Minor contribution of cytochrome P450 3A activity on fentanyl exposure in palliative care cancer patients.

Transdermal fentanyl is widely used to control pain in cancer patients. The high pharmacokinetic variability of fentanyl is assumed to be due to cytochrome P450 3A-mediated (CYP3A) N-dealkylation to norfentanyl in humans. However, recently published clinical studies question the importance of the described metabolic pathway.

Decreased Cytochrome P450 3A activity in palliative patients with haematological diseases: Potential impact on supportive drug therapies.

Cytochrome P450 3A (CYP3A) is the most relevant drug-metabolizing enzyme in human beings involved in the elimination of about 50% of the marketed drugs. Comprehensive in vivo data of CYP3A activity in palliative patients with haematological diseases are missing. Therefore, CYP3A activity was determined under real-life clinical conditions in patients to gain knowledge about dose adjustments for supportive therapies and symptom management in haematology.

Impact of patient education on plasma concentrations and effectiveness of posaconazole oral suspension under clinical conditions.

Posaconazole prophylaxis is recommended for patients with acute myeloid leukaemia during induction chemotherapy. Although a tablet formulation with better oral bioavailability is available, some patients have to rely on the oral suspension in clinical routine. Therefore, effectiveness of posaconazole oral suspension under real-life clinical conditions and impact of patient education about the correct intake on its plasma concentrations were assessed in this study.

In Vivo CYP3A Activity in Palliative Care Patients: Study Protocol for a Single Arm Prospective Trial.

Background: Drug interactions are a common cause for escalation of debilitating symptoms in palliative care patients. CYP3A is the most relevant CYP enzyme in humans involved in metabolism of about half of all available pharmaceuticals.

Objective: To increase knowledge about the CYP3A enzyme and the impact of drug interactions on its activity to improve dosing in palliative care patients.

Bleeding Control in Palliative Care Patients With the Help of Tranexamic Acid.

Background: Persistent bleeding is a common reason for admitting patients with advanced cancer to a palliative care unit. Several reports show a successful therapeutic use of the antifibrinolytic agent tranexamic acid in palliative care patients having hemorrhages. However, it is not administered routinely in severe bleeding situations in palliative care, and general dosing recommendations are unclear.

Steady-state pharmacokinetics and metabolism of voriconazole in patients.

Objectives: Voriconazole exhibits non-linear pharmacokinetics in adults and is said to be mainly metabolized by CYP2C19 and CYP3A4 to voriconazole-N-oxide. The aim of this study was to obtain data on steady-state pharmacokinetics after dosing for at least 14 days in patients taking additional medication and in vivo data on metabolites other than voriconazole-N-oxide.

Patients And Methods: Thirty-one patients receiving voriconazole as regular therapeutic drug treatment during hospitalization participated in this prospective study.