Composition, form of production and packaging
Capsules 1 caps.
azithromycin 250 mg
3 pcs. - packings of cellular contour (1) - packs cardboard.
3 pcs. - packings cellular planimetric (2) - packs cardboard.
Capsules 1 caps.
azithromycin 500 mg
3 pcs. - packings of cellular contour (1) - packs cardboard.
3 pcs. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antibacterial preparation of a wide spectrum of action from the group of macrolides-azalides, acts bacteriostatically. Linking to the 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation, suppresses protein synthesis, slows the growth and multiplication of bacteria, at high concentrations has a bactericidal effect. It acts on extracorporeal and intracellular pathogens.
Microorganisms can be initially resistant to the action of the antibiotic or can acquire resistance to it.
The sensitivity scale of microorganisms to azithromycin (Minimum inhibitory concentration (MIC), mg / l):
Microorganisms MIC, mg / l
Sensitive Resistant
Staphylococcus spp. ? 1> 2
Staphylococcus spp. groups A, B, C, G? 0.25> 0.5
Streptococcus pneumoniae? 0.25> 0.5
Haemophilus influenzae? 0.12> 4
Moraxella catarrhalis? 0.5> 0.5
Neisseria gonorrhoeae? 0.25> 0.5
Sensitive:
aerobic Gram-positive microorganisms: Staphylococcus aureus (methylcillin susceptibility), Streptococcus pneumoniae (penicillin susceptibility), Streptococcus pyogenes;
aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae;
anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp .;
Other: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdoferi.
Moderately sensitive or insensitive:
aerobic Gram-positive microorganisms: Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).
Stable:
aerobic Gram-positive microorganisms: Enterococcus faecalis, Staphylococci spp. (methicillin resistant), Staphylococus aureus (including methicillin-sensitive strains), Staphylococus pneumoniae, Staphylococcus spp. group A (beta-hemolytic). Azithromycin is not active against strains of gram positive bacteria resistant to erythromycin.
anaerobes:
group Bacteroides fragilis.
PHARMACOKINETICS
After oral administration, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single dose 0.5 g - 37% (the effect of "first pass" through the liver), C max after oral intake 0.5 g - 0.4 mg / l, the time to reach the maximum concentration (TC max ) - 2-3 hours.
Concentration in tissues and cells is 10-50 times higher than in serum. V d - 31.1 l / kg, binding to plasma proteins is inversely proportional to the concentration in the blood and leaves 7-50%.
Azithromycin is acid-fast, lipophilic. Easily passes through gistogematicheskie barriers, well penetrates the respiratory tract, urino-genital organs and tissues, incl. in the prostate gland, skin and soft tissue. To the site of infection is also transported by phagocytes (polymorphonuclear leukocytes and macrophages), where it is released in the presence of bacteria. It penetrates the cell membranes and creates high concentrations in them, which is especially important for the eradication of intracellular pathogens. In foci of infection, the concentrations are 24-34% higher than in healthy tissues and correlate with the severity of the inflammatory process. It remains in effective concentrations for 5-7 days after the last dose.
In the liver demethylated, the metabolites formed are inactive. In the metabolism of azithromycin, the isoenzymes CYP3A4, CYP3A5, CYP3A7 are involved, the inhibitor of which it is. Plasma clearance - 630 ml / min: T 1/2 between 8 and 24 hours after admission - 14-20 hours, T 1/2 in the interval from 24 to 72 hours - 41 hours.
More than 50% of azithromycin is excreted intestine unchanged, 6% - kidney. Eating significantly changes the pharmacokinetics of C max increases (by 31%), AUC does not change.
In elderly men (65-85 years) pharmacokinetic parameters do not change, in women C max increases (by 30-50%).
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- 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, pneumonia, incl. caused by atypical pathogens;
- infections of the skin and soft tissues: acne vulgaris of medium severity, erysipelas, impetigo, secondarily infected dermatoses;
- the initial stage of Lyme disease (borreliosis) - migrating erythema (erythema migrans);
- Urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).
DOSING MODE
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 of over 45 kg
When infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 500 mg 1 time / day for 3 days (exchange dose - 1.5 g).
For acne vulgaris of medium severity: 2 caps. 250 mg 1 time / day for 3 days, then 250 mg twice a week for 9 days. The course dose is 6.0 g.
