Peringatan Keamanan

Rat Oral LD 50 747 mg/kgF3196

Tumorigenicity

Because of the chronic nature of GERD, there may be a potential for long-term administration of pantoprazole. In long-term rodent studies, pantoprazole was carcinogenic and its administration lead to rare types of gastrointestinal tumors. The relevance of these findings to tumor development in humans is unknown at this time.F3202

Teratogenic Effects

This drug falls under pregnancy category B category. Reproduction studies have been performed in rats at oral doses up to 88 times the recommended human dose (RHD), as well as in rabbits at oral doses up to 16 times the RHD, and have shown no evidence of impaired fertility or harm to the fetus caused by pantoprazole. No adequate and well-controlled studies in pregnant women have been completed. Because animal reproduction studies are not always predictive of human response, this drug should only be used during pregnancy if clearly required.F3202

Nursing Mothers

Pantoprazole and its metabolites have been found to be excreted in the milk of rats. Pantoprazole excretion in human milk has been found in a study performed with a single nursing mother after one 40 mg oral dose. The clinical relevance of this finding is not known, however, it is advisable to take note of this finding when considering pantoprazole use during nursing. Many drugs excreted in human breastmilk have a risk for serious adverse effects in nursing infants.F3202

Pantoprazole

DB00213

small molecule approved

Deskripsi

Pantoprazole is a first-generation proton pump inhibitor (PPI) used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome. It can also be found in quadruple regimens for the treatment of H. pylori infections along with other antibiotics including amoxicillin, clarithromycin, and metronidazole, for example.A177271F4498 Its efficacy is considered similar to other medications within the PPI class including omeprazole, esomeprazole, lansoprazole, dexlansoprazole, and rabeprazole.

Pantoprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of pantoprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, pantoprazole's duration of antisecretory effect persists longer than 24 hours.FDA Label

Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as pantoprazole have been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal C. difficile), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life.A177571

PPIs such as pantoprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes.A177577, A177580

Pantoprazole doses should be slowly lowered, or tapered, before discontinuing as rapid discontinuation of PPIs such as pantoprazole may cause a rebound effect and a short term increase in hypersecretion.A177574

Struktur Molekul 2D

Berat 383.37
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) About 1 hour[F3202]
Volume Distribusi The apparent volume of distribution of pantoprazole is approximately 11.0-23.6 L, distributing mainly in the extracellular fluid.[FDA label]
Klirens (Clearance) **Adults**: With intravenous administration of pantoprazole to extensive metabolizers, total clearance is 7.6-14.0 L/h.[F3193] In a population pharmacokinetic analysis, the total clearance increased with increasing body weight in a non-linear fashion.[F3193] **Children**: clearance values in the children 1 to 5 years old with endoscopically proven GERD had a median value of 2.4 L/h.[F3202]

Absorpsi

Pantoprazole is absorbed after oral administration as an enteric-coated tablet with maximum plasma concentrations attained within 2 – 3 hours and a bioavailability of 77% that does not change with multiple dosing A174247. Following an oral dose of 40mg, the Cmax is approximately 2.5 ?g/mL with a tmax of 2 to 3 hours. The AUC is approximately 5 ?g.h/mL. There is no food effect on AUC (bioavailability) and Cmax.F4486 Delayed-release tablets are prepared as enteric-coated tablets so that absorption of pantoprazole begins only after the tablet leaves the stomach.

Metabolisme

Pantoprazole is heavily metabolized in the liver by the cytochrome P450 (CYP) system. Pantoprazole metabolism is independent of the route of administration (intravenous or oral). The main metabolic pathway is demethylation, by CYP2C19 hepatic cytochrome enzyme, followed by sulfation; other metabolic pathways include oxidation by CYP3A4. There is no evidence that any of the pantoprazole metabolites are pharmacologically active.F3202 After hepatic metabolism, almost 80% of an oral or intravenous dose is excreted as metabolites in urine; the remainder is found in feces and originates from biliary secretion.A174256

Rute Eliminasi

After a single oral or intravenous (IV) dose of 14C-labeled pantoprazole to healthy, normal metabolizing subjects, about 71% of the dose was excreted in the urine, with 18% excreted in the feces by biliary excretion. There was no kidney excretion of unchanged pantoprazole.F3202

