1A2 enzymes in human liver microsomes., Mol. Pharmacol., 46, 568-577.
14. Rowland K, Ellis WS, Lennard MS and Tucker GT (1996) Variable contribution of CYP2D6 to the N-Dealkylation of S-(-)-propranolol by human liver microsomes. Br. J. Clin. Pharmacol., 42, 390-393.
15. Shimada T, Yamazaki H, Mimura M, Inui Y, Guengerich FP (1994) Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: Studies with liver microsomes of 30 Japanese and 30 Caucasians. J. Pharmacol. Exp. Ther., 270, 414-423.
16. Crewe HK, Ellis SW, Lennard MS and Tucker GT (1996): Variable contribution of cytochromes P450 2D6, 2C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes. Biochem. Pharmacol., 53, 171-178.
17. Boocock DJ, Brown K, Gibbs AH, Sanchez E, Turteltaub KW and White INH (2002) Identification of human CYP forms involved in the activation of tamoxifen and irreversiblebinding to DNA. Carcinogenesis, 23, 1897-1901.
18. Yoshii K, Kobayashi K, Tsumuji M, Tani M, Shimada N and Chiba K (2000) Identification of human cytochrome P450 isoforms involved in the 7-hydroxylation of chlorpromazine by human liver microsomes. Life Sci., 67, 175-184.