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Pharmacotherapeutic profile of venlafaxine

Published online by Cambridge University Press:  16 April 2020

S Preskorn
S Preskorn*
Affiliation:
University of Kansas School of Medicine and Psychiatric Research Institute, 1100 North St Francis, Suite 200, Wichita, Kansas67214-3199, USA
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Summary

When selecting an antidepressant, a number of factors must be considered. These considerations are summarized under the mnemonic STEPS: Safety, Tolerability, Efficacy, Payment (eg, cost-effectiveness), and Simplicity of use. Venlafaxine is the first of a new class of antidepressants that selectively blocks the serotonin and noradrenaline uptake pumps without blocking muscarinic, histaminergic and adrenergic receptors or inhibiting sodium fast channels. Because venlafaxine avoids these mechanisms of action, it has a wide therapeutic index, an improved tolerability profile and a reduced risk of causing pharmacodynamically mediated drug-drug interactions when compared to tricyclic antidepressants (TCAs). In contrast to some other new antidepressants, venlafaxine also avoids effects on cytochrome P450 which are likely to cause clinically meaningful, pharmacokinetically mediated drug-drug interactions. The effects on the uptake pumps of both serotonin and noradrenaline appear to be responsible for some of venlafaxine's unique features in terms of antidepressant efficacy, including its ascending antidepressant dose-response curve and its apparent rapid onset of antidepressant action at the upper end of its clinically relevant dosing range. Venlafaxine is effective in a broad spectrum of patients, including outpatients and inpatients, those with and without melancholia, patients with symptoms of anxiety or agitation or retardation and patients with first time or recurrent episodes of major depression. An important factor when selecting an antidepressant is the simplicity of the dosing regimen and the ability to rapidly and confidently achieve the optimal dose for the patient. In this regard, venlafaxine can be initiated at a clinically effective dose from the beginning. If the patient fails to respond to this dose, there is evidence that increased antidepressant efficacy can be achieved by increasing the dose rather than having to resort to an augmentation strategy or switch to another class of antidepressants. In the immediate release form, venlafaxine has proven antidepressant efficacy when using a twice-or three-times-a-day schedule. A sustained release formulation is expected to be marketed soon and will permit once-a-day-dosing.

Keywords

venlafaxineantidepressantsserotonin-noradrenaline uptake inhibitorsclinical pharmacology
Type
Research Article
Information
European Psychiatry , Volume 12 , Issue S4 , 1997 , pp. 285s - 294s
Copyright
Copyright © Elsevier, Paris 1997

