Peringatan Keamanan

Some minor GI-related adverse effects include epigastric pain and/or fullness, nausea, constipation, heartburn, distension, and diarrhoea. Other side effects are headache, dry mouth, drowsiness, vertigo and skin allergy. Oral LD50 in mice, rats and rabbits are 1531 mg/kg, 1145 mg/kg and 154 mg/kg, respectively L873. Pinaverium displays no teratogenic, mutagenic or carcinogenic potential.

Pinaverium

DB09090

small molecule approved

Deskripsi

Pinaverium is a spasmolytic agent used for functional gastrointestinal disorders. It is a quaternary ammonium compound that acts as an atypical calcium antagonist to restore normal bowel function. It is shown to relieve GI spasm and pain, transit disturbances and other symptoms related to motility disorders A19697 and may be considered as effective first-lline therapy for patients with irritable bowel syndrome (IBS) A19702. Pinaverium bromide is the common ingredient in formulations, mostly as oral tablets. Although it is not a currently approved drug by the FDA, pinaverium is available in over 60 countries including Canada.

Struktur Molekul 2D

Berat 511.52
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 is approximately 1.5 hours [L873].
Volume Distribusi It is selectively distributed to the digestive tract due to poor absorption and marked hepatobiliary excretion [L873].
Klirens (Clearance) -

Absorpsi

After oral administration, pinaverium is poorly absorbed (5-10%) followed by uptake by liver. Poor absorption is due to its highly polar quaternary ammonium group and high molecular weight L873, which limits extensive diffusion across all cell membranes and promotes its selectivity towards the gastrointestinal tracts . Peak plasma concentration is reached within one hour after administration and the absolute oral bioavailability is reported to be less than 1%.

Metabolisme

Hepatic metabolism of pinaverium involves demethylation of one of the methoxy groups, hydroxylation of the norpinanyl ring and elimination of the benzyl group with subsequent opening of the morpholine ring L873.

Rute Eliminasi

Pinaverium is predominantly eliminated into feces L873.

Interaksi Makanan

2 Data
  • 1. Take with a full glass of water.
  • 2. Take with food. This helps prevent pinaverium from irritating the esophagus.

