Доксициклин-Ферейн®

General characteristics. Structure:

Active ingredient: 0,05 g, 0,1 g or 0,2 g of doxycycline (in the form of a hydrochloride).

Excipients: potato starch, sugar milk, calcium stearate.

The structure of a gelatin capsule - gelatin, titanium dioxide, quinolinic yellow, sanst yellow.

Pharmacological properties:

Pharmacodynamics. Semi-synthetic tetracycline, the bacteriostatic antibiotic of a broad spectrum of activity received from metacycline. Getting in a cell, works on intracellularly located activators. Inhibits synthesis of proteins in a microbic cell, breaking communication transport aminoacyl-RNA with 30S in subunit of a ribosomalny membrane. Does not influence synthesis of a cell wall of bacteria.

To it are highly sensitive: gram-positive microorganisms of Staphylococcus spp. (including Staphylococcus aureus, Staphylococcus albus), Streptococcus spp. (including Streptococcus pneumoniae), Clostridium spp., Listeria spp.; and gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Klebsiella spp., Entamoeba histo-lytica, E.coli, Shigella spp., Enterobacter, Salmonella spp., Pasterella spp., Bacteroides spp., Psytta-cosis spp., Treponema spp. (in the t.ch.shtamma steady against other antibiotics, for example, to modern penicillin and cephalosporins). Haemophilus influenzae (91-96%) and intracellular pathogens are most sensitive.

Pharmacokinetics. Absorption - bystry and high (about 100%). Has high degree of solubility in lipids and low affinity concerning calcium binding

After oral administration of 200 mg time of achievement of the maximum concentration - 2.5ch, the maximum concentration - 2.5 mkg/ml, in 24 h after reception - 1.25 mkg/ml. Communication with proteins of plasma - 80-90%.

Well gets into bodies and fabrics; in 30-45 min. after intake it is found in therapeutic concentration in a liver, kidneys, lungs, a spleen, bones, teeth, a prostate gland, eye tissues, in pleural and ascitic liquids, bile, synovial exudate, exudate of Highmore's and frontal sinuses. Badly gets into spino-brain liquid (10-20% of plasma level). Gets through a placental barrier, is defined in maternal milk.

It is metabolized in a liver of 30-60%. An elimination half-life - 16-24 h. At repeated introductions drug can kumulirovat. Collects in a bone tissue. In bones and teeth forms insoluble complexes with calcium. It is removed with bile where it is found in high concentration. Is exposed to enterohepatic recirculation, it is removed with a fecal masses (20-60%); 40% of the accepted dose are allocated with kidneys for 72 h (from them 20-50% - in not changed look), at a heavy chronic renal failure - only 1-5%. At patients with a renal failure or an azotemia an important way of removal is digestive tract.

Indications to use:

• the infectious and inflammatory diseases caused by sensitive microorganisms: respiratory infections (pharyngitis, bronchitis acute and chronic, tracheitis, bronchial pneumonia, share pneumonia, lung abscess, pleura empyema);
• infections of ENT organs (otitis, tonsillitis, sinusitis, etc.);
• infections of urinogenital system (cystitis, pyelonephritis, prostatitis, an urethritis, an urethrocystitis, urogenital mycoplasmosis, an endometritis, an endocervicitis, acute orkhiepididimit; gonorrhea);
• infections of biliary tract and GIT (cholecystitis, cholangitis, gastroenterocolitis, bacterial dysentery, diarrhea of "travelers");
• infections of skin and soft tissues (the phlegmons, abscesses, furunculosis, felons infected burns, wounds, etc.);
• infectious diseases of eyes, syphilis, frambeziya, иерсиниоз, legionellosis, rickettsiosis, clamidiosis of various localization (including prostatitis and proctitis), Ku's fever, spotty fever of the Rocky Mountains, typhus (including sypny, tick-borne returnable), borreliosis, bacillar and amoebic dysentery, tularemia, cholera, Lyme's disease (I stage), actinomycosis, malaria, leptospirosis, trachoma, psittacosis, ornithosis, granulotsitarny эрлихиоз; whooping cough, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;
• prevention of postoperative purulent complications; the malaria caused by Plasmodium falciparum at short-term travel (less than 4 months) in the territory where the strains steady against chloroquine and/or Pyrimethaminum sulphadoxine are widespread.

Route of administration and doses:

Inside, adults and children with body weight have more than 45 kg an average daily dose - 0.2 g in the first day (is divided into 2 receptions - on 0.1 g 2 times a day), further on 0.1 g/days (in 1-2 receptions). At heavy infections, in particular at persistent infections of an urinary system - 200 mg/days throughout the entire period of therapy.

At treatment of gonorrhea appoint on one of the following schemes: an acute uncomplicated urethritis - a course dose of 0.5 g (1 reception - 0.3 g, the subsequent two - on 0.1 g with an interval of 6 h) or 0.1 g/days before full treatment (at women) or on 0.1 g 2 times a day within 7 days (at men); at the complicated gonorrhea forms a course dose - 0.8-0.9 g which is distributed on 6-7 receptions (0.3 g - 1 reception, then with an interval of 6 h on 5-6 of the subsequent).

At treatment of syphilis - on 0.3 g/days within not less than 10 days (inside or in/in).

