Doksitsiklin-Darnitsa, capsules on 0.1 g No. 10

General characteristics. Structure:

Pharmacological properties:

Pharmacodynamics. Doksitsiklin-Darnitsa – a semi-synthetic antibiotic of group of tetracyclines of a broad spectrum of activity. Has generally bacteriostatic action. It is active rather gram-positive bacteria, rickettsiae, Mycoplasma pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Calymmatobacterium (Donovania) qranulomatis, Borrelia recurrentis and B. Duttonii, Ureaplasma urealyticum (T-Mycoplasma), Plasmodium falciparum. Shows activity of rather gram-negative microorganisms, such as Haemophilus ducreyi, Yersinia pestis, Bartonella bacilliformis, Bacteroides spp., Fusobacterium spp., Campylobacter fetus, Brucella spp. (in a combination with streptomycin), and also some strains of Neisseria qonorrhoeae, Vibrio cholerae, Escherichia coli, Enterobacter aeroqenes, Shiqella spp., Acinetobacter spp. Doksitsiklin-Darnitsa is alternative means for treatment of the infections caused by Treponema pallidum and Treponema pertenue, Listeria monocytoqenes, Clostridium spp., Bacillus anthracis, Leptotrichia buccalis, Actinomyces spp.

Pharmacokinetics. After intake it is almost completely absorbed (   90-100%), meal does not exert insignificant impact on absorption. Has high degree of solubility in lipids and low affinity concerning calcium binding. It is stable in plasma. After oral administration of 200 mg of doxycycline average values of pharmacokinetic parameters made: Cmax – 3,61 mkg/ml, Tmax – 2,60 hours; an elimination speed constant – 0,049 hours-1, T1/2 – 16,33 hours. Contacts proteins of plasma for 80–92%. Gets into the majority of fabrics and liquids of an organism, into bile, a secret of okolonosovy bosoms, a pleural exudate, synovial and ascitic liquids, liquid of gingival furrows. The estimated volume of distribution – 52,6–134 l. Collects in bones, teeth, a liver, a spleen, a prostate gland, in therapeutic concentration – in eye tissues. Gets through a placenta and it is found in a fruit organism. Badly gets into medullispinal liquid (10–20% of level in plasma). 20–60% of a dose are excreted by intestines, other 35–60% – kidneys (from them 20–50% – in not changed look). At normal function of kidneys (clearance of creatinine – about 75 ml/min.) excretion kidneys makes 40% in 72 hours. T1/2 does not change at a renal failure since at patients with a renal failure or an azotemia a preferential way of removal is gastrointestinal secretion. At a heavy chronic renal failure (clearance of creatinine – about 10 ml/min.) removal by kidneys can make 1–5% in 72 hours. The hemodialysis does not influence doxycycline T1/2 from plasma. T1/2 after a single dose makes 18 hours. At repeated introductions cumulation is possible. Doxycycline forms insoluble complexes with calcium in bones and teeth.

Pharmaceutical characteristics.

main physical and chemical properties: the solid gelatin capsules with a lid and the case of yellow color containing powder of color, yellow with a greenish shade, with white impregnations.

Indications to use:

The infectious diseases caused by activators, sensitive to doxycycline:

respiratory infections (pharyngitis, acute and chronic bronchitis, tracheitis, pneumonia, lung abscess, pleura empyema);

infections of ENT organs (otitis, tonsillitis, sinusitis);

infections of urinogenital system (cystitis, pyelonephritis, prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, endometritis, endocervicitis, acute orchiepididymitis; gonorrhea);

infections of zhelchevyvodny ways and digestive tract (cholecystitis, cholangitis, gastroenterocolitis, bacterial dysentery);

infections of skin and soft tissues (the phlegmons, abscesses, furunculosis, felons infected burns, wounds, acne rash);

syphilis, frambeziya, иерсиниоз, легионельоз, rickettsiosis, clamidiosis of different localization (including prostatitis and proctitis), bacillar and amoebic dysentery, tularemia, cholera, actinomycosis, malaria;

as a part of a combination therapy – leptospirosis, trachoma, a psittacosis, an ornithosis, granulotsitarny эрлихиоз; whooping cough, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis.

Route of administration and doses:

Apply inside in time or after meal (it is possible to wash down with milk or kefir). The daily dose for adults and children with body weight more than 50 kg in the first day of treatment makes 200 mg. Accept once or 100 mg with an interval of 12 h. In the next days apply 100 mg in a daily dose. At the heavy course of an infection the daily dose in the first day and all next days of treatment makes 200 mg. Drug is used for 7–10 days.

The maximum daily dose – 300 mg.

Acute gonorrhea at women: on 200 mg per day, at least 7 days.

Acute urethritis at the husband's, caused gonokokkam: daily, on 200 mg of doxycycline, for 7 days.

Acute infectious diseases of appendages which are caused by a chlamydia and/or gonokokka: on 200 mg daily, for 10 days.

