Unidox Solutab, 100 mg 10 pcs

Pharmacological action – antibacterial, bacteriostatic.

Inhibits protein synthesis in the microbial cell by disrupting the connection of the ribosomal membrane RNA transport.

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 granulomatis, 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 Cmax of doxycycline in blood plasma (2.6-3 mcg/ml) is reached 2 hours after taking 200 mg, after 24 hours the concentration of active substance in blood plasma decreases to 1.5 mcg/ml.

After administration of 200 mg on the first day of treatment and 100 mg/day on subsequent days, 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 the cerebrospinal fluid (10-20% of plasma levels), but doxycycline concentration in the 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 drug level in bile is 5-10 times higher than in plasma.

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

Doxycycline penetrates the placental barrier, in small amounts is secreted into breast milk.

Accumulates in dentin and bone tissue.

Metabolism

A small portion of doxycycline is metabolized.

Elevation

The T1/2 after a single oral dose is 16-18 hours, after repeated doses is 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 intestine increases.

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

Indications

– 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);

– ENT-organ infections (including

– infections of the ENT-organ (including otitis, sinusitis, tonsillitis);

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

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

– gastrointestinal and biliary tract infections (cholera, yersiniosis, cholecystitis, cholangitis, gastroenterocolitis, bacillary and amebic dysentery, traveler’s diarrhea);

p> – skin and soft tissue infections (including wound infections after an animal bite), severe acne (as part of combination therapy);

– other diseases: yaws, legionellosis, chlamydia of various localizations (incl.Prostatitis and proctitis), rickettsiosis, Q fever, Rocky Mountain spotted fever, typhoid fever (including rash, tick-borne return fever), Lyme disease (stage I) – erythema migrans/, tularemia, plague, actinomycosis, malaria, leptospirosis, psittacosis, ornithiasis, anthrax (including Infectious diseases of the eye (in the combined therapy) – trachoma;

Infectious diseases of the eye (in the combined therapy) – trachoma. Prevention of postoperative purulent complications and malaria caused by Plasmodium falciparum, with short-term travel (less than 4 months) in areas where strains resistant to chloroquine and/or pyrimethamine-sulfadoxine are common.

Active ingredient

Composition

Active ingredient:

doxycycline monohydrate, in terms of doxycycline 100 mg.

Auxiliary substances:

Microcrystalline cellulose – 45 mg,

saccharin – 10 mg,

Hyprolose (low substituted) – 18.75 mg,

Hypromellose – 3.75 mg,

colloidal silica (anhydrous) – 0.625 mg,

magnesium stearate – 2 mg,

lactose monohydrate – up to 250 mg.

How to take, the dosage

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

The drug is preferably taken with food. The tablets are taken sitting or standing, which reduces the chance of developing esophagitis and esophageal ulcers. The drug should not be taken immediately before going to bed.

The treatment usually lasts 5-10 days.

Adults and children over 8 years of age with body weight over 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/day in 1 dose. In case of severe infections 200 mg/day is prescribed during the whole period of treatment.

Interaction

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

The prothrombin index decreases due to the suppression of gut microflora by doxycycline, which requires adjustment of the dose of indirect anticoagulants.

When doxycycline is combined with bactericidal antibiotics that disrupt the synthesis of the cell wall (penicillins, cephalosporins), the effectiveness of the latter is reduced, which should be considered in the treatment of 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, by accelerating the metabolism of doxycycline, reduce its concentration in plasma.

The concomitant use of doxycycline and retinol promotes increased intracranial pressure.

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.

In case of long-term use of the drug it is necessary to periodically control 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 and 2-3 weeks after discontinuation of treatment it is possible to develop diarrhea caused by Clostridium dificile. In mild cases discontinuation of treatment and use of ion exchange resins (colestyramine, colestipol) is sufficient, in severe cases reimbursement of loss of fluid, electrolytes and protein is indicated,

Prescription of vancomycin or metronidazole.

Drugs that inhibit intestinal peristalsis should not be used.

Long-term use of the drug can cause dysbiosis and, consequently, development of hypovitaminosis (especially of B vitamins).

To prevent dyspeptic complaints, it is recommended that the drug be taken with food.

To prevent esophagitis or esophageal ulcers, take the drug with plenty of water and avoid taking the drug just before bedtime.

The effect on the ability to drive and operate machinery

There is no known effect on the ability to drive vehicles, machines and mechanisms. If dizziness, blurred vision or double vision develops, driving or operating machinery is not recommended.

Contraindications

– hypersensitivity to antibiotics of the tetracycline group.

– severe hepatic and/or renal dysfunction;

– porphyria;

– childhood under 8 years of age;

Side effects

Digestive system disorders: anorexia, nausea, vomiting, dysphagia, diarrhea, enterocolitis, pseudomembranous colitis, esophagitis, esophageal ulcer, dark staining of the tongue, liver damage (during long-term use or in patients with renal or hepatic impairment), cholestasis.

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

Allergic reactions: urticaria, angioneurotic edema, anaphylactic reactions, exacerbation of systemic lupus erythematosus, pericarditis, serum-like syndrome, erythema multiforme.

Hematopoietic system disorders: hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, decreased prothrombin activity.

Endocrine system disorders: in patients who received doxycycline for a long time, reversible dark brown staining of thyroid tissue is possible.

CNS disorders: benign increase in intracranial pressure (anorexia, vomiting, headache, optic nerve edema), vestibular disorders (dizziness or unsteadiness), blurred vision, double vision.

Urinary system: increase in residual urea nitrogen (due to anti-anabolic effect).

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

Others: candidiasis (glossitis, stomatitis, proctitis, vaginitis) as a manifestation of superinfection.

Overdose

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, plenty of drinking, inducing vomiting if necessary are recommended. Activated carbon and osmotic laxatives are taken. Hemodialysis and peritoneal dialysis are not recommended due to low effectiveness.

Similarities