Azimed

Azimed is an antimicrobial drug for systemic use. It belongs to the category of lincosamides, macrolides, and streptogramins.

Indications Azimeda

It is used to eliminate infections caused by bacteria sensitive to the substance azithromycin:

• ENT diseases (such as tonsillitis or bacterial pharyngitis, inflammation of the middle ear and sinusitis);
• respiratory infections (such as bacterial bronchitis and community-acquired pneumonia);
• infectious pathologies in the area of soft tissues and skin: erythema migrans (early stage of tick-borne borreliosis), impetigo and erysipelas, as well as secondary pyodermatoses;
• STD: cervicitis or urethritis, complicated/uncomplicated.

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Release form

Released in capsules, 6 or 10 pieces inside a blister. In a separate package - 1 blister plate.

Pharmacodynamics

Azithromycin is an azalide (a new category of macrolides) and has a wide range of antimicrobial action. It is synthesized with the ribosomal (70S) 50S subunit of susceptible bacteria and inhibits RNA-dependent protein binding. As a result of this process, the reproduction and growth of microbes are slowed down. At high concentrations of the drug in the body, its bactericidal properties can be manifested.

Azithromycin has a fairly wide spectrum of action and actively affects the following pathogenic microorganisms:

• individual gram-positive microbes: pneumococcus, Streptococcus pyogenes, Streptococcus agalactiae, streptococci types C, F, and G, Staphylococcus aureus, and S. Viridans;
• Gram-negative microbes: influenza bacillus, H. Parainfluenzae, Ducrey bacillus, Moraxella catarrhalis, whooping cough bacillus, parapertussis bacillus, gonococcus and Gardnerella vaginalis;
• anaerobes sensitive to the substance: peptostreptococci and peptococci, Bacteroides bivius and Clostridium perfringens;
• effectively affects intracellular and other bacteria, including: Legionella pneumophila, Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum and Borrelia burgdorferi.

Does not affect gram-positive microbes resistant to erythromycin.

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Pharmacokinetics

The bioavailability level for oral administration of the drug is approximately 37% (with the "first liver pass" effect). In the serum, the peak concentration is reached after 2-3.5 hours and is (after oral administration of 500 mg of the drug) 0.4 mg / l. The drug quickly penetrates into the tissues and organs of the genitourinary system (including the prostate), as well as the respiratory organs, soft tissues and skin. Inside the cells with tissues, the substance indicator is higher than inside the serum (10-100 times). Equilibrium plasma indicators are reached after 5-7 days. The substance accumulates in large quantities inside phagocytes, which transfer it to the site of inflammation or infection. There it is gradually released by phagocytosis.

Synthesis with proteins has a level inversely proportional to the substance index in the blood (7-50% of the drug). About 35% of the dose undergoes liver metabolism (demethylation process), as a result of which the substance loses activity. About 50% of the drug is excreted unchanged with bile, and another 4.5% with urine, within 72 hours.

The half-life from plasma is approximately 14-20 hours (the interval within 8-24 hours after taking the drug) and 41 hours (the interval within 24-72 hours). The pharmacokinetic properties of the drug change significantly if it is taken with food.

In elderly men (65-85 years old) no changes in the pharmacokinetics of the drug are observed, but in women the peak value increases by 30-50%. In young children (1-5 years old) the AUC, peak concentration and half-life of the substance decrease.

Dosing and administration

The medicine is taken orally, once a day (1 hour before meals or 2 hours after meals - this is necessary, since combined use with food affects the absorption of azithromycin). Capsules should not be opened or divided into halves.

For teenagers weighing over 45 kg, adults and seniors:

• to eliminate infections in the respiratory tract and ENT organs, as well as soft tissues and skin (excluding chronic migratory erythema) - the daily dosage is 500 mg (drink 2 capsules per dose). Take for 3 days;
• to eliminate erythema migrans, capsules should be taken once a day for 5 days. In this case, on the 1st day, the dose is 1 g (taking 4 capsules of the drug), and in the period of 2-5 days - 500 mg (taking 2 capsules of the drug);
• for the treatment of STDs: a single dose of 1 g of medicine (4 capsules).

If you miss taking a medication, you must take the missed capsule as quickly as possible, and take all subsequent doses at intervals of 24 hours.

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Use Azimeda during pregnancy

Since there is no information about the safety of taking Azimed during pregnancy or lactation, it should be prescribed only in cases where the likely benefit from its use for the woman is higher than the risk of complications in the baby or fetus.

Contraindications

Contraindications include intolerance to the active component or other elements of the drug, as well as other ketolide and macrolide antibiotics. It is prohibited to prescribe the drug in capsule form to children weighing less than 45 kg.

