JUnidoks soljutab

Active material: doxycycline
When ATH: J01AA02
CCF: The antibiotic tetracycline
ICD-10 codes (testimony): A00, A01, A03, A04.6, A06, A09, A20, A21, A22, A23, A27, A37, A40, A41, A42, A44, A48.1, A50, A51, A52, A54, A55, A56.0, A56.1, A56.4, A66, A69.2, A70, A71, A74.0, A75, B50, H66, i33, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, J85, J86, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, L70, M86, N10, N11, N30, N34, N41, N45, N70, N71, N72, T79.3
When CSF: 06.06.01
Manufacturer: ASTELLAS PHARMA EUROPE B.V. (Netherlands)

Pharmaceutical form, composition and packaging

Pills round, lenticular, from light yellow to grayish-yellow, with Valium on one party and chasing “173” – another.

Excipients: microcrystalline cellulose, saxarin, giproloza (low substituted), gipromelloza, colloidal silicon dioxide (anhydrous), magnesium stearate, lactose monohydrate.

10 PC. – blisters (1) – packs cardboard.

Pharmacological action

Broad-spectrum antibiotic tetracycline. Bacteriostatic, It inhibits protein synthesis in the bacterial cell by interacting with the ribosome 30S subunit.

It is active against gram-positive and gram-negative bacteria: Streptococcus spp., Treponema 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. (incl. Rickettsia prowazekii), 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. (other than Clostridium difficile), Actinomyces spp., Fusobacterium fusiforme, Calymmatobacterium granulomatosis, Propionibacterium acnes; some protozoa: Entamoeba spp., Plasmodium falciparum.

Usually, are not active against Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.

It should take into account the possibility of acquired resistance to doxycycline in a number of pathogens, which is often a cross inside the group (ie. strains, resistant to doxycycline, at the same time be resistant to the group of tetracyclines).

Pharmacokinetics

Absorption

Absorption – fast and high (about 100%). Food intake does not significantly affect the absorption of the drug.

C_max doxycycline plasma (2.6-3 ug / ml) achieved through 2 h after administration 200 mg, through 24 hours the concentration of active substance in blood plasma is reduced to 1.5 ug / ml.

Upon receiving 200 mg on the first day of treatment and 100 mg / day on subsequent days doxycycline concentration in plasma is 1.5-3 ug / ml.

Distribution

Doxycycline is reversibly bound to plasma proteins (80-90%), well into tissue, badly – in the cerebrospinal fluid (10-20% concentration in blood plasma), However, the concentration of doxycycline in the cerebrospinal fluid increases in inflammation of the spinal membranes.

V_d – 1.58 l / kg. Through 30-45 min after oral doxycycline found in therapeutic concentrations in the liver, kidney, light, spleen, bones, teeth, prostate, eye tissues, pleural and ascites, bile, synovial exudate, exudate maxillary and frontal sinuses, in crevicular fluid.

In normal liver function levels of the drug in the bile 5-10 times higher, than in plasma.

Saliva is determined 5-27% of doxycycline concentration values ​​in the blood plasma.

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

It accumulates in bone and dentin.

Metabolism

Only a small portion is metabolized doxycycline.

Deduction

T_1/2 after a single oral administration of 16-18 no, after receiving repeated doses – 22-23 no.

About 40% the dose is excreted in the biologically active form by tubular secretion in the kidney, 20-40% output via the intestine in the form of inactive forms (chelates).

Pharmacokinetics in special clinical situations

T_1/2 doxycycline in patients with impaired renal function does not change, tk. increasing its excretion through the intestine.

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

Testimony

Infectious-inflammatory diseases, caused by susceptible to malaria infections:

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

- Infections of upper respiratory tract (incl. otitis, sinusitis, tonsillitis);

- Infections of the genitourinary system (cystitis, pyelonephritis, bacterial prostatitis, uretrit, uretrocistit, urogenital mycoplasmosis, Acute orhiepididimit; endometritis, endocervicitis and salpingo in combined teratoma);

- Infections, Sexually Transmitted Infections (urogenital chlamydiosis, Syphilis in patients intolerant of penicillins, uncomplicated gonorrhea / as an alternative therapy /, inguinal pellets, lymphogranuloma venereum);

- Infections of the gastrointestinal tract and biliary tract (cholera, iersinioz, cholecystitis, kholangit, gastroenterocolitis, batsillyarnaya and dysentery amebnaya, travelers' diarrhea);

- Infections of the skin and soft tissues (including wound infection after being bitten by animals), severe acne (in a combination therapy);

- Other diseases (frambeziya, legionellosis, Chlamydia various localization / incl. prostatitis, proctitis /, rikketsioz, Q fever, Rocky Mountain spotted fever, fever / incl. typhus, Tick-borne relapsing /, Lyme disease / I st. – erythema migrans /, tulyaremiya, plague, actinomycosis, malaria, leptospirosis, psittacosis, ornithosis, Anthrax / incl. pulmonary form /, bartonellez, granulotsitarnyi erlikhioz, pertussis, Brucellosis);

- Infectious diseases of the eye, in a combination therapy – trachoma;

- Osteomyelitis;

- Sepsis;

- Subacute bacterial endocarditis;

- Peritonitis;

Prevention of postoperative purulent complications and malaria, caused by Plasmodium falciparum, during short journeys (less 4 Months) in the territory, where common strains, resistant to chloroquine and / or pyrimethamine-sulfadoxine.

Dosage regimen

The drug is preferably taken with food. The tablets are dissolved in a little water (about 20 ml) to form a suspension. Tablets can also be swallowed whole, divided into parts or chew, drinking water. Typically, the duration of treatment is 5-10 days.

