Sumatrolide Solution Tablets, 250 mg 6 pcs

Pharmacotherapeutic group:

Azalid antibiotic.

ATC code:J01FA10

Pharmacological properties

Pharmacodynamics

Azithromycin is a macrolide antibiotic of the azalide group. Reversibly binding to BOE-subunit of ribosomes of bacterial cells disrupts translocation of growing polypeptide chain from aminoacyl site to 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, Streptococcus group A, B, C, G; 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 resistant and azithromycin.

Pharmacokinetics

After oral administration bioavailability is 37%, maximum blood plasma concentration (C max) is reached after 2-3 hours, volume of distribution is 31 l/kg. Binding to plasma proteins is inversely proportional to the blood concentration and is 12-52%. It penetrates through cell membranes (effective in 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 tissues. 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 tissues and has a long half-life of 2-4 days. The therapeutic concentration of azithromycin is maintained for up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged – 50% by the intestine, 12% by the kidneys. It is demethylated in the liver, losing activity. In patients with renal insufficiency (creatinine clearance (CK) less than 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).

Pharmacological effect

Pharmacotherapeutic group:

azalide antibiotic.

ATX code:J01FA10

Pharmacological properties

Pharmacodynamics

Azithromycin is a macrolide antibiotic of the azalide group. By reversibly binding to the BOE ribosomal subunit of bacterial cells, it disrupts the translocation of the growing polypeptide chain from the aminoacyl region to the peptidyl region, which leads to the suppression of protein synthesis in bacterial cells.

Sensitive: aerobic gram-positive microorganisms – Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive),

Streptococcus pyogenes, Streptococcus groups A, B, C, G; 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.

Pharmacokinetics

After oral administration, bioavailability is 37%, the maximum concentration in blood plasma (Cmax) is created after 2-3 hours, the volume of distribution is 31 l/kg. Plasma protein binding is inversely proportional to blood concentration and ranges from 12 to 52%. Penetrates through cell membranes (effective against infections caused by intracellular pathogens). Transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria.

Easily passes through histohematic barriers and enters tissues. The concentration in tissues and cells is 50 times higher than in blood plasma, and at the site of infection it is 24-34% higher than in healthy tissues. It is slowly eliminated from tissues and has a long half-life of 2-4 days. The therapeutic concentration of azithromycin lasts up to 5-7 days after taking the last dose. Azithromycin is excreted mainly unchanged – 50% by the intestines, 12% by the kidneys. In the liver it is demethylated, losing activity. In patients with renal failure (creatinine clearance (CC) less than 10 ml/min), the half-life of azithromycin increases by 33%.

Special instructions

If you miss one dose of the drug, the missed dose should be taken as early as possible, and subsequent doses should be taken at intervals of 24 hours. For pharyngitis and tonsillitis caused by Streptococcus pyogenes, the antibiotics of choice are penicillins. The effectiveness of azithromycin for the prevention of rheumatic fever is unknown.

Use with caution in patients with hepatic impairment (Child-Pugh class A) due to the possibility of developing fulminant hepatitis and severe liver failure in such patients. If there are symptoms of liver dysfunction (rapidly increasing asthenia, jaundice, darkening of urine, tendency to bleeding, hepatic encephalopathy), azithromycin therapy should be discontinued and a study of the functional state of the liver should be performed. In case of renal failure (creatinine clearance more than 40 ml/min), the use of azithromycin should be carried out 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 long-term use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile is possible. 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 discontinue treatment and use ion exchange resins (colesteramine, colestipol); in severe cases, replacement of loss of fluid, electrolytes and protein, administration of vancomycin, bacitracin or metronidazole is indicated.

