Peringatan Keamanan

The acute LD50 in mice and rats is 350 mg/kg.L7733

Overdose information

The lowest dose of paroxetine reported to lead to a fatal outcome is approximately 400 mg. The largest reported paroxetine overdose from which a patient has survived and recovered is a dose of 2000 mg. Common manifestations in a paroxetine overdose include fatigue, fever, insomnia hypertension, tachycardia, nausea, vomiting, somnolence, tremor, dizziness, agitation, confusion, anxious symptoms, headache, insomnia, hyperhidrosis, dilated pupils, seizures, paresthesia, serotonin syndrome, involuntary muscle contraction, and change in mental status. It should be noted that in some cases, patients may have consumed alcohol in addition to taking an overdose of paroxetine.L7706 Some of these symptoms may also be seen with clinical use. There is no specific antidote to an overdose of paroxetine.A181775

Paroxetine

DB00715

small molecule approved investigational

Deskripsi

Paroxetine is a selective serotonin reuptake inhibitor (SSRI) drug commonly known as Paxil. It has a variety of uses, including the treatment of anxiety disorders, major depression, posttraumatic stress disorder, and symptoms of menopause, among others.T653 It was approved by the FDA in the early 1990s and marketed by SmithKline Beecham.L7712,L7715 A unique feature of this drug is that it is highly potent and selective in its inhibition of serotonin reuptake and has little effect on other neurotransmitters.A31914 Because of its potent inhibition of serotonin reuptake, paroxetine is more likely to cause withdrawal effects upon cessation. Paroxetine is well tolerated in most patients with a similar adverse effect profile to other members of its drug class.A31914 The controlled release formulation was designed to decrease the likelihood of nausea that is sometimes associated with paroxetine.L7700,L7742

Struktur Molekul 2D

Berat 329.3654
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of paroxetine is about 21 hours.[L3358] In healthy young subjects, mean elimination half-life was found to be 17.3 hours.[L7706]
Volume Distribusi Paroxetine has a large volume of distribution and is found throughout the body, including in the central nervous system. Only 1% of the drug is found in the plasma.[L3358] Paroxetine is found in the breast milk at concentrations similar to the concentrations found in plasma.[A31914]
Klirens (Clearance) The apparent oral clearance of paroxetine is 167 L/h.[A181799] The clearance of paroxetine in patients with renal failure is significantly lower and dose adjustment may be required, despite the fact that it is mainly cleared by the liver. Dose adjustments may be required in hepatic impairment.[A181799,L3358,L7706]

Absorpsi

Paroxetine is readily absorbed from the gastrointestinal tract. Due to the first-pass metabolism, the bioavailability ranges from 30-60%. Cmax is attained 2 to 8 hours after an oral dose.A181760 Mean Tmax is 4.3 hours in healthy patients.L7706 The steady-state concentration of paroxetine is achieved within 7 to 14 days of oral therapy.A31914 In a pharmacokinetic study, AUC in healthy patients was 574 ng·h/mL and 1053 ng·h/mL in those with moderate renal impairment.L7706

Metabolisme

Paroxetine metabolism occurs in the liver and is largely mediated by cytochrome CYP2D6 with contributions from CYP3A4 and possibly other cytochrome enzymes.A415,T656 Genetic polymorphisms of the CYP2D6 enzyme may alter the pharmacokinetics of this drug. Poor metabolizers may demonstrate increased adverse effects while rapid metabolizers may experience decreased therapeutic effects.A31914,A181769,L7718 The majority of a paroxetine dose is oxidized to a catechol metabolite that is subsequently converted to both glucuronide and sulfate metabolites via methylation and conjugation. In rat synaptosomes, the glucuronide and sulfate conjugates have been shown to thousands of times less potent than paroxetine itself.L7706 The metabolites of paroxetine are considered inactive.A181883,A31914,T656

Rute Eliminasi

About 2/3 of a single paroxetine dose is found to be excreted in the urine and the remainder is found to be excreted in feces. Almost all of the dose is eliminated as metabolites; 3% is found to be excreted as unchanged paroxetine.A31914 About 64% of a 30 mg oral dose was found excreted in the urine, with 2% as the parent drug and 62% appearing as metabolites. Approximately 36% of the dose was found to be eliminated in the feces primarily as metabolites and less than 1% as the parent compound.L3358

Farmakogenomik

7 Varian
ABCB1 (rs2032583)

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

CYP2D6 (rs35742686)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of paroxetine.

CYP2D6 (rs3892097)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of paroxetine.

CYP2D6 (None)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of paroxetine.

CYP2D6 (rs5030655)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of paroxetine.

CYP2D6 (rs1135824)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of paroxetine.

CYP2D6 (rs28371733)

The presence of this polymorphism in CYP2D6 is associated with reduced or poor metabolism of paroxetine.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Food does not significantly affect absorption.

