Desacetyl-diltiazem displays severalfold higher affinity to CYP2D6 compared with CYP3A4

Drug Metabolism and Disposition

Volumn 30, Issue 1, 2002, Pages 1-3

  Molden, Espen ^a   Åsberg, Anders ^a   Christensen, Hege ^a  

^a UNIVERSITY OF OSLO   (Norway)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; DEACETYLDILTIAZEM; ERYTHROMYCIN; PAROXETINE;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DEMETHYLATION; DRUG METABOLISM; DRUG STRUCTURE; GENETIC TRANSFECTION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; LIVER CELL; MICHAELIS CONSTANT; PRIORITY JOURNAL; ULTRAVIOLET SPECTROSCOPY;

CALCIUM CHANNEL BLOCKERS; CELLS, CULTURED; CYTOCHROME P-450 CYP2D6; CYTOCHROME P-450 ENZYME SYSTEM; DILTIAZEM; HEPATOCYTES; HUMANS; MIXED FUNCTION OXYGENASES;

EID: 0036135770     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.30.1.1     Document Type: Article

References (17)

1. Diltiazem in hypertensive patients with type-II diabetes-melhtus
2. Pharmacokinetic interactions between microemulsion formulated cyclosporine A and diltiazem in renal transplant recipients
3. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
4. A simple and sensitive high-performance liquid chromatography assay of diltiazem and main metabolites in renal transplanted patients
5. Randomized trial of effects of calcium antagonists compared with diuretics and beta-blockers on cardiovascular morbidity and mortality in hypertension: The Nordic Diltiazem (NORDIL) study
6. Diltiazem inhibition of cytochrome P-450 3A activity is due to metabolite intermediate complex formation
7. Inhibition of platelet aggregation by diltiazem. Comparison with verapamil and nifedipine and inhibitory potencies of diltiazem metabolites
8. Pharmacokinetic and pharmacodynamic interactions between diltiazem and quinidine
9. 2+ antagonistic activity of diltiazem metabolites
10. Aflatoxin B1-induced DNA adduct formation and p53 mutations in CYP450-expressing human liver cell lines
11. CYP2D6 is involved in O-demethylation of diltiazem - An in vitro study with transfected human liver
12. Highly efficient establishment of immortalized cells from adult liver
13. Identification of the rabbit and human cytochromes P-450IIIA as the major enzymes involved in the N-demethylation of diltiazem
14. Calcium channel receptor binding studies for diltiazem and its major metabolites: Functional correlation to inhibition of portal vein myogenic activity
15. Interindividual variations in human liver cytochrome-P-450 enzymes involved in the oxidation of drags, carcinogens and toxic-chemicals - Studies with liver-microsomes of 30 Japanese and 30 Caucasians
16. Role of CYP3A4 in human hepatic diltiazem N-demethylation: Inhibition of CYP3A4 activity by oxidized diltiazem metabolites
17. Cardiovascular effects of the metabolites of diltiazem in dogs