Peringatan Keamanan

The oral LD50 if quetiapine in rats is 2000 mg/kg.L8594

Overdose information

Some signs and symptoms of a quetiapine overdose include sedation, drowsiness, tachycardia, and hypotension. Clinical trials demonstrate that overdoses of up to 30 grams of quetiapine did not result in death. A lethal outcome was reported in a clinical trial after an overdose of 13.6 grams of quetiapine. In the case of an acute overdose, ensure to maintain an airway and provide adequate ventilation and oxygenation. Gastric lavage following intubation (if necessary) along with activated charcoal and a laxative may be considered. The possibility of obtundation, seizure or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. Cardiac monitoring should also take place.L8546

A note on QT-interval prolongation in an overdose

Postmarketing reports reveal increases in the cardiac QT interval in cases of quetiapine overdose, concomitant illness, and in those taking drugs that increase QT interval or affect electrolyte levels.L8546 Note that disopyramide, procainamide, and quinidine may exert additive QT-prolonging effects when administered in patients who have overdosed with quetiapine, and should be avoided.A185834,A185837,L8546

Quetiapine

DB01224

small molecule approved

Deskripsi

Initially approved by the FDA in 1997, quetiapine is a second-generation atypical antipsychotic used in schizophrenia, major depression, and bipolar disorder.L8546 Quetiapine demonstrates a high level of therapeutic efficacy and low risk of adverse effects during long-term treatment. It is well-tolerated and a suitable option for some patients with high sensitivity to other drugs, such as clozapine and olanzapine.A2189

Struktur Molekul 2D

Berat 383.507
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average terminal half-life of quetiapine is about 6-7 hours.[A185441,L8546]
Volume Distribusi Quetiapine distributes throughout body tissues. The apparent volume of distribution of this drug is about 10±4 L/kg.[L8546]
Klirens (Clearance) The clearance of quetiapine healthy volunteers in the fasted state during a clinical study was 101.04±39.11 L/h.[A185846] Elderly patients may require lower doses of quetiapine, as clearance in these patients may be reduced by up to 50%.[L8546] Those with liver dysfunction may also require lower doses.[A185756]

Absorpsi

Quetiapine is rapidly and well absorbed after administration of an oral dose.L50828 Steady-state is achieved within 48 hours A185840 and peak plasma concentrations are achieved within 1.5 hours.L50828 The steady-state Cmax of quetiapine in Han Chinese patients with schizophrenia after a 300 mg oral dose of the extended released formulation was approximately 467 ng/mL and the AUC at steady-state was 5094 ng·h/mL.A185858 While the absolute bioavailability has not been fully elucidated and is reported to be low,A14994 the tablet formulation is 100% bioavailable relative to solution.L50828 Absorption of quetiapine is affected by food, with Cmax increased by 25% and AUC increased by 15%.L50828

Metabolisme

The metabolism of quetiapine occurs mainly in the liver. Sulfoxidation and oxidation are the main metabolic pathways of this drug. According to in vitro studies, cytochrome P450 3A4 metabolizes quetiapine to an inactive sulfoxide metabolite and also participates in the metabolism of its active metabolite, N-desalkyl quetiapine. CYP2D6 also regulates the metabolism of quetiapine. In one study, three metabolites of N-desalkylquetiapine were identified. Two of the metabolites were identified as N-desalkylquetiapine sulfoxide and 7-hydroxy-N-desalkylquetiapine. CYP2D6 has been found to be responsible for metabolism of quetiapine to 7-hydroxy-N-desalkylquetiapine, a pharmacologically active metabolite. Individual differences in CYP2D6 metabolism may be present, which may affect the concentrations of the active metabolite.A1118,A183863,L8546

Rute Eliminasi

After an oral dose of radiolabeled quetiapine, less than 1% of unchanged drug was detected in the urineA185441, suggesting that quetiapine is heavily metabolized. About 73% of a dose was detected in the urine, and about 20% in the feces.A14994,L8546

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. If taken with food, take with a light meal.