Interaksi Obat

1803 Data
Pravastatin The risk or severity of increased glucose can be increased when Pravastatin is combined with Paroxetine.
Cyproheptadine The therapeutic efficacy of Paroxetine can be decreased when used in combination with Cyproheptadine.
Deferasirox The serum concentration of Paroxetine can be increased when it is combined with Deferasirox.
Desmopressin The risk or severity of hyponatremia can be increased when Paroxetine is combined with Desmopressin.
Ioflupane I-123 Paroxetine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Paroxetine.
Metyrosine The risk or severity of extrapyramidal symptoms can be increased when Metyrosine is combined with Paroxetine.
Peginterferon alfa-2b The serum concentration of Paroxetine can be increased when it is combined with Peginterferon alfa-2b.
Pimozide The risk or severity of QTc prolongation can be increased when Paroxetine is combined with Pimozide.
Teriflunomide The serum concentration of Paroxetine can be decreased when it is combined with Teriflunomide.
Buprenorphine Paroxetine 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 Paroxetine.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Paroxetine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Hydrocodone Paroxetine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Magnesium sulfate The therapeutic efficacy of Paroxetine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Paroxetine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Orphenadrine Paroxetine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Paroxetine 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 Paroxetine.
Pramipexole Paroxetine may increase the sedative activities of Pramipexole.
Ropinirole Paroxetine may increase the sedative activities of Ropinirole.
Rotigotine Paroxetine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Paroxetine.
Sodium oxybate Paroxetine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Paroxetine 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 Paroxetine.
Thalidomide Paroxetine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Paroxetine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dabrafenib The serum concentration of Paroxetine can be decreased when it is combined with Dabrafenib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Paroxetine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Paroxetine.
Aclidinium The risk or severity of adverse effects can be increased when Paroxetine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Paroxetine.
Mirabegron The risk or severity of urinary retention can be increased when Paroxetine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Paroxetine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Paroxetine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Paroxetine.
Tiotropium The risk or severity of adverse effects can be increased when Paroxetine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Paroxetine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Paroxetine is combined with Umeclidinium.
Luliconazole The serum concentration of Paroxetine can be increased when it is combined with Luliconazole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Paroxetine.
Colchicine The metabolism of Colchicine can be decreased when combined with Paroxetine.
Fentanyl The risk or severity of serotonin syndrome can be increased when Fentanyl is combined with Paroxetine.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Paroxetine.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Paroxetine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Paroxetine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Paroxetine.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Paroxetine.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Paroxetine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Paroxetine.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Paroxetine.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Paroxetine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Paroxetine.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Paroxetine.
Vortioxetine The metabolism of Vortioxetine can be decreased when combined with Paroxetine.
Glycopyrronium The risk or severity of adverse effects can be increased when Paroxetine is combined with Glycopyrronium.
Tetrabenazine The metabolism of Tetrabenazine can be decreased when combined with Paroxetine.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Paroxetine.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Paroxetine.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Paroxetine.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Paroxetine.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Paroxetine.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Paroxetine.
Bupropion The risk or severity of adverse effects can be increased when Bupropion is combined with Paroxetine.
Darunavir The serum concentration of Paroxetine can be decreased when it is combined with Darunavir.
Amprenavir The serum concentration of Paroxetine can be decreased when it is combined with Amprenavir.
Fosamprenavir The serum concentration of Paroxetine can be decreased when it is combined with Fosamprenavir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Paroxetine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Paroxetine.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Paroxetine.
Abiraterone The serum concentration of Paroxetine can be increased when it is combined with Abiraterone.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Paroxetine is combined with Botulinum toxin type A.
Glucagon Paroxetine may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Paroxetine may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Paroxetine is combined with Botulinum toxin type B.
Mirtazapine Paroxetine may increase the serotonergic activities of Mirtazapine.
Eluxadoline The risk or severity of constipation can be increased when Paroxetine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Paroxetine is combined with Ramosetron.
Butorphanol The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Paroxetine.
Pentazocine The risk or severity of serotonin syndrome can be increased when Pentazocine is combined with Paroxetine.
Sufentanil The risk or severity of serotonin syndrome can be increased when Sufentanil is combined with Paroxetine.
Nalbuphine The risk or severity of serotonin syndrome can be increased when Nalbuphine is combined with Paroxetine.
Levorphanol The risk or severity of serotonin syndrome can be increased when Levorphanol is combined with Paroxetine.
Remifentanil The risk or severity of serotonin syndrome can be increased when Remifentanil is combined with Paroxetine.
Diphenoxylate The risk or severity of serotonin syndrome can be increased when Diphenoxylate is combined with Paroxetine.
Dezocine The risk or severity of serotonin syndrome can be increased when Dezocine is combined with Paroxetine.
Methadyl acetate The risk or severity of serotonin syndrome can be increased when Methadyl acetate is combined with Paroxetine.
Dihydroetorphine The risk or severity of serotonin syndrome can be increased when Dihydroetorphine is combined with Paroxetine.
Diamorphine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Paroxetine.
Etorphine The risk or severity of serotonin syndrome can be increased when Etorphine is combined with Paroxetine.
Dextromoramide The risk or severity of serotonin syndrome can be increased when Dextromoramide is combined with Paroxetine.
Desomorphine The risk or severity of serotonin syndrome can be increased when Desomorphine is combined with Paroxetine.
Carfentanil The risk or severity of serotonin syndrome can be increased when Carfentanil is combined with Paroxetine.
Alphacetylmethadol The risk or severity of serotonin syndrome can be increased when Alphacetylmethadol is combined with Paroxetine.
Dihydromorphine The risk or severity of serotonin syndrome can be increased when Dihydromorphine is combined with Paroxetine.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2
5-hydroxytryptamine receptor 2A HTR2A
Alpha-1 adrenergic receptors ADRA1A
Alpha-2 adrenergic receptors ADRA2A
Beta adrenergic receptor ADRB1
D(2) dopamine receptor DRD2
Histamine H1 receptor HRH1
Serotonin Receptors HTR1A
Muscarinic acetylcholine receptor CHRM1
5-hydroxytryptamine receptor 2B HTR2B
D(1) dopamine receptor DRD1

