Venlafaxine. Pharmacology and therapeutic potential in the treatment of depression

Venlafaxine is the first available antidepressant of the structurally novel SNRI (serotonin noradrenaline‐reuptake inhibitor) class of drugs. It resembles the tricyclics in its ability to inhibit presynaptic reuptake of both serotonin and noradrenaline to a clinically significant degree. However, it does not cause appreciable effects at other receptor sites, including cholinergic, adrenergic and histaminergic, which are responsible for most of the unwanted side effects and toxicity associated with antidepressant treatment. It has the unusual ability to reduce β‐noradrenergic responsiveness after a single dose, which has led to the suggestion that it may have an earlier onset of therapeutic effect than traditional antidepressants. Clinical trials provide evidence that venlafaxine is of comparable efficacy to reference antidepressants, but may have a faster onset of antidepressant effect when given in high dosage. © 1998 John Wiley & Sons, Ltd.

[1]  J. Samuélian,et al.  A randomized, double-blind, parallel-group comparison of venlafaxine and clomipramine in outpatients with major depression , 1998, Journal of psychopharmacology.

[2]  H. Wetzel,et al.  A randomized, double-blind comparison of a rapidly escalating dose of venlafaxine and imipramine in inpatients with major depression and melancholia. , 1996, Journal of psychiatric research.

[3]  L. Ereshefsky Drug-Drug Interactions Involving Antidepressants: Focus on Venlafaxine , 1996, Journal of Clinical Psychopharmacology.

[4]  E. Sellers,et al.  Venlafaxine oxidation in vitro is catalysed by CYP2D6. , 1996, British journal of clinical pharmacology.

[5]  J. Scatina,et al.  Venlafaxine (VF): Effects on CYP2D6 dependent imipramine (IMP) and desipramine (DMP) 2‐hydroxylation; Comparative studies with fluoxetine (FLU) and effects on CYP1A2, CYP3A4 and CYP2C9 , 1996 .

[6]  T. Walle,et al.  Improved bacterial expression of the human P form phenolsulfotransferase (PST): applications to drug metabolism , 1996, Drug metabolism and disposition: the biological fate of chemicals.

[7]  Alain Martin,et al.  A double-blind comparison of venlafaxine and fluoxetine for treatment of major depression in outpatients , 1996, Progress in Neuro-Psychopharmacology and Biological Psychiatry.

[8]  J. Guelfi,et al.  Effectiveness of venlafaxine in patients hospitalized for major depression and melancholia. , 1995, The Journal of clinical psychiatry.

[9]  P. Sokoloff,et al.  The D3 receptor and its relevance in psychiatry , 1995, International Clinical Psychopharmacology.

[10]  T. Nicholas,et al.  P-2-99 A randomized double-blind comparison of venlafaxine, imipramine and placebo in general practice patients with mild moderate depression , 1995, European Neuropsychopharmacology.

[11]  S. Tamin,et al.  P-2-106 Evaluation of the potential pharmacokinetic interaction of venlafaxine and carbamazepine , 1995, European Neuropsychopharmacology.

[12]  A. Farah Combination ECT and Antidepressant Therapy. , 1995, The American journal of geriatric psychiatry : official journal of the American Association for Geriatric Psychiatry.

[13]  S. Sonne,et al.  Venlafaxine: A Structurally Unique and Novel Antidepressant , 1995, The Annals of pharmacotherapy.

[14]  S. Troy,et al.  The Pharmacokinetics of Venlafaxine When Given in a Twice‐Daily Regimen , 1995, Journal of clinical pharmacology.

[15]  P. Danjou,et al.  Safety and tolerance profile of venlafaxine , 1995, International clinical psychopharmacology.

[16]  J. Feighner,et al.  Venlafaxine for treatment-resistant unipolar depression. , 1994, Journal of clinical psychopharmacology.

[17]  S. Roose,et al.  Comparative efficacy of selective serotonin reuptake inhibitors and tricyclics in the treatment of melancholia. , 1994, The American journal of psychiatry.

[18]  J. Feighner,et al.  Long-term safety and clinical acceptability of venlafaxine and imipramine in outpatients with major depression. , 1994, Journal of clinical psychopharmacology.

[19]  J. Feighner,et al.  Long-Term Safety and Clinical Acceptability of: Venlafaxine and Imipramine in Outpatients , 1994 .

[20]  G. Clerc,et al.  A double‐blind comparison of venlafaxine and fluoxetine in patients hospitalized for major depression and melancholia , 1994 .

[21]  R. W. Schultz,et al.  The effect of renal disease on the disposition of venlafaxine , 1994, Clinical pharmacology and therapeutics.

[22]  I. Anderson,et al.  The efficacy of selective serotonin re-uptake inhibitors in depression: a meta-analysis of studies against tricyclic antidepressants , 1994, Journal of psychopharmacology.

[23]  J. Feighner,et al.  Comparison of venlafaxine and imipramine in the acute treatment of major depression in outpatients. , 1994, The Journal of clinical psychiatry.

[24]  D. Kupfer,et al.  Early response patterns associated with successful clomipramine treatment. , 1993, Journal of clinical psychopharmacology.

[25]  M D Devous,et al.  Comparison of SPECT applications in neurology and psychiatry. , 1992, The Journal of clinical psychiatry.

[26]  G. Tucker,et al.  The effect of selective serotonin re-uptake inhibitors on cytochrome P4502D6 (CYP2D6) activity in human liver microsomes. , 1992, British journal of clinical pharmacology.

