ketoconazole has been researched along with midazolam in 129 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 13 (10.08) | 18.2507 |
| 2000's | 56 (43.41) | 29.6817 |
| 2010's | 52 (40.31) | 24.3611 |
| 2020's | 8 (6.20) | 2.80 |
| Authors | Studies |
|---|---|
| Chai, SC; Chen, T; Chenge, J; Girvan, HM; Huber, AD; Munro, AW; Oladimeji, PO; Wang, J; Wright, WC; Wu, J; Yang, L | 1 |
| Dubrovskyi, O; Dye, K; Gutgesell, LM; Huang, F; Li, Y; Ratia, K; Shen, Z; Thatcher, GRJ; Tonetti, DA; Xiong, R; Zhao, H; Zhao, J | 1 |
| Chen, LZ; Huang, X; Liu, MM; Liu, XH; Ma, D; Shi, JB; Shu, HY; Wu, J; Yu, YL | 1 |
| Fukuda, T; Hasegawa, R; Murakami, T; Nagai, J; Takano, M; Yumoto, R | 1 |
| Huang, L; Humphreys, JE; Morgan, JB; Polli, JW; Serabjit-Singh, CS; Webster, LO; Wring, SA | 1 |
| Fischer, H; Huwyler, J; Poli, S; Schwab, D; Tabatabaei, A | 1 |
| Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL | 1 |
| Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A | 1 |
| Choi, SS; Contrera, JF; Hastings, KL; Kruhlak, NL; Sancilio, LF; Weaver, JL; Willard, JM | 1 |
| Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ | 1 |
| Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR | 1 |
| Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ | 1 |
| Artursson, P; Mateus, A; Matsson, P | 1 |
| Aleo, MD; Bonin, PD; Luo, Y; Potter, DM; Swiss, R; Will, Y | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Chen, F; Chen, W; Lan, L; Li, B; Li, J; Liu, Y; Mao, F; Ni, S; Wei, H; Zhu, J | 1 |
| Ring, BJ; Wrighton, SA | 1 |
| Backman, JT; Neuvonen, PJ; Olkkola, KT | 1 |
| Bayliss, MK; Eddershaw, PJ; Herriott, D; Manchee, GR; Park, GR; Ranshaw, LE; Tarbit, MH | 1 |
| Gibbs, MA; Kunze, KL; Shen, DD; Thummel, KE | 1 |
| Iga, T; Kotaki, H; Sawada, Y; Yamamoto, K; Yamano, K | 1 |
| Durol, AL; Greenblatt, DJ; Kotegawa, T; Laurijssens, BE | 1 |
| Higashikawa, F; Kaneda, T; Kato, A; Murakami, T; Takano, M | 1 |
| Backman, JT; Kivistö, KT; Neuvonen, PJ; Taavitsainen, P; Wang, JS; Wen, X | 1 |
| Balian, JD; Flockhart, DA; Yuan, R | 1 |
| Greenblatt, DJ; Tsunoda, SM; Velez, RL; von Moltke, LL | 1 |
| Antonello, S; Brucker, MJ; Carides, A; Gertz, BJ; Gillen, L; McCrea, J; Miller-Stein, C; Osborne, B; Prueksaritanont, T; Waldman, S | 1 |
| Court, MH; Greenblatt, DJ; Kotegawa, T; Perloff, MD; Shader, RI; von Moltke, LL | 1 |
| Greenblatt, DJ; Harmatz, JS; Poku, JW; Shader, RI; von Moltke, LL; Warrington, JS | 1 |
| Baillie, MT; Gibbs, MA; Kunze, KL; Shen, DD; Thummel, KE | 1 |
| Agúndez, JA; Benítez, J; Carrillo, JA; Gallardo, L; García-Gamito, FJ; Gervasini, G; Martínez, C; Ramos, SI | 1 |
| Bigler, L; Follath, F; Ha, HR; Kozlik, P; Stieger, B | 1 |
| Achira, M; Ito, K; Sugiyama, Y; Suzuki, H | 1 |
| Azumano, A; Kokue, E; Kuroha, M; Kuze, Y; Shimoda, M | 1 |
| Kokue, E; Kuroha, M; Kuze, Y; Shimoda, M | 1 |
| Cotreau, MM; Granda, BW; Greenblatt, DJ; Harmatz, JS; Kotegawa, T; Laurijssens, BE; Perloff, MD; Venkatakrishnan, K; Von Moltke, LL; Warrington, JS | 1 |
| Amico, JA; Chaves-Gnecco, D; Frye, RF; Kroboth, PD; Lee, JI; Wilson, JW | 1 |
| Akiyama, TE; Cheung, C; Elizondo, G; Feigenbaum, L; Gonzalez, FJ; Granvil, CP; Krausz, KW; Yu, AM | 1 |
| Greenblatt, DJ; Perloff, MD; Von Moltke, LL | 1 |
| Greenblatt, DJ; Patki, KC; Von Moltke, LL | 1 |
| Charman, WN; Johnson, BM; Porter, CJ | 1 |
| Alfaro, CL; Ereshefsky, L; Lam, YW; Miller, M | 1 |
| Kohno, Y; Suzuki, A; Yamamoto, T | 1 |
| Aubert, AC; Baumann, P; Bleiber, G; Buclin, T; Cucchia, G; Eap, CB; Golay, KP; Hustert, E; Kerb, R; Telenti, A; Zullino, D | 1 |
| Baba, T; Kanazu, T; Koike, M; Okamura, N; Yamaguchi, Y | 3 |
| Honda, K; Inomata, S; Misawa, S; Nagashima, A; Tanaka, E | 1 |
| Baririan, N; Desager, JP; Horsmans, Y; Petit, M | 1 |
| Davis, CL; Hashizume, T; Kalhorn, TF; Nelson, WL; Sakaki, T; Schuetz, EG; Shuhart, MC; Thummel, KE; Watkins, PB; Xu, Y | 1 |
| de Kanter, R; Groothuis, G; Martignoni, M | 1 |
| Chien, JY; Ernest, CS; Gorski, JC; Hall, SD; Lucksiri, A; Wrighton, SA | 1 |
| Fan, L; Goh, BC; Lee, HS; Lee, SC; Ong, AB; Soo, R; Sukri, N; Tham, LS; Wang, L; Yong, WP | 1 |
| Booth-Genthe, C; Carr, B; Fang, Y; Lu, P; Norcross, R; Rodrigues, AD; Rushmore, T; Shou, M | 1 |
| Bertino, JS; Chen, M; Nafziger, AN | 1 |
| Cortright, KA; Craigmill, AL | 1 |
| Kazama, E; Kume, T; Ogasawara, A | 1 |
| Lin, JH | 1 |
| Ehana, R; Iwase, M; Kurata, N; Masamoto, T; Nishimura, Y; Yasuhara, H | 1 |
| Chin, R; Flockhart, DA; Hall, SD; Li, L; Lucksiri, A; Yu, M | 1 |
| Nakamura, K; Okazaki, O; Okudaira, N; Sudo, K; Watanabe, A | 1 |
| Brown, HS; Chadwick, A; Houston, JB | 1 |
| Caporuscio, C; Cornelius, G; Mandlekar, SV; Marathe, PH; Rose, AV; Sleczka, B; Wang, J | 1 |
| Goh, BC; Lee, HS; Lee, SC; Soo, R; Sukri, N; Tham, LS; Wang, LZ; Wong, CI; Yong, WP | 1 |
| Gonzalez, FJ | 1 |
| Boulenc, X; Hachad, H; Levy, RH; Ragueneau-Majlessi, I; Rauch, C | 1 |
| Arabeyre-Fabre, C; Bourrie, M; Fabre, G; Fedeli, O; Guillou, F; Hugla, S; Klieber, S; Maurel, P; Meunier, V; Ngo, R; Rival, M; Sadoun, F | 1 |
| Cao, L; Li, G; Qiu, J; Ren, XH; Si, LQ; Yao, J | 1 |