Interaksi Obat

2233 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Quetiapine.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Quetiapine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Quetiapine is combined with Levodopa.
Risperidone Quetiapine may increase the hypotensive activities of Risperidone.
Buprenorphine Quetiapine 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 Quetiapine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Quetiapine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Quetiapine.
Hydrocodone Quetiapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Quetiapine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Quetiapine 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 Quetiapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Quetiapine.
Orphenadrine Quetiapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Quetiapine 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 Quetiapine.
Rotigotine Quetiapine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Quetiapine.
Sodium oxybate Quetiapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Quetiapine 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 Quetiapine.
Thalidomide Quetiapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Quetiapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Aclidinium The risk or severity of adverse effects can be increased when Quetiapine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Quetiapine.
Mirabegron The risk or severity of urinary retention can be increased when Quetiapine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Quetiapine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Quetiapine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Quetiapine.
Tiotropium The risk or severity of adverse effects can be increased when Quetiapine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Quetiapine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Quetiapine is combined with Umeclidinium.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Quetiapine.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Quetiapine.
Epicaptopril The risk or severity of hypertension can be increased when Quetiapine is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Quetiapine is combined with Taxifolin.
1-benzylimidazole The risk or severity of hypertension can be increased when Quetiapine is combined with 1-benzylimidazole.
Saralasin The risk or severity of hypertension can be increased when Quetiapine is combined with Saralasin.
Tyramine The risk or severity of hypertension can be increased when Quetiapine is combined with Tyramine.
Atipamezole The risk or severity of hypertension can be increased when Quetiapine is combined with Atipamezole.
Idazoxan The risk or severity of hypertension can be increased when Quetiapine is combined with Idazoxan.
Ebselen The risk or severity of hypertension can be increased when Quetiapine is combined with Ebselen.
Tramazoline The risk or severity of hypertension can be increased when Quetiapine is combined with Tramazoline.
Fenozolone The risk or severity of hypertension can be increased when Quetiapine is combined with Fenozolone.
Xenon The risk or severity of hypertension can be increased when Quetiapine is combined with Xenon.
Buflomedil The risk or severity of hypertension can be increased when Quetiapine is combined with Buflomedil.
Mefenorex The risk or severity of hypertension can be increased when Quetiapine is combined with Mefenorex.
Quinoline Yellow WS The risk or severity of hypertension can be increased when Quetiapine is combined with Quinoline Yellow WS.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Quetiapine.
Siponimod The risk or severity of hypertension can be increased when Quetiapine is combined with Siponimod.
Dihydroergocristine The risk or severity of hypertension can be increased when Quetiapine is combined with Dihydroergocristine.
Terguride The risk or severity of hypertension can be increased when Quetiapine is combined with Terguride.
Selpercatinib The risk or severity of hypertension can be increased when Quetiapine is combined with Selpercatinib.
Naxitamab The risk or severity of hypertension can be increased when Quetiapine is combined with Naxitamab.
Serdexmethylphenidate The risk or severity of hypertension can be increased when Quetiapine is combined with Serdexmethylphenidate.
Amisulpride Quetiapine may increase the antipsychotic activities of Amisulpride.
Methylphenidate The risk or severity of adverse effects can be increased when Quetiapine is combined with Methylphenidate.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Quetiapine.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Quetiapine.
Sulpiride Quetiapine may increase the antipsychotic activities of Sulpiride.
Benzylpenicilloyl polylysine Quetiapine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Quetiapine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Quetiapine.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Quetiapine.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Quetiapine.
Mequitazine Quetiapine may increase the arrhythmogenic activities of Mequitazine.
Dapoxetine Dapoxetine may increase the orthostatic hypotensive activities of Quetiapine.
Glycopyrronium The risk or severity of adverse effects can be increased when Quetiapine is combined with Glycopyrronium.
Ritonavir The serum concentration of Quetiapine can be increased when it is combined with Ritonavir.
Carbamazepine The serum concentration of the active metabolites of Carbamazepine can be increased when Carbamazepine is used in combination with Quetiapine.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Quetiapine.
Dicoumarol The risk or severity of adverse effects can be increased when Quetiapine is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Quetiapine is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Quetiapine is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Quetiapine is combined with Tioclomarol.
Phenprocoumon The risk or severity of adverse effects can be increased when Quetiapine is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Quetiapine is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Quetiapine is combined with 4-hydroxycoumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Quetiapine is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Quetiapine is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Quetiapine is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Quetiapine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Quetiapine is combined with Diphenadione.
(S)-Warfarin The risk or severity of adverse effects can be increased when Quetiapine is combined with (S)-Warfarin.
Lurasidone Quetiapine may increase the hypotensive activities of Lurasidone.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Quetiapine is combined with Botulinum toxin type A.
Glucagon Quetiapine may increase the gastrointestinal motility reducing activities of Glucagon.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Quetiapine is combined with Botulinum toxin type B.
Mirtazapine Quetiapine may increase the serotonergic activities of Mirtazapine.
Eluxadoline The risk or severity of constipation can be increased when Quetiapine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Quetiapine is combined with Ramosetron.
Ethanol Quetiapine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Quetiapine 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 Quetiapine.
Seproxetine The risk or severity of adverse effects can be increased when Quetiapine is combined with Seproxetine.
Sertraline The risk or severity of adverse effects can be increased when Quetiapine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Quetiapine is combined with Sibutramine.
Milnacipran The risk or severity of adverse effects can be increased when Quetiapine is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Quetiapine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Quetiapine is combined with Levomilnacipran.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 1E HTR1E
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 3A HTR3A
5-hydroxytryptamine receptor 6 HTR6
5-hydroxytryptamine receptor 7 HTR7
D(1A) dopamine receptor DRD1
D(1B) dopamine receptor DRD5
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
Histamine H1 receptor HRH1
Alpha-1 adrenergic receptors ADRA1A
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M5 CHRM5

