AzitRus, 50 mg 4.2g 3 pcs.

Skin infections, Otitis media, Infectious diseases, Pharyngitis, Lung inflammation (pneumonia), Urethritis, Haymorrhitis, Angina, Bronchitis, Tonsillitis, Respiratory tract infections

According to the FDA (2020), oral azithromycin is indicated to treat patients with mild to moderate infections (pneumonia: see “Precautions. “Precautions”) caused by susceptible strains of the indicated microorganisms under certain conditions listed below.

Adults

Acute bacterial exacerbations of chronic obstructive pulmonary disease caused by Haemophilus influenzae, Moraxella catarrhalis or Streptococcus pneumoniae.

Acute bacterial sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis or Streptococcus pneumoniae.

Out-of-hospital pneumonia caused by Chlamydophila pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae or Streptococcus pneumoniae in patients who are prescribed oral therapy.

. Azithromycin should not be used in patients with pneumonia who are not indicated for oral therapy because of moderate to severe disease or when risk factors are present, such as patients with cystic fibrosis, patients with nosocomial infections, patients with known or suspected bacteremia, patients requiring hospitalization, elderly or frail patients, patients with serious underlying health problems that may impede their ability to respond to disease (including immunodeficiency or functional

Pharyngitis/tonsillitis caused by Streptococcus pyogenes is an alternative to first-line therapy in patients in whom first-line therapy cannot be used.

Note. Penicillin administered by injection/m is usually the drug of choice in the treatment of infections caused by Streptococcus pyogenes and the prevention of rheumatic fever. Azithromycin is often effective in eradicating sensitive strains of Streptococcus pyogenes from the nasopharynx. Since some strains are resistant to azithromycin, tests for azithromycin sensitivity should be performed during treatment of patients. There are no data confirming the effectiveness of azithromycin in the subsequent prevention of rheumatic fever.

Uncomplicated infections of the skin and skin structures caused by Staphylococcus aureus, Streptococcus pyogenes or Streptococcus agalactiae. Abscesses usually require surgical intervention.

Urethritis and cervicitis caused by Chlamydia trachomatis or Neisseria gonorrhoeae.

Infectious genital disease in men caused by Haemophilus ducreyi (Chancroid). Because of the small number of women included in clinical trials, the effectiveness of azithromycin in the treatment of chancroid in women has not been established.

Azithromycin should not be relied on at the recommended dose to treat syphilis. Antimicrobials used in high doses for short periods of time to treat nongonococcal urethritis may mask or delay the presentation of symptoms during the incubation period of syphilis. All patients with urethritis or cervicitis as a result of a sexually transmitted infection should have a serologic test for syphilis and appropriate cultures for gonorrhea at the time of diagnosis. If the infection is confirmed, appropriate antimicrobial therapy should be started and follow-up tests for these diseases should be performed.

At the beginning of treatment, appropriate tests should be performed to determine the pathogen and its sensitivity to azithromycin. Azithromycin therapy may be initiated before the results of these tests are available; once the results are available, antimicrobial therapy should be adjusted.

In order to prevent the development of drug-resistant bacteria and to maintain the effectiveness of azithromycin and other antibacterial drugs, azithromycin should only be used to treat or prevent infections for which sensitive bacteria are proven or reasonably suspected to cause them. When culture and sensitivity information is available, it should be considered when selecting or modifying antibiotic therapy. In the absence of such data, the local epidemiologic situation and sensitivity patterns may contribute to the empirical choice of therapy.

Pediatric patients

Acute otitis media caused by Haemophilus influenzae, Moraxella catarrhalis or Streptococcus pneumoniae.

Out-of-hospital pneumonia caused by Chlamydophila pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae or Streptococcus pneumoniae in patients who are indicated for oral therapy.

. Azithromycin should not be used in pediatric patients with pneumonia who are not indicated for oral therapy because of moderate to severe disease or when risk factors are present, such as patients with cystic fibrosis, patients with hospital-acquired infections, patients with known or suspected bacteremia, patients requiring hospitalization, patients with serious underlying health problems that may impede the ability to respond to disease (including immune deficiency or functional asperity).

Pharyngitis/tonsillitis caused by Streptococcus pyogenes is an alternative to first-line therapy in patients in whom first-line therapy cannot be used.

