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Active ingredients
Azithromycin
Release form
Pills
Composition
Active ingredient: Azithromycin (Azithromycin) Active ingredient concentration: 500 mg
Pharmacological effect
Bacteriostatic antibiotic macrolide-azalide group. Possesses a wide range of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. By binding to the 50S subunit of the ribosome, it inhibits peptide translocation at the translation stage and inhibits protein synthesis, slowing the growth and reproduction of bacteria. It has a bactericidal effect in high concentrations. It has activity against a number of gram-positive, gram-negative, anaerobes, intracellular and other microorganisms. Microorganisms may initially be resistant to the action of the antibiotic or may become resistant to it. Azithromycin (MIC, mg / l) Microorganisms MIC (mg / l) Sensitive Sustainable Staphylococcus ≤1> 2Streptococcus A, B, C, G ≤0.25> 0.5Streptococcus pneumonia ≤0.25> 0.5Haemophilus influenzae ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5eleee, ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5eleee, ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5eleee, ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5eleee, ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5eleee, ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5eleee, ≤0.12> 4Moraxella catarrhalis ≤0.5> 0.5 lexee, za0ee30 ≤0.5e, which is ≤0.12 cases, the drug Sumamed is active against aerobic gram-positive bacteria: Staphylococcus aureus (methicillin-sensitive strains), Streptococcus pneumoniae (penicillin-sensitive strains), Streptococcus pyogenes; aerobic gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae; anaerobic bacteria: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp .; of other microorganisms; - Enterococcus faecalis, Staphylococci (methicillin-resistant strains of staphylococcus show a very high degree of resistance to macrolides); gram-positive bacteria resistant to erythromycin; anaerobes - Bacteroides fragilis.
Pharmacokinetics
AbsorptionAfter oral administration, azithromycin is well absorbed and quickly distributed in the body. After a single dose of 500 mg, the bioavailability is 37% due to the effect of the first passage through the liver. Cmax in plasma is reached in 2–3 hours and is 0.4 mg / l. Distribution Protein binding is inversely proportional to plasma concentration and is 7–50%. The apparent Vd is 31.1 l / kg. It penetrates cell membranes (effective for infections caused by intracellular pathogens).Transported by phagocytes to the site of infection, where it is released in the presence of bacteria. It easily penetrates through histohematogenous barriers and enters the tissues. The concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection is 24-34% more than in healthy tissues. Metabolism Demethylates in the liver, losing activity. Excretion of T1 / 2 is very long - 35-50 h T1 / 2 of tissue is much larger. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is excreted mainly unchanged - 50% through the intestines, 6% by the kidneys.
Indications
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug: - infections of the upper respiratory tract and ear (bacterial pharyngitis, tonsillitis, sinusitis, otitis media); - infections of the lower respiratory tract (bacterial bronchitis, interstitial and alveolar pneumonia, exacerbation of chronic bronchitis) ; - infections of the skin and soft tissues (chronic migrating erythema - initial stage, Lyme disease, erysipelas, impetigo, secondary dermatosis); - sexually transmitted infections (urethritis, vitsit); - diseases of stomach and duodenal ulcers associated with Helicobacter pylori.
Contraindications
- severe abnormal liver and kidney function; - hypersensitivity to azithromycin and other components of the drug; - hypersensitivity to antibiotics of the macrolide group. With caution, you should prescribe the drug during pregnancy and lactation, for disorders of the liver and kidneys, patients with impaired or susceptible to arrhythmias and prolongation of the QT interval.
Precautionary measures
Sumamed should be used with caution in patients with mild to moderate hepatic impairment due to the possibility of the development of fulminant hepatitis and severe hepatic insufficiency. If there are symptoms of abnormal liver function, such as rapidly increasing asthenia, jaundice, dark urine, bleeding tendency, hepatic encephalopathy, treatment with Sumamed should be stopped and a study of the functional state of the liver should be carried out.
Use during pregnancy and lactation
During pregnancy and during breastfeeding, the use of the drug is possible only if the expected potential benefit of therapy for the mother exceeds the potential risk to the fetus and child. If the drug needs to be used during lactation, breastfeeding should be suspended. WHO recommends azithromycin as the drug of choice for treatment of chlamydial infection in pregnant women.
