Pharmacotherapeutic group: antibiotic azalide
Code ATX: J01FA10
Pharmacological properties
Pharmacodynamics. Azithromycin is a bacteriostatic broad-spectrum antibiotic of the macrolide-azalid group. It has a broad spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with inhibition of microbial cell protein synthesis. Binding to 50S-subunit of ribosome, it inhibits peptide translocase at the translation stage and inhibits protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations it has a bactericidal effect.
It has activity against a number of Gram-positive, Gram-negative, anaerobic, intracellular and other microorganisms.
Microorganisms can be resistant to the antibiotic from the start or they can become resistant to it.
Azithromycin sensitivity scale for microorganisms (Minimum inhibitory concentration (MIC), mg/L):
> 0.5
> 4
> 0.5
Microorganisms | MIC, mg/l /p> | ||
Sensitive . | Sensitive | ||
Staphylococcus | ≤ 1 | > 2 | |
Streptococcus A, B, C, G | ≤ 0.25 /td> | > 0.5 | |
S. pneumoniae | ≤ 0.25 | ||
H. influenzae | ≤ 0.12 | ||
M. catarrhalis | ≤ 0.5 | ||
N. gonorrhoeae | ≤ 0.25 | > 0.5 |
Inmostsensitive microorganisms
- Gram-positive aerobes
Staphylococcus aureus methicillin-sensitive
Streptococcus pneumoniae penicillin-sensitive
Streptococcus pneumoniae./p>
Streptococcus pyogenes
- Gram-negative aerobes.
Haemophilus influenzae
em>Haemophilus parainfluenzae
Legionella pneumophila<
Moraxella catarrhalis
PasteurellaPasteurella multocida
Neisseria gonorrhoeae
- Anaerobes
Clostridium perfringens
Fusobacterium spp.
Prevotella spp.
Porphyriomonas spp.
- Other microorganisms
Chlamydia pneumoniae
Chlamydia psittaci
Mycoplasma pneumoniae</em/em>
Mycoplasma hominis
Borrelia burgdorferi
Gram-positive aerobes
Microorganisms that can develop resistance to azithromycin
Streptococcus pneumoniae penicillin-resistant
Initially resistant microorganisms./strong>
Grampositive aerobes
Enterococcus <emfaecalis
Staphylococci (methicillin-resistant staphylococci have a very high frequency of acquired resistance to macrolides)
Gram-positive bacteria that are resistant to erythromycin.
Anaerobes
Bacteroides fragilis
Pharmacokinetics. Azithromycin is well absorbed and rapidly distributed in the body after oral administration. After a single dose of 500 mg bioavailability is 37% (first pass effect), maximum concentration (0.4 mg/l) in blood is achieved after 2-3 hours, apparent volume of distribution is 31.1 l/kg, binding to proteins is inversely proportional to the blood concentration and is 7-50%. It penetrates through cell membranes (effective in infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes the histohematic barriers and enters the tissues. Concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection it is 24-34% higher than in healthy tissues.
Asithromycin has a very long half-life of 35-50 h. The tissue elimination half-life is much longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged – 50% by the intestine, 6% by the kidneys. In the liver it is demethylated, losing activity.
Indications
Active ingredient
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Weight | 0.011 kg |
---|---|
Shelf life | 3 years. |
Conditions of storage | Store at the temperature not more than 25 ºC. Keep out of reach of children. |
Manufacturer | Pliva Hrvatska d.o.o., Croatia |
Medication form | pills |
Brand | Pliva Hrvatska d.o.o. |
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