Azithral

Azitral is a systemic antibacterial drug with an active component of azithromycin. Included in the category of macrolides.

Indications of the azitral

It is used to eliminate infectious diseases provoked by bacteria sensitive to the effects of azithromycin:

• diseases in the area of the respiratory ducts - alveolitis, interstitial type pneumonia, and bacterial form of bronchitis;
• diseases of the ENT organs - tonsillitis with sinusitis, and in addition inflammation of the middle ear and pharyngitis;
• infectious pathologies in the area of soft tissues with skin - erysipelas, secondary-type pyodermatosis, as well as impetigo and migratory erythema of chronic type (the initial stage of development of tick-borne borreliosis);
• ZPPP - cervicitis, as well as uncomplicated form of urethritis;
• pathology in the area of the duodenum gut or stomach, caused by the bacterium Helicobacter pylori.

[1], [2],

Release form

The release is carried out in tablets.

Azitral 250 - the blister contains 6 tablets. Inside the individual package 1 blister plate, in the box - 10 packs of medicine.

Azitral 500 - inside the strip contains 3 tablets. In a separate pack - 1 plate with pills, inside the box - 5 packs of medicine.

[3], [4]

Pharmacodynamics

Azithromycin is included in a new subgroup of macrolides - the substances of azalide. It is synthesized with the ribosomal (70S) subunit of 50S sensitive bacteria, suppressing protein binding, which depends on RNA. Also, the substance inhibits reproduction and growth of microbes, and in high concentrations can have bactericidal effects.

Azithromycin has a large spectrum of antimicrobial effects. Among the bacteria that are sensitive to it are:

• Gram-positive - pneumococcus, streptococcus pyogenes, streptococcus agalactia, streptococci type C and F, and G, and in addition S.viridans and staphylococcus aureus;
• gram-negative - hemophilic rod, H. Parainfluenzae, moraxella catarrhis, pertussis stick, paracoloca stick, legionella pneumophilus, Ducrea's stick, Campylobacter vegini, gonococcus and gardnerella vaginalis;
• individual anaerobes - Bacteroides bivius, clostridium perfringence, Peptostreptococcus species, and in addition Chlamydia trachomatis, mycoplasma pneumonia, ureaplasma urealiticum, pale treponema and Borrelia Burgdorfer.

The drug does not affect gram positive bacteria resistant to erythromycin.

[5], [6]

Pharmacokinetics

When taken orally, absorption of the substance from the digestive tract occurs quickly. The level of bioavailability is approximately 37% (undergoes the first hepatic passage). After ingestion of 500 mg of the drug, the peak value within the plasma reaches 2.5-3 hours, amounting to 0.4 mg / l.

The substance is well distributed within the respiratory system, tissues with the organs of the genitourinary system (among them the prostate), and besides soft tissues and skin. The level of drug concentration inside cells with tissues exceeds similar indices inside the serum (by 10-100 times). The equilibrium plasma values reach 5-7 days later. Large amounts of drugs are accumulated inside the phagocytes, moving it to the areas of inflammation, as well as infections (there they are gradually released by phagocytosis).

The synthesis with protein is inversely proportional to the blood concentration (7-50% of the drug). About 35% of the substance is exposed to hepatic metabolism by demethylation processes. In this case, azithromycin loses its activity.

More than 50% of the drug is excreted unchanged with bile, and another 4.5% - with urine, in the period of 72 hours.

The half-life is 14-20 hours (in the interval 8-24 hours after the use of drugs), as well as the 41st hour (in the interval of 24-72 hours). The use of food significantly affects the pharmacokinetic properties of the drug.

In elderly men (over 65-85 years old), there is no change in the pharmacokinetics of drugs, and in elderly women the peak rate is increased by 30-50%. 

[7], [8]

Dosing and administration

Azitral must be consumed 1 hour before meals or 2 hours after eating, because when combined with food intake, there is a violation of absorption of the active ingredient. Tablets should be taken once a day.

For teens with a weight of 45 kg and adults:

• for the treatment of infections in the respiratory system, ENT organs, soft tissues and skin (excluding migratory erythema of a chronic type), 500 mg of medication is required for a period of 3 days;
• when the migrating erythema of a chronic type is eliminated, the medication is taken once a day during a period of 5 days: the dose on the 1st day is 1 g, and on subsequent days - 500 mg;
• for the treatment of STDs, a single dose of 1 g of medication is required;
• in the treatment of peptic ulcers of the duodenal ulcer or stomach, it is required to take 1 g of medicine (combined treatment) during the 3-day period;
• to eliminate acne vulgaris it is required to take 6 g of medicine per course. This treatment scheme is proposed: in the first 3 days, take 500 mg once a day, and during the next 9 weeks - use 500 mg of LS once a week.

If you miss a drug, the missed tablet should be taken as soon as possible, and then drink them with an interval of 24 hours.