Note. Penicillin administered by injection/m is usually the drug of choice in the treatment of infections caused by Streptococcus pyogenes and the prevention of rheumatic fever. Azithromycin is often effective in eradicating sensitive strains of Streptococcus pyogenes from the nasopharynx. Since some strains are resistant to azithromycin, tests for azithromycin sensitivity should be performed during treatment of patients. There are no data confirming the efficacy of azithromycin in the subsequent prevention of rheumatic fever.

At the beginning of treatment, appropriate tests should be performed to determine the causative agent and its sensitivity to azithromycin. Azithromycin therapy may be initiated before the results of these tests are available; once the results are available, antimicrobial therapy should be adjusted.

Active ingredient

How to take, the dosage

The drug is taken orally 1 time per day 1 hour before or 2 hours after the meal.

Adults

Infections of the upper and lower respiratory tracts are indicated with 500 mg/day for 3 days (course dose 1.5 g).

Infections of the skin and soft tissues: 1 g/day on day 1, then 500 mg daily on days 2 to 5 (cumulative dose – 3 g).

In case of uncomplicated urethritis and/or cervicitis 1 g is prescribed once.

In Lyme disease (borreliosis) to treat the initial stage (erythema migrans) 1 g is prescribed on day 1 and 500 mg daily from day 2 to day 5 (course dose – 3 g).

In case of gastric and duodenal ulcer associated with Helicobacter pylori 1 g/day is prescribed for 3 days in combined anthelicobacter therapy.

In children

. The preparation in capsule form is indicated in children over 3 years old and/or with body weight more than 25 kg in case of infections of the upper and lower respiratory tract, skin and soft tissues at the rate of 10 mg/kg of body weight once daily for 3 days (course dose – 30 mg/kg), or 10 mg/kg on the 1st day and then 5-10 mg/kg/day for 4 days.

In treatment of initial stage (erythema migrans) of Lyme disease (borreliosis) the drug is prescribed in dose of 20 mg/kg on the 1st day, then 10 mg/kg from the 2nd to 5th day.

The drug in the form of oral suspension is prescribed to children over 6 months old in case of infections of the upper and lower respiratory tract, skin and soft tissues at the rate of 10 mg/kg of body weight once/day for 3 days (the course dose is 30 mg/kg), or for 5 days: 10 mg/kg on the 1st day, then 5-10 mg/kg/day for 4 days.

The recommended doses of the drug, depending on the body weight of the child, are given in the table.

Interaction

When used concomitantly, antacids (aluminum- and magnesium-containing), ethanol and food slow down and decrease the absorption of azithromycin.

When co-administration of azithromycin in therapeutic doses with warfarin no changes in prothrombin time were observed, but taking into account that in case of interaction of macrolides with warfarin there may be increased anticoagulant effect, close monitoring of prothrombin time is necessary when prescribing this combination in patients.

Concomitant use increases plasma concentrations of digoxin.

The toxic effects (vasospasm, dysesthesia) of ergotamine and dihydroergotamine are increased with concomitant use.

Concomitant use decreases clearance and enhances the pharmacological effects of triazolam.

Azithromycin inhibits microsomal oxidation in hepatocytes which leads to delayed excretion and increased plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine as well as drugs In addition to these drugs subject to microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline), toxicity of cycloserine and other drugs subject to microsomal oxidation.including theophylline).

Lincosamines decrease the effectiveness of azithromycin.

Tetracycline and chloramphenicol increase the effectiveness of azithromycin.

Particular information

The drug is not taken with food.

If a dose is missed, the missed dose should be taken as soon as possible and subsequent doses should be taken 24 hours apart.

A gap of at least 2 hours should be observed between doses of AzitRUS® and antacid drugs.

After discontinuation of the drug hypersensitivity reactions may persist in some patients, in these cases specific therapy under medical supervision is recommended.

Contraindications

Side effects

In clinical trials, most side effects reported were mild to moderate in severity and reversible after azithromycin withdrawal. Potentially serious side effects, such as angioneurotic edema and cholestatic jaundice, were rarely reported. Approximately 0.7% of patients (adults and children) in 5-day multiple-dose clinical trials discontinued azithromycin therapy because of the development of treatment-related side effects.

