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

Active substance: omeprazole - 40.00 mg (in the form of omeprazole sodium - 42.55 mg); Excipients: disodium edetate dihydrate - 1.50 mg; sodium hydroxide 5.00 mg.

Description:Almost white to a light yellowish color, a porous mass.

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

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

Mechanism of action

Omeprazole is a

racemic mixture of two enantiomers, reduces acid secretion in the stomach due to specific inhibition of the proton pump in parietal cells. With a single dosing per day, the drug acts quickly and causes blockage of acid secretion in the stomach.

Omeprazole is a weak base, concentrated and converted into an active form in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa where it inhibits the enzyme H⁺-TO⁺-ATPase (proton pump). A drug has a dose-dependent effect on the final stage of acid synthesis and inhibits both basal and stimulated secretion of acid in the stomach, regardless of the nature of the stimulus.

Effect on gastric secretion Intravenous administration of omeprazole

causes dose-dependent suppression of acid secretion in the human stomach. To achieve a rapid reduction in the acidity of gastric juice, it is recommended

intravenous administration of 40 mg of omeprazole. The antisecretory effect is maintained for 24 hours.

The degree of oppression of hydrochloric acid secretion is proportional to the area under the "concentration-time" curve (AUC) omeprazole, but does not depend on the immediate concentration of the drug in the blood plasma.

During therapy with omeprazole, tachyphylaxis was not observed.

Influence on N. pylori

Helicobacter pylori in combination with increased production of acid is an important factor in the pathogenesis of peptic ulcer, including gastric ulcer and duodenal ulcer. II. pylori is also the cause of gastritis, incl. atrophic, which is associated with an increased risk of developing gastric cancer. Eradication N. pylori as a result of

application of omeprazole in combination with antimicrobial agents provides a long-term remission of peptic ulcers and high rates of recovery of patients.

Other effects associated with blocking acid secretion The use of drugs that suppress the secretion of hydrochloric acid in the stomach, including proton pump inhibitors, is accompanied by an increase in the content of the stomach microbial flora, normally contained in the gastrointestinal tract. The use of proton pump inhibitors can lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract caused by Salmonella spp. and Campylobacter spp.

Pharmacokinetics:

Distribution

The volume of distribution in healthy people is approximately 0.3 l / kg. The connection with plasma proteins is 97%.

Metabolism

Omeprazole undergoes complete metabolism involving the cytochrome P450 system (CYP). The main part is metabolized with the participation of a specific polymorphic isoenzyme CYP 2C19, which is responsible for the formation of the main metabolite of hydroxyomeprazole. Metabolism of the remainder isoenzyme CYP ZA4 with the formation of omeprazole sulfone.

Metabolites have no significant effect on the secretion of acid in the stomach. The half-life after intravenous administration is 40 minutes and does not change with prolonged treatment. About 80% of the dose of omeprazole when taken orally is excreted in the form of metabolites by the kidneys, the remainder is excreted through the intestine, mainly with bile.

Special populations of patients Patients with impaired hepatic function Metabolism of omeprazole in patients with impaired liver function is slowed, which leads to an increase AUC. Omeprazole does not show a tendency to cumulate when the dose is administered once a day. Patients with impaired renal function In patients with reduced renal function, pharmacokinetics, including systemic bioavailability and rate of excretion, remain unchanged.

Patients of advanced age (over 65 years)

The rate of metabolism of omeprazole in elderly patients is somewhat reduced. Children

There is limited experience with omeprazole for intravenous administration in children.

Indications:

HELICID® for intravenous use is indicated as an alternative to oral therapy for the followingindications:

- duodenal ulcer;

- prevention of recurrence of duodenal ulcer;

- stomach ulcer;

- prevention of recurrence of stomach ulcers;

- erosive and ulcerative lesions of the stomach and duodenum,

associated with Helicobacter pylori (as part of complex therapy);

- erosive and ulcerative lesions of the stomach and duodenum,

associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs);

- prevention of erosive and ulcerative lesions of the stomach and duodenum associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs), prevention of stress ulcers;

- reflux esophagitis;

- long-term monitoring of patients with cured reflux esophagitis;

- symptomatic gastroesophageal reflux disease (GERD);

- Zollinger-Ellison syndrome.

Contraindications:

- Hypersensitivity to the drug or any of its components.

- Concomitant use of nelfinavir and atazanavir.

- Children's age (up to 18 years).

Carefully:

In patients with osteoporosis; renal and / or hepatic insufficiency.

Pregnancy and lactation:

The use of Helicid ® is possible only in those cases,when the intended use for the mother exceeds the potential risk to the fetus.

Omeprazole is excreted in breast milk. If you need to take Helicid ® during breastfeeding, you need to decide whether to stop breastfeeding or stop taking the drug.

Dosing and Administration:

The drug is administered intravenously at a dose of 40 mg once a day in cases where oral administration of the drug is not possible. Zollinger-Ellison syndrome.

