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- Description en
- PANZEL INJECTION (Pantoprazole Sodium for Injection [Lyophilized]) Composition: One vial contains: Pantoprazole Sodium Sesquihydrate U.S.P., equivalent to 40 mg Pantoprazole. Pharmacological Classification Pharmacotherapeutic Group: Proton pump inhibitors. Pharmacodynamic Properties: Pantoprazole is a substituted benzimidazole which reduces the secretion of hydrochloric acid in the stomach by irreversibly blocking the proton pumps of the parietal cells. Pantoprazole is converted to its active form in the acidic environment of the parietal cells, where it inhibits the enzyme H+/K+-ATPase, the final step in the production of hydrochloric acid in the stomach. The inhibition is dose-dependent and affects both basal and stimulated acid secretion. Symptoms are relieved in most patients within 2 weeks. Like other proton pump and H2 receptor inhibitors, treatment with pantoprazole reduces gastric acidity and, proportionally to the reduction in acidity, increases gastrin levels. The increase in gastrin levels is reversible. Since pantoprazole binds to the enzyme distally to the cellular receptors, it can inhibit the secretion of hydrochloric acid independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same whether the product is taken orally or intravenously. When pantoprazole is taken on an empty stomach, gastrin values increase. In most cases, these values do not exceed the upper limit of normal with short-term use. During long-term treatment, gastrin levels double in most cases. However, excessive increases occur only in isolated cases. In very rare cases, a slight to moderate increase in the number of specific endocrine (ECL) cells in the stomach (similar to adenomatoid hyperplasia) is observed during long-term treatment. However, according to studies conducted, the formation of carcinoid precursors (atypical hyperplasia) or gastric carcinoids, which were observed in animal experiments, has not been observed in humans. Based on the results of animal studies, the effect on thyroid endocrine parameters cannot be completely ruled out with long-term treatment with pantoprazole for more than one year. Pharmacokinetic Properties: Pharmacokinetics do not change after single or repeated administration. In the dose range of 10 to 80 mg, the kinetics of pantoprazole in plasma are linear after both oral and intravenous administration. Distribution. Pantoprazole is bound to plasma proteins by approximately 98%. The volume of distribution is approximately 0.15 L/kg. Elimination: The substance is almost completely metabolized in the liver. The main metabolic pathway is demethylation via CYP2C19, followed by sulfate conjugation; other metabolic pathways include oxidation via CYP3A4. The terminal half-life is approximately 1 hour, and the clearance is approximately 0.1 L/h/kg. Several cases of delayed elimination have been observed in some subjects. Due to the specific binding of pantoprazole to the proton pumps of the parietal cells, the half-life is not related to the longer duration of action (inhibition of acid secretion). Renal elimination is the main route of elimination of pantoprazole metabolites (approximately 80%); the remainder is excreted in the feces. The main metabolite in serum and urine is desmethylpantoprazole, which is conjugated with sulfate. The half-life of the main metabolite (approximately 1.5 hours) is slightly longer than that of pantoprazole. Characteristics in Special Groups of Patients/Subjects: Approximately 3% of the European population lacks the functional CYP2C19 enzyme and is referred to as poor metabolizers. In these individuals, pantoprazole metabolism is mainly catalyzed by CYP3A4. After a single dose of 40 mg pantoprazole, the area under the plasma concentration-time curve is approximately 6 times higher in poor metabolizers than in subjects with functional CYP2C19 enzyme (extensive metabolizers). The mean peak plasma concentration increases by approximately 60%. These data are dose-independent. No dose reduction is necessary when administering pantoprazole to patients with impaired renal function (including patients on dialysis). The half-life of pantoprazole is short, similar to healthy individuals. Only a very small amount of pantoprazole is dialyzed. Although the main metabolite has a moderately slow half-life (2-3 hours), excretion is rapid, so no accumulation occurs. Although in patients with liver cirrhosis (Child-Pugh class A and B) the half-life increases to 7-9 hours, and AUC values increase 5-7-fold, the maximum serum concentration increases only slightly, by 1.5-fold compared to healthy subjects. The slight increase in AUC and Cmax in elderly volunteers compared to younger volunteers also has no clinical significance. Pediatric Population: In children aged 2 to 16 years, after a single intravenous administration of pantoprazole at a dose of 0.8 or 1.6 mg/kg body weight, no significant correlation between pantoprazole clearance and age