Nolpaz - instructions for use, dose, side effects, contraindications

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Dosage form: & nbsplyophilizate for the preparation of a solution for intravenous administration

Composition:

1 bottle contains:

Active substance:

PanToprasol sodium sesquihydrate 45.1 mg (in terms of pantoprazole 40.0 mg

Excipients: mannitol 140.0 mg, sodium citrate dihydrate 5.0 mg, sodium hydroxide 1 N solution q.s. before pH 11,3 - 11,7*

* corresponds to about 0.02 ml

Description:

Liofilizate from white to white with a slightly yellowish hue of color. Sintering is allowed.

Pharmacotherapeutic group:glands of the stomach secretion-lowering agent - proton pump inhibitor

Pharmacodynamics:Proton pump inhibitor (H⁺ /TO⁺-ATPase). It blocks the final phase of hydrochloric acid secretion, reducing basal and stimulated acid secretion irrespective of the nature of the stimulus.

Compared with other proton pump inhibitors pantoprazole has a higher chemical stability at neutral pH and a lower interaction potential with a liver oxidase system dependent on cytochrome P450. therefore not there was a clinically significant interaction between pantoprazole and other drugs.

Pharmacokinetics:

The volume of distribution is 0.15 l / kg, the clearance is 0.1 l / h / kg.

The period of zero-elimination (T1/2) paitoprazole - about 1 hour.

Several cases of delayed elimination were noted.

Pharmacokinetics does not depend on the frequency of administration of the drug and is linear in the dose range from 10 mg to 80 mg both after ingestion and after intravenous administration.

The degree of binding to plasma proteins is 98%. Metabolised in the liver. It is excreted in the form of metabolites, mainly kidneys (about 80%), in a small amount is excreted through the intestine. The main metabolite in the blood plasma and in urine is desmethylpentoprazole, conjugated with sulfate. T1/2 metabolite - about 1.5 hours.

Pharmacokinetics of special groups of patients

Impaired renal function

When pantoprazole is used in patients with impaired function of the night (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 part of pantoprazole is dialyzed. Do not cumulate.

Impaired liver function

In patients with cirrhosis of the liver (classes A and B but Child-Pugh classification), the value of T1/2 increases to 7-9 hours. The area under the "concentration-time" curve (AUC) increases 5-7 times.The maximum concentration in blood plasma (Cmax) is increased by 1.5 times in comparison with similar parameters in patients with normal liver function.

Elderly patients

In elderly patients, a small increase AUC and Cmax is not clinically relevant.

Indications:

- Stomach ulcer and duodenal ulcer (at the stage of exacerbation), erosive gastritis (including those associated with taking non-steroidal anti-inflammatory drugs (NSAIDs)).

- Gastroesophageal reflux disease (GERD): erosive reflux-esophagitis (treatment), symptomatic treatment of GERD (ie, non-erosive reflux disease - NERD).

- Zollinger-Ellison Syndrome.

- Eradication Helicobacter pylori in combination with antibacterial agents.

- Treatment and prevention of stress ulcers, as well as their complications (bleeding, perforation, penetration).

Contraindications:

- Hypersensitivity to any of the components of the drug.

- Simultaneous use with atazanavir.

- Children under 18 years.

- Pregnancy, the period of breastfeeding.

Carefully:

Hepatic insufficiency, use in elderly patients, simultaneous use with ritonavir.

Pregnancy and lactation:

The drug Nolpaz® is contraindicated in pregnancy and during breastfeeding.

Dosing and Administration:

Intravenously.

Intravenous administration of the drug should be carried out by medical personnel. Intravenous use of Nolpase® It is recommended only when it is impossible to take inside and for a period of not more than 7 days. If the patient has an oral route, intravenous administration should be replaced by taking the drug Nolpaz®, tablets, coated with enteric coating.

Peptic ulcer of the stomach and duodenum (in the stage of exacerbation), erosive gastritis (including those associated with the intake of NSAIDs) and gastroesophageal reflux disease

The recommended daily dose is 40 mg (1 bottle).

