Tetracycline

General characteristics. Structure:

International and chemical names: tetracycline; (4S, 4aS, 5aS, 6S, 12aS) -4-диметиламино-1,4,4a,5,5а,6,11,12а-октагидро-3,6,10,12,12а-пентагидрокси-6-метил-1,11-диоксонафтацен-2-карбокса-мида hydrochloride; main physical and chemical properties: tablets, coated from red till red-brown color, a round form, with a biconvex surface. On cross section the kernel surrounded with a cover layer is visible; structure: 1 tablet contains 100 mg of tetracycline of a hydrochloride in terms of 100% substance;
excipients: starch of kartofelniya, sugar, gelatin, talc, calcium stearate, methyl cellulose, titanium dioxide, polysorbate 80, понсо 4R, beeswax, liquid paraffin.

Pharmacological properties:

Pharmacodynamics. Bacteriostatic antibiotic of group of tetracyclines of a broad spectrum of activity. Aminoacyl - acceptor RNA (TRNK) with the "information RNA (IRNK)-a ribosome" complex works due to oppression of synthesis of protein owing to binding blocking.
It is active in relation to gram-positive (Staphylococcus spp., including producing a penicillinase; Streptococcus spp., including Streptococcus pneumoniae); Haemophilus influenzae, Listeria spp., Bacillus anthracis) and to gram-negative microorganisms (Neisseria gonorrhoeae, Bordetella pertussis, Escherichia coli, Enterobacter spp., Klebsiella spp., Salmonella spp., Shigella spp.), and also Ricketsia spp., Chlamydia spp., Mycoplasma spp., Treponema spp. Are steady against effect of drug: Pseudomonas aeruginosa, Proteus spp., Serratia spp., majority of strains of Bacteroides spp. and mushrooms, small viruses.

Pharmacokinetics. At oral administration 75 – 80% of drug are absorbed, 55 – 65% contact proteins of a blood plasma, the maximum concentration in blood is reached in 2 – 3 h and makes 1,5 – 3,5 mg/l. In the following of 8 h concentration gradually decreases.
In an organism it is distributed unevenly: in the maximum concentration contains in a liver, kidneys, lungs and bodies containing many RES elements (a spleen, lymph nodes).
Concentration of Tetracycline in bile is 5 - 10 times higher, than in blood serum. In fabrics of thyroid and prostatic glands the content of drug same, as well as in a blood plasma. In pleural and ascitic liquid, saliva, breast milk concentration of drug makes 60 – 100% of its concentration in a blood plasma. In large numbers collects in a bone tissue. Badly gets through a blood-brain barrier. Gets through a placental barrier and comes to fruit blood.
In a liver 30 – 50% are metabolized. In urine is defined in high concentration by 2 h after reception and remains for 6 – 12 h; for the first 12 h kidneys excrete 10 – 20% of a dose.
5 – 10% of the general dose are removed with bile in intestines where there is a partial return absorption (enterohepatic circulation) that promotes long circulation of active agent in an organism.
Excretion through intestines at intake – 20 – 50%.
The elimination half-life makes 8 h.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug: bronchitis, pneumonia, purulent pleurisy, subacute septic endocarditis, bacterial and amoebic dysentery, whooping cough, quinsy, scarlet fever, gonorrhea, brucellosis, tularemia, sypny and typhinia, psittacosis, ornithosis, infectious diseases of urinary tract, chronic cholecystitises, purulent meningitis, purulent infections of skin and soft tissues, cholera.
Prevention of postoperative infections.

Route of administration and doses:

Tetracycline is accepted inside, in time or right after food, washing down with water.
The single dose for adults makes 250 mg each 6 hours. The highest daily dose – 2 g.
Children are from 8 to 12 years old – on 10 – 15 (to 25) mg/kg a day for 3 – 4 receptions; 12 years – doses of adults, that is on 250 mg 3 – 4 times a day are more senior. The course of treatment makes 5 – 7 days. After normalization of body temperature and disappearance of clinical signs of a disease drug is accepted 1 - 3 more day.

Features of use:

At a renal failure cumulation and development of side effects are possible.
With care appoint Tetracycline at a leukopenia.
Tetracycline is not appointed to children up to 8 years as it causes long-term discoloration of teeth, a hypoplasia of enamel and delay of longitudinal growth of bones of a skeleton.
Tetracycline is not accepted along with milk and other dairy products as at the same time drug absorption is broken.
During treatment by Tetracycline it is necessary to watch a condition of the patient carefully. In case of signs of hypersensitivity to drug and by-effects do a break in treatment, in case of need appoint other antibiotic (not group of tetracyclines); in case of symptoms of candidiasis appoint antifungal antibiotics, vitamins.
Drug adult in doses less than 800 mg a day to appoint inexpedient as except insufficient therapeutic effect development of resistant forms of microorganisms is possible.
Due to the possible development of a photosensitization insolation restriction is required.
In case of long use it is necessary to carry out periodic control of function of kidneys, a liver, bodies of a hemopoiesis.
Can mask symptoms of syphilis in this connection it is necessary to carry out monthly serologic assay for 4 months.
For prevention of a hypovitaminosis it is necessary to appoint vitamins of group B and K, beer yeast.
Drug contains dye понсо 4R which can cause reactions of allergic type, including asthma. The allergy is most often shown at patients who have an allergy to acetylsalicylic acid.

Side effects:

From the alimentary system: nausea, vomiting, anorexia, an abdominal pain, diarrhea, a lock, dryness in a mouth, a glossitis, language discoloration, coloring of teeth, an esophagitis, tranzitorny increase in content in blood of hepatic transaminases, an alkaline phosphatase, bilirubin, creatinine.
From TsNS: faints, headache.
From system of a hemopoiesis: neutropenia, thrombocytopenia, hemolitic anemia.
Allergic reactions: skin rash, itch, eosinophilia, Quincke's edema.
Dermatological reactions: photosensitization.
At long use of drug there can be complications caused by development of candidiasis (the damage of skin and mucous membranes, and also a septicaemia caused by a drozhzhepodobny mushroom of Candida albicans). For treatment of candidiasis use antifungal antibiotics (nystatin, levorinum).

Interaction with other medicines:

The drugs containing ions of metals (antacids, iron preparations, magnesium, calcium), form inactive chelates in this connection it is necessary to avoid their co-administration with Tetracycline.
It is necessary to avoid a combination with penicillin, cephalosporins which have bactericidal action and are antagonists of bacteriostatic antibiotics (including Tetratsiklina).
At simultaneous use with Retinolum development of intracranial hypertensia is possible. At simultaneous use with holestiraminy Tetracycline absorption is broken.
The Tetracycline combination with Oleandomycinum and erythromycin is considered synergy.
Due to the oppression of intestinal microflora the prothrombin ratio decreases that causes the necessity of dose adjustment of indirect anticoagulants.
Chymotrypsin increases concentration and duration of circulation of Tetracycline.

Contraindications:

Hypersensitivity to drug and related antibiotics, fungus diseases, abnormal liver functions, diseases of kidneys, a leukopenia, pregnancy, a lactation (for the period of treatment stop feeding by a breast), children's age up to 8 years.

Overdose:

Strengthening of manifestations of the described by-effects is possible. Treatment – symptomatic therapy.

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 20 tablets in a blister strip packaging.