| Foti, RS; Pearson, JT; Rock, DA | 1 |
| Hall, S; Kim, S; Li, L; Wang, Z; Yu, M | 1 |
| Bergman, AJ; Chiou, R; Cote, J; Didolkar, V; Dru, J; Garg, A; Gottesdiener, K; Jin, B; Krishna, R; Laethem, T; Roadcap, B; Vets, E; Wagner, JA; Wang, RW | 1 |
| Jiao, JJ; Liu, CX; Lou, JS; Zhang, CL; Zhu, XH | 2 |
| Chien, JY; Hall, SD; Kim, S; Li, L; Lucksiri, A; Qin, Z; Quinney, SK; Wang, Z; Yu, M; Zhou, J | 1 |
| Chodakewitz, J; Fitzgerald, M; Friedman, E; Larson, P; Maes, A; Stoch, SA; Wagner, JA; Xu, Y; Yee, K | 1 |
| Krishna, G; Ma, L; Martinho, M; McLeod, J; Moton, A; Savant, I; Seiberling, M | 1 |
| Higashi, R; Matsumoto, I; Miyata, Y; Nakade, S; Nunoya, K; Ogawa, M; Sutoh, F; Yoneda, K | 1 |
| Hao, H; Shang, L; Sun, J; Wang, G; Wang, X; Xia, C; Xie, L; Zhang, R; Zhang, X | 1 |
| Hayashi, Y; Helmi, AR; Khalil, WF; Motoyama, S; Sasaki, K; Shah, SS; Shimoda, M | 1 |
| Hall, SD; Kim, S; Li, L; Qin, Z; Sara, QK; Wang, Z; Zhou, J | 1 |
| Blasco, H; Bouzom, F; Cazade, F; Chenel, M; Perdaems, N; Vinson, C; Whalley, S | 1 |
| Darnell, M; Edebert, I; Ek, M; Ingelman-Sundberg, M; Neve, EP; Sivertsson, L | 1 |
| Hubin, M; KuKanich, B | 1 |
| Brocks, DR; Hamdy, DA | 2 |
| Duan, JZ; Jackson, AJ; Zhao, P | 1 |
| Kagawa, Y; Kato, Y; Kurosawa, S; Misaka, S; Uchida, S; Yamada, S; Yoshida, A | 1 |
| Bergman, AJ; Chodakewitz, J; Fraser, IP; Friedman, EJ; Larson, PJ; Li, CC; Stoch, SA; Wagner, JA; Wang, YH | 1 |
| Court, MH; Duan, SX; Greenblatt, DJ; Harmatz, JS; Parent, SJ; Venkatakrishnan, K; von Moltke, LL; Zhao, Y | 1 |
| Li, WL; Su, MW; Xin, HW | 1 |
| Chang, S; Marathe, PH; Rodrigues, AD; Vuppugalla, R; Zhang, Y | 1 |
| Cameron, MD; Kamenecka, TM; Li, X; Song, X | 1 |
| Annes, WF; Ayan-Oshodi, MA; Brown, T; de la Peña, A; Friedrich, S; Hall, SD; Lowe, SL; Willis, BA; Wise, SD; Zhang, W | 1 |
| Burhenne, J; Fuchs, I; Haefeli, WE; Hafner-Blumenstiel, V; Markert, C; Mikus, G; Weiss, J | 1 |
| Becka, M; Kubitza, D; Mueck, W | 1 |
| Boustani, M; Chiang, C; Flockhart, D; Han, X; Karnik, S; Li, L; Liu, L; Philips, S; Quinney, SK; Rocha, LM; Subhadarshini, A; Wang, Z; Wu, HY | 1 |
| Burhenne, J; Haefeli, WE; Halama, B; Hohmann, N; Mikus, G; Weiss, J | 1 |
| Li, WL; Wu, XC; Xin, HW; Yu, AR | 1 |
| Chien, JY; Hall, SD; Han, B; Mao, J | 1 |
| Chang, SY; Grubb, MF; Isoherranen, N; Peng, CC; Rodrigues, AD; Shirasaka, Y; Thummel, KE | 1 |
| Alley, SC; Chen, R; Cooper, M; Gopal, AK; Goy, A; Grove, LE; Han, TH; Lynch, CM; Matous, JV; O'Connor, OA; Ramchandren, R | 1 |
| Cho, JY; Choi, MH; Jang, IJ; Lim, KS; Shin, KH; Yu, KS | 1 |
| Bartolomé, JM; Blobaum, AL; Bridges, TM; Byers, FW; Conn, PJ; Daniels, JS; Jones, CK; Lavreysen, H; Lindsley, CW; Macdonald, GJ; Mackie, C; Mattmann, ME; Morrison, RD; Niswender, CM; Stauffer, SR; Steckler, T; Turlington, ML | 1 |
| Dutreix, C; Lorenzo, S; Munarini, F; Roesel, J; Wang, Y | 1 |
| Hee, KH; Lee, LS; Yao, Z | 1 |
| Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Larouche, R; Ling, SY; Mayo, PR | 1 |
| Namiki, N; Tanaka, S; Uchida, S | 1 |
| Haefeli, WE; Halama, B; Hohmann, N; Mikus, G; Siller, N | 1 |
| Duchin, KL; Oo, C | 1 |
| Boulton, DW; Goodenough, A; Jemal, M; Kasichayanula, S; LaCreta, F; Lee, M; Luo, WL; Rodrigues, AD; Yang, Z | 1 |
| Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H | 1 |
| Boulenc, X; Donazzolo, Y; Hermabessière, S; Martin, V; Nicolas, O; Ollier, C; Zobouyan, I | 1 |
| Haefeli, WE; König, SK; Mahlke, NS; Mikus, G; Skopp, G; Ziesenitz, VC | 1 |
| Greenblatt, DJ; Harmatz, JS | 1 |
| Badolo, L; Gabel-Jensen, C; Hansen, SH; Janfelt, C; Kongstad, KT; Olsen, LR; Wubshet, SG | 1 |
| He, F; Huang, S; Liu, M; Xia, C; Xiong, Y; Zeng, C; Zhang, H; Zhang, W | 1 |
| Ahn, LY; Cho, JY; Choi, MH; Jang, IJ; Lee, J; Moon, JY; Shin, KH; Yu, KS | 1 |
| Che, J; Li, H; Li, Z; Lu, C; Luo, H; Wang, J; Yang, H; Yue, S; Zhang, T; Zhang, Y; Zhu, M; Zhuang, X | 1 |
| Crewe, HK; Liu, B; Ozdemir, M; Rostami-Hodjegan, A; Rowland Yeo, K; Tucker, G | 1 |
| den Adel, M; Garcia-Hernandez, A; Groenendaal-van de Meent, D; Katashima, M; Kato, K; Kusawake, T; Ohtsu, Y; Takada, A | 1 |
| Chun, DY; Dutreix, C; Einolf, HJ; Gu, H; He, H; Ouatas, T; Rebello, S; Wang, L | 1 |
| Kondo, S; Miyake, M | 1 |
| Arora, S; Christensen, J; Hughes, L; Lu, S; Wang, J; Wang, X; Zhang, ZY | 1 |
| Cho, JY; Jang, IJ; Kim, AH; Kim, B; Lee, J; Lee, S; Yi, S; Yoon, SH; Yu, KS | 1 |
| Dickinson, GL; Guo, Y; Hall, SD; Hilligoss, JK; Lucksiri, A; Vuppalanchi, RK | 1 |
| da Costa César, I; de Araújo, LL; de Castro, WV; de Lima Nascimento, M; de Oliveira, FM; Derendorf, H; do Carmo Vieira, M; do Nascimento, SB; Duarte-Almeida, JM; Siqueira, JM | 1 |
| Krishna, G; Surapaneni, S; Wu, F | 1 |
| Chen, Y; Ding, H; Girish, S; Jin, J; Li, C; Lu, D; Ma, F; Mao, J; Miles, D; Samineni, D; Shi, R; Wright, M | 1 |
| Carreño, FO; Cohen-Wolkowiez, M; Edginton, AN; Gonzalez, D; Salerno, SN | 1 |
7 review(s) available for ketoconazole and midazolam
| Article | Year |
|---|---|
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk | 2016 |
Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, midazolam, and triazolam.
