Monograph
N06AX16 - Venlafaxine |
Propably not porphyrinogenic |
PNP |
Rationale
Metabolised by CYPs, but does not inhibit CYP 3A4 or CYP 2C9. Does not induce CYP 3A4. Some clinical evidence of non-porphyrinogenicity.
Therapeutic characteristics
Serotonine and noradrenaline reuptake inhibitor, antidepressant. Common adverse reactions of venlafaxine that can be confused with an acute porphyric attack are abdominal pain, nausea, vomiting, constipation, tachycardia, insomnia, paresthesia, anxiety.
Metabolism and pharmacokinetics
Extensively metabolized via CYP 2D6 and CYP 3A3/4. Som metabolism by CYP 2C9 (Fogelman 1999). Weak inhibitor of CYP 2D6. No effect on CYP 3A4. In vitro and in vivo data indicate that venlafaxine either does not significantly inhibit or weakly inhibits the activity of isoenzymes CYP2C9, CYP2D6, CYP1A2, or CYP3A3/4 (Ereshefsky L 1996). Ball et al. (1997) reported that venlafaxine did not inhibit CYP1A2 or CYP2C9 activity.
Personal communication
Andersson; patient inquiry: used without illeffects (n=1). Peters: According to our experience probably not porphyrinogenic.
Published experience
Holroyd S et al. Psychotropic drugs in acute.. /10511069/:
IPNet drug reports
Uneventful use reported in 6 patient with acute porphyria.
References
| # |
Citation details |
PMID |
|---|
| * | Scientific articles |
| 1. |
Venlafaxine: in vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9 and CYP1A2. Br J Clin Pharmacol 1997;43(6):619-26.
Ball SE, Ahern D et al. |
|
| 2. |
Comparative CYP3A4 inhibitory effects of venlafaxine, fluoxetine, sertraline, and nefazodone in healthy volunteers. J Clin Psychopharmacol 2004;24(1):4-10.
DeVane CL, Donovan JL et al. |
14709940 |
| 3. |
Drug-drug interactions involving antidepressants: focus on venlafaxine. J Clin Psychopharmacol 1996;16(3 Suppl 2):37S-50S; discussion 50S-53S.
Ereshefsky L. |
8784647 |
| 4. |
O- and N-demethylation of venlafaxine in vitro by human liver microsomes and by microsomes from cDNA-transfected cells: effect of metabolic inhibitors and SSRI antidepressants. Neuropsychopharmacology 1999;20(5):480-90.
Fogelman SM, Schmider J et al. |
10192828 |
| 5. |
Psychotropic drugs in acute intermittent porphyria. Clin Pharmacol Ther 1999;66(3):323-5.
Holroyd S, Seward RL. |
10511069 |
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