Сравнительная таблица: дулоксетин и венлафаксин

"Venlafaxine (Effexor, Effexor XR) has the flexibility of being an SSRI at lower doses (75 mg/day), affecting the reuptake of serotonin, and an SNRI at higher doses (150-225 mg/day). It also very weakly blocks the reuptake of dopamine at very high doses (above 350 mg/day).

Duloxetine (Cymbalta) is a strong, balanced inhibitor of both norepinephrine and serotonin reuptake.

Duloxetine differs from venlafaxine in that it is comparatively more noradrenergic। Venlafaxine has a 30-fold higher affinity for serotonin than for norepinephrine while duloxetine has a 10-fold selectivity for serotonin6. Approximate potency ratios (5-HT:NE) are 1:10 for duloxetine, and 1:30 for venlafaxine."

Brief comparison table

	Venlafaxine (Effexor)	Duloxetine (Cymbalta)
Generic name	Venlafaxine hydrochloride	Duloxetine hydrochloride
Brand name/Manufacturer	Wyeth	Eli Lilly
FDA approval date	1993	2004
Active Metabolite	O-Desmethylvenlafaxine	5-hydroxy-duloxetine 6-methoxy-duloxetine
Half-life	4 (11 for O-desmethylvenlafaxine)	12 hours (range 8 to 17 hours)
Time to steady-state	3 days	3 days
Bioavailability, %	45	50
Potential for interactions	Has one of the most favorable drug-interaction profiles4 Weak or negligible inhibitor of CYP isozymes (CYP2D6, CYP1A2, CYP2C19, and CYP3A4)	Moderate inhibitor of CYP2D6, has the potential to interact with other drugs that are also metabolized by this cytochrome P450 system
Generic avalability	Yes	No
FDA Pregnancy Category	C	C
Most common side effects	nausea headache somnolence dizziness insomnia nervousness dry mouth anorexia sweating abnormal ejaculation constipation impotence	nausea somnolence headache dry mouth dizziness insomnia fatigue constipation diarrhea decreased appetite vomiting erectile dysfunction
Mode of action	Serotonergic at lower doses, modest noradrenergic effects at higher doses (> 250 mg/day)	Strong, balanced inhibitor of both norepinephrine and serotonin reuptake

Antidepressants Comparison: Effexor versus Cymbalta

"

In a study by Bymaster and colleagues it was found that duloxetine inhibited binding to the human norephinepherine (NE) and serotonin (5-HT) transporters with K(i) values of 7.5 and 0.8 nM, respectively, and with a K(i) ratio of 9. Venlafaxine inhibited binding to the human NE and 5-HT transporters with K(i) values of 2480 and 82 nM, respectively, and with a K(i) ratio of 30. Duloxetine inhibited ex vivo binding to rat 5-HT transporters and NE transporters with ED(50) values of 0.03 and 0.7 mg/kg, respectively, whereas venlafaxine had ED(50) values of 2 and 54 mg/kg, respectively.

Thus, duloxetine more potently blocks serotonin and norephinepherine transporters in vitro and in vivo than venlafaxine,^[23] arguably making it the most potent of all commercially available SNRIs. Duloxetine and venlafaxine have not been measured against milnacipran."

Duloxetine