Azithromycin pills 125mg 6pcs

Composition

The composition of 1 tablet includes:

Active ingredients:

azithromycin (in the form of dihydrate) – 125 mg,

Auxiliary substances:

microcrystalline cellulose – 9 mg,

lactose monohydrate-8.366 mg,

povidone (K-30) – 6.5 mg,

crospovidone-6.5 mg,

sodium lauryl sulfate-0.325 mg,

colloidal silicon dioxide-1.65 mg,

magnesium stearate-1.65 mg.

Composition of the film shell:  hypromellose-3 mg, talc-1 mg, titanium dioxide-0.55 mg, macrogol 4000-0.45 mg

Pharmacological action

An antibiotic of the macrolide group, it is a representative of azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. Binding to the 50S subunit of ribosomes, it inhibits peptidtranslase at the translation stage, suppresses protein synthesis, and slows down the growth and reproduction of bacteria. It acts bacteriostatically. In high concentrations, it has a bactericidal effect.

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

To azithromycin sensitive gram-positive cocci: Streptococcus pneumoniae (penicillin-susceptible strains), Streptococcus pyogenes, Staphylococcus aureus (methicillin-susceptible strains); aerobic gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae; some anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp. Porphyriomonas spp. ; as well as Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Microorganisms with acquired resistance to azithromycin: aerobic gram-positive microorganisms-Streptococcus pneumoniae (penicillin-resistant strains and strains with moderate sensitivity to penicillin).

Microorganisms with natural resistance:  aerobic gram-positive microorganisms-Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis (methicillin-resistant strains), anaerobic microorganisms – Bacteroides fragilis.

Cases of cross-resistance between Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic streptococcus group A), Enterococcus faecalis and Staphylococcus aureus (methicillin-resistant strains) to erythromycin, azithromycin, other macrolides and lincosamides are described.

Azithromycin has not been used for the treatment of infectious diseases caused by Salmonella typhi (MIC < 16 mg / l) and Shigella spp.

After oral use, azithromycin is well absorbed and quickly distributed in the body. After a single 500 mg dose, the bioavailability is 37% due to the “first pass” effect through the liver. _Cmax in blood plasma is reached in 2-3 hours and is 0.4 mg/l.

Binding to proteins is inversely proportional to the concentration in blood plasma and is 7-50%. The apparent Vd is 31.1 l / kg. Penetrates 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 penetrates through histohematic barriers and enters the tissues. The concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection-24-34% higher than in healthy tissues.

The drug is metabolized in the liver. The metabolites do not have antimicrobial activity.

T_1/2 very long – 35-50 h. T_1/2 of the fabrics is much larger. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged-50% through the intestines,6% by the kidneys.

After intravenous infusion, azithromycin quickly penetrates from the blood serum into the tissues. Concentrating in phagocytes and not disrupting their function, azithromycin migrates to the focus of inflammation, accumulating directly in infected tissues.

The pharmacokinetics of azithromycin in healthy volunteers after a single intravenous infusion lasting more than 2 hours at a dose of 1-4 g (solution concentration of 1 mg/ml) has a linear relationship and is proportional to the administered dose.

In healthy volunteers, intravenous infusion of azithromycin at a dose of 500 mg (solution concentration of 1 mg/ml) for 3 hours resulted in a serum cmax of 1.14 mcg/ml. Serum cmin (0.18 mcg/ml) was observed for 24 hours and AUC was 8.03 mcg×ml / h. Similar pharmacokinetic values were obtained in patients with community-acquired pneumonia who were given intravenous 3-hour infusions for 2 to 5 days. Vd is 33.3 l/kg.

After use of azithromycin daily at a dose of 500 mg (infusion duration 1 h) for 5 days, an average of 14% of the dose is excreted by the kidneys during the 24-hour dosing interval.

T_1/2 is 65-72 h_{. High} Vd (33.3 l / kg) and high plasma clearance (10.2 ml/min/kg) suggest that prolonged T_1/2 is a consequence of the accumulation of the antibiotic in the tissues, followed by its slow release.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

— infections of the upper respiratory tract and respiratory tract: pharyngitis, tonsillitis, sinusitis, otitis media

— infection of the lower respiratory tract: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, incl. caused by atypical pathogens;

infection of the skin and soft tissues: acne vulgaris moderate, erysipelas, impetigo, secondarily infected dermatoses;

— the initial stage of Lyme disease (borreliosis) is a migratory erythema (erythema migrans);

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

Contraindications

-severe hepatic and / or renal insufficiency;

— children under 12 years of age with a body weight of less than 45 kg (for this dosage form);

— breastfeeding;

— simultaneous use with ergotamine and dihydroergotamine;

— hypersensitivity to macrolide antibiotics.

