DORSI [Doxycycline] 100 mg Film-coated tablets
DORSI
instructions for medical use of the medicinal product
Tradename
Dorsi, Dorsi
International non-proprietary name
doxycycline, doxycycline
Composition
Each film-coated tablet contains:
active ingredient: doxycycline 100 mg
excipients: starch, dextrin, microcrystalline cellulose, hypromellose, magnesium stearate, talc
Dosage form
Tablets.
Pharmacotherapeutic group
Pharmacological properties
Pharmacodynamics
Semi-synthetic tetracycline, bacteriostatic broad-spectrum antibiotic. Penetrating into the cell, acts on intracellularly located pathogens. Suppresses the synthesis of proteins in the microbial cell, breaks the connection of transport aminoacyl-RNA with the 30S subunit of the ribosomal membrane.
Gram-positive microorganisms are highly sensitive to it: Staphylococcus spp. (including Staphylococcus aureus, Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae), Clostridium spp., Listeria spp.; Actinomyces israeli; and gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Klebsiella spp., Escherichia coli, Shigella spp., Enterobacter, Salmonella spp., Bordetella pertussis. Bacteroides spp., Treponema spp. (including strains resistant to other antibiotics, such as modern penicillins and cephalosporins). The most sensitive are Haemophilus influenzae (91-96%) and intracellular pathogens.
Doxycycline is active against most pathogens of dangerous infectious diseases : plague (Yersinia spp.), Tularemia (Francisella tularensis), anthrax (Bacillus anthracis), Legionella (Legionella spp.), Brucella (Brucella spp.), Vibrio cholera (Vibrio cholera) , rickettsia (Rickettsia spp.), pathogens of glanders (Actinobacillus mallei), chlamydia (causative agents of ornithosis (Chlamydia psittaci), psittacosis (Rickettsiaformis psittacosi), trachoma (Chlamydia trachomatis;, venereal granuloma (Calymmatobacterium granulomatis), malaria (Plasmodium falciparum) dysentery (Entamoeba histolytica).
He acts on most strains of Proteus, Pseudomonas aeruginosa and fungi.
To a lesser extent than other antibiotics of the tetracycline series, it inhibits the intestinal flora, differs from them in more complete absorption and a longer duration of action. In terms of antibacterial activity, doxycycline is superior to natural tetracyclines. Unlike tetracycline and oxytetracycline, it has a higher therapeutic efficacy, manifested in the treatment of 10 times lower doses, and a longer duration of action. There is cross-resistance to other tetracyclines as well as to penicillins.
Pharmacokinetics
Absorption - fast and high (about 100%). Eating does not significantly affect the degree of absorption. Has a high degree of solubility in lipids and low affinity for the binding of calcium ions (Ca 2+ ). After oral administration of 200 mg, the time to reach maximum plasma concentration is 2.5 hours, the maximum plasma concentration is 2.5 μg / ml, 24 hours after administration - 1.25 μg / ml.
Communication with plasma proteins - 80-93%. It penetrates well into organs and tissues; 30-45 minutes after ingestion, it is found in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate, eye tissues, in pleural and ascitic fluids, bile, synovial exudate, exudate of the maxillary and frontal sinuses, in liquid gingival sulcus. Poorly penetrates into the cerebrospinal fluid (10-20% of the plasma level). Penetrates through the placental barrier, is determined in breast milk. The volume of distribution is 0.7 l / kg.
Metabolized in the liver 30-60%. The half-life is 10-16 hours (mainly 12-14 hours, on average 16.3 hours). With repeated injections, the drug may accumulate. It accumulates in the reticuloendothelial system and bone tissue. In bones and teeth, it forms insoluble complexes with calcium ions (Ca 2+ ). It is excreted in the bile, where it is found in high concentrations. Undergoes enterohepatic recirculation, excreted by the intestines (20-60%); 40% of the dose taken is excreted by the kidneys in 72 hours (of which 20-50% is unchanged), in severe chronic renal failure - only 1-5%.
In patients with impaired renal function or azotemia, an important route of excretion is gastrointestinal secretion.