Interaksi Makanan

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

Interaksi Obat

1100 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Pantoprazole.
Dabrafenib The serum concentration of Pantoprazole can be decreased when it is combined with Dabrafenib.
Amphetamine Pantoprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Bosutinib Pantoprazole can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren The serum concentration of Cefditoren can be decreased when it is combined with Pantoprazole.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Pantoprazole resulting in a loss in efficacy.
Dabigatran etexilate Pantoprazole can cause a decrease in the absorption of Dabigatran etexilate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dasatinib Pantoprazole can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delavirdine Pantoprazole can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dextroamphetamine Pantoprazole can cause an increase in the absorption of Dextroamphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Erlotinib Pantoprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fluconazole The metabolism of Pantoprazole can be decreased when combined with Fluconazole.
Gefitinib Pantoprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Indinavir Pantoprazole can cause a decrease in the absorption of Indinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Itraconazole Pantoprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Pantoprazole can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methotrexate The excretion of Methotrexate can be decreased when combined with Pantoprazole.
Methylphenidate Pantoprazole can cause an increase in the absorption of Methylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
Dexmethylphenidate Pantoprazole can cause an increase in the absorption of Dexmethylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
Nilotinib The serum concentration of Nilotinib can be decreased when it is combined with Pantoprazole.
Pazopanib Pantoprazole can cause a decrease in the absorption of Pazopanib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Posaconazole Pantoprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Raltegravir Pantoprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Riociguat Pantoprazole can cause a decrease in the absorption of Riociguat resulting in a reduced serum concentration and potentially a decrease in efficacy.
Risedronic acid Pantoprazole can cause an increase in the absorption of Risedronic acid resulting in an increased serum concentration and potentially a worsening of adverse effects.
Voriconazole The metabolism of Pantoprazole can be decreased when combined with Voriconazole.
Luliconazole The serum concentration of Pantoprazole can be increased when it is combined with Luliconazole.
Succinic acid The excretion of Succinic acid can be decreased when combined with Pantoprazole.
Citrulline The excretion of Citrulline can be decreased when combined with Pantoprazole.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Pantoprazole.
Cefdinir The excretion of Cefdinir can be decreased when combined with Pantoprazole.
Leucovorin The excretion of Leucovorin can be decreased when combined with Pantoprazole.
Fluorescein The excretion of Fluorescein can be decreased when combined with Pantoprazole.
Quinapril The excretion of Quinapril can be decreased when combined with Pantoprazole.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Pantoprazole.
Famotidine The excretion of Famotidine can be decreased when combined with Pantoprazole.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Pantoprazole.
Tazobactam The excretion of Tazobactam can be decreased when combined with Pantoprazole.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Pantoprazole.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Pantoprazole.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Pantoprazole.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Pantoprazole.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Pantoprazole.
Avibactam The excretion of Avibactam can be decreased when combined with Pantoprazole.
Silibinin The excretion of Silibinin can be decreased when combined with Pantoprazole.
Relebactam The excretion of Relebactam can be decreased when combined with Pantoprazole.
Cefotiam The excretion of Cefotiam can be decreased when combined with Pantoprazole.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Pantoprazole.
Cephalexin The excretion of Cephalexin can be decreased when combined with Pantoprazole.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Pantoprazole.
Acyclovir The excretion of Acyclovir can be decreased when combined with Pantoprazole.
Cefaclor The excretion of Cefaclor can be decreased when combined with Pantoprazole.
Bumetanide The excretion of Bumetanide can be decreased when combined with Pantoprazole.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Pantoprazole.
Cefazolin The excretion of Cefazolin can be decreased when combined with Pantoprazole.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Pantoprazole.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Pantoprazole.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Pantoprazole.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Pantoprazole.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Pantoprazole.
Tenofovir The excretion of Tenofovir can be decreased when combined with Pantoprazole.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Pantoprazole.
Piperacillin The excretion of Piperacillin can be decreased when combined with Pantoprazole.
Trifluridine The excretion of Trifluridine can be decreased when combined with Pantoprazole.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Pantoprazole.
Doripenem The excretion of Doripenem can be decreased when combined with Pantoprazole.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Pantoprazole.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Pantoprazole.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Pantoprazole.
Pravastatin The excretion of Pravastatin can be decreased when combined with Pantoprazole.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Pantoprazole.
Indomethacin The excretion of Indomethacin can be decreased when combined with Pantoprazole.
Zidovudine The excretion of Zidovudine can be decreased when combined with Pantoprazole.
Cimetidine The excretion of Cimetidine can be decreased when combined with Pantoprazole.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Pantoprazole.
Tetracycline The excretion of Tetracycline can be decreased when combined with Pantoprazole.
Estradiol The excretion of Estradiol can be decreased when combined with Pantoprazole.
Ranitidine The excretion of Ranitidine can be decreased when combined with Pantoprazole.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Pantoprazole.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Pantoprazole.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Pantoprazole.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Pantoprazole.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Pantoprazole.
Levothyroxine Pantoprazole can cause a decrease in the absorption of Levothyroxine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bisacodyl The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Pantoprazole.
Captopril Pantoprazole can cause a decrease in the absorption of Captopril resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime The serum concentration of Cefuroxime can be decreased when it is combined with Pantoprazole.
Rifampin Pantoprazole can cause a decrease in the absorption of Rifampicin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Memantine Pantoprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Sulpiride The therapeutic efficacy of Sulpiride can be increased when used in combination with Pantoprazole.
Mesalazine Pantoprazole can cause a decrease in the absorption of Mesalazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tolevamer The therapeutic efficacy of Tolevamer can be decreased when used in combination with Pantoprazole.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Pantoprazole.
Alendronic acid The therapeutic efficacy of Alendronic acid can be decreased when used in combination with Pantoprazole.
Ibandronate The therapeutic efficacy of Ibandronate can be decreased when used in combination with Pantoprazole.
Clodronic acid The therapeutic efficacy of Clodronic acid can be decreased when used in combination with Pantoprazole.
Etidronic acid The therapeutic efficacy of Etidronic acid can be decreased when used in combination with Pantoprazole.
Incadronic acid The therapeutic efficacy of Incadronic acid can be decreased when used in combination with Pantoprazole.
Cysteamine The bioavailability of Cysteamine can be decreased when combined with Pantoprazole.
Ketoconazole Pantoprazole can cause a decrease in the absorption of Ketoconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.

