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. pulori for duodenal ulcer.

Pharmacological effect

Pilobact AM – anti-Helicobacter, anti-ulcer.

Pharmacodynamics

Triple therapy, including omeprazole, clarithromycin and amoxicillin, achieves a high percentage of Helicobacter pylori eradication (85–94%).

Omeprazole inhibits the secretion of gastric acid due to the specific inhibition of H+ K+-ATPase, an enzyme located 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 dose of the drug orally, the effect of omeprazole occurs within the first hour and continues for 24 hours, the maximum effect is achieved after 2 hours. After stopping the drug, secretory activity is completely restored after 3-5 days.

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

Amoxicillin is a semi-synthetic penicillin, has a bactericidal effect and has a wide spectrum of action. The antimicrobial effect is associated with inhibition of the synthesis of peptidoglycan (the supporting polymer of the cell wall) during division and growth. It has pronounced activity against H. pulori. Resistance of H. pulori to amoxicillin is rare.

The combination of amoxicillin and clarithromycin has a potent antimicrobial effect against H. pulori.

Pharmacokinetics

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

Omeprazole is rapidly absorbed after oral administration, and its bioavailability is 30–40%. Food intake does not affect the bioavailability of omeprazole. Cmax of the drug in plasma is achieved after 0.5–1 hour. Plasma protein binding is 90%. 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%. Eating slightly slows down the onset of absorption of clarithromycin and the formation of 14-hydroxyclarithromycin, but does not affect bioavailability. When taken on an empty stomach, Cmax in serum is achieved within 2 hours after oral administration and is 0.6 and 0.7 mcg/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 tissues exceeds that in serum. Protein binding ranges from 42 to 70%. It is excreted by the kidneys and in 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 increases by 10%, the minimum concentration by 15% compared with the same indicators with clarithromycin monotherapy. The concentration of clarithromycin in the gastric mucosa is also increased when administered simultaneously with omeprazole.

Amoxicillin is rapidly absorbed from the gastrointestinal tract. Eating does not affect the absorption of amoxicillin. The bioavailability of amoxicillin is 75–90%. The drug is quickly distributed in the tissues of the body. T1/2 is 1–1.5 hours. Protein binding is 20%. About 60% of the dose taken is excreted unchanged in the urine, and a small amount is excreted in feces.

Special instructions

Before starting therapy, it is necessary to exclude the presence of a malignant process (especially with a stomach ulcer), because Treatment, masking symptoms, can delay the correct diagnosis.

Prescribe with caution while taking medications metabolized by the liver. In case of co-administration with warfarin or other indirect anticoagulants, PT must be monitored.

If you have a history of heart disease, simultaneous use with terfenadine, cisapride, or astemizole is not recommended.

Active ingredient

Amoxicillin, Clarithromycin, Omeprazole

Composition

Pills

Active ingredient:

clarithromycin 500 mg;

Excipients:

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;

Ink composition for inscription:

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

Capsules

Active ingredient:

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

Excipients:

sodium lauryl sulfate;

colloidal silicon dioxide;

croscarmellose;

MCC;

magnesium stearate;

Capsule cap:

brilliant blue dye; Azorubine 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;

Ink for the inscription:

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

Enteric capsules

Active ingredient:

omeprazole 20 mg;

Excipients:

Non Pareil Seeds (enteric-coated sucrose and corn starch granules);

lactose;

corn starch;

mannitol;

povidone;

purified talc;

sodium lauryl sulfate;

sodium hydrogen phosphate (anhydrous);

Enteric coating composition:

hypromelose phthalate, dichloromethane*, isopropanol*, diethyl phthalate, titanium dioxide, shell of an empty hard gelatin capsule size No. 2 with a dark blue cap and a transparent pink body;

Capsule cap:

brilliant blue; carmoisine (azorubine); gelatin; methyl parahydroxybenzoate; propyl parahydroxybenzoate;

Capsule body:

carmoisine (azorubine); gelatin; methyl parahydroxybenzoate; propyl parahydroxybenzoate

Contraindications

hypersensitivity to omeprazole, clarithromycin or amoxicillin, as well as to macrolide antibiotics;
combined use with cisapride, pimozide, astemizole and terfenadine (see “Interaction”);
pregnancy;
breast-feeding;
porphyria;
childhood;
renal or liver failure.

Side Effects

From the digestive system: dysbacteriosis, diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain, dry mouth, taste disturbances, stomatitis, transient increase in the activity of liver enzymes in plasma, impaired liver function, rarely – pseudomembranous enterocolitis.

From the nervous system: headache, dizziness, agitation, drowsiness, insomnia, ataxia, paresthesia, depression, confusion, hallucinations, epileptic reactions, peripheral neuropathy.

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

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

From the skin: itching; rarely – skin rash, in some cases – photosensitivity, exudative erythema multiforme, alopecia.

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

Other: tachycardia, interstitial nephritis, blurred vision, peripheral edema, increased sweating, fever, gynecomastia.

Interaction

The simultaneous administration of theophylline and clarithromycin is accompanied by an increase in theophylline concentration.

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

Simultaneous administration of clarithromycin with indirect anticoagulants may potentiate the effect of the latter.

When co-administered with 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.

When amoxicillin is prescribed simultaneously with oral contraceptives, the effect of the latter may be reduced.

Storage conditions

In a dry place, at a temperature not exceeding 25 °C.

Shelf life

2 years

Manufacturer

Sun Pharmaceutical Industries Ltd, India