Pharmacological properties Pharmacodynamics semisynthetic tetracycline antibiotic with a broad spectrum of activity. It has a bacteriostatic effect, the mechanism of which is associated with the suppression of protein synthesis in the microbial cell, a violation of due transport of aminoacyl tRNA to the 30S ribosomal subunit of the membrane. Get inside host cells, acts on intracellular pathogens located. Doxycycline in vitro is active against gram-positive aerobic microorganisms – of Staphylococcus spp . (including S. aureus, S. epidermidis ), Streptococcus spp . (including S. pneumoniae, S. pyogenes ), Listeria spp, Corynebacterium diphtheriae, Bacillus anthracis. ; Gram-negative aerobic – of Brucella spp, of Chlamydia spp.. (C. pneumoniae, C. trachomatis, C. granulomatosis, C. psittaci), Legionella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae (including strains resistant to ampicillin),Haemophilus ducreyi, Bordetella spp., spp Klebsiella., Francisella tularensis, Escherichia coli, Moraxella catarrhalis, Rickettsia spp., Coxiella burnetii, Shigella spp., Enterobacter spp., Salmonella spp., Yersinia spp. (including Y.pestis and Y.enterocolitica), spp Pasteurella, Helicobacter pylori, Vibrio spp.. (includingV.cholera e); anaerobes – of Clostridium spp, Peptostreptococcus spp.. , actinomycetes, of Bacteroides spp . (active against most strains of B.fragilis low), by Fusobacterium spp, P.acnes. ; other microorganisms – cpirohet ( . Borellia bugdorferi, Borellai recurrenstis, Leptospira spp, of Treponema pallidum, of Treponema pertenue ), mycoplasma ( M.pneumoniae, of Ureaplasma urealyticum ), and protozoa ( of Entamoeba histolitic a and . of Plasmodium spp .) Does not affect the majority of strains Proteus, Pseudomonas aeruginosa, of Acinetobacter spp . and fungi. In the antibacterial activity superior to doxycycline and tetracycline, oxytetracycline. There is cross-resistance between tetracyclines.
after single intravenous (i / v) 100 mg of doxycycline infusion lasting 60 min (solution concentration of 0.4 mg / ml) for persons with normal renal function, the maximum serum concentration (C max ) of 2.5 g / ml; After a two-hour infusion of 200 mg (concentration 0.4 mg / ml) and C max are about 3.6 ug / ml. More lipophilic than tetracycline and oxytetracycline, so well distributed in many organs and tissues (liver, kidney, lung, spleen, bones, teeth, prostate, eye tissues, pleural and ascites fluid, bile, synovial fluid, exudate maxillary and frontal sinuses), which creates high, therapeutically relevant concentrations. For repeated administrations marked drug accumulation effect. Accumulating in the RES and bone. The bones and teeth forms insoluble complexes with Ca 2+ . Penetration through the BBB is 10-25% of serum concentrations. It penetrates through the placental barrier, determined in breast milk. High concentrations 10-20 times the serum, determined in the bile. Relationship to plasma proteins is variable – 80-93%. The volume of distribution – 0.7 l / kg. The half-life is 16 to 22 hours 40% of the administered dose excreted by the kidneys within 72 hours (of which 20-50% – unchanged)., With severe chronic renal failure – only 1-5%. 30-60% excreted in the bile, which revealed high concentrations of the active form of the antibiotic. Treated enterohepatic recycling; 20-60% is excreted in the feces. In patients with impaired renal function is important, by removing the digestive tract. In hemodialysis doxycycline is not removed from the blood serum.
Indications for use of
upper and lower respiratory tract infections (acute and exacerbation of chronic bronchitis, moderate and severe pneumonia, lung abscess, empyema); upper respiratory tract infection; reproductive system infections in men (prostatitis); infections of the reproductive system in women (inflammatory diseases of the pelvic organs – adnexitis, salpingo et al.); infections, sexually transmitted diseases (syphilis, especially in patients who are allergic to penicillin, granuloma inguinale, lymphogranuloma venereum); infections caused by chlamydia (trachoma, psittacosis, prostatitis, cervicitis) and mycoplasma; intestinal infection (yersiniosis, cholera); eye infection; actinomycosis, bacillary angiomatosis; infections of skin and soft tissues, bones and joints; intra-abdominal infections; complicated and uncomplicated urinary tract infections. It is used for the treatment of these contagious infectious diseases and bacterial zoonotic diseases: Lyme disease, relapsing fever, Q fever, Rocky Mountain spotted fever, brucellosis, leptospirosis, anthrax, plague (in combination with streptomycin or gentamicin), tularemia (in combination with streptomycin or gentamicin), cholera, whooping cough, trachoma. In combination with quinine is highly effective for the treatment of malaria. At intolerance of penicillin and other beta-lactams is used as an alternative for the treatment of infections caused by gonococci and meningococci.
Hypersensitivity to doxycycline, and other tetracyclines; pregnancy (in the experiment found that doxycycline may have a toxic effect on the fetus – delayed development of the skeleton); lactation; severe hepatic impairment. Not suitable for children under 8 years (possibility of forming insoluble complexes of Ca 2+ deposition in the bone skeleton, enamel and dentin of the teeth).