or body weight was observed. AUC and volume of distribution were consistent with data in adults. Indications: Panzell Injection is used for the following indications: - Reflux esophagitis - Gastric and duodenal ulcers - Zollinger-Ellison syndrome and other pathological hypersecretory conditions. Dosage and Administration: Gastric and duodenal ulcers, reflux esophagitis: The recommended intravenous dose is one vial (40 mg) of pantoprazole per day. Zollinger-Ellison syndrome and other pathological hypersecretory conditions: For long-term management of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, patients should initiate treatment with pantoprazole 80 mg intravenously per day. Subsequently, the dose may be increased or decreased as needed, according to the rate of gastric acid secretion. If doses greater than 80 mg per day are necessary, the dose should be divided and administered twice daily. Temporary increases in pantoprazole dosage above 160 mg are possible, but should not be used for longer than necessary to achieve adequate acid control. In cases where rapid acid control is needed, an initial dose of 2 x 80 mg pantoprazole intravenously is sufficient to reduce acid output to the target range (<10 mEq/h) within one hour in most patients. Pediatric Population: Experience in children is limited. Therefore, pantoprazole intravenously is not recommended in patients under 18 years of age until appropriate data are available. Hepatic Impairment: In patients with severe hepatic impairment, the daily dose of pantoprazole should not exceed 20 mg (half of a 40 mg vial of pantoprazole). Renal Impairment: No dose adjustment is necessary in patients with impaired renal function. Elderly: No dose adjustment is necessary in elderly patients. Method of Administration: 10 ml of 0.9% sodium chloride for injection is used to obtain the reconstituted solution. The prepared solution can be used immediately or mixed with 100 ml of 0.9% sodium chloride for injection solution or 50 mg/ml glucose (5%) for injection solution. The prepared solution should be used within 12 hours. The prepared solution is administered intravenously over 2-15 minutes. Contraindications: Hypersensitivity to the active substance, to substituted benzimidazoles or to any of the excipients. Special Warnings and Precautions for Use: Development of alarm symptoms: In the event of any alarm symptoms (e.g., significant unintentional weight loss, recurrent vomiting, dysphagia, hematemesis, anemia or melena) and in the presence or suspicion of a gastric ulcer, the possibility of a malignant neoplasm must be excluded, as treatment with pantoprazole may mask symptoms and thus hinder correct diagnosis. If symptoms persist despite adequate treatment, further investigation is required. Hepatic Impairment: In patients with severe hepatic impairment, monitoring of liver enzymes is necessary. If liver enzyme activity increases, treatment should be discontinued. Concomitant use of Atazanavir: Concomitant use of Atazanavir and proton pump inhibitors is not recommended. If concomitant use of Atazanavir and proton pump inhibitors is necessary, close clinical monitoring (e.g., determination of viral load) is required, the dose of Atazanavir is increased to 400 mg and used in combination with 100 mg Ritonavir. The daily dose of pantoprazole should not exceed 20 mg. Bacterial Gastrointestinal Infections: Pantoprazole, like other proton pump inhibitors, may increase the number of bacteria normally present in the upper gastrointestinal tract. Treatment with proton pump inhibitors may slightly increase the risk of gastrointestinal infections caused by bacteria (e.g., Salmonella and Campylobacter and C. difficile). Sodium: This medicinal product contains less than 1 mmol (23 mg) of sodium per dose, i.e., it is practically "sodium-free". Interactions with Other Medicinal Products and Other Forms of Interaction: Effect of Pantoprazole on the Absorption of Other Medicinal Products: Due to deep and prolonged inhibition of gastric acid secretion, pantoprazole may reduce the absorption of medicinal products whose bioavailability is pH-dependent, e.g., some azole antifungals, including ketoconazole, itraconazole, posaconazole, and other medicinal products, e.g., erlotinib. Coumarin Anticoagulants (Phenprocoumon or Warfarin): In clinical pharmacokinetic studies, no interaction was observed with concomitant use of phenprocoumon or warfarin, however, in the post-marketing period, several isolated cases of changes in International Normalized Ratio (INR) have been reported during concomitant treatment. Therefore, in patients treated with coumarin anticoagulants (e.g., phenprocoumon or warfarin), monitoring of prothrombin time/INR is recommended when initiating, discontinuing, or irregularly using pantoprazole. Methotrexate: In some patients, concomitant use of high doses of methotrexate (e.g., 300 mg) and proton pump inhibitors has led to increased methotrexate levels. Therefore, when using high doses of