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 inflammatory diseases caused by microorganisms sensitive to azithromycin:

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

In case of missing one dose of the drug – the missed dose should be taken as soon as possible, and the subsequent ones should be taken 24 hours apart. In pharyngitis and tonsillitis caused by Streptococcus pyogenes, penicillins are the antibiotics of choice. The effectiveness of azithromycin for prevention of rheumatic fever is unknown.

Take with caution in patients with hepatic impairment (Child-Pugh class A) because of the possibility of fulminant hepatitis and severe hepatic failure in such patients. In the presence of symptoms of hepatic impairment (rapidly increasing asthenia, jaundice, darkened urine, susceptibility to bleeding, hepatic encephalopathy) azithromycin therapy should be discontinued and liver function tests should be performed. In patients with renal insufficiency (CK more than 40 ml/min) azithromycin should be used under control of renal function.

When using azithromycin as well as when using other antibiotics there is a risk of superinfection (including fungal).

In prolonged use of azithromycin pseudomembranous colitis caused by Clostridium difficile may develop. If diarrhea develops during treatment with azithromycin, as well as 2 months after therapy termination, clostridial pseudomembranous colitis should be excluded. In mild cases it is enough to cancel the treatment and use ion exchange resins (colesteramine, colestipol), in severe cases compensation of fluid, electrolytes and protein loss, administration of vancomycin, bacitracin or metronidazole is indicated.

The use of drugs inhibiting intestinal peristalsis should be avoided.
Since Q-T interval prolongation is possible in patients receiving macrolides, including azithromycin, caution should be exercised when using azithromycin in patients with known risk factors for Q-T interval prolongation: Elderly age, electrolyte imbalance (hypokalemia, hypomagnesemia), congenital Q-T interval prolongation syndrome, heart disease (heart failure, myocardial infarction, bradycardia), concurrent administration of drugs that can prolong Q-T interval (including antiarrhythmic drugs of classes IA and III, tricyclic and tetracyclic antidepressants, neuroleptics, fluoroquinolones). When using azithromycin it is possible to develop myasthenic syndrome or exacerbation of myasthenia gravis.

In case of adverse reactions from the nervous system, patients are advised to refrain from driving and operating machinery, and to exercise caution when engaged in activities requiring high concentration and quick psychomotor reactions.

Contraindications

Side effects

Overdose

Pregnancy use

Similarities