Doxycycline - instructions for use, dose, side effects, contraindications

Semisynthetic tetracycline, bacteriostatic broad-spectrum antibiotic. Penetrating into the cell, acts on intracellularly located pathogens.Suppresses the synthesis of proteins in a microbial cell, disrupts the binding of the transport aminoacyl RNA to the 30S subunit of the ribosomal membrane.

To it are highly sensitive: gram-positive microorganisms Staphylococcus spp. (including Staphylococcus aureus, Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae), Clostridium spp., Listeria spp .; and Gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Klebsiella spp., Entamoeba histolytica, Escherichia coli, Shigella spp., Enterobacter spp., Salmonella spp., Yersinia spp. (formerly Pasteurella spp.), Bacteroides spp. Haemophilus influenzae (91-96%) and intracellular pathogens are the most sensitive. The drug is also active against Rickettsia spp., Treponema spp., Mycoplasma spp., Chlamydia spp.

Resistant to Pseudomonas aeroginosa, Proteus spp., Serratia spp., Most strains of Bacteroides fragilis.

Pharmacokinetics:Absorption is fast and high (about 100%). Eating does not have a significant effect on the degree of absorption. Has a high degree of solubility in lipids and a low affinity for binding to calcium ions. After oral administration of 200 mg, the time to reach the maximum concentration is 2.5 hours, the maximum concentration is 2.5 μg / ml, 24 hours after taking -1.25 μg / ml. Communication With plasma proteins - 80-93%. Good penetrates into organs and tissues; 30-45 minutes after ingestion is found in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate gland, eye tissues, pleural and ascitic fluids, bile, synovial exudate, exudate of maxillary sinus and frontal sinuses, in fluid gingival sulci.Poor penetrates into the cerebrospinal fluid (10-20% of the plasma level). Penetrates through the placental barrier, is determined in human milk. The volume of distribution is 0.7 l / kg. Metabolised in the liver 30-60%. The half-life is 10-16 hours (mainly 12-14 hours, on average 16.3 hours). With repeated administration, the drug can accumulate. It accumulates in the reticuloendothelial system and bone tissue. In bones and teeth forms insoluble complexes with calcium ions. It is excreted with bile, where it is found in high concentration. It is subjected to intestinal-liver recirculation, it is excreted through the intestine (20-60%); 40% of the dose is given by the kidneys for 72 hours (of which 20-50% is unchanged), in severe chronic renal failure, only 1-5%. In patients with impaired renal function or azotemia, gastrointestinal secretion is an important way of excretion.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms: - respiratory tract infections (pharyngitis, acute and chronic bronchitis, tracheitis, bronchopneumonia, lobar pneumonia, lung abscess, pleural effusion);

- infection of the ENT organs (otitis media, tonsillitis, sinusitis, etc.);

- infections of the genitourinary system (cystitis, pyelonephritis, prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, endometritis, endocervicitis, acute orchypididitis, gonorrhea, chlamydia of various localization, syphilis);

- infection of the biliary tract and gastrointestinal tract (cholecystitis, cholangitis, gastroenterocolitis, bacterial dysentery, traveler's diarrhea);

- infections of the skin and soft tissues (phlegmon, abscess, furunculosis, panaritium, infected burns, wounds, etc.);

- infectious eye diseases caused by Chlamydia spp. as a part of complex therapy, yawsiniosis, legionellosis, rickettsiosis, Ku fever, spotted fever of the Rocky Mountains, typhus (including swelling, tick-borne recurrent), Lyme I disease, bacillary and amoebic dysentery, tularemia, cholera, actinomycosis , malaria; in the combination therapy - leptospirosis, trachoma, psittacosis, ornithosis, granulocyte erlichiosis; whooping cough, brucellosis, osteomyelitis.

Prevention of postoperative purulent complications; malaria caused by Plasmodium falciparum, during short trips (less than 4 months) in a territory where strains resistant to chloroquine and / or pyrimethamine sulfadoxine are common.

Contraindications:Hypersensitivity, porphyria, severe hepatic insufficiency, leukopenia, children under 8 years old or with a body weight of less than 45 kg (up to 8 years - the possibility of formation of insoluble calcium ion complexes with deposition in the bone skeleton, enamel and dentin), pregnancy and lactation.

Pregnancy and lactation:Use during pregnancy and lactation is contraindicated.

Dosing and Administration:

Inside, in adults and children older than 8 years with a body weight of more than 45 kg, the average daily dose is 0.2 g on the first day (divided into 2 doses - 0.1 g twice a day), then 0.1 g / day (for 1-2 admission). In chronic infections (especially the urinary system) - 200 mg / day throughout the period of therapy.

In the treatment of gonorrhea, one of the following regimens is prescribed: acute uncomplicated urethritis - a course dose of 0.5 g (1 intake - 0.3 g, subsequent 2 - 0.1 g at intervals of 6 hours) or 0.1 g / day until complete cure (in women) or 0.1 g 2 times a day for 7 days (in men); with complicated forms of gonorrhea, the course dose is 0,8-0,9 g, which is divided into 6-7 receptions (0.3 g -1 reception, then with an interval of 6 h for 5-6 follow-up).

In the treatment of syphilis - 0.3 g / day for at least 10 days.