methotrexate, e.g., in cancer and psoriasis, it may be temporarily necessary to discontinue pantoprazole. Other Interaction Studies. Pantoprazole is metabolized in the liver by the cytochrome P450 enzyme system. The main metabolic pathway is demethylation by CYP2C19; other metabolic pathways include oxidation by CYP3A4. Fertility, Pregnancy and Lactation: Pregnancy: There are no adequate data on the use of pantoprazole in pregnant women. Animal studies have shown reproductive toxicity. The potential risk to humans is unknown. Pantoprazole should not be used during pregnancy, except in cases of extreme necessity. Breastfeeding: Animal studies have shown that pantoprazole is excreted into breast milk. Therefore, the decision to continue/discontinue breastfeeding or to continue/discontinue therapy with pantoprazole should be made taking into account the benefits of breastfeeding for the child and the benefits of therapy with pantoprazole for the woman. Effects on Ability to Drive and Use Machines: Side effects such as dizziness and visual disturbances may occur. In such cases, patients should not drive or operate machinery. Undesirable Effects: Headache and complaints from the gastrointestinal tract, such as upper abdominal pain, diarrhea, constipation or flatulence. Complaints usually decrease with continued treatment. There are reports of allergic reactions such as skin rash, itching and in isolated cases also urticaria, angioneurotic edema or anaphylactic shock. Less frequent are reports of nausea, dizziness or visual disturbances (blurred vision). In isolated cases, peripheral edema, depression, fever or myalgia have been reported. Overdose: Symptoms of overdose in humans are not known. Doses up to 240 mg administered intravenously over 2 minutes are well tolerated. Pantoprazole is highly bound to plasma proteins, making it difficult to eliminate by dialysis. In case of overdose, symptomatic and supportive therapy should be carried out if clinical signs of intoxication develop; there are no other specific recommendations. Shelf Life: Unopened vial: 3 years. After reconstitution, or after reconstitution and dilution, the solution is chemically and physically stable for 12 hours at 25°C. From a microbiological point of view, the product should be used immediately. Storage: Store in a dark and dry place, at a temperature not exceeding 25°C. Protect from light and moisture. Keep out of reach of children. Dispensing Category: Pharmaceutical Product Group II, dispensed with prescription form No. 3.
- Active
- pantoprazole
What is it?
PANZEL INJECTION (Pantoprazole Sodium for Injection [Lyophilized]) Composition: One vial contains: Pantoprazole Sodium Sesquihydrate U.S.P., equivalent to 40 mg Pantoprazole. Pharmacological Classification Pharmacotherapeutic Group: Proton pump inhibitors. Pharmacodynamic Properties: Pantoprazole is a substituted benzimidazole which reduces the secretion of hydrochloric acid in the stomach by irreversibly blocking the proton pumps of the parietal cells. Pantoprazole is converted to its active form in the acidic environment of the parietal cells, where it inhibits the enzyme H+/K+-ATPase, the final step in the production of hydrochloric acid in the stomach. The inhibition is dose-dependent and affects both basal and stimulated acid secretion. Symptoms are relieved in most patients within 2 weeks. Like other proton pump and H2 receptor inhibitors, treatment with pantoprazole reduces gastric acidity and, proportionally to the reduction in acidity, increases gastrin levels. The increase in gastrin levels is reversible. Since pantoprazole binds to the enzyme distally to the cellular receptors, it can inhibit the secretion of hydrochloric acid independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same whether the product is taken orally or intravenously. When pantoprazole is taken on an empty stomach, gastrin values increase. In most cases, these values do not exceed the upper limit of normal with short-term use. During long-term treatment, gastrin levels double in most cases. However, excessive increases occur only in isolated cases. In very rare cases, a slight to moderate increase in the number of specific endocrine (ECL) cells in the stomach (similar to adenomatoid hyperplasia) is observed during long-term treatment. However, according to studies conducted, the formation of carcinoid precursors (atypical hyperplasia) or gastric carcinoids, which were observed in animal experiments, has not been observed in humans. Based on the results of animal studies, the effect on thyroid endocrine parameters cannot be completely ruled out with long-term treatment with pantoprazole for more than one year. Pharmacokinetic Properties: Pharmacokinetics do not change after single or repeated administration. In the dose range of 10 to 80 mg, the kinetics of pantoprazole in plasma are linear after both oral and intravenous administration. Distribution. Pantoprazole is bound to plasma proteins by approximately 98%. The volume of