Peringatan Keamanan

Oral LD50 was 350 mg/kg in female rats and 700 mg/kg in male rats.L43025

There are reports of acute overdosage with venlafaxine either alone or in combination with other drugs including alcohol. Doses up to several-fold higher than the usual therapeutic dose have been ingested in these cases of acute overdosage. Somnolence is the most commonly reported symptom, along with other symptoms such as paresthesia of the extremities, moderate dizziness, altered consciousness, nausea, vomiting, numb hands and feet, hot-cold spells (which occur a few days after the overdose event), hypotension, convulsions, sinus and ventricular tachycardia, rhabdomyolysis, vertigo, liver necrosis, electrocardiogram changes (e.g., prolongation of QT interval, bundle branch block, QRS prolongation), serotonin syndrome, and death.L43030

There is no known antidote for venlafaxine overdose. Cases of overdose have been managed with or without symptomatic treatment, hospitalization, and activated charcoal.L43030

Retrospective studies suggest that the risk of fatal outcomes from venlafaxine overdosage is higher than that of SSRI antidepressants, but lower than that of tricyclic antidepressants.L43030

Venlafaxine

DB00285

small molecule approved

Deskripsi

Venlafaxine is an antidepressant and a serotonin and norepinephrine reuptake inhibitor (SNRI). Its active metabolite, desvenlafaxine, works by blocking the reuptake of serotonin and norepinephrine, which are key neurotransmitters in mood regulation. Venlafaxine is officially approved to treat major depressive disorder (MDD), generalized anxiety disorder (GAD), social anxiety disorder, and panic disorder in adults.L43030 The immediate formulation of the drug, marketed as Effexor, was first approved by the FDA in 1993 and the extended-release formulation, Effexor XR, was later introduced in 1997.A252065

Venlafaxine has been used as a first-line treatment for MDD, GAD, social anxiety disorder, and panic disorder in Canada for many years. It was also considered a second-line treatment for obsessive-compulsive disorder (OCD).A177226,A177235 Venlafaxine was also investigated in off-label uses for the prophylaxis of migraine headaches,A413,A177229 for reduction of vasomotor symptoms associated with menopause,A177238 and for the management of neuropathic pain (although there is only minimal evidence of efficacy for this condition).A177232

Struktur Molekul 2D

Berat 277.4018
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent elimination half-life is 5 ± 2 hours for venlafaxine and 11 ± 2 hours for ODV.[L43030]
Volume Distribusi The apparent volume of distribution at steady-state is 7.5 ± 3.7 L/kg for venlafaxine and 5.7 ± 1.8 L/kg for ODV.[L43030]
Klirens (Clearance) Mean ± SD plasma apparent clearance at steady-state is 1.3 ± 0.6 L/h/kg for venlafaxine and 0.4 ± 0.2 L/h/kg for ODV.[L43030]

Absorpsi

Venlafaxine is well absorbed after oral administration with an absolute bioavailability of approximately 45%. In mass balance studies, at least 92% of a single oral dose of venlafaxine was absorbed. After twice-daily oral administration of immediate-release formulation of 150 mg venlafaxine, Cmax was 150 ng/mL and Tmax was 5.5 hours. Cmax and Tmax of ODV were 260 ng/mL and nine hours, respectively. The extended-release formulation of venlafaxine has a slower rate of absorption, but the same extent of absorption as the immediate-release formulation. After once-daily administration of extended-release formulation of 75 mg venlafaxine, Cmax was 225 ng/mL and Tmax was two hours. Cmax and Tmax of ODV were 290 ng/mL and three hours, respectively.L43030 Food does not affect the bioavailability of venlafaxine or its active metabolite, O-desmethylvenlafaxine (ODV).L43030

Metabolisme

Following absorption, venlafaxine undergoes extensive presystemic metabolism in the liver. It primarily undergoes CYP2D6-mediated demethylation to form its active metabolite O-desmethylvenlafaxine (ODV).L43030 Venlafaxine can also undergo N-demethylation mediated by CYP2C9, and CYP2C19, and CYP3A4 to form N-desmethylvenlafaxine (NDV) but this is a minor metabolic pathway.A14753 ODV and NDV further metabolized by CYP2C19, CYP2D6 and/or CYP3A4 to form N,O-didesmethylvenlafaxine (NODV) A6998 and NODV can be further metabolized to form N, N, O-tridesmethylvenlafaxine, followed by a possible glucuronidation.A19479

Rute Eliminasi

Approximately 87% of a venlafaxine dose is recovered in the urine within 48 hours as unchanged venlafaxine (5%), unconjugated ODV (29%), conjugated ODV (26%), or other minor inactive metabolites (27%).L43030

Farmakogenomik

5 Varian
CYP2D6 (rs3892097)

Patients with this genotype have reduced metabolism of venlafaxine.

