Composition, form of production and packaging
Tablets are dispersible round, biconvex, from light yellow or gray-yellow to brown with impregnations, with engraving "173" (tablet code) on one side and risk on the other.
doxycycline monohydrate, in terms of doxycycline, 100 mg
Auxiliary substances: microcrystalline cellulose - 45 mg, saccharin - 10 mg, giprolose (low substituted) - 18.75 mg, hypromellose - 3.75 mg, silicon dioxide colloid (anhydrous) - 0.625 mg, magnesium stearate - 2 mg, lactose monohydrate - up to 250 mg.
10 pieces. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
Antibiotic of a broad spectrum of action from the group of tetracyclines. It acts bacteriostatically, suppresses protein synthesis in the microbial cell by interacting with the 30S subunit of ribosomes.
It is active against gram-positive and gram-negative aerobic and anaerobic bacteria: Streptococcus spp., Staphylococcus spp., Klebsiella spp., Enterobacter spp.(including Enterobacter aerugenes), Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Chlamydia spp., Mycoplasma spp., Ureaplasma urealyticum, Listeria monocytogenes, Rickettsia spp., 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, Treponema spp., Typhus exanthematicus;Some protozoa: Entamoeba spp., Plasmodium falciparum.
It is generally not active against Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.
The possibility of acquired resistance to doxycycline in a number of pathogens, which is often cross-over within the group (ie, strains resistant to doxycycline, will also be resistant to the entire tetracycline group) should be taken into account.
Absorption is fast and high (100%). The intake of food has a slight effect on the absorption of the drug, which has no clinical significance.
C max doxycycline in blood plasma (2.6-3 Ојg / ml) is achieved 2 hours after taking 200 mg, after 24 hours the concentration of active substance in the blood plasma is reduced to 1.5 Ојg / ml.
After taking 200 mg on the first day of treatment and 100 mg / day on subsequent days, the concentration of doxycycline in the blood plasma is 1.5-3 Ојg / ml.
Doxycycline reversibly binds to plasma proteins (80-90%), penetrates well into tissues, poorly into spinal fluid (10-20% of plasma concentration), but the concentration of doxycycline in the cerebrospinal fluid increases with inflammation of the spinal cord.
V d - 1.58 l / kg. After 30-45 minutes after ingestion, 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, exudate of maxillary sinuses and frontal sinuses, in fluid of the gingival sulci.
With normal liver function, the level of the drug in the bile is 5-10 times higher than in the plasma.
In saliva, 5-27% of the concentration of doxycycline in the blood plasma is determined.
Doxycycline penetrates the placental barrier, in small quantities is secreted into breast milk.
Accumulates in dentin and bone tissue.
Metabolized only a small part of the doxycycline.
T 1/2 after a single oral intake is 16-18 hours, after taking repeated doses - 22-23 hours.
Approximately 40% of the dose taken is excreted in the biologically active form by tubular secretion in the kidney, 20-40% is excreted through the intestines in the form of inactive forms (chelates).
Pharmacokinetics in special clinical cases
T1 / 2 doxycycline in patients with impaired renal function does not change, because increases its excretion through the intestine.
Hemodialysis and peritoneal dialysis do not affect the concentration of doxycycline in the blood plasma.
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- respiratory tract infections (including pharyngitis, acute bronchitis, exacerbation of COPD, tracheitis, bronchopneumonia, lobar pneumonia, community-acquired pneumonia, lung abscess, pleural empyema);
- infections of the ENT organs (including otitis media, sinusitis, tonsillitis);
- infections of the genitourinary system (cystitis, pyelonephritis, bacterial prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, acute orchypididymitis, endometritis, endocervicitis and salpingo-oophoritis);
- Sexually transmitted infections (urogenital chlamydia, syphilis in patients with penicillin intolerance, uncomplicated gonorrhea / as alternative therapy /, inguinal granuloma, venereal lymphogranuloma);
- infections of the gastrointestinal tract and bile ducts (cholera, iersiniosis, cholecystitis, cholangitis, gastroenterocolitis, bacillary and amoebic dysentery, travelers' diarrhea);
- 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 different localization (including prostatitis and proctitis), rickettsiosis, fever Koo, spotty fever of the Rocky Mountains, typhus (including swelling, tick-borne recurrent), Lyme disease (stage I ) - erythema migrans /, tularemia, plague, actinomycosis, malaria, leptospirosis, psittacosis, ornithosis, anthrax (including pulmonary form), bartonellosis, granulocyte erlichiosis, whooping cough, brucellosis;
- infectious diseases of the eyes (as part of combination therapy) - trachoma;
- subacute septic endocarditis;
Prevention of postoperative purulent complications and malaria caused by Plasmodium falciparum, with short trips (less than 4 months) in the area where strains resistant to chloroquine and / or pyrimethamine sulfadoxine are common.
