Azithromycin-Akrihin - instructions for use, dose, side effects, contraindications

excipients for tablets of 250 mg: corn starch - 47.0 mg, lactose - 50.0 mg, calcium hydrophosphate - 57.85 mg, microcrystalline cellulose - 25.0 mg, povidone - 6.0 mg, croscarmellose sodium 7.5 mg, sodium lauryl sulfate - 2,0 mg, talc 5.0 mg, magnesium stearate 6.0 mg, silicon dioxide colloid 2.0 mg;

composition of the film coating for tablets of 250 mg: hypromellose - 9.3 mg, titanium dioxide - 3.85 mg, talc - 4.45 mg, propylene glycol -1.85 mg.

excipients for tablets of 500 mg: corn starch - 30.0 mg, lactose - 45.0 mg, calcium hydrophosphate - 40.70 mg, microcrystalline cellulose - 50.0 mg, povidone -12.0 mg, croscarmellose sodium 20.0 mg, sodium lauryl sulfate - 40,0 mg, talc 6.0 mg, magnesium stearate 6.0 mg, silicon colloidal dioxide 3.0 mg;

composition of film coating for tablets of 500 mg: hypromellose - 15.5 mg, titanium dioxide - 6.45 mg, talc - 5.45 mg, propylene glycol - 3.1 mg.

Description:

250 mg tablets: White tablets of oblong form, covered with a film sheath.

The color at the break is white or almost white.

Tablets 500 mg: White tablets of oblong form, covered with a film sheath, with a risk on one side.

The color at the break is white or almost white.

Pharmacotherapeutic group:Antibiotic - azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Antibiotic of a wide spectrum of action. He is the first representative of a new subgroup of macrolide antibiotics - azalides. Communicating with 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation, suppresses protein synthesis, slows the growth and multiplication of bacteria, acts bacteriostatically, at high concentrations provides a bactericidal effect. Effects on extracorporeal and intracellular pathogens.

Active with respect to Gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except those resistant to erythromycin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Staphylococcus epidermidis, Staphylococcus aureus; Gram-negative bacteria: Haemophilius influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; a also Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi.

Azithromycin is inactive against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics:

Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity.

After oral administration of 500 mg, the maximum concentration of azithromycin in the blood plasma is achieved in 2.5 - 3.0 hours and is 0.4 mg / l. Bioavailability is 37% (the effect of "first passage" through the liver).

Azithromycin well penetrates the respiratory tract, organs and tissues of the urogenital tract (particularly the prostate gland), the skin and soft tissues.

High concentration (in tissues and cells 10-50 times higher than in blood serum) and a long half-life are due to low binding of azithromycin, volume of distribution is 31.1 l / kg. Easily passes the histohematological barriers. It penetrates well into the respiratory tract, organs and tissues of the urogenital tract (particularly the prostate gland), the skin and soft tissues; accumulates in a medium with a low pH, in lysosomes, which is especially important for the eradication of intracellular pathogens.It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages. It penetrates the membranes of cells and creates high concentrations in them.

The concentration in the foci of infection is significantly higher (by 24-34%) than in healthy tissues, and correlates with the severity of the inflammatory edema. In the focus of inflammation persists in effective concentrations within 5-7 days after taking the last dose. The connection with plasma proteins is 7-50% (inversely proportional to the concentration in the blood).

In the liver demethylated, the metabolites formed are not active. Plasma clearance - 630 ml / min: half-life (T1 / 2) between 8 and 24 hours after admission - 14-20 hours, T1 / 2 in the interval from 24 to 72 hours - 41 hours, which allows using the drug 1 time / day; 50% is excreted through the intestine in unchanged form, 6% - by the kidneys.

Indications:

- Infections of the upper respiratory tract and ENT organs caused by sensitive pathogens (pharyngitis, tonsillitis, laryngitis, sinusitis, otitis media);

- Scarlet fever;

- Infections of the lower respiratory tract (pneumonia (including atypical), bronchitis);

- Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

- Infections of the urogenital tract (gonorrheal and non-gonorrheal urethritis, cervicitis);

- Lyme disease (borreliosis), treatment of the initial stage (erythema migrans);

- Stomach ulcer and duodenal ulcer associated with Helicobacter pylori (as part of combination therapy).

