Active substanceDoxycyclineDoxycycline
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  • Dosage form: & nbsppills
    Composition:

    Active substance: doxycycline monohydrate 100.0 mg in terms of doxycycline;

    Auxiliary substances: microcrystalline cellulose - 45.0 mg, saccharin - 10.0 mg, giprolose (low substituted) - 18.75 mg, hypromellose - 3.75 mg, silicon dioxide colloid (anhydrous) -0.625 mg, magnesium stearate - 2, 0 mg, lactose monohydrate - up to 250.0 mg.

    Description:Round, biconvex tablets, from light yellow or gray-yellow to brown with interspersed, engraved "173" (tablet code) on one side and risk to the other.
    Pharmacotherapeutic group:Antibiotic, tetracycline
    ATX: & nbsp

    J.01.A.A.02   Doxycycline

    Pharmacodynamics:

    Antibiotic of a broad spectrum of action from the group of tetracyclines. It acts bacteriostatically, suppresses protein synthesis in the microbial cell by interacting with the 30S subunit of ribosomes. It is active against many Gram-positive and Gram-negative microorganisms: Streptococcus spp., Treponema spp., Staphylococcus spp., Klebsiella spp., Enterobacter spp. (including E. aerugenes), Neisseria gonorrhoeae, N eis seria meningitidis, Haemophilus influenzae, Chlamydia spp., Mycoplasma spp., Ureaplasma urealyticum, Lis ter ia monocytogenes, Rickettsia spp., Typhus exanthematicus, Escherichia coli, Shigella spp., Campylobacter fetus, Vibrio cholerae, Yersinia spp. (including Yersinia pestis), Brucella spp., Francisella tularensis, Bacillus anthracis, Bartonella bacilliformis, Pasteurella multocida, Borrelia recurrentis, Clostridium spp. (Besides Clostridium difficilé), Actinomyces spp., Fusobacterium fusiforme, Calymmatobacterium granulomatosis, Propionibacterium acnes, some protozoa (Entamoeba spp., Plasmodium falciparum).

    how rule, not current on Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.

    The possibility of acquired resistance to doxycycline in a number of pathogens, which is often cross-over within the group (ie, strains resistant to doxycycline, will simultaneously be resistant to the entire group of tetracyclines) should be taken into account.

    Pharmacokinetics:

    Suction

    Absorption is fast and high (about 100%). Eating slightly affects the absorption of the drug.

    The maximum level of doxycycline in the blood plasma (2.6-3 μg / ml) is achieved 2 hours after taking 200 mg, after 24 hours the concentration of active substance in the blood plasma is reduced to 1.5 μg / ml.

    After taking 200 mg on the first day of treatment and 100 mg per day on subsequent days, the concentration of doxycycline in the blood plasma is 1.5-3 μg / ml.

    Distribution

    Doxycycline reversibly binds to plasma proteins (80-90%), penetrates well into organs and tissues, badly into spinal fluid (10-20% of plasma level), but the concentration of doxycycline in the cerebrospinal fluid increases with inflammation of the spinal cord.

    The volume of distribution is 1.58 l / kg. 30-45 minutes after ingestion doxycycline is found in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate gland, eye tissues, in pleural and ascitic fluids, bile, synovial exudate, exudate of maxillary and frontal sinuses, in fluid of gingival sulci.

    With normal liver function, the level of the drug in the bile is 5-10 times higher than in the plasma.

    In saliva, 5-27% of the concentration of doxycycline in the blood plasma is determined.

    Doxycycline penetrates the placental barrier, in small quantities is secreted into breast milk.

    Accumulates in dentin and bone tissue.

    Metabolism

    An insignificant part of the doxycycline is metabolized.

    Excretion

    Half-life after a single oral intake is 16-18 hours, after taking repeated doses - 22-23 hours.

    Approximately 40% of the drug taken is excreted by the kidneys and 20 - 40% is excreted through the intestines in the form of inactive forms (chelates).

    Pharmacokinetics in special clinical cases

    The half-life of the drug in patients with impaired renal function does not change, because its excretion through the intestine increases.

    Hemodialysis and peritoneal dialysis do not affect the concentration of doxycycline in the blood plasma.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

    - respiratory tract infections, including pharyngitis, acute bronchitis, exacerbation of chronic obstructive pulmonary disease, tracheitis, bronchopneumonia, lobar pneumonia, community-acquired pneumonia, lung abscess, pleural empyema;

    - infections of the ENT organs, including otitis media, sinusitis, tonsillitis;

    - infections of the genitourinary system: cystitis, pyelonephritis, bacterial prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, acute orchidpididitis; endometritis, endocervicitis and salpingo-ophio-rhytitis in combination therapy; including sexually transmitted infections: urogenital chlamydia, syphilis in patients with penicillin intolerance, uncomplicated gonorrhea (as an alternative therapy), inguinal granuloma, venereal lymphogranuloma;

    - infections of the gastrointestinal tract and bile ducts: (cholera, iersiniosis, cholecystitis, cholangitis, gastroenterocolitis, bacillary and amoebic dysentery, diarrhea of ​​"travelers");

