Peringatan Keamanan

Acute oral toxicity (LD50) in rats is 264 mg/kg. Cases of overdose have been reported and rarely, deaths have occurred. The following signs and symptoms may be observed following overdose: stupor, coma, diminished urine output and hypotension.

Sulindac

DB00605

small molecule approved investigational

Deskripsi

Sulindac is a nonsteroidal anti-inflammatory drug (NSAID) of the arylalkanoic acid class that is marketed by Merck under the brand name Clinoril. Like other NSAIDs, it may be used in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in vivo to an active sulfide compound by liver enzymes. There is evidence from some studies that sulindac may be associated with fewer gastrointestinal side effects than other NSAIDs, except for the cyclooxygenase-2 (COX-2) inhibitor drug class. This may be due to the sulfide metabolite undergoing enterohepatic circulation thus maintaining constant blood levels of the compound without inducing gastrointestinal effects, where the drug is excreted in the bile and then reabsorbed from the intestines. While its full mechanism of action is not fully understood, sulindac is thought to primarily mediate its action by inhibiting prostaglandin synthesis by inhibiting COX-1 and COX-2.

Struktur Molekul 2D

Berat 356.411
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half-life of sulindac is 7.8 hours while the mean half-life of the sulfide metabolite is 16.4 hours.
Volume Distribusi -
Klirens (Clearance) * Renal cl=68.12 +/- 27.56 mL/min [NORMAL (19-41 yrs)]

Absorpsi

Approximately 90% absorbed in humans following oral administration.

Metabolisme

Undergoes two major biotransformations: reversible reduction to the sulfide metabolite, and irreversible oxidation to the sulfone metabolite. Sulindac and its sulfide and sulfone metabolites undergo extensive enterohepatic circulation. Available evidence indicates that the biological activity resides with the sulfide metabolite. Side chain hydroxylation and hydration of the double bond also occur.

Rute Eliminasi

Sulindac is excreted in rat milk; concentrations in milk were 10 to 20% of those levels in plasma. It is not known if sulindac is excreted in human milk. Approximately 50% of the administered dose of sulindac is excreted in the urine with the conjugated sulfone metabolite accounting for the major portion. Hepatic metabolism is an important elimination pathway.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Ingesting alcohol may increase the risk of gastrointestinal bleeding.
  • 2. Take with food.

