Azivok

Azivok is an antimicrobial drug for systemic use. It is part of the group of macrolides. Contains azithromycin, which affects the intra-, as well as extracellular pathogens.

[1]

Indications Azivok

Among the indications of the pathology of infectious-inflammatory nature, which are caused by microbes that are sensitive to the drug:

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

[2], [3], [4], [5], [6]

Release form

Produced in the form of capsules. One blister contains 6 capsules, in one package 1 blister plate.

[7]

Pharmacodynamics

Azithromycin has a wide range of antimicrobial effects. Sensitive to this substance are such Gram-positive cocci: pneumococcus, streptococcus pyogenes, streptococcus agalactia, S.viridans, and in addition streptococci included in groups C, F, and also G and staphylococcus aureus. Sensitive Gram-negative microbes: Influenza rod, H. Parainfluenzae, Moraxella cataralis, Pertussis stick, Paracoloca stick, Legionella pneumophilus, Ducrea's stick, Campylobacter vagina, and also Gonococcus and Gardnerella vaginalis. Individual anaerobes are also sensitive: Bacteroides bivius, Clostridia perforings, peptostreptococci, and in addition Chlamydia trachomatis, Mycoplasma pneumonia, Ureaplasma urealiticum and spirochetes of pale treponema and Borrelia Burgdorfer. The drug has no effect on gram-positive microbes, which are resistant to the substance erythromycin.

[8], [9]

Pharmacokinetics

The active substance is rapidly absorbed from the digestive tract, which is due to its high resistance to acidic gastric environment, as well as lipophilicity. The peak of serum concentration reaches 2.5-3 hours later. After oral administration of 500 mg of the drug, the concentration is 0.4 mg / L.

Azivok passes well into the respiratory system, and besides this tissue with organs of the urogenital tract (including the prostate), as well as soft tissues and skin. Drug concentration inside cells with tissues is 10-15 times higher than serum.

High concentrations inside the tissues, as well as a prolonged half-life are due to the fact that azithromycin is poorly synthesized with a plasma protein, and besides it can pass into eukaryotic cells and accumulate in a medium with a low level of acidity that surrounds the lysosomes. The consequence of this is a large distributional volume (conditional) - 31.1 l / kg, as well as a high index of the plasma purification coefficient.

The research data show that the phagocytes transport the medicine to the location of the infectious focus, and there it is released. The rapid passage of azithromycin into cells, as well as its accumulation inside phagocytes, which transfer it to the sites of inflammation, contribute to the antimicrobial activity of the drug. Although in phagocytes the concentration of the active component is rather high, it does not have a significant effect on their functioning.

The bactericidal concentration of the drug inside infectious foci is maintained for 5-7 days after the last dose. This allows you to apply Azivok short courses (3 or 5 days each).

Excretion of the active substance from the blood serum is carried out in 2 stages: the half-life is 14-20 hours in the interval 8-24 hours after the use of drugs, and then 41 hours - in the interval of 24-72 hours, which makes it possible to use the medicine only 1 once a day.

The bioavailability index is 37%.

[10], [11], [12]

Dosing and administration

For children from 12 years (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 parts with the upper parts of the respiratory system, and in addition, 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 once weekly for 9 weeks. Begin weekly reception should be 7 days after the use of the first 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 medication.

For the treatment of tick-borne borreliosis (in the 1st stage of migrating erythema) - 1 g of medication on the first day of the course, and then 0.5 g every day (2-5 days). At the same time, the dosage will be 3 g.

[17], [18], [19]

Use Azivok during pregnancy

Pregnant women are prescribed medicine only in cases when the possible benefits of using it are higher than the potential development of negative effects in the fetus.

Contraindications

Among the contraindications:

• severe form of hepatic or renal insufficiency;
• compound with ergotamine, as well as dihydroergotamine;
• the period of breastfeeding;
• age less than 12 years (and also weight less than 45 kg for this dosage form);
• individual lactose intolerance (lactase deficiency), and in addition malabsorption of glucose-galactose (because the drug contains lactose in its composition);
• hypersensitivity (also to other macrolide drugs).

