Azithromax

Azithromax is an antibacterial drug used systemically. Included in the category of lincomycins, streptogramins and macrolides.

[1], [2], [3], [4]

Indications of the azithromax

It is used in the treatment of infectious pathologies, which are caused by bacteria sensitive to azithromycin:

• diseases in the upper part of the respiratory system, as well as ENT organs: tonsillitis, middle ear inflammation, as well as sinusitis with pharyngitis;
• pathology in the lower respiratory system: community-acquired pneumonia and bacterial-type bronchitis;
• infectious diseases in the subcutaneous layer and on the skin: impetigo, erysipelas, and dermatitis secondary type of infection;
• STDs: cervicitis, and uncomplicated urethritis;
• to prevent the spread of Mycobacterium avium bacteria in people with HIV infection (used in combination with rifabutin or monotherapy).

[5], [6],

Release form

Release in tablets (250 or 600 mg), which is packed in a bottle (30 pieces) or a blister (6 pieces). Inside a single pack contains 1 bottle or 1 blister plate with tablets.

[7], [8]

Pharmacodynamics

Azithromycin is included in the category of macrolide antibiotics (specifically - a subgroup of azalides). It has antibacterial properties - it is synthesized with a ribosomal 50s-unit pathogenic microbe and inhibits protein binding.

The active ingredient has a large range of antimicrobial efficacy. The medicine actively acts against such bacteria:

• Gram-positive cocci - pneumococcus, streptococcus pyogenic and streptococcus agalactia, and in addition S. Viridans, Staphylococcus aureus and Streptococcus type C, F, and G;
• Gram-negative microbes - stick Ducreya, Legionella pneumophilus, Haemophilus stick, Haemophilus parainfluenzae, Moraxella cataralis, pertussis and paracoloca sticks, gonococcus and Campylobacter vagina, and Helicobacter pylori and Gardnerella vaginalis;
• individual anaerobes - clostridia, Bacteroides bivius, peptococci and peptostreptococci, and in addition mycoplasma pneumonia, borrelia Burgdorfer, Chlamydia trachomatis, listeria monocytogenes, pale treponema and ureaplasma urealiticum.

[9], [10], [11]

Pharmacokinetics

After internal use, the active ingredient is quickly absorbed and distributed within the body. Peak plasma levels reach 2-3 hours later. Quickly passes inside the tissues, cumulating in them in values that significantly exceed the plasma parameters (up to 50 times). The level of bioavailability is 37%. The use of tablets with food does not affect the absorption of the substance.

The average half-life of the component is about 68 hours. In the case of drugs in doses ranging from 250-1000 mg, the indices inside the blood depend on the size of the dose. The long half-life of the substance, as well as its large distributional volume within the body, is due to the fact that the drug passes inside the cell cytoplasm, and is also retained in the lysosomal complexes of phospholipids.

The drug is excreted mainly with bile (most of it is excreted unchanged). Approximately 6% of the dosage is excreted unchanged together with the urine, after a therapeutic course lasting 7 days.

[12], [13], [14],

Dosing and administration

Orally. Reception in combination with food does not affect the absorption of the drug in any way, therefore it is allowed to take tablets with or without food.

The sizes of doses for teenagers in weight from 45 kg and adults.

Infectious diseases in the area of the respiratory system, subcutaneous layers and skin: a one-time intake of 500 mg per day, and then during the next 4 days take 250 mg of medication daily (total dose per course is 1.5 g) or 500 mg once a day in the period of 3 days.

Pathology of the organs of the urogenital tract: when eliminating urethritis and cervicitis of non-gonococcal origin, provoked by the bacterium Clamydia trachomatis, it is required to take once 1 g of medicine (4 tablets with a volume of 250 mg). To treat gonococcal cervicitis or urethritis, take 2 grams of the drug once (8 tablets with a volume of 250 mg).

When preventing the spread of microbes from the group Mycobacterium avium: should be taken once a week 1200 mg of the drug (2 tablets with a volume of 600 mg). It is permitted to combine Azithromax with a suitable dose of rifabutin.

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

Use of the azithromax during pregnancy

It is forbidden to use Azithromax during pregnancy or lactation.

Contraindications

Among the contraindications:

• the presence of hypersensitivity against erythromycin with azithromycin and other elements of the drug or other macrolide antibiotics;
• It is forbidden to use in people suffering from kidney failure in acute form or a pronounced disorder in the work of the liver;
• children whose weight does not reach 45 kg;
• combined reception with ergot alkaloids.

