Producer: Astellas Pharma Europe B.V. (Astellas of Pharm Yurop B. V.) Netherlands
Code of automatic telephone exchange: J01AA02
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agent: doxycycline of monohydrate of 100,0 mg in terms of doxycycline
Excipients: cellulose microcrystallic, saccharin, the hypro rod (low-replaced), a gipromelloza, silicon dioxide colloid (anhydrous), magnesium stearate, lactoses monohydrate
Round, biconvex tablets from light yellow till gray-yellow color with an engraving "173" (a tablet code) on one party and risky on another.
Pharmacodynamics. An antibiotic of a broad spectrum of activity from group of tetracyclines. Works bacteriostatically, suppresses synthesis of protein in a microbic cell by interaction with 30S in subunit of ribosomes. It is active concerning 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, does not affect Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.
It is necessary to take into account a possibility of the acquired doxycycline resistance at a number of activators which often is cross in group (i.e. the strains steady against doxycycline, at the same time will be steady against all group of tetracyclines).
Absorption - bystry and high (about 100%). Meal slightly influences drug absorption.
The maximum level of doxycycline in a blood plasma (2,6-3 mkg/ml) is reached in 2 h after reception of 200 mg, in 24 h concentration of active agent in a blood plasma decreases to 1,5 mkg/ml.
After reception of 200 mg in the first day of treatment and 100 mg a day in the next days the level of concentration of doxycycline in a blood plasma makes 1,5-3 mkg/ml.
Doxycycline reversibly contacts proteins of plasma (80-90%), well gets into bodies and fabrics, it is bad – in cerebrospinal fluid (10-20% of level in a blood plasma), however concentration of doxycycline in cerebrospinal fluid increases at an inflammation of a spinal cover.
Distribution volume - 1,58 l/kg. In 30–45 minutes after intake doxycycline is found in therapeutic concentration in a liver, kidneys, lungs, a spleen, bones, teeth, a prostate gland, eye tissues, in pleural and ascitic liquids, bile, synovial exudate, exudate of Highmore's and frontal sinuses, in liquid of gingival furrows.
At normal function of a liver drug level in bile is 5-10 times higher, than in plasma.
In saliva 5-27% of the size of concentration of doxycycline in a blood plasma are defined.
Doxycycline gets through a placental barrier, in small amounts cosecretes in breast milk.
Collects in dentine and a bone tissue.
Insignificant part of doxycycline is metabolized.
The elimination half-life after a single dose inside makes 16-18 h, after reception of repeated doses – 22-23 h.
About 40% of the accepted drug are excreted by kidneys and 20 - 40% are removed through intestines in the form of inactive forms (chelates).
Pharmacokinetics in special clinical cases
The drug elimination half-life at patients with renal failures does not change since its excretion through intestines increases.
The hemodialysis and peritoneal dialysis do not influence concentration of doxycycline in a blood plasma.
Indications to use:
The infectious and inflammatory diseases caused by sensitive
to drug microorganisms:
- respiratory infections, including pharyngitis, acute bronchitis, exacerbation of a chronic obstructive pulmonary disease, tracheitis, bronchial pneumonia, share pneumonia, community-acquired pneumonia, lung abscess, pleura empyema;
- infections of urinogenital system: cystitis, pyelonephritis, bacterial prostatitis, an urethritis, an urethrocystitis, urogenital mycoplasmosis, acute orkhiepididimit; the endometritis, an endocervicitis also salpingoofiorit as a part of the combined teratiya; including infections, sexually transmitted: urogenital clamidiosis, syphilis at patients with intolerance of penicillin, uncomplicated gonorrhea (as alternative therapy), an inguinal granuloma, a venereal lymphogranuloma;
- infections of skin and soft tissues (including wound fevers after a sting of animals), a serious acne illness (as a part of a combination therapy);
- other diseases: a frambeziya, legionellosis, clamidiosis of various localization (including prostatitis and a proctitis), a rickettsiosis, Ku's fever, spotty fever of the Rocky Mountains, typhus (including sypny, tick-borne returnable), Lyme's disease (the I Art. - erythema migrans), a tularemia, plague, an actinomycosis, malaria; infectious diseases of eyes, as a part of a combination therapy – trachoma; hay fever, psittacosis, ornithosis, malignant anthrax (including pulmonary form), bartonellosis, granulotsitarny эрлихиоз; whooping cough, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;
- Prevention of postoperative purulent complications; the malaria caused by Plasmodium falciparum at short-term travel (less than 4 months) in the territory where the strains steady against chloroquine and/or Pyrimethaminum sulphadoxine are widespread.
Route of administration and doses:
Usually duration of treatment makes 5-10 days. Tablets dissolve in a small amount of water (about 20 ml) with receiving suspension, it is also possible to swallow entirely, to divide into parts or to chew, washing down with water. It is preferable to accept during food.
To adults and children 8 years with body weight more than 50 kg are more senior appoint 200 mg in 1-2 receptions in the first day of treatment, further on 100 mg daily. In cases of heavy infections of Yunidoks appoint in a dose 200 mg daily during all treatment.
Children are 8-12 years old with body weight less than 50 kg an average daily dose - 4 mg/kg in the first day, further - on 2 mg/kg a day (in 1-2 receptions). In cases of heavy infections of Yunidoks appoint in a dose 4 mg/kg daily during all treatment.
Features of dosing at some diseases
At the infection caused by S.pyogenes of Yunidoks accept not less than 10 days.
At uncomplicated gonorrhea (except for anorectal infections at men):
The adult appoint 100 mg two times a day before full treatment (on average within 7 days), or within one day appoint 600 mg - on 300 mg in 2 receptions (the second reception in 1 h after the first).