Topics: Alprazolam; Anti-Anxiety Agents; Data Collection; Drug Interactions; Enzyme Induction; Enzyme Inhibitors; Humans; Itraconazole; Ketoconazole; Midazolam; Triazolam | 1999 |
Transporter-mediated drug interactions: clinical implications and in vitro assessment.
Topics: Animals; Area Under Curve; Cytochrome P-450 Enzyme System; Drug Interactions; Humans; Ketoconazole; Membrane Transport Proteins; Midazolam; Pharmaceutical Preparations; Rifampin | 2007 |
Drug-drug interaction prediction: a Bayesian meta-analysis approach.
Topics: Anti-Anxiety Agents; Antifungal Agents; Area Under Curve; Bayes Theorem; Drug Interactions; Forecasting; Humans; Ketoconazole; Midazolam; Models, Statistical; Pharmacokinetics; United States | 2007 |
CYP3A4 and pregnane X receptor humanized mice.
Topics: Animals; Chromosomes, Artificial, Bacterial; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Estrogens; Forecasting; Humans; Ketoconazole; Male; Mice; Mice, Knockout; Mice, Transgenic; Midazolam; Models, Animal; Pregnane X Receptor; Receptors, Steroid; Rifampin; Sex Factors | 2007 |
A Bayesian meta-analysis on published sample mean and variance pharmacokinetic data with application to drug-drug interaction prediction.
Topics: Administration, Oral; Bayes Theorem; Bias; Computer Simulation; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Inhibitors; Female; Humans; Ketoconazole; Male; Markov Chains; Midazolam; Models, Biological; Models, Statistical; Monte Carlo Method; Reproducibility of Results | 2008 |
Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450-3A in drug-drug interaction studies.
Topics: Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Design; Drug Interactions; Humans; Ketoconazole; Midazolam; Ritonavir; United States; United States Food and Drug Administration | 2015 |
29 trial(s) available for ketoconazole and midazolam
| Article | Year |
|---|---|
Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole.
Topics: Adult; Analysis of Variance; Cytochrome P-450 Enzyme Inhibitors; Double-Blind Method; Drug Synergism; Female; Humans; Itraconazole; Ketoconazole; Male; Midazolam; Psychomotor Performance; Reference Values | 1994 |
Concurrent administration of the erythromycin breath test (EBT) and oral midazolam as in vivo probes for CYP3A activity.
Topics: Administration, Oral; Adult; Anti-Bacterial Agents; Aryl Hydrocarbon Hydroxylases; Breath Tests; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Inhibitors; Erythromycin; Humans; Ketoconazole; Male; Midazolam; Oxidoreductases, N-Demethylating; Reproducibility of Results | 1999 |
Application of semisimultaneous midazolam administration for hepatic and intestinal cytochrome P450 3A phenotyping.
Topics: Administration, Oral; Adolescent; Adult; Anti-Anxiety Agents; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Biological Availability; Biomarkers; Cross-Over Studies; Cytochrome P-450 CYP3A; Drug Administration Schedule; Female; Gas Chromatography-Mass Spectrometry; Humans; Infusions, Intravenous; Intestinal Mucosa; Intestines; Ketoconazole; Liver; Male; Midazolam; Middle Aged; Oxidoreductases, N-Demethylating; Phenotype; Reference Values | 2002 |
Pharmacokinetic and pharmacodynamic interactions of oral midazolam with ketoconazole, fluoxetine, fluvoxamine, and nefazodone.
Topics: Administration, Oral; Adult; Analysis of Variance; Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Interactions; Female; Fluoxetine; Fluvoxamine; Humans; Ketoconazole; Male; Midazolam; Piperazines; Triazoles | 2003 |
Oral administration of a low dose of midazolam (75 microg) as an in vivo probe for CYP3A activity.
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 |
Ketoconazole renders poor CYP3A phenotype status with midazolam as probe drug.
Topics: Administration, Oral; Anesthetics, Intravenous; Antifungal Agents; Antineoplastic Agents, Phytogenic; Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Docetaxel; Female; Half-Life; Humans; Infusions, Intravenous; Isoenzymes; Ketoconazole; Male; Metabolic Clearance Rate; Midazolam; Middle Aged; Taxoids | 2006 |
Drug-metabolizing enzyme inhibition by ketoconazole does not reduce interindividual variability of CYP3A activity as measured by oral midazolam.
Topics: Administration, Oral; Adolescent; Adult; Cross-Over Studies; Cytochrome P-450 CYP3A Inhibitors; Enzyme Inhibitors; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged | 2006 |
A phase I study of docetaxel with ketoconazole modulation in patients with advanced cancers.
Topics: Antineoplastic Agents; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Docetaxel; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Humans; Ketoconazole; Male; Maximum Tolerated Dose; Midazolam; Middle Aged; Neoplasm Invasiveness; Neoplasm Metastasis; Neoplasms; Neutropenia; Taxoids | 2008 |
Assessment of the CYP3A-mediated drug interaction potential of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy volunteers.
Topics: Adolescent; Adult; Cholesterol Ester Transfer Proteins; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Hepatocytes; Humans; In Vitro Techniques; Ketoconazole; Microsomes, Liver; Midazolam; Middle Aged; Oxazolidinones; Young Adult | 2009 |
Effect of different durations of ketoconazole dosing on the single-dose pharmacokinetics of midazolam: shortening the paradigm.
Topics: Adult; Biological Availability; Computer Simulation; Cross-Over Studies; Cytochrome P-450 CYP3A Inhibitors; Drug Administration Schedule; Drug Interactions; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Models, Theoretical; Reproducibility of Results; Time Factors | 2009 |
Effects of oral posaconazole on the pharmacokinetic properties of oral and intravenous midazolam: a phase I, randomized, open-label, crossover study in healthy volunteers.
Topics: Adult; Anti-Anxiety Agents; Antifungal Agents; Area Under Curve; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Half-Life; Humans; Injections, Intravenous; Ketoconazole; Male; Midazolam; Middle Aged; Triazoles | 2009 |
The pharmacokinetics of ketoconazole and its effects on the pharmacokinetics of midazolam and fentanyl in dogs.
Topics: Animals; Antifungal Agents; Area Under Curve; Dogs; Dose-Response Relationship, Drug; Drug Interactions; Female; Fentanyl; GABA Modulators; Half-Life; Ketoconazole; Male; Midazolam; Narcotics | 2010 |
Effect of different durations and formulations of diltiazem on the single-dose pharmacokinetics of midazolam: how long do we go?
Topics: Adult; Area Under Curve; Chemistry, Pharmaceutical; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Diltiazem; Drug Interactions; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Sensitivity and Specificity; Young Adult | 2011 |
The effects on metabolic clearance when administering a potent CYP3A autoinducer with the prototypic CYP3A inhibitor, ketoconazole.
Topics: Administration, Oral; Adult; Aged; Alanine; Amyloid Precursor Protein Secretases; Area Under Curve; Azepines; Cells, Cultured; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Enzyme Induction; Enzyme Inhibitors; Female; Half-Life; Hepatocytes; Humans; Hydroxylation; Ketoconazole; Male; Metabolic Clearance Rate; Midazolam; Middle Aged; Models, Biological; Nifedipine; Testosterone; Young Adult | 2012 |
Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity.
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 |
Co-administration of rivaroxaban with drugs that share its elimination pathways: pharmacokinetic effects in healthy subjects.