Zollinger-Ellison Syndrome

With long-term treatment of Zollinger-Ellison syndrome and other pathological hypersecretory conditions, the recommended daily dose at the beginning of treatment is 80 mg of the drug Nolpaz® intravenously. In the future, the dose may be increased or decreased. In the case of Nolpaz® in a daily dose of more than 80 mg the dose should be divided and administered 2 times a day.It is possible to temporarily increase the daily dose to 160 mg, but not longer than necessary for adequate acidity control.

If an emergency acidity control is required, the initial dose of 80 mg 2 times is sufficient to reduce the acid release in the range of less than 10 mEq / h for 1 hour in most patients.

Treatment and prevention of stress ulcers and their complications (bleeding, perforation, penetration)

The recommended daily dose is 80 mg. If Nolpaz® is used in a daily dose of more than 80 mg, the dose should be divided and injected 2 times into bitches. Perhaps a temporary increase in the daily dose to 160 mg.

Impaired renal function, elderly patients

Dose correction is not required, but the daily dose of pantoprazole should not exceed 40 mg.

Impaired liver function

In patients with severe impairment of liver function, the daily dose of pantoprazole should not exceed 20 mg (half a vial).

Preparation of a solution for intravenous administration

To prepare a ready-to-use solution for intravenous administration, 10 ml of a 0.9% solution of sodium chloride are introduced into the vial containing the lyophilizate.The prepared solution can be introduced in a volume of 10 ml or diluted in 100 ml of a 0.9% solution of sodium chloride or 5% glucose solution.

Do not use any other solvents!

The drug is administered intravenously for 2-15 minutes.

The prepared solution is stable for 12 hours after preparation. However, it is recommended to use the solution immediately after preparation in order to avoid microbial contamination.

Side effects:

When using pantoprazole, lyophilizate for the preparation of a solution for intravenous administration in accordance with indications and in recommended doses, side effects occur extremely rarely. The most common undesirable side effect is thrombophlebitis at the injection site. Diarrhea and headache are observed in about 1% of patients.

The following are data on undesirable side reactions, depending on the incidence.

Classification of the frequency of development of side effects of the World Health Organization (WHO):

very often ≥ 1/10

often from ≥ 1/100 to <1/10

infrequently from ≥ 1/1000 to <1/100

rarely from ≥ 1/10000 to <1/1000

very rarely <1/10000

frequency unknown - can not be evaluated based on available data

Violations from the blood and lymphatic system:

rarely: agranulocytosis;

Very rarely: thrombocytopenia, leukopenia, pancytopenia.

Impaired nervous system:

infrequently: headache, dizziness;

rarely: dysgeusia (a taste disorder).

Disturbances on the part of the organ of sight:

rarely: visual impairment (fogging).

Disorders from the gastrointestinal tract:

infrequently: diarrhea, nausea / vomiting, bloating and flatulence, constipation, dryness of the oral mucosa, discomfort and abdominal pain.

Disorders from the kidneys and urinary tract:

frequency unknown: interstitial nephritis.

Disturbances from the skin and subcutaneous tissues:

infrequently: exanthema / skin rash, itchy skin;

rarely: urticaria, angioedema;

frequency is unknown: malignant exudative erythema (Stevens-Johnson), exudative erythema multiforme, toxic epidermal necrolysis, photosensitivity.

Disturbances from the musculoskeletal and connective tissue:

rarely: arthralgia, myalgia.

Disorders from the metabolism and nutrition:

rarely: hyperlipidemia and rise concentrations lipids (triglycerides, cholesterol) in blood plasma, change in body weight;

frequency is unknown: hyponatremia, hypomagnesemia.

General disorders and disorders at the site of administration:

often: thrombophlebitis at the injection site;

infrequently: weakness, fatigue and malaise;

rarely: fever, peripheral edema.

Immune system disorders:

rarely: increased sensitivity (including anaphylactic reactions, including anaphylactic shock).

Disturbances from the liver and bile ducts:

infrequently: increased activity of "hepatic" enzymes (aspartate aminotransferase (ACT), gamma-glutamyltransferase (PT)) in the blood plasma;

rarely: an increase in the concentration of bilirubin in the blood plasma;

frequency unknown: hepatocellular injury, jaundice.

Violations of the genitals and breast:

rarely: gynecomastia.