[27]  Karen J. Klamerus,et al.  Introduction of a Composite Parameter to the Pharmacokinetics of Venlafaxine and its Active O‐Desmethyl Metabolite , 1992, Journal of clinical pharmacology.

[28]  H. Semlitsch,et al.  PHARMACODYNAMICS OF VENLAFAXINE EVALUATED BY EEG BRAIN MAPPING, PSYCHOMETRY AND PSYCHOPHYSIOLOGY. , 1992, British journal of clinical pharmacology.

[29]  D E Parker,et al.  Human Vestibular Function and Weightlessness , 1991, Journal of clinical pharmacology.

[30]  C. Clary,et al.  Placebo‐Controlled Trial of Venlafaxine for the Treatment of Major Depression , 1991, Journal of clinical psychopharmacology.

[31]  N. Bowery,et al.  Effect of paroxetine, a selective 5-hydroxytryptamine uptake inhibitor, on β-adrenoceptors in rat brain: Autoradiographic and functional studies , 1991, Neuropharmacology.

[32]  J. Westermeyer Fluoxetine‐Induced Tricyclic Toxicity: Extent and Duration , 1991, Journal of clinical pharmacology.

[33]  C. Mazure,et al.  A preliminary, open study of the combination of fluoxetine and desipramine for rapid treatment of major depression. , 1991, Archives of general psychiatry.

[34]  M. James,et al.  2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity. , 1990, Journal of medicinal chemistry.

[35]  J. Davidson,et al.  Seizures and bupropion: a review. , 1989, The Journal of clinical psychiatry.

[36]  J. Stegeman,et al.  Rapid down regulation of beta-adrenoceptors by co-administration of desipramine and fluoxetine. , 1988, European journal of pharmacology.

[37]  James H. Brown,et al.  The Antidepressant Effect of β-Adrenoreceptor Subsensitivity: A Brief Review and Clinical Implications* , 1987 .

[38]  J. Haskins,et al.  Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative. , 1986, Biochemical pharmacology.

[39]  J. Haskins,et al.  DMI, Wy-45,030, Wy-45,881 and ciramadol inhibit locus coeruleus neuronal activity. , 1985, European journal of pharmacology.

[40]  A. Janowsky,et al.  Role of serotonergic input in the regulation of the beta-adrenergic receptor-coupled adenylate cyclase system. , 1982, Science.

[41]  M. Barbaccia,et al.  Down-regulation of β-adrenergic receptors following repeated injections of desmethylimipramine: Permissive role of serotonergic axons , 1982, Neuropharmacology.

[42]  M. Dubocovich,et al.  High-affinity [3H]imipramine binding in rat hypothalamus: association with uptake of serotonin but not of norepinephrine. , 1980, Science.

[43]  M. Briley,et al.  Specific tricyclic antidepressant binding sites in rat brain characterised by high-affinity 3H-imipramine binding. , 1980, European journal of pharmacology.

[44]  J. Vetulani,et al.  Mode of action of antidepressant drugs. , 1978, Biochemical pharmacology.

[45]  J. Vetulani,et al.  Action of various antidepressant treatments reduces reactivity of noradrenergic cyclic AMP-generating system in limbic forebrain , 1975, Nature.

[46]  C. Hiemke,et al.  Pharmacokinetics of selective serotonin reuptake inhibitors. , 2000, Pharmacology & therapeutics.

[47]  J. Amchin,et al.  Effect of venlafaxine on the pharmacokinetics of alprazolam. , 1998, Psychopharmacology bulletin.

[48]  J. Mendels,et al.  Efficacy and safety of b.i.d. doses of venlafaxine in a dose-response study. , 1993, Psychopharmacology bulletin.

[49]  S. R. Howell,et al.  Metabolic disposition of 14C-venlafaxine in mouse, rat, dog, rhesus monkey and man. , 1993, Xenobiotica; the fate of foreign compounds in biological systems.

[50]  H. Semlitsch,et al.  Acute effects of the novel antidepressant venlafaxine on cognitive event‐related potentials (P300), eye blink rate and mood in young healthy subjects , 1993, International clinical psychopharmacology.

[51]  E. Richelson,et al.  Blockade by newly-developed antidepressants of biogenic amine uptake into rat brain synaptosomes. , 1993, Life sciences.

[52]  I. Lucki,et al.  VENLAFAXINE PHARMACOKINETICS AND PHARMACODYNAMICS , 1992 .

[53]  C. P. Wang,et al.  The disposition of venlafaxine enantiomers in dogs, rats, and humans receiving venlafaxine. , 1992, Chirality.

[54]  A. Fletcher,et al.  THE PROFILE OF VENLAFAXINE, A NOVEL ANTIDEPRESSANT AGENT, IN BEHAVIOURAL ANTIDEPRESSANT DRUG MODELS. , 1992 .

[55]  A. Fletcher,et al.  VENLAFAXINE EXHIBITS AN ANTIDEPRESSANT‐LIKE PROFILE OF ACTIVITY ON THE SOCIAL AND AGONISTIC BEHAVIOUR OF RATS. , 1992 .

[56]  J. Haskins,et al.  Biochemical, neurophysiological, and behavioral effects of Wy‐45,233 and other identified metabolites of the antidepressant venlafaxine , 1991 .

[57]  ArifUllah Khan,et al.  Venlafaxine in depressed outpatients. , 1991, Psychopharmacology bulletin.

[58]  L. Fabre,et al.  An ascending single-dose tolerance study of WY-45,030, a bicyclic antidepressant, in healthy men , 1987 .

[59]  R. Lydiard,et al.  Speed of onset of action of the newer antidepressants. , 1984, Psychopharmacology bulletin.