Doxycycline

General characteristics. Structure:

International and chemical names: doxycycline; hydrochloride гемиэтанол гемигидрат (4S, 4aR, 5S, 5aR, 6R, 12aS)-4 (dimethylamines) -3,5,10,12,12а-пентагидрокси-6-метил-1,11-диоксо-1,4,4а,5,5а,6,11,12а-октагидротетрацен-2-карбоксамида;основные physical and chemical properties: the solid capsules with a lid and the case of yellow color containing powder of color, yellow with a greenish shade. White impregnations are allowed; structure: 1 capsule contains 100 mg of doxycycline of a hiklat in terms of doxycycline; excipients: lactoses monohydrate, potato starch, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Doxycycline – a semi-synthetic antibiotic of group of tetracyclines of a broad spectrum of activity. Causes bacteriostatic action due to oppression of synthesis of protein of activators as a result of communication blocking aminoacyl - acceptor RNA (TRNK) with the "information RNA (IRNK)-a ribosome" complex.
It is active in relation to gram-positive bacteria: to aerobic cocci – Staphylococcus spp. (including producing a penicillinase), Streptococcus spp. (including Streptococcus pneumoniae); to aerobic spore-forming bacteria – Bacillus anthracis; to aerobic asporous bacteria – Clostridium spp. Doxycycline is active also in relation to gram-negative bacteria: to aerobic cocci – Neisseria gonorrhoeae; to aerobic bacteria – Escherichia coli; Shigella spp., Salmonella spp., Enterobacter spp., Klebsiella spp., Bordetella pertussis, and also in relation to Rickettsia spp., Treponema spp., Mycoplasma spp., Chlamydia spp.
Pseudomonas aeruginosa, Proteus spp are steady against effect of doxycycline., Serratia spp., majority of strains of Bacteroides fragilis.

Pharmacokinetics. Drug is quickly soaked up from a digestive tract and slowly removed from an organism; depending on a dose therapeutic concentration in blood remains during 18 – 24 h. Contacts blood proteins for 80 – 90%. It is quickly distributed in the majority of liquids of an organism, including bile, a secret of okolonosovy bosoms, a pleural exudate, synovial and ascitic liquids. Concentration in cerebrospinal fluid varies and after parenteral use can make 10 – 25% of concentration in blood serum. A drug elimination half-life – 12 – 22 h. A considerable part is removed in an invariable view with excrements, about 40% – with urine.

Indications to use:

The infections caused by microorganisms, sensitive to Doksitsiklin, including: respiratory organs and ENT organs, digestive tract, purulent infections of skin and soft tissues (including acne rash), bodies of urinogenital system (including gonorrhea, primary and secondary syphilis), sapropyra, brucellosis, rickettsioses, osteomyelitis, trachoma, clamidioses, tropical malaria, cholera, hay fever.

Route of administration and doses:

Appoint Doxycycline inside to adults and children of 12 years. Appoint in the first day of treatment 200 mg a day. In the next days – on 100 – 200 mg a day, depending on weight of a clinical course of a disease. Frequency rate of reception – 1 – 2 time a day.
Duration of a course of treatment is established individually, continuing treatment not less than 24 - 48 hours after disappearance of symptoms of a disease and normalization of body temperature.
At treatment of gonorrhea Doxycycline is appointed: a sick acute uncomplicated urethritis – in a course dose of 500 mg (the 1st reception – 300 mg, the subsequent 2 receptions – on 100 mg with an interval of 6 h); at the complicated gonorrhea form the course dose of an antibiotic (800 – 900 mg) is divided into 6 - 7 receptions (300 mg on the 1st reception, on 100 mg with an interval of 6 h – on 5 – 6 subsequent receptions).
At not complicated infections of an urethra, neck of uterus and a rectal zone caused by Chlamydia trachomatis – 100 mg 2 times a day, not less than 7 days.
At the orchitis or an epididymite caused by Chlamydia trachomatis or Neisseria gonorrhoeae, –100 mg 2 times a day; treatment duration – not less than 10 days.
At infections of generative organs at the men called by Ureaplasma urealyticum, the patient and his sexual partner have to receive medical treatment for drug in a dose of 100 mg 2 times a day within 4 weeks.
At primary and secondary syphilis the daily dose of drug makes 300 mg for several receptions, a course of treatment – not less than 10 days.
For treatment of the tropical malaria steady against chloroquine, drug is used in a daily dose 200 mg by not less than 7 days. For prevention of malaria – 100 mg a day for adults. Preventive treatment can be begun for 1 – 2 day to a trip to the region with an unreliable epidemic situation and to continue for 4 weeks after return from it.
Treatment of patients with returnable and a sapropyra is carried out by single use of drug in a dose by 100 – 200 mg.
For treatment and prevention of cholera at adults inside appoint 300 mg of Doxycycline once; for prevention of the Japanese river fever – once 200 mg of drug.
For treatment of a hay fever drug is appointed on 100 mg by 2 times a day within 7 days.

Features of use:

Drug is accepted inside, after food (in order to avoid irritation of a mucous membrane of a stomach), washing down with a large amount of water.
For prevention of development of candidiases along with Doxycycline it is recommended to appoint nystatin or levorinum.
It is incompatible with the drugs having alkaline рН and also with unstable in acid medium (Aminophyllinum, a hydrocortisone, erythromycin).
At hepatonephric insufficiency drug is used under control of a functional condition of a liver and kidneys.
Perhaps tranzitorny increase in content in blood of hepatic aminotransferases, alkaline phosphatase, bilirubin.
Do not apply during pregnancy as, getting through a placenta, drug can break normal development of teeth, cause oppression of growth of bones of a skeleton of a fruit, and also fatty infiltration of a liver.
In case of need uses of drug in the period of a lactation it is necessary to stop feeding by a breast.
Doxycycline is not appointed to children up to 8 years as tetracyclines, including Doksitsiklin, cause long-term discoloration of teeth and a hypoplasia of enamel, oppression of longitudinal growth of bones of a skeleton. To children from 8 to 12 years drug in this dosage form is not appointed.
There are no references that drug can negatively influence drivers and people who work with the equipment.

Side effects:

The loss of appetite, nausea, vomiting, diarrhea, lock, glossitis, dysphagy, stomatitis, gastritis, proctitis, candidiasis are possible. There can be allergic skin reactions, a Quincke's edema.
From bodies of a hemopoiesis the neutropenia, thrombocytopenia, hemolitic anemia are possible.
It is necessary to be careful at a renal failure, a liver (cumulation of drug and a hepatotoxic action of high concentration are possible). Drug causes a photosensitization, discoloration of teeth in children.

Interaction with other medicines:

The hydrosodium carbonate, antacids containing salts of aluminum, bismuth, magnesium, iron preparations of calcium reduce absorption of Doxycycline and its level in a blood plasma, forming inactive chelates in this connection it is necessary to avoid their simultaneous appointment with drug.
At simultaneous use with barbiturates, carbamazepine, Phenytoinum concentration of Doxycycline in a blood plasma decreases in connection with induction of microsomal enzymes that can be the cause of reduction of its antibacterial action.
It is necessary to avoid a drug combination with the penicillin, cephalosporins having bactericidal effect and being antagonists of bacteriostatic antibiotics, including Doksitsiklin.

Contraindications:

Drug is contraindicated at hypersensitivity to tetracyclines, at fungus diseases, during the periods of pregnancy and feeding by a breast, to children up to 8 years.
With care apply it at abnormal liver functions and kidneys.

Overdose:

So far about cases of overdose of drug it was not reported.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in a blister strip packaging, on 1 packaging in a pack.