Dosage and administration
The drug is administered orally 1 time / day. Capsules and suspension are taken at least 1 hour before or 2 hours after a meal. The bioavailability of the drug in the form of pills does not depend on food intake. Children aged 6 months and older are recommended to prescribe the drug in the form of a suspension for oral administration or 125 mg pills. In infections of the upper and lower respiratory tract, skin and soft tissues (with the exception of chronic migratory erythema) for adults, the drug is prescribed in a dose of 500 mg 1 time / day for 3 days, a course dose of 1.5 g. Children are prescribed at the rate of 10 mg / kg of body weight 1 time / day for 3 days, a course dose of 30 mg / kg .In chronic erythema migrans reparative administered 1 time / day for 5 days: Day 1 - 1 g (2 pills at 500 mg.) followed by 2 to 5 days - 500 mg; course dose - 3 g. Children are prescribed on the first day at a dose of 20 mg / kg body weight and then from 2 to 5 days - daily at a dose of 10 mg / kg body weight, course dose - 60 mg / kg. In case of stomach and duodenal ulcers intestines associated with Helicobacter pylori are prescribed 1 g (2 tab. 500 mg) per day for 3 days in combination with an antisecretory agent and other drugs. In sexually transmitted infections, for the treatment of uncomplicated urethritis / cervicitis, the drug is prescribed in a dose of 1 g once; For the treatment of complicated long-term urethritis / cervicitis caused by Chlamydia trachomatis, 1 g is prescribed 3 times with an interval of 7 days (1, 7, 14 days), the course dose is 3 g.
Side effects
Rarely (≤1%). From the digestive system: melena, cholestatic jaundice, flatulence, nausea, vomiting, diarrhea, constipation, decreased appetite, gastritis, reversible moderate increase in liver enzymes. From the urinary system: nephritis. From the sexual systems: vaginal candidiasis. From the cardiovascular system: feeling of heartbeat, pain in the chest. From the side of the central nervous system and peripheral nervous system: dizziness, headache, vertigo, drowsiness, increased fatigue; in children - headache (in the treatment of otitis media),hyperkinesia, anxiety, neurosis, sleep disorders. Allergic reactions: skin rashes, angioedema, urticaria, conjunctivitis. Dermatological reactions: photosensitization, pruritus. From laboratory indicators: in some cases - neutrophilia, eosinophilia (the changed indicators return to normal through 3 weeks after cessation of treatment).
Overdose
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea. Treatment: symptomatic therapy.
Interaction with other drugs
Antacid drugsAntacid drugs do not affect the bioavailability of azithromycin, but reduce Cmax in the blood by 30%, so Sumamed should be taken at least 1 hour before or 2 hours after taking these drugs and food. Cetirizine is a simultaneous use for 5 days in healthy Azithromycin volunteers with cetirizine (20 mg) did not lead to pharmacokinetic interactions and a significant change in the QT interval. Didanosine (didpoxyinosine) Simultaneous use of azithromycin (1200 mg / day) and didanosine (400 mg / day) in 6 HIV-infected pa no changes in the pharmacokinetic parameters of didanosine compared with the placebo group. Digoxin (P-glycoprotein substrates) Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates, such as digoxin, leads to an increase in serum P-glycoprotein substrate concentration. Thus, with simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum. kidney excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear. Azitromycin weakly interacts with cytochrome P450 isoenzymes. It was not revealed that azithromycin is involved in the pharmacokinetic interaction similar to erythromycin and other macrolides.Azithromycin is not an inhibitor and inducer of the cytochrome P450 system. atorvastatin (10 mg daily) and azithromycin (500 mg daily) n Atorvastatin caused changes in plasma concentrations (based inhibition assay MMC-CoA reductase). However, in the post-registration period, there were separate reports of cases of rhabdomyolysis in patients receiving azithromycin and statins at the same time. Carbamazepine In pharmacokinetic studies involving healthy volunteers, no significant effect was found on the concentration of carbamazepine and its active metabolite in the blood plasma of patients receiving azithromycin simultaneously. studies of the effect of a single dose of cimetidine on azithromycin pharmacokinetics revealed no changes in pharmacoqui YETİK azithromycin, cimetidine, subject to application 2 hours before azitromitsina.Antikoagulyanty indirect (coumarin derivatives) The pharmacokinetic studies azithromycin had no effect on the anticoagulant effect of a single dose of 15 mg warfarin received healthy volunteers. The potentiation of the anticoagulant effect has been reported after the simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Despite the fact that a causal relationship has not been established, consideration should be given to the need for frequent monitoring of prothrombin time when azithromycin is used