CYP2D6 (rs5030655)

Patients with this genotype have reduced metabolism of venlafaxine.

CYP2D6 (None)

Patients with this genotype have reduced metabolism of venlafaxine.

ABCB1 (rs2032583)

Patients with this genotype have an increased likelihood of remission when using venlafaxine to treat major depressive disorder

ABCB1 (rs2032583)

Patients with this genotype have increased risk of adverse events with venlafaxine

Interaksi Makanan

3 Data
  • 1. Avoid alcohol. The safety of using venlafaxine with other CNS-active drugs, including alcohol, has not been evaluated.
  • 2. Avoid St. John's Wort. Co-administration of St. John's Wort may lead to additive serotonergic activity and an increased risk of serotonin syndrome.
  • 3. Take with food. Co-administration with food helps to alleviate or mitigate gastrointestinal upset.

Interaksi Obat

1903 Data
Buprenorphine Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Hydrocodone Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Venlafaxine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine The risk or severity of serotonin syndrome can be increased when Methotrimeprazine is combined with Venlafaxine.
Metyrosine Venlafaxine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Orphenadrine Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Pramipexole Venlafaxine may increase the sedative activities of Pramipexole.
Ropinirole Venlafaxine may increase the sedative activities of Ropinirole.
Rotigotine The risk or severity of serotonin syndrome can be increased when Rotigotine is combined with Venlafaxine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Venlafaxine.
Sodium oxybate Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Thalidomide Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Brexpiprazole The risk or severity of serotonin syndrome can be increased when Brexpiprazole is combined with Venlafaxine.
Eliglustat The metabolism of Venlafaxine can be decreased when combined with Eliglustat.
Indinavir The serum concentration of Indinavir can be decreased when it is combined with Venlafaxine.
Ioflupane I-123 Venlafaxine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Linezolid Linezolid may increase the serotonergic activities of Venlafaxine.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Venlafaxine.
Propafenone The serum concentration of Venlafaxine can be increased when it is combined with Propafenone.
Trazodone Venlafaxine may increase the serotonergic activities of Trazodone.
Voriconazole The risk or severity of adverse effects can be increased when Voriconazole is combined with Venlafaxine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Venlafaxine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Venlafaxine.
Mirabegron The serum concentration of Venlafaxine can be increased when it is combined with Mirabegron.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Venlafaxine.
Acetylsalicylic acid Venlafaxine may increase the antiplatelet activities of Acetylsalicylic acid.
Mirtazapine Venlafaxine may increase the serotonergic activities of Mirtazapine.
Ethanol Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Zimelidine The risk or severity of serotonin syndrome can be increased when Zimelidine is combined with Venlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Venlafaxine is combined with Seproxetine.
Sibutramine The risk or severity of serotonin syndrome can be increased when Sibutramine is combined with Venlafaxine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Milnacipran is combined with Venlafaxine.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Venlafaxine.
Indalpine The risk or severity of serotonin syndrome can be increased when Indalpine is combined with Venlafaxine.
Alaproclate The risk or severity of serotonin syndrome can be increased when Alaproclate is combined with Venlafaxine.
Midodrine Venlafaxine may increase the tachycardic activities of Midodrine.
Bethanidine Venlafaxine may increase the tachycardic activities of Bethanidine.
Isoetharine Venlafaxine may increase the tachycardic activities of Isoetharine.