distribution is approximately 0.15 L/kg. Elimination: The substance is almost completely metabolized in the liver. The main metabolic pathway is demethylation via CYP2C19, followed by sulfate conjugation; other metabolic pathways include oxidation via CYP3A4. The terminal half-life is approximately 1 hour, and the clearance is approximately 0.1 L/h/kg. Several cases of delayed elimination have been observed in some subjects. Due to the specific binding of pantoprazole to the proton pumps of the parietal cells, the half-life is not related to the longer duration of action (inhibition of acid secretion). Renal elimination is the main route of elimination of pantoprazole metabolites (approximately 80%); the remainder is excreted in the feces. The main metabolite in serum and urine is desmethylpantoprazole, which is conjugated with sulfate. The half-life of the main metabolite (approximately 1.5 hours) is slightly longer than that of pantoprazole. Characteristics in Special Groups of Patients/Subjects: Approximately 3% of the European population lacks the functional CYP2C19 enzyme and is referred to as poor metabolizers. In these individuals, pantoprazole metabolism is mainly catalyzed by CYP3A4. After a single dose of 40 mg pantoprazole, the area under the plasma concentration-time curve is approximately 6 times higher in poor metabolizers than in subjects with functional CYP2C19 enzyme (extensive metabolizers). The mean peak plasma concentration increases by approximately 60%. These data are dose-independent. No dose reduction is necessary when administering pantoprazole to patients with impaired renal function (including patients on dialysis). The half-life of pantoprazole is short, similar to healthy individuals. Only a very small amount of pantoprazole is dialyzed. Although the main metabolite has a moderately slow half-life (2-3 hours), excretion is rapid, so no accumulation occurs. Although in patients with liver cirrhosis (Child-Pugh class A and B) the half-life increases to 7-9 hours, and AUC values increase 5-7-fold, the maximum serum concentration increases only slightly, by 1.5-fold compared to healthy subjects. The slight increase in AUC and Cmax in elderly volunteers compared to younger volunteers also has no clinical significance. Pediatric Population: In children aged 2 to 16 years, after a single intravenous administration of pantoprazole at a dose of 0.8 or 1.6 mg/kg body weight, no significant correlation between pantoprazole clearance and age or body weight was observed. AUC and volume of distribution were consistent with data in adults. Indications: Panzell Injection is used for the following indications: - Reflux esophagitis - Gastric and duodenal ulcers - Zollinger-Ellison syndrome and other pathological hypersecretory conditions. Dosage and Administration: Gastric and duodenal ulcers, reflux esophagitis: The recommended intravenous dose is one vial (40 mg) of pantoprazole per day. Zollinger-Ellison syndrome and other pathological hypersecretory conditions: For long-term management of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, patients should initiate treatment with pantoprazole 80 mg intravenously per day. Subsequently, the dose may be increased or decreased as needed, according to the rate of gastric acid secretion. If doses greater than 80 mg per day are necessary, the dose should be divided and administered twice daily. Temporary increases in pantoprazole dosage above 160 mg are possible, but should not be used for longer than necessary to achieve adequate acid control. In cases where rapid acid control is needed, an initial dose of 2 x 80 mg pantoprazole intravenously is sufficient to reduce acid output to the target range (<10 mEq/h) within one hour in most patients. Pediatric Population: Experience in children is limited. Therefore, pantoprazole intravenously is not recommended in patients under 18 years of age until appropriate data are available. Hepatic Impairment: In patients with severe hepatic impairment, the daily dose of pantoprazole should not exceed 20 mg (half of a 40 mg vial of pantoprazole). Renal Impairment: No dose adjustment is necessary in patients with impaired renal function. Elderly: No dose adjustment is necessary in elderly patients. Method of Administration: 10 ml of 0.9% sodium chloride for injection is used to obtain the reconstituted solution. The prepared solution can be used immediately or mixed with 100 ml of 0.9% sodium chloride for injection solution or 50 mg/ml glucose (5%) for injection solution. The prepared solution should be used within 12 hours. The prepared solution is administered intravenously over 2-15 minutes. Contraindications: Hypersensitivity to the active substance, to substituted benzimidazoles or to any of the excipients. Special Warnings and Precautions for Use: Development of alarm symptoms: In the event of any alarm symptoms (e.g., significant unintentional weight loss, recurrent vomiting, dysphagia, hematemesis, anemia or melena) and in the presence or