[16]

Use of the azitral during pregnancy

Use of pills during pregnancy is permitted only on strict indications, in cases where the probable benefit to the patient is higher than the risk of complications in the fetus.

The active substance penetrates into the mother's milk, because of which during the treatment with Azitral it is required to cancel breastfeeding.

Contraindications

Among the contraindications:

• intolerance of the elements of the drug, and also other macrolides;
• disorders in the work of the kidney or liver, as well as the violation of the balance of electrolytes in severe form (in particular cases of hypomagnesemia or hypokalemia);
• expressed by clinical symptoms bradycardia, heart failure in severe form or arrhythmia;
• simultaneous reception with medicines of alkaloids of ergot;
• appointment to children weighing less than 45 kg.

[9], [10], [11], [12],

Side effects of the azitral

The use of tablets can cause the following side effects:

• reaction of the hematopoietic system: development of thrombocytopenia or transient neutropenia with mild severity;
• manifestations from the NA: development of headaches, asthenia, and vertigo / vertigo. In addition, a feeling of drowsiness or insomnia, paresthesia, seizures or fainting may occur, and olfactory or taste perception may be disturbed;
• mental disorders: occasionally there are feelings of anxiety, anxiety, aggressiveness, nervousness and hyperactivity;
• auditory responses: ear ringing, deafness development or hearing impairment (most such disorders are curable);
• violations of the CAS: the development of heartbeat, and in addition arrhythmia (because of ventricular tachycardia). Occasionally prolongation of QT-interval, ventricular fibrillation, sternal pain and a decrease in blood pressure are observed;
• Gastrointestinal reactions: diarrhea, nausea, abdominal discomfort, vomiting, dyspepsia, loose stools or constipation, swelling and changes in the shade of the tongue. Anorexia, gastritis with pancreatitis and, occasionally, pseudomembranous form of colitis can develop;
• disorders in the hepatobiliary system: occasionally there is hepatitis, intrahepatic cholestasis, as well as a curable increase in the activity of liver transaminases. Hepatic dysfunction develops (sometimes leads to death) and hepatitis of necrotic type;
• the reaction of the skin: the appearance of edema Quinck, rashes with itching and urticaria, and in addition the development of photosensitivity, Lyell syndrome or Stevens-Johnson, as well as multiform erythema;
• disorders of ODA function: the occurrence of pain in the joints;
• manifestations on the part of the system of urination: insufficiency of the kidneys in the acute form or tubulointerstitial nephritis;
• Reactions from the part of the reproductive organs: development of vaginitis;
• Other: the occurrence of anaphylaxis (this includes the swelling, which sometimes leads to death) or candidiasis.

[13], [14], [15]

Overdose

In the case of an overdose, there are symptoms such as diarrhea, vomiting and severe nausea, as well as a transient loss of hearing.

To eliminate the disturbances, gastric lavage is required using a probe.

[17], [18], [19]

Interactions with other drugs

It is required to pay attention to the combined use of Azithril with such substances as warfarin, digoxin, theophylline with ergotamine and carbamazepine, and in addition terfenadine and phenytoin with cyclosporin and triazolam. This is necessary, because macrolides can enhance the properties of the above drugs.

Azithromycin is not synthesized with enzymes of the hemoprotein system 450, which differs from most macrolide antibiotics.

Linkomycins reduce the properties of azithromycin, and chloramphenicol with tetracycline on the contrary - increase. The drug has no pharmaceutical compatibility with the substance of heparin.

It is required to use with caution the drug in combination with other means that can prolong the QT-interval.

Studies on the effect of antacids on the pharmacokinetic parameters of azithromycin showed no change in bioavailability, but a decrease in the peak level of the substance inside the plasma (by 30%) was observed. In the case of taking cimetidine 2 hours before the use of azithromycin, the pharmacokinetics of the latter did not change. Antacids can inhibit the absorption of azithromycin. It is required to withstand a gap of at least 2 hours between the use of Azitral and antacid.

Combination of a drug with warfarin or with anticoagulants coumarinovogo number (oral form) increases the likelihood of bleeding. Therefore, during the period of therapy, it is required to constantly monitor the indices of PTV.

The combination of a single dose of zidovudine at a dose of 1000 mg and repeated use of azithromycin 600 or 1200 mg did not affect the pharmacokinetics of zidovudine within the plasma or its (and its glucuronic degradation products) excretion with urine. However, the use of azithromycin increased phosphorylated zidovudine (a drug-active degradation product) inside mononuclear cells in the peripheral blood stream.

Taking Azitral with rifabutin does not change the indices of these drugs inside the plasma. However, people who used them together sometimes developed neutropenia. But it must be taken into account that the disorder was caused by the use of rifabutin, it could not be linked with the use of azithromycin.

[20], [21], [22]

Storage conditions

Azitral should be kept in a place inaccessible to small children. Temperature conditions - no more than 25 ° С.

[23], [24]

Shelf life

Azitral can be used during the 3 years since the release of the drug.