Pilobact set of tablets and capsules, No. 7

Each strip of PilobactЃ contains two capsules of omeprazole (20 mg each), two clarithromycin tablets (250 mg each) and two tinidazole tablets (500 mg each), and is designed for 1 day of treatment.

Take one omeprazole capsule, one clarithromycin tablet and one tinidazole tablet by mouth 2 times a day during or after meals in the morning and evening. Tablets and capsules should not be broken or chewed and should be swallowed whole.

Duration of treatment is 7 days.

Combined set (daily dose)

Blister contains:

capsules (2 pcs. per pack) 1 caps.

omeprazole 20 mg

coated tablets (2 pcs. per pack) 1 tab.

clarithromycin 250 mg

coated tablets (2 pcs. per pack) 1 tab.

tinidazole 500 mg

• hypersensitivity to omeprazole, clarithromycin or tinidazole, as well as macrolide antibiotics;

• combined use with cisapride, pimozide, astemizole, terfenadine, ethanol is prohibited;

• pregnancy;

• lactation period;

• organic diseases of the central nervous system;

• porphyria;

• oppression of bone marrow hematopoiesis;

• childhood;

• renal and / or hepatic impairment.

pharmachologic effect

Omeprazole inhibits gastric acid secretion due to specific inhibition of H + K + -ATPase - an enzyme found in the membranes of parietal cells of the gastric mucosa. Reduces basal and stimulated secretion regardless of the nature of the stimulus. After a single oral dose of the drug, the effect of omeprazole occurs within the first hour and lasts for 24 hours, the maximum effect is achieved after 2 hours. After stopping the drug intake, the secretory activity is fully restored after 3-5 days.

Clarithromycin is a semi-synthetic antibiotic from the group of broad-spectrum macrolides. It has an antimicrobial effect, which is associated with the suppression of protein synthesis by interacting with the 50S ribosomal subunit of a microbial cell. Effective against a large number of gram-positive, gram-negative aerobic and anaerobic microorganisms, including Helicobacter pylori. The metabolite 14-hydroxyclarithromycin formed in the body also has a pronounced antimicrobial activity.

Tinidazole inhibits synthesis and damages the DNA structure of bacteria. Has activity against anaerobic bacteria, protozoa and Helicobacter pylori.

Pharmacokinetics

All three drugs in PilobactЃ are well absorbed when taken orally.

Omeprazole is rapidly absorbed after oral administration, its bioavailability is 30-40%. Food intake does not affect the bioavailability of omeprazole. Cmax is achieved in 0.5-1 hours. The connection with plasma proteins is 90%. It is almost completely metabolized in the liver. The main route of excretion is in the urine (80%).

Clarithromycin is rapidly absorbed from the gastrointestinal tract. The absolute bioavailability of 250 mg clarithromycin is approximately 50%. Food intake slightly slows down the onset of clarithromycin absorption and the formation of 14-hydroxyclarithromycin, but does not affect bioavailability. When taken on an empty stomach, peak serum concentrations are reached within 2 hours after oral administration and are 0.6 and 0.7 ?g / ml for clarithromycin and its main metabolite. T1 / 2 of clarithromycin is 3-4 hours. Clarithromycin is widely distributed in the body. The concentration of clarithromycin in the tissues is higher than that in the serum. The connection with proteins ranges from 42 to 70%. It is excreted by the kidneys and with feces (20-30% in unchanged form, the rest in the form of metabolites). The simultaneous administration of clarithromycin and omeprazole improves the pharmacokinetic properties of clarithromycin:the average Cmax value increases by 10%, the minimum concentration - by 15% in comparison with the same indicators with clarithromycin monotherapy. The concentration of clarithromycin in the gastric mucosa with simultaneous administration with omeprazole is also increased.

