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Active ingredients
Azithromycin
Release form
Capsules
Composition
Active ingredient: azithromycin Auxiliary substances: microcrystalline cellulose, sodium lauryl sulfate, magnesium stearate. Base volume: Capsule Concentration of active ingredient (mg): 250 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. binding to the 50s subunit of the ribosome, inhibits peptide translocation at the translational stage and inhibits protein synthesis, slowing the growth and reproduction of bacteria. in high concentrations 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 the action of the antibiotic or may acquire resistance to it. microorganisms mic (mg / l) sensitive resistantstaphylococcus ≤1> 2streptococcus a, b, c, g ≤0.25> 0.5streptococcus pneumonia ≤0.25> 0.5haemophilus influenzae ≤0.12> 4moraxella catarrhalis ≤0.5> 0.5neisseria gonorrhoe usa 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; , 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
After 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 upper respiratory tract (pharyngitis / tonsillitis, sinusitis, otitis media); - lower respiratory infections (acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including caused by atypical pathogens); - diseases of the stomach and duodenum associated with Helicobacter pylori (for powder); - infections of the skin and soft tissues (moderate acne, erysipelas, impetigo, and secondarily infected dermatoses); The first stage of Lyme disease (borreliosis) is erythema migrans (erythema migrans); urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).
Contraindications
- severe violations of the liver and kidneys; - lactation period (breastfeeding); - concomitant use with ergotamine and dihydroergotamine; - hypersensitivity to macrolide antibiotics; - children under 12 years old and body weight less than 45 kg (for capsules and pills 500 mg); children's age up to 3 years (for pills 125 mg). With caution, you should prescribe the drug for moderate violations of the liver and kidneys, patients with disorders or susceptibility to arrhythmias and prolongation of the QT interval, together with terfenadine, warfarin, digoxin.
Precautionary measures
The drug should be stored out of reach of children at a temperature not exceeding 25 ° C.
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 necessary, the use of the drug during lactation breastfeeding should be suspended.
Dosage and administration
The drug is administered orally 1 time / day, at least 1 h before or 2 h after a meal. Tablets are taken without chewing. Adults (including the elderly) and children over 12 years old with a body weight of more than 45 kg are prescribed the drug in the form of pills and capsules. Children 6 months and older should be given the drug in the form of oral suspension, children 3 years and older, the drug can also be prescribed in the form of pills 125 mg. The drug in the form of pills 125 mg is metered according to the body weight of the child, as shown in the table. Body weight Amount of azithromycin (125 mg pills) 18-30 kg 2 pills (250 mg) 31-44 kg 3 pills (375 mg) ≥45kg prescribed doses recommended for adultsWhen infections of the upper respiratory tract, upper and lower respiratory tract, skin and soft tissues (except for chronic erythema migrans) adults and children over 12 years old with a body weight of more than 45 kg, the drug is prescribed at a dose of 500 mg 1 time / day for 3 days, course dose - 1.5 g. Children aged 6 months and one hundred rshe is prescribed at the rate of 10 mg / kg of body weight 1 time / day for 3 days, the course dose is 30 mg / kg. In diseases of the stomach and duodenum associated with Helicobacter pylori, the drug is prescribed in powder form at a dose of 1 g / day for 3 days in combination with antisecretory agents and other drugs. In case of erythema migrans, the drug is prescribed 1 time per day for 5 days. Adults and children over 12 years old with a body weight of more than 45 kg are prescribed on day 1 — 1 g, then from 2 to 5 days — 500 mg each; course dose - 3 g. Children aged 6 months and older are prescribed on the 1st day at a dose of 20 mg / kg of body weight and then from 2 to 5 days - daily at a dose of 10 mg / kg of body weight, course dose - 60 mg / kg. In case of moderately severe acne, the course dose is 6.0 g. Adults and children over 12 years old with a body weight of more than 45 kg are prescribed in a dose of 500 mg 1 time / day for 3 days, then 500 mg 1 time per week for 9 weeks. The first weekly dose should be taken 7 days after taking the first daily dose (the 8th day from the start of treatment), the next 8 weekly doses should be taken at an interval of 7 days. In sexually transmitted infections, for the treatment of uncomplicated urethritis / cervicitis caused by Chlamydia trachomatis, 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),course dose - 3 g. For patients with moderately impaired renal function (CC> 40 ml / min), dose adjustment is not required. The rules for preparing and receiving suspension In a vial containing 17 g of powder, make 12 ml of distilled or boiled water. The volume of the resulting suspension is 23 ml. The shelf life of the prepared suspension is 5 days. Before taking the contents of the vial thoroughly shaken to obtain a homogeneous suspension. Immediately after taking the suspension, the child is allowed to drink a few sips of tea in order to wash off and swallow the remaining amount of suspension in the oral cavity. After use, the syringe is disassembled and washed with running water, dried and stored in a dry place with the preparation. The tablet should be washed down with a sufficient amount of water.
