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Active ingredients
Pantoprazole
Release form
Pills
Composition
Active ingredient: Pantoprazole Concentration of active ingredient (mg): 20 mg
Pharmacological effect
Inhibitory proton pump.
Pharmacokinetics
For enteric-coated pills. Pantoprazole is rapidly absorbed from the gastrointestinal tract, Cmax in plasma (1–1.5 mcg / ml) is reached 2–2.5 hours after ingestion, while the value of Cmax remains constant during repeated administration. Bioavailability of the drug is 77%. Simultaneous food intake does not affect the AUC, Cmax and bioavailability; there is only a change in the onset of the drug action. Communication with plasma proteins is about 98%. Vd is about 0.15 L / kg, and clearance is 0.1 L / h / kg. Pantoprazole is almost completely metabolized in the liver. It is an inhibitor of the CYP2C19 enzyme system. T1 / 2 - 1 h. Due to the specific binding of pantoprazole to the proton pump of parietal cells, T1 / 2 does not correlate with the duration of the therapeutic effect. Excretion of metabolites (80%) mainly through the kidneys; the rest is excreted in the bile. The main metabolite, determined in serum and urine, is desmethylpanthoprazole, which is conjugated with sulfate. T1 / 2 of desmethyl pantoprazole, the main metabolite (approximately 1.5 hours) is much more than the T1 / 2 of pantoprazole itself. In chronic renal failure (including those on hemodialysis), no dose change is required. T1 / 2 is short, as in healthy individuals. Very small amounts of pantoprazole can be dialyzed. In patients with liver cirrhosis (grades A and B, according to the Child, Pugh classification), when taking pantoprazole 20 mg / day, T1 / 2 increases to 3–6 hours, AUC increases 3–5 times and Cmax - 1.3 times compared with healthy individuals. A small increase in AUC and an increase in Cmax in elderly patients compared with the corresponding data in younger patients are not clinically significant. For the lyophilisate for preparing the solution for intravenous administration. Vd is about 0.15 L / kg, and clearance is 0.1 L / h / kg. T1 / 2 pantoprazole - about 1 hour. Several cases of delayed elimination were noted. The pharmacokinetics do not depend on the frequency of administration of the drug and are linear in the dose range from 10 to 80 mg both after oral administration and after intravenous administration. The degree of binding with plasma proteins is 98%. Metabolized in the liver.It is excreted in the form of metabolites, mainly by the kidneys (about 80%), in a small amount excreted through the intestines. The main metabolite in the blood plasma and in the urine is desmethyl pantoprazole conjugated with sulfate. T1 / 2 metabolite - about 1.5 hours. Special patient groups Disruption of renal function. When using pantoprazole in patients with impaired renal function (including patients on hemodialysis), no dose reduction is required. As in patients with normal renal function, T1 / 2 pantoprazole is short. Only a very small portion of pantoprazole is dialyzed. Not cumulative. Violation of the liver. In patients with cirrhosis of the liver (classes A and B according to Child-Pugh classification), the T1 / 2 value increases to 7–9 hours. The AUC increases 5–7 times. Cmax increases by 1.5 times compared with similar indicators in patients with normal liver function. Elderly patients. In elderly patients, a slight increase in AUC and Cmax is not clinically significant.
Indications
Hypertension mild to moderate severity.
Contraindications
Hypersensitivity to pantoprazole or drug; Nolpaza contains sorbitol, so the drug is not recommended for people with a rare hereditary fructose intolerance; Dyspepsia neurotic genesis; Children under 18 years of age (efficacy and safety have not been studied) .With caution: pregnancy, lactation, hepatic failure, risk factors for cyanocobalamin deficiency (vitamin B12) (especially against the background of hypo- and achlorhydria).