in patients who receive oral anticoagulants of indirect action (coumarin derivatives). Cyclosporine In a pharmacokinetic study involving healthy volunteers who took 3 days azithromycin (500 mg / day once), and then cyclosporine (10 mg / kg / day once), there was a significant increase in plasma Cmax and AUC0-5 cyclosporine on. Caution should be exercised with the simultaneous use of these drugs.If necessary, the simultaneous use of these drugs, should be monitored concentrations of cyclosporine in the blood plasma and adjust the dose accordingly. Efavirenz Simultaneous use of azithromycin (600 mg / day once) and efavirenz (400 mg / day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction. Fluconazole Simultaneous use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1 / 2 azithromycin did not change with simultaneous use of fluconazole, however, a decrease in azithromycin Cmax (by 18%) was observed, which had no clinical significance. 800 mg 3 times / day for 5 days). Methylprednisolone Azitromycin does not significantly affect the pharmacokinetics of methylprednisolone. Nelfinavir Simultaneous use of azithromycin (1200 mg) and nelfinavir ( about 750 mg 3 times / day) causes an increase Css azithromycin in serum. No clinically significant side effects were observed, and dose adjustment of azithromycin when used simultaneously with nelfinavir is not required. Rifabutin Simultaneous use of azithromycin and rifabutin does not affect the concentration of each of the drugs in the blood serum. With simultaneous use of azithromycin and rifabutin, neutropenia has sometimes been observed. Despite the fact that neutropenia was associated with the use of rifabutin, a causal relationship between the use of azithromycin and rifabutin and neutropenia has not been established. Sildenafil When used in healthy volunteers, no evidence of the effect of azithromycin (500 mg / day for 3 days) on AUC and Cmax of sildenafil or its major circulating metabolite. Terfenadine In pharmacokinetic studies, no evidence of interaction between azithromycin and terfenadine was obtained. It was reported on isolated cases where the possibility of such an interaction could not be completely excluded, but there was not a single concrete proof that such an interaction took place.It was found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and lengthening of the QT interval. trimethoprim / sulfamethoxazole with azithromycin showed no significant effect on Cmax, the total exposure Theological or renal excretion of trimethoprim or sulfamethoxazole. Serum azithromycin concentrations were consistent with those found in other studies.
special instructions
In case of missing a single dose of the drug - the missed dose should be taken as soon as possible, and the next - with interruptions of 24 hours. Sumamed should be taken at least 1 hour before or 2 hours after taking antacids. Mild and moderate severity (CC> 40 ml / min) Sumamed drug therapy should be carried out with caution under the control of the state of kidney function. As with other antibacterial drugs, patients with Sumamed drug therapy should regularly examine patients for the presence of refractory microorganisms and signs of the development of superinfections, incl. Fungal. Sumamed should not be used for longer courses than specified in the instructions, because The pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosing regimen. There is no data on the possible interaction between azithromycin and ergotamine and dihydroergotamine derivatives, but due to the development of ergotism with the simultaneous use of macrolides with ergotamine and dihydroergotamine derivatives, this combination is not recommended. development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea and severe colitis. With the development of antibiotic-associated diarrhea while taking the drug Sumamed, as well as 2 months after the end of therapy, pseudomembranous colitis should be excluded. When treated with macrolides, incl. azithromycin, prolonged cardiac repolarization and QT interval were observed, increasing the risk of developing cardiac arrhythmias, including arrhythmias of the pirouette type. Care should be taken when using Sumamed in patients with pro-arrhythmogenic factors (especially in elderly patients), includingwith congenital or acquired prolongation of the QT interval; in patients taking class I antiarrhythmic drugs (quinidine, procainamide), III (dofetilide, amiodarone, and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), antidepressants (citalopram), anti-depressants (moxifloxacin, anti-depressants) electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmias or severe heart failure. The use of Sumamed may trigger the development of myasthenic syndrome or cause exacerbation of myasthenia. Effect on the ability to drive motor vehicles and control mechanisms. In the development of undesirable effects on the nervous system and the organ of vision, caution should be exercised when performing actions that require an increased concentration of attention and quickness of psychomotor reactions.