    - skin and soft tissue infections (including wound infections after an animal bite), severe acne (as part of combination therapy);

    - Other diseases: yaws, legionellosis, chlamydia of various localizations (including prostatitis and proctitis), rickettsiosis, fever, spotted fever of the Rocky Mountains, typhus (including swelling, tick-borne recurrent), Lyme disease (I st - erythema migrans), tularemia, plague, actinomycosis, malaria; infectious diseases of the eyes, as part of combination therapy - trachoma; leptospirosis, psittacosis, ornithosis, anthrax (including pulmonary form), bartonellosis, granulocyte erlichiosis; whooping cough, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;

    - Prevention of postoperative purulent complications: malaria caused by Plasmodium falciparum, during short travel (less than 4 months) in the area where common strains resistant to chloroquine and / or pyrimethamine-sulfadoxine.

    Contraindications:

    - Hypersensitivity to tetracyclines

    - pregnancy

    - lactation

    - age up to 8 years

    - Severe dysfunction of the liver and / or kidneys

    - porphyria

    Pregnancy and lactation:Doxycycline penetrates the hematoplacental barrier. Tetracyclines have an adverse effect on the fetus (slowing osteogenesis) and on the formation of tooth enamel (irreversible color change, hypoplasia). In view of this, as well as an increased risk of liver damage in the mother, tetracyclines are not used in pregnancy, except when the drug is the only way to treat or prevent especially dangerous and severe infections (spotted fever of the rocky mountains, inhalation exposure Bacillus anthracis and etc.). Before prescribing doxycycline to women of childbearing age, pregnancy should be excluded. Doxycycline penetrates into breast milk. Due to adverse effects on the fetus, doxycycline, like other tetracyclines, are not used during breastfeeding. In the event that the appointment of tetracyclines is necessary, breastfeeding is discontinued.

    Dosing and Administration:

    Usually the duration of treatment is 5-10 days. The tablets are dissolved in a small amount of water (about 20 ml) to obtain suspensions, can also be swallowed whole, divided into parts or chewed, washed down with water. Preferably eat.

    Take pills sitting or standing, which reduces the likelihood of developing esophagitis and ulcers of the esophagus. The drug should not be taken immediately before bedtime.

    Adults and children older than 8 years with a body weight of more than 50 kg prescribe 200 mg in 1-2 doses on the first day of treatment, then 100 mg daily. In cases of severe infections, Unidox is administered at a dose of 200 mg daily throughout the treatment.

    Children 8-12 years old with a body weight of less than 50 kg the average daily dose is 4 mg / kg on the first day, then - 2 mg / kg per day (in 1-2 divided doses). In cases of severe infection, Unidox is administered at a dose of 4 mg / kg daily throughout the treatment.

    Features of dosing in certain diseases

    With infection caused by S.pyogenes Unidox take at least 10 days. With uncomplicated gonorrhea (with the exception of anorectal infections in men):

    Adults prescribe 100 mg twice a day until complete recovery (on average for 7 days), or within one day appoint 600 mg - 300 mg in 2 divided doses (second reception 1 hour after the first).

    When primary syphilis is prescribed for 100 mg twice a day for 14 days, with secondary syphilis - 100 mg twice a day for 28 days. In uncomplicated urogenital infections caused by Chlamydia trachomatis, cervicitis, non-gonococcal urethritis caused by Ureaplasma urealiticum, 100 mg are administered twice a day for 7 days.

    With acne, 100 mg / day are prescribed, and the course of treatment is 6-12 weeks.

    Malaria (prevention): 100 mg once a day 1-2 days before the trip, then daily during the trip and within 4 weeks after the return; children older than 8 years of 2 mg / kg 1 time per day.

    The duration of prevention should not exceed 4 months. Diarrhea "travelers" (prevention) - 200 mg on the first day of the trip (for 1 dose or 100 mg twice a day), then 100 mg once a day during the stay in the region (no more than 3 weeks).

    Treatment of leptospirosis - 100 mg orally 2 times a day for 7 days; prophylaxis of leptospirosis - 200 mg once a week during a stay in a dysfunctional area and 200 mg at the end of a trip.

    To prevent infections, medical abortion is prescribed 100 mg 1 hour before and 200 mg after the intervention.

    Maximum daily doses for adults - up to 300 mg / day or 600 mg / day for 5 days with severe gonococcal infection. For children older than 8 years with a body weight of more than 50 kg - up to 200 mg, for children 8 - 12 years with a body weight of less than 50 kg - 4 mg / kg daily for the entire treatment period.

    In the presence of renal (creatinine clearance less than 60 ml / min) and / or liver failure, a daily dose of doxycycline is required, as this gradually accumulates in the body (the risk of hepatotoxic action).

    Side effects:

    From the gastrointestinal tract:

    anorexia, nausea, vomiting, dysphagia, diarrhea, anal itching, esophagitis, ulcer of the esophagus, dark staining of the tongue. With prolonged therapy, a deficiency of B vitamins can be observed in connection with the suppression of vitamin B-producing bacteria growth in the normal intestinal microflora.

