Peringatan Keamanan

At present, there is little information concerning overdosage with ondansetron F3178, F3181, F3184. Nevertheless, there have been certain cases of somewhat idiosyncratic adverse effects associated with particular dosages of ondansetron used F3178, F3181, F3184.

“Sudden blindness” (amaurosis) of 2 to 3 minutes duration plus severe constipation occurred in one patient that was administered 72 mg of ondansetron intravenously as a single dose F3178, F3181, F3184. Hypotension (and faintness) occurred in another patient that took 48 mg of oral ondansetron F3178, F3181, F3184. Following infusion of 32 mg over only a 4-minute period, a vasovagal episode with transient second-degree heart block was observed F3178, F3181, F3184. Neuromuscular abnormalities, autonomic instability, somnolence, and a brief generalized tonic-clonic seizure (which resolved after a dose of benzodiazepine) were observed in a 12-month-old infant who ingested seven or eight 8-mg ondansetron tablets (approximately forty times the recommended 0.1-0.15 mg/kg dose for a pediatric patient) F3178, F3181, F3184. In all instances, however, the events resolved completely F3178, F3181, F3184.

The safety of ondansetron for use in human pregnancy has not been established F3181, F3184. Ondansetron is not teratogenic in animals F3181, F3184. However, as animal studies are not always predictive of human response, the use of ondansetron in pregnancy is not recommended F3181, F3184.

Ondansetron is excreted in the milk of lactating rats F3181, F3184. It is not known if it is excreted in human milk, however, nursing is not recommended during treatment with ondansetron F3181, F3184.

Insufficient information is available to provide dosage recommendations for children 3 years of age or younger F3181, F3184.

Ondansetron

DB00904

small molecule approved withdrawn

Deskripsi

A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

Having been developed in the 1980s by GlaxoSmithKline and approved by the US FDA since January 1991, ondansetron has demonstrated a long history of use and efficacy. Commonly formulated as oral tablets, orally disintegrating tablets (ODT), and injections, and available as generic products as well, ondansetron continues to see contemporary innovations in its formulation and use, including the development of orally soluble films that are both discreet in administration and less of a burden in comparison to having patients attempt to swallow pills during emesis.L5221

The FDA withdrew its approval for the use of all intravenous drug products containing more than 16 mg of ondansetron hydrochloride in a single dose, due to a high risk of QT prolongation.L44067,L43942

Struktur Molekul 2D

Berat 293.363
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 ondansetron after either an 8 mg oral dose or intravenous dose was approximately 3-4 hours and could be extended to 6-8 hours in the elderly [F3181, F3184].
Volume Distribusi The volume of distribution of ondansetron has been recorded as being approximately 160L [A174250].
Klirens (Clearance) The clearance values determined for ondansetron in various patient age groups were recorded as approximately 0.38 L/h/kg in normal adult volunteers aged 19-40 yrs, 0.32 L/h/kg in normal adult volunteers aged 61-74 yrs, 0.26 L/h/kg in normal adult volunteers aged >=75 yrs [FDA Label].

Absorpsi

Ondansetron is absorbed from the gastrointestinal tract and undergoes some limited first-pass metabolism F3178. Mean bioavailability in healthy subjects, following administration of a single 8-mg tablet, was recorded as being approximately 56% to 60% F3178, F3181, F3184. Bioavailability is also slightly enhanced by the presence of food F3178. Ondansetron systemic exposure does not increase proportionately to dose F3178. The AUC from a 16-mg tablet was 24% greater than predicted from an 8-mg tablet dose F3178. This may reflect some reduction of first-pass metabolism at higher oral doses F3178.

Metabolisme

In vitro metabolism studies have shown that ondansetron is a substrate for human hepatic cytochrome P450 enzymes, including CYP1A2, CYP2D6 and CYP3A4 F3178, F3181, F3184. In terms of overall ondansetron turnover, CYP3A4 played the predominant role F3178, F3181, F3184. Because of the multiplicity of metabolic enzymes capable of metabolizing ondansetron, it is likely that inhibition or loss of one enzyme (e.g. CYP2D6 enzyme deficiency) will be compensated by others and may result in little change in overall rates of ondansetron clearance F3178, F3181, F3184. Following oral or IV administration, ondansetron is extensively metabolised and excreted in the urine and faeces F3178, F3181, F3184. In humans, less than 10% of the dose is excreted unchanged in the urine F3178, F3181, F3184. The major urinary metabolites are glucuronide conjugates (45%), sulphate conjugates (20%) and hydroxylation products (10%) F3178, F3181, F3184. The primary metabolic pathway is subsequently hydroxylation on the indole ring followed by subsequent glucuronide or sulfate conjugation F3178, F3181, F3184. Although some nonconjugated metabolites have pharmacologic activity, these are not found in plasma at concentrations likely to significantly contribute to the biological activity of ondansetron F3178, F3181, F3184.

Rute Eliminasi

Following oral or IV administration, ondansetron is extensively metabolised and excreted in the urine and faeces F3181, F3184.

Farmakogenomik

2 Varian
CYP2D6 (None)

Patients with this genotype in CYP2D6 are ultrarapid metabolizers with an increased risk of poor therapeutic response and vomiting when treated with ondansteron.

