Azitral
Azitral: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Azitral
ATX code: J01FA10
Active ingredient: azithromycin (azithromycin)
Manufacturer: Shreya Life Sciences (India)
Description and photo update: 2019-16-09
Prices in pharmacies: from 159 rubles.
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Azitral is a broad-spectrum antibiotic that is part of the macrolide group. Has a bactericidal effect in the focus of infection.
Release form and composition
Release form Azitral:
- Capsules of 250 mg, in a blister (6 capsules), cardboard pack;
- Capsules of 500 mg, in a blister strip packaging (3 capsules), cardboard pack.
It is a white powder, packaged in hard gelatin capsules, consisting of a body and a white cap.
One capsule of Azitral contains 250 or 500 mg of azithromycin as a dihydrate; and as auxiliary substances: anhydrous lactose, sodium lauryl sulfate, titanium dioxide, magnesium stearate, corn starch, purified water, propylparaben, methylparaben, gelatin.
Pharmacological properties
Pharmacodynamics
Azithromycin is a broad-spectrum antibiotic, a member of the azalide subgroup (macrolide antibiotics). The active substance has a wide spectrum of antimicrobial action. Azithromycin binds to the 50S ribosomal subunit, suppressing the biosynthesis of microorganism proteins. In the case of high concentrations in the focus of inflammation, it has a bactericidal effect. Differs in activity against the following gram-positive aerobic microorganisms: Streptococcus pneumoniae (penicillin-sensitive), Streptococcus spp. (groups a / b / c / g), Staphylococcus aureus (methicillin-sensitive), Streptococcus pyogenes. Also, the drug is effective against gram-negative aerobic microorganisms (Haemophilus parainfluenzae, Haemophilus influenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae),some anaerobic microorganisms (Clostridium perfringens, Prevotella spp., Porphyromonas spp., Fusobacterium spp.) and Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma pneumoniae, Chlamydia psittaci, Borrelia burgdorferi, Mycoplas.
Gram-positive aerobes [Streptococcus pneumoniae (penicillin-resistant)] can develop resistance to azithromycin. Gram-positive aerobes [Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant staphylococci show a very high degree of resistance to macrolides), erythromycin-resistant gram-positive bacteria], anaerobes (Bacteroides fragilis).
Pharmacokinetics
Azithromycin is rapidly absorbed from the gastrointestinal tract due to its lipophilicity and stability in an acidic environment. After internal administration of 500 mg of azithromycin, the time to reach its maximum concentration in blood plasma (C max) is from 2.5 to 2.96 hours, and the concentration itself is estimated at 0.4 mg / l. The bioavailability of azithromycin is 37%.
The active substance of Azitral penetrates well into the tissues and organs of the urogenital tract (for example, the prostate gland), respiratory tract, soft tissues and skin. The increased content in tissues (10-50 times higher than those in blood plasma) and a rather long half-life are explained by the low binding of the substance to blood plasma proteins and its penetration into eukaryotic cells with accumulation in the environment with a low pH value surrounding the lysosome. As a result, azithromycin is characterized by a large apparent volume of distribution (31.1 l / kg) with a high plasma clearance. The predominant accumulation of azithromycin in lysosomes is especially important for combating intracellular pathogens. Phagocytes deliver azithromycin to the sites of infection, where it is released during phagocytosis. In the foci of infection, the concentration of the drug is significantly higher (by 24–34%) than in healthy tissues, and depends on the degree of inflammatory edema. Despite the increased concentration in phagocytes, azithromycin does not significantly affect their function. The active substance in bactericidal concentrations remains for 5-7 days after administration, which allows the use of short courses of treatment (3 or 5 days each). About 50% of azithromycin is excreted unchanged in the bile, 6% in the urine. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, and therefore Azitral can be used once a day.and depends on the degree of inflammatory edema. Despite the increased concentration in phagocytes, azithromycin does not significantly affect their function. The active substance in bactericidal concentrations remains for 5-7 days after administration, which allows the use of short courses of treatment (3 or 5 days each). About 50% of azithromycin is excreted unchanged in the bile, 6% in the urine. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, and therefore Azitral can be used once a day.and depends on the degree of inflammatory edema. Despite the increased concentration in phagocytes, azithromycin does not significantly affect their function. The active substance in bactericidal concentrations remains for 5-7 days after administration, which allows the use of short courses of treatment (3 or 5 days each). About 50% of azithromycin is excreted unchanged in the bile, 6% in the urine. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, and therefore Azitral can be used once a day. The active substance in bactericidal concentrations remains for 5-7 days after administration, which allows the use of short courses of treatment (3 or 5 days each). About 50% of azithromycin is excreted unchanged in the bile, 6% in the urine. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, and therefore Azitral can be used once a day. The active substance in bactericidal concentrations remains for 5-7 days after administration, which allows the use of short courses of treatment (3 or 5 days). About 50% of azithromycin is excreted unchanged in the bile, 6% in the urine. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, in connection with which Azitral can be used once a day. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, in connection with which Azitral can be used once a day. The active substance is demethylated in the liver to form inactive metabolites. Excretion from blood plasma is carried out in 2 stages: the half-life is from 14 to 20 hours in the range of 8-24 hours after administration, 41 hours - in the range of 24-72 hours, in connection with which Azitral can be used once a day.