    Allergic reactions:

    exacerbation of systemic lupus erythematosus, a syndrome similar to serum sickness, erythema multiforme, lowering of arterial pressure, tachycardia,Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms (DRESS syndrome).

    From the skin:

    urticaria, photosensitization, angioedema, anaphylactic reactions, maculopapular and erythematous rash, exfoliative dermatitis, Schonlein purpura - Genocha, photoionicholysis.

    From the cardiovascular system:

    pericarditis.

    From the side of the liver:

    liver damage, sometimes associated with pancreatitis (with long-term drug intake or in patients with renal or hepatic insufficiency), cholestasis.

    From the side of the kidneys:

    an increase in residual urea nitrogen due to the anti-anabolic effect of the drug, aggravation of azotemia in patients with renal insufficiency. The use of products containing citric acid on the background of doxycycline may cause symptoms similar to Fanconi's syndrome: albuminuria, glucosuria, hypophosphatemia, hypokalemia and renal

    tubular acidosis.

    On the part of the hematopoiesis system:

    hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, decreased prothrombin activity.

    From the nervous system:

    benign increase in intracranial pressure (anorexia, vomiting, headache, tinnitus, tremor, edema of the optic nerve), vestibular disorders (dizziness or instability), hallucinations, blurred vision, scotoma, double vision.

    From the side of the thyroid gland:

    in patients who received antibiotics for a long time from the group of tetracyclines, a reversible dark brown staining of the thyroid tissue is possible, in most cases not accompanied by a violation of its function.
    From the teeth and bones:

    doxycycline slows down osteogenesis, disrupts the normal development of teeth in children (the color of teeth changes irreversibly, and enamel hypoplasia develops).

    From the musculoskeletal system:

    arthralgia, myalgia.

    Other:

    Superinfection: candidiasis, glossitis, staphylococcal enterocolitis, pseudomembranous colitis, anogenital candidiasis, stomatitis, and vaginitis.

    Overdose:

    Symptoms:

    Increased adverse reactions caused by liver damage - vomiting, febrile condition, jaundice, azotemia, increased transaminase levels, increased prothrombin time.

    Treatment:

    Immediately after taking large doses, it is recommended to wash the stomach, drink plenty, if necessary - induce vomiting. Accepted Activated carbon and osmotic laxatives. Hemodialysis and peritoneal dialysis is not recommended due to low efficiency.

    Interaction:

    Antacids containing aluminum, magnesium, calcium, iron preparations, sodium hydrogen carbonate, magnesium-containing laxatives reduce the absorption of doxycycline, so their use should be separated by an interval of 3 hours.

    In connection with the suppression of intoxic microflora by doxycycline, the prothrombin index decreases, which requires correction of the dose of indirect anticoagulants.

    When the combination of doxycilin with bactericidal antibiotics, which violate the synthesis of the cell wall (penicillins, cephalosporins), the effectiveness of the latter is reduced.

    Doxycycline reduces the reliability of contraception and increases the frequency of acyclic bleeding when taking estrogen-containing hormonal contraceptives.

    Ethanol, barbiturates, rifampicin, carbamazepine, phenytoin and other stimulants of microsomal oxidation, accelerating the metabolism of doxycycline, reduce its concentration in the blood plasma.

    Simultaneous use of doxycycline and retinol helps increase intracranial pressure.

    Special instructions:

    There is the possibility of cross-resistance and hypersensitivity with other drugs of the tetracycline series.

    Tetracyclines may increase prothrombin time, the appointment of tetracyclines in patients with coagulopathies should be carefully monitored.

    The anti-anabolic effect of tetracyclines can lead to an increase in the level of residual urea nitrogen in the blood. As a rule, this is not significant for patients with normal renal function. However, in patients with renal insufficiency, an increase in azotemia may occur. The use of tetracyclines in patients with impaired renal function requires medical supervision.

    With prolonged use of the drug requires periodic monitoring of laboratory blood parameters, liver and kidney function.

    In connection with the possible development of photodermatitis, it is necessary to limit insolation during treatment and for 4-5 days after it.

    Prolonged use of the drug can cause dysbacteriosis and as a result - the development of hypovitaminosis (especially B vitamins).

    To prevent dyspeptic phenomena, it is recommended to take the drug while eating.

    Effect on the ability to drive transp. cf. and fur:It is not known how to influence the ability to drive vehicles, machines and mechanisms.

    In the case of dizziness, blurred vision or double vision in the eyes, management of vehicles or mechanisms is not recommended. See Side actions - From the nervous system.

    Form release / dosage:Tablets dispersible 100 mg;
    Packaging:For 10 tablets in a blister of PVC / aluminum foil. 1 blister with instructions for use in a cardboard box.
    Storage conditions:
    At a temperature of 15 to 25 ° C.
    Keep out of the reach of children!
    Shelf life:
    5 years.
    Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013102 / 01
    Date of registration:12.09.2008 / 07.09.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Astellas Farma Europe BVAstellas Farma Europe BV Netherlands
    Manufacturer: & nbsp
    Representation: & nbspASTELLAS PHARMA YUROP BV ASTELLAS PHARMA YUROP BV Netherlands
    Information update date: & nbsp31.03.2017
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