At primary syphilis appoint 100 mg twice a day within 14 days, at secondary syphilis - on 100 mg twice a day within 28 days.
At the uncomplicated urogenital infections caused by Chlamydia trachomatis, a cervicitis, not gonococcal urethritis caused by Ureaplasma urealiticum appoint 100 mg 2 times a day within 7 days.
At acne rash appoint 100 mg/days, a course of treatment of 6-12 weeks.
Malaria (prevention): on 100 mg of 1 times a day in 1-2 days prior to a trip, then daily during a trip and within 4 weeks after return; to children 8 years on 2 mg/kg of 1 times a day are more senior.
Diarrhea of "travelers" (prevention) – 200 mg in the first day of a trip (for 1 reception or on 100 mg 2 times a day), further on 100 mg of 1 times a day during all stay in the region (no more than 3 weeks).
Treatment of a hay fever - on 100 mg in 2 times a day within 7 days; prevention of a hay fever - on 200 mg once a week during stay in the unsuccessful area and on 200 mg at the end of a trip.
For the purpose of prevention of infections at medical abortion appoint 100 mg in 1 hour prior to and 200 mg after intervention.
The maximum daily doses for adults - to 300 mg/days or to 600 mg/days within 5 days at heavy gonococcal infections. For children 8 years with body weight more than 50 kg – to 200 mg, for children of 8-12 years with body weight less than 50 kg – 4 mg/kg daily during all treatment are more senior.
In the presence of renal (клириенс creatinine less than 60 ml/min.) and/or a liver failure decrease in a daily dose of doxycycline as at the same time there is its gradual accumulation in an organism (risk of a hepatotoxic action) is required.
Features of use:
There is a possibility of cross stability and hypersensitivity with other drugs of a tetracycline row.
Tetracyclines can increase a prothrombin time, purpose of tetracyclines at patients with coagulopathies has to be controlled carefully.
The anti-anabolic effect of tetracyclines can lead to increase in level of residual nitrogen of urea in blood. As a rule, it has no essential value for patients with normal function of kidneys. However at patients with a renal failure increase of an azotemia can be observed. Use of tetracyclines for patients with a renal failure demands medical control.
At prolonged use of drug periodic control of laboratory indicators of blood, function of a liver and kidneys is required.
Due to the possible development of a photodermatitis restriction of insolation is necessary during treatment and within 4-5 days after it.
Prolonged use of drug can cause dysbacteriosis and thereof – development of a hypovitaminosis (especially group B vitamins).
For prevention of the dispeptic phenomena it is recommended to accept drug during food.
Features of influence on ability to drive the car and to manage mechanisms were not investigated.
Dermatological and allergic reactions:
small tortoiseshell, photosensitization, Quincke's disease, anaphylactic reactions, aggravation of a system lupus erythematosus, makulopapulezny and erythematic rash, pericardis, exfoliative dermatitis.
From a liver:
damage of a liver (at long administration of drug or at patients with a renal or liver failure).
From kidneys: the increase in residual nitrogen of urea caused by anti-anabolic effect of drug.
From system of a hemopoiesis:
hemolitic anemia, thrombocytopenia, neutropenia, eosinophilia, decrease of the activity of a prothrombin.
From a nervous system:
high-quality increase in intracranial pressure (anorexia, vomiting, headache, hypostasis of an optic nerve), vestibular disturbances (dizziness or instability).
From a thyroid gland:
at patients, it is long receiving doxycycline, perhaps reversible dark brown prokrashivaniye of tissue of thyroid gland.
From teeth and bones:
doxycycline slows down bone formation, breaks normal development of teeth in children (it is irreversible color of teeth changes, the enamel hypoplasia develops).
candidiasis (stomatitis, glossitis, proctitis, vaginitis) as manifestation of superinfection.
Interaction with other medicines:
The antacids containing aluminum, magnesium, calcium, iron preparations, Natrii hydrocarbonas, magnesium - the containing laxatives reduce doxycycline absorption therefore their use has to be divided by an interval of 3 h.
Due to the suppression by doxycycline of intestinal microflora the prothrombin ratio decreases that demands dose adjustment of indirect anticoagulants.
At a doxycycline combination to the bactericidal antibiotics breaking synthesis of a cell wall (penicillin, cephalosporins), efficiency of the last decreases.
Doxycycline reduces reliability of contraception and increases the frequency of acyclic bleedings at reception estrogen - the containing hormonal contraceptives.
Ethanol, barbiturates, rifampicin, carbamazepine, Phenytoinum, etc. stimulators of a microsomal oxidation, accelerating doxycycline metabolism, reduce its concentration in a blood plasma.
Simultaneous use of doxycycline and Retinolum promotes increase in intracranial pressure.
- hypersensitivity to tetracyclines
- age up to 8 years
- heavy abnormal liver functions and/or kidneys
Strengthening of the side reactions caused by injury of a liver – vomiting, a feverish condition, jaundice, an azotemia, increase in level of transaminases, increase in a prothrombin time.
Right after reception of high doses recommend a gastric lavage, plentiful drink, if necessary - induction of vomiting. Accept absorbent carbon and osmotic laxatives. The hemodialysis and peritoneal dialysis is not recommended in view of a low performance.
At a temperature from 15 to 25 ºС. To store in places unavailable to children! Period of validity: 5 years. Not to use after the period of validity specified on packaging.
According to the recipe
Tablets the dispersed 100 mg; on 10 tablets in the blister from PVC / aluminum foil. On 1 blister together with the application instruction in a cardboard pack.