Видокцин®

General characteristics. Structure:

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

Excipients: sodium disulphite, dinatrium эдетат.

Pharmacological properties:

Pharmacodynamics. A semi-synthetic antibiotic from group of tetracyclines with a wide range of activity. Possesses bacteriostatic action which mechanism is connected with suppression of synthesis of proteins in a microbic cell, disruption of communication transport aminoacyl-RNA with 30S in subunit of a ribosomalny membrane. Gets in macroorganism cells, works on intracellularly located activators. 

In vitro doxycycline is active concerning gram-positive aerobic microorganisms - Staphylococcus spp. (including S. aureus, S. epidermidis), Streptococcus spp. (including S. pneumoniae, S. pyogenes), Listeria spp., Corynebacterium diphtheriae, Bacillus anthracis; gram-negative aerobes - Brucella spp., Chlamydia spp. (C. pneumoniae, C. trachomatis, C. granulomatosis, C. psittaci), Legionella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae (including strains steady against ampicillin), Haemophilus ducreyi, Bordetella spp., Klebsiella spp., Francisella tularensis, Escherichia coli, Moraxella catarrhalis, Rickettsia spp., Coxiella burnetii, Shigella spp., Enterobacter spp., Salmonella spp., Yersinia spp. (including Y.pestis and Y.enterocolitica), Pasteurella spp., Helicobacter pylori, Vibrio spp. (including V.cholerae); anaerobe bacterias - Clostridium spp., Peptostreptococcus spp., actinomyce, Bacteroides spp. (activity concerning the majority of strains of B.fragilis low), Fusobacterium spp., P.acnes; other microorganisms - spirochetes (Borellia bugdorferi, Borellai recurrenstis, Leptospira spp., Treponema pallidum, Treponema pertenue), mycoplasmas (M.pneumoniae, Ureaplasma urealyticum), and also protozoa (Entamoeba histolitica and Plasmodium spp.). 

The protea, a pyocyanic stick, Acinetobacter spp does not affect the majority of strains. and mushrooms.

Doxycycline surpasses tetracycline and Oxytetracyclinum in antibacterial activity. Between tetracyclines there is a cross stability.

Pharmacokinetics. After single intravenous (in/in) infusion of 100 mg of doxycycline lasting 60 min. (concentration of solution of 0,4 mg/ml) to persons with normal function of kidneys the maximum serumal concentration _(Cmax) make 2,5 mkg/ml; after two-hour infusion of 200 mg of drug (concentration of solution of 0,4 mg/ml), _Cmax make about 3,6 mkg/ml. More липофилен, than tetracycline and Oxytetracyclinum therefore it is well distributed in many bodies and fabrics (a liver, kidneys, lungs, a spleen, bones, teeth, a prostate gland, eye tissues, in pleural and ascitic liquids, bile, synovial fluid, exudate of Highmore's and frontal sinuses) where creates high, therapeutic significant concentration.

At repeated introductions the effect of cumulation of drug is noted. Collects in RES and a bone tissue. In bones and teeth forms insoluble complexes with ^Ca2+. The penetration through GEB makes 10-25% of serumal concentration.

Gets through a placental barrier, is defined in maternal milk. High concentration, at 10-20 times the exceeding serumal, are defined in bile. Communication with proteins of plasma is variable - 80-93%. Distribution volume - 0,7 l/kg. The elimination half-life makes from 16 to 22 h 40% of the entered dose are excreted by kidneys for 72 h (from them 20-50% - in not changed look), at heavy HPN - only 1-5%. 30-60% are removed with bile where high concentration of an active form of an antibiotic are found.

Is exposed to enterohepatic recirculation; 20-60% are removed with a fecal masses. At patients with a renal failure an important way of removal is the GIT. At a hemodialysis doxycycline is not removed from blood serum.

