SUMAMECIN
Active material: Azithromycin
When ATH: J01FA10
CCF: Macrolide antibiotics – azalid
ICD-10 codes (testimony): A31.0, A38, A46, A48.1, A56.0, A56.1, A56.4, A69.2, B96.0, H66, J01, J03, J15, J15.7, J20, J32, J35.0, J42, K25, K26, L01, L30.3, N30, N34, N72
When CSF: 06.07.01
Manufacturer: OP OBOLENSKOE CJSC (Russia)
Pharmaceutical form, composition and packaging
Capsules gelatin, size №1, с крышечкой синего цвета и голубым корпусом; contents of capsules – White granules.
| 1 caps. | |
| azithromycin (in the form of dihydrate) | 250 mg |
Excipients: calcium stearate, low molecular weight polyvinyl Medical, microcrystalline cellulose.
6 PC. – packings Valium planimetric (1) – packs.
10 PC. – packings Valium planimetric (1) – packs.
Pharmacological action
Macrolide antibiotics. Является представителем подгруппы азалидов. When you create inflammation in high concentrations has a bactericidal effect.
It has a broad spectrum of action. Active against gram-positive bacteria: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, стрептококки групп CF и G, Staphylococcus aureus, Staphylococcus viridans; Gram negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; Some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; and also Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pale, Borrelia burgdorferi.
Азитромицин неактивен в отношении грамположительных бактерий, erythromycin resistant.
Pharmacokinetics
Absorption
Азитромицин быстро всасывается из ЖКТ, due to its stability in an acidic medium and lipophilicity. Once inside 500 mg Cmax azithromycin plasma levels achieved after 2.5-2.96 h and is 0.4 mg / l. Bioavailability is 37%.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (в частности в предстательную железу), in skin and soft tissue. High concentrations in tissues (in 10-50 times higher, than in blood plasma) and a long T1/2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrated in a low pH environment, environmental lysosomes. It, in turn, It defines a large apparent Vd (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important for elimination of intracellular pathogens. Proved, that phagocytes deliver azithromycin to the localization of infection, where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher, than in healthy tissues (on average 24-34%) and correlate with the degree of inflammatory edema. Despite the high concentration in phagocytes, Azithromycin has no significant effect on their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatments.
Metabolism and excretion
Demetiliruetsa in the liver, образующиеся метаболиты не активны.
Derivation of azithromycin in plasma passes 2 Phase: T1/2 is 14-20 hours, ranging from 8 to 24 hours after dosing and 41 no – in the range of 24 to 72 no, allowing you to use the drug 1 time / day.
Testimony
Infectious-inflammatory diseases, caused by susceptible to malaria infections:
- Infections of the upper respiratory tract and ENT (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);
- Scarlet fever;
- Infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
- Infections of the skin and soft tissues (mug, impetigo, secondarily infected dermatitis);
- Urogenitalynogo tract infections (uncomplicated urethritis and / or cervicitis);
- Lyme disease (ʙorrelioz), for the treatment of early stage (Erythema migrans);
— заболевание желудка и двенадцатиперстной кишки, associated with Helicobacter pylori (in a combination therapy).
Dosage regimen
The drug is taken orally, for 1 hours before or after 2 hours after meals 1 time / day.
Adults at infections of the upper and lower respiratory tract administered at a dose of 500 mg / day 1 Reception for 3 days (kursovaya dose – 1.5 g).
At infections of skin and soft tissue – 1000 мг/сут в первый день за 1 reception, hereinafter 500 mg/day every day with 2 by 5 day (kursovaya dose – 3 g).
At острых инфекциях мочеполовых органов (uncomplicated urethritis or cervicitis) – single 1 g.
At Lyme disease (ʙorrelioz) for the treatment of stage I (Erythema migrans) – 1 г в первый день и 500 mg daily with 2 by 5 day (kursovaya dose – 3 g).
At gastric ulcer and duodenal ulcer, associated with Helicobacter pylori – 1 g / day for 3 days in a combination therapy of H. pylori.
Babies appoint at 10 mg / kg 1 times / day for 3 days or the first day of – 10 mg / kg, then 4 day – by 5-10 mg / kg / day for 3 days (kursovaya dose – 30 mg / kg).
At treatment of erythema migrans in children the drug is prescribed on the basis of 20 мг/кг в первый день и по 10 mg / kg at a 2 by 5 day.
Side effect
From the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%), dyspepsia, flatulence, vomiting, ground, cholestatic jaundice, increase in liver transaminases (≤ 1%); children – constipation, anorexia, gastritis (≤ 1%).
Cardio-vascular system: heartbeat, chest pain (≤ 1%).
CNS: dizziness, headache, drowsiness; children – headache (for the treatment of otitis media), giperkineziya, anxiety, neurosis, sleep disturbance (≤ 1%).
From the urinary system: jade (≤ 1%).
On the part of the reproductive system: vaginal candidiasis.
Allergic reactions: rash, angioedema; children – itch, hives.
Other: fatigue, photosensitivity; children – conjunctivitis, itch, hives.
Contraindications
- Liver and / or kidney failure;
- Lactation;
- Children up to age 12 Months;
- Hypersensitivity (incl. to other macrolides);
FROM caution prescribed medication during pregnancy, arrhythmia (ventricular arrhythmias and QT prolongation), а также детям с выраженными нарушениями функции печени или почек.
Pregnancy and lactation
Препарат можно назначать при беременности только в том случае, когда польза от его применения значительно превышает риск, существующий всегда при использовании любого препарата в течение беременности.
При необходимости назначения препарата Сумамецин в период лактации грудное вскармливание на время лечения следует приостанавить.
Cautions
Observe break 2 ч при одновременном применении с антацидами.
После отмены препарата реакции гиперчувствительности у некоторых пациентов могут сохраняться, which require a specific therapy under the supervision of a physician.
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea.
Drug Interactions
Antacids (aluminum and magnesium-), ethanol and food slows down and reduces the absorption of azithromycin.
The joint appointment of warfarin and azithromycin (at conventional doses) changes in prothrombin time is not revealed, However, considering, что при взаимодействии макролидов и варфарина возможно усиление антикоагуляционного эффекта, Patients should be closely monitored prothrombin time.
При одновременном применении с дигоксином отмечается повышение его концентрации в плазме.
При одновременном применении с эрготамином и дигидроэрготамином наблюдается усиление их токсического действия (vasospasm, dysesthesia).
На фоне одновременного применения Сумамецина отмечается снижение клиренса и увеличение фармакологического действия триазолама.
Азитромицин за счет ингибирования микросомального окисления в гепатоцитах замедляет выведение и повышает концентрацию в плазме и токсичность циклосерина, anticoagulants, methylprednisolone, Felodipine, and drugs, undergoing microsomal oxidation (Carbamazepine, terfenadine, cyclosporine, geksoʙarʙital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemics, Theophylline and other xanthine derivatives).
Linkozaminy weaken the effectiveness of azithromycin, тетрациклин и хлорамфеникол – increase.
Сумамецин фармацевтически несовместим с гепарином.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in a dry, protected from light, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 3 year.