With caution

-moderate violations of liver and kidney function—

– with arrhythmias or predisposition to arrhythmias and prolongation of the QT interval;

– with the combined use of terfenadine, warfarin, digoxin.

Side effects

From the digestive system:  nausea, vomiting, diarrhea, abdominal pain, loose stools, flatulence, indigestion, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory liver function, liver failure, liver necrosis (possibly fatal).

Allergic reactions: pruritus, skin rashes, angioedema, urticaria, photosensitization, anaphylactic reaction (rarely fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the cardiovascular system:  palpitations, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.

Nervous system disorders: dizziness/vertigo, headache, seizures, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, restlessness, nervousness.

From the side of the senses: tinnitus, reversible hearing loss up to deafness (when taking high doses for a long time), impaired perception of taste and smell.

From the circulatory and lymphatic systems: thrombocytopenia, neutropenia, and eosinophilia.

From the musculoskeletal system: arthralgia.

From the genitourinary system: interstitial nephritis, acute renal failure.

Other services: vaginitis, candidiasis.

Interaction

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum concentration in the blood by 30%, so the drug should be taken at least 1 hour before or 2 hours after taking these drugs and eating.

When used parenterally, azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, co-trimoxazole (sulfamethoxazole + trimethoprim) in plasma when administered together, however, the possibility of such interactions should not be excluded when prescribing azithromycin for oral use.

If necessary, combined use with cyclosporine is recommended to monitor the content of cyclosporine in the blood.

When taking digoxin and azithromycin together, it is necessary to monitor the concentration of digoxin in the blood, since many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma.

If co-use with warfarin is necessary, careful monitoring of prothrombin time is recommended.

Concomitant use of terfenadine and macrolide antibiotics causes arrhythmia and prolongation of the QT interval. Based on this, the above-mentioned complications cannot be excluded when taking terfenadine and azithromycin together.Since there is a possibility of inhibition of the CYP3A4 isoenzyme by azithromycin in parenteral form when co-administered with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs that are metabolized with the participation of this isoenzyme, the possibility of such interaction should be considered when prescribing azithromycin for oral use.

When azithromycin and zidovudine are co-administered, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or the renal excretion of zidovudine and its glucuronated metabolite. However, the concentration of the active metabolite, phosphorylated zidovudine, increases in peripheral vascular mononuclear cells. The clinical significance of this fact is unclear.

Concomitant use of macrolides with ergotamines and dihydroergotamine may cause their toxic effects.

How to take, course of use and dosage

Azithromycin is taken orally 1 time/day for 500 mg, regardless of food intake.

Adults (including the elderly) and children over 12 years of age with a body weight over 45 kg

For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 500 mg 1 time/day for 3 days (course dose-1.5 g).

For acne vulgaris of moderate severity: 2 capsules of 250 mg 1 time/day for 3 days, then 250 mg 2 times a week for 9 days. The course dose is 6.0 g.

With erythema migrans: on the first day,2 capsules of 500 mg at the same time, then from the 2nd to the 5th day,500 mg daily. The course dose is 3.0 g.

For urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): simultaneously 2 capsules of 500 mg each.

Use in patients with impaired renal function: no correction is required for patients with moderate renal impairment (creatinine clearance > 40 ml/min).

Overdose

Symptoms: temporary hearing loss, nausea, vomiting, diarrhea. Treatment: symptomatic.

Special instructions

If you miss taking an antibiotic, the missed dose should be taken as early as possible, and subsequent doses should be taken at 24-hour intervals.

After discontinuation of azithromycin therapy, hypersensitivity reactions in some patients may persist for a long time and may require specific therapy under the supervision of a doctor.

Influence on the ability to drive motor vehicles and manage mechanisms

Given the likelihood of side effects from the central nervous system, caution should be exercised when driving vehicles and working with mechanisms.

Storage conditions

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

Shelf life

3 years

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for children as prescribed by a doctor

Indications

Infectious diseases, Sinusitis, Tonsillitis, Respiratory Tract Infections, Chlamydia, Urethritis, Sore Throat, Pneumonia, Bronchitis, Urinary Tract Infections, Pharyngitis, Sinusitis, Skin Infections, Otitis