Indications to use:

- infections of upper and lower respiratory tracts (acute and exacerbations of chronic bronchitis, medium-weight and heavy pneumonia, lung abscess, pleura empyema);

- infections of ENT organs; infections of reproductive system at men (prostatitis);

- infections of reproductive system at women (inflammatory diseases of bodies of a small pelvis - an adnexitis, a salpingo-oophoritis, etc.);

- infections, sexually transmitted (syphilis, especially at patients with an allergy to penicillin, an inguinal granuloma, a venereal lymphogranuloma);

- the infections caused by chlamydias (trachoma, a psittacosis, prostatitis, a cervicitis) and mycoplasmas;

- intestinal infections (иерсиниоз, cholera);

- infections of eyes;

- actinomycosis, bacillar angiomatosis;

- infections of skin and soft tissues, bones and joints;

- intraabdominal infections; the complicated and uncomplicated infections of urinary tract.

It is applied to therapy of the following contagious infectious diseases and bacterial zoonoz: Lyme's disease, a typhinia, the Q fever, spotty fever of the Rocky Mountains, a brucellosis, a hay fever, a malignant anthrax, plague (in a combination with streptomycin or gentamycin), tularemias (in a combination with streptomycin or gentamycin), cholera, whooping cough, trachoma.

In combination with quinine it is highly effective for treatment of malaria.

At intolerance of penicillin and other beta lactams it is applied as an alternative for treatment of the infections caused by gonokokka and meningokokka.

Route of administration and doses:

In/in administration of doxycycline preferably at severe forms of infections and in cases when oral administration is complicated. Step therapy, that is transition to reception of peroral forms of doxycycline as soon as it becomes possible is recommended.

^{Видокцин®} it is entered in the way slow into infusions of freshly cooked solution lasting 1-2 hours, depending on a dose (see Rules solution preparation). The recommended duration of infusion of the solution containing 100 mg ^{of Vidoktsina®} in concentration of 0,5 mg/ml - 60 min.
For adults in the first day of therapy the dose makes 200 mg which enter into one or two (on 100 mg each 12 h) infusions; in the subsequent, depending on weight of an infection, appoint 100 mg of 1 times a day or on 200 mg a day which enter into one or two (100 mg each 12 h) infusions. 

Duration of therapy is defined by a form and weight of an infection; in/in enter 3-5 days, if necessary and/or good tolerance prolong parenteral administration up to 7 days; in the subsequent (ACCORDING TO INDICATIONS!) pass to oral administration of doxycycline.

At inflammatory diseases of a small pelvis at women in an acute stage of a disease each 12 h enter in/in 100 mg; the combination therapy with generation cephalosporins II-III is recommended. At affirmative answer on therapy and stabilization of a condition of the patient, continue therapy by peroral forms of doxycycline on 100 mg in 2 times a day within 14 days. 

For treatment of syphilis the daily dose makes 200 mg/days; treatment is continued not less, than by 2 weeks at primary and 4 weeks at secondary syphilis. Parenteral administration is shown only at impossibility of administration of drug of per os; earlier replacement in/in introductions by oral administration is recommended.

For therapy of a malignant anthrax use 200 mg which is divided into 2 introductions in a daily dose. Therapy duration at a pulmonary form - 60 days, at a skin form - 2 weeks. Considering duration of reception of an antibiotic, earlier transition to reception of peroral forms of doxycycline is recommended.

At patients with a renal failure and a renal failure it is applied in usual therapeutic dosages; dose adjustment is not required. At patients with a heavy liver failure use ^{of Vidoktsina®} is contraindicated.

At children 8 years are more senior, in the first day of therapy each 12 hours, or 4,4 mg/kg of 1 times a day enter in a dose 2,2 mg/kg; the daily dose should not exceed 200 mg; in the next days, depending on weight of an infection, appoint 2,2 mg/kg of 1 times a day or on 4,4 mg/kg a day which enter into one or two (2,2 mg/kg each 12 h) infusions. At children with body weight more than 45 kg use the dosages specified for adults. For treatment of a malignant anthrax therapeutic dosages are recommended (to 2,2 mg/kg there are each 12 hours); therapy duration the same, as at adults.