Disorders of the psyche:

nechasto: sleep disturbance;

rarely: depression (including exacerbations of existing disorders);

Very rarely: disorientation (including exacerbations of existing disorders);

frequency is unknown: hallucinations, confusion (especially in patients susceptible to this), as well as worsening of symptoms before initiation of therapy.

Overdose:

The case of an overdose resulting from the use of the drug Nolpaz® was not noted. Doses of pantoprazole up to 240 mg were administered intravenously for 2 min and were tolerated well.

In case of an overdose and only when there are clinical manifestations, symptomatic and supportive therapy is performed. Hemodialysis is ineffective.

Interaction:

The simultaneous use of atazanavir 300 mg / ritonavir 100 mg with omeprazole (40 mg 1 pgz per day) or atazanavir 400 mg with lansoprazole (60 mg once) in healthy volunteers led to a significant decrease in the bioavailability of atazanavir. Absorption of atazanavir depends on the pH of the gastrointestinal tract, therefore pgnoprazole should not be used concomitantly with atazanavir.

Simultaneous use of the drug Nolpaz® can reduce absorption drugs whose bioavailability depends on the pH of the stomach (for example: ketoconazole, intraconazole, posaconazole and such as erlotinib).

A drug Nolpaz® can be used without the risk of negative drug interactions:

- in patients with diseases of the cardiovascular system, taking cardiac glycosides (digoxin), blockers of "slow" calcium channels (nifedipine), beta-blockers (metoprolol);

- in patients with diseases of the gastrointestinal tract, taking antacids, antibacterial agents (amoxicillin, clarithromycin, metronidazole);

- in patients taking oral contraceptives, containing levonorgestrel and ethinyl estradiol;

- in patients taking NSAIDs (diclofenac, naproxen, piroxicam);

- in patients with endocrine system diseases, taking glibenclamide;

- in patients with anxiety and sleep disorders receiving diazepam;

- in patients with epilepsy taking carbamazepine and phenytoin;

- in patients taking indirect anticoagulants (warfarin and fenprokumone) under the control of prothrombin time and the international normalized relationship (INR) at the beginning and at the end of therapy, as well as during an irregular application of pantoprazole;

There was also a lack of clinically significant drug interaction with caffeine, ethanol, theophylline.

Special instructions:

The use of pantoprazole is not recommended for the treatment of mild symptoms from the gastrointestinal tract, such as dyspepsia of a neurogenic genesis.

Patients should consult a physician if the following symptoms occur:

- significant unintended weight loss;

- periodic vomiting;

- Swallowing disorder;

- gastrointestinal bleeding;

- anemia or melena.

If you suspect or have a stomach ulcer before starting treatment with pantoprazole

It should be excluded the possibility of malignant neoplasm, since the use of the drug Nolpaz® can mask symptoms and delay the correct diagnosis. If the symptoms persist despite adequate therapy, then an additional examination is necessary.

In patients with severe impairment of liver function, it is necessary to monitor the biochemical parameters of blood serum. When the activity of "liver" enzymes increases, the drug should be discontinued.

With the use of drugs that reduce the acidity of gastric juice, the risk of developing gastrointestinal infections is slightly increased, the causative agents of which are yavlbacteria of the genus Salmonella spp., Campylobacter spp.

Effect on the ability to drive transp. cf. and fur:

It is necessary to refrain from driving and other mechanisms that require increased attention, as dizziness and visual impairment are possible.

Form release / dosage:Lyophilizate for the preparation of a solution for intravenous administration, 40 mg.

Packaging:

For 40 mg of pantoprazole, a 15 ml bottle of colorless glass (Type I) capped with a color stopper made of chlorobutyl rubber, with an aluminum cap and a colored plastic cover of the first autopsy control, is placed on 40 mg of pantoprazole.

By 1,5, 10 or 20 bottles together with instructions for use are placed in a cardboard pack.

Storage conditions:

In the dark place at a temperature of no higher than 25° C, in the original packaging. The shelf life of the drug after dilution is 12 hours at a temperature of not more than 25° C. Keep out of reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003081

Date of registration:06.07.2015

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp22.08.2015

Illustrated instructions

Instructions

Nolpaz (Nolpaza)