Azithromycin 125mg

Composition, form of release and packaging

Tablets - 1 tab.:

active substance: azithromycin dihydrate (in terms of azithromycin) - 125,000 mg;

excipients: microcrystalline cellulose - 9,000 mg; lactose monohydrate - 8.366 mg; povidone K-30 - 6.500 mg; crospovidone - 6,500 mg; sodium lauryl sulfate - 0.325 mg; colloidal silicon dioxide - 1.650 mg; magnesium stearate - 1.650 mg;

film coating: [hypromellose - 3,000 mg, talc - 1,000 mg, titanium dioxide - 0.550 mg, macrogol 4000 (polyethylene glycol 4000) - 0.450 mg] or [dry film coating mix containing hypromellose (60%), talc (20%) , titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] - 5,000 mg.

3 or 6 tablets in a blister pack made of PVC film and aluminum foil.

6 tablets in a high-density polyethylene jar.

2 blister packs of 3 tablets, 1 blister pack of 6 tablets or one jar together with instructions for medical use in a cardboard pack.

Description of the dosage form

Round biconvex tablets, film-coated white or almost white. In cross section, the nucleus is white or almost white.

Pharmacotherapeutic group

Antibiotic azalide.

Pharmacokinetics

After oral administration, azithromycin is well absorbed and rapidly distributed in the body. After a single dose of 500 mg, bioavailability is 37% (the "first pass" effect), the maximum concentration in the blood (0.4 mg / l) is created after 2-3 hours, the apparent volume of distribution is 31 l / kg, binding to plasma proteins inversely proportional to the concentration in the blood and is 7-50%. Penetrates through cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. It easily passes histohematic barriers and enters the tissues. The concentration in tissues and cells is 10-50 times higher than in blood plasma, and in the focus of infection it is 24-34% higher than in healthy tissues.

Azithromycin has a very long half-life of 30-50 hours. The elimination half-life from tissues is much longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is excreted mainly unchanged 50% by the intestines, 6% by the kidneys. Demethylated in the liver, losing activity.

Pharmacodynamics

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of azalide macrolides. It has a wide spectrum of antimicrobial activity. The mechanism of action of azithromycin is associated with the suppression of protein synthesis of microbial cells.

By binding to the 50S subunit of the ribosome, it inhibits the peptide translocase at the translation stage and inhibits protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations, it has a bactericidal effect.

It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms.

Microorganisms may initially be resistant to the action of an antibiotic or may acquire resistance to it.

Indications for use

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:

infections of the upper respiratory tract and ENT organs (pharyngitis, tonsillitis, sinusitis, otitis media);

infections of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis);

community-acquired pneumonia, incl. caused by atypical pathogens (see section "Special Instructions");

infections of the skin and soft tissues (acne vulgaris of moderate severity, erysipelas, impetigo, secondarily infected dermatoses);

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

urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications for use

Hypersensitivity to azithromycin, erythromycin, other macrolides, ketolides or other components of the drug;

severe liver dysfunction;

severe renal impairment (creatinine clearance (CC) less than 40 ml / min);

children under 12 years of age weighing less than 45 kg (for 500 mg tablets);

children's age up to 3 years (for tablets 125 mg);

breastfeeding period;

simultaneous reception with ergotamine and dihydroergotamine;

lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution: pregnancy; myasthenia gravis; liver dysfunction of mild and moderate severity; impaired renal function of mild and moderate severity (CC more than 40 ml / min); elderly patients; in patients with the presence of proarrhythmic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin, levofloxacin), with impaired water and electrolyte balance, especially in case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; concomitant use of digoxin, warfarin, cyclosporine

Pregnancy and lactation

Azithromycin is used during pregnancy only when the benefit to the mother outweighs the possible risk to the fetus. During treatment with azithromycin, breastfeeding is suspended.

Side effects

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - at least 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01% (including isolated cases).

Infectious diseases: infrequently - candidiasis, including the mucous membrane of the oral cavity and genitals; very rarely - pseudomembranous colitis.

From the side of metabolism and nutrition: often - anorexia.

Allergic reactions: often - skin itching, skin rash; infrequently - hypersensitivity reactions, photosensitivity reactions, urticaria, Stevens-Johnson syndrome, angioedema; very rarely - anaphylactic reaction, erythema multiforme, toxic epidermal necrolysis.

From the blood and lymphatic systems: often - eosinophilia, lymphopenia; infrequently - leukopenia, neutropenia; very rarely - thrombocytopenia, hemolytic anemia.

From the respiratory system: infrequently - pneumonia, pharyngitis, respiratory diseases, rhinitis, shortness of breath, epistaxis.

From the nervous system: often - headache, dizziness, paresthesia, impaired taste sensations; infrequently - hypesthesia, drowsiness, insomnia, nervousness; rarely - agitation; very rarely - anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell (or anosmia) and taste sensations, myasthenia gravis, anxiety; frequency unknown - perversion of smell, delirium, hallucinations.

On the part of the organ of vision: often - a violation of the clarity of vision.

On the part of the organ of hearing and labyrinth disorders: often - deafness; infrequently - tinnitus, hearing disorder; rarely - vertigo.

From the side of the cardiovascular system: infrequently - a feeling of palpitations, "tides" of blood to the skin of the face; very rarely - a decrease in blood pressure, an increase in the QT interval, pirouette-type arrhythmia, ventricular tachycardia.

From the gastrointestinal tract: very often - nausea, flatulence, abdominal pain, diarrhea; often - dyspepsia, vomiting; infrequently - constipation, gastritis, gastroenteritis, dysphagia, bloating, dryness of the oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - discoloration of the tongue, pancreatitis.

From the side of the liver and biliary tract: infrequently - an increase in the activity of "liver" transaminases, an increase in the concentration of bilirubin, hepatitis; rarely - impaired liver function; very rarely - cholestatic jaundice, liver failure (in rare cases with a fatal outcome, mainly against the background of severe liver dysfunction), liver necrosis, fulminant hepatitis.

With torons of the skin: infrequently - dermatitis, dry skin, increased sweating.

From the musculoskeletal system and connective tissue: often - arthralgia; infrequently - osteoarthritis, myalgia, back pain, neck pain.

From the genitourinary system: infrequently - an increase in the concentration of urea and creatinine in the blood plasma, dysuria, pain in the kidney area, metrorrhagia, testicular dysfunction; very rarely - interstitial nephritis, acute renal failure.

Laboratory indicators: often - a decrease in the concentration of bicarbonates in the blood plasma, an increase in the number of: basophils, monocytes, neutrophils; infrequently - an increase in the number of platelets, an increase in hematocrit; increase in alkaline phosphatase activity, increase in chlorine, increase in plasma glucose concentration, increase in plasma bicarbonate concentration, change in sodium content in blood plasma, change in potassium concentration.

Others: often - weakness; infrequently - chest pain, peripheral edema, asthenia, malaise, fatigue, swelling of the face, fever.