Peringatan Keamanan

In a report that included 234 fluoxetine overdose cases, it was concluded that symptoms resulting from fluoxetine overdose were generally minor and short in duration.A181898 The most common overdose adverse effects included drowsiness, tremor, tachycardia, nausea and vomiting, and providing the patient with aggressive supportive care was the recommended intervention.A181892A181898

Despite this evidence, more severe adverse effects have been linked to fluoxetine ingestion although most of these reports involved co-ingestion with other substances or drugs as well as other factors.A181892 For example, there is a case report that details a patient who ingested 1400 mg of fluoxetine in a suicide attempt and as a result, experienced a generalized seizure three hours later.A181892 In a separate case, a 14 year old patient ingested 1.2 g of fluoxetine and subsequently experienced tonic/clonic seizures, symptoms consistent with serotonin syndrome, and rhabdomyolysis, although the patient did not experience sustained renal injury.A182216

Fluoxetine

DB00472

small molecule approved vet_approved

Deskripsi

Fluoxetine is a 2nd generation antidepressant categorized as a selective serotonin reuptake inhibitor (SSRI).A181673 It gained FDA approval in 1987 and although it was initially intended for the treatment of depression, today it is commonly prescribed to manage depression in addition to various other pathologies.L7721

Struktur Molekul 2D

Berat 309.3261
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of fluoxetine is significant with the elimination half-life of the parent drug averaging 1-3 days after acute administration, and 4-6 days after chronic administration.[L7664] Further, the elimination half life of it's active metabolite, norfluoxetine, ranges from 4-16 days after both acute and chronic administration.[L7664] The half-life of fluoxetine should be considered when switching patients from fluoxetine to another antidepressant since marked accumulation occurs after chronic use.[L7664] Fluoxetine's long half-life may even be beneficial when discontinuing the drug since the risk of withdrawal is minimized.[L7721]
Volume Distribusi The volume of distribution of fluoxetine and it's metabolite varies between 20 to 42 L/kg.[A182216]
Klirens (Clearance) The clearance value of fluoxetine in healthy patients is reported to be 9.6 ml/min/kg.[A185210]

Absorpsi

The oral bioavailability of fluoxetine is <90% as a result of hepatic first pass metabolism.L7721 In a bioequivalence study, the Cmax of fluoxetine 20 mg for the established reference formulation was 11.754 ng/mL while the Cmax for the proposed generic formulation was 11.786 ng/ml.A185285 Fluoxetine is very lipophilic and highly plasma protein bound, allowing the drug and it's active metabolite, norfluoxetine, to be distributed to the brain.L7721

Metabolisme

Fluoxetine is metabolized to norfluoxetine by CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5 upon ingestion.L7721A16881 Although all of the mentioned enzymes contribute to N-demethylation of fluoxetine, CYP2D6, CYP2C9 and CYP3A4 appear to be the major contributing enzymes for phase I metabolism.A16881 In addition, there is evidence to suggest that CYP2C19 and CYP3A4 mediate O-dealkylation of fluoxetine and norfluoxetine to produce para-trifluoromethylphenol which is subsequently metabolized to hippuric acid.A185246A185255 Both fluoxetine and norfluoxetine undergo glucuronidation to facilitate excretion.L7721 Notably, both the parent drug and active metabolite inhibit CYP2D6 isozymes, and as a result patients who are being treated with fluoxetine are susceptible to drug interactions.L7721L162

Rute Eliminasi

Fluoxetine is primarily eliminated in the urine.L8468

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food.

