Doxycycline Solution Tablets, 100 mg 10 pcs

Pharmacotherapeutic group: antibiotic – tetracycline

ATX code: J01AA02

Pharmacological action

Pharmacodynamics

A broad spectrum antibiotic of tetracycline group. It has bacteriostatic action, inhibits protein synthesis in microbial cell by interaction with 30S ribosome subunit. Active against many Gram-positive and Gram-negative microorganisms: Streptococcus spp., Treponema spp., Staphylococcus spp., Klebsiella spp., Enterobacter spp. (including E. aerugenes), Neisseria gonorrhoeae. Neisseria meningitidis, Haemophilus influenzae, Chlamydia spp., Mycoplasma spp., Ureaplasma urealyticum, Listeria monocytogenes, Rickettsia spp, Typhus exanthematicus, Escherichia coli, Shigella spp, Campylobacter fetus, Vibrio cholerae, Yersinia spp. (including Yersinia pestis), Brucella spp., Francisella tularensis, Bacillus anthracis, Bartonella bacilliformis, Pasteurella multocida, Borrelia recurrentis, Clostridium spp. (except Clostridium difficile), Actinomyces spp, Fusobacterium fusiforme, Calymmatobacterium granulomatosis, Propionibacterium acnes, some protozoa (Entamoeba spp, Plasmodium falciparum).

As a rule, it has no effect on Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.

The possibility of acquired resistance to doxycycline in a number of pathogens should be taken into account, which is often cross-over within the group (i.e., strains resistant to doxycycline will simultaneously be resistant to the entire tetracycline group).

Pharmacokinetics

Intake

Absorption is fast and high (about 100%). Food intake has little effect on absorption of the drug.

The maximum plasma concentration of doxycycline (2.6-3 mcg/ml) is reached 2 hours after 200 mg administration; after 24 hours the plasma concentration of the active substance decreases to 1.5 mcg/ml.

After administration of 200 mg on the first day of treatment and 100 mg daily thereafter, the plasma concentration of doxycycline is 1.5-3 mcg/ml.

Distribution

Doxycycline reversibly binds to plasma proteins (80-90%), penetrates well into organs and tissues, poorly – into cerebrospinal fluid (10-20% of plasma concentration), but doxycycline concentration in cerebrospinal fluid increases with inflammation of the spinal cord.

The volume of distribution is 1.58 l/kg. Within 30-45 minutes after oral administration doxycycline is found in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate, eye tissues, pleural and ascitic fluid, bile, synovial exudate, exudate of maxillary and frontal sinuses and gingival sinus fluid.

In normal hepatic function, the concentration of doxycycline in bile is 5-10 times higher than in plasma.

In saliva, 5-27% of the value of doxycycline concentration in plasma is determined.

Doxycycline penetrates the placental barrier, in small amounts is secreted into breast milk. It accumulates in dentin and bone tissue.

Metabolism

Metabolizes a small part of doxycycline.

Elimation

The elimination half-life after a single oral dose is 16-18 hours, after repeated doses – 22-23 hours. Approximately 40% of doxycycline taken is excreted by kidneys and 20-40% is excreted in the intestines as inactive forms (chelates).

Pharmacokinetics in special clinical cases

The half-life of doxycycline in patients with impaired renal function does not change, as its excretion by the intestine increases. Hemodialysis and peritoneal dialysis have no effect on plasma concentration of doxycycline.

Indications

Infectious inflammatory diseases caused by doxycycline-sensitive microorganisms:

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

There is a possibility of cross-resistance and hypersensitivity with other tetracycline drugs.

Tetracyclines can increase prothrombin time, the use of tetracyclines in patients with coagulopathies should be carefully monitored.

The anti-anabolic effect of tetracyclines may cause an increase in residual urea nitrogen concentration in the blood. Generally, this is not significant in patients with normal renal function. However, in patients with renal insufficiency, an increase in azotemia may be observed.

The use of tetracyclines in patients with impaired renal function requires medical monitoring.

Per long-term use of the drug requires periodic monitoring of laboratory blood parameters, liver and kidney function.

Perhaps due to the development of photodermatitis it is necessary to limit sun exposure during treatment and for 4-5 days afterwards.

When using the drug, both during treatment and 2-3 weeks after discontinuation, diarrhea caused by Clostridium difficile may develop. In mild cases withdrawal of treatment and use of ion exchange resins (colestiramine, colestipol) is sufficient, in severe cases compensation of loss of fluid, electrolytes and protein, prescription of vancomycin, metronidazole is indicated. Do not use drugs that inhibit intestinal peristalsis.

Long use of the drug may cause dysbacteriosis and, as a consequence, the development of hypovitaminosis (especially B vitamins).

To prevent dyspeptic complaints, it is recommended to take the drug with meals.

To prevent esophagitis or esophageal ulcers, take the drug with plenty of water and avoid using it right before bedtime.

There is no known effect on the ability to drive vehicles, machines and mechanisms.

If dizziness, blurred vision, or double vision develops, driving motor vehicles or machinery is not recommended (see Side Effects).

Contraindications

Side effects

Overdose

Pregnancy use

Contraindicated in pregnancy (possible formation of insoluble complexes with calcium and deposition of doxycycline in the bone skeleton) and lactation.

The FDA fetal category of action is D.

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