Referensi & Sumber

Synthesis reference: Charles M. Zepp, Yun Gao, Donald L. Heefner, "Method of preparing optically pure precursors of paroxetine." U.S. Patent US5258517, issued November 1993.
Artikel (PubMed)
  • PMID: 16272179
    Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU: Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology. J Psychopharmacol. 2005 Nov;19(6):567-96.
  • PMID: 10627793
    Baldwin D, Bobes J, Stein DJ, Scharwachter I, Faure M: Paroxetine in social phobia/social anxiety disorder. Randomised, double-blind, placebo-controlled study. Paroxetine Study Group. Br J Psychiatry. 1999 Aug;175:120-6.
  • PMID: 8834412
    Yonkers KA, Gullion C, Williams A, Novak K, Rush AJ: Paroxetine as a treatment for premenstrual dysphoric disorder. J Clin Psychopharmacol. 1996 Feb;16(1):3-8.
  • PMID: 9690692
    Waldinger MD, Hengeveld MW, Zwinderman AH, Olivier B: Effect of SSRI antidepressants on ejaculation: a double-blind, randomized, placebo-controlled study with fluoxetine, fluvoxamine, paroxetine, and sertraline. J Clin Psychopharmacol. 1998 Aug;18(4):274-81.
  • PMID: 30606186
    Zhang D, Cheng Y, Wu K, Ma Q, Jiang J, Yan Z: Paroxetine in the treatment of premature ejaculation: a systematic review and meta-analysis. BMC Urol. 2019 Jan 3;19(1):2. doi: 10.1186/s12894-018-0431-7.
  • PMID: 27738376
    Nevels RM, Gontkovsky ST, Williams BE: Paroxetine-The Antidepressant from Hell? Probably Not, But Caution Required. Psychopharmacol Bull. 2016 Mar 1;46(1):77-104.
  • PMID: 7959522
    Hiemke C: Paroxetine: pharmacokinetics and pharmacodynamics. Fortschr Neurol Psychiatr. 1994 Sep;62 Suppl 1:2-8.
  • PMID: 22435778
    van Zeeland YR, Schoemaker NJ, Haritova A, Smit JW, van Maarseveen EM, Lumeij JT, Fink-Gremmels J: Pharmacokinetics of paroxetine, a selective serotonin reuptake inhibitor, in Grey parrots (Psittacus erithacus erithacus): influence of pharmaceutical formulation and length of dosing. J Vet Pharmacol Ther. 2013 Feb;36(1):51-8. doi: 10.1111/j.1365-2885.2012.01391.x. Epub 2012 Mar 21.
Menampilkan 8 dari 25 artikel.
Textbook
  • Prabina Shrestha; Sara Abdijadid (2018). Paroxetine. NIH StatPearls.
  • Siu Wa Tang and Daiga Helmeste (2008). Expert opinion on pharmacotherapeutics; Paroxetine. Taylor and Francis online.

Contoh Produk & Brand

Produk: 551 • International brands: 5
Produk
  • Act Paroxetine
    Tablet • 10 mg • Oral • Canada • Approved
  • Act Paroxetine
    Tablet • 20 mg • Oral • Canada • Approved
  • Act Paroxetine
    Tablet • 30 mg • Oral • Canada • Approved
  • Ag-paroxetine
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ag-paroxetine
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Ag-paroxetine
    Tablet • 30 mg • Oral • Canada • Generic • Approved
  • Ag-paroxetine Tablets
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ag-paroxetine Tablets
    Tablet • 20 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 551 produk.
International Brands
  • Aropax
  • PAXILCR
  • Sereupin
  • Seroxat
  • Seroxat CR

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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