NOLPAZA
Active material: Pantoprazole
When ATH: A02BC02
CCF: Inhibitor N+-K+-ATPase. Anti-ulcer drug
ICD-10 codes (testimony): E16.8, K21, K21.0, K25, K26, K27
When CSF: 11.01.03
Manufacturer: KRKA d.d. (Slovenia)
Pharmaceutical form, composition and packaging
Pills, enteric coated light tan color, Oval, slightly biconcave; of presentations – weight from white to light tan, with a rough surface, cladding layer with a light tan color.
| 1 tab. | |
| pantoprazole sodium sesquihydrate | 22.55 mg, |
| that corresponds to the content of pantoprazole | 20 mg |
Excipients: mannitol, krospovydon, anhydrous sodium carbonate,, sorbitol, calcium stearate.
The composition of the shell: gipromelloza, povidone, Titanium dioxide (E171), dye iron oxide yellow (E172), propylene glycol, dispersion Eudragit L30D (a copolymer of methacrylic acid and ethyl acrylate (1:1) variance 30%, water, sodium lauryl, polysorbate-80), talc, macrogol 6000.
14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
Pills, enteric coated light tan color, Oval, slightly biconcave; of presentations – weight from white to light tan, with a rough surface, cladding layer with a light tan color.
| 1 tab. | |
| pantoprazole sodium sesquihydrate | 45.10 mg, |
| that corresponds to the content of pantoprazole | 40 mg |
Excipients: mannitol, krospovydon, anhydrous sodium carbonate,, sorbitol, calcium stearate.
The composition of the shell: gipromelloza, povidone, Titanium dioxide (E171), dye iron oxide yellow (E172), propylene glycol, dispersion Eudragit L30D (a copolymer of methacrylic acid and ethyl acrylate (1:1) variance 30%, water, sodium lauryl, polysorbate-80), talc, macrogol 6000.
14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
Pharmacological action
Anti-ulcer drug. It inhibits the enzyme H -K -ATPase (proton pump) in the gastric parietal cells, and thereby blocks, the final stage of the synthesis of hydrochloric acid. This leads to a reduction in basal and stimulated secretion of hydrochloric acid, regardless of the nature of the stimulus.
After a single oral dose of the drug 20 mg pantoprazole action develops within the first hour, the maximum effect is achieved through 2-2.5 no. No effect on the motility of the gastrointestinal tract. After discontinuation secretory activity is completely restored by 3-4 Nights.
Pharmacokinetics
Absorption
Pantoprazole is rapidly absorbed from the gastrointestinal tract, FROMmakh achieved through 2-2.5 hours after ingestion and is 1-1.5 ug / ml, wherein the value of Cmakh It remains constant during multiple dose. The bioavailability of the drug is 77%. Simultaneous food intake does not affect the AUC, FROMmakh and bioavailability; there is only a change in the beginning of the drug.
Distribution
Plasma protein binding – about 98%. Vd is approximately 0.15 l / kg, and clearance - 0.1 L / h / kg.
Metabolism
Pantoprazole is almost completely metabolized in the liver. It is an inhibitor of the isozyme CYP2C19.
Deduction
T1/2 – 1 no. Because of the specific binding of pantoprazole with proton pump parietal cells by T1/2 It does not correlate with the duration of the therapeutic effect. Excretion of metabolites (80%) – primarily through the kidneys; the remaining part is excreted in the bile. The major metabolite, determined in serum and urine, – desmetilpantoprazol, which is conjugated with sulphate. T1/2 desmetilpantoprazola (about 1.5 no) a lot more, than T1/2 of pantoprazole.
Pharmacokinetics in special clinical situations
In chronic renal failure (incl. patients, hemodialysis) no changes are required doses. T1/2 – short, in healthy individuals. Pantoprazole in very small quantities can be displayed by dialysis.
In patients with liver cirrhosis (Classes A and B on the Child-Pugh classification) upon receipt of the pantoprazole dose 20 mg / day T1/2 increases to 3-6 no, AUC increases 3-5 time, and Cmakh – in 1.3 fold compared with healthy individuals.
The slight increase in AUC and C increasemakh elderly patients compared with corresponding data in younger patients are not clinically significant.
Testimony
- Gastroesophageal reflux disease (GERD), incl. erosive or ulcerative reflux esophagitis and symptoms associated with GERD (heartburn, acid regurgitation, pain when swallowing);
- Erosive and ulcerative lesions of the stomach and duodenum, associated with taking NSAIDs;
- Gastric ulcer and duodenal ulcer, Treatment and Prevention;
- Helicobacter pylori eradication in combination with two antibiotics;
- Zollinger-Ellison syndrome, and other pathological conditions, associated with increased gastric secretion.
Dosage regimen
The drug is taken orally. Tablets should be swallowed whole, without chewing or breaking a, drinking a small amount of liquid, before eating, usually before breakfast. When taken twice a second dose is recommended to take a pre-dinner.
At GERD, incl. erosive and ulcerative esophagitis and reflux-associated symptoms (heartburn, acid regurgitation, pain when swallowing) mild, the recommended dose – 20 mg / day, moderate and severe – 40-80 mg / day. Relief of symptoms usually occurs within 2-4 weeks. The course of therapy is 4-8 weeks.