At the uncomplicated infections of an urethra, neck of uterus and rectum caused by Cl.trachomatis appoint 0.1 g 2 times a day within not less than 7 days.

Infections of men's generative organs - on 0.1 g 2 times a day during 4 weeks.

Treatment of the malaria steady against chloroquine - 0.2 g/days within 7 days (in combination with shizontotsidny drugs - quinine); prevention of malaria - 0.1 g of 1 times a day in 1-2 days prior to a trip, then daily during a trip and during 4 weeks after return; to children, 8 years - 0.002 g/kg of 1 times a day are more senior.

Diarrhea of travelers (prevention) - 0.2 g in the first day of a trip (for 1 reception or on 0.1 g 2 times a day), further on 0.1 g of 1 times a day during all stay in the region (no more than 3 weeks).

Treatment of a hay fever - 0.01 g in 2 times a day within 7 days; prevention of a hay fever - 0.02 g once a week during stay in the unsuccessful area and 0.02 g at the end of a trip.

Prevention of infections after medical abortion - 0.1 g for 1 h before abortion and 0.2 g - in 30 min. after.

The maximum daily doses for adults - to 300 mg a day or to 600 mg a day within 5 days at heavy gonococcal infections.

Children have 9-12 years with body weight to 45 kg an average daily dose - 0.004 g/kg in the first day, further - on 0.002 g/kg a day (in 1-2 receptions). At heavy infections it is appointed each 12 h on 0.004 g/kg.

In the presence of a heavy liver failure decrease in a daily dose of doxycycline as at the same time there is its gradual accumulation in an organism (risk of a hepatotoxic action) is required.

Features of use:

Pregnancy and lactation. Use in the period of a lactation is contraindicated. Use during pregnancy is hazardous to health of a fruit.

For prevention of local irritative action (an esophagitis, gastritis, a GIT ultseration) reception with a large amount of liquid, food is recommended in the afternoon.

Due to the possible development of a photosensitization restriction of insolation is necessary during treatment and within 4-5 days after it.

At long use periodic control of function of kidneys (KK), a liver, bodies of a hemopoiesis is necessary.

Can mask displays of syphilis in this connection at a possibility of a mikst-infection monthly carrying out serologic assay for 4 months is necessary.

Appointment during development of teeth can become the reason of irreversible change of their color.

Perhaps false increase in level of catecholamines in urine at their definition by a fluorescent method. At a research of a bioptat of a thyroid gland at patients, it is long receiving doxycycline, perhaps dark brown prokrashivaniye of fabric in microdrugs without disturbance of its function. In an experiment it is established that doxycycline can cause toxic action on fetation - a skeleton arrest of development.

Side effects:

From a nervous system: increase in intracranial pressure (anorexia, vomiting, a headache, a papilledema), toxic action on TsNS (dizziness or an ataxy).

From the alimentary system: nausea, diarrhea, a lock, a glossitis, a dysphagy, an esophagitis (including erosive), gastritis, an ulceration of a stomach and duodenum, an inflammation in an anogenitalny zone of a crotch, a coloenteritis (due to proliferation of resistant strains of stafilokokk).

Allergic reactions: makulopapulezny rash, skin itch, dermahemia, Quincke's disease, anaphylactoid reactions, medicinal lupus erythematosus.

From blood: hemolitic anemia, thrombocytopenia, neutropenia, eosinophilia.

Others: photosensitization, superinfection; steady discoloration of an adamantine substance of tooth.

Fungal infections: (vaginitis, glossitis, stomatitis, proctitis), dysbacteriosis.

Interaction with other medicines:

Absorption the antacids containing aluminum, magnesium and calcium, food, calciferous (milk, cottage cheese), iron preparations, sodium reduce bicarbonate, magniysoderzhashchy laxatives, Colestyraminum and колестипол therefore their use has to be divided by an interval of 3 h.

Due to the suppression of intestinal microflora reduces a prothrombin ratio that demands dose adjustment of indirect anticoagulants.

At a combination to the bactericidal antibiotics breaking synthesis of a cell wall (penicillin, cephalosporins) - decrease in efficiency of the last.

Reduces reliability of contraception and increases the frequency of bleedings of "break" against the background of reception of estrogensoderzhashchy oral contraceptives.

Ethanol, barbiturates, rifampicin, carbamazepine, Phenytoinum, etc. stimulators of a microsomal oxidation accelerate doxycycline metabolism.

At simultaneous use of a metoksifluran the risk of development of fatal nephrotoxicity increases.

Simultaneous use of Retinolum promotes increase in intracranial pressure.

Contraindications:

Hypersensitivity, porphyria, heavy liver failure, leukopenia, pregnancy the II-III trimester, the lactation period, children's age (up to 8 years - a possibility of formation of insoluble complexes with calcium and adjournment in a bone skeleton, enamel and dentine of teeth).

Storage conditions:

List B. In dry, protected - from light the place, at a temperature not above 25 °C, in unavailable to children. A period of validity - 4 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Mg capsules 50, 100, 200. Packaging: on 1, 10 capsules in a blister strip packaging. On 10 or 20 capsules in bank of orange glass or in banks polymeric. Each can, 1 blister strip packaging together with the instruction are placed in a pack of a cardboard or 2 blister strip packagings.