Azithromycin-VERTEX - Instructions For Use, Price, Reviews, 250 Mg

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Azithromycin-VERTEX

Azithromycin-VERTEX: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Azithromycin-VERTEX

ATX code: J01FA10

Active ingredient: azithromycin (Azithromycin)

Manufacturer: JSC "VERTEX" (Russia)

Description and photo update: 2020-07-05

Prices in pharmacies: from 186 rubles.

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Azithromycin-VERTEX is an oral antibiotic that belongs to the group of macrolides-azalides.

Release form and composition

The preparation is produced in the form of capsules: hard gelatinous, size No. 0, white; the contents of the capsules are white with a pale yellow tint or white powder; it is possible that conglomerates are easily transformed into a free-flowing powder when pressed (6 or 10 pieces in a blister, 6 pieces in a polyethylene can; in a cardboard box 1 package / can and instructions for the use of Azithromycin-VERTEX).

1 capsule contains:

• active substance: azithromycin dihydrate - 262.02 mg, which is equivalent to azithromycin in the amount of 250 mg;
• additional components: sodium lauryl sulfate, povidone K-17 (low molecular weight polyvinylpyrrolidone), microcrystalline cellulose, lactose monohydrate, magnesium stearate;
• capsule shell: titanium dioxide, gelatin.

Pharmacological properties

Pharmacodynamics

Azithromycin-VERTEX is a broad-spectrum antibiotic azalide with pronounced bacteriostatic efficacy. The mechanism of action of the drug is based on the inhibition of bacterial protein production. As a result of binding to the 50S-subunit of the ribosome, the active substance suppresses peptide translocase at the stage of translation and inhibits protein synthesis, inhibiting the growth and reproduction of pathogenic microbes. When used in high concentrations, the agent has a bactericidal effect. Azithromycin is active against a number of anaerobic, intracellular, gram-negative, gram-positive and other pathogens. Microorganisms may initially show resistance to the effect of the active substance or acquire resistance to it.

Below is the minimum inhibitory concentration (MIC) of azithromycin (in mg / L) for the following microorganisms (a - sensitive; b - resistant):

• Streptococcus A, B, C, G: a ≤ 0.25; b> 0.5;
• Staphylococcus spp.: a ≤ 1; b> 2;
• pneumoniae: a ≤ 0.25; b> 0.5;
• M. catarrhalis: a ≤ 0.5; b> 0.5;
• H. Influenzae: a ≤ 0.12; b> 4;
• gonorrhoeae: a ≤ 0.25; b> 0.5.

Spectrum of antimicrobial effect of Azithromycin-VERTEX:

• pathogens, mainly sensitive: gram-positive aerobes - Streptococcus pneumoniae (penicillin-sensitive), Staphylococcus aureus (methicillin-sensitive), Streptococcus pyogenes; gram-negative aerobes - Haemophilus parainfluenzae, Haemophilus influenzae, Legionella pneumophila, Neisseria gonorrhoeae, Pasteurella multocida, Moraxella catarrhalis; anaerobes - Fusobacterium spp., Clostridium perfringens, Porphyromonas spp., Prevotella spp.; other microorganisms - Mycoplasma pneumoniae, Chlamydia pneumoniae, Chlamydia trachomatis, Chlamydia psittaci, Borrelia burgdorferi, Mycoplasma hominis;
• pathogens that can acquire resistance: Streptococcus pneumoniae (penicillin-resistant);
• pathogens initially refractory: gram-positive bacteria resistant to erythromycin; gram-positive aerobes - Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant staphylococci with a very high frequency have acquired resistance to macrolides); anaerobes: Bacteroides fragilis.

Pharmacokinetics

When taken orally, azithromycin is intensively absorbed and rapidly distributed in the body. After taking the active substance in a dose of 500 mg, its maximum concentration in the blood (C _max) is observed after 2-3 hours and is 0.4 mg / l. Due to the first pass effect, bioavailability is 37%.