Usually the duration of treatment is 5-10 days.
The tablets are dissolved in a small amount of water (about 20 ml) to obtain a suspension. Tablets can also be swallowed whole, divided into parts or chewed, washed down with water.
The drug is preferably taken with food. Take pills sitting or standing, which reduces the likelihood of esophagitis and ulcers of the esophagus. The drug should not be taken immediately before bedtime.
Adults and children older than 8 years with a body weight of more than 50 kg on the first day of treatment appoint 200 mg / day in 1 or 2 admission, in the following days of treatment - 100 mg / day in 1 reception. In the case of severe infections , 200 mg / day are prescribed throughout the 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 at 2 mg / kg / day (1-2 times). In cases of severe infections, the drug is prescribed at a dose of 4 mg / kg daily throughout the treatment.
With infection caused by Streptococcus pyogenes , the duration of treatment is at least 10 days.
For uncomplicated gonorrhea (except for anorectal infections in men), adults are prescribed 100 mg 2 times / day until complete recovery (on average for 7 days) or within one day 600 mg are prescribed - 300 mg in 2 divided doses (second dose 1 hour after the first).
When primary syphilis is prescribed for 100 mg 2 times / day for 14 days, with secondary syphilis - 100 mg 2 times / day for 28 days.
In uncomplicated urogenital infections caused by Chlamydia trachomatis, cervicitis, non-gonococcal urethritis caused by Ureaplasma urealiticum , 100 mg 2 times / day are prescribed for 7 days.
With acne , 100 mg / day are prescribed, and the course of treatment is 6-12 weeks.
For the prevention of malaria appoint 100 mg 1 time / day for 1-2 days before travel, then - daily during the trip and within 4 weeks after return; children older than 8 years - 2 mg / kg 1 time / day. The duration of prevention should not exceed 4 months.
To prevent traveler's diarrhea - 200 mg on the first day of travel in 1 or 2 admission, then - 100 mg 1 time / day during the 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 1 time / week during stay in a dysfunctional area and 200 mg - at the end of the trip.
To prevent infections, medical abortion is prescribed 100 mg per hour before and 200 mg after the intervention.
Maximum daily doses for adults - up to 300 mg / day or 600 mg / day for 5 days with severe gonococcal infection . For children older than 8 years with a body weight of more than 50 kg - up to 200 mg, for children 8-12 years with a body weight of less than 50 kg - 4 mg / kg daily for the entire treatment.
In renal (KK less than 60 ml / min) and / or liver failure , a daily dose of doxycycline is required, since this gradually accumulates in the body (the risk of hepatotoxic action).
From the digestive system: anorexia, nausea, vomiting, dysphagia, diarrhea, anal itching, esophagitis, ulcer of the esophagus, dark staining of the tongue. With prolonged therapy, a deficiency of B vitamins can be observed in connection with the suppression of vitamin B-producing bacteria growth in the normal intestinal microflora.
On the part of the liver: liver damage, sometimes associated with pancreatitis (with long-term drug intake or in patients with renal or hepatic insufficiency), cholestasis.
Allergic reactions: urticaria, angioedema, anaphylactic reactions, exacerbation of systemic lupus erythematosus, a syndrome similar to serum sickness, erythema multiforme, lowering of blood pressure, tachycardia, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms (DRESS- syndrome).
On the part of the skin: photosensitization, maculopapular and erythematous rash, exfoliative dermatitis, purpura Shenlaine-Henoch, photoionicholysis.
From the cardiovascular system: pericarditis.
From the urinary system: an increase in residual urea nitrogen, caused by the anti-anabolic effect of the drug, aggravation of azotemia in patients with renal insufficiency. The use of products containing citric acid against the background of doxycycline may cause symptoms similar to Fanconi syndrome: albuminuria, glucosuria, hypophosphatemia, hypokalemia and renal tubular acidosis.
From the hemopoietic system: hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, decreased prothrombin activity.
From the side of the nervous system: a benign increase in intracranial pressure (anorexia, vomiting, headache, tinnitus, tremor, edema of the optic nerve), vestibular disorders (dizziness or instability), hallucinations, blurred vision, scotoma, double vision.
