|Vibramycin 100 mg|
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Semisynthetic tetracycline, a broad-spectrum bacteriostatic antibiotic. By penetrating into the cell, it acts on intracellular pathogens. It inhibits protein synthesis in the microbial cell, breaks binding of transport aminoacyl-RNA to 30S subunit of ribosomal membrane.
Gram-positive microorganisms are highly sensitive to it: Staphylococcus spp. (including Staphylococcus aureus, Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae), Clostridium spp., Listeria spp.; Actinomyces israeli; and Gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Klebsiella spp., Escherichia coli, Shigella spp., Enterobacter, Salmonella spp., Bordetella pertussis. Bacteroides spp., Treponema spp. (including strains resistant to other antibiotics, such as modern penicillins and cephalosporins). Haemophilus influenzae (91-96%) and intracellular pathogens are most sensitive.
Doxycycline is active against most pathogens of dangerous infectious diseases: plague (Yersinia spp.), tularemia (Francisella tularensis), syphoresis (Bacillus anthracis), legionella (Legionella spp.), Brucella (Brucella spp.), cholera vibriones (Vibrio cholera), rickettsia (Rickettsia spp. ), glanders (Actinobacillus mallei), chlamydia (Chlamydia psittaci), psittacosis (Rickettsiaformis psittacosi), trachoma (Chlamydia trachomatis; , venereal granuloma (Calymmatobacterium granulomatis), malaria (Plasmodium falciparum), amebic dysentery (Entamoeba histolytica).
He acts on most strains of Proteus, Pseudomonas aeruginosa and fungi.
Inhibits intestinal flora to a lesser extent than other tetracycline antibiotics, differs from them by more complete absorption and longer duration of action. In terms of antibacterial activity doxycycline surpasses natural tetracyclines. In contrast to tetracycline and oxytetracycline it has higher therapeutic efficacy, manifested by treatment with 10 times lower doses, and longer duration of action. There is cross-resistance to other tetracyclines as well as to penicillins.
Absorption is fast and high (about 100%). Food intake has no significant effect on the degree of absorption. It has a high degree of lipid solubility and low affinity for binding calcium ions (Ca2+). After oral administration of 200 mg, time to reach maximum plasma concentration is 2.5 hours, maximum plasma concentration is 2.5 mcg/ml, 24 hours after administration is 1.25 mcg/ml.
Binding with plasma proteins is 80-93%. It penetrates into organs and tissues well; in 30-45 minutes after oral administration it is found in therapeutic concentrations in liver, kidneys, lungs, spleen, bones, teeth, prostate, eye tissues, pleural and ascitic fluid, bile, synovial exudate, maxillary and frontal sinuses exudate, gingival sulcus fluid. It penetrates poorly into cerebrospinal fluid (10-20% of plasma level). Penetrates through the placental barrier and is determined in maternal milk. Distribution volume is 0.7 l/kg.
Metabolized in the liver 30-60%. Period of half-life is 10-16 hours (mostly 12-14 hours, on average 16.3 hours). The drug may cumulate when administered repeatedly. It accumulates in the reticulo-endothelial system and bone tissue. In bones and teeth it forms insoluble complexes with calcium ions (Ca2+). It is excreted with bile, where it is found in high concentrations. It undergoes intestinal-hepatic recirculation and is excreted in the intestine (20-60%); 40% of the taken dose is excreted by the kidneys during 72 hours (including 20-50% - unchanged), in severe chronic renal failure - only 1-5%.
In patients with impaired renal function or azotemia, gastrointestinal secretion is an important route of excretion.
Contraindications to use
- Hypersensitivity to doxycycline, components of the drug, other tetracyclines;
- lactase deficiency;
- lactose intolerance;
- glucose-galactose malabsorption;
- severe hepatic insufficiency;
- childhood (up to 12 years of age - possibility of formation of insoluble complexes with calcium ions (Ca2+) with deposition in the bone skeleton, enamel and dentin of teeth);
- Children after 12 years of age with body weight less than 45 kg.
Use during pregnancy and lactation
The use of the drug during pregnancy is contraindicated because, penetrating through the placenta, the drug can disrupt normal dental development, cause suppression of fetal skeletal bone growth, as well as cause fatty infiltration of the liver.
During lactation, the use of doxycycline is contraindicated. If it is necessary to use the drug, breastfeeding should be discontinued for the period of treatment.
Administration in liver function disorders
It is contraindicated in severe hepatic insufficiency. In case of severe hepatic insufficiency a reduction of daily dose of doxycycline is required, since there is a gradual accumulation in the body (risk of hepatotoxic effect).
