Instructions for Sumamed (Azithromycin)
Active ingredients Sumamed:
Azithromycin
Release form:
Pills
Composition Sumamed:
Active ingredient: Azithromycin (Azithromycinum) Active ingredient concentration (mg): 125
Pharmacological effect Sumamed:
Bacteriostatic of the macrolide-azalide group. possesses a wide spectrum of antimicrobial action. the mechanism of action of azithromycin is associated with the suppression of protein synthesis of the microbial cell. binding to the 50s-subunit of the ribosome, inhibits peptide translocase at the stage of translation and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. in high concentrations it has a bactericidal effect; has activity against a number of gram-positive, gram-negative, anaerobes, intracellular and other microorganisms; microorganisms may initially be resistant to action or may acquire resistance to it; scale of microorganism sensitivity to azithromycin (mic, mg / l) microorganisms mic (mg / l) sensitive resistant staphylococcus ≤1> 2streptococcus a, b, c, g ≤0.25> 0.5streptococcus pneumonia ≤0.25> 0.
Sumamed (Azithromycin) has a broad spectrum of antimicrobial action against various infectious
5haemophilus influenzae ≤0.12> 4moraxella catarrhalis ≤0.5> 0.5neisseria gonorrhoeae ≤0.25> 0.5 In most cases, Sumamed is active against aerobic gram-positive bacteria: staphylococcus aureus (methicillin-sensitive strains), streptococcus pneumoniae; 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 .; other microorganisms: chlamydia trachomatis, chlamydia pneumoniae, chlamydia psittaci, mycoplasma pneumoniae, mycoplasma hominis, borrelia burgdorferi. microorganisms capable of developing resistance to azithromycin: gram-positive aerobes - streptococcus pneumoniae (penicillin-resistant strains). initially resistant microorganisms: gram-positive aerobes - enterococcus faecalis, staphylococci (methicillin-resistant strains of staphylococcus exhibit a very high degree of resistance to macrolides); gram-positive bacteria resistant to erythromycin; anaerobes - bacteroides fragilis.
Pharmacokinetics Sumamed:
After oral administration, azithromycin is well absorbed and rapidly distributed in the body. After a single dose of 500 mg, bioavailability is 37% due to the effect of the first passage through the liver. Cmax in blood plasma is achieved after 2-3 hours and is 0.4 mg / L. Distribution Protein binding is inversely proportional to the concentration in blood plasma and is 7-50%. The apparent Vd is 31.1 l / kg. Penetrates through cell membranes (effective for 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 penetrates histohematogenous barriers and enters tissues. Concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection - 24-34% higher than in healthy tissues. Metabolism In the liver, it is demethylated, losing activity. Excretion of T1 / 2 is very long - 35-50 hours. T1 / 2 from tissues is much larger. The therapeutic concentration of azithromycin lasts up to 5-7 days after taking the last dose. Azithromycin is excreted mainly unchanged - 50% through the intestines, 6% by the kidneys.
Indications Sumamed:
Infectious and inflammatory diseases caused by microorganisms sensitive
incl.
bronchitis
pneumonia
infections of the skin and soft tissues
otitis media
sinusitis
pharyngitis
tonsillitis
gonorrheal and non-gonorrheal urethritis and
or cervicitis
Lyme disease (borreliosis).
Contraindications Sumamed:
Hypersensitivity to azithromycin and other macrolide.
Precautions
The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C.
Application during pregnancy and lactation
During pregnancy and during breastfeeding, the use of the drug is possible only if the expected potential benefit of therapy to the mother outweighs the potential risk to the fetus and child.If necessary, the use of the drug during lactation, breastfeeding should be suspended.
Method of administration and dosage Sumamed:
Set individually, taking into account the nosological form, the severity of the course of the disease and the sensitivity of the pathogen. For adults inside - 0.25-1 g 1 time / day; children - 5-10 mg / kg 1 time / day. Duration of admission is 2-5 days.
Side effects Sumamed:
From the digestive system: nausea, vomiting, flatulence, diarrhea, abdominal pain, a transient increase in the activity of liver enzymes; rarely - cholestatic jaundice. Allergic reactions: rarely - skin rash, angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Dermatological reactions: rarely - photosensitization. From the side of the central nervous system: dizziness, headache; rarely - drowsiness, weakness. On the part of the hematopoietic system: rarely - leukopenia, neutropenia, thrombocytopenia. On the part of the cardiovascular system: rarely - chest pain. On the part of the genitourinary system: vaginitis; rarely - candidiasis, nephritis, increased residual urea nitrogen; Other: rarely - hyperglycemia, arthralgia.
Overdose Sumamed:
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea. Treatment: symptomatic therapy.