In adults who received azithromycin at a dose of 500 mg/day, the rate of discontinuation due to treatment-related side effects after 3 days of treatment was 0.6%. In clinical trials involving pediatric patients, when 30 mg/kg was administered either as a single dose of azithromycin or for 3 days, discontinuation of azithromycin associated with the development of treatment-associated side effects was about 1%. Most side effects leading to discontinuation were GI-related, including nausea, vomiting, diarrhea, or abdominal pain.

The results of clinical trials

Because clinical trials are conducted with a different set of conditions, the incidence of adverse reactions observed in these clinical trials may not match that obtained in other clinical trials and observed in clinical practice.

Adults

Multidose regimens. Overall, the most common treatment-associated adverse reactions in adult patients receiving multiple doses of azithromycin were gastrointestinal effects. The most commonly reported adverse reactions were diarrhea/ fluid stools (4-5%), nausea (3%), and abdominal pain (2-3%).

There were no other treatment-related adverse effects with an incidence greater than 1% in patients receiving multiple doses of azithromycin.

The undesirable reactions that occurred with a frequency of ≤1% included the following.

Cardiovascular side: palpitations, chest pain.

Gastrointestinal disorders: dyspepsia, flatulence, vomiting, melena, cholestatic jaundice.

Urinary system: candidiasis, vaginitis, nephritis.

Nervous system disorders: dizziness, headache, vertigo, drowsiness.

General: fatigue.

Allergic reactions: rash, skin itching, photosensitivity, angioedema.

The single dose regimen is 1 g. In general, the most frequent adverse effects in patients who received azithromycin single dose 1 g were gastrointestinal related and were reported more frequently than in patients who received the multiple-dose regimen.

The side effects reported in patients on a single-dose azithromycin regimen with a frequency of 1% or more included diarrhea/iodine stool (7%), nausea (5%), abdominal pain (5%), vomiting (2%), dyspepsia (1%), vaginitis (1%).

The single dose regimen is 2 g. Overall, the most frequent side effects in patients who received azithromycin in a single dose of 2 g were gastrointestinal related.

The side effects reported in patients on a single dose of azithromycin in this study with a frequency of 1% or more included nausea (18%), diarrhea/ fluid stools (14%), vomiting (7%), abdominal pain (7%), vaginitis (2%), dyspepsia (1%), and dizziness (1%). Most complaints were moderate in nature.

Pediatric patients

Single- and multiple-dose regimens. The types of side effects in pediatric patients were comparable to those in adults, with different frequencies for the dosing regimens recommended in pediatric practice.

Acute otitis media: at the recommended total dosage of 30 mg/kg, the most frequent treatment-related side effects (≥1%) were diarrhea, abdominal pain, vomiting, nausea, and rash.

The frequency of side effects, depending on dosing regimen, for 1-, 3-, and 5-day dosing regimens were: diarrhea, 4.3; 2.6 and 1.8%; abdominal pain, 1.4; 1.7 and 1.2%; vomiting, 4.9; 2.3 and 1.1%; nausea, 1, 0.4 and 0.5%; rash, 1, 0.6 and 0.4%.

Out-of-hospital pneumonia: for the recommended dosing regimen of 10 mg/kg on day 1 followed by 5 mg/kg on days 2-5, the most common treatment-related side effects were diarrhea/ladder stool (5.8%), abdominal pain (1.9%), vomiting (1.9%), nausea (1.9%), and rash (1.6%).

Pharyngitis/tonsillitis: with a recommended dosing regimen of 12 mg/kg on days 1-5, the most common treatment-related side effects were diarrhea (5.4%), abdominal pain (3.4%), vomiting (5.6%), nausea (1.8%), rash (0.7%), and headache (1.1%).

There were no other treatment-related side effects occurring at a frequency of >1% in pediatric practice with any treatment regimen.

The side effects observed with a frequency of ≤1% included the following.

Cardiovascular side: chest pain.

Gastrointestinal disorders: dyspepsia, constipation, anorexia, enteritis, flatulence, gastritis, jaundice, loose stools, oral candidiasis.

With the blood and lymphatic system: anemia, leukopenia.

Nervous system disorders: headache (in otitis media), hyperkinesia, dizziness, agitation, nervousness, insomnia.

General: fever, facial swelling, fatigue, fungal infection, malaise, pain.