Dose is selected individually in depending on the initial level of gastric secretion, usually starting at 60 mg per day. If necessary, increase the dose to 80-120 mg per day, dividing it into 2 injections. The duration of treatment in each case is determined by the doctor depending on the patient's condition.

The solution should be administered intravenously for at least 20-30 minutes. Patients with impaired hepatic function In patients with severe hepatic insufficiency, the daily dose should not exceed 20 mg.

Patients with impaired renal function In patients with impaired renal function, dose adjustment is not required.

Patients of advanced age (over 65 years)

In elderly patients, dose adjustment is not required.

Instructions for preparing an infusion solution.

The contents of one vial are dissolved in 100 ml of 0.9% sodium chloride solution (the prepared solution should be used within 12 hours) or in 100 ml of 5% glucose solution for infusion (the prepared solution should be used within 6 hours).

The resulting solution should be uniform and transparent from colorless to slightly yellow in color.

1. In a syringe, 5 ml of infusion solution is taken from a vial or infusion bag.

2. Introduce the infusion solution into a vial of omeprazole lyophilizate, gently shake until the drug dissolves completely.

3. A solution of omeprazole is injected into the syringe.

4. Transfer the solution to a vial or infusion bag.

5. Repeat steps 1-4 until all omeprazole will not be transferred to a vial or infusion bag.

Alternative cooking infusion solution in flexible containers

1. To prepare the solution, use a two-sided needle (adapter). One end of the needle is pierced by the membrane of the infusion bag, the other end of the needle is connected with a vial of omeprazole lyophilizate.

2. Dissolve the lyophilizate of omeprazole, pumping the infusion solution from the bag into the bottle and back.

3. Make sure that the lyophilizate is completely dissolved, then disconnect the empty vial and remove the needle from the infusion bag.

Side effects:

The frequency of unwanted reactions,

is presented in accordance with the classification of the Medical Dictionary of Regulatory Activities (MedDRA):

Often: (>10 %),

Often: (>1%< 10%),

Infrequently: (>0,1 % < 1 %),

Rarely: (>0,01% <0,1 %),

Rarely: (<0,01 %),

The frequency is unknown: (it is not possible to determine the frequency of occurrence according to the available data).

Disorders from the gastrointestinal tract

Often: abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting.

Rarely: dry mouth, stomatitis, gastrointestinal candidiasis, microscopic colitis.

Disturbances from the liver and bile ducts Infrequently: a transient increase in the activity of "liver" enzymes.

Rarely: a violation of the liver, hepatitis with jaundice or without.

Rarely: hepatic insufficiency, encephalopathy in patients with previous severe impairment of liver function.

Disorders from the central nervous system

Often: headache.

Infrequently: dizziness, paresthesia, insomnia, drowsiness, vertigo.

Rarely: a taste disorder.

Disorders of the psyche Infrequently: insomnia.

Rarely: confusion, a state of arousal, depression.

Rarely: aggressiveness, hallucinations. Disturbances from musculoskeletal and connective tissue Rarely: myalgia, arthralgia.

Rarely: muscle weakness. Violations of the blood and lymphatic system Rarely: leukopenia, thrombocytopenia.

Rarely: agranulocytosis, pancytopenia. Disturbances from the skin and subcutaneous tissues

Infrequently: skin itching, peripheral edema, skin rash, dermatitis, urticaria. Rarely: alopecia, photosensitivity.

Rarely: multiforme exudative erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis. Disorders from the kidneys and urinary tract Rarely: interstitial nephritis. Disturbances on the part of the organ of sight Rcaustically: impaired vision.

Hearing disorders and labyrinthine disorders Infrequently: Vertigo.

Violations of the genitals and

mammary gland Rarely: gynecomastia.

Immune system disorders

Rarely: hypersensitivity reactions, such as angioedema, anaphylactic reactions, anaphylactic shock.

Disturbances from the respiratory system, chest and mediastinal organs Rarely: bronchospasm.

General disorders and disorders at the site of administration

Infrequently: general weakness, peripheral edema.

Rarely: increased sweating.

Disorders from the metabolism and nutrition

Rarely: hyponatremia.

Frequency unknown: hypomagnesemia.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, diarrhea; dizziness, headache. In isolated cases, apathy, depression, and fogging of consciousness were also noted. Treatment: there is no specific antidote.

Treatment is symptomatic. Hemodialysis is not effective enough.

Interaction:

Increased acidity in the stomach during treatment with omeprazole may lead to a decrease or increase in absorption of other drugs, the absorption mechanism of which depends on the acidity of the medium.

When combined use of omeprazole and HIV protease inhibitors drugs, such as nelfinavir and atazanavir, there is a decrease in their concentrations in the blood plasma.The use of omeprazole in combination with nelfinavir and atazanavir it is contraindicated.

The administration of omeprazole (20 mg once daily) in combination with digoxin to healthy volunteers caused an increase in the bioavailability of digoxin by 10%.