Interaksi Obat

1919 Data
Peginterferon alfa-2b The serum concentration of Fluoxetine can be decreased when it is combined with Peginterferon alfa-2b.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Fluoxetine.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Fluoxetine.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Fluoxetine.
Deferasirox The serum concentration of Fluoxetine can be increased when it is combined with Deferasirox.
Desmopressin The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Desmopressin.
Ioflupane I-123 Fluoxetine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Metyrosine The risk or severity of extrapyramidal symptoms can be increased when Metyrosine is combined with Fluoxetine.
Leflunomide The serum concentration of Fluoxetine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Fluoxetine can be decreased when it is combined with Teriflunomide.
Buprenorphine Fluoxetine 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 Fluoxetine.
Hydrocodone Fluoxetine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Fluoxetine can be increased when used in combination with Magnesium sulfate.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Fluoxetine.
Pramipexole Fluoxetine may increase the sedative activities of Pramipexole.
Suvorexant Fluoxetine 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 Fluoxetine.
Thalidomide Fluoxetine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Fluoxetine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dabrafenib The serum concentration of Fluoxetine can be decreased when it is combined with Dabrafenib.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Fluoxetine resulting in a loss in efficacy.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Fluoxetine.
Luliconazole The serum concentration of Fluoxetine can be increased when it is combined with Luliconazole.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Fluoxetine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Fluoxetine.
Phenytoin The risk or severity of Anticonvulsant Toxicity can be increased when Fluoxetine is combined with Phenytoin.
Fosphenytoin The risk or severity of Anticonvulsant Toxicity can be increased when Fluoxetine is combined with Fosphenytoin.
Haloperidol The metabolism of Haloperidol can be decreased when combined with Fluoxetine.
Mirabegron The serum concentration of Fluoxetine 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 Fluoxetine.
Abiraterone The serum concentration of Fluoxetine can be increased when it is combined with Abiraterone.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Fluoxetine is combined with Botulinum toxin type A.
Mirtazapine The serum concentration of Mirtazapine can be increased when it is combined with Fluoxetine.
Cyproterone acetate The metabolism of Fluoxetine can be increased when combined with Cyproterone acetate.
Iobenguane Fluoxetine may decrease effectiveness of Iobenguane as a diagnostic agent.
Methyclothiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Methyclothiazide.
Chlorthalidone The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Chlorthalidone.
Bendroflumethiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Bendroflumethiazide.
Metolazone The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Metolazone.
Benzthiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Benzthiazide.
Hydroflumethiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Hydroflumethiazide.
Chlorothiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Chlorothiazide.
Trichlormethiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Trichlormethiazide.
Polythiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Polythiazide.
Quinethazone The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Quinethazone.
Cyclopenthiazide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Cyclopenthiazide.
Epitizide The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Epitizide.
Ethanol Fluoxetine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Fluoxetine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Benzhydrocodone The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Fluoxetine.
Naloxegol The risk or severity of serotonin syndrome can be increased when Naloxegol is combined with Fluoxetine.
Mecamylamine The risk or severity of adverse effects can be increased when Fluoxetine is combined with Mecamylamine.
Tropicamide The risk or severity of adverse effects can be increased when Fluoxetine is combined with Tropicamide.
Cyclopentolate The risk or severity of adverse effects can be increased when Fluoxetine is combined with Cyclopentolate.
Pentolinium The risk or severity of adverse effects can be increased when Fluoxetine is combined with Pentolinium.
Trimethaphan The risk or severity of adverse effects can be increased when Fluoxetine is combined with Trimethaphan.
Fenoterol The risk or severity of adverse effects can be increased when Fluoxetine is combined with Fenoterol.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The risk or severity of adverse effects can be increased when Fluoxetine is combined with Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione.
Homatropine The risk or severity of adverse effects can be increased when Fluoxetine is combined with Homatropine.
Agmatine The risk or severity of adverse effects can be increased when Fluoxetine is combined with Agmatine.
Lumacaftor The serum concentration of Fluoxetine can be decreased when it is combined with Lumacaftor.
Dexpropranolol The serum concentration of Dexpropranolol can be increased when it is combined with Fluoxetine.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Fluoxetine.
Salmon calcitonin The therapeutic efficacy of Salmon calcitonin can be decreased when used in combination with Fluoxetine.
Thyrotropin alfa The therapeutic efficacy of Thyrotropin alfa can be decreased when used in combination with Fluoxetine.
Follitropin The therapeutic efficacy of Follitropin can be decreased when used in combination with Fluoxetine.
Liothyronine The therapeutic efficacy of Liothyronine can be decreased when used in combination with Fluoxetine.