CYP2D6 (None)

Patients with this genotype in CYP2D6 are ultrarapid metabolizers with an increased risk of poor therapeutic response and vomiting when treated with ondansteron.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1479 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Ondansetron.
Deferasirox The serum concentration of Ondansetron can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Ondansetron can be increased when it is combined with Peginterferon alfa-2b.
Teriflunomide The serum concentration of Ondansetron can be decreased when it is combined with Teriflunomide.
Leflunomide The serum concentration of Ondansetron can be decreased when it is combined with Leflunomide.
Buprenorphine Ondansetron 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 Ondansetron.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Ondansetron.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Ondansetron.
Hydrocodone Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Ondansetron can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Ondansetron may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Ondansetron.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Ondansetron.
Orphenadrine Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Ondansetron 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 Ondansetron.
Pramipexole Ondansetron may increase the sedative activities of Pramipexole.
Ropinirole Ondansetron may increase the sedative activities of Ropinirole.
Rotigotine Ondansetron may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Ondansetron.
Sodium oxybate Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Ondansetron 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 Ondansetron.
Thalidomide Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Yohimbine The therapeutic efficacy of Ondansetron can be increased when used in combination with Yohimbine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Ondansetron.
Apomorphine The risk or severity of adverse effects can be increased when Ondansetron is combined with Apomorphine.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Ondansetron.
Phenindione The risk or severity of adverse effects can be increased when Ondansetron is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Ondansetron is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Ondansetron is combined with Tioclomarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Ondansetron is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Ondansetron is combined with Ethyl biscoumacetate.
Clorindione The risk or severity of adverse effects can be increased when Ondansetron is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Ondansetron is combined with Diphenadione.
Mirabegron The serum concentration of Ondansetron can be increased when it is combined with Mirabegron.
Abiraterone The serum concentration of Ondansetron can be increased when it is combined with Abiraterone.
Mirtazapine Ondansetron may increase the serotonergic activities of Mirtazapine.
Cyproterone acetate The metabolism of Ondansetron can be increased when combined with Cyproterone acetate.
Ethanol Ondansetron may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Ondansetron 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 Ondansetron.
Zimelidine The risk or severity of adverse effects can be increased when Ondansetron is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Ondansetron is combined with Dapoxetine.
Sertraline The risk or severity of adverse effects can be increased when Ondansetron is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Ondansetron is combined with Sibutramine.
Milnacipran The risk or severity of adverse effects can be increased when Ondansetron is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Ondansetron.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Ondansetron is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Ondansetron is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Ondansetron is combined with Alaproclate.
Seproxetine The risk or severity of adverse effects can be increased when Ondansetron is combined with Seproxetine.
Methylene blue Ondansetron may increase the serotonergic activities of Methylene blue.
Trospium The metabolism of Ondansetron can be decreased when combined with Trospium.
Tiotropium The metabolism of Tiotropium can be decreased when combined with Ondansetron.
Doxepin The risk or severity of CNS depression can be increased when Ondansetron is combined with Doxepin.
Scopolamine The risk or severity of CNS depression can be increased when Scopolamine is combined with Ondansetron.
Fesoterodine The metabolism of Fesoterodine can be decreased when combined with Ondansetron.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Ondansetron.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Ondansetron.
Zopiclone The risk or severity of adverse effects can be increased when Ondansetron is combined with Zopiclone.
Anagrelide The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Ibutilide.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Grepafloxacin.
Toremifene The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Toremifene.
Imatinib The serum concentration of Ondansetron can be increased when it is combined with Imatinib.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Trovafloxacin.
Mifepristone The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Mifepristone.
Cocaine The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Cocaine.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Arsenic trioxide.
Domperidone The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Domperidone.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Sparfloxacin.
Bepridil The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Bepridil.
Temafloxacin The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Temafloxacin.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Tetrabenazine.
Vandetanib The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Vandetanib.
Romidepsin The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Romidepsin.
Artemether The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Artemether.
Glasdegib The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Glasdegib.
Deutetrabenazine The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Deutetrabenazine.
Macimorelin The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Terodiline.
Citalopram The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Citalopram.
Thioridazine The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Thioridazine.
Paliperidone The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Paliperidone.
Lithium cation The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Lithium cation.
Zuclopenthixol The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Zuclopenthixol.
Iloperidone The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Iloperidone.
Asenapine The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Asenapine.
Eliglustat The metabolism of Ondansetron can be decreased when combined with Eliglustat.
Cisapride The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Cisapride.
Dofetilide The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Dofetilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Valproic acid.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Ondansetron.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Ondansetron.

Target Protein

5-hydroxytryptamine receptor 3A HTR3A
5-hydroxytryptamine receptor 4 HTR4
Mu-type opioid receptor OPRM1
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B

Referensi & Sumber

Synthesis reference: Peter Bod, Kalman Harsanyi, Ferenc Trischler, Eva Fekecs, Attila Csehi, Bela Hegedus, Eva Mersich nee Donat, Gyorgyi Szabo nee Komlosi, Erika Horvath nee Sziki, "Process for preparing ondansetron." U.S. Patent US5478949, issued September, 1990.
Artikel (PubMed)
  • PMID: 11919526
    Ramsook C, Sahagun-Carreon I, Kozinetz CA, Moro-Sutherland D: A randomized clinical trial comparing oral ondansetron with placebo in children with vomiting from acute gastroenteritis. Ann Emerg Med. 2002 Apr;39(4):397-403.
  • PMID: 19758398
    Yilmaz HL, Yildizdas RD, Sertdemir Y: Clinical trial: oral ondansetron for reducing vomiting secondary to acute gastroenteritis in children--a double-blind randomized study. Aliment Pharmacol Ther. 2010 Jan;31(1):82-91. doi: 10.1111/j.1365-2036.2009.04145.x. Epub .
  • PMID: 9506240
    Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89.
  • PMID: 15740177
    Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38.
  • PMID: 7586904
    Roila F, Del Favero A: Ondansetron clinical pharmacokinetics. Clin Pharmacokinet. 1995 Aug;29(2):95-109. doi: 10.2165/00003088-199529020-00004.

Contoh Produk & Brand

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