Page last updated: 2024-09-02

1-hydroxymethylmidazolam and ketoconazole

1-hydroxymethylmidazolam has been researched along with ketoconazole in 9 studies

Compound Research Comparison

Studies
(1-hydroxymethylmidazolam)
Trials
(1-hydroxymethylmidazolam)
Recent Studies (post-2010)
(1-hydroxymethylmidazolam)
Studies
(ketoconazole)
Trials
(ketoconazole)
Recent Studies (post-2010) (ketoconazole)
16346496,2027061,269

Protein Interaction Comparison

ProteinTaxonomy1-hydroxymethylmidazolam (IC50)ketoconazole (IC50)
Solute carrier family 22 member 1 Homo sapiens (human)2.6
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrialHomo sapiens (human)0.34
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrialMus musculus (house mouse)0.36
Bile salt export pumpHomo sapiens (human)3.44
Steroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)1.5811
ATP-dependent translocase ABCB1Mus musculus (house mouse)6.7
ATP-dependent translocase ABCB1Homo sapiens (human)4.6771
Cytochrome P450 3A4Homo sapiens (human)0.1969
Steroid 21-hydroxylaseHomo sapiens (human)6.655
Cytochrome P450 2C8Homo sapiens (human)0.06
AromataseHomo sapiens (human)1.4111
Steroid 17-alpha-hydroxylase/17,20 lyase Rattus norvegicus (Norway rat)2.0802
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)5.425
Cholesterol side-chain cleavage enzyme, mitochondrial Rattus norvegicus (Norway rat)3.32
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)1.067
Cytochrome P450 2A2Rattus norvegicus (Norway rat)0.456
Cytochrome P450 11B1, mitochondrial Bos taurus (cattle)0.38
Cytochrome P450 11B1, mitochondrialHomo sapiens (human)0.162
Translocator proteinRattus norvegicus (Norway rat)3.76
Cytochrome P450 7A1 Rattus norvegicus (Norway rat)1.2975
Cytochrome P450 11B2, mitochondrialHomo sapiens (human)0.5179
ATP-dependent translocase ABCB1Mus musculus (house mouse)3.8
Thromboxane-A synthase Homo sapiens (human)2.165
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)2
Sodium-dependent serotonin transporterHomo sapiens (human)0.531
Type-1 angiotensin II receptorOryctolagus cuniculus (rabbit)0.0078
Cytochrome P450 4F2Homo sapiens (human)1.6
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)0.4144
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)1.9036
Lanosterol 14-alpha demethylaseHomo sapiens (human)0.19
Cytochrome P450 7A1Mus musculus (house mouse)1.2975
Lanosterol 14-alpha demethylase Rattus norvegicus (Norway rat)0.083

Research

Studies (9)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's2 (22.22)18.2507
2000's4 (44.44)29.6817
2010's3 (33.33)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Ring, BJ; Wrighton, SA1
Bayliss, MK; Eddershaw, PJ; Herriott, D; Manchee, GR; Park, GR; Ranshaw, LE; Tarbit, MH1
Akiyama, TE; Cheung, C; Elizondo, G; Feigenbaum, L; Gonzalez, FJ; Granvil, CP; Krausz, KW; Yu, AM1
Aubert, AC; Baumann, P; Bleiber, G; Buclin, T; Cucchia, G; Eap, CB; Golay, KP; Hustert, E; Kerb, R; Telenti, A; Zullino, D1
Cao, L; Li, G; Qiu, J; Ren, XH; Si, LQ; Yao, J1
Foti, RS; Pearson, JT; Rock, DA1
Li, WL; Su, MW; Xin, HW1
Burhenne, J; Fuchs, I; Haefeli, WE; Hafner-Blumenstiel, V; Markert, C; Mikus, G; Weiss, J1
He, F; Huang, S; Liu, M; Xia, C; Xiong, Y; Zeng, C; Zhang, H; Zhang, W1

Trials

2 trial(s) available for 1-hydroxymethylmidazolam and ketoconazole

ArticleYear
Oral administration of a low dose of midazolam (75 microg) as an in vivo probe for CYP3A activity.
    European journal of clinical pharmacology, 2004, Volume: 60, Issue:4

    Topics: Adult; Aryl Hydrocarbon Hydroxylases; Cross-Over Studies; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Enzyme Induction; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Oxidoreductases, N-Demethylating

