Is Wellbutrin a CYP2D6 inhibitor?
Is Wellbutrin a CYP2D6 inhibitor?
Bupropion is therefore a potent inhibitor of CYP2D6 activity, and care should be exercised when initiating or discontinuing bupropion use in patients taking drugs metabolized by CYP2D6.
What is metabolized by CYP2B6?
Drugs metabolized mainly by CYP2B6 include artemisinin, bupropion, cyclophosphamide, efavirenz, ketamine, and methadone. CYP2B6 is one of the most polymorphic CYP genes in humans and variants have been shown to affect transcriptional regulation, splicing, mRNA and protein expression, and catalytic activity.
What gene metabolizes Wellbutrin?
Background. Bupropion, an antidepressant and smoking cessation medication, is metabolized to hydroxybupropion (HB), an active metabolite, primarily by CYP2B6.
How is bupropion metabolized?
Results: : Bupropion is extensively metabolized by the liver (t(1/2), approximately 21 hours). Hydroxybupropion, the primary active metabolite (t(1/2), approximately 20 hours), is formed by cytochrome P450 (CYP) 2B6.
What drugs are CYP2D6 inhibitors?
| Strong inhibitors | Weak inhibitors | |
|---|---|---|
| CYP2D6 | bupropion, fluoxetine(g), paroxetine, quinidine(h), terbinafine | amiodarone, celecoxib, cimetidine, clobazam, cobicistat, escitalopram, fluvoxamine(a), labetalol, ritonavir(h,i,j), sertraline, vemurafenib |
What induces CYP2D6?
Dexamethasone and corticosterone were the most potent inducers of CYP2D6 followed by prednisolone and cortisol.
What is CYP2B6 * 6?
CYP2B6 (Cytochrome P450 Family 2 Subfamily B Member 6) is a Protein Coding gene. Diseases associated with CYP2B6 include Efavirenz, Poor Metabolism Of and Acute Frontal Sinusitis.
Does everyone have CYP2C9?
CYP2C9∗2 is frequent among Caucasians with approximately 1% of the population being homozygous carriers and 22% heterozygous. The corresponding figures for the CYP2C9∗3 allele are 0.4% and 15%, respectively. Worldwide, a number of other variants have also to be reported.
What does CYP2C19 rapid metabolizer mean?
In people who are rapid metabolizers, the CYP2C19 enzyme has high activity. People who are rapid metabolizers break down some medicines quickly and may need different doses or a different medicine. About 29% of our patients are rapid metabolizers.
What is a sensitive substrate?
Moderate sensitive substrates are drugs that demonstrate an increase in AUC of ≥2 to <5-fold with strong index inhibitors of a given metabolic pathway in clinical DDI studies.
Does bupropion damage the liver?
Bupropion is an aminoketone antidepressant that is widely used in therapy of depression and smoking cessation. Bupropion therapy can be associated with transient, usually asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.