Use during pregnancy and lactation
For enteric-coated pills. Before starting treatment, it is necessary to exclude the presence of a malignant neoplasm (endoscopic control, if necessary with a biopsy - especially in case of a stomach ulcer), since treatment, masking the symptoms, may delay the correct diagnosis. If after 4 weeks of treatment with pantoprazole, the patient does not have the desired therapeutic effect, he should be re-examined. Like other proton pump inhibitors, pantoprazole may reduce the absorption of cyanocobalamin (vitamin B12) on the background of hypo- and achlorhydria. This should be especially taken into account in long-term treatment and in patients with risk factors for vitamin B12 deficiency. Conducting long-term therapy, especially for more than 1 year, requires regular monitoring of the patient. Effect on the ability to drive and other mechanical means.The drug does not affect the ability to drive a car or other technical means. For a lyophilisate for preparing a solution for intravenous administration, the use of pantoprazole is not recommended for treating mild gastrointestinal symptoms such as neurogenic dyspepsia. Patients should consult a physician when the following symptoms occur: - significant unintended weight loss; - intermittent vomiting; - swallowing disorder; - gastrointestinal bleeding; - anemia or melena. rhenium or the presence of a stomach ulcer before starting treatment with pantoprazole should exclude the possibility of a malignant neoplasm, since use of the drug Nolpaza can mask the symptoms and delay the correct diagnosis. If the symptoms persist despite adequate therapy, an additional examination is necessary. Patients with severely impaired liver function must be monitored for serum biochemical parameters. With increasing activity of liver enzymes, the use of the drug should be discontinued. When using drugs that reduce the acidity of gastric juice, the risk of developing gastrointestinal infections, caused by bacteria of the genus Salmonella spp., Campylobacter spp, increases slightly. Influence on the ability to drive motor vehicles and other technical devices You should refrain from driving vehicles and other mechanisms that require increased attention, because possible development of vertigo and visual impairment.
Dosage and administration
Inside, the pill should not be chewed and broken. The tablet is swallowed whole, washed down with a small amount of liquid, before meals, usually before breakfast. When taking a second dose of the drug is recommended to take before dinner. GERD, including erosive-ulcerative reflux esophagitis and associated symptoms: heartburn, acid regurgitation, pain when swallowing: mild: recommended dose - 1 tablet Nolpazy (20 mg) per day. Medium and severe: recommended dose - 1- 2 pills Nolpaza 40 mg per day (40-80 mg / day). Symptom relief usually occurs within 2–4 weeks. The course of therapy is 4-8 weeks.For prophylaxis, as well as as a supporting long-term therapy, take 20 mg / day (1 tablet of Nolpazy 20 mg), if necessary, increase the dose to 40-80 mg / day. It is possible to take the drug "on demand" when symptoms occur. Erosive and ulcerative lesions of the stomach and duodenum associated with taking NSAIDs: The recommended dosage is 40-80 mg / day (1-2 pills Nolpazy 40 mg). The course of therapy is 4-8 weeks. For the prevention of erosive lesions on the background of long-term use of NSAIDs - 20 mg. Peptic ulcer and duodenal ulcer, treatment and prevention: Assign 40-80 mg / day. The course of treatment for acute exacerbation of duodenal ulcer is usually 2 weeks, and gastric ulcer is 4-8 weeks. If necessary, the duration of therapy is increased. Eradication of Helicobacter pylori (in combination with antibiotics): Recommended dose: 1 tablet Nolpazy (40 mg) 2 times a day in combination with two antibiotics, usually a course of anti-helicobacter therapy is 7-14 days. Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion: The recommended starting dose of long-term therapy with pantoprazole: 80 mg (2 pills of Nolpaza 40 mg) per day, divided into 2 doses. In the future, the daily dose can be titrated depending on the initial level of gastric secretion. Perhaps a temporary increase in the daily dose of pantoprazole to 160 mg in order to adequately control gastric secretion. The duration of therapy is selected individually. In patients with severely impaired liver function, the dose of pantoprazole should not exceed 40 mg per day and it is recommended to regularly monitor the activity of “liver” enzymes, especially with long-term treatment with pantoprazole. With an increase in the activity of “liver” enzymes, it is recommended to discontinue the drug. In elderly people and patients with kidney disease, the maximum daily dose of pantoprazole is 40 mg. In elderly individuals receiving Helicobacter pylori eradication therapy, the duration of therapy usually does not exceed 7 days.