Administration in children
It is contraindicated in children under 12 years of age (possibility of formation of insoluble complexes with calcium ions (Ca2+) with deposition in bone skeleton, enamel and dentin of teeth); and in children after 12 years of age with body weight less than 45 kg.
Administration is possible in children over 12 years of age with body weight over 45 kg according to the dosing regimen.
Indications of Vibramycin (Doxycycline)
- Infectious and inflammatory diseases caused by susceptible microorganisms: respiratory tract infections (pharyngitis, acute and chronic bronchitis, tracheitis, bronchopneumonia, lobular pneumonia, lung abscess, pleural empyema);
- ENT-organ infections (otitis, tonsillitis, sinusitis, etc.);
- Infections of urogenital system (cystitis, pyelonephritis, prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, endometritis, endocervicitis, acute orchiepididymitis; gonorrhea);
- biliary tract and gastrointestinal infections (cholecystitis, cholangitis, gastroenterocolitis, bacterial dysentery, traveler's diarrhea);
- Skin and soft tissue infections (phlegmons, abscesses, furunculosis, panaritis, infected burns, wounds, etc.)
- Eye infections, syphilis, yersinosis, legionellosis, rickettsiosis, various localized chlamydia (including prostatitis and proctitis), Q fever, Rocky Mountain spotted fever, typhus (including rash, tick-borne, relapsing fever), Lyme disease (Stage I), erythema migrans. - erythema migrans), bacillary and amebic dysentery, tularemia, cholera, actinomycosis, malaria; in combined therapy - leptospirosis, trachoma, psittacosis, ornithiasis, granulocytic ehrlichiosis; pertussis, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;
- prevention of postoperative purulent complications; malaria caused by Plasmodium falciparum, during short-term travels (less than 4 months) in areas where strains resistant to chloroquine and/or pyrimethamine-sulfadoxine are spread;
- as a first-line drug is prescribed to patients under 65 years of age for exacerbations of chronic bronchitis (including bronchial asthma) without concomitant diseases (these exacerbations are often caused by Haemophilus influenzae). It is effective in exacerbations of bronchopulmonary infection (usually of staphylococcal etiology) in patients with cystic fibrosis, chlamydial arthritis, granulocytic ehrlichiosis. In elderly patients, it is used to treat acute prostatitis and urinary infection caused by Escherichia coli.
Orally, in adults and children over 12 years of age with body mass over 45 kg, the average daily dose is 200 mg on the first day (divided into 2 doses - 100 mg twice a day), further 100 mg/day.
In chronic urinary tract infections, 200 mg/day during the entire period of therapy.
In the treatment of gonorrhea, one of the following regimens is prescribed: Acute uncomplicated urethritis - a course dose of 500 mg (1 reception - 300 mg, the next 2 - 100 mg at 6-hour intervals) or 100 mg/day until complete cure (in women) or 100 mg 2 times a day for 7 days (in men); in complicated forms of gonorrhea the course dose -800-900 mg, which is distributed in 6-7 receptions (300 mg - 1 reception, then with 6-hour intervals for 5-6 subsequent).
In treatment of syphilis, 300 mg/day for at least 10 days.
In uncomplicated infections of the urinary tract, cervix and rectum caused by Chlamydia trachomatis, 100 mg twice daily for at least 7 days.
Male genital infections - 100 mg 2 times a day for 4 weeks. Treatment of chloroquine-resistant malaria - 200 mg/day for 7 days (in combination with schizontocidal drugs - quinine); malaria prophylaxis - 100 mg 1 time per day 1-2 days before travel, then daily during travel and for 4 weeks after return;
Diarrhea of "travelers" (prophylaxis) - 200 mg on the first day of the trip (1 dose or 100 mg 2 times a day), 100 mg once a day during the entire stay in the region (not more than 3 weeks).
Treatment of leptospirosis - 100 mg orally 2 times a day for 7 days; prophylaxis of leptospirosis - 200 mg once a week during the stay in a disadvantaged area and 200 mg at the end of the trip.
Prophylaxis of infections after medical abortion - 100 mg 1 hour before the abortion and 200 mg - 30 minutes after.
For acne - 100 mg/day, course - 6-12 weeks.
Maximum daily doses for adults are up to 300 mg/day or up to 600 mg/day for 5 days in severe gonococcal infections.
In the presence of severe hepatic impairment a reduction in the daily dose of doxycycline is required, since there is a gradual accumulation in the body (risk of hepatotoxicity).