Azithromycin Forte-Alium pills 500mg, 3pcs

Composition

Azithromycin 500 mg

Pharmacological action

Pharmacology:

A broad-spectrum antibacterial agent, azalide, acts bacteriostatically. Binding to the 50S subunit of ribosomes, it inhibits peptidtranslase at the translation stage, suppresses protein synthesis, slows down the growth and reproduction of bacteria, and has a bactericidal effect in high concentrations. It acts on extracellular and intracellular pathogens.

Active against gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except for erythromycin resistant), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, viridans group Streptococcus, Staphylococcus epidermidis, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Prevotella bivia, Clostridium perfringens, Peptostreptococcus spp; and Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi.

Inactive against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics:  

Absorption – high, acid-resistant, lipophilic. Bioavailability after a single dose of 0.5 g – 37% (the effect of “first pass” through the liver), Cmax after oral use of 0.5 g – 0.4 mg/l, TCmax-2.5-2.9 h; in tissues and cells, the concentration is 10-50 times higher than in blood serum, the volume of distribution is 31.1 l/kg. Easily passes histohematic barriers.

It penetrates well into the respiratory tract, genitourinary organs and tissues, into the prostate gland, into the skin and soft tissues; it accumulates in a low pH environment, in lysosomes (which is especially important for the eradication of intracellularly located pathogens). It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages. Penetrates through cell membranes 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 inflammatory edema. In the focus of inflammation, it remains in effective concentrations for 5-7 days after taking the last dose. The relationship with plasma proteins is 7-50% (inversely proportional to the concentration in the blood).

It is demethylated in the liver, and the resulting metabolites are not active. The drug is metabolized by CYP3A4, CYP3A5, and CYP3A7 isoenzymes, of which it is an inhibitor. Plasma clearance – 630 ml / min: T1 / 2 between 8 and 24 hours after use-14-20 hours, T1 / 2 in the range from 24 to 72 hours-41 hours. 50% is excreted unchanged in the bile,6% – by the kidneys.

Food intake significantly changes the pharmacokinetics (depending on the dosage form): capsules – Cmax decreases (by 52%) and AUC (by 43%); suspension – Cmax increases (by 46%) and AUC (by 14%); tablets – Cmax increases (by 31%), AUC does not change.

Pharmacokinetic parameters do not change in elderly men (65-85 years), Cmax increases in women (by 30-50%), and Cmax, T1/2, and AUC decrease in children aged 1-5 years.

Indications

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

infections of the lower respiratory tract: pneumonia (including atypical, exacerbation of chronic) bronchitis;

infections of skin and soft tissues: acne vulgaris (average article of gravity), erysipelas, impetigo, secondarily infected dermatoses;

urinary tract infection: degeneracy and gonorrheal urethritis, cervicitis;

Lyme disease (early stage – erythema migrans).

Powder for the preparation of a long-acting suspension for oral use:

acute bacterial sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pneumoniae, mild to moderate severity;

community-acquired pneumonia caused by Chlamydia pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae or Streptococcus pneumoniae, mild to moderate severity.

Contraindications

Hypersensitivity (including to macrolides), severe hepatic and / or renal insufficiency, lactation, children’s age (up to 12 years with a body weight of less than 45 kg – capsules, tablets; up to 6 months – suspension for oral use: efficacy and safety have not been established).

With caution.

Pregnancy, arrhythmia (risk of ventricular arrhythmias and prolongation of the Q-T interval), hepatic and / or renal failure.

Side effects

From the digestive system: when taken orally – diarrhea (5%), nausea (3%), abdominal pain (3%); 1% or less – flatulence, vomiting, melena, cholestatic jaundice, increased activity of “liver” transaminases; in addition, in children – constipation, decreased appetite, gastritis; candidiasis of the oral mucosa.

From the cardiovascular system: palpitations, chest pain (1% or less).

From the nervous system: dizziness, headache, vertigo, drowsiness; in children-headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disorders (1% or less).

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

Allergic reactions: rash, urticaria, itchy skin, angioedema; with intravenous use-bronchospasm (1% or less).

Local reactions: with intravenous use-pain and inflammation at the injection site.

Other: asthenia, photosensitization; conjunctivitis in children; taste changes (1% or less).

Interaction

Antacids (Al3+ and Mg2+-containing), ethanol and food slow down and reduce the absorption of azithromycin (for oral forms), so the interval between their intake should be 1 hour before or 2 hours after food intake and these drugs.

When warfarin and azithromycin were co-administered (in normal doses), no changes in prothrombin time were detected, however, given that the interaction of macrolides and warfarin may increase the anticoagulation effect, patients should carefully monitor prothrombin time.

It does not bind to cytochrome P450 enzymes, and unlike macrolides, it does not interact with theophylline, terfenadine, carbamazepine, triazolam, or digoxin.

Caution should be exercised when co-prescribing terfenadine and azithromycin, as it has been found that concomitant use of terfenadine and various types of antibiotics causes arrhythmia and prolongation of the Q-T interval. Based on this, the above-mentioned complications cannot be excluded when taking terfenadine and azithromycin together.

Ergotamine and dihydroergotamine: increased toxic effects (vasospasm, dysesthesia).

Macrolides slow down the elimination, increase the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic drugs), However, when using azalides (including azithromycin), this type of interaction was not observed.

Lincosamides weaken, and tetracycline and chloramphenicol enhance the effectiveness of azithromycin Pharmacologically incompatible with heparin.

How to take, course of use and dosage

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

Adults with infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues – 0.5 g / day for 1 dose for 3 days (course dose-1.5 g). Acne vulgaris-0.5 g / day for 1 dose for 3 days, then 0.5 g / day 1 time a week for 9 weeks. The first weekly tablet should be taken 7 days after taking the first daily tablet (8 days from the start of treatment), the next 8 weekly tablets – at intervals of 7 days.

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

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

Children are prescribed 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 (the course dose is 30 mg/kg).

Overdose

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

Special instructions

If a missed dose is missed, the missed dose should be taken as early as possible, and subsequent doses should be taken at 24 – hour intervals. It is necessary to observe a break of 2 hours with simultaneous use of antacids.

The safety of prescribing azithromycin (intravenously, as well as in the form of capsules and tablets) in children and adolescents under 16 years of age has not been definitively established (it is possible to use it as an oral suspension in children from 6 months and older).

After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a doctor.

Form of production

Pills.

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Nursing mothers as prescribed by a doctor, Pregnant women as prescribed by a doctor, Children over 12 years of age, For adults

Indications

Otitis Media, Pneumonia, Infectious Diseases, Sore Throat, Bronchitis, Urethritis, Skin infections