In uncomplicated infections of the urethra, cervix and rectum caused by Chlamydia trachomatis, appoint 0.1 g 2 times a day for at least 7 days.

Infections of male genital organs - 0.1 g 2 times a day for up to 4 weeks.

. Treatment of malaria resistant to chloroquine, 0.2 g / day for 7 days (in combination with schizontocid drugs - quinine); malaria prophylaxis - 0,1 g once a day 1-2 days before the trip, then daily during the trip and within 4 weeks after the return; children older than 8 years - 2 mg / kg 1 time per day.

Diarrhea "travelers" (prophylaxis) - 0.2 g on the first day of travel (for 1 reception or 0.1 g 2 times a day), then 0.1 g once a day during the entire period of stay in the region (no more than 3 weeks).

Treatment of leptospirosis - 0,1 g orally 2 times a day for 7 days; prevention of leptospirosis - 0.2 g once a week for a period of stay in a dysfunctional area and 0.2 g at the end of the trip.

Prevention of infections after medical abortion - 0.1 g for 1 hour before abortion and 0.2 g - 30 minutes after.

With acne, 0.1 g / day, the course - 6-12 weeks.

Maximum daily doses for adults - up to 0.3 g / day Or up to 0.6 g / day for 5 days with severe gonococcal infections:

In the presence of severe hepatic insufficiency, a decrease in the daily dose of doxycycline is required, since in this case a gradual accumulation of it in the body takes place (the risk of hepatotoxic action).

Side effects:

From the nervous system:

benign increase in intracranial pressure (loss of appetite, vomiting, headache, edema of the optic nerve), toxic effects on the central nervous system (dizziness).

From the digestive system:

nausea, constipation or diarrhea, glossitis, dysphagia, esophagitis (including erosive), gastritis, ulceration of the stomach and duodenum, enterocolitis (due to the proliferation of resistant strains of staphylococci).

Allergic reactions:

maculopapular rash, skin itch, skin hyperemia, angioedema, anaphylactoid reactions, drug lupus erythematosus.

From the hematopoiesis:

hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia.

Other:

photosensitivity, superinfection; stable change in the color of tooth enamel, inflammation in the anogenital crotch area.

Candidiasis (vaginitis, glossitis, stomatitis, proctitis), dysbiosis.

Overdose:

There is no information on acute poisoning of people with doxycycline. In case of an overdose and any complaints, stop taking the medication immediately and take measures to quickly eliminate the non-sucking drug from the body or reduce its absorption from the digestive tract (gastric lavage, activated charcoal intake - in case consciousness is stored).

Treatment for overdose, especially symptomatic, is the monitoring and maintenance of basic life functions.

Doxycycline is not excreted from the body by hemodialysis.

Interaction:

Absorption is reduced by antacids containing ions of aluminum, magnesium, calcium, iron preparations, sodium hydrogen carbonate, magnesium-containing laxatives, colestramine and colestipol, therefore their use should be separated by an interval of 3 hours.

In connection with the suppression of the intestinal microflora reduces the prothrombin index, which requires correction of the dose of indirect anticoagulants.

When combined with bactericidal antibiotics that disrupt the synthesis of the cell wall (penicillins, cephalosporins), the effectiveness of the latter is reduced.

Reduces the reliability of contraception and increases the frequency of bleeding "breakthrough" against the background of taking estrogen-containing oral contraceptives.

Ethanol, barbiturates, rifampicin, carbamazepine, phenytoin and other stimulators of microsomal oxidation, accelerating the metabolism of doxycycline, reduce its concentration in the plasma.

The simultaneous use of retinol helps to increase intracranial pressure.

Special instructions:

To prevent locally irritating effects (esophagitis, gastritis, ulceration of the mucous membrane of the gastrointestinal tract) it is recommended to take in the daytime hours with a lot of liquid, food.

In connection with the possible development of photosensitization, it is necessary to limit the insolation during treatment and for 4-5 days after it.

With prolonged use, periodic monitoring of liver function, hematopoiesis is necessary.

May mask the manifestations of syphilis, in connection with which, with the possibility of a mixed infection, a monthly serological analysis is necessary for 4 months.

All tetracyclines form stable complexes with calcium ions in any bone-forming tissue.In this regard, reception during the development of teeth can cause long-term staining of teeth in yellow-gray-brown color, as well as hypoplasia of the enamel.

Perhaps a false increase in the level of catecholamines in urine when determined by the fluorescent method. In the study of the thyroid biopsy in patients who received long-term doxycycline, it is possible to dark brown staining of tissue in micropreparations without disturbing its function.

When the dose is increased above 4 g, the pharmacokinetics of doxycycline does not depend on the dose and the concentration in the blood does not increase.

Form release / dosage:Capsules 100 mg.

Packaging:

10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

1,2,50 or 100 contour packs together with instructions for use are placed in a pack of cardboard.

Storage conditions:

List B.

In a dry, protected from light, place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:4 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006131/08

Date of registration: 01.08.2008 / 10.12.2012

The owner of the registration certificate:Barnaul Plant of Medical Preparations, LLC Barnaul Plant of Medical Preparations, LLC Russia

Information update date: & nbsp16.02.2016

Illustrated instructions

Instructions

Doxycycline (Doxycycline)