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Pharmacological properties:
Pharmacodynamics.
Doxycycline is an antibiotic drug. Its bacteriostatic action is inhibition of protein synthesis by attaching to the 30S and 50S ribosomal units. The drug has a broad spectrum of activity.
The percentage of resistant organisms, which are resistant due to their nature, may depend on numerous factors. For this reason it is necessary to closely control their stability.
As a rule, the stability of plasmids is predetermined. Cross-sensitivity is common in the group of tetracycline antibiotics.
Pharmacokinetics.
Absorbance. Doxycycline is almost completely absorbed after oral administration. Eating food or milk to a small extent affects the absorption of the drug. After intake of 200 mg on the first day of treatment and 100 mg / day in the next few days, therapeutic levels in plasma concentrations (1.5-3 mg / ml) maintained. The maximum level of Doxycycline in plasma (2,6-3 mg / ml) achieved after 2 h after administration of 200 mg over 24 h the concentration of active substance in plasma decreased to 1.5 mg / ml.
The distribution. Doxycycline reversibly binds to plasma proteins (80-90%). Volume of distribution is 1.58 L / kg of body weight. It penetrates into the tissue, is bad - in the CSF (10-20% level in blood plasma), but penetration is increased with inflammation of the meninges.
Accumulates in the reticuloendothelial system and bone tissue. Doxycycline crosses the placental barrier, into breast milk. In the saliva detected 5-27% concentration of Doxycycline in plasma.
Metabolism. Metabolized fraction of Doxycycline.
Excretion. T 1/2 - 16-18 hours after receiving a single oral dose and 22-23 h after administration of repeated oral doses. About 40% is excreted in unchanged form in urine and 20-40% in an inactive form (as hellats) in the feces.
Pharmacokinetics in special clinical situations. T 1/2 of the drug in patients with impaired renal function does not change, since it increases excretion through the intestine. Hemodialysis and peritoneal dialysis does not affect the concentration of Doxycycline in plasma.
INDICATIONS:
Doxycycline is used to treat infections caused by susceptible strains of Gram-positive and gram-negative microorganisms, such as:
<ul>
<li>respiratory tract infections: pneumonia and other lower respiratory tract disease caused by Streptococcus pneumoniae, Haemophilus influenza, Klebsiella pneumoniae. Pneumonia caused by Mycoplasma pneumoniae. Treatment of chronic bronchitis, sinusitis;
<li>urinary tract infection: infections caused by susceptible strains of the species Klebsiella, Enterobacter, and the bacteria Escherichia coli, Streptococcus faecalis, and the like;
<li>diseases, sexually transmitted infections: infections caused by Chlamydia trachomatis, including uncomplicated urethral and endocervical infection, and infection of the rectum. Non-gonococcal urethritis caused by Ureaplasma urealyticum (T-mycoplasma). Chancroid, granuloma inguinale, granuloma venereum. Doxycycline is an alternative drug for the treatment of gonorrhea and syphilis;
<li>infections of the skin: acne at the need for antibiotics.
</ul>
Since Doxycycline belongs to the tetracycline antibiotics, it can be used for infections caused by microorganisms sensitive to tetracycline, as follows:
ophthalmic infections: infections caused by susceptible bacteria gonococci, staphylococci, and Haemophilus influenza. Trachoma is an infectious and although the agent, but, as shown by immunofluorescence, not always elliminated;
rickettsial infections: typhus.
APPLICATION:
usual duration of treatment is 5-10 days. Infections caused by ?-hemolytic streptococcus should be treated no less than 10 days.
Adults and children aged >12 years with a body weight > 50 kg on the first day of treatment are prescribed 200 mg / day in 1 or 2 doses, on subsequent days of treatment - 100 mg 1 time a day. In the case of severe infections used 200 mg daily throughout the treatment period.
Children aged >12 years with a body weight ? 50 kg in 1-day treatment are prescribed daily dose rate of 4 mg / kg body weight for a reception in the next few days of treatment - 2 mg / kg of body weight one time per day. For infections that are difficult to treat, apply at a daily dose of 4 mg / kg body weight throughout the course of treatment.
Use of the drug to treat certain infections
Acne. The recommended dose of 50 mg 1 time per day with food or liquid for 6-12 weeks.