Topics: Adolescent; Adult; Anticoagulants; ATP Binding Cassette Transporter, Subfamily B, Member 1; Clarithromycin; Cytochrome P-450 CYP2J2; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Inhibitors; Erythromycin; Humans; Ketoconazole; Metabolic Clearance Rate; Midazolam; Middle Aged; Morpholines; Rivaroxaban; Substrate Specificity; Thiophenes; Young Adult | 2013 |
A nanogram dose of the CYP3A probe substrate midazolam to evaluate drug interactions.
Topics: Adolescent; Adult; Alleles; Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Drug Interactions; Female; Genotype; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Sex Characteristics | 2013 |
CYP3A-mediated drug-drug interaction potential and excretion of brentuximab vedotin, an antibody-drug conjugate, in patients with CD30-positive hematologic malignancies.
Topics: Adolescent; Adult; Aged; Antineoplastic Agents; Brentuximab Vedotin; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Feces; Female; Hematologic Neoplasms; Humans; Immunoconjugates; Ketoconazole; Ki-1 Antigen; Male; Midazolam; Middle Aged; Oligopeptides; Rifampin; Young Adult | 2013 |
Evaluation of endogenous metabolic markers of hepatic CYP3A activity using metabolic profiling and midazolam clearance.
Topics: Adult; Biomarkers; Cortisone; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Enzyme Induction; Gas Chromatography-Mass Spectrometry; Humans; Hydrocortisone; Hydroxycholesterols; Ketoconazole; Liver; Male; Metabolomics; Midazolam; Pharmacogenetics; Rifampin; Young Adult | 2013 |
Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers.
Topics: Adult; Antineoplastic Agents; Chromatography, Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Administration Schedule; Drug Interactions; Enzyme Induction; Enzyme Inhibitors; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Rifampin; Staurosporine; Tandem Mass Spectrometry; Young Adult | 2013 |
Simultaneous determination of probe drugs, metabolites, inhibitors and inducer in human plasma by liquid chromatography/tandem mass spectrometry and its application to pharmacokinetic study.
Topics: Calibration; Chromatography, Liquid; Cross-Over Studies; Cytochrome P-450 CYP3A; Freezing; Glucuronosyltransferase; Healthy Volunteers; Humans; Ketoconazole; Midazolam; Particle Size; Pyrrolidinones; Quality Control; Raltegravir Potassium; Reproducibility of Results; Rifampin; Ritonavir; Solid Phase Extraction; Tandem Mass Spectrometry; Xenobiotics | 2014 |
Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin.
Topics: Adolescent; Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1; Calcineurin Inhibitors; Cyclosporine; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Digoxin; Drug Interactions; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Verapamil | 2014 |
Validation of 4β-hydroxycholesterol and evaluation of other endogenous biomarkers for the assessment of CYP3A activity in healthy subjects.
Topics: Adolescent; Adult; Biomarkers; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inducers; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Healthy Volunteers; Humans; Hydroxycholesterols; Injections, Intravenous; Ketoconazole; Limit of Detection; Midazolam; Middle Aged; Rifampin; Saliva; Substrate Specificity; Time Factors; Tissue Distribution; Young Adult | 2014 |
CYP3A4-based drug-drug interaction: CYP3A4 substrates' pharmacokinetic properties and ketoconazole dose regimen effect.
Topics: Adolescent; Adult; Alprazolam; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Drug Interactions; Humans; Ketoconazole; Male; Midazolam; Substrate Specificity; Young Adult | 2016 |
Pharmacokinetic interaction of intravenous fentanyl with ketoconazole.
Topics: Administration, Intravenous; Adult; Analgesics, Opioid; Chromatography, Liquid; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Fentanyl; Healthy Volunteers; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Naloxone; Prospective Studies; Tandem Mass Spectrometry; Young Adult | 2015 |
Urinary 6β-Hydroxycortisol/Cortisol Ratio Most Highly Correlates With Midazolam Clearance Under Hepatic CYP3A Inhibition and Induction in Females: A Pharmacometabolomics Approach.
Topics: Administration, Intravenous; Administration, Oral; Adult; Biomarkers; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Enzyme Induction; Female; Humans; Hydrocortisone; Ketoconazole; Liver; Metabolic Clearance Rate; Metabolomics; Midazolam; Middle Aged; Rifampin; Young Adult | 2016 |
Pharmacokinetic Interactions of Rolapitant With Cytochrome P450 3A Substrates in Healthy Subjects.
Topics: Administration, Oral; Adult; Area Under Curve; Cytochrome P-450 CYP3A; Drug Interactions; Female; Humans; Ketoconazole; Male; Midazolam; Middle Aged; Neurokinin-1 Receptor Antagonists; Rifampin; Spiro Compounds | 2019 |
Quantitative prediction of hepatic CYP3A activity using endogenous markers in healthy subjects after administration of CYP3A inhibitors or inducers.
Topics: Adult; Biomarkers; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Healthy Volunteers; Humans; Itraconazole; Ketoconazole; Male; Midazolam; Rifampin; Young Adult | 2019 |
Quantitative Prediction of CYP3A4- and CYP3A5-Mediated Drug Interactions.
Topics: Area Under Curve; Chromatography, Liquid; Cross-Over Studies; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Drug Interactions; Genotype; Humans; Intestine, Small; Ketoconazole; Liver; Mass Spectrometry; Midazolam; Models, Biological | 2020 |
93 other study(ies) available for ketoconazole and midazolam
| Article | Year |
|---|---|
Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.
Topics: Cell Line, Tumor; Clobetasol; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Enzyme Assays; Heme; High-Throughput Screening Assays; Humans; Molecular Docking Simulation; Molecular Dynamics Simulation; Protein Binding | 2020 |
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
Topics: Animals; Breast Neoplasms; Drug Resistance, Neoplasm; Fulvestrant; Humans; MCF-7 Cells; Mice; Models, Molecular; Piperazines; Protein Domains; Pyridines; Pyridones; Receptors, Estrogen; Tissue Distribution; Transcription Factors; Xenograft Model Antitumor Assays | 2020 |
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
Topics: Administration, Oral; Animals; Arthritis; Cells, Cultured; Dimerization; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Development; Enzyme Inhibitors; Freund's Adjuvant; Humans; Lipopolysaccharides; Male; Mice; Molecular Structure; Nitric Oxide; Nitric Oxide Synthase Type II; Pyrazoles; Pyrimidines; Rats; Rats, Sprague-Dawley; RAW 264.7 Cells; Structure-Activity Relationship | 2021 |
Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells.
Topics: Anti-Bacterial Agents; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; ATP Binding Cassette Transporter, Subfamily B; Biological Transport; Caco-2 Cells; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Erythromycin; GABA Modulators; Humans; Ketoconazole; Midazolam; Oxidoreductases, N-Demethylating; Rhodamine 123; Substrate Specificity; Vasodilator Agents; Verapamil | 1998 |
Rational use of in vitro P-glycoprotein assays in drug discovery.
