Review of the pharmacokinetics, pharmacogenetics, and drug interaction potential of antidepressants: focus on venlafaxine
Ereshefsky L, Dugan D
College of Pharmacy,
University of Texas at Austin, USA.
Depress Anxiety 2000; 12 Suppl 1:30-44


Improving outcomes for patients with depression involves selecting the best possible drug therapy. Considerations relevant to drug product selection include: 1) pharmacokinetic issues such as half-life and time to steady-state, and protein binding; 2) pharmacodynamic drug-drug interactions; and 3) drug metabolism-related drug interactions. A comparison of selected antidepressants with an emphasis on venlafaxine's similarities and differences is presented. Based on these parameters, selecting an antidepressant medication, such as venlafaxine, that has a low potential for drug interactions at the Cytochrome P450 (CYP) enzyme system, and is easy to monitor and dose, facilitate successful treatment of patients. Venlafaxine has been evaluated in clinical studies that demonstrate low to negligible drug interaction potential at CYP2D6, CYP1A2, CYP2C19, and CYP3A4. Its short half-life and time to steady-state, when coupled with the extended release characteristics of the preferred dosage formulation allow for once daily dosing and rapid attainment of therapeutic effects. The CYP3A4 system is involved in both first-pass metabolism and systemic clearance of medications. Drug interactions at this isoenzyme have proven to be of high clinical relevance ranging from cardiovascular toxicity and death with commonly used drugs such as cisapride, to subtherapeutic levels of cyclosporine or protease inhibitors leading to transplant rejection or HIV relapse. Reasons for the under detection and reporting of drug interaction mediated adverse events include healthcare system structure, the poor return to follow up of non-adherent patients, the need for greater education and training of clinicians to recognize drug-related adverse events, and the reluctance of patients to spontaneously communicate about the unpleasant effects of their medication.
Venlafaxine v SSRIs
Venlafaxine compared
Venlafaxine v fluoxetine
High-dose venlafaxine XL
Venlafaxine pharmacology
Venlafaxine plus bupropion
Venlafaxine and depression
Venlafaxine and neuropeptides
Venlafaxine and major depression
Venlafaxine for depressive cocaine users
Venlafaxine (Effexor) v clomipramine for OCD
Venlafaxine for treatment-resistant depression
Venlafaxine, emotional processing and the brain
Depression treated with different formulations of venlafaxine
February 2008: FDA licenses antidepressant desvenlafaxine (Pristiq)

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