Solution preparation: 1 stage - bottle contents from 100 mg of the sterile ^{powder Vidoktsina®} are parted by 10 ml of sterile water for injections or 0,9% with sodium chloride solution; The 2nd stage - ^{the Vidoktsina® solution} received at primary cultivation to concentration of 10 mg/ml is added to 100-500 ml of one of the following infusional environments: 0.9% of solution of sodium of chloride, 5% of solution of a dextrose, to Ringer's solution. The recommended range of concentration of ready solution for infusions - from 0,1 mg/ml to 1 mg/ml. Infusion duration depending on a dose (0,1 or 0,2 g) and the volume of ready solution - about from 1 to 2 h at rate of administering of 60-80 caps/min. During infusion solutions should be protected from action of direct sunshine, artificial ultraviolet rays and artificial light from other sources.

Features of use:

Due to the possible development of a photosensitization insolation restriction is necessary; to avoid impact of artificial UF-radiation during treatment and within 4-5 days after it.

At long use periodic control of function of a liver, bodies of a hemopoiesis is necessary. 

The anti-anabolic action characteristic of tetracyclines can be the cause of increase in an urea nitrogen in blood serum.

All tetracyclines form resistant complexes with ^{Ca2 +} in any kostnoobrazuyushchy fabric therefore inclusion in the period of development of teeth can become the reason of long-term coloring of teeth in yellow-gray-brown color, and also enamel hypoplasias.

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; function of a thyroid gland is not broken.

Side effects:

^{Видокцин®} it is well transferred. Undesirable reactions arise seldom and are most often stopped independently after drug withdrawal, without demanding special treatment. There are instructions on the following manifestations of side effect (on systems):
from a nervous system: high-quality increase in intracranial pressure, or a brain pseudoneoplasm syndrome (a loss of appetite, vomiting, a headache, a papilledema), toxic action on TsNS (dizziness or instability); the state is quickly stopped after doxycycline cancellation; 

from the alimentary system: glossitis, dysphagy, nausea, unstable chair, esophagitis (including erosive), coloenteritis;

from a liver and biliary tract: seldom - a hepatotoxic;
allergic reactions: makulopapulezny rash, a skin itch, a dermahemia, a Quincke's disease, anaphylactoid reactions, isolated cases - exfoliative dermatitis; 

from bodies of a hemopoiesis: hemolitic anemia, thrombocytopenia, neutropenia, eosinophilia;

from kidneys: increase in level of an urea nitrogen in blood serum;
local reactions: thrombophlebitis in the place in/in infusion, especially at long therapy in/in a doxycycline form;

others: a photosensitization, superinfection, steady discoloration of an adamantine substance of tooth, orofaringealny, intestinal and vaginal candidiasis (one of manifestations - an inflammation in an anogenitalny zone of a crotch).

Interaction with other medicines:

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

In view of possible physical and chemical incompatibility ^{Vidoktsina® solution} cannot be mixed and to enter at the same time with other medicines.
Tetracyclines can weaken effect of estrogensoderzhashchy oral contraceptives, reducing reliability of contraception and increasing the frequency of bleedings of "break" against the background of reception. 

Ethanol, barbiturates, rifampicin, carbamazepine, Phenytoinum, etc. stimulators of a microsomal oxidation, accelerating doxycycline metabolism, reduce its concentration in plasma that can demand dose adjustment of this antibiotic. 

Simultaneous use of Retinolum promotes increase in intracranial pressure.

Tetracyclines can strengthen effect of indirect anticoagulants (due to suppression of intestinal microflora) in this connection control of a prothrombin time and dose adjustment of indirect anticoagulants can be required.

Contraindications:

Hypersensitivity to doxycycline and other tetracyclines; pregnancy (in an experiment it is established that doxycycline can have toxic effect on a fruit - a skeleton arrest of development); feeding by a breast; heavy liver failure. It is not applied at children up to 8 years (a possibility of formation of insoluble complexes with ^{Ca2 +} with adjournment in a bone skeleton, enamel and dentine of teeth).

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

100 mg of active agent in bottles glass, hermetically corked by rubber bungs, pressed out by caps aluminum or combined (aluminum with safety plastic covers).

1 bottle together with the application instruction in a pack from a cardboard.