[15], [16]

Side effects of the azithromax

Reception of tablets can provoke occurrence of such by-effects:

• manifestations of allergy: there is a single anaphylaxis (occasionally with a fatal outcome) and swelling, and besides urticaria, rash, Quincke edema, vasculitis and serum syndrome;
• skin reaction: Lyell's syndrome or Stevens-Johnson syndrome is isolated, and in addition, the exfoliative form of dermatitis and polyformiform erythema;
• disturbances in the work of the CAS: ventricular tachycardia or sinus and ventricular fibrillation develops individually, and a decrease in blood pressure and prolongation of the QT interval are observed. Such manifestations disappeared when the medicine was withdrawn;
• disorders of the function of the gastrointestinal tract: often there is diarrhea. Occasionally there is dehydration, constipation, vomiting (due to which dehydration develops), nausea, anorexia, and the shade of the tongue changes. Single pancreatitis and colitis pseudomembranous type appears;
• functional hepatic disorders: there is a single liver failure (sometimes with a fatal outcome), hepatitis of toxic type and intrahepatic cholestasis. There are also cases of hepatic necrosis;
• manifestations of the urogenital tract: occasionally appears vaginitis. The insufficiency of the kidneys is developing in an acute degree, and in addition tubulointerstitial nephritis and nephrosis;
• reaction of the hematopoietic system: single appears thrombocytopenia;
• manifestations from the NA: occasionally there is a feeling of nervousness or anxiety, as well as convulsions. There is a dizziness, a feeling of excitement and increased activity, aggressive behavior and an attack of epilepsy develops, as well as a loss of consciousness;
• reactions of the senses: single vision disorders develop either hearing or hearing (ear noise, hearing loss, and hearing loss) and taste buds;
• Systemic disorders: Paresthesia, pain in the joints or muscles are observed singly, and in addition a feeling of weakness or asthenia develops;
• changes in the values of laboratory studies: most often observed a decrease in the level of lymphocytes, hemoglobin, as well as albumins with monocytes and sugar with hematocrit. Potassium, creatinine, and also GGTP, CK, AST, eosinophils, ALT, platelets and monocytes inside the serum can also increase. Rarely leuko-or neutropenia occurs, the index of AP, platelets, LDH and bilirubin with phosphates inside the serum decreases. Such violations were, in most cases, curable.

[17], [18], [19], [20]

Overdose

In the case of using large doses of drugs, the development of manifestations that are similar to side effects is possible. Overdose is expressed as follows: vomiting, diarrhea and nausea of a marked nature, as well as a curable hearing disorder.

For the treatment of violations will require gastric lavage, the use of activated charcoal, as well as symptomatic therapy that will help support the work of life-critical organs.

[24]

Interactions with other drugs

Magnesium-containing and aluminum-containing antacids inhibit the absorption of azithromycin, as a result of which it is required to take these drugs at intervals of at least 2 hours.

Combination of the drug with warfarin requires constant monitoring of the level of DTV during the therapeutic course. With the simultaneous use of warfarin with macrolides, potentiation of anticoagulant effects is observed.

In the case of concomitant reception of Azithromax with cyclosporine, it is necessary to monitor the pharmacokinetics of the latter and adjust the dose in accordance with the indications.

When combined with nelfinavir, it is required to monitor the patient's condition in order to determine in a timely manner the possible development of side effects.

The combination of macrolides with theophylline increases the latter's indices inside the plasma. The use of azithromycin does not affect the pharmacokinetic characteristics of theophylline, nor does it depend on the size of the dosage (one-time IV injection or a multiple dose of 300 mg LS every 12 hours). To obtain more accurate information about the level of theophylline within the plasma, it is necessary to monitor the health status of the medications treated during combined use of the above medicines.

One-time use of 1st gidovudine in combination with azithromycin (600 or 1200 mg) does not affect the pharmacokinetic characteristics, as well as the excretion of zidovudine (together with its glucuronic derivative). But the use of azithromycin leads to an increase in the zidovudine phosphorylated type within the cells of mononuclears in the peripheral blood flow.

[25], [26]

Storage conditions

Azithromax should be kept out of the reach of small children. Temperature indices are within 15-30 ° С.

[27], [28], [29]

Shelf life

Azithromax can be used in the period of 5 years since the release of the medicine.

[30], [31],