Gonorrhea. Men: a single dose of 200-300 mg once a day every day for 2-4 days, or within 1 day to 300 mg 2 times a day (the second reception at 1 h after the first).
Women: 200 mg daily until complete recovery (treatment for about 5 days).
Urethritis caused by Chlamydia trachomitis, endocervical or rectal infections in adults negonokokovy urethritis caused by Ureaplasma urealyticum. 100 mg 2 times daily for 7 days.
Acute epididimoorhit caused by Chlamydia trachomatis or Neisseria gonorrhea. 100 mg 2 times a day for 10 days.
Primary or secondary syphilis. 200 mg 2 times a day for 2 weeks as an alternative therapy penicillins.
Typhus. Depending on the severity of the disease the dose is 100-200 mg once daily.
Elderly patients. Individual may need a dosage adjustment.
The tablet should be taken with plenty of water. Also, before taking the pill can be diluted in at least 20 ml of water to make slurry. If the drug is taken at bedtime, you need to do it while sitting or standing to reduce the risk of inflammation and ulceration of the esophagus.
Advised to take tablets with meals.
CONTRAINDICATIONS:
hypersensitivity to Doxycycline and tetracycline or any component of the drug. Any conditions that include severe kidney or liver failure. During pregnancy and lactation. Children aged <12 years.
SIDE EFFECTS:
The following adverse reactions reported in patients taking tetracyclines, including Doxycycline.
Gastrointestinal: anorexia, loss of appetite, indigestion, nausea, diarrhea, glossitis, vomiting, dysphagia, enterocolitis, including staphylococcal enteritis, pseudomembranous colitis, an inflammation in the anal-genital area, accompanied by excessive growth of Candida (which is clinically manifested by diarrhea, glossitis, stomatitis , proctitis, vaginitis), itching at the anus area, blackening of the tongue, stomatitis. Possible deficiency of vitamin B, associated with inhibition of the activity of bacteria that produce it.
In rare cases - a violation of swallowing, marked inflammation of the esophagus and esophageal ulcer.
Skin and subcutaneous tissue: maculopapular and erythematous rashes, exfoliative dermatitis.
Sometimes, urticaria, angioedema, anaphylaxis, anaphylactic purpura, pericarditis, and exacerbation of systemic lupus erythematosus, exudative erythema multiforme, erythema malignant and toxic epidermal necrolysis.
Photodermatitis (see PRECAUTIONS) and fotooniholizis.
Hepatobiliary system: liver damage, sometimes accompanied by prolonged treatment of pancreatitis in patients with hepatic or renal failure, hepatitis, isolated cases of hepatotoxicity, pancreatitis.
The kidneys and urinary tract infections: a higher level of urea (nitrogen) in the blood, increasing azotemia in patients with renal insufficiency. Metabolized tetracyclines cause a syndrome similar to Fanconi syndrome, including albuminuria, aminoaciduria, hypophosphatemia, hypokalemia, and acidosis in renal tubules, interstitial nephritis.
In the blood and lymphatic system: hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, decrease in the activity of prothrombin, and porphyria atsidotsitoz.
CNS: bulging benevolent in children caused by increased intracranial pressure. In older children and adults were also reported malignant increased intracranial pressure, which was accompanied by irritation and swelling of the meninges of the optic nerve. This may be accompanied by headache, nausea, ringing in the ears, dizziness and blurred vision. These reversible symptoms disappear after a few days after cessation of treatment.
Vestibular Disorders: tinnitus, vertigo and visual disturbances such as hallucinations, scotoma, and diplopia.
On the part of the musculoskeletal system and bone tissue can break down the development of bones and teeth. The bones become brittle, and the teeth irreversibly change color. There are arthralgia, and myalgia.
Part of the endocrine system: the continued use of the drug observed brownish-red color of the thyroid gland that does not impair its function.
Other: flushing, hypersensitivity reactions, including anaphylactic shock, anaphylaxis, pseudoanaphylactic reaction, anaphylactoid purpura, decreased blood pressure, angioedema, exacerbation of systemic congestive seborrhoea, shortness of breath, serum sickness, peripheral edema, and tachycardia.
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