Allergic: rash and allergic reaction.

Respiratory system: increased cough, pharyngitis, pleural effusion, rhinitis.

Skin and its appendages: eczema, fungal dermatitis, itching, sweating, urticaria, vesiculobulic rash.

Sensory organs: conjunctivitis.

Postmarketing experience

Unwanted reactions reported when taking azithromycin during the postmarketing period in adult and/or pediatric patients for which a causal relationship has not been established include the following.

Allergic reactions: arthralgia, edema, urticaria and angioedema.

Systemic reactions: arrhythmias, including ventricular tachycardia and hypotension. There have been reports of cases of prolonged QT interval and torsade de pointes.

Gastrointestinal disorders: anorexia, constipation, dyspepsia, flatulence, vomiting/diarrhea, rarely leading to dehydration, pseudomembranous colitis, pancreatitis, oral candidiasis, gateway stenosis; there have been rare reports of discolored tongue.

General: asthenia, paresthesia, fatigue, malaise and anaphylaxis (rarely fatal).

Urogenital system disorders: interstitial nephritis, acute renal failure and vaginitis.

Hematopoietic disorders: thrombocytopenia.

Liver/biliary tract disorders: adverse reactions associated with liver dysfunction.

Nervous system disorders: seizures, dizziness/vertigo, headache, drowsiness, hyperactivity, nervousness, agitation and fainting.

Mental disorders: aggressive reactions and anxiety.

Skin and skin appendages: itching, severe skin reactions including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis and DRESS syndrome.

Sensory organs: hearing disorders, including hearing loss, deafness and/or tinnitus, as well as reports of perversion and/or loss of taste/sensation.

Laboratory abnormalities

Adults

Clinically significant abnormalities (without regard to drug association) reported during clinical trials with an incidence greater than 1% have been reported: Decreased Hb, hematocrit, lymphocytes, neutrophils and blood glucose, increased serum CPK, potassium, ALT, GGT, AST, bilirubin, creatinine, blood glucose, platelet count, lymphocytes, neutrophils and eosinophils; with a frequency less than 1%: Leukopenia, neutropenia, decreased sodium, potassium, platelet count, increased monocyte count, basophils, bicarbonate, serum ALP, bilirubin, LDH, and phosphate. Most patients with elevated serum creatinine also had abnormal baseline values.

The changes in laboratory tests were reversible.

In multiple-dose clinical trials involving more than 5,000 patients, 4 patients discontinued azithromycin therapy because of treatment-related liver enzyme abnormalities and 1 because of impaired renal function.

Pediatric patients

One-, three-, and five-day regimens. Laboratory data collected in comparative clinical trials using two 3-day regimens (30 or 60 mg/kg in divided doses for 3 days) or two 5-day regimens (30 or 60 mg/kg) in divided doses for 5 days) were similar in all azithromycin regimens, with the most clinically significant laboratory abnormalities occurring at a rate of 1-5%.

Laboratory data for patients receiving 30 mg/kg as a single dose were collected in a single-center study. In this trial, absolute neutrophil counts between 500-1500 cells/mm3 were observed in 10 of 64 patients receiving 30 mg/kg once, in 9 of 62 patients receiving 30 mg/kg for 3 days, and in 8 of 63 patients in the comparison group. No patient had an absolute neutrophil count < 500 cells/mm3.

In multiple-dose clinical trials involving approximately 4,700 pediatric patients, not one patient had therapy discontinued because of treatment-related laboratory abnormalities.

Overdose

Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: gastric lavage, symptomatic therapy.

Pregnancy use

Pregnancy

The FDA fetal category is B.

Teratogenic effects. Reproduction studies have been performed on rats and mice when administered orally at doses to moderately toxic maternal concentrations (i.e., 200 mg/kg/day). These daily doses for rats and mice, depending on body surface area, are estimated to be 4 and 2 times the daily dose of 500 mg for adults, respectively. No evidence of fetal harm due to the effects of azithromycin has been found in animal studies. However, adequate and well-controlled studies in pregnant women have not been conducted. Because animal studies do not always predict effects in humans, azithromycin should only be used during pregnancy if absolutely necessary.

Breastfeeding

It has been reported that azithromycin is excreted in small amounts into human breast milk. Caution should be exercised when azithromycin is used in breastfeeding women.

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