INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Inhibits the enzyme H + / K + -ATP-asu ("proton pump") in parietal cells of the stomach and blocks, thus, the final stage of the synthesis of hydrochloric acid. This leads to a decrease in basal and stimulated secretion of hydrochloric acid, regardless of the nature of the stimulus. After a single admission of 20 mg of pantoprazole, the action of pantoprazole occurs within the first hour, the maximum effect is achieved in 2-2.5 hours. Does not affect the motility of the gastrointestinal tract (GIT).After discontinuation of the drug secretory activity is completely restored after 3-4 days.
PHARMACOKINETICS
Pantoprazole is rapidly absorbed from the gastrointestinal tract, C max (1-1.5 Ојg / ml) is achieved 2-2.5 hours after ingestion, while the C max value remains constant after repeated administration. Bioavailability of the drug is 77%. Simultaneous food intake does not affect the area under the concentration-time curve (AUC), C max , and bioavailability; there is only a change in the beginning of the drug.
The connection with plasma proteins is about 98%. V d is approximately 0.15 l / kg, and the ground clearance is 0.1 l / h / kg. Pathoprazole is almost completely metabolized in the liver. It is an inhibitor of the enzyme system CYP2C19. The half-life (T ? ) Is 1 hour. Due to the specific binding of pantoprazole to the proton pump of parietal cells, T 1/2 does not correlate with the duration of the therapeutic effect. Excretion of metabolites (80%) mainly through the kidneys; the remainder is excreted with bile. The main metabolite, determined in serum and urine, desmethylpentoprazole, which is conjugated with sulfate. T 1/2 desmethylpentoprazole, the main metabolite (about 1.5 h) is much larger than T 1/2 of pantoprazole itself.
In chronic renal failure (including patients who are not hemodialysis), there is no need to change the dose of the drug. T 1/2 - short, as in healthy individuals. Very small amounts of pantoprazole can be dialyzed.
In patients with cirrhosis of the liver (classes A and B according to the Child-Pugh classification) with pantoprazole 20 mg / day, T 1/2 increases to 3-6 hours, AUC increased by 3-5 times, and C max by 1.3 times compared with with healthy faces.
A slight increase in AUC and an increase in C max in elderly patients compared with the corresponding data in younger patients are not clinically significant.
INDICATIONS
- Gastroesophageal reflux disease (GERD), including erosive-ulcerative reflex-esophagitis and associated with GERD symptoms: heartburn, acid regurgitation, pain when swallowing;
- Stomach ulcer and duodenal ulcer (treatment and prevention);
Helicobacter pylori eradication in combination therapy;
- Zollinger-Ellison syndrome.
DOSING MODE
Inside, the tablet should not be chewed and broken. The tablet should be swallowed whole, with a small amount of liquid, before eating, usually before breakfast.When taking twice a second dose of the drug is recommended before dinner.
With peptic ulcer of the stomach and duodenum, the syndrome of Zollinger-Ellison is 40-80 mg / day.
When reflux-esophagitis - 20-40 mg / day.
In elderly patients and with chronic renal failure - no more than 40 mg / day. With hepatic insufficiency, 40 mg once every 2 days.
The course of treatment for scarring of the ulcer of the duodenum is 2 weeks, stomach ulcers and reflux esophagitis - 4-8 weeks.
Helicobacter pylori eradication:
pantoprazole 20 mg twice a day, amoxicillin 1000 mg 2 times a day, clarithromycin 500 mg 2 times a day; pantoprazole 20 mg 2 times a day, metronidazole 500 mg 2 times a day, clarithromycin 500 mg 2 times a day; pantoprazole 20 mg 2 times a day, amoxicillin 1000 mg 2 times a day, metronidazole 500 mg 2 times a day. The treatment is carried out for 7-14 days.
SIDE EFFECT
Side effects are described according to WHO classification: often (1-10%), infrequently (0.1-1%), rarely (0.1-0.01%), very rarely (less than 0.01%).
On the part of the organs of hematopoiesis: 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 - an increase in the activity of "liver" transaminases and gamma-glutamyltransferase (GTT), severe liver damage leading to jaundice with or without hepatic insufficiency.
From the side of the immune system: very rarely - anaphylactic reactions, including anaphylactic shock.
