Pharmacokinetics of Dapaconazole, A Novel Antifungal Agent, in Beagle Dogs and Inhibition of Cytochrome P450 Family 51 / Juliana S. Palo, Noedi L. de Freitas, Samuel G.N.e Silva, Julio A. Rojas-Moscoso, Tiago Zaminelli, Caroline H. Lescano, Gustavo D. Mendes, Gilberto De Nucci
Objectives: Pharmacokinetics of dapaconazole and inhibition of cytochrome P450 family 51. Methods: Pharmacokinetics of dapaconazole, a novel imidazolic antifungal compound, was studied in male beagle dogs following intravenous (1, 2 and 20 mg/kg) and oral (20 mg/kg) administration. Results: Oral bioavailability was calculated to be 97.3%. The elimination half-life (t½) after intravenous administration was 2.1-2.5 h, the total body clearance was 2.5-4.2 L/h/kg and the apparent volume of distribution was 9.0-14.4 L/kg. Dapaconazole caused concentration-dependent inhibition of cytochrome P450 family 51 (CYP51) activity with an IC50 of 1.4 ± 0.3 μM (mean ± SEM, n=3), compared to that of ketoconazole (IC50 = 1.2 ± 0.6 μM, n=3). Conclusion: Results indicate that dapaconazole could be a potentially useful drug for systemic administration.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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| Enthalten in: |
Anti-infective agents - 16(2018), 1, Seite 15- |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Palo, Juliana S. [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (7 p) |
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| Förderinstitution / Projekttitel: |
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KFL008994072 |
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| 245 | 1 | 0 | |a Pharmacokinetics of Dapaconazole, A Novel Antifungal Agent, in Beagle Dogs and Inhibition of Cytochrome P450 Family 51 |c Juliana S. Palo, Noedi L. de Freitas, Samuel G.N.e Silva, Julio A. Rojas-Moscoso, Tiago Zaminelli, Caroline H. Lescano, Gustavo D. Mendes, Gilberto De Nucci |
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| 520 | |a Objectives: Pharmacokinetics of dapaconazole and inhibition of cytochrome P450 family 51. Methods: Pharmacokinetics of dapaconazole, a novel imidazolic antifungal compound, was studied in male beagle dogs following intravenous (1, 2 and 20 mg/kg) and oral (20 mg/kg) administration. Results: Oral bioavailability was calculated to be 97.3%. The elimination half-life (t½) after intravenous administration was 2.1-2.5 h, the total body clearance was 2.5-4.2 L/h/kg and the apparent volume of distribution was 9.0-14.4 L/kg. Dapaconazole caused concentration-dependent inhibition of cytochrome P450 family 51 (CYP51) activity with an IC50 of 1.4 ± 0.3 μM (mean ± SEM, n=3), compared to that of ketoconazole (IC50 = 1.2 ± 0.6 μM, n=3). Conclusion: Results indicate that dapaconazole could be a potentially useful drug for systemic administration | ||
| 700 | 1 | |a de Freitas, Noedi L. |e verfasserin |4 aut | |
| 700 | 1 | |a Silva, Samuel G.N.e. |e verfasserin |4 aut | |
| 700 | 1 | |a Rojas-Moscoso, Julio A. |e verfasserin |4 aut | |
| 700 | 1 | |a Zaminelli, Tiago |e verfasserin |4 aut | |
| 700 | 1 | |a Lescano, Caroline H. |e verfasserin |4 aut | |
| 700 | 1 | |a D. Mendes, Gustavo |e verfasserin |4 aut | |
| 700 | 1 | |a De Nucci, Gilberto |e verfasserin |4 aut | |
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