Food intake affects the pharmacokinetics (depends on the dosage form of the drug): when using capsules, the maximum plasma concentration decreases by 52%, and the area under the concentration-time pharmacokinetic curve (AUC) - by 43%. In elderly men (age from 65 to 85 years), pharmacokinetic characteristics do not change, and in women, C max increases by 30-50%.
Indications for use
Indications for the use of Azitral are infectious and inflammatory diseases caused by bacteria sensitive to the drug:
- Inflammatory diseases of the upper respiratory tract (sinusitis, tonsillitis, pharyngitis, tonsillitis, etc.);
- Inflammatory diseases of the lower respiratory tract (atypical and bacterial pneumonia, bronchitis);
- Scarlet fever;
- Infections of soft tissues and skin (impetigo, erysipelas, secondarily infected dermatoses);
- Infectious lesions of the urogenital zone (cervicitis or gonorrheal urethritis);
- Stomach ulcer;
- Lyme disease (initial stage).
Contraindications
The main contraindications for taking Azitral are:
- Liver failure;
- Renal failure;
- Pregnancy;
- Breast-feeding;
- Child's age up to 12 years;
- Hypersensitivity to this drug or other macrolides.
Instructions for the use of Azitral: method and dosage
Azithromycin retains its bactericidal effect inside the inflammatory focus for 5-7 days after the end of the last dose. It is this fact that makes the course of treatment with this drug short - 3 or 5 days.
Azitral 500 mg is usually prescribed in a course of three days, one tablet once a day. The tablet should be taken either one hour before meals or two hours after.
If the patient missed the time, then the medicine should be taken as soon as possible, and then the time interval should be restored to 24 hours.
The standard pediatric dosage of Azitral is calculated by the weight of the child - the daily dose is 10 mg / kg of the drug, the course dose is 30 mg / kg.
In each individual case, only the attending physician prescribes the dose and schedules the course of taking Azitral.
Side effects
According to the instructions, Azitral can cause the following side effects:
- Diarrhea, nausea, vomiting, flatulence - from the digestive system;
- Chest pain, palpitations - from the cardiovascular system;
- Dizziness, headache, anxiety, sleep disturbance - from the central nervous system;
- Vaginal candidiasis, nephritis - from the genitourinary system;
- Numerous allergic reactions.
During an overdose with Azitral, the following side effects may appear: vomiting, nausea, temporary hearing loss. Their appearance requires the appointment of symptomatic therapy.
Overdose
Symptoms: temporary hearing loss, severe nausea, vomiting, diarrhea.
There is no specific antidote.
Treatment should be prescribed in accordance with the existing symptoms.
special instructions
Care should be taken when prescribing Azitral for people suffering from arrhythmia.
During pregnancy, the drug is used only when the risk from use is less than the risk of developing dangerous consequences of the existing disease.
After taking Azitral 500 mg, it is worth considering the appearance of allergic reactions.
Application during pregnancy and lactation
During pregnancy, Azitral must be used with caution. The decision to prescribe the drug is made based on the ratio of the potential benefit to the mother and the perceived risk to the fetus.
In cases of need for use during lactation, it is recommended to stop breastfeeding.
Pediatric use
It is forbidden to use Azitral to treat patients under the age of 12 years with a body weight of up to 45 kg.
With impaired renal function
In severely impaired renal function, the drug is contraindicated.
In case of mild or moderate impairment of renal function, Azitral should be used with caution (dose adjustment is not required).
For violations of liver function
In severe hepatic impairment, the drug is contraindicated.
In case of mild or moderate impairment of liver function, Azitral should be used with caution (dose adjustment is not required).
Use in the elderly
When treating elderly patients, dose adjustment of Azitral is not required.
Drug interactions
Taking antacids (containing magnesium and aluminum) and food reduces the absorption of azithromycin, so Azitral must be taken 1 hour before or 2 hours after taking these drugs or food.
In healthy volunteers with the simultaneous use of cetirizine at a dose of 20 mg and azithromycin for 5 days, no pharmacokinetic interaction and a significant change in the QT interval were recorded.
In a study involving 6 HIV-infected patients, when didanosine at a dose of 400 mg per day and azithromycin at a dose of 1200 mg per day were taken together, there were no changes in the pharmacokinetic parameters of didanosine in comparison with the placebo group.
If it is necessary to jointly take Azitral with warfarin, it is recommended to carefully monitor the prothrombin time.
Pharmacokinetic studies did not reveal changes in the pharmacokinetics of azithromycin with a single use of cimetidine 120 minutes before taking azithromycin.
