(British Approved Name, US Adopted Name, rINN)
INNs in main languages (French, Latin, Russian, and Spanish):
(British Approved Name Modified, US Adopted Name, rINNM)
INNs in main languages (French, Latin, Russian, and Spanish):
Pharmacopoeias. In China, and Europe.
European Pharmacopoeia, 6th ed. (Pantoprazole Sodium Sesquihydrate). A white or almost white powder. Freely soluble in water and in alcohol practically insoluble in hexane. Protect from light.
Stability. A suspension of pantoprazole 2 mg/mL in sterile water and sodium bicarbonate was deemed to be physically and chemically stable in amber polyethylene terephthalate bottles for 62 days at 2° to 8°.
Adverse Effects and Precautions
Incidence of adverse effects
In a postmarketing surveillance study of the 6-month period after the launch of pantoprazole in England (UK), the adverse effects reported most frequently were diarrhoea, nausea, and headache. Other effects included malaise or lassitude, rash, other gastrointestinal disturbances, myalgia, and oedema.
Effects on the blood
For a report of thrombocytopenia with pantoprazole, see under Omeprazole.
Effects on the kidneys
For reports of interstitial nephritis associated with pantoprazole.
Effects on the skin
For mention of skin reactions to pantoprazole.
As for Omeprazole.
For reference to a lack of effect of pantoprazole on diazepam, see Gastrointestinal Drugs, and for a lack of effect on theophylline. Licensed product information states that there are reports of increased prothrombin time in patients taking pantoprazole and warfarin, but for reports suggesting a lack of effect on warfarin. For a report of severe generalised myalgia and bone pain attributed to the use of methotrexate with pantoprazole, see Gastrointestinal Drugs.
Pantoprazole is rapidly absorbed and peak plasma-pantoprazole concentrations are achieved about 2 to 2.5 hours after an oral dose. The oral bioavailability is about 77% with the enteric-coated tablet formulation, and does not vary after single or multiple doses. Pantoprazole is about 98% bound to plasma proteins. It is extensively metabolised in the liver, primarily by the cytochrome P450 isoenzyme CYP2C19, to desmethyl-pantoprazole small amounts are also metabolised by CYP3 A4, CYP2D6, and CYP2C9.
Metabolites are excreted mainly (about 80%) in the urine, with the remainder being excreted in faeces via the bile. The terminal elimination half-life is about 1 hour, and is prolonged in hepatic impairment the half-life in patients with cirrhosis was 3 to 6 hours. Although the elimination half-life has been reported to be 3.5 to 10 hours in slowmetabolisers (see also Metabolism under Omeprazole), minimal accumulation occurs with once-daily dosing.
A suspension of pantoprazole in sodium bicarbonate solution was rapidly absorbed, and peak plasma concentrations were comparable to that of the tablet. However, bioavailability of the suspension was about 25% lower than that of the tablet the amount of sodium bicarbonate used may affect the bioavailability.
Uses and Administration
Pantoprazole is a proton pump inhibitor with actions and uses similar to those of omeprazole. It is given as the sodium salt but doses are expressed in terms of the base. Pantoprazole sodium 11.28 mg is equivalent to about 10 mg of pantoprazole. Once-daily doses should be taken in the morning. In the treatment of gastro-oesophageal reflux disease, the usual oral dose is 20 to 40 mg once daily for 4 weeks, increased to 8 weeks if necessary in the USA, up to 16 weeks of therapy is permitted for healing of erosive oesophagitis. For maintenance therapy, treatment can be continued with 20 to 40 mg daily. Alternatively, for recurring symptoms, an on-demand regimen of 20 mg daily may be given.
The usual dose for the treatment of peptic ulcer disease is 40 mg once daily. Treatment is usually given for 2 to 4 weeks for duodenal ulceration, or 4 to 8 weeks for benign gastric ulceration. For the eradication of Helicobacter pylori pantoprazole may be combined with two antibacterials in a 1-week triple therapy regimen. Effective regimens include pantoprazole 40 mg twice daily combined with clarithromycin 500 mg twice daily and amoxicillin 1 g twice daily, or combined with clarithromycin 250 mg twice daily and metronidazole 400 mg twice daily. Patients who require prophylaxis for NSAID-associated ulceration may take 20 mg daily. In the treatment of pathological hypersecretory states such as the Zollinger-Ellison syndrome, the initial dose is 80 mg daily, adjusted as required. Doses of up to 240 mg daily have been used. Daily doses greater than 80 mg should be given in 2 divided doses.
Pantoprazole may also be given intravenously, as the sodium salt, over 2 to 15 minutes, either as a slow injection or a short-term infusion. For peptic ulceration or gastro-oesophageal reflux disease, the recommended dose is 40 mg daily. A dose of 80 mg once or twice daily may be used for Zollinger-Ellison syndrome up to 240 mg daily may be given in divided doses. Patients should be switched to oral therapy as soon as possible.
Doses of pantoprazole may need to be reduced in patients with hepatic impairment (see below).
The safety and tolerability profiles of intravenous pantoprazole given in 10 mL of sodium chloride 0.9% over 2 minutes were similar to those given over 15 minutes in 100 mL.
Administration in hepatic impairment
Dosage of pantoprazole may need to be reduced in severe hepatic impairment, or doses given only on alternate days. A maximum dose of 20 mg daily orally or intravenously, or 40 mg orally on alternate days, has been suggested. Doses above 40 mg daily have not been studied in patients with hepatic impairment. Liver enzymes should be monitored during therapy, and pantoprazole should be stopped if elevations occur.
Administration in renal impairment
Most studies have not found the pharmacokinetics of pantoprazole to be altered in patients with renal impairment and licensed drug information in the UK and US generally does not recommend dosage adjustment in this group however some UK sources, including the BNF, suggest that a maximum dose of 40 mg daily should be observed.
Argentina: Gastromax Pangest Pantocas Pantop Pantus Peptazol Sipar Supracam Ulserch Zurcal
Austria: Pantoloc Zurcal
Belgium: Pantozol Zurcale
Brazil: Gastropan Noprop Pantocal Pantopaz Pantozol Pantrat Peptovit Ziprol Zurcal
Canada: Panto Pantoloc
Chile: Singastril Ulcemex Zurcal
Czech Republic: Apo-Panto Controloc Nolpaza Panogastin
France: Eupantol Inipomp
Germany: Pantozol Pantozol-Rifun Rifun
Greece: Controloc Pantosec Zurcazol
Hong Kong: Pantoloc
Hungary: Controloc Nolpaza Pantacid Zimpax
India: Eracid Pantodac Pantop Pantosec Pentaloc Praize
Italy: Pantecta Pantopan Pantorc Peptazol
Mexico: Pantozol Prazolan Tecta Zolpra Zurcal
The Netherlands: Pantorc Pantozol
New Zealand: Somac
Philippines: Pantoloc Ulcepraz
Portugal: Apton Pantoc Praoz Zurcal
South Africa: Controloc Pantocid Pantoloc Topzole
Spain: Anagastra Pantecta Pantocarm Ulcotenal
Switzerland: Pantozol Zurcal
Turkey: Panthec Panto Pantpas Pulcet
India: Pantosec D Praize-D
The Netherlands: PantoPAC