The manifestations of toxicity of digoxin were rarely reported. However, caution should be exercised in prescribing high doses of omeprazole to elderly patients. In this case, patients receiving therapy with digoxin should be under close medical supervision.

There was a decrease in activity of the metabolite clopidogrel at the interaction of clopidogrel and omeprazole. The clinical significance of this interaction remains unclear. In this regard, it is not recommended to apply omeprazole at combination with clopidogrel.

Absorption of posaconazole, erlotinib, ketoconazole and itraconazole is significantly reduced when combined with omeprazole, and therefore their clinical efficacy may be reduced. It is not recommended to apply omeprazole in combination with pozanazole, erlotinib, ketoconazole and itraconazole.

Omeprazole is an inhibitor of the isoenzyme CYP 2S19, therefore, the joint use of omeprazole with drugs in the metabolism of which isoenzyme participates CYP 2C19, such as warfarin and other antagonists of vitamin K, cilostazol, diazepam, phenytoin, can lead to an increase in the concentrations of these drugs in the blood plasma and require a dose reduction.

During the first two weeks after starting treatment with omeprazole, it is recommended to monitor the concentration of phenytoin in the blood plasma and continue this control until the end of treatment with omeprazole if a dose adjustment of phenytoin is carried out.

The use of omeprazole in combination with saquinavir / ritonavir resulted in an increase in plasma saquinavir concentration of approximately 70%, which was associated with good tolerability in HIV-infected patients. It was reported that the application of tacrolimus in combination with omeprazole caused an increase in its concentration in the blood plasma. It is necessary to carry out an increased control of tacrolimus concentration in plasma, as well as control of renal function (creatinine clearance) and, if necessary, dose correction of tacrolimus.

With the combined use of methotrexate with proton pump inhibitors (PPI) in somepatients there was a slight increase in the concentration of methotrexate in blood plasma. When treating high doses of methotrexate, you should temporarily stop taking omeprazole.

In the metabolism of omeprazole, isozymes participate CYP 2C19 and CYP AP4. Joint use of drugs that inhibit isoenzymes CYP 2C19 and CYP 4, such as clarithromycin and voriconazole, can cause an increase in the level of omeprazole in blood plasma as a result of a decrease in metabolic rate. Conducting concomitant treatment with voriconazole results in an increase in the effect of omeprazole by more than twofold. Since high doses of omeprazole are well tolerated, there is usually no need to adjust the dose of omeprazole. Dose adjustment may be required in patients with severe impairment of liver function and with prolonged use.

Medicines that induce isoenzymes CYP 2C19 and CYP AP4, such as rifampicin and preparations of St. John's wort perfumed, when combined with omeprazole may lead to a decrease in the concentration of omeprazole in the blood plasma, due to the acceleration of the metabolism of omeprazole.

When combined with omeprazole with clarithromycin or erythromycin, the concentration of omeprazole in the blood plasma is increased. The simultaneous administration of omeprazole with amoxicillin or metronidazole does not affect the concentration of omeprazole in the blood plasma.

The effect of omeprazole on medicines has not been revealed: antacids, theophylline, caffeine, quinidine, lidocaine, propranolol, ethanol.

Special instructions:Before the start of therapy, it is necessary to exclude the presence of a malignant process (especially with gastric ulcer), since treatment, masking symptoms (for example, significant unintended weight loss, recurrent vomiting, dysphagia, vomiting with blood or melena), may delay the correct diagnosis. Omeprazole, like all drugs that block the secretion of acid, can reduce the absorption of vitamin B12 (cyanocobalamin) because of the insufficient content of chlorine in the stomach. it

should be provided in patients with reduced body weight or with risk factors for absorption of vitamin B12 with long-term therapy.

Level up CgA may interfere with the study of neuroendocrine tumors; To avoid this, omeprazole treatment should be temporarily discontinued (five days before measurement CgA).

There is an interaction between clopidogrel and omeprazole. The clinical significance of this interaction remains unclear. As a precaution, it is not recommended to apply omeprazole in combination with clopidogrel.

Treatment with proton pump inhibitors may result in a slight increase in the risk of infectious diseases of the gastrointestinal tract caused by Salmonella and Campylobacter.

As with all long periods of treatment, especially when the treatment period is more than 1 year, patients should undergo a regular examination.

Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA). Increase in concentration CgA in blood plasma can influence the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, you must temporarily stop receiving.

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

Due to the fact that during the therapy with Helicid ® can occur: dizziness, drowsiness, blurred vision, you should be careful when driving vehicles and other potentially hazardous activities, requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Liofilizate for the preparation of a solution for infusions 40 mg.

Packaging:40 mg in bottles of colorless glass, sealed with rubber stoppers and caps of combined aluminum type "flip-off". Each vial with instructions for use is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000286

Date of registration:27.04.2010

Date of cancellation:2017-11-28

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA ZENTIVA Czech Republic

Information update date: & nbsp28.11.2017

Illustrated instructions

Instructions

Helicid® (Helicid®)