drugSideffecT

A drug used to treat hypertension.
We're studying to review this drug, giving general informations about its pharmacology.
We will point our attention on Losartan pharmacodynamics.

It is one of the most selling drug.

Drug Brand: Effexor.
Other brand names: Effexor, Effexor XR, Elafax.
Active principle: Venlafaxine.
Active metabolite: O-desmethylvenlafaxine (ODV).
All trademarks are property of Wyeth.
Drug type: Small Molecule, antidepressant, serotonin uptake inhibitors.
Chemical formula: C17H27NO2.
Systematic IUPAC name: 1-[2-dimethylamino-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol
Drug Bank link: APRD00125
Brand Mixture: Fluticasone Propionate + Venlafaxine Xinafoate.
Disease: anxiety disorders, clinical depression.
Molecular target: 5-hydroxytryptamine 1A receptor, 5-hydroxytryptamine 2A receptor, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, 5-hydroxytryptamine 1B receptor.


GENERAL DESCRIPTION
Venlafaxine, by Wyeth, was released as Effexor in 1993.

It is ised to treat clinical depression and Effexor belongs to the class of Serotonin Uptake Inhibitors.

SIDE EFFECTS OF VENLAFAXINE

Toxicity is reported with typical symptoms of CNS depression, serotonin toxicity, or cardiac conduction disorders.
Venlafaxine's toxicity appears to be higher than other SSRIs, with a fatal toxic dose closer to that of the tricyclic antidepressants than the SSRIs.
Doses of 900 mg or more are likely to cause moderate toxicity.
Deaths have been reported following large doses. [drugBank]

MAIN INTERACTION WITH OTHER DRUGS:
5-HTP, 5-hydroxytryptophan, Actiq, Acutrim 16 Hour, Acutrim II, Maximum Strength, Acutrim Late Day, Adapin, Adipex-P, Adipost, Alfenta, alfentanil, almotriptan, Amerge, amitriptyline, amoxapine, amphetamine, Anafranil, Anorex-SR, Aplenzin, Appecon, Asendin, Atapryl, Aventyl HCl, Axert, Azilect, Babee Cof, Balminil DM, Balminil DM Pour Enfants, Balminil DM Sans Sucrose, Benadryl for the Family Dry Forte, Benylin.

OTHER INTERACTION WITH OTHER DRUGS:
12 Hour Nasal, 12 Hour Nasal Decongestant, 4-Way, 4-Way Menthol, 40 Winks, Abbokinase, Abbokinase Open-Cath, abciximab, Abilify, Abilify Discmelt, Accuneb, Accupril, acebutolol, Aceon, acetaZOLAMIDE, acetaZOLAMIDE extended release, acetylcarbromal, Acetylsalicylic Acid, Acova, Actibine, Activase, Actron, Acuprin 81, Adalat, Adalat CC, Adgan, Adrenalin, AdreView, Advil, Advil Childrens.

PHARMACOLOGY OF VENLAFAXINE
Venlafaxine is a serotonin uptake inhibitor.
Like the other SSRIs it acts stopping the uptake of serotonin at the level o CNS. It is used to treat melancholia, generalized anxiety disorder (GAD), panic disorder, post-traumatic stress disorder, and hot flashes in breast cancer survivors also.

PHARMACODYNAMICS OF VENLAFAXINE
In the absence of a simple mechanistic theory to account for antidepressant action, it is useful to look for pharmacological effects that the various drugs have in common, concentrating more on the slow adaptive changes that follow a similar time course to the therapeutic effect.
This approach has led to the discovery that certain monoamine (MAO) receptors, in particular beta1 and alfa2-adrenoceptors, are consistently down-regulated following chronic antidepressant treatment. This can be demonstrated in experimental animals as a reduction in the number of binding sites, as well as by a reduction in the functional response to agonists (e.g. stimulation of cAMP formation by beta-adrenoceptor agonists).
Receptor down-regulation probably also occurs in humans, because endocrine responses to clonidine, an alfa2-adrenoceptor agonist, are reduced by long-term antidepressant treatment. Other receptors have also been studied; beta1-adrenoceptors are not consistently affected, but 5-HT2-receptors are also down-regulated.

The pharmacologic effects of this antidepressant (venlafaxine) drug, are in attributable to its active metabolite: O-desmethylvenlafaxine (ODV).
It inhibites the re-uptake process of serotonin and noradrenaline.


FOR DRUG SPECIALISTS:
Download the file containing the Venlafaxine 3D structure and the Effexor FDA label:
"Venlafaxine 3D structure"
"Effexor FDA label"