Unidox Solutab (Doxycycline) 100 mg, 10 pcs.

Active substance:

doxycycline monohydrate, in terms of doxycycline 100 mg.

Excipients:

microcrystalline cellulose - 45 mg,

saccharin - 10 mg,

hyprolose (low substituted) - 18.75 mg,

hypromellose - 3.75 mg,

silicon dioxide colloidal (anhydrous) - 0.625 mg,

magnesium stearate - 2 mg,

lactose monohydrate - up to 250 mg.

Unidox - bacteriostatic, antibacterial.

It inhibits the synthesis of proteins in a microbial cell, disrupting the binding of transport RNA of the ribosomal membrane.

Pharmacodynamics

A broad-spectrum antibiotic from the tetracycline group. It acts bacteriostatically, inhibits protein synthesis in a microbial cell by interacting with the 30S subunit of ribosomes. 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, Escheribella coli campiella colibella colibella 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 granulomatis, Propionibacterium acnes,  some protozoa  (Entamoeba spp., Plasmodium falciparum).

As a rule, it does not  affect Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.

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

Pharmacokinetics

Suction

Absorption is fast and high (about 100%). Eating slightly affects the absorption of the drug.

C _{max of}  doxycycline in blood plasma (2.6–3 μg / ml) is achieved 2 hours after ingestion of 200 mg, after 24 hours the concentration of the active substance in blood plasma decreases to 1.5 μg / ml.

After taking 200 mg on the first day of treatment and 100 mg / day on the following days, the plasma concentration of doxycycline is 1.5–3 μg / ml.

Distribution

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

Distribution volume - 1,58 l / kg. 30–45 min after oral administration, doxycycline is found in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate gland, eye tissues, pleural and ascitic fluids, bile, synovial exudate, maxillary and frontal sinuses exudate, in fluid gingival fissures.

With normal liver function, the level of the drug in bile is 5-10 times higher than in plasma.

In saliva, 5–27% of the concentration of doxycycline in the blood plasma is determined.

Doxycycline crosses the placental barrier and is secreted in breast milk in small amounts.

Accumulates in dentin and bone tissue.

Metabolism

A small portion of doxycycline is metabolized.

Breeding

T _1/2  after a single oral administration is 16-18 hours, after taking repeated doses - 22-23 hours.

About 40% of the drug taken is excreted by the kidneys and 20–40% is excreted through the intestines as 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 intestines increases.

Hemodialysis and peritoneal dialysis do not affect the concentration of doxycycline in blood plasma.

- osteomyelitis;

- sepsis;

- subacute septic endocarditis;

- peritonitis.

- respiratory tract infections (including pharyngitis, acute bronchitis, exacerbation of chronic obstructive pulmonary disease, tracheitis, bronchopneumonia, lobar pneumonia, community-acquired pneumonia, lung abscess, pleural empyema);

- infections of ENT organs (including otitis media, sinusitis, tonsillitis);

- infections of the genitourinary system (cystitis, pyelonephritis, bacterial prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, acute orchiepididymitis; endometritis, endocervicitis and salpingoophoritis / as part of combination therapy /);

- Sexually transmitted infections (urogenital chlamydia, syphilis in patients with penicillin intolerance, uncomplicated gonorrhea / as an alternative therapy /, inguinal granuloma, venereal lymphogranuloma);

- gastrointestinal tract and biliary tract infections (cholera, yersiniosis, cholecystitis, cholangitis, gastroenterocolitis, bacillary and amoebic dysentery, travelers diarrhea);

- infections of the skin and soft tissues (including wound infections after an animal bite), severe acne (as part of combination therapy);

- other diseases: phrambesia, legionellosis, chlamydia of various localization (including prostatitis and proctitis), rickettsiosis, Q fever, Rocky Mountain spotted fever, typhoid (including rash, tick-borne relapsing), Lyme disease (Stage I ) - erythema migrans /, tularemia, plague, actinomycosis, malaria, leptospirosis, psittacosis, ornithosis, anthrax (including pulmonary form), bartonellosis, granulocytic ehrlichiosis, whooping cough, brucellosis;

- Infectious diseases of the eyes (as part of combination therapy) - trachoma;

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

- hypersensitivity to antibiotics of the tetracycline group.

- severe violations of the liver and / or kidneys;

- porphyria;

- children's age up to 8 years;

From the digestive system: anorexia, nausea, vomiting, dysphagia, diarrhea, enterocolitis, pseudomembranous colitis, esophagitis, esophageal ulcer, dark staining of the tongue, liver damage (during prolonged use or in patients with renal or liver failure), cholestasis.

Dermatological reactions: photosensitization, maculopapular and erythematous rashes, exfoliative dermatitis.

Allergic reactions: urticaria, angioedema, anaphylactic reactions, exacerbation of systemic lupus erythematosus, pericarditis, a syndrome similar to serum sickness, erythema multiforme.

From the hemopoietic system: hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, a decrease in prothrombin activity.

From the endocrine system: in patients who have been taking doxycycline for a long time, a reversible dark brown staining of the thyroid tissue is possible.

From the side of the central nervous system: benign increase in intracranial pressure (anorexia, vomiting, headache, swelling of the optic nerve), vestibular disorders (dizziness or instability), blurred vision, double vision.

From the urinary system: increased residual urea nitrogen (due to the anti-anabolic effect).

From the musculoskeletal system: doxycycline slows down osteogenesis, disrupts the normal development of teeth in children (irreversibly changes the color of teeth, enamel hypoplasia develops).

Other: candidiasis (glossitis, stomatitis, proctitis, vaginitis) as manifestations of superinfection.