2004
Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity.
    European journal of clinical pharmacology, 2013, Volume: 69, Issue:3

    Topics: Adult; Area Under Curve; Biotransformation; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Administration Schedule; Drug Interactions; Enzyme Induction; Enzyme Inhibitors; Germany; Humans; Hydroxylation; Hypericum; Ketoconazole; Male; Metabolic Clearance Rate; Midazolam; Middle Aged; Plant Extracts; Plants, Medicinal; Pregnane X Receptor; Receptors, Steroid; Substrate Specificity; Transcription, Genetic; Young Adult

2013

Other Studies

7 other study(ies) available for 1-hydroxymethylmidazolam and ketoconazole

ArticleYear
Inhibition of human CYP3A catalyzed 1'-hydroxy midazolam formation by ketoconazole, nifedipine, erythromycin, cimetidine, and nizatidine.
    Pharmaceutical research, 1994, Volume: 11, Issue:6

    Topics: Chromatography, High Pressure Liquid; Cimetidine; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Erythromycin; Humans; In Vitro Techniques; Ketoconazole; Microsomes, Liver; Midazolam; Nifedipine; Nizatidine

1994
The aliphatic oxidation of salmeterol to alpha-hydroxysalmeterol in human liver microsomes is catalyzed by CYP3A.
    Drug metabolism and disposition: the biological fate of chemicals, 1996, Volume: 24, Issue:5

    Topics: Adrenergic beta-Agonists; Albuterol; Biomarkers; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Disulfiram; Humans; Isoenzymes; Ketoconazole; Microsomes, Liver; Midazolam; Molecular Structure; Oxidation-Reduction; Quinidine; Recombinant Proteins; Salmeterol Xinafoate; Sulfaphenazole; Theophylline

1996
Expression of the human CYP3A4 gene in the small intestine of transgenic mice: in vitro metabolism and pharmacokinetics of midazolam.
    Drug metabolism and disposition: the biological fate of chemicals, 2003, Volume: 31, Issue:5

    Topics: Administration, Oral; Animals; Area Under Curve; Biological Availability; Blotting, Southern; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dexamethasone; Drug Interactions; Enzyme Inhibitors; Half-Life; Humans; In Vitro Techniques; Intestine, Small; Ketoconazole; Male; Mice; Mice, Transgenic; Microsomes; Midazolam; Polymerase Chain Reaction; Rifampin; Time Factors

2003
[Effect of polyoxyl ether analogous surfactants on the activity of cytochromes P450 3A in rats in vivo].
    Yao xue xue bao = Acta pharmaceutica Sinica, 2008, Volume: 43, Issue:5

    Topics: Animals; Area Under Curve; Biological Availability; Biotransformation; Cytochrome P-450 CYP3A; Ketoconazole; Male; Midazolam; Octoxynol; Polyethylene Glycols; Random Allocation; Rats; Rats, Sprague-Dawley; Surface-Active Agents

2008
The combination of chemical and antibody inhibitors for superior P450 3A inhibition in reaction phenotyping studies.
    Drug metabolism and disposition: the biological fate of chemicals, 2008, Volume: 36, Issue:12

    Topics: Antibodies, Monoclonal; Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Inhibitors; Humans; Hydroxytestosterones; Ketoconazole; Microsomes, Liver; Midazolam; Protein Isoforms; Testosterone

2008
Inhibitory effects of continuous ingestion of Schisandrin A on CYP3A in the rat.
    Basic & clinical pharmacology & toxicology, 2012, Volume: 110, Issue:2

    Topics: Administration, Oral; Animals; Area Under Curve; Chromatography, High Pressure Liquid; Cyclooctanes; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Ketoconazole; Lignans; Male; Microsomes, Liver; Midazolam; Polycyclic Compounds; Rats; Rats, Sprague-Dawley

2012
Mechanism of Action of Panaxytriol on Midazolam 1'-Hydroxylation and 4-Hydroxylation Mediated by CYP3A in Liver Microsomes and Rat Primary Hepatocytes.
    Biological & pharmaceutical bulletin, 2015, Volume: 38, Issue:10

    Topics: Animals; Cells, Cultured; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dexamethasone; Enediynes; Fatty Alcohols; Hepatocytes; Humans; Hydroxylation; Ketoconazole; Microsomes, Liver; Midazolam; Rats; RNA, Messenger

2015
chemdatabank.com