Side effects
For enteric-coated pills, Nolpaza reduces the absorption of drugs whose bioavailability depends on the pH of the stomach and is absorbed at acidic pH values (for example ketoconazole). Pantoprazole is metabolized in the liver through the enzyme system of cytochrome P450. Pantoprazole interactions with drugs that are metabolized by the same system cannot be ruled out.However, in clinical studies, no significant interaction with digoxin, diazepam, diclofenac, ethanol, phenytoin, glibenclamide, carbamazepine, caffeine, metoprolol, naproxen, nifedipine, piroxicam, theophylline, oral contraceptive, teofillin, and contraceptive, terofillin, nopedipine, pheroxicam, theophylline, oral contraceptive, teofillin, nopedipine, pheroxicam, theophylline, metoproline, naproxen, nofedin, pheroxycam, teofillin, and contraceptive marrow has been found. pharmacokinetic studies did not reveal significant interaction, there were several separate reports of changes in MHO. In patients receiving coumarin anticoagulants simultaneously with pantoprazole, it is recommended to regularly monitor PV or MHO. If you are taking pantoprazole with antacids at the same time, no drug interactions have been registered. For a lyophilisate to prepare a solution for intravenous administration Simultaneous use of atazanavir 300 mg / 100 mg ritonavir with omeprazole. 40 mg 1 time per day) or atazanavir 400 mg with lansoprazole (60 mg once) in healthy volunteers resulted in a significant decrease in the bioavailability of ataz navira. Atazanavir absorption depends on the pH of the gastrointestinal tract, so pantoprazole should not be used concurrently with atazanavir. Simultaneous use of the drug Nolpaza can reduce the absorption of drugs whose bioavailability depends on the pH of the stomach (for example, ketoconazole, intraconazole, posaconazole, and such as erlotinib). the risk of negative drug interactions: - in patients with cardiovascular disease, taking cardiac glycosides (digoxin), BPC (nifedipine), beta-blockers (metoprolol); - in patients with gastrointestinal diseases taking antacids, antibacterial agents (amoxicillin, clarithromycin, metronidazole); - in patients taking oral contraceptives containing levonorgestrel and ethinyl estradiol; - in patients taking NSAIDs (diclofenac, naproxen, pyroxicam); with endocrine diseases taking glibenclamide; - in patients with anxiety and sleep disorders taking diazepam; - in patients with epilepsy, taking carbamazepine and phenytoin; - in patients taking x indirect anticoagulants (warfarin and fenprokumon) under the control of PV and INR at the beginning and at the end of therapy, as well as during the irregular use of pantoprazole; Also, there is no clinically significant drug interaction with caffeine, ethanol, theophylline.
Overdose
The side effects of the WHO classification are given: On the part of the blood-forming organs: very rarely - leukopenia, thrombocytopenia On the part of the digestive system: often - abdominal pain, diarrhea, constipation, flatulence; infrequently - nausea, vomiting; rarely, dry mouth; very rarely, increased activity of liver transaminases and gamma-glutamine transferase (GGT), severe liver damage, leading to jaundice with or without liver failure. On the part of the immune system: very rarely - anaphylactic reactions, including anaphylactic shock. From the musculoskeletal system: rarely - arthralgia; very rarely - myalgia. From the central and peripheral nervous system: often - a headache; infrequently - dizziness, visual disturbances (blurred vision). Mental disorders: very rarely - depression. From the genitourinary system: very rarely - interstitial nephritis. Allergic reactions: infrequently - itching and rash; very rarely - urticaria, angioedema, Stnwens-Johnson syndrome, erythema polymorphism or Lyell's syndrome, photosensitization. General disorders: very rarely - peripheral edema, hyperthermia, weakness, painful breast tension, increased triglyceride levels. With the development of severe adverse effects, drug treatment should be discontinued.
Interaction with other drugs
Precautionary measures
special instructions
For enteric-coated pills. The symptoms of an overdose in humans are unknown. Treatment: symptomatic, there is no specific antidote. In the case of an overdose of the drug, accompanied by the usual signs of intoxication, detoxification measures are used. For the lyophilisate for preparing a solution for intravenous administration, no overdose was observed as a result of using Nolpaza. Doses of pantoprazole up to 240 mg were injected intravenously for 2 minutes and were well tolerated. Treatment: in case of overdose, and only with the appearance of clinical manifestations symptomatic and supportive therapy is carried out. Hemodialysis is ineffective.