Composition, form of production and packaging
Capsules hard gelatinous, size в„–0, white; the content of the capsules is a mixture of granules and white or white powder with a yellowish hue.
azithromycin dihydrate 262.02 mg,
which corresponds to the content of azithromycin 250 mg
Auxiliary substances: corn starch - 45.4 mg, lactose monohydrate (sugar milk) - 18.2 mg, lactose anhydrous (lactopress) - 102.89 mg, povidone (polyvinylpyrrolidone) - 7.49 mg, sodium lauryl sulfate - 0.9 mg, silicon colloidal dioxide (aerosil) - 4.4 mg, magnesium stearate - 8.7 mg.
The composition of the hard gelatin capsule: titanium dioxide - 2%, gelatin - up to 100%.
6 pcs. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
Azithromycin is a bacteriostatic antibiotic from the macrolide-azalide group. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis of a microbial cell. Linking to the 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation and suppresses protein synthesis, slows the growth and multiplication of bacteria. In high concentrations has a bactericidal effect.
It has activity against a number of extra- and intracellular gram-positive and gram-negative microorganisms, as well as a number of anaerobic microorganisms. Microorganisms may initially be resistant to the action of the antibiotic or may acquire resistance to it.
Microorganisms sensitive to azithromycin
Gram-positive aerobes: Staphylococcus aureus methicillin-sensitive, Streptococcus pneumoniae penicillin-sensitive Streptococcus pyogenes.
Gram-negative aerobes: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae
Anaerobes: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp.
Other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.
Microorganisms capable of developing resistance to azithromycin
Gram-positive aerobes: Streptococcus pneumoniae penicillin-resistant.
Microorganisms initially resistant to azithromycin
Gram-positive aerobes: Enterococcus faecalis, Staphylococci (methicillin-resistant show a high degree of resistance to macrolides).
Gram-positive bacteria resistant to erythromycin.
Anaerobes: Bacteroides fragilis.
After oral administration, azithromycin is well absorbed and quickly distributed in the body. After a single dose of 500 mg bioavailability - 37% (the effect of "first pass" through the liver),
C max in blood plasma (0.4 mg / l) is created after 2-3 hours, apparent V d - 31.1 l / kg, binding to plasma proteins is 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 the pathogen. Easily passes the histohematological barriers and enters the tissues. Concentration in tissues and cells is 10-50 times higher than in plasma, and in foci of infection - 24-34% higher than in healthy tissues. In the liver, demethylated, losing activity.
T 1/2 azithromycin - 35-50 h, T 1/2 of the tissues - much more. Therapeutic concentrations of azithromycin persist up to 5-7 days after the last dose. Azithromycin is excreted mainly in unchanged form - 50% of the intestine, 6% of the kidneys.
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infection of the urogenital tract (uncomplicated urethritis and / or cervicitis);
- infections of the upper respiratory tract and ENT organs (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);
- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
- Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
- Diseases of the stomach and duodenum, associated with Helicobacter pylori (in combination therapy).
Inside for 1 hour or 2 hours after eating 1 time / day.
When infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 500 mg / day (2 caps.) For 1 time / day for 3 days (course dose - 1500 mg).
With migrating erythema: 1 time / day for 5 days: 1st day - 1000 mg (4 caps.), Then from the 2nd to the 5th day - 500 mg (2 caps.) (Course dose - 3000 mg).
In acute infections of the genitourinary tract caused by Chlamydia trachomatis: uncomplicated urethritis / cervicitis - 1000 mg (4 caps.) Once.
Purpose for patients with impaired renal function
For patients with moderate renal dysfunction (CK> 40 ml / min) dose adjustment is not required.
Classification of adverse reactions according to the frequency of development (number of reported cases / number of patients): often (? 1/100, <1/10), infrequently (? 1/1000 and <1/100), rarely (? 1/10 000 and < 1/1000) and very rarely (<1/10 000).
From the central and peripheral nervous system: infrequently - dizziness / vertigo, headache, convulsions, drowsiness; rarely - paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.
From the senses: rarely - noise in the ears, 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 digestive system: often - nausea, vomiting, diarrhea, abdominal pain; infrequently - loose stools, flatulence, indigestion, anorexia; rarely - constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory parameters of liver function; very rarely - necrosis of the liver.