Referensi & Sumber

Synthesis reference: Kansal VK., Lal K.Suhail, Leonov AD.,(2006).US7687622B2.Retrieved from https://patents.google.com/patent/US7687622B2/en
Artikel (PubMed)
  • PMID: 11051217
    Dev V, Raniwalla J: Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 2000 Oct;23(4):295-307.
  • PMID: 14642017
    Mukaddes NM, Abali O: Quetiapine treatment of children and adolescents with Tourette's disorder. J Child Adolesc Psychopharmacol. 2003 Fall;13(3):295-9.
  • PMID: 11245917
    Tallerico T, Novak G, Liu IS, Ulpian C, Seeman P: Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex. Brain Res Mol Brain Res. 2001 Mar 5;87(2):160-5.
  • PMID: 18537577
    Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8.
  • PMID: 11510628
    DeVane CL, Nemeroff CB: Clinical pharmacokinetics of quetiapine: an atypical antipsychotic. Clin Pharmacokinet. 2001;40(7):509-22. doi: 10.2165/00003088-200140070-00003.
  • PMID: 10830145
    McConville BJ, Arvanitis LA, Thyrum PT, Yeh C, Wilkinson LA, Chaney RO, Foster KD, Sorter MT, Friedman LM, Brown KL, Heubi JE: Pharmacokinetics, tolerability, and clinical effectiveness of quetiapine fumarate: an open-label trial in adolescents with psychotic disorders. J Clin Psychiatry. 2000 Apr;61(4):252-60. doi: 10.4088/jcp.v61n0403.
  • PMID: 26834458
    Maneeton N, Maneeton B, Woottiluk P, Likhitsathian S, Suttajit S, Boonyanaruthee V, Srisurapanont M: Quetiapine monotherapy in acute treatment of generalized anxiety disorder: a systematic review and meta-analysis of randomized controlled trials. Drug Des Devel Ther. 2016 Jan 12;10:259-76. doi: 10.2147/DDDT.S89485. eCollection 2016.
  • PMID: 25912535
    Muneer A: Pharmacotherapy of bipolar disorder with quetiapine: a recent literature review and an update. Clin Psychopharmacol Neurosci. 2015 Apr 30;13(1):25-35. doi: 10.9758/cpn.2015.13.1.25.
Menampilkan 8 dari 17 artikel.
Textbook
  • Jasdave S. Maan; Abdolreza Saadabadi (2019). Quetiapine. Stat Pearls Publishing.

Contoh Produk & Brand

Produk: 1001 • International brands: 0
Produk
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