Application
Azithromycin finds its use in the fight against respiratory tract infections. Most often used to treat the following diseases:
- pneumonia (pneumonia),
- exacerbation of chronic bronchitis,
- sinusitis,
- acute tonsillitis,
- pharyngitis.
Moreover, azithromycin is used to treat acute middle ear infections, skin and wound infections, Lyme borreliosis, bacterial conjunctivitis, chlamydial urethritis, and for the prevention of mycobacterial infections in immunocompromised patients.
In dogs it is used to treat canine papillomatosis.
Azithromycin
From the digestive system: nausea, vomiting, diarrhea, abdominal pain, loose stools, flatulence, indigestion, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory parameters of liver function, liver failure, liver necrosis (possibly fatal).
Allergic reactions: itching, skin rashes, angioedema, urticaria, photosensitivity, anaphylactic reaction (in rare cases fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the cardiovascular system: palpitations, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.
From the nervous system: dizziness/vertigo, headache, convulsions, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.
From the senses: tinnitus, reversible hearing impairment up to deafness (when taking high doses for a long time), impaired perception of taste and smell.
From the circulatory and lymphatic systems: thrombocytopenia, neutropenia, eosinophilia.
From the musculoskeletal system: arthralgia.
From the genitourinary system: interstitial nephritis, acute renal failure.
Other: vaginitis, candidiasis.
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Mechanism of action
Macrolide antibiotics interfere with the process of protein synthesis by binding to the 50S subunit of bacterial ribosomes. With such a connection, translocation is blocked, that is, the shift of peptidyl t-RNA from the acceptor site to the donor site. This leads to premature interruption of protein biosynthesis and, consequently, to a bacteriostatic effect.
Azithromycin is slightly less effective against gram-positive than against gram-negative bacteria.
A feature of azithromycin is its long residence time in affected tissues, such as the neck, throat, and respiratory tract. And, at the same time, it is slowly metabolized. That is why azithromycin should be taken by the patient for only three days , and the effect lasts up to 4 days due to its slow metabolism. This feature reduces the negative impact on the gastrointestinal tract.
The disadvantage is that the substance remains in the body for too long in low concentrations. This point contributes to the development of resistance, since protein synthesis is no longer inhibited and the substance is still effective (insufficient concentration).
Side effects and contraindications
- Common side effects (less than 10% of patients): gastrointestinal disorders such as anorexia, nausea, vomiting, diarrhea, soft stools, abdominal pain, abdominal cramps, indigestion and constipation.
- Rare side effects (less than 1% of patients): flatulence, taste disturbances, fungal infections, vaginal thrush, allergic reactions such as skin rashes, itching and urticaria, nervousness, dizziness, drowsiness, headaches, paresthesia and fatigue.
- Very rare side effects (less than 0.1% of patients): colic, seizures, hyperactivity, aggression, malaise, general weakness, anxiety, rage, low blood pressure, palpitations, arrhythmias, severe persistent diarrhea, photosensitivity reactions (skin reactions to sunlight), joint pain, discoloration of the tongue. Serious allergic reactions are very rare.
Azithromycin therapy may lead to an increase in transaminases.
Azithromycin is contraindicated in severe liver failure . Another important contraindication is allergic reactions to azithromycin or other macrolide antibiotics.
Cardiovascular risk and azithromycin
An American study found that taking azithromycin for five days slightly increased the risk of cardiac death. Additional cardiovascular death was reported in 1:21,000 patients, especially in people who had a history of cardiovascular disease.
A further large Danish population-based cohort study, which was conducted in patients under 65 years of age, showed that there was no increased risk of mortality. So treatment with azithromycin in young people with cardiovascular disease is not associated with an increase in cardiovascular risk.
Azithromycin
Azithromycin Azithromycinum (genus Azithromycini)
9-Deoxo-9a-aza-9a-methyl-9a-homoerythromycin A (and as dihydrate)
C38H72N2O1283905-01-5
White crystalline powder.
Pharmacological action: broad spectrum antibacterial.
It binds to the 50S subunit of ribosomes, inhibits peptide translocase at the translation stage and suppresses protein biosynthesis, slowing down the growth and reproduction of bacteria; at high concentrations, a bactericidal effect is possible.
The spectrum of action is wide and includes gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, streptococci of groups C, F, G, Streptococcus viridans), except for those resistant to erythromycin, and gram-negative (Haemophilus influenzae, Moraxella catarrhalis, Bordet ella pertussis , Bordetella parapertussis, Campylobacter jejuni, Legionella pneumophila, Neisseria gonorrhoeae, Gardnerella vaginalis) microorganisms, anaerobes (Bacteroides bivius, Peptostreptococcus spp., Peptococcus, Clostridium perfringens), chlamydia (Chlamydia trachomatis, Chlamydia pneumoniae), mycobacteria (Mycobacter ia avium complex), mycoplasma (Mycoplasma pneumoniae), ureaplasma (Ureaplasma urealyticum), spirochetes (Treponema pallidum, Borrelia burgdorferi).
