Last Updated on October 18, 2021 by Dr.Derek Fhisher
Most popular brand: Protonix
Active ingredient: Pantoprazole
Available dosage forms: 20, 40 mg
Purchase Pantoprazole without a prescription or Generic Protonix from 500mg.org and get excellent drug on reduced international costs. To purchase Protonix online will be to have much more privacy than what is available when taking a prescription to a drugstore that is local. 500mg.org offers you the possibility to purchase cheap Pantoprazole 20, 40 mg online and also find out more about Pantoprazole side effects, dosage info and drug interactions. Ask your pharmacist any questions you might have relating to Pantoprazole, especially if it’s new to you. Buy generic Protonix online at the best affordable cost from 500mg.org and get your Pantoprazole pills sent at your doorstep in time. Being able to buy Pantoprazole online or have other prescriptions filled online saves time, effort, and the price of an extended excursion. They have the power to compare prices more readily when individuals purchase Pantoprazole online. By contrast, the best online sources for prescription drugs like Pantoprazole frequently have wide-ranging drug information right on the website, so consumers can get answers to their questions quickly and readily when they purchase Pantoprazole 20, 40 mg online, and they can easily print out the information for future reference. Nevertheless, accessibility to a licensed pharmacist is only a phone call away when individuals buy Pantoprazole online with trusted sources that are on-line.
What is Pantoprazole?
Pantoprazole is a “proton pump” inhibitor (H+,K+-ATPase). It reduces basal and stimulated (regardless of the type of stimulus) gastric hydrochloric acid secretion.
Pantoprazole is a substituted benzimidazole, which inhibits hydrochloric acid secretion in the stomach by specific proton pump blockade of the parietal cells. Pantoprazole is transformed into its active form in the acid environment in the parietal cells, where it inhibits the enzyme H+-K+-ATPase, that is, it blocks the final stage of hydrochloric acid production in the stomach. Inhibition is dose-dependent; pantoprazole suppresses both basal and stimulated acid secretion. In most patients, symptoms disappear within 2 weeks. As with other proton pump inhibitors (PPIs) and H2-receptor inhibitors, pantoprazole reduces acidity in the stomach and thus increases gastrin secretion in proportion to the decrease in acidity. The increase in gastrin secretion is reversible. Because pantoprazole binds the enzyme distally to the cell receptor, it can inhibit hydrochloric acid secretion independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same with oral and IV administration of the drug.
Proton pump inhibitors are among the most widely used medications in the United States. They have made a dramatic difference in the treatment of diseases associated with increased secretion of hydrochloric acid. The first drug from this group of drugs appeared in the U.S. in 1989. Over the elapsed time, the indications for their use have expanded considerably.
The mechanism of action of pantoprazole is the same as that of other drugs from the group of proton pump inhibitors.
Pantoprazole is the first of the proton pump inhibitors that is available for both oral and intravenous use.
In the United States, pantoprazole is considered the primary indication for the treatment of erosive esophagitis associated with gastroesophageal reflux disease.
formula: C16H15F2N3O4S, chemical name: 5 – (difluoromethoxy) – 2 – [[[(3,4 – dimethoxy – 2 – pyridinyl) methyl] sulfinyl] – 1H – benzimidazole (as sodium salt).
Pharmacological group: Organotropic agents / gastrointestinal agents / proton pump inhibitors.
Mode of action: anti-ulcer.
Pantoprazole accumulates in the tubules of the parietal cells of the stomach and is converted into cyclic sulfenamide (the active form of the drug), which selectively interacts with H+ – K+ – ATPase (forms a covalent bond and inhibits it). Thus, pantoprazole provides transport of hydrogen ions into the lumen of the stomach by the parietal cells and blocks the terminal phase of hydrochloric acid. Pantoprazole dose-dependently stimulated and permanently suppressed basal hydrochloric acid production. In in vivo studies, mean effective doses ranged from 0.2 to 2.4 mg/kg. The maximum effect of pantoprazole is only possible in a strongly acidic environment (pH = 3). Pantoprazole is practically inactive at higher pH values. Pantoprazole has antibacterial activity against Helicobacter pylori and also contributes to the effects of other drugs on H. pylori.
IPC of pantoprazole is 128 mg/l. The therapeutic effect of single drug administration is rapid and lasts for several days. Pantoprazole quickly reduces symptoms and promotes healing of duodenal ulcers. When 40 mg is taken, pH>3 lasts more than 19 hours. After 2 weeks of treatment, 89% of patients had complete healing of duodenal ulcers. After 4 weeks of treatment complete healing of gastric ulcers was observed in 88% of patients. Recurrence rate is 55% after treatment of peptic ulcers. After 4 weeks of therapy 82% of patients with gastroesophageal reflux disease of 2 – 3 stages have complete remission, after 8 weeks – 92%. In 4 weeks of therapy in 57% of children 6-13 years old with gastroesophageal reflux disease of 1c/stage 2 full endoscopic remission is achieved. During 4-8 weeks of therapy, plasma gastrin levels increased 1.5-fold. Maintenance treatment of patients with peptic ulcer disease was accompanied by a slight increase in the number of enterochromaffin-like (ECL) cells.