The apparent volume of distribution is 31.1 l / kg, the binding of the drug to plasma proteins is inversely proportional to its content in the blood and can vary from 7 to 50%. Since the substance passes through the plasma membrane, its use is effective in infections caused by intracellular pathogens. Azithromycin is transported to the site of infection by phagocytes, where it is released in the presence of bacteria. Easily penetrates histohematogenous barriers and enters tissues. The content of the active substance in cells and tissues is 10-50 times higher than in plasma, and in the focus of infection it is 24-34% higher than that in healthy tissues.

Azithromycin is characterized by a rather long half-life (T _1/2) - 35-50 hours, from tissues T _{1/2 is} much longer. After using the last dose, the therapeutic concentration of the drug lasts up to 5-7 days. Eliminated mainly unchanged by the intestines - 50%, and by the kidneys - 6%. In the liver, the agent is demethylated and loses its activity.

Indications for use

Azithromycin-VERTEX is recommended for use in the treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• infections of the lower respiratory tract - chronic bronchitis in the acute phase, acute bronchitis, pneumonia, including those caused by atypical pathogens;
• infections of the ENT organs and upper respiratory tract - tonsillitis, pharyngitis, sinusitis, otitis media;
• urinary tract infections associated with Chlamydia trachomatis - cervicitis, urethritis;
• infections of soft tissues and skin - moderate acne vulgaris, impetigo, erysipelas, secondarily infected dermatoses;
• the initial stage of borreliosis (Lyme disease) is erythema migrans (erythema migrans).

Contraindications

Absolute:

• age up to 12 years and body weight less than 45 kg;
• severe liver failure;
• lactose intolerance, glucose-galactose malabsorption, lactase deficiency;
• simultaneous use with dihydroergotamine and ergotamine;
• hypersensitivity to erythromycin, azithromycin, other macrolides or ketolides, or to additional components of the drug.

Relative (it is necessary to take Azithromycin-VERTEX with caution):

• functional impairment of the liver of mild / moderate severity;
• myasthenia gravis;
• end-stage renal failure with a glomerular filtration rate (GFR) less than 10 ml / min;
• proarrhythmogenic factors, mainly present in elderly patients: congenital / acquired lengthening of the QT interval, concomitant therapy with class IA (procainamide, quinidine) and III (amiodarone, dofetilide, sotalol) antiarrhythmic drugs, cisapride, terfenadine, fluoroquinolones (levofloxacin), moxifloxacinans (citalopram), antipsychotics (pimozide); clinically significant bradycardia, cardiac arrhythmias, or severe heart failure; violations of water and electrolyte balance, especially with hypomagnesemia or hypokalemia;
• combined treatment with warfarin, digoxin, terfenadine, cyclosporine.

Azithromycin-VERTEX, instructions for use: method and dosage

Azithromycin-VERTEX capsules are taken orally 1 time / day, at least 1 hour before or 2 hours after a meal.

The recommended dosage regimen for adults (including elderly patients) and adolescents over 12 years of age with a body weight of more than 45 kg:

• infections of ENT organs, upper and lower respiratory tract, soft tissues and skin: 500 mg / day (2 capsules) for 3 days; course dose - 1500 mg;
• urinary tract infections, excited by Chlamydia trachomatis (uncomplicated urethritis, cervicitis): 1000 mg once (4 capsules);
• borreliosis (Lyme disease) in the initial stage (erythema migrans): on the first day, 1000 mg / day, from 2 to 5 days, 500 mg / day daily; duration of therapy - 5 days, dose per course - 3000 mg;
• acne vulgaris of moderate severity: 500 mg / day for 3 days, then in the same dose 1 time in 1 week; course - 9 weeks, total dose - 6000 mg; the first weekly dose of 500 mg should be used 7 days after taking the first daily dose, that is, on the eighth day of the course, the next 8 weekly doses of 500 mg should be taken at intervals of 7 days.

