Sumatrolide Solution pills Dispersible pills, 6pcs

Composition

Composition for 1 tablet: Active ingredient:  azithromycin dihydrate 265.3 mg, based on azithromycin 250.0 mgsupport substances: microcrystalline cellulose 225.9 mg, crospovidone 60.3 mg, pregelatinized starch 67.0 mg, blackcurrant flavor 5.0 mg, magnesium stearate 6.0 mg, sodium saccharinate 15.0 mg, vanillin 1.5 mg, colloidal silicon dioxide 24.0 mg

Pharmacological action

Azithromycin is a macrolide antibiotic of the azalide group. Reversibly binding to the BoE subunit of bacterial ribosomes disrupts translocation of the growing polypeptide chain from the aminoacyl site to the peptidyl site, which leads to suppression of protein synthesis in bacterial cells. Sensitive: aerobic gram – positive microorganisms-Staphylococcus aureus (methicillin – sensitive), Streptococcus pneumoniae (penicillin – sensitive), Streptococcus pyogenes, Group A, B, C, G Streptococcus; aerobic gram-negative microorganisms-Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae; anaerobic microorganisms-Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp. ; others-Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi. Moderately sensitive or insensitive: aerobic gram-positive microorganisms-Streptococcus pneumoniae (moderately sensitive or resistant to penicillin). Resistant: aerobic gram-positive microorganisms-Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant); Anaerobes: Bacteroides fragilis group. Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. group A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains), resistant to erythromycin and other macrolides, lincosamides are also resistant to azithromycin.

Pharmacokineticsafter oral use, the bioavailability is 37%, the maximum concentration in blood plasma (cmax) is created in 2-3 hours, the volume of distribution is 31 l/kg. Binding to plasma proteins is inversely proportional to the concentration in the blood and is 12-52%. Penetrates cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria. It easily passes through histohematic barriers and enters the tissues. The concentration in tissues and cells is 50 times higher than in blood plasma, and in the focus of infection-24-34% higher than in healthy tissues. It is slowly excreted from the tissues and has a long half-life of 2-4 days. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged-50% by the intestines,12% by the kidneys. In the liver, it is demethylated, losing its activity. In patients with renal insufficiency (creatinine clearance < 10 ml/min), the half-life of azithromycin is increased by 33%.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:

• Infections of the upper respiratory tract and ENT organs (pharyngitis, tonsillitis, sinusitis, otitis media);
• Lower respiratory tract infections (acute bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia, including those caused by atypical pathogens);
• Infections of the skin and soft tissues (acne vulgaris of moderate severity, erysipelas, impetigo, secondary infected dermatoses);
• The initial stage of Lyme disease (borreliosis) is erythema migrans.
• Uncomplicated urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications

Hypersensitivity to azithromycin, other macrolides, components of the drug, simultaneous use with ergot derivatives, severe hepatic insufficiency (class B and C on the Child-Pugh scale). Severe renal insufficiency (creatinine clearance less than 40 ml / min). Children under 6 months of age. With caution, prolonged Q-T syndrome, chronic renal failure (creatinine clearance greater than 40 ml / min), hepatic insufficiency (Child-Pugh class A), myasthenia gravis, concomitant use with terfenadine, warfarin, digoxin, drugs that prolong the Q-T interval.

Side effects

Hematopoietic disorders: lymphocytopenia, eosinophilia, leukopenia, thrombocytopenia, transient neutropenia, hemolytic anemia. Nervous system disorders: dizziness, vertigo, drowsiness, headache, convulsions, paresthesia, hyposthesia, asthenia, insomnia, hyperactivity, aggressiveness, restlessness, anxiety, nervousness. From the sensory organs: hearing impairment, deafness, ringing in the ears, perversion of taste or smell, decreased visual acuity. From the cardiovascular system, palpitations, decreased blood pressure, arrhythmia (including ventricular tachycardia, pirouette tachycardia), prolongation of the Q-T interval. From the digestive system: nausea, vomiting, diarrhea, abdominal pain or abdominal cramps, loose stools, flatulence, digestive disorders, gastritis, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, hepatitis, cholestatic jaundice, impaired liver function tests, liver necrosis and liver failure (up to fatal outcome), pancreatitis, fulminant hepatitis. Skin disorders: pruritus and rash, angioedema, urticaria, photosensitization, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactic reactions. Musculoskeletal system disorders: arthralgia. From the genitourinary system: vaginitis, interstitial nephritis, acute renal failure. Laboratory parameters: increased serum concentrations of bilirubin, urea, creatinine, potassium ions, decreased serum concentrations of bicarbonates. Others: candidiasis, chest pain, peripheral edema, syncope, exacerbation of myasthenia gravis, malaise, hyperglycemia.