From the cardiovascular system: rarely - palpitation, arrhythmia (including ventricular tachycardia), an increase in the QT interval.
From the blood and lymphatic system: rarely thrombocytopenia, neutropenia.
From the genitourinary system: nephritis, acute renal failure, vaginitis.
From the musculoskeletal system: infrequently - arthralgia.
Allergic reactions: infrequently - itching, skin rashes; rarely - angioedema, urticaria, photosensitivity, anaphylactic reaction, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
- hypersensitivity to azithromycin or other macrolides;
severe hepatic impairment;
- severe renal dysfunction;
- Children under 12 years of age with a body weight of less than 45 kg (for this dosage form);
- lactation period;
- simultaneous administration with ergotamine and dihydroergotamine;
- genetic intolerance to galactose, insufficiency of lactase, glucose-galactose malabsorption (for a given dosage form containing lactose).
- moderate violations of the liver and kidneys;
- arrhythmia or predisposition, arrhythmia and lengthening of the QT interval;
- a joint appointment of terfenadine, warfarin, digoxin.
PREGNANCY AND LACTATION
Azithromycin is used in pregnancy only if the expected benefit from its use is greater than the possible risk to the fetus.
At the time of treatment with azithromycin, breastfeeding is suspended.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in patients with moderate renal dysfunction.
For patients with moderate renal dysfunction (CK> 40 ml / min) dose adjustment is not required.
The drug is contraindicated in patients with severe renal dysfunction.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in patients with moderate impaired hepatic function.
The drug is contraindicated in patients with severe impairment of liver function.
APPLICATION FOR CHILDREN
The drug is contraindicated in children under 12 years of age.
In case of missed intake of a single dose of the drug, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours.
Just as with any antibiotic therapy, in the treatment of azithromycin, it is possible to attach superinfection (including fungal).
In the treatment of pharyngitis / tonsillitis caused by Streptococcus pyogenes, as well as for the prevention of acute rheumatic fever, the drug of choice is usually penicillin. Azithromycin is also active against streptococcal infection in these cases, but is ineffective for the prevention of acute rheumatic fever.
Influence on ability to drive vehicles and other mechanisms
Azithromycin does not affect the ability to drive vehicles and other mechanisms.
Symptoms: nausea, temporary loss of hearing, vomiting, diarrhea.
Antacids reduce the maximum concentration of azithromycin in blood plasma by 30%, so the drug should be taken at least 1 hour before or 2 hours after taking these drugs and food.
Azithromycin does not affect the concentration of carbamazepine, Didanosine, rifabutin and methylprednisolone in blood plasma when combined. The effect of azithromycin (for oral administration) on the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, trimethoprim / sulfamethoxazole in blood plasma can not be ruled out when combined.
Azithromycin does not affect the pharmacokinetics of theophylline, but when combined with other macrolides, the concentration of theophylline in the blood plasma may increase.
If it is necessary to use together with cyclosporine, it is recommended to monitor the content of the latter in blood plasma. Despite the fact that there are no data on the effect of azithromycin on the concentration of cyclosporine in blood plasma, other macrolides are capable of changing its level in blood plasma.
With the joint use of azithromycin with digoxin, it is necessary to monitor the level of the latter in blood plasma, because many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma.
When co-administered with warfarin, it is recommended that prothrombin time be carefully monitored.
It was found that 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 side effect in the joint use of terfenadine and azithromycin.
Since it is possible to inhibit the isoenzyme CYP3A4 with azithromycin in parenteral form when co-administered with cycloserine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole, etc., the metabolism of which occurs with the participation of this enzyme, the possibility of such interaction when prescribing azithromycin for reception inside.
When combined, azithromycin does not affect the pharmacokinetic parameters of zidovudine and its metabolite, glucuronide. Nevertheless, the concentration of its active metabolite - phosphorylated zidovudine in mononuclear cells of peripheral vessels - increases. The clinical significance of this fact is not clear.
With the simultaneous use of macrolides with ergotamine and dihydroergotamine, their toxic effect is possible.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 3 years.
Do not use after the expiration date.