Carbimazole The therapeutic efficacy of Carbimazole can be decreased when used in combination with Fluoxetine.
Propylthiouracil The therapeutic efficacy of Propylthiouracil can be decreased when used in combination with Fluoxetine.
3,5-Diiodotyrosine The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Fluoxetine.
Tiratricol The therapeutic efficacy of Tiratricol can be decreased when used in combination with Fluoxetine.
Parathyroid hormone The therapeutic efficacy of Parathyroid hormone can be decreased when used in combination with Fluoxetine.
Teriparatide The therapeutic efficacy of Teriparatide can be decreased when used in combination with Fluoxetine.
Dibromotyrosine The therapeutic efficacy of Dibromotyrosine can be decreased when used in combination with Fluoxetine.
Thyroid, porcine The therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Fluoxetine.
Potassium perchlorate The therapeutic efficacy of Potassium perchlorate can be decreased when used in combination with Fluoxetine.
Protirelin The therapeutic efficacy of Protirelin can be decreased when used in combination with Fluoxetine.
Methylthiouracil The therapeutic efficacy of Methylthiouracil can be decreased when used in combination with Fluoxetine.
Elcatonin The therapeutic efficacy of Elcatonin can be decreased when used in combination with Fluoxetine.
Benzylthiouracil The therapeutic efficacy of Benzylthiouracil can be decreased when used in combination with Fluoxetine.
Thyrotropin The therapeutic efficacy of Thyrotropin can be decreased when used in combination with Fluoxetine.
Potassium Iodide The therapeutic efficacy of Potassium Iodide can be decreased when used in combination with Fluoxetine.
Levothyroxine The therapeutic efficacy of Levothyroxine can be decreased when used in combination with Fluoxetine.
Liotrix The therapeutic efficacy of Liotrix can be decreased when used in combination with Fluoxetine.
3,5-diiodothyropropionic acid The therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Fluoxetine.
Icosapent The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Icosapent.
Ketorolac The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Ketorolac.
Tolmetin The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Tolmetin.
Fenoprofen The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Fenoprofen.
Sulindac The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Sulindac.
Sulfasalazine The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Sulfasalazine.
Carprofen The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Carprofen.
Diflunisal The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Diflunisal.
Meclofenamic acid The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Meclofenamic acid.
Oxaprozin The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Oxaprozin.
Balsalazide The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Balsalazide.
Magnesium salicylate The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Magnesium salicylate.
Salsalate The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Salsalate.
Choline magnesium trisalicylate The risk or severity of gastrointestinal bleeding can be increased when Fluoxetine is combined with Choline magnesium trisalicylate.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
5-hydroxytryptamine receptor 2C HTR2C
Neuronal acetylcholine receptor subunit alpha-2 CHRNA2
Neuronal acetylcholine receptor subunit alpha-3 CHRNA3
Neuronal acetylcholine receptor subunit beta-4 CHRNB4
Cyclin-dependent kinases regulatory subunit 1 CKS1B
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Synthesis reference: Eduard Schwartz, Joseph Kaspi, Zinovi Itov, Gidon Pilarski, "Production of fluoxetine and new intermediates." U.S. Patent US5225585, issued October, 1990.
Artikel (PubMed)
  • PMID: 7623609
    Wong DT, Bymaster FP, Engleman EA: Prozac (fluoxetine, Lilly 110140), the first selective serotonin uptake inhibitor and an antidepressant drug: twenty years since its first publication. Life Sci. 1995;57(5):411-41.
  • PMID: 3554156
    Sommi RW, Crismon ML, Bowden CL: Fluoxetine: a serotonin-specific, second-generation antidepressant. Pharmacotherapy. 1987 Jan-Feb;7(1):1-15.
  • PMID: 29083803
    Sohel AJ, Molla M: Fluoxetine .
  • PMID: 19561732
    Suchard JR: Fluoxetine overdose-induced seizure. West J Emerg Med. 2008 Aug;9(3):154-6.
  • PMID: 1586402
    Borys DJ, Setzer SC, Ling LJ, Reisdorf JJ, Day LC, Krenzelok EP: Acute fluoxetine overdose: a report of 234 cases. Am J Emerg Med. 1992 Mar;10(2):115-20.
  • PMID: 30301727
    Lee-Kelland R, Zehra S, Mappa P: Fluoxetine overdose in a teenager resulting in serotonin syndrome, seizure and delayed onset rhabdomyolysis. BMJ Case Rep. 2018 Oct 8;2018. pii: bcr-2018-225529. doi: 10.1136/bcr-2018-225529.
  • PMID: 3262026
    Schenker S, Bergstrom RF, Wolen RL, Lemberger L: Fluoxetine disposition and elimination in cirrhosis. Clin Pharmacol Ther. 1988 Sep;44(3):353-9. doi: 10.1038/clpt.1988.161.
  • PMID: 10997938
    Margolis JM, O'Donnell JP, Mankowski DC, Ekins S, Obach RS: (R)-, (S)-, and racemic fluoxetine N-demethylation by human cytochrome P450 enzymes. Drug Metab Dispos. 2000 Oct;28(10):1187-91.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 628 • International brands: 5
Produk
  • Accel-fluoxetine
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Accel-fluoxetine
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  • Ach-fluoxetine
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Ach-fluoxetine
    Capsule • 20 mg • Oral • Canada • Generic • Approved
  • Act Fluoxetine
    Capsule • 20 mg • Oral • Canada • Approved
  • Act Fluoxetine
    Capsule • 40 mg • Oral • Canada • Approved
  • Act Fluoxetine
    Capsule • 10 mg • Oral • Canada • Approved
  • Ag-fluoxetine
    Capsule • 10 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 628 produk.
International Brands
  • Adofen — Brainpharma
  • Animex-On — Laboratorios
  • Fluoxeren — Menarini
  • Fontex — Lilly
  • Ladose — Lilly

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