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

The drug, in difference from erythromycin, less effective against staphylococci and more effective against hemophilic rods, enterobacteria, legionella, toxoplasm. Creates the highest concentrations among macrolides in tissues. It is an agonist of the motilin receptors of the gastrointestinal tract.

Azithromycin is a semi-synthetic 15-membered macrolide that belongs to the subclass of azalides, since it contains a nitrogen atom in the macrocyclic ring.

A bacteriostatic antibiotic interacts with the 50S subunit of bacterial ribosomes, blocking the synthesis of the protein during the translocation stage. The preparation disrupts the process of transferring the formed peptide from the A site to the P region by binding to a specific ligand in the ribosomal tunnel from which the resulting peptides leave.In high concentrations bactericidal effect on pneumococci, β-hemolytic group A streptococcus, causative agents of pertussis and diphtheria. Effective against gram-positive cocci (streptococci, staphylococcus), gram-negative cocci (gonococci, meningococcus), hemophilic rod, Borrelia, pale treponema, Helicobacter pylori. Well penetrates into cells and is active against intracellular pathogens (chlamydia, legionella, ureaplasma and mycoplasma).

The drug is active against: Staphylococcus aureus, Streptococcus spp., Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus ducreyi, Moraxella catarrhalis, Escherichia coli, Bordetella pertussis, Bordetella parapertussis, Borrelia burgdorferi, Neisseria gonorrhoeae, Campylobacter spp., Legionella pneumophila, Bacteroides fragilis, Chlamydia trachomatis, Mycoplasma pneumoniae, Mycoplasma hominis, Treponema pallidum, Toxoplasma gondii.

Pharmacokinetics:

It is well absorbed from the gastrointestinal tract. Bioavailability - 37%, decrease when eating. Relationship with plasma proteins 7-50%. V_d - 31 l / kg, the concentration in the tissues is 10-100 times higher than in the blood plasma; accumulates intracellularly in phagocytes and fibroblasts, weakly penetrates into the central nervous system. 35% of the drug is metabolized in the liver by demethylation. Half-life - 11-14 hours (single dose), 2-4 days (several doses).

More than 59% are excreted with bile in the unchanged form, approximately 4.5% is excreted by the kidneys in an unchanged form.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms.

For oral administration: infection of the upper (streptococcal pharyngitis / tonsillitis) and lower (bacterial bronchitis, interstitial and alveolar pneumonia, exacerbation of chronic bronchitis) of the respiratory tract, ENTorganisms (otitis media, laryngitis and sinusitis), urogenital system (urethritis and cervicitis), skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses), chronic stage of migrating erythema (Lyme disease), stomach and duodenal diseases associated with Helicobacter pylori.

For infusions: severe infections caused by sensitive strains of microorganisms: community-acquired pneumonia, infectious-inflammatory diseases of the pelvic organs.

ICD-10

I.A30-A49.A31.0 Pulmonary infection caused by Mycobacterium

I.A30-A49.A46 Erys

I.A30-A49.A48.1 Legionnaires' disease

I.A50-A64.A54 Gonococcal infection

I.A65-A69.A69.2 Lyme disease

VIII.H65-H75.H66 Purulent and unspecified otitis media

X.J00-J06.J01 Acute Sinusitis

X.J00-J06.J02 Acute pharyngitis

X.J00-J06.J02.0 Streptococcal pharyngitis

X.J00-J06.J04.0 Acute laryngitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J10-J18.J15.7 Pneumonia caused by Mycoplasma pneumoniae

X.J10-J18.J16.0 Pneumonia caused by chlamydia

X.J10-J18.J18 Pneumonia without clarification of the pathogen

X.J20-J22.J20 Acute bronchitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J35.0 Chronic tonsillitis

X.J30-J39.J37.0 Chronic laryngitis

X.J40-J47.J40 Bronchitis, not specified as acute or chronic

X.J40-J47.J42 Chronic bronchitis, unspecified

XI.K20-K31.K25 Stomach ulcer

XI.K20-K31.K26 Duodenal ulcer

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XII.L20-L30.L30.3 Infectious dermatitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N30-N39.N39.0 Urinary tract infection without established localization

XIV.N40-N51.N49 Inflammatory diseases of male genital organs, not elsewhere classified

XIV.N70-N77.N72 Inflammatory disease of the cervix

XIV.N70-N77.N73.9 Inflammatory diseases of female pelvic organs, unspecified

Contraindications:

Hypersensitivity, liver and kidney disease, age of up to 6 months (as a suspension), age of 12 years with a body weight of less than 45 kg (oral administration in the form of tablets), age 16 years (infusion).