Norepinephrine Venlafaxine may increase the tachycardic activities of Norepinephrine.
Phenylephrine Venlafaxine may increase the tachycardic activities of Phenylephrine.
Phenylpropanolamine Venlafaxine may increase the tachycardic activities of Phenylpropanolamine.
Metaraminol Venlafaxine may increase the tachycardic activities of Metaraminol.
Guanabenz Venlafaxine may increase the tachycardic activities of Guanabenz.
Epinephrine Venlafaxine may increase the tachycardic activities of Epinephrine.
Methoxamine Venlafaxine may increase the tachycardic activities of Methoxamine.
Orciprenaline Venlafaxine may increase the tachycardic activities of Orciprenaline.
Dobutamine Venlafaxine may increase the tachycardic activities of Dobutamine.
Ritodrine Venlafaxine may increase the tachycardic activities of Ritodrine.
Terbutaline Venlafaxine may increase the tachycardic activities of Terbutaline.
Bitolterol Venlafaxine may increase the tachycardic activities of Bitolterol.
Oxymetazoline Venlafaxine may increase the tachycardic activities of Oxymetazoline.
Salmeterol Venlafaxine may increase the tachycardic activities of Salmeterol.
Albuterol Venlafaxine may increase the tachycardic activities of Salbutamol.
Isoprenaline Venlafaxine may increase the tachycardic activities of Isoprenaline.
Arbutamine Venlafaxine may increase the tachycardic activities of Arbutamine.
Fenoterol Venlafaxine may increase the tachycardic activities of Fenoterol.
Pirbuterol Venlafaxine may increase the tachycardic activities of Pirbuterol.
Ephedra sinica root Venlafaxine may increase the tachycardic activities of Ephedra sinica root.
Ephedrine Venlafaxine may increase the tachycardic activities of Ephedrine.
Procaterol Venlafaxine may increase the tachycardic activities of Procaterol.
Clenbuterol Venlafaxine may increase the tachycardic activities of Clenbuterol.
Bambuterol Venlafaxine may increase the tachycardic activities of Bambuterol.
4-Bromo-2,5-dimethoxyphenethylamine Venlafaxine may increase the tachycardic activities of 4-Bromo-2,5-dimethoxyphenethylamine.
Phendimetrazine Venlafaxine may increase the tachycardic activities of Phendimetrazine.
Indacaterol Venlafaxine may increase the tachycardic activities of Indacaterol.
Amibegron Venlafaxine may increase the tachycardic activities of Amibegron.
Nylidrin Venlafaxine may increase the tachycardic activities of Nylidrin.
Solabegron Venlafaxine may increase the tachycardic activities of Solabegron.
Droxidopa Venlafaxine may increase the tachycardic activities of Droxidopa.
Xylometazoline Venlafaxine may increase the tachycardic activities of Xylometazoline.
Isometheptene Venlafaxine may increase the tachycardic activities of Isometheptene.
Levonordefrin Venlafaxine may increase the tachycardic activities of Levonordefrin.
Naphazoline Venlafaxine may increase the tachycardic activities of Naphazoline.
Tetryzoline Venlafaxine may increase the tachycardic activities of Tetryzoline.
Protokylol Venlafaxine may increase the tachycardic activities of Protokylol.
Adrafinil Venlafaxine may increase the tachycardic activities of Adrafinil.
Isoxsuprine Venlafaxine may increase the tachycardic activities of Isoxsuprine.
Hexoprenaline Venlafaxine may increase the tachycardic activities of Hexoprenaline.
Etilefrine Venlafaxine may increase the tachycardic activities of Etilefrine.
Olodaterol Venlafaxine may increase the tachycardic activities of Olodaterol.
Vilanterol Venlafaxine may increase the tachycardic activities of Vilanterol.
Cirazoline Venlafaxine may increase the tachycardic activities of Cirazoline.
Synephrine Venlafaxine may increase the tachycardic activities of Synephrine.
Moxonidine Venlafaxine may increase the tachycardic activities of Moxonidine.
Doxofylline Venlafaxine may increase the tachycardic activities of Doxofylline.
Racepinephrine Venlafaxine may increase the tachycardic activities of Racepinephrine.
DL-Methylephedrine Venlafaxine may increase the tachycardic activities of DL-Methylephedrine.
Amitraz Venlafaxine may increase the tachycardic activities of Amitraz.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2
Sodium-dependent dopamine transporter SLC6A3