Indications for use
· infectious and inflammatory diseases caused by susceptible microorganisms: respiratory tract infections (pharyngitis, acute and chronic bronchitis, tracheitis, bronchopneumonia, lobar pneumonia, lung abscess, pleural empyema);
·
infections of ENT organs (otitis media, tonsillitis, sinusitis, etc.);
·
infections of the genitourinary system (cystitis, pyelonephritis, prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, endometritis, endocervicitis, acute orchiepididymitis; gonorrhea);
·
infections of the biliary tract and gastrointestinal tract (cholecystitis, cholangitis, gastroenterocolitis, bacillary dysentery, travelers' diarrhea);
·
skin and soft tissue infections (cellulitis, abscesses, furunculosis, felons, infected burns, wounds, etc.);
·
infectious eye diseases, syphilis, yaws, yersiniosis, legionellosis, rickettsiosis, chlamydia of various localization (including prostatitis and proctitis), Q fever, Rocky Mountain spotted fever, typhus (including typhus, tick-borne, relapsing), Lyme disease ( I stage - erythema migrans ), bacillary and amoebic dysentery, tularemia, cholera, actinomycosis, malaria; as part of combination therapy - leptospirosis, trachoma, psittacosis, ornithosis, granulocytic ehrlichiosis; whooping cough, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;
·
prevention of postoperative purulent complications; malaria caused by Plasmodium falciparum , during short-term travel (less than 4 months) in areas where strains resistant to chloroquine and / or pyrimethamine-sulfadoxine are common;
·
as a first-line drug, it is prescribed to patients under 65 years of age with an exacerbation of chronic bronchitis (including against the background of bronchial asthma) without concomitant diseases (these exacerbations are often caused by Haemophilus influenzae ). Effective in exacerbation of bronchopulmonary infection (usually staphylococcal etiology) in patients with cystic fibrosis, chlamydial arthritis, granulocytic ehrlichiosis. In elderly patients, it is used to treat acute prostatitis and Escherichia urinary infection. coli .
Contraindications
· hypersensitivity to doxycycline, drug components, other tetracyclines;
· lactase deficiency;
· lactose intolerance;
· glucose-galactose malabsorption;
· porphyria;
· severe liver failure;
· leukopenia;
·
children's age up to 12 years (possibility of formation of insoluble complexes with calcium ions (Ca 2+ ) with deposition in the bone skeleton, enamel and dentin of teeth);
·
children aged after 12 years old with body weight up to 45 kg.
Dosage and administration
Inside, without chewing, drinking water.
Adults and children over 12 years of age weighing more than 45 kg. The average daily dose is 200 mg on the first day (divided into 2 doses - 100 mg 2 times a day), then 100 mg / day.
In chronic infections of the urinary system - 200 mg / day throughout the entire period of therapy.
In the treatment of gonorrhea , it is prescribed according to one of the following schemes: acute uncomplicated urethritis - a course dose of 500 mg (1 dose - 300 mg, subsequent 2 - 100 mg with an interval of 6 hours) or 100 mg / day until complete cure (in women) or 100 mg 2 times a day for 7 days (in men); in complicated forms of gonorrhea, the course dose is 800-900 mg, which is divided into 6-7 doses (300 mg - 1 dose, then with an interval of 6 hours for 5-6 subsequent ones).
In the treatment of syphilis - 300 mg / day for at least 10 days.
For uncomplicated infections of the urethra, cervix and rectum caused by Chlamydia trachomatis , 100 mg is prescribed 2 times a day for at least 7 days.
Infections of the male genital organs - 100 mg 2 times a day for 4 weeks. Treatment of malaria resistant to chloroquine - 200 mg / day for 7 days (in combination with schizontocidal drugs - quinine); malaria prophylaxis -100 mg 1 time per day for 1-2 days before the trip, then daily during the trip and within 4 weeks after the return;
Diarrhea "travelers" (prevention) - 200 mg on the first day of the trip (per 1 dose or 100 mg 2 times a day), 100 mg 1 time per day during the entire stay in the region (no more than 3 weeks).
Treatment of leptospirosis - 100 mg orally 2 times a day for 7 days; prevention of leptospirosis - 200 mg once a week during a stay in a disadvantaged area and 200 mg at the end of the trip.
Prevention of infections after medical abortion - 100 mg 1 hour before abortion and 200 mg - 30 minutes after.
With acne - 100 mg / day, course - 6-12 weeks.
The maximum daily dose for adults is up to 300 mg / day or up to 600 mg / day for 5 days in severe gonococcal infections.
In the presence of severe hepatic insufficiency, a decrease in the daily dose of the drug is required, since in this case it gradually accumulates in the body (risk of hepatotoxic action).
