DZHOZAMITSIN (Josamycin)

     Chemical name : Acetate 3-B-4 - (3-metilbutanoat) leykomitsin V

     Synonyms : Vilprafen, Vilprafen solyutab

     Description : Antibiotics group macrolides. Produtsiruetsya aktinomitsetami Streptomyces narbonensis var. josamyceticus. Well soluble in ethanol and methanol, soluble in air and very little water.

     Pharmacology : anti-drugs operation.

Reversible associated with the 50S rBS ribosom inhibits protein synthesis and distribution of microbial cells (bakteriostatichesky effect). When a hotbed of inflammation in high concentrations has a bactericidal effect. It has a broad range of actions, including gram (Staphylococcus spp. , Produce and produce penitsillinazu, Streptococcus spp. , Bacillus anthracis, Corynebacterium diphtheriae) and gram (Neisseria gonorrhoeae, N. meningitidis, some Shigella, Haemophilus influenzae, Bordetella pertussis) bacteria, endocellular microorganisms (Legionella spp, Mycoplasma spp. , Chlamydia spp. , Ureaplasma urealyticum) and some anaeroby (Peptococcus, Peptostreptococcus, Clostridium perfringens, Bacteroides fragillis). Light affects enterobakterii because little change natural bacterial flora digestive tract. Effective resistance to erythromycin.

In a pregnant female mice and rats during organogeneza dose of 3 g / kg increased mortality and cause delay fruit growth without signs teratogennogo action.

Once inside quickly and completely absorbed from the digestive tract, eating does not affect the bioavailability. Cmax achieved through 0,5-2 h with a single dose of 400 mg, 0.33 mg / L, 500 mg-0,67-0,71 mg / l, 1000 mg, 2.4 mg / l, 1250 mg - 2.08 ± 1.13 mg / l, 2000 mg, 5.79 ± 2.47 mg / l. Linking plasma proteins is 15%. Well soluble in fat and little ionize under normal pH values of the blood and tissue fluids, well penetrates through gistogematicheskie barriers to the various organs and tissues. The volume of 300.56-l. The largest concentrations are established in the respiratory system, including the lungs, sputum (maximum level in sputum achieved within 1 h and over concentration in plasma at 8-9 times), pyelonephritis, adenoids, exudation middle ear, okolonosovyh secret ingredient, lachrymal fluid, saliva , gums, bone, prostate gland and the port. Little enters the spinal fluid passes through the placenta and breast milk in sekretiruetsya. Biotransformiruetsya in liver education inactive metabolites 3 : 14-gidroksidzhozamitsin, gidroksidzhozamitsin and deizovalerildzhozamitsin. T1 / 2-0,9-2 hours (an average of 1.5 h) increases in liver cirrhosis. Excreted primarily with bile and urine (20%).

     Application : Infectious and inflammatory diseases of the respiratory tract and ear organs : tonsillitis, pharyngitis, laryngitis, sinusitis, middle ear, and paratonzillit tonsillitis, bronchitis, pneumonia, bronhoektaticheskaya disease; Dental disease (gingivitis, periodontitis); Infection of skin and soft tissue ( acne, piodermiya, abrasions, anthrax, rozhistoe inflammation, limfangit, lymphadenitis, venereal limfogranulema); urinary tract infection (prostatitis, Urethritis); as diphtheria, scarlet fever, whooping cough, gonorrhea, syphilis, chlamydia, psittacosis, dysentery, dakriotsistit, Blepharitis.

     Contraindications : Giperchuvstvitelnost (including other macrolides), serious violations of liver function, low children.

     Restrictions on the use : Pregnancy, breast-feeding, old age.

     Application of pregnancy and breastfeeding : Perhaps during pregnancy if the expected effect of treatment outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

     Side Effects : So part of the digestive tract : oblozhennost language, anorexia, nausea, heartburn, vomiting, flatulence, abdominal pain, diarrhoea, Melena, the effects on the liver, increasing the liver transaminaz (AST, ALT), holestatichesky hepatitis psevdomembranozny Colitis.

Other : swelling of the feet, hearing, goiter, candidiasis, allergic reactions (urticaria, rash), very rarely, fever, general malaise.

     Networking : Zamedlyaet down teofillina (increasing side effects), and astemizola terfenadina (zheludochkovyh increased risk of arrhythmias). Potentsiruet vazokonstriktornoe of alkaloids LPV. Weakens the effect of hormonal contraceptives. Decreases effective microbicides antibiotics and linkomitsina (each). It increases the concentration of cyclosporine (risk of nefrotoksichnosti) midazolama, triazolama, digoxin and bromokriptina plasma. Dizopiramida metabolism stops moving (increases T1 / 2) carbamazepine.

     Overdosing : Symptoms : Symptoms increased side effects.

Treatment : symptomatic therapy.

     Dosing and Administration : inside, between meals. Pills are not liquid, squeezed a small amount of water. Adults and children over 14 1-2 g / day for 2-3 reception. Treatment ordinary and tip acne-500 mg, 2 times a day for 2-4 weeks, then 500 mg once a day 1 for 8 weeks. Children (preferably in the form of suspensions) : 6-14 years old (weight over 21 kg) dose of 30-45 ml / day, 1-6 years old (weight 10-21 kg) 15-30 ml / day, 3 months 1 year (5,5-10 weight kg) 7,5-15 ml / day, divided into three installments.

     Precautions : In order to prevent the emergence of resistant strains to a minimum duration of the course (with streptococcal infection of not less than 10 days), not to increase or double dose, if admission was missing.

During therapy needed EKG monitoring (particularly in patients while receiving digoxin), the control function of liver and kidneys.

With caution should be appointed in the face of kidney failure.

When treating diabetes, keep in mind that 5 ml suspension containing 3.25 g glucose. People older designate smaller doses and treatments under the supervision of a doctor.

     Special instructions : Suspension should be used during the 4 weeks after the opening of a bottle.

Materials allowed to copy only with the active hyperlink to the handbook of medicines