Topics: Adenosine Triphosphatases; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cells, Cultured; Chromatography, Liquid; Enzyme Inhibitors; Fluoresceins; Fluorescent Dyes; Humans; Mass Spectrometry; Pharmacology; Spodoptera | 2001 |
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
Topics: Adenosine Triphosphatases; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Cells, Cultured; Drug Evaluation, Preclinical; Fluoresceins; Fluorescent Dyes; Humans; Indicators and Reagents; Mice; Models, Molecular; Rhodamines; Species Specificity; Swine | 2003 |
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Topics: Adverse Drug Reaction Reporting Systems; Artificial Intelligence; Computers; Databases, Factual; Drug Prescriptions; Drug-Related Side Effects and Adverse Reactions; Endpoint Determination; Models, Molecular; Quantitative Structure-Activity Relationship; Software; United States; United States Food and Drug Administration | 2004 |
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
Topics: Animals; Chemical and Drug Induced Liver Injury; Cluster Analysis; Databases, Factual; Humans; MEDLINE; Mice; Models, Chemical; Molecular Conformation; Quantitative Structure-Activity Relationship | 2010 |
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
Topics: | 2008 |
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Assay; Biological Transport; Cell Line; Cell Membrane; Chemical and Drug Induced Liver Injury; Cytoplasmic Vesicles; Drug Evaluation, Preclinical; Humans; Liver; Rats; Reproducibility of Results; Spodoptera; Transfection; Xenobiotics | 2010 |
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Topics: Atorvastatin; Biological Transport; Drug Interactions; Estradiol; Estrone; HEK293 Cells; Heptanoic Acids; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; In Vitro Techniques; Least-Squares Analysis; Liver; Liver-Specific Organic Anion Transporter 1; Models, Molecular; Multivariate Analysis; Organic Anion Transporters; Organic Anion Transporters, Sodium-Independent; Protein Isoforms; Pyrroles; Solute Carrier Organic Anion Transporter Family Member 1B3; Structure-Activity Relationship; Transfection | 2012 |
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Chemical and Drug Induced Liver Injury; Cluster Analysis; Drug-Related Side Effects and Adverse Reactions; Humans; Liver; Male; Multidrug Resistance-Associated Proteins; Pharmacokinetics; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Risk Assessment; Risk Factors; Toxicity Tests | 2013 |
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
Topics: Animals; Brain; Dialysis; HEK293 Cells; High-Throughput Screening Assays; Humans; Pharmaceutical Preparations; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization | 2014 |
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Chemical and Drug Induced Liver Injury; Humans; Male; Mitochondria, Liver; Rats; Rats, Sprague-Dawley; Severity of Illness Index | 2014 |
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
Topics: Animals; Drug Design; Enzyme Inhibitors; ERG1 Potassium Channel; HEK293 Cells; Hep G2 Cells; Humans; Inhibitory Concentration 50; Methicillin-Resistant Staphylococcus aureus; Mice; Oxidoreductases; Rats; Safety; Solubility; Structure-Activity Relationship; Water | 2018 |
Inhibition of human CYP3A catalyzed 1'-hydroxy midazolam formation by ketoconazole, nifedipine, erythromycin, cimetidine, and nizatidine.
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.
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 |
Inhibition of cytochrome P-450 3A (CYP3A) in human intestinal and liver microsomes: comparison of Ki values and impact of CYP3A5 expression.
Topics: Algorithms; Antifungal Agents; Blotting, Western; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; DNA, Complementary; Drug Interactions; Enzyme Inhibitors; Fluconazole; Humans; In Vitro Techniques; Intestine, Small; Ketoconazole; Kinetics; Microsomes; Microsomes, Liver; Midazolam; Mixed Function Oxygenases | 1999 |
Quantitative prediction of metabolic inhibition of midazolam by itraconazole and ketoconazole in rats: implication of concentrative uptake of inhibitors into liver.
Topics: Animals; Antifungal Agents; Blood Proteins; Hypnotics and Sedatives; Itraconazole; Ketoconazole; Male; Microsomes, Liver; Midazolam; Predictive Value of Tests; Protein Binding; Rats; Rats, Sprague-Dawley | 1999 |
Pharmacokinetics and electroencephalographic effects of ketoconazole in the rat.
Topics: Animals; Anti-Anxiety Agents; Antifungal Agents; Biological Availability; Chromatography, High Pressure Liquid; Electroencephalography; Half-Life; Injections, Intraperitoneal; Ketoconazole; Male; Metabolic Clearance Rate; Midazolam; Rats; Rats, Sprague-Dawley | 1999 |
Dose-dependent intestinal and hepatic first-pass metabolism of midazolam, a cytochrome P450 3A substrate with differently modulated enzyme activity in rats.
Topics: Animals; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; Biological Availability; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dexamethasone; Dose-Response Relationship, Drug; Injections, Intravenous; Intestinal Mucosa; Ketoconazole; Liver; Male; Midazolam; Oxidoreductases, N-Demethylating; Rats; Rats, Sprague-Dawley | 1999 |
Midazolam alpha-hydroxylation by human liver microsomes in vitro: inhibition by calcium channel blockers, itraconazole and ketoconazole.
Topics: Antifungal Agents; Biotransformation; Calcium Channel Blockers; GABA Modulators; Humans; Hydroxylation; Itraconazole; Ketoconazole; Male; Microsomes, Liver; Midazolam | 1999 |
Differentiation of intestinal and hepatic cytochrome P450 3A activity with use of midazolam as an in vivo probe: effect of ketoconazole.
Topics: Administration, Oral; Adult; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; Biological Availability; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Female; GABA Modulators; Humans; Infusions, Intravenous; Intestines; Ketoconazole; Liver; Male; Midazolam; Oxidoreductases, N-Demethylating; Regression Analysis; Time Factors | 1999 |
Midazolam and triazolam biotransformation in mouse and human liver microsomes: relative contribution of CYP3A and CYP2C isoforms.
Topics: Animals; Antibodies; Aryl Hydrocarbon Hydroxylases; Biotransformation; Blotting, Western; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Humans; Immunochemistry; In Vitro Techniques; Inhibitory Concentration 50; Ketoconazole; Mice; Microsomes, Liver; Midazolam; Mixed Function Oxygenases; Oxidoreductases, N-Demethylating; Protein Isoforms; Species Specificity; Steroid 16-alpha-Hydroxylase; Steroid Hydroxylases; Triazolam | 2000 |
Effects of age on in vitro midazolam biotransformation in male CD-1 mouse liver microsomes.
Topics: Age Factors; Alprazolam; Animals; Anti-Anxiety Agents; Aryl Hydrocarbon Hydroxylases; Biotransformation; Blotting, Western; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; In Vitro Techniques; Ketoconazole; Male; Mice; Microsomes, Liver; Midazolam; Oxidoreductases, N-Demethylating | 2000 |
Persistent inhibition of CYP3A4 by ketoconazole in modified Caco-2 cells.
Topics: Antifungal Agents; Caco-2 Cells; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Enzyme Activation; GABA Modulators; Humans; Hydroxylation; Ketoconazole; Midazolam; Mixed Function Oxygenases; Vitamin D | 2000 |
Modulation of midazolam 1-hydroxylation activity in vitro by neurotransmitters and precursors.
Topics: Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Epinephrine; gamma-Aminobutyric Acid; Humans; Hydroxytryptophol; In Vitro Techniques; Ketoconazole; Microsomes, Liver; Midazolam; Neurotransmitter Agents; Oxidoreductases, N-Demethylating; Protein Isoforms; Serotonin | 2000 |
Metabolism of amiodarone (Part III): identification of rabbit cytochrome P450 isoforms involved in the hydroxylation of mono-N-desethylamiodarone.
Topics: Amiodarone; Animals; Anti-Anxiety Agents; Anti-Arrhythmia Agents; Aryl Hydrocarbon Hydroxylases; Benzoflavones; Chromatography, High Pressure Liquid; Cimetidine; Cyclosporine; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Ketoconazole; Kinetics; Microsomes, Liver; Midazolam; Models, Chemical; Oxidoreductases, N-Demethylating; Protein Isoforms; Quinidine; Rabbits; Rifampin; Time Factors | 2001 |
Comparative studies to determine the selective inhibitors for P-glycoprotein and cytochrome P4503A4.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Caco-2 Cells; Cyclosporins; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Humans; Indans; Intestine, Small; Ketoconazole; Liver; Microsomes; Midazolam; Mixed Function Oxygenases; Piperazines; Verapamil; Vinblastine | 1999 |
Effect of multiple dosing of ketoconazole on pharmacokinetics of midazolam, a cytochrome P-450 3A substrate in beagle dogs.
Topics: Administration, Oral; Animals; Antifungal Agents; Biotransformation; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dogs; Drug Antagonism; Enzyme Inhibitors; In Vitro Techniques; Ketoconazole; Male; Microsomes, Liver; Midazolam | 2002 |
In vitro characterization of the inhibitory effects of ketoconazole on metabolic activities of cytochrome P-450 in canine hepatic microsomes.
