Doxycycline Express, 100 mg 10 pcs

Pharmacotherapeutic group: antibiotic – tetracycline

ATX code: J01AA02

Pharmacological properties

Pharmacodynamics

A broad spectrum antibiotic of tetracycline group. It has bacteriostatic activity, inhibits protein synthesis in microbial cell by interaction with 30S ribosome subunit. It is 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 within the group (i.e. strains resistant to doxycycline will simultaneously be resistant to the entire group of tetracyclines).

Pharmacokinetics

Intake

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

The maximum level of doxycycline in plasma (2.6-3 mcg/ml) is reached 2 hours after taking 200 mg, after 24 hours the concentration of active substance in plasma 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 levels), but the concentration of doxycycline 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, maxillary and frontal sinuses exudate, gingival sinus fluid.

In normal hepatic function, the drug level 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 and is secreted into breast milk in small amounts. It accumulates in dentin and bone tissue.

Metabolism

A small portion of doxycycline is metabolized.

Elimation

The elimination half-life after a single oral dose is 16-18 hours, after repeated doses – 22-23 hours.

About 40% of taken preparation is excreted by kidneys and 20-40% is excreted through intestine in the form of inactive forms (chelates).

Pharmacokinetics in special clinical cases

The half-life of the drug in patients with impaired renal function does not change, because its excretion through the intestine increases.

Hemodialysis and peritoneal dialysis have no effect on plasma concentration of doxycycline.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

Active ingredient

Composition

Excipients: microcrystalline cellulose – 35.00 mg, saccharin – 20.00 mg, hyprolose (hydroxypropyl cellulose) – 18.75 mg, hypromellose (hydroxypropyl methylcellulose) – 3.75 mg, colloidal silica (aerosil) – 0.63 mg, magnesium stearate – 2.00 mg, lactose monohydrate – 65.82 mg.

How to take, the dosage

Interaction

Special Instructions

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

Tetracyclines may increase prothrombin time, the prescription of tetracyclines in patients with coagulopathies should be carefully controlled.

The anti-anabolic effect of tetracyclines may lead to increased levels of residual urea nitrogen in the blood. This is generally 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.

With long-term use of the preparation it is necessary to periodically control laboratory blood parameters, liver and kidney function.

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

When using the drug both against the background of treatment and 2-3 weeks after discontinuation of treatment, development of diarrhea caused by Clostridium difficile is possible. In mild cases discontinuation of treatment and use of ion exchange resins (colestiramine, colestipol) is sufficient; in severe cases reimbursement of loss of fluid, electrolytes and protein and administration of vancomycin or metronidazole is indicated.

Drugs that inhibit intestinal peristalsis should not be used.

Long use of the drug may cause intestinal dysbiosis and, consequently, development of hypovitaminosis (B vitamins).

In order 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 the drug just before bedtime.

There is no known effect on driving, operating machinery. If dizziness, blurred vision or double vision develops, driving motor transport or operating machinery is not recommended (see side effect).

Contraindications

Side effects

Overdose

Pregnancy use

Similarities