With migrating erythema: the first day at the same time 2 caps. 500 mg, then from day 2 to day 5, 500 mg daily. Rate of dose 3.0 g.
For infections of the genitourinary tract caused by Chlamydia trachomatis (urethritis, cervicitis): one-time 2 caps. on 500 mg.
The appointment to patients with impaired renal function : for patients with moderate impaired renal function (CK> 40 ml / min), correction is not required.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain, loose stools, flatulence, digestive disorders, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in liver function tests, hepatic insufficiency, liver necrosis (possibly fatal).
Allergic reactions: itching, skin rashes, angioedema, urticaria, photosensitivity, anaphylactic reaction (in rare cases, fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal nSCROLIZATION.
From the cardiovascular system: a feeling of heartbeat, arrhythmia, ventricular tachycardia, an increase in the QT interval, bidirectional ventricular tachycardia.
From the nervous system: dizziness / vertigo, headache, cramps, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.
From the senses: tinnitus, reversible hearing loss down to deafness (when taking high doses for a long time), a violation of the perception of taste and smell.
From the blood and lymphatic systems: thrombocytopenia, neutropenia, eosinophilia.
From the musculoskeletal system: arthralgia.
From the genitourinary system: interstitial nephritis, acute renal failure.
Other: vaginitis, candidiasis.
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);
- breast-feeding;
- simultaneous administration with ergotamine and dihydroergotamine;
- hypersensitivity to antibiotics of the macrolide group.
With caution
- moderate violations of the liver and kidneys;
- with arrhythmias or predisposition to arrhythmias and lengthening of the QT interval;
- with the combined use of terfenadine, warfarin, digoxin.
PREGNANCY AND LACTATION
Azithromycin during pregnancy is recommended to be used only in cases when the expected benefit from its admission for the mother exceeds the potential risk to the fetus.
During treatment with azithromycin, breastfeeding is suspended.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure.
For patients with moderate impaired renal function (CK> 40 mL / min), correction is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency. Use with caution for moderate violations of the liver.
APPLICATION FOR CHILDREN
Contraindications for this dosage form are children under 12 years of age with a body weight of less than 45 kg.
APPLICATION IN ELDERLY PATIENTS
Assigned to adults (including the elderly)
SPECIAL INSTRUCTIONS
In case of missing the antibiotic, the missed dose should be taken as soon as possible, and subsequent doses should be taken at intervals of 24 hours.
After the withdrawal of azithromycin therapy, hypersensitivity reactions in some patients may persist for a long time and may require specific therapy under the supervision of a physician.
Impact on the ability to drive vehicles and manage mechanisms
Given the likelihood of side effects from the central nervous system, care should be taken when driving vehicles and working with mechanisms.
OVERDOSE
Symptoms: temporary loss of hearing, nausea, vomiting, diarrhea.
Treatment: symptomatic.
DRUG 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 food.
In parenteral administration, azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, co-trimoxazole (sulfamethoxazole + trimethoprim) in plasma when combined, but should not exclude the possibility of such interactions in the administration of azithromycin for oral administration.
If it is necessary to use together with cyclosporine, it is recommended to monitor the content of cyclosporin in the blood.
With the joint administration of digoxin and azithromycin, it is necessary to monitor the concentration of digoxin in the blood, many macrolides increase absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma.
If it is necessary to share with warfarin, careful monitoring of prothrombin time is recommended.
Simultaneous reception of terfenadine and antibiotics of the macrolide class causes arrhythmia and lengthening of the QT interval. Proceeding from this, it is impossible to exclude the aforementioned complications in the joint administration of terfenadine and azithromycin. Since it is possible to inhibit the isoenzyme CYP3A4 with azithromycin in parenteral form when combined with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism occurs with the participation of this isoenzyme, the possibility of such interaction in the administration of azithromycin for administration inside.
With the combined use of azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or the excretion of zidovudine by the kidneys and its glucuronated metabolite. Nevertheless, the concentration of the active metabolite - phosphorylated zidovudine - increases in mononuclear cells of peripheral vessels. The clinical significance of this fact is unclear.
With the simultaneous administration of macrolides with ergotamines and dihydroergotamine, their toxic effect is possible.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dry place, protected from light, out of reach of children, at a temperature of no higher than 25 В° C. Shelf life - 3 years.