Adults and children over 8 years old with a body weight more 50 kg on the first day of treatment prescribed 200 mg / day 1 or 2 admission, in the following days of treatment – by 100 mg / day 1 reception. When severe infections appoint 200 mg / day during the treatment period.

To children 8-12 years old with a body weight of less than 50 kg Average daily dose – 4 mg / kg on the first day, further – by 2 mg / kg / day (in 1-2 admission). In cases severe infections the drug is prescribed in a dose 4 mg / kg daily during the entire treatment.

For infections, caused by Streptococcus pyogenes, treatment duration of at least 10 days.

At uncomplicated gonorrhea (except anorectal infections in men) adult appoint 100 mg 2 times / day until complete recovery (on average during 7 days), or within one day prescribe 600 mg – by 300 mg 2 admission (a second receiving through 1 hours after the first).

At primary syphilis appoint 100 mg 2 times / day for 14 days, at secondary syphilis – by 100 mg 2 times / day for 28 days.

At uncomplicated urogenital infections, caused by Chlamydia trachomatis, cervicite, negonokokkovom urethra, caused by Ureaplasma urealiticum, appoint 100 mg 2 times / day for 7 days.

At acne appoint 100 mg / day, a course of treatment 6-12 weeks.

To prevention of malaria appoint 100 mg 1 time / day for 1-2 the day before the trip, then – daily during the trip and for the 4 Weeks after his return; older children 8 years – by 2 mg / kg 1 time / day.

To prevention of diarrhea “travelers” – 200 mg on the first day of the trip in 1 or 2 admission, further – by 100 mg 1 time / day for the entire stay in the region (no more 3 weeks).

To treatment of leptospirosis – by 100 mg orally 2 times / day for 7 days; to prevention of leptospirosis – by 200 mg 1 times / week for staying in disadvantaged areas and 200 mg – at the end of travel.

FROM for the prevention of infections in medical abortion appointed 100 mg for 1 hour before and 200 mg after intervention.

The maximum daily dose Adult – to 300 mg / day, or to 600 mg / day for 5 days at Heavy gonococcal infection. To older children 8 years old with a body weight more 50 kg – to 200 mg, to children 8-12 years old with a body weight of less than 50 kg – 4 mg / kg daily during the entire treatment.

At kidney (CC less than 60 ml / min) and / or liver failure requires reduction of the daily dose of doxycycline, since in this case there is a gradual accumulation of it in the body (the risk of hepatotoxicity).

Side effect

From the digestive system: anorexia, nausea, vomiting, dysphagia, diarrhea, enterocolitis, psevdomembranoznыy colitis, liver (during long-term administration or in patients with renal or hepatic insufficiency).

Dermatological reactions: photosensitivity.

Allergic reactions: hives, maculo-papular and erythematous rash, angioedema, anaphylactic reactions, perikardit, exacerbation of systemic lupus erythematosus, exfoliative dermatitis.

From the hematopoietic system: gemoliticheskaya anemia, thrombocytopenia, neutropenia, eozinofilija, reduction in the activity of prothrombin.

On the part of the endocrine system: patients, receiving long-term doxycycline, possible reversible dark brown staining of thyroid tissue.

CNS: benign intracranial hypertension (anorexia, vomiting, headache, swelling of the optic nerve), vestibular disorders (dizziness or unsteadiness).

From the urinary system: increase in BUN (by antianabolicheskogo effect).

On the part of the musculoskeletal system: doxycycline zamedlяet osteogenesis, It interferes with the normal development of teeth in children (irreversibly alter the color of teeth, developing enamel hypoplasia).

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

Contraindications

- Severe liver and / or kidney;

- Porphyria;

- Pregnancy;

- Lactation (breast-feeding);

- Children up to age 8 years;

- Hypersensitivity to the antibiotic tetracycline.

Pregnancy and lactation

JUnidoks Soljutab^® contraindicated during pregnancy.

The drug is contraindicated during lactation (breast-feeding). Doxycycline is excreted in breast milk.

Cautions

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

Tetracyclines can increase prothrombin time, appointment of tetracycline in patients with coagulopathies should be carefully monitored.

Antianabolichesky effect of tetracyclines may cause an increase in residual blood urea nitrogen. Usually, it is not significant in patients with normal renal function. However, in patients with renal insufficiency may be observed the growth of azotemia. 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 photodermatitis need to limit sun exposure during treatment and during 4-5 days after.

Long term use may cause a dysbacteriosis and thereby – the development of hypovitaminosis (especially B vitamins).

To prevent dyspepsia is recommended to take the drug during meals.

Effects on ability to drive vehicles and management mechanisms

Features of influence on the ability to drive and operate machinery has not been studied.

Overdose

Symptoms: increased adverse reactions, cause liver damage – vomiting, febrility, jaundice, azotemia, transaminase elevation, increased prothrombin time.

Treatment: immediately after taking large doses recommended gastric lavage, excessive drinking, if necessary – induction of vomiting. Take activated carbon and osmotic laxatives. Hemodialysis and peritoneal dialysis are not recommended due to the low efficiency.

Drug Interactions

Antacids, aluminum-containing, magnesium, calcium, iron supplements, natriya carbonate, magnesium-containing laxatives reduce the absorption of doxycycline, therefore, their use should be divided three-hour intervals.

In connection with the suppression of intestinal microflora doxycycline decreased prothrombin index, that require dose adjustment of indirect anticoagulants.

When combined with bactericidal antibiotics doxycyline, violating cell wall synthesis (penicillins, cephalosporins), the effectiveness of recent declines.

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 blood plasma.

The simultaneous use of doxycycline and retinol improves intracranial pressure.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at temperature from 15 ° to 25 ° C. Shelf life – 5 years.