suspicion of a gastric ulcer, the possibility of a malignant neoplasm must be excluded, as treatment with pantoprazole may mask symptoms and thus hinder correct diagnosis. If symptoms persist despite adequate treatment, further investigation is required. Hepatic Impairment: In patients with severe hepatic impairment, monitoring of liver enzymes is necessary. If liver enzyme activity increases, treatment should be discontinued. Concomitant use of Atazanavir: Concomitant use of Atazanavir and proton pump inhibitors is not recommended. If concomitant use of Atazanavir and proton pump inhibitors is necessary, close clinical monitoring (e.g., determination of viral load) is required, the dose of Atazanavir is increased to 400 mg and used in combination with 100 mg Ritonavir. The daily dose of pantoprazole should not exceed 20 mg. Bacterial Gastrointestinal Infections: Pantoprazole, like other proton pump inhibitors, may increase the number of bacteria normally present in the upper gastrointestinal tract. Treatment with proton pump inhibitors may slightly increase the risk of gastrointestinal infections caused by bacteria (e.g., Salmonella and Campylobacter and C. difficile). Sodium: This medicinal product contains less than 1 mmol (23 mg) of sodium per dose, i.e., it is practically "sodium-free". Interactions with Other Medicinal Products and Other Forms of Interaction: Effect of Pantoprazole on the Absorption of Other Medicinal Products: Due to deep and prolonged inhibition of gastric acid secretion, pantoprazole may reduce the absorption of medicinal products whose bioavailability is pH-dependent, e.g., some azole antifungals, including ketoconazole, itraconazole, posaconazole, and other medicinal products, e.g., erlotinib. Coumarin Anticoagulants (Phenprocoumon or Warfarin): In clinical pharmacokinetic studies, no interaction was observed with concomitant use of phenprocoumon or warfarin, however, in the post-marketing period, several isolated cases of changes in International Normalized Ratio (INR) have been reported during concomitant treatment. Therefore, in patients treated with coumarin anticoagulants (e.g., phenprocoumon or warfarin), monitoring of prothrombin time/INR is recommended when initiating, discontinuing, or irregularly using pantoprazole. Methotrexate: In some patients, concomitant use of high doses of methotrexate (e.g., 300 mg) and proton pump inhibitors has led to increased methotrexate levels. Therefore, when using high doses of methotrexate, e.g., in cancer and psoriasis, it may be temporarily necessary to discontinue pantoprazole. Other Interaction Studies. Pantoprazole is metabolized in the liver by the cytochrome P450 enzyme system. The main metabolic pathway is demethylation by CYP2C19; other metabolic pathways include oxidation by CYP3A4. Fertility, Pregnancy and Lactation: Pregnancy: There are no adequate data on the use of pantoprazole in pregnant women. Animal studies have shown reproductive toxicity. The potential risk to humans is unknown. Pantoprazole should not be used during pregnancy, except in cases of extreme necessity. Breastfeeding: Animal studies have shown that pantoprazole is excreted into breast milk. Therefore, the decision to continue/discontinue breastfeeding or to continue/discontinue therapy with pantoprazole should be made taking into account the benefits of breastfeeding for the child and the benefits of therapy with pantoprazole for the woman. Effects on Ability to Drive and Use Machines: Side effects such as dizziness and visual disturbances may occur. In such cases, patients should not drive or operate machinery. Undesirable Effects: Headache and complaints from the gastrointestinal tract, such as upper abdominal pain, diarrhea, constipation or flatulence. Complaints usually decrease with continued treatment. There are reports of allergic reactions such as skin rash, itching and in isolated cases also urticaria, angioneurotic edema or anaphylactic shock. Less frequent are reports of nausea, dizziness or visual disturbances (blurred vision). In isolated cases, peripheral edema, depression, fever or myalgia have been reported. Overdose: Symptoms of overdose in humans are not known. Doses up to 240 mg administered intravenously over 2 minutes are well tolerated. Pantoprazole is highly bound to plasma proteins, making it difficult to eliminate by dialysis. In case of overdose, symptomatic and supportive therapy should be carried out if clinical signs of intoxication develop; there are no other specific recommendations. Shelf Life: Unopened vial: 3 years. After reconstitution, or after reconstitution and dilution, the solution is chemically and physically stable for 12 hours at 25°C. From a microbiological point of view, the product should be used immediately. Storage: Store in a dark and dry place, at a temperature not exceeding 25°C. Protect from light and moisture. Keep out of reach of children. Dispensing Category: Pharmaceutical Product Group II, dispensed with prescription form No. 3.