Aziwok

Azivok is an antimicrobial drug for systemic use. It belongs to the macrolide group. Contains azithromycin, which has an effect on intra- and extracellular pathogenic microorganisms.

Indications Aziwok

Among the indications are pathologies of an infectious and inflammatory nature, which are caused by microbes sensitive to the drug:

• infectious diseases of the ENT organs and respiratory system (in the upper sections) - such as sinusitis or pharyngitis, as well as inflammation of the middle ear or tonsillitis;
• infectious pathologies of the lower respiratory tract (bronchitis or pneumonia (also caused by atypical microorganisms));
• infectious processes in soft tissues and skin (such as acne vulgaris (moderate severity), erysipelas, impetigo, and also recurrent dermatoses);
• infectious processes in the urinary system (cervicitis or urethritis (caused by Chlamydia trachomatis));
• tick-borne borreliosis (at an early stage – erythema migrans).

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Release form

Available in capsule form. One blister contains 6 capsules, one package contains 1 blister strip.

Pharmacodynamics

Azithromycin has a wide range of antimicrobial action. The following gram-positive cocci are sensitive to this substance: pneumococcus, streptococcus pyogenes, streptococcus agalactiae, S.viridans, as well as streptococci of groups C, F, and G and Staphylococcus aureus. Sensitive gram-negative microbes: influenza bacillus, H. parainfluenzae, Moraxella catarrhalis, whooping cough bacillus, parapertussis bacillus, Legionella pneumophila, Ducrey bacillus, campylobacter jejuni, as well as gonococcus and Gardnerella vaginalis. Also sensitive are individual anaerobes: Bacteroides bivius, Clostridium perfringens, peptostreptococci, and in addition Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum and spirochetes of pale treponema and Borrelia burgdorferi. The drug does not affect gram-positive microbes that are resistant to the substance erythromycin.

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Pharmacokinetics

The active substance is rapidly absorbed from the gastrointestinal tract, which is due to its high stability relative to the acidic gastric environment, as well as lipophilicity. The peak serum concentration is reached after 2.5-3 hours. After oral administration of 500 mg of the drug, the concentration indicator is 0.4 mg / l.

Azivok penetrates well into the respiratory system, and also tissues with organs of the urogenital tract (including the prostate), as well as soft tissues and skin. The medicinal concentration inside cells with tissues is 10-15 times higher than the serum concentration.

The high concentration inside tissues, as well as the long half-life, are due to the fact that azithromycin is poorly synthesized with plasma protein, and in addition, it can penetrate into eukaryotic cells and accumulate in a low-acid environment that surrounds lysosomes. The consequence of this is a large distribution volume (conditional) - 31.1 l / kg, as well as a high plasma clearance coefficient.

Research data show that phagocytes transport the drug to the site of infection and release it there. Rapid passage of azithromycin into cells, as well as its accumulation inside phagocytes, which transport it to sites of inflammation, contribute to the antimicrobial activity of the drug. Although the concentration of the active component in phagocytes is quite high, it does not significantly affect their functioning.

The bactericidal concentration of the drug inside the infectious foci lasts for 5-7 days after the last dose. This allows using Azivok in short courses (3 or 5 days).

The excretion of the active substance from the blood serum occurs in 2 stages: the half-life is 14-20 hours in the period of 8-24 hours after taking the drug, and then 41 hours in the period of 24-72 hours, as a result of which it becomes possible to use the drug only once a day.

The bioavailability index is 37%.

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Dosing and administration

For children over 12 years of age (weight over 45 kg) and adults: 1 time per day (1 hour before meals or 2 hours after), orally.

For the treatment of infectious processes in the lower and upper respiratory tract, as well as in the ENT organs, soft tissues and skin - 0.5 g per day once for 3 days (the course dosage is 1.5 g).

To eliminate common acne - 0.5 g per day once for 3 days, and then 0.5 g weekly once for 9 weeks. Weekly intake should begin 7 days after taking the 1st daily capsule (this is the 8th day from the beginning of the treatment course).

To eliminate infections in the urinary system (treatment of urethritis or cervicitis) – a single dose of 1 g of the drug.

For the treatment of tick-borne borreliosis (at stage I of erythema migrans) – 1 g of the drug on the first day of the course, and then 0.5 g every day (2-5 days). In this case, the course dosage will be 3 g.

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Use Aziwok during pregnancy

Pregnant women are prescribed the drug only in cases where the possible benefit from its use is greater than the potential development of negative effects on the fetus.

Contraindications

Among the contraindications:

• severe liver or kidney failure;
• compound with ergotamine, as well as dihydroergotamine;
• breastfeeding period;
• age less than 12 years (and weight less than 45 kg for this dosage form);
• individual lactose intolerance (lactase deficiency), and also glucose-galactose malabsorption (because the medicine contains lactose);
• hypersensitivity (also to other macrolide drugs).

