Venlafaxine chemical structureAn Effexor XR 75mg Capsule
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Venlafaxine

Venlafaxine hydrochloride is a synthetic derivative of phenethylamine and a prescription antidepressant first introduced by Wyeth in 1993, and marketed under the trade names Effexor® for tablets and Effexor XR® for extended-release capsules. Efexor® / Efectin® and Efexor XR® / Efexor® Depot / Efectin ER® are alternate trade name spellings used in some countries. Since venlafaxine is under patent, under current United States law, a generic will not be available to U.S. citizens until 2008. The European patent on the drug will hold until 2017. more...

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Uses

Venlafaxine is used primarily for the treatment of depression, generalized anxiety disorder, and social anxiety disorder in adults. It is known as one of the most activating of the newer antidepressants. While this can be helpful to some, as many depressed patients report feeling exhausted and unmotivated, to others it poses the risk of increased anxiety and agitation.

Venlafaxine is an effective antidepressant for many persons; however, it seems to be especially effective for those with treatment-resistant depression. Some of these persons have taken two or more antidepressants prior to venlafaxine with no relief. It has also been found to reduce the severity of 'hot-flashes' in menopausal women. In addition, a September 2004 Consumer Reports study ranked venlafaxine as the most effective among six commonly prescribed antidepressants. (However, this should not be considered a definitive finding, and responses to psychiatric medications vary significantly from individual to individual.)

Off-label / Investigational Uses

Substantial weight loss in patients with major depression, generalized anxiety disorder, and social phobia has been noted, but the manufacturer does not recommend the use as anorectical drug either alone or in combination with phentermine or other amphetamine-like drugs.

Description of Compound

The chemical structure of venlafaxine is designated (R/S)-1- cyclohexanol hydrochloride or (±)-1- cyclohexanol hydrochloride and it has the empirical formula of C17H27NO2 · HCl. It is a white to off-white crystalline solid, distributed in pentagon-shaped peach-colored tablets of 25 mg, 37.5 mg, 50 mg, 75 mg, and 100 mg. There is also an extended-release version distributed in capsules of 37.5 mg (gray/peach), 75 mg (peach), and 150 mg (brownish red).

Mechanism of Action

Venlafaxine is a bicyclic antidepressant, and is usually categorized as a serotonin-norepinephrine reuptake inhibitor, but it has been referred to as a serotonin-norepinephrine-dopamine reuptake inhibitor. It works by blocking the transporter "reuptake" proteins for key neurotransmitters affecting mood, thereby leaving more active in the synapse. At low dosages, venlafaxine blocks serotonin reuptake alone, similarly to a selective serotonin reuptake inhibitor (SSRI). At medium dosages (about 225mg/day), venlafaxine blocks the reuptake of norepinephrine as well as serotonin. At dosages above 300mg/day, it blocks dopamine reuptake in addition to serotonin and norepinephrine.

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Venlafaxine XR matches paroxetine for panic disorder: equal efficacy, tolerability - Clinical Rounds
From OB/GYN News, 10/15/03 by Bruce Jancin

SAN FRANCISCO -- The serotonin-norepinephrine reuptake inhibitor venlafaxine is as effective as paroxetine in the treatment of panic disorder, Dr. Mark Pollack reported at the annual meeting of the American Psychiatric Association.

Venlafaxine extended-release (Effexor XR) achieves remission faster than paroxetine (Paxil), a selective serotonin reuptake inhibitor with a Food and Drug Administration-approved indication for treatment of panic disorder. But after 12 weeks of therapy, the proportion of patients who are panic-free is virtually identical with the two drugs. Side effect profiles are quite similar, too, with the exception of significantly more somnolence with paroxetine, added Dr. Pollack of Massachusetts General Hospital, Boston.

He reported on 634 patients with panic disorder who participated in a 12-week, multicenter, randomized, double-blind head-to-head comparison of venlafaxine XR at 75 mg/day, venlafaxine XR at 150 mg/day, paroxetine at 40 mg/day, or placebo. The trial was funded by Wyeth Research, which markets Effexor XR.

The remission rate in the venlafaxine group was significantly better than that of placebo-group patients by week 4. Paroxetine-treated patients were ahead in remission rates by week 6.

After 12 weeks, 54% of those on venlafaxine XR 75 mg/day were panic-free, as were 61% on venlafaxine XR 150 mg/day, 60% on paroxetine, and 34% on placebo. Rates of remission, defined as being panic-free and having a Clinical Global Impression-Improvement score of 1, were 45% and 47% on 75 and 150 mg/day of venlafaxine XR, 46% on paroxetine, and 27% on placebo.

COPYRIGHT 2003 International Medical News Group
COPYRIGHT 2003 Gale Group

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