Contraindications:

Hypersensitivity to antibiotics of macrolides;

Renal and / or liver failure;

Pregnancy, lactation;

Children under 12 years.

Carefully:

Arrhythmia, children with impaired liver function and / or kidney function.

Pregnancy and lactation:

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside, 1 hour before or 2 hours after meals 1 time per day.

Adults at infections of the upper and lower respiratory tract - 0.5 g / day for 1 reception for 3 days (exchange dose - 1.5 g).

With infections of the skin and soft tissues - 1 g / day on the first day for 1 reception, then 0.5 g / day daily from 2 to 5 days (course dose - 3 g).

In acute infections of the urogenital organs (uncomplicated urethritis or cervicitis) - once 1 g.

With Lyme disease (borreliosis) for treatment of stage I (erythema migrans) - 1 g on the first day and 0.5 g daily from 2 to 5 days (course dose - 3 g).

With gastric ulcer and 12 duodenal ulcer associated with Helicobacter pylori, - 1 g / day for 3 days as a combination of anti-Helicobacter therapy.

Children over 12 years old prescribe at the rate of 10 mg / kg once a day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day for 3 days (exchange dose - 30 mg / kg ).

In the treatment erythema migrans in children, the dose is 20 mg / kg on the first day and 10 mg / kg on the second to the fifth day.

Side effects:

From the digestive system: nausea (3%), diarrhea (5%), abdominal pain (3%), vomiting, flatulence, increased activity of "liver" transaminases; in children - constipation, anorexia, gastritis.

From the cardiovascular system: palpitation, pain in the chest (very rare).

From the nervous system: dizziness, headache, drowsiness, anxiety, neurosis, sleep disturbance (rarely).

From the genitourinary system: vaginal candidiasis, nephritis (less than 1%).

Allergic reactions: in some cases - rash, itching, swelling of the Quincke.

Other: increased fatigue, candidomycosis of the oral mucosa.

Overdose:

Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea.

Treatment: gastric lavage, the appointment of activated charcoal, the conduct of symptomatic therapy.

Interaction:

Antacids (Al3+ and Mg2 + -containing), ethanol and food slow down and reduce the absorption of azithromycin.

When co-administration of warfarin and azithromycin (in normal doses) changes in prothrombin time were found, however, given that the interaction of macrolides and warfarin may be increased anticoagulant effect, patients requires careful monitoring of the prothrombin time.

Digoxin: increases the concentration of digoxin by weakening its inactivation by intestinal flora.

Ergotamine and dihydroergotamine: enhance the toxic effect (vasospasm, dysesthesia).

Triazolam: reduces clearance and enhances the pharmacological action of triazolam. Slows the elimination and increases the concentration in the plasma and the toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, ciclosporin, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic drugs, theophylline and other xanthine derivatives) by inhibiting microsomal oxidation in hepatocytes with azithromycin.

Lincosamides weaken, and tetracycline and chloramphenicol increase the effectiveness of azithromycin.

Azithromycin is incompatible with heparin.

Special instructions:

In case of skipping the drug, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours.

After the drug is discontinued, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a physician.

It is necessary to observe a break of 2 hours with the simultaneous use of antacids.

Form release / dosage:Tablets, film-coated, 250 mg, 500 mg.

Packaging:

Film-coated tablets, 250 mg:

For 6 tablets per blister, PVC / aluminum. 1 blister with instructions for use in a cardboard box.

10 tablets per blister PVC / aluminum. 10 blisters with instructions for use in a cardboard box.

Film-coated tablets, 500 mg:

3 tablets per blister PVC / aluminum. 1 blister with instructions for use in a cardboard box.

10 tablets per blister PVC / aluminum. 1 or 10 blisters with instructions for use in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-000393/09

Date of registration:26.01.2009 / 19.04.2017

Expiration Date:Unlimited

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

MICRO LABS, Limited India

Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia

Information update date: & nbsp21.06.2017

Illustrated instructions

Instructions

Azithromycin-Abrichin (Azithromycin-Abrichin)