It should be prescribed with caution in case of kidney or liver dysfunction (moderate severity), the presence of arrhythmia in the patient (also with a predisposition to the development of arrhythmia and prolongation of the QT interval), and in addition in combination with warfarin, terfenadine, and digoxin.

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Side effects Aziwok

The use of the drug may lead to the development of side effects:

• organs of the circulatory system: neutro- and thrombocytopenia;
• organs of the nervous system: headaches or dizziness/vertigo, feeling of anxiety, drowsiness, aggressiveness, nervousness. In addition, the development of asthenia, the appearance of insomnia, paresthesia or convulsions;
• sensory organs: hearing impairment, leading to deafness (reversible), in case of prolonged use of the drug in large doses, the appearance of noise in the ears, impairment of the olfactory and taste receptors;
• cardiovascular system: development of ventricular tachycardia (including polymorphic) or arrhythmia, sensation of palpitations, as well as prolongation of the QT interval;
• Digestive system organs: nausea with vomiting, diarrhea, bloating, constipation, digestive disorders, abdominal cramps, tongue discoloration. In addition, the development of hepatitis, anorexia, pseudomembranous colitis, intrahepatic cholestasis, and liver failure. Laboratory data regarding liver function may change, and liver necrosis may begin (in some cases, with a fatal outcome);
• allergies: skin rash and itching. Urticaria, anaphylaxis or angioedema (sometimes fatal), eosinophilia, erythema multiforme, malignant exudative erythema, and toxic epidermal necrolysis may develop;
• musculoskeletal system: development of arthralgia;
• urogenital system organs: development of tubulointerstitial nephritis or acute renal failure;
• others: development of candidiasis or vaginitis, as well as photosensitivity.

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Overdose

Symptoms of overdose include severe nausea and vomiting, as well as temporary hearing loss and diarrhea.

As a therapy: perform gastric lavage, and then carry out treatment aimed at eliminating symptoms. The hemodialysis procedure does not give results.

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Interactions with other drugs

Antacids do not affect the bioavailability of azithromycin, but they reduce the peak concentration in the blood by 30%. That is why it is necessary to take Azivok either 1 hour before or 2 hours after using these drugs, as well as eating.

Azithromycin does not affect the concentration of didanosine, carbamazepine, or rifabutin with methylprednisolone when these drugs are used in combination.

Azithromycin used parenterally does not change the blood accumulation level of cimetidine, fluconazole, midazolam, and in addition efavirenz and triazolam with indinavir, as well as co-trimoxazole when combined, but the possibility of such an interaction cannot be excluded if azithromycin is used orally.

The active component of the drug does not affect the pharmacokinetic properties of theophylline, but as a result of combination with other macrolide drugs, the plasma concentration level of theophylline may increase.

Taking the drug in combination with cyclosporine requires careful monitoring of the latter's blood levels. Although there is no information that azithromycin can change the concentration of cyclosporine, other drugs from the macrolide category can affect this indicator.

The combined use of azithromycin with digoxin requires careful monitoring of the concentration of the latter in the blood, because most macrolides enhance its intestinal absorption, as a result of which the plasma concentration of this substance increases.

If combined use with warfarin is necessary, prothrombin time indicators must be carefully monitored.

Studies have shown that the combined use of macrolide antibiotics with terfenadine can prolong the QT interval and also provoke the development of arrhythmia. Therefore, in case of simultaneous use of these substances, the above-described complications may develop.

There is a risk of azithromycin inhibiting the CYP3A4 isoenzyme due to parenteral use in combination with terfenadine and cyclosporine, as well as cisapride, ergot alkaloids and quinidine with pimozide, as well as astemizole and other drugs in the metabolism of which this enzyme is involved. Therefore, in case of prescribing oral azithromycin, the risk of such interaction must be taken into account.

The combined use of azithromycin with zidovudine does not change the pharmacokinetic properties of the latter, and does not affect the process of its (together with the glucuronidated decay product) excretion through the kidneys. But it is necessary to take into account that inside mononuclear cells (in peripheral vessels) the concentration of the active decay product - phosphorylated zidovudine - increases. Although the clinical significance of this property has not yet been determined.

The combined use of macrolide drugs and ergotamine with dihydroergotamine may lead to the development of their toxic effects.

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Storage conditions

The medicine must be stored in conditions that are standard for most medications - a dry place, protected from light, and inaccessible to small children. The temperature should be within 15-30°C.

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Shelf life

Azivok is suitable for use for 2 years from the date of manufacture of the medicine.