Side effects

• blood and lymphatic system: infrequently - eosinophilia, leukopenia, neutropenia; extremely rare - hemolytic anemia, thrombocytopenia;
• infectious diseases: infrequently - candidiasis, including the oral mucosa; bacterial infection, fungal infection, rhinitis, pharyngitis, respiratory lesions, pneumonia, gastroenteritis, vaginal infection; with an unknown frequency - pseudomembranous colitis;
• metabolism and nutritional disorders: infrequently - anorexia;
• nervous system: often - headache; infrequently - drowsiness / insomnia, impaired taste, nervousness, dizziness, paresthesia; rarely - agitation; with an unknown frequency - loss of taste, loss / perversion of smell, hypesthesia, psychomotor hyperactivity, anxiety, aggression, convulsions, fainting, myasthenia gravis, hallucinations, delirium;
• immune system: infrequently - hypersensitivity reaction, angioedema; with an unknown frequency - anaphylactic reaction;
• organ of vision: infrequently - visual impairment;
• hearing organ and labyrinthine disorders: infrequently - vertigo, hearing impairment; with an unknown frequency - hearing impairment, including tinnitus and / or deafness;
• respiratory system: infrequently - nosebleeds, shortness of breath;
• liver and biliary tract: infrequently - hepatitis; rarely - cholestatic jaundice, liver dysfunction; with an unknown frequency - liver failure, in some cases with fatal outcome (mainly against the background of serious liver dysfunctions), fulminant hepatitis, liver necrosis;
• gastrointestinal tract (GIT): very often - diarrhea; often - nausea, abdominal pain, vomiting; infrequently - increased secretion of salivary glands, dryness / ulcers of the oral mucosa, flatulence, belching, dysphagia, dyspepsia, bloating, constipation, gastritis; extremely rare - discoloration of the tongue, pancreatitis;
• skin and subcutaneous tissues: infrequently - sweating, dry skin, itching, skin rash, urticaria, dermatitis; rarely - photosensitivity reaction; with an unknown frequency - erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, drug rash accompanied by systemic manifestations and eosinophilia - drug hypersensitivity syndrome (DRESS syndrome);
• cardiovascular system: infrequently - flushing of the face, palpitations; with an unknown frequency - a decrease in blood pressure (BP), an increase in the QT interval on an electrocardiogram (ECG), ventricular tachycardia, pirouette-type arrhythmia;
• genitals and mammary gland: infrequently - dysfunction of the testicles, metrorrhagia;
• kidneys and urinary tract: infrequently - pain in the kidney area, dysuria; with an unknown frequency - acute renal failure, interstitial nephritis;
• musculoskeletal system: infrequently - back / neck pain, myalgia, osteoarthritis; with an unknown frequency - arthralgia;
• laboratory data: often - a decrease in the number of lymphocytes, an increase in the number of monocytes / eosinophils / neutrophils / basophils, a decrease in the plasma level of bicarbonates in the blood; infrequently - increased activity of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP); an increase in the plasma concentration of chlorides / bicarbonates in the blood, an increase in the content of urea / creatinine / bilirubin in the blood plasma, a change in the level of sodium / potassium in the blood, an increase in the level of glucose in the blood, a decrease in hematocrit, an increase in the number of platelets;
• others: infrequently - a feeling of fatigue, malaise, asthenia, edema, chest pain, facial edema, peripheral edema, fever.

Overdose

Symptoms of an Azithromycin-VERTEX overdose may include the following effects: temporary hearing loss, nausea, diarrhea, vomiting.

Treatment is symptomatic.

special instructions

If the next dose of Azithromycin-VERTEX is missed, it must be taken as early as possible, and subsequent doses - at intervals of 24 hours.

If symptoms of liver dysfunction are found, including darkening of urine, rapidly increasing asthenia, jaundice, a tendency to bleeding and hepatic encephalopathy, treatment with the drug should be discontinued and a study should be carried out to determine the functional state of the liver.

During therapy with azithromycin, you need to be regularly examined for the presence of resistant microorganisms and signs of superinfections, including fungal infections.