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Side effects Azimeda

Often, the substance azithromycin is tolerated quite well, but in some cases, when taking it, the following side effects may occur:

• reactions from the cardiovascular system: there have been cases of arrhythmia such as pirouette (this also includes ventricular tachycardia), palpitations, and decreased blood pressure;
• gastrointestinal manifestations: diarrhea, bloating, nausea, change in the color of the tongue, abdominal pain, dyspepsia, constipation and vomiting, as well as the development of pancreatitis, gastritis and pseudomembranous colitis;
• organs of the hepatobiliary system: development of hepatitis (also its necrotic and fulminant forms), intrahepatic cholestasis and renal failure (can occasionally lead to death), as well as disorders in the functioning of the liver;
• neurological disorders: the appearance of paresthesia, convulsions, headaches and dizziness. In addition, the development of hypoesthesia, ageusia and dysgeusia, parosmia, myasthenia gravis and anosmia. Fainting, psychomotor agitation, as well as a feeling of drowsiness or, conversely, insomnia are observed;
• mental disorders: feelings of aggression, nervousness, anxiety or anxious agitation;
• reactions of the vestibular apparatus and auditory organs: curable deafness, vertigo, and tinnitus;
• visual disorders: visual impairment;
• reactions of the lymph and hematopoietic system: development of hemolytic anemia, as well as leuko-, thrombocyto- or neutropenia;
• subcutaneous tissues and skin: itching, photosensitivity and rashes, development of urticaria, Lyell's syndrome or Stevens-Johnson syndrome, erythema multiforme or Quincke's edema;
• manifestations from the connective tissues and musculoskeletal organs: development of arthralgia;
• urinary system organs: development of acute renal failure or tubulointerstitial nephritis;
• invasive or infectious diseases: the appearance of candidiasis (also in the mouth), vaginal infection;
• allergic disorders: anaphylactic reactions, hypersensitivity;
• general reactions: development of anorexia, asthenia, severe fatigue, the appearance of pain in the sternum, malaise and swelling;
• changes in laboratory test results: development of eosinophilia or lymphocytopenia, increase in creatinine, AST, ALT and bilirubin levels, decrease in blood bicarbonate levels, prolongation of the QT interval on the ECG and changes in potassium levels.

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Overdose

Overdose may result in the development of disorders similar to side effects after taking standard medicinal doses.

To eliminate the disorders, activated charcoal should be taken and symptomatic treatment should be performed to support the functioning of vital organs.

Interactions with other drugs

Azithromycin should be taken with caution in case of simultaneous use of other drugs that can prolong the QT interval.

During the study of the drug's interaction with antacids, no changes in its bioavailability were noted, although peak plasma levels were reduced by approximately 25%. As a result, it is recommended to take azithromycin before (1 hour) or after (2 hours) taking antacid drugs.

Ergot derivatives in combination with azithromycin may, in theory, cause ergotism.

Some representatives of related macrolides affect the process of cyclosporine metabolism. Since clinical and pharmacokinetic tests for possible interaction in case of combined administration of Azimed with cyclosporine have not been conducted, it is necessary to carefully evaluate the clinical picture before prescribing the combined administration of these drugs. If combined therapy is considered justified, it will be necessary to carefully monitor cyclosporine indicators during its course and adjust the dose accordingly.

Azithromycin does not affect the anticoagulant properties of a single dose (15 mg) of warfarin, although there is evidence of an increase in these properties with the simultaneous use of coumarin anticoagulants (orally) with azithromycin. It was not possible to identify the cause of this effect, but this fact must be taken into account. Therefore, it is recommended to constantly monitor the PT index in individuals treated with these agents.

In some patients, individual macrolides may affect the intestinal metabolism of digoxin. Therefore, when combining azithromycin with this drug, it is necessary to remember the possible increase in digoxin levels and monitor their changes during treatment.

There is no information on the interaction of azithromycin and the substance terfenadine. The simultaneous administration of these drugs should be carried out with caution.

Combined use with theophylline does not change the pharmacokinetic characteristics of this substance. However, combined use of theophylline with other macrolides in some cases may cause an increase in its serum levels.

A single dose of 1000 mg zidovudine in combination with multiple doses of azithromycin at doses of 600 or 1200 mg does not change the plasma pharmacokinetics of zidovudine, nor its (together with glucuronide decay products) excretion in urine. However, azithromycin increases the levels of phosphorylated zidovudine (a medicinally active decay product inside mononuclear cells in the peripheral bloodstream).

Combined use of the drug with rifabutin does not affect their plasma parameters. As a result of such a combination, neutropenia may develop (although in this case, the cause is most likely the intake of rifabutin, since it was not possible to link the development of this disorder with the intake of this substance in combination with azithromycin).

Serum azithromycin levels increase with nelfinavir administration. No dosage adjustment is required when combined with nelfinavir, but the patient should be monitored for azithromycin-related side effects.

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Storage conditions

Azimed should be kept in a place inaccessible to small children. The temperature values should not exceed 25°C.

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Shelf life

Azimed is permitted to be used for a period of 3 years from the date of release of the drug.