Referensi & Sumber

Synthesis reference: Thomas P. Jerussi, Chrisantha H. Senanayake, "Derivatives of (+)-venlafaxine and methods of preparing and using the same." U.S. Patent US6197828, issued June, 1994.
Artikel (PubMed)
  • PMID: 15705120
    Ozyalcin SN, Talu GK, Kiziltan E, Yucel B, Ertas M, Disci R: The efficacy and safety of venlafaxine in the prophylaxis of migraine. Headache. 2005 Feb;45(2):144-52.
  • PMID: 27486148
    Kennedy SH, Lam RW, McIntyre RS, Tourjman SV, Bhat V, Blier P, Hasnain M, Jollant F, Levitt AJ, MacQueen GM, McInerney SJ, McIntosh D, Milev RV, Muller DJ, Parikh SV, Pearson NL, Ravindran AV, Uher R: Canadian Network for Mood and Anxiety Treatments (CANMAT) 2016 Clinical Guidelines for the Management of Adults with Major Depressive Disorder: Section 3. Pharmacological Treatments. Can J Psychiatry. 2016 Sep;61(9):540-60. doi: 10.1177/0706743716659417. Epub 2016 Aug 2.
  • PMID: 22683887
    Pringsheim T, Davenport W, Mackie G, Worthington I, Aube M, Christie SN, Gladstone J, Becker WJ: Canadian Headache Society guideline for migraine prophylaxis. Can J Neurol Sci. 2012 Mar;39(2 Suppl 2):S1-59.
  • PMID: 26298465
    Gallagher HC, Gallagher RM, Butler M, Buggy DJ, Henman MC: Venlafaxine for neuropathic pain in adults. Cochrane Database Syst Rev. 2015 Aug 23;(8):CD011091. doi: 10.1002/14651858.CD011091.pub2.
  • PMID: 25081580
    Katzman MA, Bleau P, Blier P, Chokka P, Kjernisted K, Van Ameringen M, Antony MM, Bouchard S, Brunet A, Flament M, Grigoriadis S, Mendlowitz S, O'Connor K, Rabheru K, Richter PM, Robichaud M, Walker JR: Canadian clinical practice guidelines for the management of anxiety, posttraumatic stress and obsessive-compulsive disorders. BMC Psychiatry. 2014;14 Suppl 1:S1. doi: 10.1186/1471-244X-14-S1-S1. Epub 2014 Jul 2.
  • PMID: 24944075
    Handley AP, Williams M: The efficacy and tolerability of SSRI/SNRIs in the treatment of vasomotor symptoms in menopausal women: a systematic review. J Am Assoc Nurse Pract. 2015 Jan;27(1):54-61. doi: 10.1002/2327-6924.12137. Epub 2014 Jun 19.
  • PMID: 11750180
    Bymaster FP, Dreshfield-Ahmad LJ, Threlkeld PG, Shaw JL, Thompson L, Nelson DL, Hemrick-Luecke SK, Wong DT: Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80.
  • PMID: 10192828
    Fogelman SM, Schmider J, Venkatakrishnan K, von Moltke LL, Harmatz JS, Shader RI, Greenblatt DJ: O- and N-demethylation of venlafaxine in vitro by human liver microsomes and by microsomes from cDNA-transfected cells: effect of metabolic inhibitors and SSRI antidepressants. Neuropsychopharmacology. 1999 May;20(5):480-90.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 887 • International brands: 1
Produk
  • Act Venlafaxine XR
    Capsule, extended release • 37.5 mg • Oral • Canada • Approved
  • Act Venlafaxine XR
    Capsule, extended release • 75 mg • Oral • Canada • Approved
  • Act Venlafaxine XR
    Capsule, extended release • 150 mg • Oral • Canada • Approved
  • Apo-venlafaxine XR
    Capsule, extended release • 37.5 mg • Oral • Canada • Generic • Approved
  • Apo-venlafaxine XR
    Capsule, extended release • 75 mg • Oral • Canada • Generic • Approved
  • Apo-venlafaxine XR
    Capsule, extended release • 150 mg • Oral • Canada • Generic • Approved
  • Auro-venlafaxine XR
    Capsule, extended release • 75 mg • Oral • Canada • Generic • Approved
  • Auro-venlafaxine XR
    Capsule, extended release • 150 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 887 produk.
International Brands
  • Elafax

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