Azithromycin-VERTEX should not be used for longer courses than indicated in the instructions, since the pharmacokinetic properties of the drug make it possible to recommend a simple and short-term dosing regimen.

There are no data on the reactions of possible interactions of azithromycin with dihydroergotamine and ergotamine derivatives, however, since ergotism develops with the simultaneous use of these derivatives with macrolides, such combinations are contraindicated.

If treatment with azithromycin is carried out for a long time, there is a possibility of developing pseudomembranous colitis, excited by Clostridium difficile, and manifests itself both in the form of mild diarrhea and severe colitis. If antibiotic-associated diarrhea develops during the period of therapy, as well as 2 months after its completion, it is necessary to exclude the occurrence of clostridial diarrhea (pseudomembranous colitis). In this situation, you cannot use drugs that inhibit intestinal peristalsis.

On the background of treatment with macrolides, including azithromycin, lengthening of cardiac repolarization and QT interval was recorded, increasing the threat of cardiac arrhythmias, including ventricular tachycardia of the pirouette type. There are also reports of the development in patients taking azithromycin, exacerbations of symptoms of myasthenia gravis or a new myasthenic syndrome.

After discontinuation of Azithromycin-VERTEX, hypersensitivity reactions may persist in some patients, which requires specific therapy.

Influence on the ability to drive vehicles and complex mechanisms

Patients driving vehicles or working with other complex mechanisms should be careful during the period of therapy, since Azithromycin-VERTEX can provoke the development of adverse events from the organ of vision and the nervous system.

Application during pregnancy and lactation

During pregnancy, you can use Azithromycin-VERTEX only if the benefits of treatment significantly outweigh the possible risk to the fetus.

If an antibiotic is needed during lactation, it is necessary to suspend breastfeeding.

Pediatric use

For children under 12 years of age and with a body weight of less than 45 kg, drug therapy is contraindicated.

With impaired renal function

Patients with end-stage renal failure, with GFR less than 10 ml / min, drug therapy should be carried out with caution, monitoring the state of renal function.

Against the background of mild to moderate renal dysfunction, with a GFR of 10–80 ml / min, dose changes are not required.

For violations of liver function

In the presence of severe hepatic impairment (class C according to the Child-Pugh classification), the use of Azithromycin-VERTEX is contraindicated.

Patients with mild / moderate hepatic impairment (Child-Pugh grades A and B) do not need to adjust the dose of the antibiotic, but it should be taken with extreme caution due to the increased risk of severe liver failure and fulminant hepatitis.

Use in the elderly

No dose adjustment of Azithromycin-VERTEX is required for the elderly. However, elderly patients should take the drug with extreme caution due to the possible presence of proarrhythmogenic conditions in them, which significantly increases the risk of developing cardiac arrhythmias, including pirouette-type arrhythmias.