Topics: Animals; Antifungal Agents; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dogs; Drug Interactions; Ethanolamines; Isoenzymes; Ketoconazole; Kinetics; Male; Microsomes, Liver; Midazolam; Oxazines; Tolbutamide | 2002 |
In vitro, pharmacokinetic, and pharmacodynamic interactions of ketoconazole and midazolam in the rat.
Topics: Algorithms; Animals; Anti-Anxiety Agents; Antifungal Agents; Biotransformation; Body Weight; Cytochrome P-450 Enzyme System; Drug Interactions; Injections, Intravenous; Intestinal Mucosa; Intestines; Intubation, Gastrointestinal; Ketoconazole; Liver Circulation; Male; Microsomes, Liver; Midazolam; Protein Binding; Rats; Rats, Sprague-Dawley | 2002 |
Expression of the human CYP3A4 gene in the small intestine of transgenic mice: in vitro metabolism and pharmacokinetics of midazolam.
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 |
Differential metabolism of midazolam in mouse liver and intestine microsomes: a comparison of cytochrome P450 activity and expression.
Topics: Algorithms; Animals; Anti-Anxiety Agents; Antibodies, Blocking; Biotransformation; Blotting, Western; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; In Vitro Techniques; Intestinal Mucosa; Isoenzymes; Ketoconazole; Kinetics; Mice; Mice, Inbred ICR; Microsomes; Microsomes, Liver; Midazolam; Organ Specificity; Ritonavir; Troleandomycin | 2003 |
In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5.
Topics: Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Humans; Ketoconazole; Microsomes, Liver; Midazolam; Nifedipine; Recombinant Proteins; Testosterone; Triazolam | 2003 |
Application of compartmental modeling to an examination of in vitro intestinal permeability data: assessing the impact of tissue uptake, P-glycoprotein, and CYP3A.
Topics: Animals; Aryl Hydrocarbon Hydroxylases; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Cyclosporins; Cytochrome P-450 CYP3A; In Vitro Techniques; Intestinal Absorption; Jejunum; Ketoconazole; Male; Midazolam; Models, Biological; Oxidoreductases, N-Demethylating; Permeability; Rats; Rats, Sprague-Dawley; Time Factors; Verapamil | 2003 |
High-throughput screening for the assessment of time-dependent inhibitions of new drug candidates on recombinant CYP2D6 and CYP3A4 using a single concentration method.
Topics: Amiodarone; Animals; Baculoviridae; Binding, Competitive; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Diltiazem; Enzyme Inhibitors; Fluorescence; Humans; Inhibitory Concentration 50; Ketoconazole; Miconazole; Midazolam; Propafenone; Quinolines; Recombinant Proteins; Troleandomycin; Verapamil | 2004 |
Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. I: evaluation of cynomolgus monkeys as surrogates for humans.
Topics: Administration, Oral; Animals; Antibodies; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Diltiazem; Drug Interactions; Enzyme Inhibitors; Erythromycin; Female; Humans; In Vitro Techniques; Ketoconazole; Kinetics; Macaca fascicularis; Microsomes, Liver; Midazolam; Models, Animal; Oxidoreductases, N-Demethylating | 2004 |
Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. II: establishment and evaluation of dexamethasone-pretreated female rats.
Topics: Administration, Oral; Animals; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP3A; Dexamethasone; Drug Interactions; Enzyme Inhibitors; Female; Humans; In Vitro Techniques; Ketoconazole; Kinetics; Microsomes, Liver; Midazolam; Models, Animal; Oxidoreductases, N-Demethylating; Rats; Rats, Sprague-Dawley | 2004 |
A study of the in vitro interaction between lidocaine and premedications using human liver microsomes.
Topics: Animals; Cimetidine; Clonidine; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP1A2 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Combinations; Drug Interactions; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Ketoconazole; Lidocaine; Microsomes, Liver; Midazolam; Neuromuscular Depolarizing Agents; Pentobarbital; Pharmacogenetics; Premedication; Rats; Theophylline; Thiamylal | 2005 |
Assessment of the hepatic and intestinal first-pass metabolism of midazolam in a CYP3A drug-drug interaction model rats.
Topics: Animals; Anti-Anxiety Agents; Anti-Inflammatory Agents; Antifungal Agents; Aryl Hydrocarbon Hydroxylases; Biotransformation; Cytochrome P-450 CYP3A; Dexamethasone; Drug Interactions; Female; Intestinal Mucosa; Ketoconazole; Liver; Midazolam; Oxidoreductases, N-Demethylating; Rats; Rats, Sprague-Dawley | 2005 |
CYP3A4 activity in four different animal species liver microsomes using 7-benzyloxyquinoline and HPLC/spectrofluorometric determination.
Topics: Animals; Calibration; Chemistry Techniques, Analytical; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dogs; Dose-Response Relationship, Drug; Haplorhini; Hydroxyquinolines; Inhibitory Concentration 50; Ketoconazole; Kinetics; Male; Mice; Microsomes, Liver; Midazolam; Quinolines; Rats; Rats, Wistar; Reproducibility of Results; Species Specificity; Spectrometry, Fluorescence; Steroid Hydroxylases; Substrate Specificity | 2006 |
Intestinal and hepatic CYP3A4 catalyze hydroxylation of 1alpha,25-dihydroxyvitamin D(3): implications for drug-induced osteomalacia.
Topics: Base Sequence; Caco-2 Cells; Calbindins; Calcitriol; Catalysis; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; DNA Primers; Gas Chromatography-Mass Spectrometry; Humans; Hydroxylation; Intestine, Small; Ketoconazole; Kinetics; Liver; Midazolam; Osteomalacia; Recombinant Proteins; S100 Calcium Binding Protein G; Troleandomycin | 2006 |
Comparison of mouse and rat cytochrome P450-mediated metabolism in liver and intestine.
Topics: Animals; Carbamazepine; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Hydroxytestosterones; In Vitro Techniques; Intestinal Mucosa; Intestines; Ketoconazole; Liver; Male; Membrane Proteins; Mice; Mice, Nude; Microsomes; Midazolam; Oxidoreductases; Rats; Rats, Sprague-Dawley; RNA, Messenger; Substrate Specificity | 2006 |
Stochastic prediction of CYP3A-mediated inhibition of midazolam clearance by ketoconazole.
Topics: Age Factors; Body Weight; Computer Simulation; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Enzyme Inhibitors; Forecasting; Humans; Ketoconazole; Liver; Midazolam; Models, Biological; Pharmacokinetics; Reproducibility of Results; Sex Factors; Software; Stochastic Processes | 2006 |
Characterization of the rhesus monkey CYP3A64 enzyme: species comparisons of CYP3A substrate specificity and kinetics using baculovirus-expressed recombinant enzymes.
Topics: Amino Acid Sequence; Animals; Baculoviridae; Base Sequence; Blotting, Western; Cell Line; Cloning, Molecular; Coumarins; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; DNA, Complementary; Humans; Ketoconazole; Kinetics; Liver; Macaca mulatta; Microsomes, Liver; Midazolam; Molecular Sequence Data; Nifedipine; Recombinant Proteins; Sequence Analysis, DNA; Spodoptera; Substrate Specificity; Testosterone | 2006 |
Cytochrome P450-dependent metabolism of midazolam in hepatic microsomes from chickens, turkeys, pheasant and bobwhite quail.
Topics: Animals; Anti-Anxiety Agents; Antifungal Agents; Birds; Chickens; Cytochrome P-450 CYP3A; Inhibitory Concentration 50; Ketoconazole; Microsomes, Liver; Midazolam; Quail; Species Specificity; Turkeys | 2006 |
Effect of oral ketoconazole on intestinal first-pass effect of midazolam and fexofenadine in cynomolgus monkeys.
Topics: Animals; Antifungal Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Intestinal Mucosa; Intestines; Ketoconazole; Liver; Macaca fascicularis; Male; Microsomes; Midazolam; Terfenadine | 2007 |
Evaluation of the effects of hydrophilic organic solvents on CYP3A-mediated drug-drug interaction in vitro.