Interaksi Obat

978 Data
Ceritinib Pinaverium may increase the bradycardic activities of Ceritinib.
Ivabradine Pinaverium may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Pinaverium.
Cimetidine The serum concentration of Pinaverium can be increased when it is combined with Cimetidine.
Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Pinaverium.
Efavirenz The serum concentration of Pinaverium can be decreased when it is combined with Efavirenz.
Melatonin The therapeutic efficacy of Pinaverium can be decreased when used in combination with Melatonin.
Nafcillin The therapeutic efficacy of Pinaverium can be decreased when used in combination with Nafcillin.
Nitroprusside Pinaverium may increase the hypotensive activities of Nitroprusside.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Pinaverium.
Lithium citrate The risk or severity of adverse effects can be increased when Pinaverium is combined with Lithium citrate.
Lithium carbonate The risk or severity of adverse effects can be increased when Pinaverium is combined with Lithium carbonate.
Lithium hydroxide The risk or severity of adverse effects can be increased when Pinaverium is combined with Lithium hydroxide.
Boceprevir The serum concentration of Pinaverium can be increased when it is combined with Boceprevir.
Tocainide Tocainide may increase the arrhythmogenic activities of Pinaverium.
Aprindine Aprindine may increase the arrhythmogenic activities of Pinaverium.
Xylometazoline Xylometazoline may increase the arrhythmogenic activities of Pinaverium.
Sparteine Sparteine may increase the arrhythmogenic activities of Pinaverium.
Fasudil Fasudil may increase the arrhythmogenic activities of Pinaverium.
Carteolol Pinaverium may increase the arrhythmogenic activities of Carteolol.
Metipranolol Pinaverium may increase the arrhythmogenic activities of Metipranolol.
Tropisetron Pinaverium may increase the arrhythmogenic activities of Tropisetron.
Spiradoline Pinaverium may increase the arrhythmogenic activities of Spiradoline.
Tiracizine Pinaverium may increase the arrhythmogenic activities of Tiracizine.
Ethacizine Pinaverium may increase the arrhythmogenic activities of Ethacizine.
Hydroquinine Pinaverium may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin Pinaverium may increase the arrhythmogenic activities of Bioallethrin.
Fosfructose Pinaverium may increase the arrhythmogenic activities of Fosfructose.
Hydroquinidine Pinaverium may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13 Pinaverium may increase the arrhythmogenic activities of SOR-C13.
Digoxin Digoxin may increase the arrhythmogenic activities of Pinaverium.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Pinaverium.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Pinaverium.
Cymarin Pinaverium may increase the arrhythmogenic activities of Cymarin.
Metildigoxin Pinaverium may increase the arrhythmogenic activities of Metildigoxin.
Acetyldigoxin Pinaverium may increase the arrhythmogenic activities of Acetyldigoxin.
Niguldipine Pinaverium may increase the arrhythmogenic activities of Niguldipine.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Pinaverium.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Pinaverium.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Pinaverium.
Atropine Atropine may increase the arrhythmogenic activities of Pinaverium.
Adenosine Adenosine may increase the arrhythmogenic activities of Pinaverium.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Pinaverium.
Nifedipine Nifedipine may increase the arrhythmogenic activities of Pinaverium.
Flecainide Flecainide may increase the arrhythmogenic activities of Pinaverium.
Prenylamine Prenylamine may increase the arrhythmogenic activities of Pinaverium.
Fluspirilene Fluspirilene may increase the arrhythmogenic activities of Pinaverium.
Azimilide Azimilide may increase the arrhythmogenic activities of Pinaverium.
Tedisamil Tedisamil may increase the arrhythmogenic activities of Pinaverium.
Nilvadipine Nilvadipine may increase the arrhythmogenic activities of Pinaverium.
Fendiline Fendiline may increase the arrhythmogenic activities of Pinaverium.
Eperisone Eperisone may increase the arrhythmogenic activities of Pinaverium.
Melperone Pinaverium may increase the arrhythmogenic activities of Melperone.
Benidipine Pinaverium may increase the arrhythmogenic activities of Benidipine.
Simendan Pinaverium may increase the arrhythmogenic activities of Simendan.
Otilonium Pinaverium may increase the arrhythmogenic activities of Otilonium.
Nizofenone Pinaverium may increase the arrhythmogenic activities of Nizofenone.
Bunaftine Pinaverium may increase the arrhythmogenic activities of Bunaftine.
Lorcainide Pinaverium may increase the arrhythmogenic activities of Lorcainide.
Penfluridol Pinaverium may increase the arrhythmogenic activities of Penfluridol.
Dexverapamil Pinaverium may increase the arrhythmogenic activities of Dexverapamil.
Disopyramide Disopyramide may increase the arrhythmogenic activities of Pinaverium.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Pinaverium.
Procainamide Procainamide may increase the arrhythmogenic activities of Pinaverium.
Bepridil Bepridil may increase the arrhythmogenic activities of Pinaverium.
Terodiline Pinaverium may increase the arrhythmogenic activities of Terodiline.
Isradipine Isradipine may increase the arrhythmogenic activities of Pinaverium.
Trimethadione Trimethadione may increase the arrhythmogenic activities of Pinaverium.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Pinaverium.
Lercanidipine Lercanidipine may increase the arrhythmogenic activities of Pinaverium.
Lamotrigine Lamotrigine may increase the arrhythmogenic activities of Pinaverium.
Nicardipine Nicardipine may increase the arrhythmogenic activities of Pinaverium.
Verapamil Verapamil may increase the arrhythmogenic activities of Pinaverium.
Losartan Losartan may increase the arrhythmogenic activities of Pinaverium.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Pinaverium.
Zonisamide Zonisamide may increase the arrhythmogenic activities of Pinaverium.
Nitrendipine Nitrendipine may increase the arrhythmogenic activities of Pinaverium.
Perhexiline Perhexiline may increase the arrhythmogenic activities of Pinaverium.
Nimesulide Nimesulide may increase the arrhythmogenic activities of Pinaverium.
Cyclandelate Cyclandelate may increase the arrhythmogenic activities of Pinaverium.
Flunarizine Flunarizine may increase the arrhythmogenic activities of Pinaverium.
Clevidipine Clevidipine may increase the arrhythmogenic activities of Pinaverium.
Methsuximide Methsuximide may increase the arrhythmogenic activities of Pinaverium.
Seletracetam Seletracetam may increase the arrhythmogenic activities of Pinaverium.
Nylidrin Nylidrin may increase the arrhythmogenic activities of Pinaverium.
Ziconotide Ziconotide may increase the arrhythmogenic activities of Pinaverium.
Dotarizine Dotarizine may increase the arrhythmogenic activities of Pinaverium.
Tranilast Tranilast may increase the arrhythmogenic activities of Pinaverium.
Agmatine Agmatine may increase the arrhythmogenic activities of Pinaverium.
Trimebutine Trimebutine may increase the arrhythmogenic activities of Pinaverium.
Nicorandil Pinaverium may increase the arrhythmogenic activities of Nicorandil.
Barnidipine Pinaverium may increase the arrhythmogenic activities of Barnidipine.
Aranidipine Pinaverium may increase the arrhythmogenic activities of Aranidipine.
Azelnidipine Pinaverium may increase the arrhythmogenic activities of Azelnidipine.
Cilnidipine Pinaverium may increase the arrhythmogenic activities of Cilnidipine.
Darodipine Pinaverium may increase the arrhythmogenic activities of Darodipine.
Efonidipine Pinaverium may increase the arrhythmogenic activities of Efonidipine.
Lacidipine Pinaverium may increase the arrhythmogenic activities of Lacidipine.
Manidipine Pinaverium may increase the arrhythmogenic activities of Manidipine.
Niludipine Pinaverium may increase the arrhythmogenic activities of Niludipine.