From the side of the thyroid gland: in patients who have been receiving antibiotics from the tetracycline group for a long time, a reversible dark brown staining of the thyroid tissue is possible, in most cases not accompanied by a violation of its function.
From the musculoskeletal system: doxycycline slows down osteogenesis, disrupts the normal development of teeth in children (the color of teeth changes irreversibly, hypoplasia of enamel develops), arthralgia, myalgia.
Other: superinfection - candidiasis, glossitis, staphylococcal enterocolitis, pseudomembranous colitis, anogenital candidiasis, stomatitis and vaginitis.
- Severe violations of the liver and / or kidney function;
- the period of lactation (breastfeeding);
- Children's age till 8 years;
- hypersensitivity to antibiotics of the tetracycline group.
PREGNANCY AND LACTATION
Doxycycline penetrates the hemato-placental barrier. Tetracyclines have an adverse effect on the fetus (slowing osteogenesis) and on the formation of tooth enamel (irreversible color change, hypoplasia). In view of this, as well as an increased risk of liver damage in the mother, tetracyclines are not used in pregnancy, except when the drug is the only remedy for the treatment or prevention of particularly dangerous and severe infections (spotted fever of the rocky mountains, inhalation effects of Bacillus anthracis and others).
Before prescribing doxycycline to women of childbearing age , pregnancy should be excluded.
Doxycycline penetrates into breast milk. Due to adverse effects on the fetus, doxycycline, like other tetracyclines, is not used during breastfeeding. In the event that the appointment of tetracyclines is necessary, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal dysfunction.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
Patients with impaired liver function Unidox Solutab В® is prescribed only if it is not possible to treat other drugs.
In case of violations of the liver function, a dose reduction is necessary.
APPLICATION FOR CHILDREN
Contraindicated in childhood to 8 years.
There is the possibility of cross-resistance and hypersensitivity with other drugs of the tetracycline series.
Tetracyclines may increase prothrombin time, the appointment of tetracyclines in patients with coagulopathies should be carefully 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 insufficiency, an increase in azotemia may occur. The use of tetracyclines in patients with impaired renal function requires medical supervision.
With prolonged use of the drug requires periodic monitoring of laboratory blood parameters, liver and kidney function.
In connection with the possible development of photodermatitis, it is necessary to limit insolation during treatment and for 4-5 days after it.
With the use of the drug, both in the background of taking and 2-3 weeks after discontinuation of treatment, it is possible to develop diarrhea caused by Clostridium difficile. In mild cases, it is sufficient to cancel treatment and use ion-exchange resins (colestyramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole.
Do not use drugs that inhibit the intestinal motility.
Prolonged use of the drug may cause dysbacteriosis and, as a result, the development of hypovitaminosis (especially B vitamins).
To prevent dyspeptic phenomena, it is recommended to take the drug while eating.
To avoid the development of esophagitis or ulcers of the esophagus, it is necessary to take the drug with a lot of water and avoid the use of the drug just before bedtime.
Impact on the ability to drive vehicles and manage mechanisms
It is not known how to influence the ability to drive vehicles, machines and mechanisms. In the case of dizziness, blurred vision or double vision in the eyes, management of vehicles or mechanisms is not recommended.
Symptoms: increased adverse reactions caused by liver damage - vomiting, febrile condition, jaundice, azotemia, increased transaminase levels, increased prothrombin time.
Treatment: immediately after taking large doses, it is recommended to wash the stomach, drink plenty, if necessary - induce vomiting. Take activated charcoal and osmotic laxatives. Hemodialysis and peritoneal dialysis is not recommended due to low efficiency.
Antacids containing aluminum, magnesium, calcium, iron preparations, sodium hydrogen carbonate, magnesium-containing laxatives reduce the absorption of doxycycline, so their use should be separated by a 3-hour interval.
In connection with the suppression of intoxic microflora by doxycycline, the prothrombin index decreases, which requires correction of the dose of indirect anticoagulants.
When doxycilin is combined with bactericidal antibiotics that disrupt the cell wall synthesis (penicillins, cephalosporins), the efficacy of the latter is reduced, which should be taken into account 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, speeding up the metabolism of doxycycline, reduce its concentration in the blood plasma.
Simultaneous use of doxycycline and retinol helps increase intracranial pressure.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of 15 В° to 25 В° C. Shelf life - 5 years.