Topics: Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Interactions; Enzyme Inhibitors; Humans; Hydroxylation; In Vitro Techniques; Ketoconazole; Liver; Microsomes, Liver; Midazolam; Solvents; Steroid Hydroxylases; Substrate Specificity; Testosterone | 2006 |
Effect of ion suppression on judgment of enzyme inhibition and avoidance of error by utilizing a stable isotope-labeled probe substrate: example of CYP3A4 inhibition with [13C4,15N] labeled midazolam as a substrate.
Topics: Artifacts; Carbon Isotopes; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dextrorphan; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Enzyme Inhibitors; Erythromycin; Humans; Hydroxylation; In Vitro Techniques; Ketoconazole; Liver; Microsomes, Liver; Midazolam; Molecular Probes; Nitrogen Isotopes; Reproducibility of Results; Tandem Mass Spectrometry | 2007 |
Use of isolated hepatocyte preparations for cytochrome P450 inhibition studies: comparison with microsomes for Ki determination.
Topics: Animals; Catalysis; Cells, Cultured; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dextromethorphan; Enzyme Inhibitors; Fluconazole; Fluoxetine; Fluvoxamine; Hepatocytes; Ketoconazole; Kinetics; Male; Miconazole; Microsomes, Liver; Midazolam; Phenytoin; Quinine; Rats; Rats, Sprague-Dawley; Tolbutamide | 2007 |
Development of an in vivo rat screen model to predict pharmacokinetic interactions of CYP3A4 substrates.
Topics: Animals; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Evaluation, Preclinical; Drug Interactions; Humans; In Vitro Techniques; Ketoconazole; Male; Microsomes, Liver; Midazolam; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Substrate Specificity; Xenobiotics | 2007 |
Quantitative correlations among CYP3A sensitive substrates and inhibitors: literature analysis.
Topics: Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Databases, Factual; Drug Interactions; Enzyme Inhibitors; Erythromycin; Fluconazole; Ketoconazole; Midazolam; Substrate Specificity; Verapamil | 2007 |
Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans.
Topics: Adolescent; Adult; Aged; Cells, Cultured; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Glucuronides; Glucuronosyltransferase; Hepatocytes; Humans; Ketoconazole; Male; Microsomes, Liver; Midazolam; Middle Aged | 2008 |
[Effect of polyoxyl ether analogous surfactants on the activity of cytochromes P450 3A in rats in vivo].
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.
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 |
[A limited sampling strategy of phenotyping probe midazolam to predict inhibited activities of hepatic CYP3A in rats].
Topics: Animals; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Enzyme Inhibitors; Injections, Intravenous; Ketoconazole; Male; Metabolic Clearance Rate; Midazolam; Phenotype; Random Allocation; Rats; Rats, Wistar | 2008 |
A new probabilistic rule for drug-dug interaction prediction.
Topics: Algorithms; Area Under Curve; Bayes Theorem; Computer Simulation; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Fasting; Female; Humans; Ketoconazole; Male; Meta-Analysis as Topic; Midazolam; Models, Statistical; Monte Carlo Method; Pharmacokinetics; Probability | 2009 |
Limited sampling strategy in rats to predict the inhibited activities of hepatic CYP3A.
Topics: Adjuvants, Anesthesia; Animal Use Alternatives; Animals; Antifungal Agents; Cytochrome P-450 CYP3A; Drug Interactions; Enzyme Inhibitors; Injections, Intravenous; Ketoconazole; Liver; Male; Midazolam; Predictive Value of Tests; Rats; Rats, Wistar; Specific Pathogen-Free Organisms | 2009 |
In vitro metabolism and inhibitory effects of pranlukast in human liver microsomes.
Topics: Anti-Asthmatic Agents; Antibodies, Blocking; Antifungal Agents; Cell Line, Tumor; Chromones; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Interactions; Humans; Hypnotics and Sedatives; Hypoglycemic Agents; Ketoconazole; Leukotriene Antagonists; Microsomes, Liver; Midazolam; Oxygenases; Terfenadine; Tolbutamide | 2009 |
Differential effect of Shenmai injection, a herbal preparation, on the cytochrome P450 3A-mediated 1'-hydroxylation and 4-hydroxylation of midazolam.
Topics: Animals; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Combinations; Drugs, Chinese Herbal; Humans; Hydroxylation; Ketoconazole; Kinetics; Microsomes, Liver; Midazolam; Rats; Recombinant Proteins | 2009 |
Inhibitory effects of ketoconazole, cimetidine and erythromycin on hepatic CYP3A activities in cats.
Topics: Animals; Anti-Bacterial Agents; Antifungal Agents; Area Under Curve; Cats; Cimetidine; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Enzyme Inhibitors; Erythromycin; Female; Half-Life; Hypnotics and Sedatives; Ketoconazole; Microsomes, Liver; Midazolam | 2009 |
Drug-drug interaction prediction assessment.
Topics: Analysis of Variance; Area Under Curve; Bayes Theorem; Bias; Computer Simulation; Data Interpretation, Statistical; Drug Interactions; Humans; Ketoconazole; Midazolam; Models, Statistical; Research Design; Sample Size | 2009 |
Predictions of metabolic drug-drug interactions using physiologically based modelling: Two cytochrome P450 3A4 substrates coadministered with ketoconazole or verapamil.
Topics: Algorithms; Area Under Curve; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Metabolic Clearance Rate; Midazolam; Models, Biological; Monte Carlo Method; Verapamil | 2010 |
CYP3A4 catalytic activity is induced in confluent Huh7 hepatoma cells.
Topics: Aflatoxin B1; Catalysis; Cell Line; Cell Line, Tumor; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Interactions; Gene Expression; Humans; Ketoconazole; Microsomes, Liver; Midazolam; Rifampin; Testosterone; Transcription Factors | 2010 |
High performance liquid chromatographic assay for the simultaneous determination of midazolam and ketoconazole in plasma.
Topics: Animals; Calibration; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Midazolam; Rats | 2010 |
Bioavailability considerations in evaluating drug-drug interactions using the population pharmacokinetic approach.
Topics: Algorithms; Biological Availability; Biotransformation; Computer Simulation; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Metabolic Clearance Rate; Midazolam; Models, Biological; Pharmacokinetics | 2011 |
Evaluation of the pharmacokinetic interaction of midazolam with ursodeoxycholic acid, ketoconazole and dexamethasone by brain benzodiazepine receptor occupancy.
Topics: Administration, Oral; Animals; Brain; Cytochrome P-450 CYP3A; Dexamethasone; Drug Interactions; Enzyme Induction; Enzyme Inhibitors; GABA Modulators; Ketoconazole; Male; Midazolam; Protein Binding; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, GABA-A; Time Factors; Ursodeoxycholic Acid | 2011 |
Mechanism of cytochrome P450-3A inhibition by ketoconazole.
Topics: Adult; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Humans; Inhibitory Concentration 50; Ketoconazole; Male; Microsomes, Liver; Midazolam; Middle Aged; Nifedipine; Testosterone; Triazolam; Young Adult | 2011 |
Effect of hyperlipidemia on ketoconazole-midazolam drug-drug interaction in rat.
Topics: Animals; Blood Proteins; Drug Interactions; Hyperlipidemias; Ketoconazole; Male; Midazolam; Protein Binding; Rats; Rats, Sprague-Dawley | 2011 |
Inhibitory effects of continuous ingestion of Schisandrin A on CYP3A in the rat.
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 |
Impact of nonlinear midazolam pharmacokinetics on the magnitude of the midazolam-ketoconazole interaction in rats.
Topics: Administration, Intravenous; Administration, Oral; Animals; Antifungal Agents; Blood Proteins; Chromatography, Liquid; Computer Simulation; Drug Interactions; Humans; Hypnotics and Sedatives; Ketoconazole; Male; Mass Spectrometry; Microsomes, Liver; Midazolam; Models, Chemical; Rats; Rats, Sprague-Dawley | 2012 |
Discovery of a highly selective CYP3A4 inhibitor suitable for reaction phenotyping studies and differentiation of CYP3A4 and CYP3A5.
