Доксициклин-Ферейн®

General characteristics. Structure:

Active ingredient: 100 mg of doxycycline (in the form of a hydrochloride).

Excipients: sodium disulphite (sodium metabisulphite), dinatrium эдетат (disodium salt of ethylene diamine tetraacetic acid).

Pharmacological properties:

Pharmacodynamics. Doxycycline - a semi-synthetic antibiotic of a tetracycline row with a wide range of antibacterial action. Getting in a cell, works on inside - cellular 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.

It is active concerning the majority of gram-positive microorganisms: aerobic cocci - Staphylococcus spp. (including Staphylococcus aureus), Streptococcus spp. (including Streptococcus pneumoniae); aerobic spore-forming bacteria - Bacillus anthracis; aerobic asporous bacteria - Listeria monocytogenes; anaerobic spore-forming bacteria - Clostridium spp. Drug is active also in the relation gra-motritsatelny microorganisms: aerobic bacteria - Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Klebsiella spp., Entamoeba histolytica, Escherichia coli, Shigella spp., Treponema spp. (including the strains steady against other antibiotics, for example, to modern penicillin and cephalosporins).

Haemophilus influenzae (91-96%) and intracellular pathogens are most sensitive.

The protea, a pyocyanic stick and mushrooms does not affect the majority of strains. There is a cross other tetracyclines resistance, and also to penicillin.

Pharmacokinetics. At intravenous administration drug well gets into bodies and fabrics and till 24 o'clock it is found in effective concentration in blood, a liver, kidneys, lungs, a spleen, in pleural and ascitic liquids.

Badly gets into medullispinal 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 by intestines (20-60%).

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:
- lower respiratory tract infections - bronchitis acute and chronic, bronchial pneumonia, share pneumonia, lung abscess, pleura empyema;
infections of ENT organs - otitis, sinusitis;
- infections of urinogenital system - cystitis, pyelonephritis, prostatitis, an urethritis, an urethrocystitis, an endometritis, an endocervicitis, acute orkhiepididimit;
- infections of skin and soft tissues - the phlegmons, abscesses, a furunculosis infected burns, wounds;
- 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), actinomycosis, malaria, leptospirosis, trachoma, psittacosis, ornithosis, gra-nulotsitarny эрлихиоз, dysentery; brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;
- prevention of postoperative purulent complications.

Route of administration and doses:

Intravenously enter at severe forms it is purulent - septic diseases when it is necessary to create quickly high concentration of drug in blood, and also in cases when administration of drug is inside complicated or it is badly transferred by patients.

The adult in the first day of treatment enter 0,2 g once a day or on 0,1 g each 12 hours; in the next days treatments - on 0,1 g once a day.

The maximum daily doses for adults - to 0,3 g/days or 0,6 g/days within 5 days at heavy gonococcal infections.

To children 12 years drug are more senior appoint at the rate of 4 mg/kg in the first day of treatment, in the next days - 2 mg/kg also once a day.

Intravenously kapelno enter in the form of solution which is prepared by ex tempore. For this purpose contents of each ampoule or a bottle (0,1 g of drug) dissolve in 5 ml of water for injections, then add 0,9% of solution of sodium chloride or 5% of solution of glucose to 250 ml. Concentration of drug in solution should not exceed 1 mg/ml. Infusion duration depending on the entered dose (0,1 g or 0,2 g of drug) makes 1-2 hours at rate of administering of 60-80 drops in a minute.

Treatment duration at intravenous administration makes 3-5 days with the subsequent transition, if necessary, to administration of drug inside.

Features of use:

Pregnancy and lactation. Use during a lactation is contraindicated.

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, a liver, bodies of a hemopoiesis is necessary.

Can mask displays of syphilis in this connection at an opportunity a mix - the infection needs monthly carrying out serologic assay for 4 months.

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.

During infusions solution should be protected from light (solar and artificial).

Side effects:

From a nervous system: increase in intracranial pressure (anorexia, vomiting, a headache, a papilledema), toxic action on the central nervous system (dizziness and 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 stafilokok).

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

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

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

Fungal infections: vaginitis, glossitis, stomatitis, proctitis; dysbacteriosis.

Interaction with other medicines:

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 and other 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.

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

Pharmaceutical it is incompatible with other antibacterial drugs.

Contraindications:

Hypersensitivity, porphyria, heavy liver failure, leukopenia, pregnancy, the lactation period, children's age (up to 12 years - a possibility of formation of insoluble complexes with calcium with adjournment in a bone skeleton, enamel and dentine of teeth), a myasthenia.

Storage conditions:

List B. In the place protected from light, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 4 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Lyophilisate for preparation of solution for infusions of 100 mg. Packaging: on 0,1 g of active agent in an ampoule of neutral glass with a capacity of 5 ml. On 0,1 g of active agent in the bottle of neutral glass with a capacity of 10 ml which is hermetically corked by a stopper from the rubber mix which is pressed out by a cap the aluminum or combined cap from aluminum and plastic. 5 ampoules in a blister strip packaging from a film polyvinyl chloride. 5 ampoules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil or a packing material. 1, 2 blister strip packagings with ampoules together with the application instruction and the scarificator or a knife ampoule in a pack from a cardboard. On 5 or 10 ampoules together with the application instruction and the scarificator or a knife ampoule with an insert with cells for ampoules in 1 go 2 rows from a cardboard to a pack. When using ampoules with a notch, a break ring the knife ampoule or the scarificator is not put. 1 bottle together with the application instruction is placed in a pack from a cardboard. 5 bottles in a blister strip packaging from a film polyvinyl chloride. 5 bottles in a blister strip packaging from a film of polyvinyl chloride and aluminum foil or a packing material. 1,2 blister strip packagings with bottles together with the application instruction in a box from a cardboard. On 5 or 10 bottles together with the application instruction in a pack with an insert with cells for bottles in 1 or 2 rows from a cardboard.