Experimental studies of carcinogenicity show that long-term use of pantoprazole is associated with an increased probability of ECL-cell hyperplasia and development of carcinomas and adenomas of the liver, carcinoid of the stomach, neoplastic processes in the thyroid gland.
Pantoprazole is completely and rapidly absorbed when taken orally. The absolute bioavailability of pantoprazole is 70-80%. Maximum concentration is reached after 2-4 hours. Plasma proteins are 98% bound to pantoprazole. The elimination half-life is 0.9-1.9 hours, the clearance is 0.1 l/h/kg, the volume of distribution is 0.15 l/kg. Pantoprazole is excreted in breast milk; it penetrates the blood-brain barrier very poorly. When taken with antacids or at maximum concentration, AUC and bioavailability are not altered. Proportional increase in dose increases maximum concentration and AUC. Clearance and elimination half-life values are independent of dose. Pantoprazole is metabolized in the liver by oxidation, conjugation, dealkylation. The drug has a low affinity to cytochrome P450, CYP2C19 and CYP3A4 isoenzymes are mainly involved in metabolism. The main metabolites of pantoprazole are -2 demethylpantoprazole sulfated conjugate (with a half-life of 1.5 hours). Pantoprazole does not accumulate. Metabolites are mainly excreted in the urine (82%) and are detected in small amounts in the feces. In patients with liver cirrhosis the elimination half-life is increased to 7-9 hours, in renal insufficiency it is increased slightly, but the elimination half-life of the main metabolite is 2-3 hours. Maximum concentration and AUC are slightly higher in older age group.
Exacerbation of peptic ulcer disease (including refractory to histamine H2 – receptor treatment or associated with the use of non-steroidal anti-inflammatory drugs).
Zollinger-Ellison syndrome of gastroesophageal reflux disease (moderate and severe forms). Zollinger-Ellison syndrome occurs when a tumor in the stomach or pancreas causes the stomach to produce too much gastrin. Gastrin stimulates the stomach to produce acid. People with Zollinger-Ellison syndrome may also have a tumor in the pancreas, small bowel, or esophagus.
Combined treatment of H. pylori eradication in patients with ulcer disease to reduce relapse rate.
How to use and dosage of pantoprazole
Pantoprazole ingested (not crush or dissolve, regardless of the meal), administered intravenously (only if oral administration is not possible). Monotherapy with gastroesophageal reflux disease, peptic ulcer disease – usually 40 mg / day, may increase the dose to 80 mg / day. The duration of treatment of duodenal ulcer is 2 weeks, gastroesophageal reflux disease and peptic ulcer stomach- 4 weeks. Eradication of Helicobacter pylori: use only in accordance with the recommended combinations; duration of treatment 7 days (maximum 14 days).
Before treatment pantoprazole is necessary to exclude malignant disease of the stomach and esophagus. Reflux disease should be confirmed endoscopically. Do not use pantoprazole in patients with non-ulcer dyspepsia origin. Elderly patients and for violations of renal function the dose of 40 mg / day are not recommended to exceed. In severe hepatic insufficiency dosage regimen must be adjusted under the supervision of a physician.
Inside, before a meal (usually before breakfast), with the necessary amount of water. The tablets should be swallowed whole, without chewing.
Adults and adolescents over 12 years of age.
Treatment of gastroesophageal reflux disease, reflux esophagitis:
1 tablet of pantoprazole per day. In individual cases, the dose may be increased to 2 pantoprazole tablets per day. It usually takes 4 weeks to treat reflux inflammation of the esophagus. If necessary, the duration of treatment is increased to 8 weeks.
Eradication of Helicobacter pylori (in complex therapy):
In Helicobacter pylori-positive patients with gastric and duodenal ulcers, eradication of the microorganism should be achieved with combination therapy.
Reference should be made to official local guidelines (e.g., national guidelines) regarding bacterial resistance and the appropriate prescription and use of antibacterial agents. Depending on the spectrum of resistance, the following combinations may be recommended:
a. One tablet of pantoprozole twice daily
– 1000 mg amoxicillin twice daily
– 500 mg clarithromycin twice daily
b. One tablet of pantoprazole twice daily
– 400-500 mg metronidazole (or 500 mg tinidazole) twice daily
– 250-500 mg clarithromycin twice daily
c. One tablet of pantoprazole twice daily
– 1000 mg amoxicillin twice a day
– 400-500 mg metronidazole (or 500 mg tinidazole) twice a day.