Dosing and Administration
In / in the introduction of doxycycline preferably severe infections and in cases when oral administration is difficult. Recommended treatment step, ie the transition to receiving doxycycline oral forms as soon as it becomes possible.
anavar cycle ® is administered by slow / in freshly prepared infusion lasting 1-2 hours, depending on the dose (see. Terms preparing a solution). The recommended duration of infusion solution containing 100 mg anavar cyclea ® . At a concentration of 0.5 mg / ml, – 60 minutes for adults for the first day of therapy, the dose is 200 mg, which is administered in one or two (100 mg every 12 hours) infusion; subsequently, depending on the severity of the infection, administered at 100 mg 1 time per day, or 200 mg per day, which is administered in one or two (100 mg every 12 hours) infusion. Duration of therapy is determined by the form and severity of the infection; in / injected 3-5 days, if necessary and / or parenteral administration good tolerability extend up to 7 days; later (! indicated) move on to oral doxycycline. In inflammatory diseases of the pelvic organs in women in the acute stage of the disease is introduced into / from 100 mg every 12 hours; recommended combination therapy with cephalosporins II-III generation. If a positive response to therapy and the patient stabilization continue therapy with oral forms doxycycline 100 mg orally two times a day for 14 days. For the treatment of syphilis daily dose is 200 mg / day; treatment is continued for at least 2 weeks. with primary and 4 weeks. in secondary syphilis. Parenteral administration is shown only if you can not receive the drug per os; It is recommended as a possible early replacement / in the introduction to oral for treatment of anthrax used in a daily dose of 200 mg, divided into 2 of the introduction. The duration of therapy for pulmonary form – 60 days, with cutaneous – 2 weeks. Given the duration of administration of the antibiotic, it is recommended as a possible early transition to the use of oral doxycycline forms. In patients with impaired renal function, and renal failure is used in usual therapeutic doses; dose adjustment is required. In patients with severe hepatic impairment use anavar cyclea ® is contraindicated. In children older than 8 years old , on the first day of therapy is administered at a dose of 2.2 mg / kg every 12 hours or 4.4 mg / kg, 1 time per day; daily dose should not exceed 200 mg; on subsequent days, depending on the severity of the infection, administered at 2.2 mg / kg one time per day or 4.4 mg / kg per day, which is administered in one or two (2.2 mg / kg every 12 hours) infusion. In children weighing more than 45 kg dosages are used as defined for adults. Recommended dosages for therapeutic treatment of anthrax (2.2 mg / kg every 12 hours); duration of therapy was the same as in adults.
Terms solution preparation
stage 1 – contents of the vial with 100 mg sterile powder anavar cyclea ® diluted with 10 ml of sterile water for injection or 0.9% sodium chloride; Stage 2 – obtained during the initial dilution solution anavar cyclea ®at 10 mg / ml was added to 100-500 ml infusion of one of the following media: 0.9% sodium chloride, 5% dextrose, Ringer’s solution. The recommended range of concentrations of the prepared solution for infusion – 0.1 mg / ml to 1 mg / ml. The duration of infusion in a dose dependent manner (0.1 or 0.2 g) and the final solution volume – about 1 to 2 hours at an infusion rate of 60-80 drops / min. During the infusion solutions should be protected from direct sunlight, artificial ultraviolet light and artificial light from other sources.
anavar cycle ® is well tolerated. Adverse reactions are rare and most often cropped own after discontinuation of the drug, without the need for special treatment. There are indications of the following symptoms of side effects (Systems): of the nervous system : benign increased intracranial pressure, or syndrome of cerebral pseudotumor (loss of appetite, vomiting, headache, disc swelling of the optic nerve), a toxic effect on the central nervous system (dizziness or unsteadiness ); state quickly docked after the abolition of doxycycline, of the digestive system : glossitis, dysphagia, nausea, unstable chair, esophagitis (including erosive), enterocolitis, of the liver and biliary tract : rarely – liver toxicity, allergic reactions : maculopapular rash, itching, redness of the skin, angioedema, anaphylactoid reactions, isolated cases – exfoliative dermatitis, with the side of hematopoiesis : hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, by the kidneys : increase the level of urea nitrogen in serum, local reactions : thrombophlebitis in place in / infusion, especially during prolonged therapy / in the form of doxycycline, other : photosensitivity, superinfection, sustainable change in color of tooth enamel, oropharyngeal, intestinal and vaginal candidiasis (one of the manifestations – inflammation in the anogenital area of the perineum).
Interaction with other medicinal products
When combining tetracycline with bactericidal antibiotics disturb the synthesis of the cell wall (penicillins, cephalosporins), the effectiveness of the latter is reduced.
In view of the possible physical and chemical incompatibility anavar cyclea solution ® should not be mixed and simultaneously administered with other drugs.
Tetracyclines may reduce the effect of estrogensoderjath oral contraceptives, reducing the reliability of contraception and increasing bleeding frequency “breakthrough” at a reception.
ethanol, barbiturates, rifampicin, carbamazepine, phenytoin, and others. stimulants microsomal oxidation, accelerating metabolism of doxycycline, reduce its concentration in the plasma, which may require correction of the dose of the antibiotic .
Concomitant use of retinol improves intracranial pressure.
The tetracyclines may enhance the effect of anticoagulants (due to suppression of intestinal microflora), and therefore may require monitoring of prothrombin time and dose adjustment of indirect anticoagulants.
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In connection with the possible development of photosensitivity need to limit sun exposure; avoid exposure to artificial UV radiation during treatment and 4-5 days after it.
With prolonged use, requires periodic monitoring of liver function of hematopoiesis.
Antianabolicheskoe actions that are typical of tetracyclines may be the cause of increase of urea nitrogen in the blood serum.
All tetracyclines form stable complexes with Ca 2+ in tissue of any kostnoobrazuyuschey therefore receive a tooth development may cause staining of the teeth in the long yellow-gray-brown color, as well as hypoplasia of enamel.
Perhaps a false increase in catecholamines in urine when determining the fluorescence method. In the study biopsy of the thyroid gland in patients receiving long-term doxycycline, possibly dark brown staining of tissue in the slides; Thyroid function is not impaired. steroiden kaufen
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