Target Protein

Potassium-transporting ATPase alpha chain 1 ATP4A
Potassium-transporting ATPase subunit beta ATP4B
N(G),N(G)-dimethylarginine dimethylaminohydrolase 1 DDAH1

Referensi & Sumber

Synthesis reference: Rudolf Linder, "Freeze-dried pantoprazole preparation and pantoprazole injection." U.S. Patent US20030003058, issued January 02, 2003.
Artikel (PubMed)
  • PMID: 21694841
    Mathews S, Reid A, Tian C, Cai Q: An update on the use of pantoprazole as a treatment for gastroesophageal reflux disease. Clin Exp Gastroenterol. 2010;3:11-6. Epub 2010 Jan 20.
  • PMID: 29657605
    Dabrowski A, Stabuc B, Lazebnik L: Meta-analysis of the efficacy and safety of pantoprazole in the treatment and symptom relief of patients with gastroesophageal reflux disease - PAN-STAR. Prz Gastroenterol. 2018;13(1):6-15. doi: 10.5114/pg.2018.74556. Epub 2018 Mar 26.
  • PMID: 27840364
    Strand DS, Kim D, Peura DA: 25 Years of Proton Pump Inhibitors: A Comprehensive Review. Gut Liver. 2017 Jan 15;11(1):27-37. doi: 10.5009/gnl15502.
  • PMID: 11117653
    Jungnickel PW: Pantoprazole: a new proton pump inhibitor. Clin Ther. 2000 Nov;22(11):1268-93.
  • PMID: 23350044
    Shin JM, Kim N: Pharmacokinetics and pharmacodynamics of the proton pump inhibitors. J Neurogastroenterol Motil. 2013 Jan;19(1):25-35. doi: 10.5056/jnm.2013.19.1.25. Epub 2013 Jan 8.
  • PMID: 18433349
    Bardou M, Martin J: Pantoprazole: from drug metabolism to clinical relevance. Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):471-83. doi: 10.1517/17425255.4.4.471 .
  • PMID: 15498502
    Shin JM, Sachs G: Differences in binding properties of two proton pump inhibitors on the gastric H+,K+-ATPase in vivo. Biochem Pharmacol. 2004 Dec 1;68(11):2117-27. doi: 10.1016/j.bcp.2004.07.035.
  • PMID: 8793599
    Huber R, Hartmann M, Bliesath H, Luhmann R, Steinijans VW, Zech K: Pharmacokinetics of pantoprazole in man. Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S7-16.
Menampilkan 8 dari 15 artikel.

Contoh Produk & Brand

Produk: 509 • International brands: 1
Produk
  • Abbott-pantoprazole
    Tablet, delayed release • 20 mg • Oral • Canada • Generic • Approved
  • Abbott-pantoprazole
    Tablet, delayed release • 40 mg • Oral • Canada • Generic • Approved
  • Act Pantoprazole
    Tablet, delayed release • 40 mg • Oral • Canada • Approved
  • Ag-pantoprazole
    Tablet, delayed release • 40 mg • Oral • Canada • Generic • Approved
  • Ag-pantoprazole
    Tablet, delayed release • 20 mg • Oral • Canada • Generic • Approved
  • Ag-pantoprazole Sodium
    Tablet, delayed release • 40 mg • Oral • Canada • Generic • Approved
  • Ag-pantoprazole Sodium
    Tablet, delayed release • 20 mg • Oral • Canada • Generic • Approved
  • Apo-pantoprazole
    Tablet, delayed release • 20 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 509 produk.
International Brands
  • Pantozol

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