Interaction with other drugs
Antacids Antacids do not affect the bioavailability of azithromycin, but reduce the Cmax in the blood by 30%, therefore Sumamed should be taken at least 1 hour before or 2 hours after taking these drugs and food. volunteers azithromycin with cetirizine (20 mg) did not lead to pharmacokinetic interaction and a significant change in the QT interval. Didanosine (dideoxyinosine) Simultaneous use of azithromycin (1200 mg / day) and didanosine (400 mg / day) in 6 HIV-infected patients did not reveal any pharmacokinetic changes indicators of didanosine compared with the placebo group. Digoxin (substrates of P-glycoprotein) Simultaneous use of macrolide, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to an increase in the concentration of the substrate P-glycoprotein in the blood serum. Thus, with the 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. Zidovudine Simultaneous use of azithromycin (single dose of 1000 mg and repeated administration of 1200 mg or 600 mg) has a slight effect on pharmacokinetics, incl. excretion by the kidneys 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.
Azithromycin weakly interacts with isoenzymes of the cytochrome P450 system. Not found, that azithromycin is involved in a pharmacokinetic interaction similar to that of erythromycin and other macrolides.
Azithromycin is not an inhibitor and inducer of isoenzymes of the cytochrome P450 system. Ergot alkaloids Taking into account the theoretical possibility of ergotism, the simultaneous use of azithromycin with derivatives of ergot alkaloids is not recommended. Pharmacokinetic studies have been carried out on the simultaneous use of azithromycin and drugs whose metabolism4 of the system occurs with the participation of cytoplasm O2. atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in plasma concentrations of atorvastatin (based on the analysis of inhibition of MMC-CoA reductase). It was reported about the potentiation of the anticoagulant effect after the simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, consideration should be given to the need for frequent monitoring of prothrombin time when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives). Cyclosporine In a pharmacokinetic study with healthy volunteers who were taken orally for 3 days azithromycin (500 mg / day once), and then cyclosporine (10 mg / kg / day once), a significant increase in Cmax in blood plasma and AUC0-5 of cyclosporine was revealed. Caution should be exercised with the simultaneous use of these drugs. If necessary, the simultaneous use of these drugs, the concentration of cyclosporine in the blood plasma should be monitored and the dose adjusted accordingly. Efavirenz The 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 of azithromycin did not change with the simultaneous use of fluconazole, however, a decrease in the Cmax of azithromycin (by 18%) was observed, which had no clinical significance. Indinavir Simultaneous use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir ( 800 mg 3 times / day for 5 days). Methylprednisolone Azithromycin does not significantly affect the pharmacokinetics of methylprednisolone. Nelfinavir
Simultaneous administration of azithromycin (1200 mg) and nelfinavir (750 mg 3 times / day) causes an increase in Css of azithromycin in blood plasma. No clinically significant side effects were observed and dose adjustment of azithromycin when used simultaneously with nelfinavir is not required. Rifabutin The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood plasma. With the simultaneous use of azithromycin and rifabutin, neutropenia was sometimes observed. Despite the fact that neutropenia was associated with the use of rifabutin, a causal relationship between the use of a combination of azithromycin and rifabutin and neutropenia has not been established. Sildenafil When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg / day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite. Terfenadine In pharmacokinetic studies, no evidence of an interaction between azithromycin and terfenadine was obtained. Isolated cases were reported where the possibility of such an interaction could not be completely ruled out, but there was no concrete evidence that such an interaction took place. It was found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval. Theophylline No interaction has been identified between azithromycin and theophylline. Triazolam / midazolam There were no significant changes in pharmacokinetic parameters with the simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses. Serum azithromycin concentrations were consistent with those found in other studies.
special instructions Sumamed:
If you miss one dose of the drug, the missed dose should be taken as early as possible, and the subsequent ones should be taken at intervals of 24 hours. The drug Sumamed should be taken at least 1 hour before or 2 hours after taking antacids. The drug Sumamed should be taken. use with caution in patients with mild and moderate hepatic dysfunction due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency. In the presence of symptoms of liver dysfunction, such as rapidly increasing asthenia, jaundice, dark urine, a tendency to bleeding, hepatic encephalopathy, therapy with Sumamed should be discontinued and a study of the functional state of the liver should be carried out. dose adjustment is not required, therapy with Sumamed should be carried out with caution under the control of the state of renal function.
As with the use of other antibacterial drugs, during therapy with Sumamed, patients should be regularly examined for the presence of refractory microorganisms and signs of the development of superinfections, incl. fungal The drug Sumamed should not be used for longer courses than indicated in the instructions, because The pharmacokinetic properties of azithromycin make it possible to recommend a short and simple dosing regimen. There is no data on a possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but due to the development of ergotism with the simultaneous use of macrolides with derivatives of ergotamine and dihydroergotamine, this combination is not recommended. With prolonged use of Sumamed, the development of pseudomembranous colitis caused by Clostridium difficile is possible, both in the form of mild diarrhea and severe colitis. With the development of diarrhea while taking the drug
Sumamed, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. Do not use drugs that inhibit intestinal motility. azithromycin, lengthening of cardiac repolarization and QT interval was observed, increasing the risk of developing cardiac arrhythmias, incl. arrhythmias of the pirouette type. Care should be taken when using Sumamed in patients with the presence of proarrhythmogenic factors (especially in elderly patients), incl. with congenital or acquired lengthening of the QT interval; in patients