Target Protein

Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2177709
    Christen MO: Action of pinaverium bromide, a calcium-antagonist, on gastrointestinal motility disorders. Gen Pharmacol. 1990;21(6):821-5.
  • PMID: 1313732
    Feron O, Wibo M, Christen MO, Godfraind T: Interaction of pinaverium (a quaternary ammonium compound) with 1,4-dihydropyridine binding sites in rat ileum smooth muscle. Br J Pharmacol. 1992 Feb;105(2):480-4.
  • PMID: 4052731
    Baumgartner A, Drack E, Halter F, Scheurer U: Effects of pinaverium bromide and verapamil on the motility of the rat isolated colon. Br J Pharmacol. 1985 Sep;86(1):89-94.
  • PMID: 25632806
    Zheng L, Lai Y, Lu W, Li B, Fan H, Yan Z, Gong C, Wan X, Wu J, Huang D, Wang Y, Mei Y, Li Z, Jiang Z, Liu X, Ye J, Yang Y, Huang H, Xiao J: Pinaverium Reduces Symptoms of Irritable Bowel Syndrome in a Multicenter, Randomized, Controlled Trial. Clin Gastroenterol Hepatol. 2015 Jul;13(7):1285-1292.e1. doi: 10.1016/j.cgh.2015.01.015. Epub 2015 Jan 26.
  • PMID: 8201843
    Bobo MH, Magous R, Christen MO, Bali JP: Effect of pinaverium and other calcium channel blockers on contraction of isolated gastric antral smooth muscle cells caused by gastrointestinal hormones. Life Sci. 1994;54(25):1947-54.
  • PMID: 8600700
    Awad R, Dibildox M, Ortiz F: Irritable bowel syndrome treatment using pinaverium bromide as a calcium channel blocker. A randomized double-blind placebo-controlled trial. Acta Gastroenterol Latinoam. 1995;25(3):137-44.
  • PMID: 7197953
    Itoh Z, Takahashi I: Inhibitory effect of pinaverium bromide on gastrointestinal contractile activity in conscious dogs. Arzneimittelforschung. 1981;31(9):1450-3.
  • PMID: 19416978
    Tikhonov DB, Zhorov BS: Structural model for dihydropyridine binding to L-type calcium channels. J Biol Chem. 2009 Jul 10;284(28):19006-17. doi: 10.1074/jbc.M109.011296. Epub 2009 May 5.
Textbook
  • ISBN: 940111725X
    Godfraind T, Govoni S, Paoletti R, Vanhoutte PM (2013). Calcium Antagonists: Pharmacology and Clinical Research (pp. 306-307). Springer Science & Business Media.

Contoh Produk & Brand

Produk: 5 • International brands: 16
Produk
  • Dicetel
    Tablet • 50 mg • Oral • Canada • Approved
  • Dicetel
    Tablet • 100 mg • Oral • Canada • Approved
  • Pinaverium
    Tablet • 50 mg • Oral • Canada • Approved
  • Pinaverium
    Tablet • 100 mg • Oral • Canada • Approved
  • Truemed Group LLC
    Tablet • 100 mg/100mg • Oral • US
International Brands
  • Alevian Duo — Takeda
  • Blocafer — Liferpal, Mexico
  • Delibs — CONMED, Taiwan
  • Ilyang Dicetel — Ilyang
  • Nulite — Dominguez, Argentina
  • Pakab — Wermar, Mexico
  • Pinar — ABL Pharma, Peru
  • Pinaven — Johnson, Taiwan
  • Pladuet — Interlab Pharmaceutica, Mexico
  • Planex — Rimsa, Mexico

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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