AZITHROMYCIN

Azithromycin - official * instructions for use

                                               * registered by the Ministry of Health of the Russian Federation

INSTRUCTIONS

on medical use of the drug

Registration number:

LSR-002099/10

Trade name: AZITROMYCIN (Name in Cyrillic АЗИТРОМИЦИН)

International non-proprietary name:

azithromycin

Dosage Form:

film coated tablets

Composition

1 tablet, film coated, contains

Active ingredient: Azithromycin dihydrate (equivalent to anhydrous azithromycin) - 524 mg (500 mg)

Excipients: starch, pregelatinized starch, hyprolose, copovidone, crospovidone, anhydrous calcium phosphate, talc, sodium lauryl sulfate, magnesium stearate, hypromellose, macrogol 6000, titanium dioxide, dimethicone.

Description: oval biconvex tablets, film-coated, white, with transverse notch on one side, dividing the tablet into two equal halves. A white core and a thin white film coating are visible on the cross-section of the tablet.

Pharmacotherapeutic group:

antibiotic - azalide

ATX Code: J01FA10

pharmachologic effect

Pharmacodynamics

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of macrolide-azalides. Possesses a wide range of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. By binding to the 508 subunit of ribosomes, it inhibits peptide translocation at the translation stage and inhibits protein synthesis, slowing the growth and reproduction of bacteria. In high concentrations has a bactericidal effect.

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

Microorganisms may initially be resistant to the action of the antibiotic or may become resistant to it.

In most cases, sensitive microorganisms

1.    Gram-positive aerobes

            Staphylococcus aureus - methicillin-sensitive, Streptococcus pneumoniae -    penicillin-sensitive, Streptococcus pyogenes

2.    Gram-negative aerobes

           Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae

3.    Anaerobes

          Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp.

4.    Other microorganisms

           Chlamydia trachomatis, Chlamydia phneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi

Microorganisms capable of developing azithromycin resistance

Gram-positive aerobes

Streptococcus pneumoniae penicillin-resistant

Initially resistant microorganisms

Gram positive aerobes

Enterococcus faecalis, Staphylococci (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides).

Gram-positive bacteria resistant to erythromycin.

Anaerobes

Bacteroides fragilis

Pharmacokinetics

After oral administration, azithromycin is well absorbed and quickly distributed in the body. After a single dose of 500 mg, bioavailability is 37% (“first pass” effect), the maximum concentration (0.4 mg / ml) in the blood is created in 2-3 hours, the apparent volume of distribution is 31.1 l / kg, binding back to proteins proportional to the concentration in the blood and is 7-50%. Penetrates through the cell membrane (effective for infections caused by intracellular pathogens). Transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes histohematic barriers and enters the tissue. Concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection is 24-34% more than in healthy tissues.

Azithromycin has a very long half-life of 35-50 hours. The half-life of tissues is much longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is excreted mainly unchanged - 50% of the intestines, 6% - by the kidneys. In the liver it is demethylated, losing activity.

Indications for use

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

·         infections of the upper respiratory tract and upper respiratory tract (sinusitis, tonsillitis, pharyngitis, otitis media);

·         lower respiratory tract infections: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including those caused by atypical pathogens;

·         infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatosis, common acne of moderate severity);

·         the initial stage of Lyme disease (borreliosis) - erythema migrans (erythema migrans);

·         urinary tract infections caused by Chlamidia trachomatis (urethritis, cervicitis).

Contraindications

Hypersensitivity to macrolide antibiotics, severe hepatic and / or renal failure, children under 12 years old (weighing less than 45 kg), breastfeeding, concomitant use with ergotamine and dihydroergotamine.

Carefully

Moderate dysfunction of the liver and kidneys, with arrhythmias or susceptibility to arrhythmias and prolongation of the QT interval, with co-administration of terfenadine, warfarin, digoxin.

Use during pregnancy and lactation

In pregnancy, the drug is prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus.

If necessary, the use of the drug during lactation should decide on the termination of breastfeeding at the time of use of the drug.

Dosage and administration

Inside, 1 time per day, at least 1 hour or 2 hours after meals. Adults (including the elderly) and children over 12 years old weighing over 45 kg.

With infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 0.5 g / day for 1 reception for 3 days (course dose - 1.5 g).