Drug interactions

• atorvastatin (10 mg / day): there are no changes in the plasma concentration of this substance in the blood when combined with azithromycin at a dose of 500 mg / day, however, there are separate reports of the occurrence of rhabdomyolysis with the simultaneous use of azithromycin and statins;
• digoxin (substrates of P-glycoprotein): the plasma concentration of this substance in the blood increases, which must be taken into account when carrying out the combination;
• cetirizine (20 mg): no pharmacokinetic interaction and significant changes in the QT interval were recorded when used in combination in healthy volunteers for 5 days;
• antacids: the bioavailability of azithromycin does not change, but it decreases by 30% of its C _max in the blood, as a result of which the drug should be used at least 1 hour before or 2 hours after taking these funds;
• didanosine (dideoxyinosine) (400 mg / day): no changes in its pharmacokinetic characteristics were detected when combined with azithromycin (1200 mg / day) in HIV-infected individuals compared with a placebo group;
• zidovudine: there is no significant effect on the pharmacokinetics (including urinary excretion) of this substance and its glucuronide derivative when combined with azithromycin 1000 mg once and with repeated 1200/600 mg administration, but an increase in the concentration of a clinically active metabolite, phosphorylated zidovudine, is recorded. peripheral blood mononuclear cells;
• cimetidine: when used 2 hours before taking azithromycin, no changes in the pharmacokinetics of the latter are observed;
• indirect anticoagulants (coumarin derivatives): there is no change in the anticoagulant effect when using warfarin in a single dose of 15 mg; since there is information about an increase in the anticoagulant effect with the combination of Azithromycin-VERTEX with coumarin derivatives, it is recommended to monitor the prothrombin time in this combination;
• carbamazepine: in blood plasma, the concentration of this substance and its active metabolite does not undergo significant changes;
• indinavir (5 days, 3 times / day, 800 mg): no effect on the pharmacokinetics of this drug when combined with azithromycin (1200 mg once) is observed;
• efavirenz (7 days at 400 mg / day): no clinically significant pharmacokinetic interaction is detected when combined with azithromycin once at a dose of 600 mg / day;
• cyclosporine (10 mg / kg / day): there is an increase in C _max and the area under the concentration-time curve for a period of 0-5 hours (AUC _0-5) of this substance, if combined use is necessary, it is required to monitor its concentration in the blood and adjust the dose;
• fluconazole (800 mg once): in combination with azithromycin (1200 mg once), the pharmacokinetics of fluconazole does not change; the total exposure and T _{1/2 of} azithromycin remain unchanged, and its C _max decreases by 18%, which has no clinical significance;
• rifabutin: the effect on the plasma concentration of each of these substances in the blood is not determined; with combined treatment with azithromycin and rifabutin, neutropenia was sometimes observed associated with taking rifabutin, the relationship of this complication with the combination has not been established;
• nelfinavir (750 mg 3 times / day): with concomitant treatment with azithromycin (1200 mg), the equilibrium concentration of the latter in the blood plasma increases; no significant side effects are observed, dose adjustment is not required;
• sildenafil: C _max and AUC of a given substance or its main circulating metabolite does not change in the case of combination with azithromycin (3 days, 500 mg / day);
• terfenadine: no interaction was found in studies; the simultaneous use of terfenadine and macrolides can provoke arrhythmia and prolongation of the QT interval;
• methylprednisolone: no pronounced effect on its pharmacokinetics is observed;
• theophylline: no interaction detected;
• triazolam / midazolam; trimethoprim / sulfamethoxazole: no pronounced changes in the pharmacokinetic characteristics of these drugs are found;
• ergot alkaloids: the simultaneous use of Azithromycin-VERTEX with derivatives of these drugs is not recommended due to the possible development of ergotism.

Analogs

Azithromycin-VERTEX analogs are Azithromycin, Azitral, Azibiot, Azitrox, AzitRus, ZI-Factor, Azithromycin Sandoz, Azithromycin Avexim, Sumamed, Hemomycin, etc.

Terms and conditions of storage

Store out of the reach of children and protected from light, at a temperature not exceeding 25 ° C.

The shelf life is 3.5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Azithromycin-VERTEX

The patient reviews about Azithromycin-VERTEX are mostly positive. The advantages of the drug include a wide spectrum of action, convenient form of release and dosage regimen, high efficiency in infectious lesions caused by sensitive microorganisms, a short course of therapy, as well as availability and low cost.

However, there are many reports in which they indicate the appearance of side effects, including of a pronounced nature, mainly from the side of the digestive tract. In rare cases, an insufficient therapeutic effect of the drug is noted. Patients consider Azithromycin-VERTEX to be a rather serious antibiotic and recommend consulting a doctor if adverse events develop.

Price for Azithromycin-VERTEX in pharmacies

The price of Azithromycin-VERTEX 250 mg can be 190 rubles. per package containing 6 capsules.

Azithromycin-VERTEX: prices in online pharmacies

Drug name Price Pharmacy

Azithromycin-Vertex capsules 250mg 6pcs RUB 186 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!