From the side of the musculoskeletal system: rarely - arthralgia; very rarely - myalgia.
From the central and peripheral nervous system: often - headache, infrequently - dizziness, visual impairment (blurred vision).
Mental disorders: very rarely - depression, hallucinations, disorientation, confusion (especially in predisposed individuals).
From the genitourinary system: very rarely - interstitial nephritis. Allergic reactions: infrequently - itching and rash; very rarely - urticaria, angioedema, Stevens-Johnson syndrome, erythema polymorph, Lyell's syndrome, photosensitivity.
General disorders: very rarely - peripheral edema, hyperthermia, weakness, painful tension of the mammary glands, increased concentration of triglycerides,
With the development of severe adverse effects, drug treatment should be discontinued.
CONTRAINDICATIONS
- Hypersensitivity to pantoprazole or other components of the drug;
- dyspepsia of neurotic genesis;
- Children under 18 years of age (effectiveness and safety not studied).
With caution: pregnancy, lactation, liver failure, risk factors.
PREGNANCY AND LACTATION
The experience with pantoprazole in pregnant women is limited. The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus. There is no data on the isolation of pantoprazole with breast milk.
APPLICATION FOR FUNCTIONS OF THE LIVER
In chronic renal failure, dose adjustment is required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use this medication with caution in case of liver failure (dose adjustment is required).
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years of age (efficacy and safety not studied).
APPLICATION IN ELDERLY PATIENTS
In elderly patients, dose adjustment is required.
SPECIAL INSTRUCTIONS
Before the start of therapy, it is necessary to exclude the presence of malignant neoplasm (endoscopic control, if necessary with biopsy - especially with stomach ulcer), i.e. , To. Treatment, masking the symptomatology, can delay the formulation of the correct diagnosis. If, after 4 weeks of pantoprazole therapy, the patient does not have the desired curative effect, he should undergo a second examination.
Like other proton pump inhibitors, pantoprazole can reduce the absorption of cyanocobalamin (vitamin B12) against hypo- and achlorhydria. Especially it should be taken into account in long-term treatment and in patients with risk factors for vitamin BI2 deficiency.
Long-term therapy, especially for longer than 1 year, requires regular monitoring of the patient.
It can lead to false-positive results in the test for determination of tetrahydrocannabinol in urine.
Impact on the ability to drive cars and other mechanical means
Studies on the effect of the drug on the ability to drive a car or other technical means have not been carried out, however, some side effects (blurred vision, dizziness) can affect the performance of occupations requiring increased concentration and speed of psychomotor reactions.
OVERDOSE
Symptoms of an overdose in people are not known.
Treatment: there is no specific antidote. In case of an overdose of the drug, symptomatic and supportive treatment is performed.
DRUG INTERACTION
Pantoprazole reduces the absorption of drugs whose bioavailability depends on the pH of the stomach and is absorbed at acidic pH values ​​(eg, ketoconazole, gland preparations ).
Pantoprazole is metabolized in the liver by means of the cytochrome P 450 enzyme system. It is impossible to exclude interactions of pantoprazole with drugs that are metabolized by the same system. Nevertheless, no significant interactions with digoxin, diazepam, diclofenac, ethanol, phenytoin, glibenclamide, carbamazepine, caffeine, metoprolol, naproxen, nifedipine were found in clinical studies . piroxicam, theophylline and oral contraceptives. Although no significant interactions were found in clinical pharmacokinetic studies with concomitant use with warfarin , several separate reports on the change in the International Normalized Ratio (MHO) were noted. In patients receiving coumarin anticoagulants, simultaneous with pantoprazole, it is recommended to monitor prothrombin time or MHO regularly.
At simultaneous reception of pantoprazole with antacids of any medicinal interactions is not registered.
It is not recommended simultaneous administration of atazanavir and nelfinavir with inhibitors of the purine pump (including pantoprazole), since they can reduce the concentration of atazanavir and nelfinavir in blood plasma and lead to a decrease in the therapeutic effect of antiretroviral therapy.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored at a temperature of no higher than 25 В° C, in a dry place.
Keep out of the reach of children.
Shelf life - 3 years.
Do not use the drug after the expiration date.