Special instructions and precautions
To prevent local irritating action (esophagitis, gastritis, ulceration of the mucous membrane of the gastrointestinal tract), it is recommended to take it during the daytime with plenty of liquid, food. In connection with the possible development of photosensitivity, it is necessary to limit insolation during treatment and for 4-5 days after it. With prolonged use, periodic monitoring of liver function, hematopoietic organs is necessary. It can mask the manifestations of syphilis, and therefore, if mixed infection is possible, monthly serological analysis is necessary for 4 months. All tetracyclines form stable complexes with calcium ions (Ca 2+ ) in any bone-forming tissue. In this regard, taking during the period of tooth development can cause long-term staining of teeth in a yellow-gray-brown color, as well as enamel hypoplasia. Perhaps a false increase in the level of catecholamines in the urine when they are determined by the fluorescent method. When examining a biopsy of the thyroid gland in patients who have been receiving doxycycline for a long time, a dark brown staining of the tissue in micropreparations is possible without disturbing its function.
When using the drug, both against the background of taking it and 2-3 weeks after stopping treatment, diarrhea caused by Clostridium difficile may develop. In mild cases, it is sufficient to cancel treatment and use ion-exchange resins (colestyramine, colestipol), in severe cases, compensation for the loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole is indicated. Do not use drugs that inhibit intestinal motility.
Influence on the ability to drive vehicles and mechanisms
Patients should refrain from all activities that require increased attention.
Use during pregnancy and during breastfeeding
The use of the drug during pregnancy and during breastfeeding is contraindicated. If it is necessary to use the drug during breastfeeding, breastfeeding should be discontinued for the period of treatment.
Interaction with other drugs
Preparations containing metal ions (antacids, preparations containing iron, magnesium, calcium) form inactive chelates with doxycycline, and therefore their simultaneous administration should be avoided.
With simultaneous use with barbiturates, carbamazepine, phenytoin, the concentration of doxycycline in the blood plasma decreases due to the induction of microsomal liver enzymes, which may be the reason for the decrease in its antibacterial action.
It is necessary to avoid combination with penicillins, cephalosporins, which have a bactericidal effect and are antagonists of bacteriostatic antibiotics (including doxycycline).
The absorption of doxycycline is reduced by cholestyramine and colestipol (observe an interval between doses of at least 3 hours).
With simultaneous use with methoxyflurane, the development of acute renal failure, up to death, is possible.
Due to the suppression of the intestinal microflora, doxycycline reduces the prothrombin index, which requires dose adjustment of indirect anticoagulants.
Taking doxycycline reduces the reliability of contraception and increases the incidence of breakthrough bleeding while taking estrogen-containing oral contraceptives.
The simultaneous use of retinol increases intracranial pressure.
Side effect
From the nervous system: increased intracranial pressure, decreased appetite, vomiting, headache, papilledema, dizziness.
Metabolic disorders: anorexia.
On the part of the hearing and vestibular apparatus: ringing in the ears.
On the part of the organs of vision: blurred vision, scotoma and diplopia as a result of increased intracranial pressure.
From the digestive system: nausea, constipation or diarrhea, abdominal pain, glossitis, dysphagia, esophagitis (including erosive), gastritis, gastric and duodenal ulceration, pseudomembranous colitis, enterocolitis (due to the proliferation of resistant strains of staphylococci ).
Allergic reactions: maculopapular rash, pruritus, skin flushing, angioedema, anaphylactoid reactions, drug lupus erythematosus, rash erythematous, exfoliative dermatitis, urticaria, anaphylaxis, anaphylactic shock, anaphylactoid reactions, Stevens-Johnson syndrome.
From the side of the cardiovascular system: pericarditis, lowering blood pressure, tachycardia, erythema multiforme.
On the part of the hematopoietic organs: hemolytic anemia, thrombocytopenia, neutropenia, leukopenia, eosinophilia, decreased prothrombin index.
From the hepatobiliary system: impaired liver function, increased levels of hepatic transaminases, autoimmune hepatitis, cholestasis.
Musculoskeletal system: arthralgia, myalgia.
Violation of the function of the kidneys and urinary tract: increased levels of residual urea nitrogen.
Others: photosensitivity, superinfection; permanent discoloration of tooth enamel. Candidiasis (vaginitis, glossitis, stomatitis, proctitis), dysbacteriosis, a syndrome similar to serum sickness, toxic epidermal necrolysis.
If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms: dizziness, nausea, vomiting, convulsions, impaired consciousness due to increased intracranial pressure.
Treatment: drug withdrawal, gastric lavage with activated charcoal, symptomatic therapy, oral antacids and magnesium sulfate are prescribed to prevent the absorption of doxycycline. There is no specific antidote. Hemodialysis and peritoneal dialysis are ineffective.
Storage conditions
Store in a cool and dry place, at a temperature not exceeding 25º C. Keep out of the reach of children.
Best before date
3 years. Do not use after the expiry date stated on the packaging.
Holiday conditions
Released by prescription.
Release form
10 tablets in an aluminum foil blister. 1 blister with instructions for use in a cardboard box.