venlafaxine

Venlafaxine is a selective serotonin and norepinephrine reuptake inhibitor (SNRI) for treating depression. Other drugs in this class include milnacipran (Savella), duloxetine (Cymbalta), and desvenlafaxine (Pristiq). Venlafaxine affects neurotransmitters, the chemicals that nerves within the brain make and release to communicate with one another. Neurotransmitters either travel across the space between nerves, attach to receptors on the surface of nearby nerves or attach to receptors on the surface of the nerves that produced them, to be taken up by the nerve and rereleased (a process referred to as re-uptake).

Many experts believe that an imbalance among neurotransmitters is the cause of depression as well as other psychiatric disorders. Serotonin and norepinephrine are two neurotransmitters released by nerves in the brain. Venlafaxine prevents the reuptake of serotonin and epinephrine by nerves after they have been released. Since uptake is an important mechanism for removing released neurotransmitters and terminating their actions on adjacent nerves, the reduced uptake caused by venlafaxine increases the effect of serotonin and norepinephrine in the brain. Venlafaxine is available in an extended-release formulation (Effexor XR).

The FDA approved venlafaxine in December 1993.

Effexor XR is used for the treatment of depression, depression with associated symptoms of anxiety, generalized anxiety disorder, and social anxiety disorder. Effexor XR is approved for the treatment of adults with panic disorder.

Venlafaxine, like most anti-depressants, can cause:

• nausea,
• headaches,
• anxiety,
• insomnia,
• drowsiness, and
• loss of appetite.

Other side effects that can occur are:

• dizziness,
• ejaculation disorder,
• sweating,
• dry mouth, and
• weight loss

Increased blood pressure can occur, and blood pressure should be monitored.

Seizures have been reported.

The FDA suggests if anti-depressants are discontinued abruptly, symptoms may occur such as dizziness, headache, nausea, changes in mood, or changes in the sense of smell, taste, etc. (Such symptoms even may occur when even a few doses of anti-depressant are missed.) Therefore, it is generally recommended that the dose of anti-depressant be reduced gradually when therapy is discontinued.

Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term studies in children, adolescents, and young adults with depression and other psychiatric disorders. Anyone considering the use of venlafaxine or any other antidepressant in a child or adolescent must balance this risk with the clinical need. Patients who are started on therapy should be closely observed for clinical worsening, suicidality, or unusual changes in behavior.

Venlafaxine should be taken with food at doses specifically directed by a physician. Individual doses vary significantly among individuals. The anti-depressant effects are not maximal for 1-2 weeks. If discontinued, the dose of venlafaxine should gradually be reduced under the direction of a physician. For patients with difficulty swallowing tablets or capsules, capsules of Effexor XR can be opened and the contents sprinkled on a spoonful of applesauce but removal from the capsule allows immediate release of the drug. Hence, it is no longer an extended-release drug.

The dose for treatment of depression using the immediate-release formulation is 75 to 375 mg daily divided into 2 or 3 doses and given every 8 or 12 hours. The extended-release dose is 37.5 mg to 225 mg once daily. Dosing usually begins with low initial concentrations and is adjusted as the treating doctor needs.

Generalized anxiety and panic disorder are treated with 37.5 mg to 225 mg once daily using the extended release formulation. Social anxiety is treated with 75 mg daily using the extended release formulation.

Venlafaxine should not be used in combination with a monoamine oxidase inhibitor (MAOI) such as phenelzine (Nardil), tranylcypromine (Parnate), isocarboxazid (Marplan), and selegiline (Eldepryl), or within 14 days of discontinuing the MAOI. At least 5 days should be allowed after stopping venlafaxine before starting an MAOI. Combinations of SNRIs and MAOIs may lead to serious, sometimes fatal, reactions including very high body temperature, muscle rigidity, rapid fluctuations of heart rate and blood pressure, extreme agitation progressing to delirium, and coma. Similar reactions may occur if venlafaxine is combined with antipsychotics, tricyclic antidepressants, or other drugs that affect serotonin in the brain. Examples include tryptophan, sumatriptan (Imitrex), lithium, linezolid (Zyvox), tramadol (Ultram), and St. John's wort.

Combining venlafaxine with aspirin, nonsteroidal anti-inflammatory drugs (NSAIDs), warfarin (Coumadin), or other drugs associated with bleeding may increase the risk of bleeding because venlafaxine is associated with bleeding.

Most medications affecting the brain such as venlafaxine have the potential to slow reflexes or impair judgment. Therefore, caution is advised especially early in the course of treatment.

Safety has not been established in children below the age of 18 years.

The effects of venlafaxine on the fetus during pregnancy are unknown.

It is not known if venlafaxine is secreted in breast milk, and therefore, if it may have an effect on nursing infants.

• Venafaxine is available as:
  • Tablets: 25, 37.5, 50, 75, and 100 mg.
  • Tablets (Extended Release): 37.5, 75, 150, 225 mg;
  • Capsules (Extended Release): 37.5, 75, and 150 mg.
• Store venafaxine in a dry place at 20 C to 25 C (68 F to 77 F).
• Venafaxine is available in generic form. You need a prescription to obtain this drug.