Topics: Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Drug Discovery; Enzyme Inhibitors; Half-Life; Humans; Hydroxylation; Imidazoles; Ketoconazole; Liver; Microsomes, Liver; Midazolam; Molecular Structure; Phenotype; Phenylurea Compounds; Recombinant Proteins; Structure-Activity Relationship; Substrate Specificity; Testosterone | 2012 |
An integrated pharmacokinetics ontology and corpus for text mining.
Topics: Cytochrome P-450 Enzyme System; Data Mining; Databases, Factual; Drug Interactions; Ketoconazole; Midazolam; Pharmacokinetics; Tamoxifen | 2013 |
In vivo effect of Schisandrin B on cytochrome P450 enzyme activity.
Topics: Administration, Oral; Animals; Biological Availability; Cyclooctanes; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Drug Interactions; Ketoconazole; Lignans; Liver; Male; Medicine, Chinese Traditional; Microsomes, Liver; Midazolam; Polycyclic Compounds; Rats; Rats, Sprague-Dawley | 2013 |
Optimization of drug-drug interaction study design: comparison of minimal physiologically based pharmacokinetic models on prediction of CYP3A inhibition by ketoconazole.
Topics: Area Under Curve; Cytochrome P-450 CYP3A Inhibitors; Dose-Response Relationship, Drug; Drug Interactions; Enzyme Inhibitors; Humans; Ketoconazole; Midazolam; Models, Biological; Research Design | 2013 |
Effect of CYP3A5 expression on the inhibition of CYP3A-catalyzed drug metabolism: impact on modeling CYP3A-mediated drug-drug interactions.
Topics: Biocatalysis; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Genotype; Humans; Itraconazole; Ketoconazole; Male; Microsomes, Liver; Midazolam; Terfenadine; Testosterone; Vincristine | 2013 |
Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions.
Topics: Allosteric Regulation; Animals; Cytochrome P-450 CYP3A; Drug Interactions; Hepatocytes; Humans; Intestinal Mucosa; Intestines; Ketoconazole; Kinetics; Liver; Male; Mice; Microsomes; Microsomes, Liver; Midazolam; Mixed Function Oxygenases; Rats; Rats, Sprague-Dawley | 2013 |
Simultaneous and comprehensive in vivo analysis of cytochrome P450 activity by using a cocktail approach in rats.
Topics: Animals; Caffeine; Cytochrome P-450 Enzyme Inducers; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dexamethasone; Dextromethorphan; Drug Interactions; Fluconazole; Fluvoxamine; Ketoconazole; Losartan; Male; Midazolam; Omeprazole; Rats, Sprague-Dawley | 2014 |
Response to "can CYP3A activity be evaluated for drug interaction using a nanogram dose of probe drug?": evaluation of CYP3A activity with microdoses of midazolam.
Topics: Cytochrome P-450 CYP3A; Female; Humans; Ketoconazole; Male; Midazolam | 2014 |
Can CYP3A activity be evaluated for drug interaction using a nanogram dose of probe drug?
Topics: Cytochrome P-450 CYP3A; Female; Humans; Ketoconazole; Male; Midazolam | 2014 |
Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Topics: Brentuximab Vedotin; Computer Simulation; Drug Interactions; Humans; Immunoconjugates; Ketoconazole; Midazolam; Models, Biological; Oligopeptides; Rifampin | 2015 |
Characterization of midazolam metabolism in locusts: the role of a CYP3A4-like enzyme in the formation of 1'-OH and 4-OH midazolam.
Topics: Animals; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Glycosylation; Grasshoppers; Insect Proteins; Ketoconazole; Magnetic Resonance Imaging; Male; Midazolam | 2016 |
Mechanism of Action of Panaxytriol on Midazolam 1'-Hydroxylation and 4-Hydroxylation Mediated by CYP3A in Liver Microsomes and Rat Primary Hepatocytes.
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 |
Allosteric activation of midazolam CYP3A5 hydroxylase activity by icotinib - Enhancement by ketoconazole.
Topics: Allosteric Regulation; Animals; Antineoplastic Agents; Crown Ethers; Cytochrome P-450 CYP3A; Dogs; Dose-Response Relationship, Drug; Drug Interactions; Haplorhini; Humans; In Vitro Techniques; Ketoconazole; Mice; Microsomes, Liver; Midazolam; Quinazolines; Rats; Species Specificity; Substrate Specificity | 2016 |
The absorption kinetics of ketoconazole plays a major role in explaining the reported variability in the level of interaction with midazolam: Interplay between formulation and inhibition of gut wall and liver metabolism.
Topics: Adult; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug Interactions; Female; Gastrointestinal Tract; Humans; Ketoconazole; Liver; Male; Midazolam; Middle Aged; Models, Biological | 2017 |
Pharmacokinetic Evaluation of the Interactions of Amenamevir (ASP2151) with Ketoconazole, Rifampicin, Midazolam, and Warfarin in Healthy Adults.
Topics: Adolescent; Adult; Area Under Curve; Cross-Over Studies; Cytochrome P-450 CYP3A; Double-Blind Method; Drug Interactions; Enzyme Induction; Humans; Ketoconazole; Male; Metabolic Clearance Rate; Midazolam; Middle Aged; Oxadiazoles; Rifampin; Warfarin; Young Adult | 2017 |
Simultaneous Physiologically Based Pharmacokinetic (PBPK) Modeling of Parent and Active Metabolites to Investigate Complex CYP3A4 Drug-Drug Interaction Potential: A Case Example of Midostaurin.
Topics: Adult; Biomarkers; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inducers; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Humans; Hydroxycholesterols; Ketoconazole; Male; Midazolam; Middle Aged; Models, Biological; Rifampin; Staurosporine; Young Adult | 2018 |
Simultaneous Prediction of Intestinal Absorption and Metabolism Using the Mini-Ussing Chamber System.
Topics: Animals; Drug Delivery Systems; Intestinal Absorption; Intestinal Mucosa; Ketoconazole; Male; Midazolam; Nifedipine; Permeability; Pharmaceutical Preparations; Rats; Rats, Sprague-Dawley | 2019 |
Evaluation of the Effects of Maytenus ilicifolia on the Activities of Cytochrome P450 3A and P-glycoprotein.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Caco-2 Cells; Cell Line; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Ketoconazole; Male; Maytenus; Midazolam; Plant Extracts; Quinolines; Rats; Rats, Wistar; Terfenadine | 2020 |
Physiologically based pharmacokinetic modeling to assess metabolic drug-drug interaction risks and inform the drug label for fedratinib.
Topics: Area Under Curve; Computer Simulation; Cytochrome P-450 CYP2C8; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Drug Labeling; Healthy Volunteers; Humans; Janus Kinase 2; Ketoconazole; Midazolam; Models, Biological; Primary Myelofibrosis; Protein Kinase Inhibitors; Pyrrolidines; Sulfonamides | 2020 |
Physiologically Based Pharmacokinetic Model-Informed Drug Development for Polatuzumab Vedotin: Label for Drug-Drug Interactions Without Dedicated Clinical Trials.
Topics: Antibodies, Monoclonal; Brentuximab Vedotin; Computer Simulation; Cytochrome P-450 CYP3A; Drug Development; Drug Interactions; Drug Labeling; Humans; Immunoconjugates; Ketoconazole; Midazolam; Models, Biological; Oligopeptides; Rifampin | 2020 |
Leveraging Physiologically Based Pharmacokinetic Modeling and Experimental Data to Guide Dosing Modification of CYP3A-Mediated Drug-Drug Interactions in the Pediatric Population.
Topics: Adolescent; Adult; Anti-Anxiety Agents; Antifungal Agents; Child; Child, Preschool; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Humans; Infant; Ketoconazole; Macrolides; Midazolam; Tandem Mass Spectrometry; Triazoles | 2021 |