With the simultaneous use of zidovudine, its pharmacokinetics changes slightly. In particular, azithromycin has an effect on the excretion of zidovudine and its glucuronide metabolite by the kidneys. Also, due to the use of azithromycin, the concentration of phosphorylated zidovudine (a clinically active metabolite in peripheral blood mononuclear cells) increases, but the clinical significance of this effect is unclear.
Azithromycin is characterized by weak interaction with isoenzymes of the cytochrome P 450 family, while not being an inducer and inhibitor of cytochrome P 450 isoenzymes. The participation of azithromycin in the processes of pharmacokinetic interactions similar to erythromycin and other macrolides was not revealed.
Simultaneous daily intake of azithromycin at a dose of 600 mg per day once and efavirenz at a dose of 400 mg per day for a week did not lead to a clinically significant pharmacokinetic interaction.
The combined single use of azithromycin at a dose of 1200 mg and fluconazole at a dose of 800 mg did not change the pharmacokinetics of the latter. At the same time, no changes in the total exposure and half-life of azithromycin were recorded, but a decrease of 18% in its C max was observed, which has no clinical significance.
With the simultaneous use of azithromycin at a dose of 1200 mg and indinavir (3 times a day, 800 mg for 5 days), a statistically significant effect on pharmacokinetics was not revealed.
Azithromycin has no significant effect on the pharmacokinetics of methylprednisolone.
The simultaneous administration of macrolide antibiotics (including azithromycin) and substrates of P-glycoprotein (eg, digoxin) increases the concentration of the latter in the blood serum.
With simultaneous use with ergotamine and dihydroergotamine, the toxic effect (dysesthesia, vasospasm) increases.
In the case of combined use with triazolam, its clearance decreases and the pharmacological effect increases.
Simultaneous administration of azithromycin with atorvastatin did not cause changes in the concentration of the latter in plasma (in terms of inhibition of MMC-CoA reductase). At the same time, in the post-registration period, isolated cases of rhabdomyolysis were recorded in patients who simultaneously received statins and azithromycin.
During a pharmacokinetic study involving healthy volunteers who took azithromycin (once orally 500 mg per day) for 3 days, and then cyclosporin (once 10 mg / kg per day), the maximum concentration of cyclosporine in blood plasma and the area under the pharmacokinetic concentration-time curve. With the simultaneous use of these drugs, care should be taken. If it is necessary to take it together, it is necessary to control the plasma levels of cyclosporine and adjust the dose accordingly.
The simultaneous administration of nelfinavir and azithromycin leads to an increase in the equilibrium concentration of the latter in the blood serum. At the same time, clinically significant side effects were not recorded, and dose adjustment of azithromycin against the background of simultaneous use of nelfinavir is not required.
In the case of joint use of rifabutin and azithromycin, the concentration of each of them in the blood serum does not change. With the simultaneous use of these drugs, cases of neutropenia were sometimes observed, which were associated with taking rifabutin. No causal relationship was found between the development of neutropenia and the use of a combination of rifabutin and azithromycin.
In the course of studies involving healthy volunteers, no cases of the effect of azithromycin (500 mg daily for 3 days) on C max and AUC of sildenafil or the main circulating metabolite were recorded.
In cases of joint administration of terfenadine and azithromycin, care must be taken, since it has been established that the combination of terfenadine and various antibiotics can lead to the development of arrhythmias and prolongation of the QT interval. Based on this, it is impossible to exclude the manifestation of the above complications while taking azithromycin and terfenadine.
Interaction between theophylline and azithromycin has not been identified.
With the combined administration of azithromycin with midazolam or triazolam in therapeutic doses, significant changes in pharmacokinetic parameters were not revealed.
In cases of simultaneous use of azithromycin and sulfamethoxazole / trimethoprim, there was no significant change in C max, total exposure or renal excretion of sulfamethoxazole or trimethoprim. The serum azithromycin concentration was in line with those reported in other studies.
Analogs
Azitral's analogs for the active substance: Azivok, Azitrox, Azitrocin, Zitrolide, Sumamed, Sumamox, Hemomycin, Ecomed, etc.
Drugs of the same pharmacological subgroup, similar in the mechanism of action: Arvicin, Vilprafen, Klabaks, Clarexid, Clarithromycin, Claricin, Lecoclar, Macropen, Oleandomycin, Roxolit, Safotsid, etc.
Terms and conditions of storage
Store in a dry place, out of reach of children, with an air temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Azitral
Reviews of Azitral indicate its effectiveness in the treatment of various infectious diseases (for example, sinusitis, tonsillitis, urogenital and concomitant infections). The tolerance of the drug is individual, the most common side effects are abdominal pain, diarrhea and vomiting.
Azitral price in pharmacies
The approximate price for Azitral is 300 rubles (in a package of 6 capsules of 250 mg each).
Azitral: prices in online pharmacies
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Drug name Price Pharmacy |
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Azitral 250 mg capsules 6 pcs. 159 r Buy |
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Azitral 500 mg capsules 3 pcs. 220 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