Interaksi Obat

1403 Data
Amlodipine Sulindac may decrease the antihypertensive activities of Amlodipine.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Sulindac.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Sulindac.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Sulindac.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Sulindac.
Ziprasidone The risk or severity of hypertension can be increased when Ziprasidone is combined with Sulindac.
Methysergide The risk or severity of hypertension can be increased when Methysergide is combined with Sulindac.
Cabergoline The risk or severity of hypertension can be increased when Cabergoline is combined with Sulindac.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Sulindac.
Dihydroergotamine The risk or severity of hypertension can be increased when Dihydroergotamine is combined with Sulindac.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Sulindac.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Sulindac.
Mirtazapine The risk or severity of hypertension can be increased when Mirtazapine is combined with Sulindac.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Sulindac.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Sulindac.
Promazine The risk or severity of hypertension can be increased when Promazine is combined with Sulindac.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Sulindac.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Sulindac.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Sulindac.
Lisuride The risk or severity of hypertension can be increased when Lisuride is combined with Sulindac.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Sulindac.
Metaraminol The risk or severity of hypertension can be increased when Sulindac is combined with Metaraminol.
Furazolidone The risk or severity of hypertension can be increased when Sulindac is combined with Furazolidone.
Epinephrine The risk or severity of hypertension can be increased when Sulindac is combined with Epinephrine.
Thioridazine The risk or severity of hypertension can be increased when Sulindac is combined with Thioridazine.
Ergotamine The risk or severity of hypertension can be increased when Sulindac is combined with Ergotamine.
Nicergoline The risk or severity of hypertension can be increased when Sulindac is combined with Nicergoline.
Sufentanil The risk or severity of hypertension can be increased when Sulindac is combined with Sufentanil.
Methoxamine The risk or severity of hypertension can be increased when Sulindac is combined with Methoxamine.
Risperidone The risk or severity of hypertension can be increased when Sulindac is combined with Risperidone.
Tranylcypromine The risk or severity of hypertension can be increased when Sulindac is combined with Tranylcypromine.
Isoflurane The risk or severity of hypertension can be increased when Sulindac is combined with Isoflurane.
Propiomazine The risk or severity of hypertension can be increased when Sulindac is combined with Propiomazine.
Alfentanil The risk or severity of hypertension can be increased when Sulindac is combined with Alfentanil.
Minaprine The risk or severity of hypertension can be increased when Sulindac is combined with Minaprine.
Orciprenaline The risk or severity of hypertension can be increased when Sulindac is combined with Orciprenaline.
Propofol The risk or severity of hypertension can be increased when Sulindac is combined with Propofol.
Phenmetrazine The risk or severity of hypertension can be increased when Sulindac is combined with Phenmetrazine.
Trifluoperazine The risk or severity of hypertension can be increased when Sulindac is combined with Trifluoperazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Sulindac is combined with Pseudoephedrine.
Benzphetamine The risk or severity of hypertension can be increased when Sulindac is combined with Benzphetamine.
Ritodrine The risk or severity of hypertension can be increased when Sulindac is combined with Ritodrine.
Flupentixol The risk or severity of hypertension can be increased when Sulindac is combined with Flupentixol.
Remifentanil The risk or severity of hypertension can be increased when Sulindac is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Sulindac is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Sulindac is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Sulindac is combined with Diethylpropion.
Salmeterol The risk or severity of hypertension can be increased when Sulindac is combined with Salmeterol.
Naratriptan The risk or severity of hypertension can be increased when Sulindac is combined with Naratriptan.
Formoterol The risk or severity of hypertension can be increased when Sulindac is combined with Formoterol.
Frovatriptan The risk or severity of hypertension can be increased when Sulindac is combined with Frovatriptan.
Methoxyflurane The risk or severity of hypertension can be increased when Sulindac is combined with Methoxyflurane.
Selegiline The risk or severity of hypertension can be increased when Sulindac is combined with Selegiline.
Ergoloid mesylate The risk or severity of hypertension can be increased when Sulindac is combined with Ergoloid mesylate.
Isoprenaline The risk or severity of hypertension can be increased when Sulindac is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Sulindac is combined with Arbutamine.
Dutasteride The risk or severity of hypertension can be increased when Sulindac is combined with Dutasteride.
Halothane The risk or severity of hypertension can be increased when Sulindac is combined with Halothane.
Moclobemide The risk or severity of hypertension can be increased when Sulindac is combined with Moclobemide.
Pergolide The risk or severity of hypertension can be increased when Sulindac is combined with Pergolide.
Desflurane The risk or severity of hypertension can be increased when Sulindac is combined with Desflurane.
Bromocriptine The risk or severity of hypertension can be increased when Sulindac is combined with Bromocriptine.
Finasteride The risk or severity of hypertension can be increased when Sulindac is combined with Finasteride.
Aripiprazole The risk or severity of hypertension can be increased when Sulindac is combined with Aripiprazole.
Isocarboxazid The risk or severity of hypertension can be increased when Sulindac is combined with Isocarboxazid.
Ergometrine The risk or severity of hypertension can be increased when Sulindac is combined with Ergometrine.
Lisdexamfetamine The risk or severity of hypertension can be increased when Sulindac is combined with Lisdexamfetamine.
Fenoterol The risk or severity of hypertension can be increased when Sulindac is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Sulindac is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Sulindac is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Sulindac is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Sulindac is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Sulindac is combined with Procaterol.
Yohimbine The risk or severity of hypertension can be increased when Sulindac is combined with Yohimbine.
Methotrimeprazine The risk or severity of hypertension can be increased when Sulindac is combined with Methotrimeprazine.
Clenbuterol The risk or severity of hypertension can be increased when Sulindac is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Sulindac is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Sulindac is combined with MMDA.
Midomafetamine The risk or severity of hypertension can be increased when Sulindac is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Sulindac is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Sulindac is combined with 4-Methoxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Sulindac is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Sulindac is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Sulindac is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Sulindac is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Sulindac is combined with Phendimetrazine.
Solifenacin The risk or severity of hypertension can be increased when Sulindac is combined with Solifenacin.
Periciazine The risk or severity of hypertension can be increased when Sulindac is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Sulindac is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Sulindac is combined with Thioproperazine.
Zuclopenthixol The risk or severity of hypertension can be increased when Sulindac is combined with Zuclopenthixol.
Epicaptopril The risk or severity of hypertension can be increased when Sulindac is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Sulindac is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Sulindac is combined with 1-benzylimidazole.
Iproniazid The risk or severity of hypertension can be increased when Sulindac is combined with Iproniazid.
Nialamide The risk or severity of hypertension can be increased when Sulindac is combined with Nialamide.
Lysergic acid diethylamide The risk or severity of hypertension can be increased when Sulindac is combined with Lysergic acid diethylamide.
Dronedarone The risk or severity of hypertension can be increased when Sulindac is combined with Dronedarone.
Flibanserin The risk or severity of hypertension can be increased when Sulindac is combined with Flibanserin.
Iloperidone The risk or severity of hypertension can be increased when Sulindac is combined with Iloperidone.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Aldo-keto reductase family 1 member B1 AKR1B1
Prostaglandin G/H synthase 1 PTGS1
Mitogen-activated protein kinase 3 MAPK3
Peroxisome proliferator-activated receptor delta PPARD
Prostaglandin D2 receptor 2 PTGDR2
Aldo-keto reductase family 1 member B10 AKR1B10

Referensi & Sumber

Synthesis reference: Gary Piazza, Robert Reynolds, "Derivatives of sulindac, use thereof and preparation thereof." U.S. Patent US20070244122, issued October 18, 2007.

Contoh Produk & Brand

Produk: 71 • International brands: 0
Produk
  • Apo-sulin Tab 150mg
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Apo-sulin Tab 200mg
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Clinoril
    Tablet • 200 mg/1 • Oral • US • Approved
  • Clinoril
    Tablet • 150 mg/1 • Oral • US • Approved
  • Clinoril Tab 150mg
    Tablet • 150 mg / tab • Oral • Canada • Approved
  • Clinoril Tab 200mg
    Tablet • 200 mg / tab • Oral • Canada • Approved
  • Nu-sulindac Tab 150mg
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Nu-sulindac Tab 200mg
    Tablet • 200 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 71 produk.

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