Stable in an acidic environment, lipophilic, when taken orally, it is quickly absorbed from the gastrointestinal tract. After a single oral dose of 500 mg, bioavailability is 37% (first pass effect), Cmax (0.4 mg/l) is created in 2–3 hours, apparent volume of distribution is 31.1 l/kg, protein binding is inversely proportional concentration in the blood is 7–50%, T1/2 is 68 hours. A stable plasma level is achieved after 5–7 days. Easily passes histohematic barriers and enters tissues. It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria. Penetrates through cell membranes (effective against infections caused by intracellular pathogens). Concentrations in tissues and cells are 10–50 times higher than in plasma, and at the site of infection they are 24–34% higher than in healthy tissues. High levels (antibacterial) remain in tissues for 5–7 days after the last injection. Food intake significantly changes the pharmacokinetics (depending on the dosage form): capsules - Cmax decreases (by 52%) and AUC (by 43%); suspension - increases Cmax (by 46%) and AUC (by 14%); tablets - Cmax increases (by 31%), AUC does not change. In the liver it is demethylated, losing activity. Plasma clearance - 630 ml/min. 50% is excreted unchanged in bile, 6% in urine. In elderly men (65–85 years), the pharmacokinetic parameters do not change; in women, Cmax increases (by 30–50%), in children aged 1–5 years, Cmax, T1/2, and AUC decrease.
For oral administration: infections of the upper (streptococcal pharyngitis/tonsillitis) and lower (bacterial bronchitis, interstitial and alveolar pneumonia, exacerbation of chronic bronchitis) respiratory tract, ENT organs (otitis media, laryngitis and sinusitis), genitourinary system (urethritis and cervicitis) , skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses), chronic stage of erythema migrans (Lyme disease), diseases of the stomach and duodenum associated with Helicobacter pylori.
For infusions: severe infections caused by sensitive strains of microorganisms: community-acquired pneumonia, infectious and inflammatory diseases of the pelvic organs.
Hypersensitivity (including to other macrolides), severe impairment of liver and/or kidney function, age up to 16 years (infusion), up to 12 years with body weight less than 45 kg (capsules, tablets), up to 6 months (suspension for ingestion).
Impaired liver and/or kidney function, arrhythmia or predisposition to arrhythmia and prolongation of the QT interval.
During pregnancy, it is possible if the expected effect of therapy exceeds the potential risk to the fetus.
FDA category of effect on the fetus is B.
Breastfeeding should be stopped during treatment.
From the nervous system and sensory organs: dizziness, vertigo, headache, paresthesia, agitation, fatigue, drowsiness; rarely - tinnitus, reversible hearing loss up to deafness (when taken in high doses for a long time); in children - headache (during treatment of otitis media), hyperkinesia, nervousness, anxiety, sleep disturbance, conjunctivitis.
From the cardiovascular system and blood (hematopoiesis, hemostasis): chest pain, palpitations.
From the gastrointestinal tract: nausea, vomiting, diarrhea, flatulence, abdominal pain, increased ALT and AST activity, bilirubin levels, cholestasis, jaundice; rarely - constipation, discoloration of the tongue, pseudomembranous colitis, pancreatitis, liver necrosis, liver failure (possibly fatal); in children - loss of appetite, gastritis, candidomycosis of the oral mucosa.
From the genitourinary system: vaginal candidiasis, nephritis.
Allergic reactions: rash, itching, urticaria; rarely - angioedema, anaphylactic shock.
Other: photosensitivity, eosinophilia, transient neutrophilia; with intravenous administration (optional) - bronchospasm, pain and inflammation at the injection site.
Antacids, ethanol, and food slow down and reduce absorption (azithromycin should be taken 1 hour before or 2 hours after taking antacids and food). Tetracycline and chloramphenicol enhance the effectiveness of azithromycin, while lincosamides weaken it. When used in therapeutic doses, azithromycin has a weak effect on the pharmacokinetics of atorvastatin, carbamazepine, cetirizine, didanosine, efavirenz, fluconazole, indinavir sulfate, midazolam, rifabutin, sildenafil, theophylline (iv and orally), triazolam, co-trimoxazole, zidovudine. Efavirenz and fluconazole have little effect on the pharmacokinetics of azithromycin. Nelfinavir significantly increases the Cmax and AUC of azithromycin (when taken together, strict monitoring is necessary with regard to side effects of azithromycin such as impaired liver function and hearing impairment). It is necessary to conduct careful monitoring while taking azithromycin with digoxin (possible increase in the concentration of digoxin in the blood), with ergot alkaloids (possible manifestation of their toxic effect - vasospasm, dysesthesia), with cyclosporine and phenytoin (monitoring of their concentration in the blood is necessary). If it is necessary to take it together with warfarin, it is recommended to carefully monitor the PT (there may be an increase in PT and the incidence of hemorrhages). Pharmaceutically incompatible with heparin.
Symptoms: nausea, vomiting, diarrhea, temporary hearing loss.
Treatment: gastric lavage (if taken orally), symptomatic therapy.
Inside, intravenously.
After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under medical supervision.
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Azithromycin recipe in Latin
A prescription for azithromycin in Latin is written depending on its dosage form and according to generally accepted rules for writing a prescription in Latin. Azithromycin is available in the following forms:
Capsules (250 mg) – more details about the recipe for capsules in Latin.
Rp.: Azithromycini 250 mg Dtd N 6 in caps. S. Orally, 1 capsule 2 times a day.
Tablets (125, 500 mg) – more details about the recipe for tablets in Latin.
Rp.: Azithromycini 500 mg Dtd N 3 in tab. S. Orally, 1 tablet 1 time per day.
Syrup (100 or 200 mg/5ml) – syrup recipe in Latin.
Rp.: Sir. Azithromycini 200/5 mg DS Orally, 1 tablespoon 2 times a day.
500 mg bottles – bottle recipe in Latin and powder recipe in Latin.
Rp.: Pulv. Azithromycini 500 mg Dtd N 3 S. Intramuscularly 500 mg 1 time per day.