During eradication therapy, the second tablet of pantoprazole should be taken 1 hour before the evening meal. Combination therapy is usually carried out for 7 days and can be continued for another 7 days for a total duration of 14 days. Further therapy with pantoprazole using doses recommended for duodenal and gastric ulcers is then indicated to ensure healing of the ulcers.
If combination therapy is not indicated (Helicobacter pylori-negative patient), the following dosing regimens for pantoprazole monotherapy should be followed.
Treatment of peptic ulcer:
1 tablet of pantoprazole per day. In individual cases, the dose may be increased to 2 pantoprazole tablets per day. It usually takes 4 weeks to treat a peptic ulcer. If necessary, the duration of treatment is increased to 8 weeks.
Treatment of duodenal ulcer:
1 tablet of pantoprazole per day. In individual cases the dose can be increased to 2 pantoprazole tablets per day. It usually takes 2 weeks to treat a duodenal ulcer. If necessary, the duration of treatment is increased to 4 weeks.
Zollinger-Ellison syndrome and other pathological hypersecretory diseases:
For long-term treatment of Zollinger-Ellison syndrome and other pathological hypersecretory disorders, treatment begins with a daily dose of 80 mg (2 40 mg pantoprazole tablets). Thereafter, the dose can be increased or decreased as needed based on gastric acid secretion rates. If the daily dosage is over 80 mg, the dose should be divided and used twice daily. A temporary increase in dosage above 160 mg is possible, but only for the time necessary to adequately suppress hydrochloric acid secretion. The duration of treatment of Zollinger-Ellison syndrome and other pathological hypersecretory disorders is not limited and may be conducted according to clinical necessity.
Children under 12 years of age:
Pantoprazole is not recommended for use in children younger than 12 years of age due to limited safety and efficacy data in this age group.
Special patient groups
Patients with hepatic impairment
In patients with severe hepatic impairment the daily dose of pantoprazole 20 mg should not be exceeded (other 20 mg preparations should be used). During treatment with pantoprazole, plasma liver enzyme levels should be monitored in such patients. If liver enzyme activity is elevated, pantoprazole should be discontinued. Pantoprazole should not be used as part of a combination therapy for eradication of Helicobacter pylori in patients with moderate or severe hepatic impairment, since there are currently no data on the efficacy and safety of pantoprazole in such patients.
Patients with impaired renal function
No dosage adjustment is required in patients with impaired renal function. It should not be used as part of combined therapy for eradication of Helicobacter pylori with impaired renal function because currently there are no data on efficacy and safety of pantoprazole in combined therapy in these patients.
No dose adjustment is required.
Hypersensitivity, liver cirrhosis and hepatitis, which are accompanied by severe hepatic failure.
Violations of the functional state of the liver, the age of 6 years (no experience of use of the drug).
Pregnancy and breastfeeding
When pregnancy is possible the use of pantoprazole only under strict indications, where the benefits to the mother above the possible risk to the fetus. At the time of treatment pantoprazole must stop breastfeeding.
Pantoprazole Canon may only be used during pregnancy if the benefit to the mother outweighs the possible potential risk to the fetus.
Experimental studies have shown that pantoprazole is excreted with the breast milk, therefore if Pantoprazole Canon should be used, breastfeeding should be discontinued.
Adverse effects of pantoprazole
digestive system: diarrhea, dry mouth, nausea, increased appetite, belching, flatulence, vomiting, abdominal pain, increased liver transaminases activity, constipation, gastrointestinal carcinoma;
sense organs and the nervous system: headache, asthenia, somnolence, dizziness, insomnia, nervousness, tremor, depression, paresthesia, visual disturbances, photophobia, tinnitus;
urogenital system: swelling, hematuria, impotence;
skin: acne, alopecia, exfoliative dermatitis;
allergic reactions: urticaria, rash, angioedema itching;
other: myalgia, hyperglycemia, fever, hyperlipoproteinemia, eosinophilia, hypercholesterolemia.
The interaction of pantoprazole with other substances
Pantoprazole may reduce the pH – dependent absorption of ketoconazole and other drugs (absorption depends on the level of pH). Pantoprazole is compatible with drugs that are metabolized by the enzyme system involving cytochrome P450: diazepam, phenazepam, digoxin, carbamazepine, theophylline, diclofenac, piroxicam, naproxen, phenytoin, nifedipine, metoprolol, warfarin, ethanol. Pantoprazole on the effectiveness of hormonal contraceptives is not affected.
When pantoprazole overdose symptoms are not described. If you suspect an overdose of pantoprazole must be symptomatic and supportive treatment; hemodialysis ineffective.