Drug Interactions Involving 17α‐Ethinylestradiol: Considerations Beyond Cytochrome P450 3A Induction and Inhibition

2021 ◽  
Author(s):  
A. David Rodrigues
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Cytochrome P450 3A

scholarly journals Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin

2014 ◽  
Vol 77 (6) ◽  
pp. 1039-1050 ◽  
Author(s):  
Spencer Y. Ling ◽  
Robert B. Huizinga ◽  
Patrick R. Mayo ◽  
Richard Larouche ◽  
Derrick G. Freitag ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Cytochrome P450 3A ◽  
P Glycoprotein

Clinical Drug-Drug Interactions Through Cytochrome P450 3A (CYP3A) for the Selective ALK Inhibitor Alectinib

2016 ◽  
Vol 6 (3) ◽  
pp. 280-291 ◽  
Author(s):  
Peter N. Morcos ◽  
Yumi Cleary ◽  
Elena Guerini ◽  
Georgina Dall ◽  
Katrijn Bogman ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Cytochrome P450 3A ◽  
Alk Inhibitor ◽  
Clinical Drug

scholarly journals Complex Drug Interactions of HIV Protease Inhibitors 1: Inactivation, Induction, and Inhibition of Cytochrome P450 3A by Ritonavir or Nelfinavir

2011 ◽  
Vol 39 (6) ◽  
pp. 1070-1078 ◽  
Author(s):  
Brian J. Kirby ◽  
Ann C. Collier ◽  
Evan D. Kharasch ◽  
Dale Whittington ◽  
Kenneth E. Thummel ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Cytochrome P450 3A ◽  
Complex Drug

Alteration of drug-metabolizing enzyme activity in palliative care patients: Microdosed assessment of cytochrome P450 3A

2019 ◽  
Vol 33 (7) ◽  
pp. 850-855
Author(s):  
Marcus Geist ◽  
Hubert Bardenheuer ◽  
Juergen Burhenne ◽  
Gerd Mikus
Keyword(s):  
Palliative Care ◽  
Cytochrome P450 ◽  
Drug Interactions ◽  
Real Life ◽  
Palliative Care Unit ◽  
Metabolic Clearance ◽  
Cytochrome P450 3A ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme ◽  
Clinical Conditions

Background: Cytochrome P450 3A is the most relevant drug-metabolizing enzyme in humans as it is involved in the elimination of 50% of marketed drugs. Nothing is known about the activity of cytochrome P450 3A in palliative care patients who have complicated symptoms often associated with a terminal illness. Aim: In order to improve drug dosing in end-of-life care and to avoid drug interactions, cytochrome P450 3A activity was determined in patients of a palliative care unit under real-life clinical conditions. Design: As midazolam is an established marker substance for cytochrome P450 3A activity, this single-arm prospective trial was designed to obtain a 4-h pharmacokinetic profile of midazolam after oral administration of a 10-µg dose from each enrolled patient. Plasma concentrations of midazolam and its primary metabolite 1′-hydroxy-midazolam were quantified by mass spectrometry techniques. Cytochrome P450 3A activity was calculated as partial metabolic clearance from a limited sampling area under the curve. All other drugs taken by the participating patients were considered, as well as recent blood test results and patients’ diagnoses. The trial was registered at German Clinical Trials Register ( www.drks.de ): DRKS00011753. Setting/participants: The trial was carried out at a university palliative care unit under real-life clinical conditions. Every patient admitted to the ward was screened for possible participation, independent of the individual performance status. Results: Partial metabolic clearance of midazolam in palliative care patients was 31.7 ± 32.1 L/h. This was a highly significant 40% reduction ( p < 0.0001) in comparison with the cytochrome P450 3A activity of healthy subjects. Conclusion: Dosing of cytochrome P450 3A substrate drugs (e.g. macrolide antibiotics, benzodiazepines, calcium channel blockers) needs to be adjusted in palliative care patients; otherwise, escalation of debilitating symptoms due to drug interactions might occur.

Inhibition of Cytochrome P450 3A: Relevant Drug Interactions in Gastroenterology

Digestion ◽  
2003 ◽  
Vol 68 (1) ◽  
pp. 41-48 ◽  
Author(s):  
A. Sagir ◽  
M. Schmitt ◽  
K. Dilger ◽  
D. Häussinger
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
Cytochrome P450 3A
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