When erythema migrans (Lyme disease) for treatment of stage I - 1 time per day for 5 days: 1st day - 1.0 g, then from the 2nd to the 5th day - 0.5 g daily (course Dose - 3 g).

Acne ordinary - 6 g course dose, 0.5 g / day for 1 reception for 3 days, then 0.5 g / day 1 time per week for 9 weeks. The first weekly pill should be taken 7 days after taking the first daily pill (8 days from the start of treatment), the next 8 weekly pills - with an interval of 7 days.

In urinary tract infections caused by Chlamidia trachomatis (uncomplicated urethritis or cervicitis) - once 1 g.

Appointment to patients with impaired renal function: for patients with moderately impaired renal function (creatinine clearance> 40 ml / min), dose adjustment is not necessary.

Side effects

On the circulatory and lymphatic systems: thrombocytopenia, neutropenia.

On the side of the central nervous system: dizziness / vertigo, headache, convulsions, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.

On the part of the senses: tinnitus, reversible hearing impairment up to deafness (when taking high doses for a long time), impaired taste and smell.

On the cardiovascular system: heartbeat, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.

Gastrointestinal disorders: nausea, vomiting, diarrhea, abdominal pain / cramps, flatulence, indigestion, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory indicators of liver function, liver failure, hepatic necrosis (possibly fatal).

Allergic reactions: itching, skin rashes, angioedema, urticaria, photosensitivity, anaphylactic reaction, including edema (in rare cases with fatal outcome), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the musculoskeletal system: arthralgia.

On the part of the genitourinary system: nephritis, acute renal failure.

Other: vaginitis, candidiasis.

Overdose

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

Treatment: reception of activated carbon, gastric lavage, symptomatic therapy.

Interaction with other drugs

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

Azithromycin does not affect the concentration of carbamazepine, didanosine, rifabutin and methylprednisolone in the blood when used together.

When used parenterally, azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, trimethoprim / sulfamethoxazole in the blood when used together, but do not exclude the possibility of such interactions when prescribing azithromycin for oral administration.

Azithromycin does not affect the pharmacokinetics of theophylline, but when taken together with other macrolides, the concentration of theophylline in the blood plasma may increase.

If necessary, combined with cyclosporine, it is recommended to control the content of cyclosporine in the blood. Despite the fact that there is no data on the effect of azithromycin on the change in the concentration of cyclosporine in the blood, other representatives of the macrolide class are able to change its level in the blood plasma. When co-administration of digoxin and azithromycin, it is necessary to control the level 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 necessary, the joint reception with warfarin is recommended to carefully monitor the prothrombin time.

It was found that the simultaneous use of terfenadine and macrolide antibiotics causes arrhythmia and prolongation of the QT interval. Based on this, it is impossible to exclude the above complications when co-administering terfenadine and azithromycin.

Since there is a possibility of inhibiting CYP3A4 isoenzyme azithromycin in parenteral form when administered jointly with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs, the metabolism of which occurs with the participation of this enzyme, it is necessary. inside.

When azithromycin and zidovudine are taken together, azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or the kidneys of his and his metabolite, glucuronide. However, the concentration of the active metabolite, phosphorylated zidovudine, in multicore cells of peripheral vessels increases. The clinical significance of this fact is not clear.

While taking macrolides with ergotamine and dihydroergotamine at the same time, their toxic action (vasospasm, dysesthesia) is possible.

Special instructions

In case of skipping a single dose of the drug - the missed dose should be taken as early as possible, and the next - with an interval of 24 hours.

Also, as with any antibiotic therapy, with azithromycin treatment, superinfection (including fungal) may be added.

Azithromycin should be taken at least one hour before or two hours after taking antacids.

Impact on the ability to drive vehicles and mechanisms. During the period of treatment it is necessary to refrain from driving vehicles and practicing potentially hazardous activities that require increased concentration and psychomotor speed.

Release form

Tablets, film coated, 500 mg

On 3 tablets in the blister from the PVC / PVDK film and aluminum printed lacquer foil, one blister is placed in a cardboard pack together with the application instruction.

Shelf life

2 years.

Do not use after the expiration date.

Storage conditions

List B.

In a dry, dark place, at a temperature not higher than 25 ° C.

Keep out of the reach of children.

Pharmacy sales terms:

Prescribed drug.


BUY AZITHROMYCIN