To prevention, and as long as maintenance therapy appoint 20 mg / day, if necessary, increase the dose to 40-80 mg / day. You can receive the drug “on demand” in the event of symptoms.
At erosive and ulcerative lesions of the stomach and duodenum, associated with taking NSAIDs, the recommended dose – 40-80 mg / day. The course of therapy – 4-8 weeks.
To prevention of erosive lesions on the background of the prolonged use of NSAIDs – by 20 mg.
To treatment and prevention of gastric ulcer and duodenal ulcer appoint 40-80 mg / day. The course of treatment during exacerbation of duodenal ulcer is usually 2 of the week, stomach ulcer – 4-8 weeks. If necessary, the duration of therapy increases.
To eradication of Helicobacter pylori (in combination with antibiotics) the recommended dose – 40 mg 2 twice a day in combination with two antibiotics, Usually the course of therapy of H. pylori 7-14 days.
At Zollinger-Ellison syndrome and other pathological conditions, associated with increased gastric secretion, The recommended starting dose of pantoprazole long-term treatment 80 mg / day, razdelennaya of 2 admission. Subsequently, the daily dose can be titrated according to the starting level of gastric secretion. Possibly a temporary increase in the daily dose of pantoprazole to 160 mg to adequately control gastric secretion. The duration of therapy is selected individually.
In patients with severely impaired hepatic function pantoprazole dose should not exceed 40 mg / day and should regularly monitor the activity of liver enzymes, especially during prolonged treatment pantoprazole. An increase in liver enzymes is recommended to remove the drug.
In elderly patients and patients with kidney disease the maximum daily dose of pantoprazole – 40 mg.
In the elderly, receiving eradication therapy Helicobacter pylori, Duration of therapy is usually not more than 7 days.
Side effect
From the side of hematopoiesis: rarely – leukopenia, thrombocytopenia.
From the digestive system: often – abdominal pain, diarrhea, constipation, flatulence; infrequently – nausea, vomiting; rarely – dry mouth; rarely – increase in liver transaminases and GGT, severe liver injury, causing jaundice with or without hepatic insufficiency.
On the part of the immune system: rarely – anaphylactic reactions, including anaphylactic shock.
On the part of the musculoskeletal system: rarely – arthralgia; rarely – myalgia.
From the central and peripheral nervous system: often – headache; infrequently – dizziness, visual impairment (blurred vision); rarely – depression.
With the genitourinary system: rarely – interstitial nephritis.
Allergic reactions: infrequently – itch, rash; rarely – hives, angioedema, Stevens-Johnson syndrome, erythema multiforme, or Lyell's syndrome, photosensitivity.
Other: rarely – peripheral edema, hyperthermia, weakness, painful tension of the mammary glands, elevated triglycerides.
With the development of severe adverse effects of drug treatment should be discontinued.
Contraindications
- Dyspepsia nevroticheskogo genesis;
- Children up to age 18 years (efficacy and safety have not been studied);
- Hypersensitivity to pantoprazole or other ingredients.
Nolypaza soderzhit sorbitol, so the drug is not recommended for patients with rare hereditary fructose intolerance.
FROM caution should be prescribed during pregnancy, lactation, hepatic insufficiency, risks of deficiency of cyanocobalamin (especially against hypo- and achlorhydria).
Pregnancy and lactation
Experience with pantoprazole in pregnant women is limited. During pregnancy and lactation may be used only, if the positive effects for the mother justifies the potential risk to the fetus and child. Data on the allocation of pantoprazole in breast milk is not.
Cautions
Before therapy is necessary to exclude the presence of cancer (endoscopic control, optionally with biopsy – especially gastric ulcer), tk. treatment, maskyruya symptoms, may delay the correct diagnosis.
If after 4 weeks pantoprazole therapy in a patient is not the desired therapeutic effect, it should be retested.
As with other proton pump inhibitors, pantoprazole may reduce the absorption of cyanocobalamin (vitamin B12) on the hypothesis of phonemes- and achlorhydria. Especially it should be considered when long-term treatment and in patients with risk factors for deficiency of vitamin B12.
Conducting long-term therapy, especially of more than 1 year, It requires regular patient monitoring.
Effects on ability to drive vehicles and management mechanisms
The drug does not affect the ability to drive a car or other technical means.
Overdose
Overdose symptoms in humans are not known.
Treatment: There is no specific antidote. In the case of drug overdose, usually accompanied by signs of intoxication, used detoxification activities. Treatment of symptomatic.
Drug Interactions
Nolpaza reduces the absorption of drugs, bioavailability which is dependent on the pH of the stomach, and is sucked at acidic pH (eg, ketoconazole).
Pantoprazole is metabolized in the liver by the cytochrome P450 enzyme system. We can not exclude interactions of pantoprazole with drugs, are metabolized by the same system. Nonetheless, in clinical studies there was no significant interaction with digoxin, diazepamom, diclofenac, ethanol, phenytoin, glibenclamide, karʙamazepinom, caffeine, metoprolol, naproxen, nifedipine, piroksikamom, theophylline and oral contraceptives.
Although the simultaneous use of warfarin in clinical pharmacokinetic studies found no significant interactions, It noted several separate change messages MHO. Patients, receiving coumarin anticoagulants, simultaneously with pantoprazole, to regularly monitor the prothrombin time or MHO.
At the same time taking pantoprazole with antacids any drug interactions are not registered.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 2 year.
