Pantoprazole is a drug belonging to the class of proton pump inhibitors (IPP), whose chemical structure is very similar to the progenitor of this pharmaceutical category: omeprazole.
Pantoprazole is marketed under the name of several registered specialties, including Pantecta ®, Pantopan ®, Pantorc ® and Peptazol ®. The name of the generic drug is the same as that of the active ingredient: pantoprazole.
Pantoprazole is a pro-drug that acts after protonating and activating in the parietal cells of the stomach; at this level, it covalently binds to cysteine residues that are on the luminal surface of the enzyme H + / K + / ATPase, in turn linked to the proton pump which is inhibited by this bond leading to the blocking of hydrochloric acid secretion in the stomach.
Pantoprazole, at neutral pH, is a weaker proton pump inhibitor (about 3 times) than omeprazole, while at acid pH the above inhibitory power is greater than that of omeprazole and lansoprazole. In the treatment of gastritis, the efficacy of pantoprazole on the healing of gastric ulcer was similar to that of omeprazole, while in the treatment of duodenal ulcer pantoprazole was more effective than omeprazole in terms of scarring and decreasing secretion sour.
Pantoprazole is quickly absorbed in the gastrointestinal tract after oral administration, therefore the presence of food slows its absorption.
Pantoprazole has a half-life ranging from 0.9 to 1.9 hours; however this characteristic does not influence its duration of action, since pantoprazole, like all IPPs, irreversibly inhibits the proton pump until the synthesis of a new proton pump.
Posology and method of use
Pantoprazole is administered in the form of gastro-resistant tablets, since it is an amphoteric molecule that would undergo degradation in the acidic environment of the stomach.
Before the prescription it is very important to make sure that the patient is not suffering from a neoplastic ulcer (malignant ulcer), especially if he complains of a sudden drop in body weight, accompanied by recurrent dysphagia or vomiting; pantoprazole, in fact, relieving the symptoms of this fearsome disease would hide the true nature of the ulcer and make the correct diagnosis more difficult.
When doses of pantoprazole between 40 and 60 mg / day are administered there is a reduction in gastric secretion of around 97% for the 24 hours following the intake.
The following recommendations on the amount of drug to be used in the treatment of different diseases are only an average of the doses commonly used in therapy. In fact, the doses to be taken differ from patient to patient; therefore, even if your doses differ from those indicated in the article, do not change them for any reason, unless your doctor explicitly advises you.
In the treatment of gastritis, 40 mg / day of pantoprazole is used in a single administration in the morning, before breakfast, for 4 weeks. In severe cases, if the gastritis has not healed, treatment can continue up to 8 weeks.
In the treatment of duodenal ulcer 40 mg / day of pantoprazole is administered in a single dose in the morning, before breakfast, for 2 weeks. If the ulcer does not heal, you can extend the treatment for another two weeks, for a total of 4 weeks; alternatively the dose can be increased up to 80 mg / day.
For gastroesophageal reflux disease, 20 mg / day of pantoprazole is administered in a single dose, before or during breakfast, for 2-4 weeks, while in more severe cases the dose can be increased up to 40 mg / day and prolonged treatment up to 8 weeks. In maintenance therapy the dose to be taken is 20 mg / day, which in case of relapse can be doubled to 40 mg / day, and then reduced again to 20 mg / day once the recurrence is resolved.
In the eradication treatment of Helicobacter pylori, with the triple therapy, 80 mg / day of pantoprazole is used, divided into two administrations together with antibiotics: claritomycin 1000 mg / day, also divided into two daily administrations, and amoxicillin 2000 mg / day (or metronidazole 1000 mg / day), always divided into two different daily assumptions.
For the prophylaxis of gastritis caused by the continuous use of Non Steroidal Anti-inflammatory Drugs, 20 mg / day of pantoprazole is used in a single administration before breakfast.
In the treatment of Zollinger-Ellison syndrome the attack dose is 80 mg of pantoprazole per day in a single morning dose; only later, based on the individual therapeutic response, is the dose most suitable for the individual patient decided. However, in elderly patients it is not advisable to exceed the dose of 40 mg / day.
Contraindications and warnings for use
The metabolization of pantoprazole, by the large family of CYP450 enzymes, involves a series of interactions with other drugs that are metabolized by the same enzymatic family. One of the drugs to watch out for is clopidogrel. Proton pump inhibitors reduce the bioavailability of clopidogrel by inhibiting the metabolizing isoenzyme, converting it into the active form (even clopidogrel is a pro drug). However, pantoprazole is the proton pump inhibitor that has the least inhibiting effect on the anti-aggregating activity of clopidogrel.
Another drug that becomes less bioavailable when taken together with pantoprazole is Azatanavir; as the absorption of this drug requires an acid stomach pH, it is not recommended to take it together with pantoprazole.
Thanks to an animal study, it was confirmed that when Diazepam is taken together with pantoprazole, the therapeutic efficacy of diazepam increases; therefore, it is advisable to take particular care when taking the two drugs at the same time.
Taking pantoprazole together with Warfarin may lead to an increase in the anticoagulant effect of the latter, due to the metabolic interactions between the two active ingredients; therefore, monitoring of patients taking these drugs at the same time is advised, especially care should be taken when taking pantoprazole is discontinuous.
In patients with severely reduced liver function it is not recommended to take more than 20 mg / day of pantoprazole; alternatively you can take 40 mg / day on alternate days.
Pregnancy and breastfeeding
The use of proton pump inhibitors during pregnancy occurs for the treatment of gastroesophageal reflux disease. From in vivo clinical studies regarding the intake of pantoprazole during pregnancy, there was no adverse effect on the fetus or peri or postnatal toxicity on it.
A rat study showed that pantoprazole is excreted in breast milk up to a value that does not exceed 0.02% of the dose taken. It has also been seen that the drug passes the placenta and that this passage is intensified as the pregnancy progresses; however, certain data are not available for humans. Therefore, before starting therapy with pantoprazole, it is advisable to take into account the advantages of the treatment for the mother and any risks that this treatment may entail for the fetus.
Side and unwanted effects
The most common side effects of pantoprazole include, as with all proton pump inhibitors, those related to the gastrointestinal system such as: diarrhea, nausea, vomiting, flatulence and dry mouth. Among these side effects the most widespread in pantoprazole-treated patients is diarrhea, which occurs in about 4% of subjects. A study carried out on the use of lansoprazole, omeprazole and pantoprazole showed that pantoprazole causes less side effects than lansoprazole but more than omeprazole.
After the gastrointestinal side effects, the most frequent are the central ones such as: headache, dizziness, drowsiness, tiredness and nervousness. Of the aforementioned side effects, the most manifest is headache, which affects about 1.4% of patients treated with pantoprazole.
Other side effects that may occur, but with an even lower incidence, are dermatological ones such as itching and skin rashes, which have been reported in about 0.5% of patients taking pantoprazole.
