Pilobakt AM, tablets and capsules set 7 pcs

Pilobact AM is an anti-Helicobacter, antiulcer.

Pharmacodynamics

The triple therapy including omeprazole, clarithromycin and amoxicillin allows to achieve a high percentage of eradication of Helicobacter pylori (85-94%).

Omeprazole inhibits gastric acid secretion through specific inhibition of H⁺ K⁺-ATPase, an enzyme located in the membranes of the parietal cells of the gastric mucosa. It reduces basal and stimulated secretion regardless of the nature of the stimulus. After a single oral dose, the action of omeprazole occurs within the first hour and continues for 24 hours, the maximum effect being reached after 2 hours. After discontinuation of the drug secretory activity is fully restored after 3-5 days.

Clarithromycin is an antibiotic of the macrolide group, a semi-synthetic derivative of erythromycin A. It has antimicrobial action, which is associated with inhibition of protein synthesis by interaction with 50S ribosomal subunit of the microbial cell. It is effective against a large number of Gram-positive, Gram-negative aerobic and anaerobic microorganisms, including H. рylori. Metabolite 14-hydroxyclarithromycin, which forms in the body, also has marked antimicrobial activity.

Amoxicillin is a semisynthetic penicillin with bactericidal action, has a broad spectrum of action. Its antimicrobial action is due to inhibition of peptidoglycan synthesis (support polymer of cell wall) during division and growth. It has a pronounced activity against H.rulori. Resistance of H.рylori to amoxicillin is rare.

The combination of amoxicillin and clarithromycin has potentiated antimicrobial effect against H. рylori.

Pharmacokinetics

All three drugs in Pilobact ^® AM have good absorption when taken orally.

Omeprazole is rapidly absorbed after oral administration and its bioavailability is 30-40%. Food intake has no effect on the bioavailability of omeprazole. C_max of the drug in plasma is reached after 0.5-1 h. Binding to plasma proteins is 90%. The drug is almost completely metabolized in the liver. The main route of excretion is with urine (80%).

Clarithromycin is rapidly absorbed from the gastrointestinal tract. Absolute bioavailability of 250 mg clarithromycin is approximately 50%. Food intake slightly slows down the onset of clarithromycin absorption and formation of 14-hydroxyclarithromycin, but does not affect bioavailability. When taken on an empty stomach, C_max in serum is reached within 2 h after oral administration and is 0.6 and 0.7 µg/mL for clarithromycin and its major metabolite. T_1/2 of clarithromycin is 3-4 h. Clarithromycin is widely distributed in the body. Clarithromycin concentration in tissues is higher than that in serum. Protein binding is 42 to 70%. It is excreted by the kidneys and in the faeces (20-30% unchanged, the rest as metabolites). Concomitant administration of clarithromycin and omeprazole improves pharmacokinetic properties of clarithromycin: mean C_max is increased by 10% and minimum concentration by 15% compared to those of clarithromycin monotherapy. The concentration of clarithromycin in the gastric mucosa is also increased when concomitantly administered with omeprazole.

Amoxicillin is rapidly absorbed from the gastrointestinal tract. Food intake has no effect on the absorption of amoxicillin. Bioavailability of amoxicillin is 75-90%. The drug is rapidly distributed in the body tissues. T_1/2 is 1-1.5 h. Protein binding is 20%. About 60% of the dose taken is excreted unchanged in the urine, a small amount in the feces.

Indications

Eradication therapy of H. рylori in duodenal ulcer disease.