Carefully:

Predisposition to arrhythmia and lengthening of the interval QT, arrhythmia.

Pregnancy and lactation:

Category FDA - B. Application in pregnancy only in the case when the potential benefit to the mother exceeds the potential risk for the child. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Adults: 0,25-1 g once a day.

Children: 5-10 mg / kg once a day.

Before use, consult a doctor, the final dosage is determined individually.

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

With infection of the upper and lower respiratory tract, infections of the skin and soft tissues - 500 mg each dayki for 3 days (the course dose is 1.5 g).

With uncomplicated urethritis and / or cervicitis - once 1 g (4 capsules of 250 mg).

With Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) - 1 g (4 250 mg capsules) on the first day and 500 mg daily from the 2nd to the 5th day (the course dose is 3 g).

With peptic ulcer of the stomach and duodenum, associated with Helicobacter pylori - 1 g (4 capsules of 250 mg) per day for 3 days as part of a combination therapy.

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 in day for 3 days (the course dose is 30 mg / kg).

If you miss a dose of 1 dose, the missed dose should be taken as soon as possible, and the subsequent dose - with a break of 24 hours.

Side effects:

From the cardiovascular system: pain in the chest, palpitation.

From the side of the blood: neutropenia, leukopenia, thrombocytopenia, eosinophilia, transient neutrophilia.

From the genitourinary system: candidiasis, vaginitis, nephritis, increasing residual urea nitrogen.

On the part of organs GIT: nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity hepatic transaminases, bilirubin, cholestasis, jaundice; rarely - constipation, discoloration of the tongue, pseudomembranous colitis, pancreatitis, liver necrosis, hepatic insufficiency (possibly fatal); in children - a decrease in appetite, gastritis, candidiasis of the oral mucosa.

From the nervous system and sensory organs: dizziness, vertigo, headache, paresthesia, agitation, increased fatigue, drowsiness; rarely - tinnitus, reversible hearing loss down to deafness (when taken in high doses for a long time); children - headache (with medication otitis media), hyperkinesia, nervousness, anxiety, sleep disturbances, conjunctivitis, neurotoxicity (psychotic reactions and nightmares), myasthenic syndrome.

Other: photosensitivity, hyperglycemia, allergic reactions, arthralgia, at intravenous introduction (in addition) - bronchospasm, pain and inflammation at the injection site.

Overdose:

Violation of liver function, acute liver failure, diarrhea, vomiting, hearing loss. Treatment: gastric lavage (with oral administration), symptomatic.

Interaction:

Antacids, ethanol, food slows down and reduces absorption (azithromycin should be taken 1 hour before or 2 hours after taking antacids and eating).

Ergot alkaloids - risk of ergotism (possibly the manifestation of their toxic effects - vasospasm, dysesthesia).

Warfarin is an intensification of the effect of warfarin. If it is necessary to share with warfarin, careful monitoring is recommended prothrombin time (possibly an increase in prothrombin time and the frequency of development of hemorrhages).

Digoxin - a significant increase in the concentration of cardiac glycosides in plasma, the risk of glycosidic intoxication.

Lovastatin is rhabdomyolysis.

Cyclosporine - side effects, characteristic of cyclosporine. With cyclosporine and phenytoin - it is necessary to control their concentration in the blood.

Dysopyramide - ventricular fibrillation.

Rifabutin - development of leukopenia and neutropenia.

Tetracycline and chloramphenicol increase the effectiveness of azithromycin, lincosamides - weaken.

When used in therapeutic doses azithromycin has little effect on the pharmacokinetics of atorvastatin, carbamazepine, cetirizine, didanosine, efavirenz, fluconazole, indinavir sulfate, midazolam, rifabutin, sildenafil, theophylline (intravenously and inside), triazolam, co-trimoxazole, zidovudine.

Efavirenz and fluconazole have little effect on the pharmacokinetics of azithromycin. Nelfinavir significantly increases C_max and AUC azithromycin (co-administration requires strict monitoring for such side effects of azithromycin as a violation of liver function and hearing impairment).

Pharmaceutically incompatible with heparin.

Special instructions:

Take for an hour or 2 hours after a meal.

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

Impact on the ability to drive vehicles and manage mechanisms

Not found.

Instructions

Azithromycin (Azithromycinum)