Interaction

Antacids reduce the maximum concentration of azithromycin by 30%, so azithromycin should be taken 1 hour before or 2 hours after taking antacids. Consideration should be given to the possibility of inhibition of the CYP3A4 isoenzyme azithromycin with concomitant use of cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs that are metabolized with the participation of this isoenzyme. When used concomitantly with cyclosporine, the concentration of cyclosporine in the blood should be monitored. When used concomitantly with indirect anticoagulants, the frequency of bleeding may increase, prothrombin time and international normalized ratio (MHO) should be monitored. When used concomitantly with digoxin, it is possible to increase the concentration in the blood of the latter, so the concentration of digoxin in the blood should be monitored. When used concomitantly with ergotamine, ergotism may develop; concomitant use is not recommended. Caution should be exercised when using terfenadine and azithromycin together, since it has been found that simultaneous use of terfenadine and macrolides causes arrhythmia and prolongation of the Q-T interval. Based on this, it is impossible to exclude the above-mentioned complications when taking azithromycin and terfenadine together. When used concomitantly with neofinavir, the frequency of azithromycin side effects may increase (hearing loss, increased activity of “hepatic” transaminases). Azithromycin increases the content of zidovudine triphosphate (the active metabolite of zidovudine) in mononuclear cells, the clinical significance of this phenomenon is unknown. Concomitant use with rifabutin may lead to neutropenia. Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim/sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin, methylprednisolone in the blood when used simultaneously.

How to take, course of use and dosage

Inside, once a day, at least 1 hour before or 2 hours after a meal. Adults (including the elderly) and children over 12 years of age with a body weight over 45 kg. For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 500 mg (2 tablets) 1 time a day for 3 days (course dose of 1.5 g)The initial stage of Lyme disease: once a day for 5 days: Day 1-1.0 g (4 tablets), then from day 2 to day 5-500 mg (2 tablets) (course dose 3.0 g)For uncomplicated urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): 1 g (4 tablets) once. For acne: the course dose is 6 g: 500 mg (2 tablets) 1 time a day for 3 days, then 500 mg 1 time a week for 9 weeks. Children from 6 months to 12 years old. For infections of the respiratory tract, ENT organs, skin and soft tissues: Based on 10 mg / kg of body weight once a day for 3 days (a course dose of 30 mg / kg). For streptococcal pharyngitis: At the rate of 10-20 mg / kg once a day for 3 days. Initial stage of Lyme disease: On day 1-at a dose of 20 mg/kg of body weight and then from day 2 to 5-daily at a dose of 10 mg/kg of body weight (a course dose of 60 mg/kg). use to patients with impaired renal function: No dose adjustment is necessary for patients with moderate renal impairment (creatinine clearance >40 ml / min). Dispersible tablets can be taken in a variety of ways: the tablet can be swallowed whole, washed down with water or previously, before taking, dissolved in water. Tablets should be dissolved in at least 50 ml of water. Before taking it, the resulting suspension should be thoroughly mixed.

Overdose

Symptoms: temporary hearing loss, nausea and vomiting, diarrhea. Treatment: taking activated charcoal, maintaining vital body functions.

Special instructions

If one dose of the drug is missed, the missed dose should be taken as early as possible, and the subsequent ones should be taken at intervals of 24 hours. For pharyngitis and tonsillitis caused by Streptococcus pyogenes, the antibiotics of choice are penicillins. The efficacy of azithromycin for the prevention of rheumatic fever is unknown. Use with caution in patients with hepatic insufficiency (Child-Pugh class A) due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency in such patients. In the presence of symptoms of impaired liver function (rapidly increasing asthenia, jaundice, darkening of the urine, tendency to bleeding, hepatic encephalopathy), azithromycin therapy should be discontinued and a study of the functional state of the liver should be conducted. In patients with renal insufficiency (creatinine clearance greater than 40 ml/min), azithromycin should be administered under the control of renal function. When using azithromycin, as well as when using other antibiotics, there is a risk of developing superinfection (including fungal). With prolonged use of azithromycin, pseudomembranous colitis caused by Clostridium difficile may develop. If diarrhea develops while taking azithromycin, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. In mild cases, it is sufficient to cancel treatment and use ion-exchange resins (colesteramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole is indicated. Do not use medications that inhibit intestinal motility. Since prolongation of the Q-T interval is possible in patients treated with macrolides, including azithromycin, when using azithromycin, caution should be exercised in patients with known risk factors for prolongation of the Q-T interval: elderly age, electrolyte imbalance (hypokalemia, hypomagnesemia), congenital prolongation of the Q-T interval, heart disease (heart failure, myocardial infarction, bradycardia), simultaneous use of drugs that can prolong the Q-T interval (including antiarrhythmic drugs of classes IA and III, tricyclic and tetracyclic antidepressants, neuroleptics, fluoroquinolones). When using azithromycin, myasthenic syndrome may develop or exacerbate myasthenia gravis.

Influence on the ability to drive vehicles and mechanisms

In case of adverse reactions from the nervous system, patients are advised to refrain from driving a car and other mechanisms, as well as to exercise caution when engaging in activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

In a dark place at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date.

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

tablets soluble