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 Effectively Treats Generalized Anxiety Disorder
From American Family Physician, 12/15/00 by Karl E. Miller

Generalized anxiety is a common disorder with an estimated lifetime prevalence of 5.1 percent. It usually begins in the early 20s and has a low rate of spontaneous remission. The popular view of this disorder is that it is mild, but studies have shown that it can cause substantial interference in the lives of affected patients. Many patients seek professional help that usually results in the use of medication to treat the symptoms. Many medications have been used to treat generalized anxiety disorder, but each has safety limitations or limited research indicating effectiveness. Venlafaxine affects the serotonergic and noradrenergic pathways and may have some anxiolytic properties. Rickels and colleagues studied the safety and efficacy of extended-release venlafaxine in the treatment of generalized anxiety disorder without concomitant major depressive disorder.

The study was a multicenter, randomized, placebo-controlled trial using outpatients with generalized anxiety disorder. To be included in the study, the patients had to score 18 or higher on the Hamilton Rating Scale for Anxiety and score 2 or more on its anxious mood and tension factors. Patients were excluded if they had a concomitant major depressive disorder within six months of the study or a current diagnosis based on the screening interview. Patients were randomly assigned to receive placebo or extended-release venlafaxine in a dosage of 75, 150 or 225 mg per day for up to eight weeks. Primary efficacy variables included total and psychic anxiety factor scores on the Hamilton anxiety scale, and severity and global improvement scores on the Clinical Global Impression scale at the end of the study. Safety evaluation was based on patients' reports of adverse events, routine physical examinations, laboratory evaluations and electrocardiography.

Patients who received extended-released venlafaxine scored better on all four of the primary measurements when compared with the placebo group. In addition, they scored better on the Clinical Global Impression scale than those who received placebo. Patients responded well to three doses of venlafaxine, with the 225-mg-per-day dosage providing the best response. The most common adverse events reported in the venlafaxine group included nausea, insomnia, dry mouth, somnolence, dizziness and asthenia. These symptoms tended to be mild, to occur early in the treatment course and to subside with continued treatment.

The authors conclude that extended-release venlafaxine is a safe and effective alternative for the treatment of generalized anxiety disorder in patients without concomitant major depressive disorder. All dosages of venlafaxine were effective, but 225 mg per day provided the best results. The majority of the side effects of the medication were mild and subsided with time.

COPYRIGHT 2000 American Academy of Family Physicians
COPYRIGHT 2001 Gale Group

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