The bioavailability of tinidazole is about 100%. Communication with plasma proteins 12%. Time to reach Cmax 2 hours. Penetrates the BBB, placenta. Excreted in breast milk. It is metabolized in the liver with the formation of pharmacologically active hydroxylated derivatives, which can enhance the effect of tinidazole. T1 / 2 is 12-14 hours. It is excreted in the bile 50%, by the kidneys - 25% unchanged and 12% in the form of metabolites. It undergoes reabsorption in the renal tubules.

Side effect

On the part of the digestive system: dysbiosis, diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mouth, taste disturbance, metallic taste in the mouth, decreased appetite, stomatitis, transient increase in the activity of liver enzymes in plasma, impaired liver function, hepatitis (including jaundice), in patients with previous liver disease - encephalopathy; rarely pseudomembranous enterocolitis.

From the side of the central nervous system: headache, dizziness, agitation, fatigue, weakness, drowsiness, insomnia, ataxia, paresthesia, depression, confusion, hallucinations, epileptic reactions, peripheral neuropathy, convulsions, fear, nightmares, disorientation, psychosis, depersonalization, noise in ears.

From the musculoskeletal system: muscle weakness, myalgia, arthralgia.

From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, thrombocytopenic purpura, anemia.

On the part of the skin: itching; rarely - skin rash; in some cases - photosensitivity, exudative erythema multiforme, alopecia.

Allergic reactions: urticaria, angioedema, bronchospasm and anaphylactic shock.

Others: tachycardia, interstitial nephritis, visual impairment, peripheral edema, increased sweating, fever, gynecomastia.

Application during pregnancy and lactation

Contraindicated during pregnancy and lactation.

Application for violations of liver function

The drug is contraindicated in liver failure.

Application for impaired renal function

The drug is contraindicated in renal failure.

Application in children

The drug is contraindicated in childhood.

special instructions

Before starting therapy, it is necessary to exclude the presence of a malignant process, because treatment, masking the symptoms, can delay the correct diagnosis.

It is prescribed with caution while taking medications metabolized by the liver. In the case of a joint appointment with warfarin or other indirect anticoagulants, it is necessary to control the prothrombin time.

With a history of heart disease, concomitant use with terfenadine, cisapride, astemizole is not recommended.

Tinidazole causes dark discoloration of urine.

Influence on the ability to drive vehicles and control mechanisms.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Clarithromycin

Symptoms: from the gastrointestinal tract (nausea, vomiting, diarrhea); headache, confusion.

Treatment: immediate gastric lavage and symptomatic treatment. Hemodialysis and peritoneal dialysis do not significantly alter serum clarithromycin levels.

Amoxicillin

Symptoms: nausea, vomiting, diarrhea, imbalance in water and electrolyte balance (as a result of vomiting and diarrhea).

Treatment: gastric lavage, activated charcoal, saline laxatives, medicines to correct water-electrolyte balance, hemodialysis.

Tinidazole

In case of an overdose of tinidazole, symptomatic treatment is prescribed. Hemodialysis is effective.

Drug interactions

The simultaneous administration of theophylline and clarithromycin is accompanied by an increase in theophylline concentration. Clarithromycin reduces the absorption of zidovudine (there should be an interval of at least 4 hours between the use of drugs). Cross-resistance may develop between clarithromycin, lincomycin and clindamycin.

Concomitant administration of clarithromycin with terfinadine increases the concentration of the latter and may lead to prolongation of the QT interval.

The simultaneous administration of clarithromycin with indirect anticoagulants can potentiate the effect of the latter.

With the simultaneous administration of clarithromycin, the levels of carbamazepine, cyclosporine, phenytoin, disopyramide, lovastatin, valproate, cisapride, pimozide, astemizole, digoxin may be increased.

Omeprazole can slow down the elimination of phenytoin, diazepam, warfarin, and also affect the absorption of ketoconazole, ampicillin and iron salts by inhibiting acid secretion in the stomach. Strengthens the inhibitory effect on the hematopoietic system and other drugs.

Tinidazole enhances the effect of indirect anticoagulants and the effect of ethanol - disulfiram-like reactions are possible. It is not recommended to prescribe together with ethionamide. Phenobarbital accelerates the metabolism of tinidazole.