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References

Altamura, AC, Montgomery, SA, Wernicke, JFThe evidence for 20 mg a day of fluoxetine as the optimal dose in the treatment of depression. Br J Psychiatry 153suppl 31988 109–112CrossRefGoogle Scholar
Baron, BM, Ogden, A-M, Siegel, BW, Stegeman, J, Ursillo, RC, Dudley, MWRapid down regulation of β-adrenoceptors by co-administration of desipramine and fluoxetine. Eur J Pharmacol 1988; 154: 125–134CrossRefGoogle ScholarPubMed
Beasley, CM Jr, Bosomworth, JC, Wernicke, JFFluoxetine: relationships among dose, response, adverse events, and plasma concentrations in the treatment of depression. Psychopharmacol Bull 26 1990 18–24Google ScholarPubMed
Bolden-Watson, C, Richelson, EBlockade by newly-developed antidepressants of biogenic amine uptake into rat brain synaptosomes. Life Sci 1993; 52: 1023–1029CrossRefGoogle ScholarPubMed
Burke, MJ, Silkey, B, Preskorn, SHPharmacoeconomic considerations when evaluating treatment options for major depressive disorder. J Clin Psychiatry 55 suppl A 1994 42–52Google ScholarPubMed
Clerc, GE, Ruimy, P, Verdeau-Paillés, JA double-blind comparison of venlafaxine and fluoxetine in patients hospitalized for major depression and melancholia. Int Clin Psychopharmacol 1994; 9: 139–143CrossRefGoogle ScholarPubMed
Cunningham, LA, Borison, RL, Carman, JSet al.A comparison of venlafaxine, trazodone, and placebo in major depression. J Clin Psychopharmacol 1994; 14: 99–106CrossRefGoogle ScholarPubMed
Cusack, B, Nelson, A, Richelson, EBinding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology 1994; 114: 559–565CrossRefGoogle ScholarPubMed
Dierick, M, Ravizza, L, Realini, R, Martin, AA double-blind comparison of venlafaxine and fluoxetine for treatment of major depression in outpatients. Prog Neuropsychopharmacol Biol Psychiatry 1996; 20: 57–71CrossRefGoogle ScholarPubMed
Dornseif, BE, Dunlop, SR, Potvin, JH, Wernicke, JFEffect of dose escalation after low-dose fluoxetine therapy. Psychopharmacol Bull 1989; 25: 71–79Google ScholarPubMed
Ereshefsky, L, Alfaro, CL, Lam, YWFTreating depression: Potential drug interactions. Psychiatric Annuals 1997; 17: 244–258CrossRefGoogle Scholar
Guelfi, JD, White, C, Hackett, Det al.Effectiveness of venlafaxine in patients hospitalized for major depression and melancholia. J Clin Psychiatry 1995; 56: 450–458Google ScholarPubMed
Moyer, JA, Muth, EA, Haskins, JTet al.In vivo antidepressant profiles of the novel bicyclic compounds Wy-45,030 and Wy-45,881 (abstract). Soc Neurosci 1984; 10: 261Google Scholar
Muth, EA, Haskins, JT, Moyer, JA, Husbands, GEMet al.Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative. Biochem Pharmacol 1986; 35: 4493–4497CrossRefGoogle ScholarPubMed
Muth, EA, Moyer, JA, Haskins, JTet al.Biochemical, neurophysiological, and behavioral effects of Wy-45,233 and other identified metabolites of the antidepressant venlafaxine. Drug Dev Res 1991; 23: 191–199CrossRefGoogle Scholar
Nelson, JC, Mazure, CM, Bowers, MB, Jatlow, PIA preliminary, open study of the combination of fluoxetine and desipramine for rapid treatment of major depression. Arch Gen Psychiatry 1991; 48: 303–307CrossRefGoogle ScholarPubMed
Otton, SV, Ball, SE, Cheung, SWet al.Venlafaxine oxidation in vitro is catalysed by CYP2D6. Br J Clin Pharmacol 1996; 41: 149–156CrossRefGoogle ScholarPubMed
Preskorn, SHTargeted pharmacotherapy in depression management: comparative pharmacokinetics of fluoxetine, paroxetine and sertraline. Int Clin Psychopharmacol 9 suppl 3 1994 13–19CrossRefGoogle ScholarPubMed
Preskorn, SHOutpatient Management of Depression 1994 Professional Communications Inc.Google Scholar
Preskorn, SHAntidepressant drug selection: criteria and options. J Clin Psychiatry 55 suppl A 1994 6–22Google ScholarPubMed
Preskorn, SHClinical Pharmacology of Selective Serotonin Reuptake Inhibitors 1996 Professional Communications Inc CaddoGoogle Scholar
Preskorn, SHClinically relevant pharmacology of selective serotonin reuptake inhibitors: An overview with emphasis on pharmacokinetics and effects on oxidative drug metabolism. Clin Pharmacokinet 32 1 1997 1–21CrossRefGoogle ScholarPubMed
Preskorn, SH, Fast, GATherapeutic drug monitoring for antidepressants: efficacy, safety, and cost effectiveness. J Clin Psychiatry 1991; 52: 23–33Google ScholarPubMed
Preskorn, SH, Janicak, PG, Davis, JM, Ayd, FJAdvances in the pharmacotherapy of depressive disorders In: Janicak, PG, Davis, JM, Preskorn, SH, Ayd, FJPrinciples and Practice of Psychopharmacotherapy 1995 Williams and Wilkins Caddo1–24Google Scholar
Rudolph, R, Entsuah, R, Derivan, AA low relapse rate confirms the long-term efficacy of venlafaxine in the treatment of major depression. Neuropsychopharmacology 1994; 10: 105Google Scholar
Rudolph, RL, Fabre, L, Feighner, J, Rickels, KA randomized, placebo-controlled, dose-response trial of venlafaxine hydrochloride in the treatment of major depression. J Clin Psychiatry 1997Google Scholar
Schweizer, E, Feighner, J, Mandos, LA, Rickels, KComparison of venlafaxine and imipramine in the acute treatment of major depression in outpatients. J Clin Psychiatry 1994; 55: 104–108Google ScholarPubMed
Shrivastava, RK, Cohn, C, Crowder, J, Davidson, Jet al.Long-term safety and clinical acceptability of venlafaxine and imipramine in outpatients with major depression. J Clin Psychopharmacol 1994; 14: 322–329CrossRefGoogle ScholarPubMed
Shad, MU, Carmichael, CA, Preskorn, SH, Horst, WEPrevalence of polypharmacy in different clinical settings and its relation to drug-drug interactions San Diego: Annual Meeting of the American Psychiatric Association 1997Google Scholar
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