Do not use medications that inhibit intestinal motility.
Since QT interval prolongation is possible in patients receiving macrolides, including azithromycin, when using azithromycin, caution should be exercised in patients with known risk factors for QT interval prolongation: advanced age, electrolyte imbalance (hypokalemia, hypomagnesemia), congenital long QT interval syndrome, heart disease (heart failure, myocardial infarction, bradycardia), concomitant taking medications that can prolong the QT interval (including class IA and III antiarrhythmic drugs, tricyclic and tetracyclic antidepressants, antipsychotics, fluoroquinolones). When using azithromycin, myasthenic syndrome or exacerbation of myasthenia may develop.

Impact on the ability to drive vehicles and machinery

In the event of adverse reactions from the nervous system, patients are advised to refrain from driving a car or other machinery, and also to exercise caution when engaging in activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Azithromycin

Composition

Composition per 1 tablet:

active substance:

azithromycin dihydrate 265.3 mg, equivalent to azithromycin 250.0 mg

excipients: 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.

Pregnancy

The use of the drug during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

Contraindications

Hypersensitivity to azithromycin, other macrolides, components of the drug, simultaneous use with ergot derivatives, severe liver failure (class B and C on the Child-Pugh scale). Severe renal failure (creatinine clearance less than 40 ml/min). Children up to 6 months.

With caution
Long Q-T interval syndrome, chronic renal failure (creatinine clearance more than 40 ml/min), liver failure (class A on the Child-Pugh scale), myasthenia gravis, concomitant use with terfenadine, warfarin, digoxin, drugs that prolong the Q-T interval.

Side Effects

From the hematopoietic organs: lymphocytopenia, eosinophilia, leukopenia, thrombocytopenia, transient neutropenia, hemolytic anemia.

From the nervous system: dizziness, vertigo, drowsiness, headache, convulsions, paresthesia, hypoesthesia, asthenia, insomnia, hyperactivity, aggressiveness, restlessness, anxiety, nervousness.

From the senses: hearing impairment, deafness, ringing in the ears, distortion of taste or smell, decreased visual acuity.

From the cardiovascular system, palpitations, decreased blood pressure, arrhythmia (including ventricular tachycardia, torsade de pointes), prolongation of the QT interval.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain or abdominal cramps, loose stools, flatulence, indigestion, gastritis, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, hepatitis, cholestatic jaundice, impaired liver function tests, liver necrosis and liver failure (including death), pancreatitis, fulminant hepatitis.

From the skin: itching and rash, angioedema, urticaria, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactic reactions.

From the musculoskeletal system: arthralgia.

From the genitourinary system: vaginitis, interstitial nephritis, acute renal failure.

Laboratory indicators: increased concentrations of bilirubin, urea, creatinine, potassium ions in the blood serum, decreased concentrations of bicarbonates in the blood serum.

Other: candidiasis, chest pain, peripheral edema, fainting, 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.

The possibility of inhibition of the CYP3A4 isoenzyme by azithromycin should be taken into account with the simultaneous use of cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism occurs with the participation of this isoenzyme.

When used simultaneously with cyclosporine, the concentration of cyclosporine in the blood should be monitored.

When used simultaneously with indirect anticoagulants, the frequency of bleeding may increase; prothrombin time and international normalized ratio (IHO) should be monitored.

When used simultaneously with digoxin, the concentration in the blood of the latter may increase, so the concentration of digoxin in the blood should be monitored.

When used simultaneously with ergotamine, ergotism may develop; simultaneous use is not recommended. Caution should be exercised when co-administering terfenadine and azithromycin, as concomitant use of terfenadine and macrolides has been found to cause arrhythmia and prolongation of the QT interval. Based on this, the above complications cannot be excluded when taking azithromycin and terfenadine together.

When used simultaneously with neofinavir, it is possible to increase the frequency of adverse reactions of azithromycin (decreased hearing, increased activity of liver 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.

Overdose

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

Treatment: taking activated carbon, maintaining vital body functions.

Storage conditions

In a place protected from light at a temperature not exceeding 25°C.

Keep out of the reach of children.

Shelf life

3 years. Do not use after expiration date.

Manufacturer

Ozon, Russia