Sumamox tablets 500mg, No. 3

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 (simple acne of moderate severity, erysipelas, impetigo, secondarily infected dermatoses);

• the initial stage of Lyme disease (borreliosis) - erythema migrans (erythema migrans);

• uncomplicated urinary tract infections caused by Chlamidia trachomatis (urethritis, cervicitis).

Inside, 1 time / day, at least 1 hour before or 2 hours after meals.

Adults (including the elderly) and children over 12 years of age weighing over 45 kg.

For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 500 mg (1 tablet) 1 time / day for 3 days (course dose 1.5 g).

The initial stage of Lyme disease: 1 time / day for 5 days: 1st day - 1.0 g (2 tablets), then from 2nd to 5th day - 500 mg each (1 tablet) (course dose 3.0 g)

For uncomplicated urinary tract infections caused by Chlamidia trachomatis (urethritis, cervicitis): 1 g (2 tablets) as a single dose.

For acne: the course dose is 6 g: 500 mg (1 tablet) 1 time / day for 3 days, then 500 mg 1 time per week for 9 weeks.

Prescribing to patients with impaired renal function: For patients with moderate impairment of renal function (CC> 40 ml / min), dose adjustment is not required.

Film-coated tablets of white or almost white color, in the form of a capsule (caplet), with a line on both sides; cross-section - white or almost white core.

1 tab.

azithromycin dihydrate 524 mg,

which corresponds to the content of azithromycin 500 mg

Excipients: corn starch - 250 mg, corn starch for paste - 40 mg, calcium phosphate - 150 mg, talc - 3 mg, magnesium stearate - 2 mg, sodium carboxymethyl starch - 3 mg, croscarmellose sodium - 2 mg.

• Hypersensitivity to azithromycin, other macrolides, to the constituent components of the drug; simultaneous use with ergot derivatives;

• severe hepatic / renal impairment;

• children under 12 years of age.

• With care: long QT interval syndrome, chronic renal failure (CC more than 40 ml / min), simultaneous administration with terfenadine, warfarin, digoxin, drugs that prolong the QT interval.

pharmachologic effect

Azithromycin is a macrolide antibiotic of the azalide group. Reversibly binding to the 50S-subunit of ribosomes of bacterial cells, it disrupts the translocation of the growing polypeptide chain from the aminoacyl site to the peptidyl one, 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; 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. groups A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains) resistant to erythromycin and other macrolides, lincosamides are resistant to azithromycin.Resistant: aerobic gram-positive microorganisms - Enterococcus faecalis, Staphylococcus spp. (methicillin resistant); anaerobes: Bacteroides fragilis group, Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. groups A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains) resistant to erythromycin and other macrolides, lincosamides are resistant to azithromycin.Resistant: aerobic gram-positive microorganisms - Enterococcus faecalis, Staphylococcus spp. (methicillin resistant); anaerobes: Bacteroides fragilis group, Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. groups A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains) resistant to erythromycin and other macrolides, lincosamides are resistant to azithromycin.

Pharmacokinetics

After oral administration, bioavailability is 37%, Cmax in blood plasma is created after 2-3 hours, Vd - 31 l / kg. Plasma protein binding is inversely proportional to blood concentration and amounts to 12-52%. Penetrates through 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. Easily passes through the histohematogenous barriers and enters the 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 T1 / 2 2-4 days. The therapeutic concentration of azithromycin lasts up to 5-7 days after taking the last dose. Azithromycin is excreted mainlyunchanged - 50% by the intestines, 12% by the kidneys. In the liver, it is demethylated, losing activity. In patients with renal insufficiency (creatinine clearance (CC) less than 10 ml / min), T1 / 2 of azithromycin increases by 33%.

Side effect

From the side of hematopoiesis: lymphocytopenia, eosinophilia, leukopenia, thrombocytopenia, transient neutropenia, hemolytic anemia.

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

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

From the side of the cardiovascular system: palpitations, arrhythmia (including ventricular tachycardia, pirouette tachycardia), 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, necrosis liver and liver failure (up to death).

From the musculoskeletal system: arthralgia.

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

Allergic reactions: itching and rash, angioedema, urticaria, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal nscrolysis, anaphylactic reactions.

Laboratory indicators: an increase in the concentration of bilirubin, urea, creatinine, potassium ions in the blood serum, a decrease in the concentration of bicarbonates in the blood serum. Others: candidiasis, chest pain, swelling, fainting, exacerbation of myasthenia gravis.

Application during pregnancy and lactation

The use of the drug during pregnancy is possible only in cases where the intended 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 resolved.

Application for violations of liver function

Contraindicated in severe hepatic impairment.

Application for impaired renal function

Contraindicated in severe renal failure. With care: chronic renal failure (CC more than 40 ml / min).

Application in children

Contraindicated in children under 12 years of age.

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. In case of 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. When using azithromycin, as well as when using other antibiotics, there is a risk of developing superinfection (including fungal). With prolonged use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile is possible. With the development of diarrhea while taking azithromycin, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded.

Influence on the ability to drive vehicles and work with mechanisms

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

Overdose

Symptoms: temporary hearing loss, nausea and vomiting, diarrhea. Treatment: intake of activated carbon, maintenance of vital body functions.

Drug interactions

Antacids reduce the Cmax of azithromycin by 30%, therefore, azithromycin should be taken 1 hour before or 2 hours after taking antacids. With simultaneous use with cyclosporine, the concentration of cyclosporine in the blood should be monitored. With simultaneous use with indirect anticoagulants, the frequency of bleeding may increase, prothrombin time and international normalized ratio (MHO) should be monitored. With simultaneous use with digoxin, an increase in the concentration in the blood of the latter is possible, therefore, the concentration of digoxin in the blood should be monitored. With simultaneous use with ergotamine, ergotism may develop; simultaneous use is not recommended. The simultaneous use of macrolides and theophylline in some cases led to an increase in the concentration of the latter.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 can lead to neutropenia. When taken simultaneously, fluconazole reduces the Cmax of azithromycin by 18%.