Composition

Tablets

The active ingredient:

clarithromycin 500 mg;

Associates:

MCC;

povidone;

magnesium stearate;

steric acid;

purified talc;

colloidal silicon dioxide;

croscarmellose sodium;

Film coating:

Hypromellose; hyprolose; propylene glycol; sorbitan monooleate; titanium dioxide; quinoline yellow dye; vanillin; purified talc;

Composition of ink for inscription:

The Opacode S-1-27794 black ink (IMS 74 OP methylated alcohol, 47.5% solution of shellac in IMS 74 OP methylated alcohol, black iron oxide dye, n-butyl alcohol, propylene glycol, purified water);

Capsules

Active substance:

amoxicillin trihydrate 592.856 mg (corresponding to 500 mg of amoxicillin);

Associates:

sodium lauryl sulfate;

silicon dioxide colloid;

p> croscarmellose;

MCC;

Magnesium stearate;

Capsule cap:

Brilliant blue dye; azorubin dye; quinoline yellow dye; titanium dioxide; methyl parahydroxybenzoate; propyl parahydroxybenzoate; sodium lauryl sulfate; gelatin;

Capsule body:

Sunset yellow dye; quinoline yellow dye; titanium dioxide; methyl parahydroxybenzoate; propyl parahydroxybenzoate; sodium lauryl sulfate; gelatin;

Inscription ink:

dehydrated alcohol; butyl alcohol; shellac; iron oxide black dye; concentrated ammonia solution; propylene glycol;

Energy-soluble capsules

Active ingredient:

omeprazole 20 mg;

Associates:

Non Pareil Seeds (sucrose and corn starch granules, coated with an enteric soluble coating);

Lactose;

Corn starch;

Mannitol;

How to take, the dosage

Ingestion. Each strip containing Pilobact® tablets and capsules AM is for one day of treatment and consists of two parts: the red part labeled “morning” and the blue part labeled “evening.

In the morning dose, the entire contents of the “morning” part (one omeprazole capsule, one clarithromycin tablet and two amoxicillin capsules) should be taken before meals. In the evening, take the entire contents of the “evening” part before meals (one capsule of omeprazole, one tablet of clarithromycin, and two capsules of amoxicillin).

The tablets and capsules must not be crushed or chewed, they must be swallowed whole. The duration of treatment is 7 days.

Interaction

The concomitant administration of theophylline and clarithromycin is accompanied by an increase in theophylline concentrations.

The concomitant administration of clarithromycin with terfenadine increases the concentration of the latter and may lead to prolongation of the QT interval.

The concomitant administration of clarithromycin with indirect anticoagulants may potentiate the effects of the latter.

The levels of carbamazepine, cyclosporine, phenytoin, disopyramide, lovastatin, valproate, cisapride, pimozide, astemizole, digoxin may be elevated when concomitantly prescribed with clarithromycin.

Omeprazole may delay elimination of phenytoin, diazepam, warfarin, and affect absorption of ketoconazole, ampicillin and iron salts by inhibiting acid secretion in the stomach.

When concomitant administration of amoxicillin with oral contraceptives may reduce the effect of the latter.

Special Instructions

Before starting therapy, it is necessary to rule out the presence of a malignant process (especially for gastric ulcers), because treatment, by masking symptoms, can delay the correct diagnosis.

With caution, it is prescribed while taking drugs that are metabolized by the liver. If co-administered with warfarin or other indirect anticoagulants, PV should be monitored.

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

Contraindications

With caution: renal and/or hepatic insufficiency, glucose-6-phosphate dehydrogenase deficiency, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), viral hepatitis, alcoholic hepatitis, advanced age.

Side effects

Digestive system disorders: dysbacteriosis, diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mouth, taste disorders, stomatitis, transient increase in plasma liver enzyme activity, liver function impairment, rarely – pseudomembranous enterocolitis.

Nervous system disorders: headache, dizziness, agitation, somnolence, insomnia, ataxia, paresthesia, depression, confusion, hallucinations, epileptic reactions, peripheral neuropathy.

Musculoskeletal system: muscle weakness, myalgia, arthralgia.

Hematopoietic system disorders: leukopenia, neutropenia, thrombocytopenia, thrombocytopenic purpura, anemia.

Skin disorders: itching; rarely – skin rash, in some cases – photosensitization, erythema multiforme exudative, alopecia.

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

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