At acne rash reception on 100 mg a day for 7–21 days is allowed.

At primary or secondary syphilis apply 300 mg a day in stages, duration of a course of treatment – is not less than 10 days.

At treatment of a hay fever appoint 100 mg 2 times a day for 7 days; for prevention of a hay fever – on 200 mg once a week throughout stay in the unsuccessful area and 200 mg at the end of a trip.

At the uncomplicated infections of the urinary channel, a neck of uterus and rectum caused by C.trachomatis appoint 100 mg 2 times a day for         not less than 7 days.

For treatment of children with body weight to 50 kg (aged from 8 years): dosage forms are not applied to oral administration through their high dosing.

After disappearance of symptoms of a disease of treatment 1-3 more days have to last.

Features of use:

For reduction of irritation of a stomach of Doksitsiklinom-Darnitsa of the capsule it is necessary to accept during food, washing down with enough water.

During treatment by doxycycline and within 4–5 days after its termination contraindicated solar radiation or UV rays (photosensitization).

At prolonged use it is regularly necessary to control cellular composition of peripheral blood, to carry out functional hepatic trials, to determine the content of urea in serum.

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 applying doxycycline, it is necessary to consider a possibility of coloring of fabric in microdrugs in dark brown color.

Along with Doksitsiklinom-Darnitsa it is recommended to apply nystatin or levorinum to prevention of development of candidiases.

Not to take alcoholic drinks during treatment.

Ability to influence the speed of reactions at control of motor transport or work with other mechanisms. During treatment it is necessary to abstain from control of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Disturbance of blood and lymphatic system: hemolitic anemia, thrombocytopenia, neutropenia and eosinophilia.

Disturbance of immune system: allergic reactions, including an acute anaphylaxis, an anaphylaxis, anaphylactic reactions, anaphylactoid purple, hypotension, a pericardis, a Quincke's disease, an aggravation of a system red top, an asthma, a serum disease, peripheral hypostases, tachycardia and urticaria.

Disturbance of endocrine system: at use of tetracyclines throughout long time microscopic coloring of tissue of thyroid gland was observed brown чорная. Any pathology of a thyroid gland was not revealed.

Metabolism and disbolism: anorexia.

Disturbance of a nervous system: a headache, swelling of the top of the head at newborns and benign intracranial hypertensia at adults.

Hearing disorder and vestibular mechanism: feeling of a sonitus.

Disturbance of a digestive tract: an abdominal pain, nausea, vomiting, diarrhea, a glossitis, a dysphagy, dyspepsia, a coloenteritis, pseudomembranous colitis, S. d_ff_c_le diarrhea, inflammatory damages of the anogenitalny site (owing to candidiasis). Also ulceration at patients who took capsules and a pill of doxycycline was reported about emergence of an esophagitis.

Disturbance of gepatobiliarny system: disturbance of hepatic function, hepatitis. Arrived the message on single cases of a hepatotoxic.

Skin: makulopapulyozny and erythematic rashes, reactions of photosensitivity of skin, photo-onikholizis, multiformny erythema, exfoliative dermatitis, Stephens-Johnson's syndrome and toxic epidermal necrolysis.

Skeletal and muscular device: arthralgia and mialgiya.

Renal failure and uric ways: increase in level of residual nitrogen of urea.

Interaction with other medicines:

Doxycycline reduces efficiency of contraception and increases the frequency of "breakthrough" bleedings at reception of estrogensoderzhashchy oral contraceptives.

Exponentiates effect of indirect anticoagulants.

Simultaneous use of iron preparations, Natrii hydrocarbonas, aluminum, calcic or magnesian antacids, magniysoderzhashchy laxatives, Colestyraminum and kolestipol reduces absorption. Barbiturates, carbamazepine, Phenytoinum, rifampicin – reduce concentration in plasma and reduce doxycycline T1/2 (induction of monooxygenases and acceleration of biotransformation) that can lead to decrease in antibacterial effect.

Simultaneous use of Retinolum promotes increase in intracranial pressure.

Contraindications:

Doksitsiklin-Darnitsa is contraindicated at hypersensitivity to tetracyclines and other components of drug, a porphyria, a heavy liver failure, a leukopenia, pregnancy (especially the II-III trimester), the feeding period a breast, children's age up to 8 years (because of a possibility of formation of insoluble complexes with calcium and their deposits in bones, enamel and dentine of teeth).

Use during pregnancy or feeding by a breast. Drug is contraindicated at pregnancy (possibly formation of insoluble complexes with calcium and adjournment of doxycycline in bones). During treatment it is necessary to stop feeding by a breast.

Children. Doksitsiklin-Darnitsa is contraindicated to children aged up to 8 years.

Overdose:

Treatment: phase-out, symptomatic and maintenance therapy. The hemodialysis is not effective.

Storage conditions:

Period of validity. 2 years. To store in the place protected from children, in original packaging, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in a blister strip packaging, on 1 or 2 blister strip packagings in a pack; on 1000 capsules in a plastic container.