Antacids containing aluminum, magnesium, calcium, preparations of iron, sodium bicarbonate, magnesium-containing laxatives reduce the absorption of doxycycline, so their use should be separated by a 3-hour interval.

Due to the suppression of intestinal microflora by doxycycline, the prothrombin index decreases, which requires dose adjustment of indirect anticoagulants.

With the combination of doxycycline with bactericidal antibiotics that disrupt cell wall synthesis (penicillins, cephalosporins), the effectiveness of the latter decreases, which should be considered when treating meningitis and tonsillopharyngitis caused by Streptococcus pyogenes.

Doxycycline reduces the reliability of contraception and increases the frequency of acyclic bleeding when taking estrogen-containing hormonal contraceptives.

Ethanol, barbiturates, rifampicin, carbamazepine, phenytoin, accelerating the metabolism of doxycycline, reduce its concentration in blood plasma.

The simultaneous use of doxycycline and retinol increases intracranial pressure.

The tablets are dispersed (dissolved) in a small amount of water (about 20 ml) to give a suspension. Tablets can also be swallowed whole, divided into parts or chewed with water.

The drug is preferably taken with meals. Take pills while sitting or standing, which reduces the likelihood of developing esophagitis and ulcers of the esophagus. The drug should not be taken immediately before bedtime.

Typically, the duration of treatment is 5-10 days.

Adults and children over 8 years of age with a body weight of more than 50 kg are prescribed 200 mg / day in 1 or 2 doses on the first day of treatment, and 100 mg / day in 1 dose on the following days of treatment. In case of severe infections, 200 mg / day is prescribed for the entire treatment period.

For children aged 8-12 years with a body weight of less than 50 kg, the average daily dose is 4 mg / kg on the first day, then 2 mg / kg / day (in 1-2 doses). In cases of severe infections, the drug is prescribed at a dose of 4 mg / kg daily during the entire treatment.

In case of infection caused by Streptococcus pyogenes, the duration of treatment is at least 10 days.

With uncomplicated gonorrhea (with the exception of anorectal infections in men), adults are prescribed 100 mg 2 times / day until they are completely cured (on average for 7 days), or 600 mg is prescribed in one day - 300 mg in 2 divided doses (second dose 1 hour after the first).

With primary syphilis, 100 mg 2 times / day for 14 days is prescribed, with secondary syphilis - 100 mg 2 times / day for 28 days.

For uncomplicated urogenital infections caused by Chlamydia trachomatis, cervicitis, non-gonococcal urethritis caused by Ureaplasma urealiticum, 100 mg 2 times / day for 7 days are prescribed.

With acne, 100 mg / day is prescribed, the course of treatment is 6-12 weeks.

For the prevention of malaria, 100 mg is prescribed 1 time / day 1-2 days before the trip, then daily during the trip and for 4 weeks after return; children over 8 years old - 2 mg / kg 1 time / day. The duration of prophylaxis should not exceed 4 months.

For the prevention of travelers diarrhea - 200 mg on the first day of the trip in 1 or 2 doses, then - 100 mg 1 time / day for the entire stay in the region (no more than 3 weeks).

For the treatment of leptospirosis - 100 mg orally 2 times / day for 7 days; for the prevention of leptospirosis - 200 mg once a week during a stay in a disadvantaged area and 200 mg at the end of the trip.

In order to prevent infections during medical abortion, 100 mg is prescribed 1 hour before and 200 mg after the intervention.

The maximum daily dose for adults is up to 300 mg / day or up to 600 mg / day for 5 days for severe gonococcal infections. For children over 8 years old with a body weight of more than 50 kg - up to 200 mg, for children of 8-12 years old with a body weight of less than 50 kg - 4 mg / kg daily during the entire treatment.

In renal (CC less than 60 ml / min) and / or liver failure, a reduction in the daily dose of doxycycline is required, since this gradually accumulates in the body (risk of hepatotoxicity).

Symptoms: increased adverse reactions caused by liver damage - vomiting, fever, jaundice, azotemia, increased transaminases, increased prothrombin time.

Treatment: immediately after taking large doses, gastric lavage, heavy drinking are recommended, and if necessary, inducing vomiting. Take activated charcoal and osmotic laxatives. Hemodialysis and peritoneal dialysis are not recommended due to low efficacy.

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

Tetracyclines can increase prothrombin time; the administration of tetracyclines in patients with coagulopathy should be closely monitored.

The anti-anabolic effect of tetracyclines can lead to an increase in the level of residual urea nitrogen in the blood. As a rule, this is not significant for patients with normal renal function. However, in patients with renal failure, an increase in azotemia may be observed. The use of tetracyclines in patients with impaired renal function requires medical supervision.

With prolonged use of the drug, periodic monitoring of laboratory blood parameters, liver and kidney function is required.

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

When using the drug, both on the background of taking it, and 2-3 weeks after the cessation of treatment, the development of diarrhea caused by Clostridium dificile is possible. In mild cases, it is sufficient to cancel the treatment and use of ion-exchange resins (colestyramine, colestipol), in severe cases, compensation for the loss of fluid, electrolytes and protein is indicated,

administration of vancomycin or metronidazole.

Do not use drugs that inhibit intestinal motility.

Prolonged use of the drug can cause dysbiosis and, as a result, the development of hypovitaminosis (especially B vitamins).

To prevent dyspeptic phenomena, it is recommended to take the drug with food.

In order to avoid the development of esophagitis or ulcers of the esophagus, it is necessary to take the drug with plenty of water and avoid using the drug immediately before bedtime.

Influence on the ability to drive vehicles and control mechanisms

The effect on the ability to drive vehicles, machines and mechanisms is unknown. In the case of dizziness, blurred vision or double vision, driving vehicles or machinery is not recommended.

Dispersible tablets.