Side effects
Determination of the frequency of adverse reactions: often (> 1/100 and <1/10), sometimes (> 1/1000 and <1/100), rarely (> 1/10 000 and <1/1000), very rarely (<1 / 10 000). From the hematopoietic system: rarely - thrombocytopenia, neutropenia, eosinophilia. From the side of the central nervous system and the peripheral nervous system: sometimes - dizziness / vertigo, headache, drowsiness, convulsions; rarely - paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness. From the senses: rarely - tinnitus, reversible hearing impairment until deafness (when taken in high doses for a long time), impaired taste and smell For the cardiovascular system: rarely - heartbeat, arrhythmia, including ventricular tachycardia, prolongation of the QT interval, bidirectional ventricular tachycardia. On the part of the digestive system: often - nausea, vomiting, diarrhea, abdominal pain and spa snakes; sometimes - diarrhea, flatulence, indigestion, anorexia; rarely - constipation, change in the color of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in the values of laboratory parameters of liver function; very rarely - abnormal liver function and liver necrosis (possibly fatal). Allergic reactions: sometimes - itching, skin rashes; rarely - angioedema, urticaria, photosensitivity, anaphylactic reaction (in rare cases with fatal outcome), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the musculoskeletal system: sometimes - arthralgia. From the urinary system: rarely - interstitial nephritis, acute renal failure. Other: rarely - vaginitis, candidiasis.
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 cimetidine when taken in a single dose on azithromycin pharmacokinetics revealed no measurable neny pharmacokinetics of azithromycin provided use of cimetidine for 2 h before azitromitsina.Antikoagulyanty indirect (coumarin derivatives) The pharmacokinetic studies azithromycin had no effect on the anticoagulant effect of warfarin at its reception in a single dose of 15 mg in 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 the simultaneous use of fluconazole,however, a decrease in Cmax of azithromycin (by 18%) was observed, which had no clinical significance. IndinavirAt 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). MethylprednisoloneAzithromycin no significant effect on the pharmacokinetics of methylprednisolone. Nelfinavir Simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times / day) causes an increase in Css of azithromycin in the blood plasma. 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 plasma. 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 early 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. Sumamed should be use 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 discontinued and a functional study of the liver should be performed. If kidney function is impaired in patients with GFR 10-80 ml / min dose adjustment is not required, drug therapy Sumamed should be carried out with caution under the control of the state of kidney function. As with the use of other antibacterial drugs, with drug therapy Sum Honey should regularly examine patients for the presence of non-susceptible organisms and signs of superinfection, including Fungal. The drug Sumamed should not be used for longer courses than indicated 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, clostridial pseudomembranous colitis should be excluded. Do not use drugs that inhibit intestinal peristalsis. When treating 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), including with 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 arrhythmia, or severe heart failure. The use of Sumamed may trigger the development of myasthenic syndrome or cause exacerbation of myasthenia. When used in patients with diabetes mellitus, as well as in patients on a low-calorie diet, it is necessary to take into account that sucrose (0.32 XU / 5 ml) is included in the powder for preparing Sumamed suspension as an auxiliary substance. When driving motor vehicles and controlling mechanisms. If undesirable effects develop on the part of the nervous system and the organ of vision, caution should be exercised when performing actions that require increased concentration and attention. trots of psychomotor reactions.