Caution should be prescribed for disorders in the work of the kidney or liver (moderate severity), the presence of arrhythmia in the patient (also with a predisposition to the development of arrhythmias and lengthening the QT interval), and in addition to the combination with warfarin, terfenadine, and digoxin.

[13], [14], [15]

Side effects Azivok

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

• organs of the circulatory system: neutron, as well as thrombocytopenia;
• organs of the National Assembly: headaches or dizziness / vertigo, a sense of anxiety, drowsiness, aggressiveness, nervousness. In addition, the development of asthenia, the emergence of insomnia, paresthesias or seizures;
• sensory organs: hearing impairment, reaching deafness (reversible), in case of prolonged use of the drug in large dosages, the appearance of tinnitus, the breakdown of the olfactory and taste buds;
• organs of the cardiovascular system: the development of ventricular tachycardia (including polymorphic), or arrhythmias, palpitations, and prolongation of the QT interval;
• organs of the digestive system: nausea along with vomiting, diarrhea, bloating, constipation, digestive process disorders, abdominal cramps, discoloration of the tongue. In addition, the development of hepatitis, anorexia, pseudomembranous colitis, intrahepatic cholestasis, and liver failure. Laboratory data on hepatic function may change, as well as necrosis of the liver (in some cases, with a fatal outcome);
• allergies: the appearance of rashes on the skin, as well as itching. May develop hives, anaphylaxis or angioedema (sometimes fatal), eosinophilia, erythema multiforme, malignant exudative erythema, and toxic epidermal necrolysis;
• ODA organs: development of arthralgia;
• organs of the urogenital system: development of tubulointerstitial nephritis or renal failure in acute form;
• others: the development of candidiasis or vaginitis, and besides this photosensitivity.

[16]

Overdose

Manifestations of an overdose: a feeling of severe nausea, as well as vomiting, and besides this, a temporary loss of hearing and diarrhea.

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

[20], [21], [22], [23]

Interactions with other drugs

Antacids do not affect the level of bioavailability of azithromycin, but at the same time reduce the peak concentration in the blood by 30%. That's why you need to take Azivok either 1 hour before or 2 hours after using the drugs, as well as eating.

Azithromycin does not affect the indices of the concentration of didanosine, as well as carbamazepine, and in addition rifabutin with methylprednisolone with the combined use of these drugs.

Parenteral azithromycin does not alter the level of accumulation in the blood of cimetidine, fluconazole, midazolam, and in addition to efavirenz and triazolam with indinavir, as well as co-trimoxazole when combined, but the likelihood of such interaction can not be ruled out if azithromycin is used orally.

The active component of the drug has no effect on the pharmacokinetic properties of theophylline, but as a result of the combination with other macrolide drugs, the level of plasma concentration of theophylline may increase.

Taking medication 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 may have an effect on this indicator.

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

If necessary, combined use with warfarin requires careful monitoring of prothrombin time.

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

There is a risk of azithromycin inhibition of CYP3A4 isoenzyme due to the parenteral route of use in combination with terfenadine and cyclosporine, and in addition cisapride, ergot alkaloids and quinidine with pimozide as well as astemizole and other drugs in which the enzyme participates in the metabolism. Therefore, in the case of the administration of oral azithromycin, the risk of such interaction must be considered.

The combined use of azithromycin with zidovudine does not lead to a change in the pharmacokinetic properties of the latter, nor does it affect the process of excretion through the kidneys (together with the glucuronated degradation product). But it must be taken into account that inside the mononuclear cells (in peripheral vessels) the concentration index of the active decay product - phosphorylated zidovudine - increases. Although it has not yet been possible to determine the clinical significance of this property.

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

[24], [25], [26]

Storage conditions

Contain medication is required in conditions that are standard for most medicines - dry place, closed from light, and also inaccessible to small children. The temperature is within 15-30 ° C.

[27], [28], [29]

Shelf life

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

[30], [31]