Azithromycin pharmachologic effect:
Broad-spectrum antibiotic. Antibiotic-azalide, a representative of a new subgroup of macrolide antibiotics. When creating in inflammation in high concentrations has a bactericidal effect.
Azithromycin To a sensitive Gram-positive cocci: Streptococcus pneumoniae, St. pyogenes, St. agalactiae, Streptococcus groups CF and G, Staphylococcus aureus, St. viridans; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, B. parapertussis, Legionella pneumophila, H. ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; Some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; and Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Azithromycin is inactive against Gram-positive bacteria resistant to erythromycin.
Azithromycin pharmacokinetics.
Suction. Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic medium and lipophilicity. After oral administration of 500 mg Azithromycin azithromycin maximum concentration in plasma is reached after 2.5 hours, -2.96 and 0.4 mg / l. Bioavailability is 37%.
Azithromycin distribution.
Azithromycin well into the respiratory tract, genitourinary organs and tissues (in particular in the prostate gland), the skin and soft tissue. The high concentration in tissues (10-50 times higher than in blood plasma) and a long half-life of azithromycin due to low binding to plasma proteins, and its ability to penetrate into eukaryotic cells and concentrated in a low pH environment, environmental lysosomes. This, in turn, determines the apparent volume of distribution is high (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important to eliminate intracellular pathogens. It proved that phagocytes deliver azithromycin localization of infection sites where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissue (on average 24-34%) and correlated with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin has no significant effect on their function.
Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.
Azithromycin withdrawal.
Excretion of azithromycin from plasma passes in 2 stages: half-life of 14-20 hours in the range of 8 to 24 hours after dosing, and 41 h - in the range from 24 to 72 hours, which allows the use of drug 1 time / day.
Azithromycin Indications for use:
Infectious diseases caused by pathogens susceptible to the drug: infections of the upper respiratory tract and upper respiratory tract - tonsillitis, sinusitis (inflammation of the sinuses), tonsillitis (inflammation of the tonsils / glands /), otitis media (inflammation of the middle ear cavity); scarlet fever; infections of the lower respiratory tract - bacterial and atypical pneumonia (pneumonia), bronchitis (inflammation of the bronchi); infections of skin and soft tissue -rozha, impetigo (a superficial pustular skin lesions with the formation of purulent crusts), secondarily infected dermatitis (skin disease); urinary tract infections - and gonorrheal negonoreyny urethritis (inflammation of the urethra) and / or cervicitis (inflammation of the cervix); Lyme disease (borreliosis - an infectious disease caused by the spirochete Borrelia).
Azithromycin mode of application:
Before you assign patient drug to determine sensitivity to the hair that caused the disease in this patient. Azithromycin should always be taken one hour before meals or 2 hours after a meal. 1 The drug is taken once a day.
Adults with infections of the upper and lower respiratory tract, skin and soft tissue infections designate 0.5 g in 1 day, and then 0.25 g of the 2nd to 5th day or 0.5 g daily within 3 days (course dose 1.5 g).
In acute infections of the urogenital (genitourinary) tract designate single 1 g (2 tablets of 0.5 g).
When Lyme disease (borreliosis) for the treatment of the first stage (erythemamigrans) appoint 1 g (2 tablets of 0.5 g) in 1-day and 0.5 g daily from the 2 nd to 5 th day (course dose 3 g).
Children prescribed medication based on body weight. Children weighing more than 10 kg of calculation: s Day 1 - 10 mg / kg body weight; in the next 4 days - 5 mg / kg. Chance of a 3-day course of treatment; in this case, a single dose of 10 mg / kg. (Heading dose of 30 mg / kg body weight).
Recommended break of 2 hours between taking azithromycin and antacid (reducing stomach acidity) drugs in their simultaneous appointment.
Azithromycin side effects:
Nausea, diarrhea, abdominal pain, rarely - vomiting and flatulence (gas accumulation in the intestine). Perhaps transient (transient) increase in liver enzymes. It is extremely rare - skin rash.
Azithromycin contraindications:
Hypersensitivity to macrolide antibiotics. Care should be taken when administering the drug to patients with severely impaired liver and kidney function. During pregnancy and breastfeeding, azithromycin is not appointed, except in cases where use of the drug is greater than the possible risk. The drug should be used with caution in patients with an indication of the allergic reactions in the anamnesis (medical history).
Azithromycin drug Interactions.
It enhances the effect of ergot alkaloids, dihydroergotamine. Tetracycline and chloramphenicol - reinforce action (synergy), lincosamides - lowering effect. Antacids, ethanol, food slow down and reduce absorption. It slows excretion, increases in serum concentrations and enhances the toxicity of cycloserine, indirect anticoagulants, methylprednisolone and felodipine. By inhibiting microsomal oxidation in hepatocytes, lengthens T1 / 2, slows excretion, increases the concentration and toxicity of carbamazepine, ergot alkaloids, valproic acid, hexobarbital, phenytoin, disopyramide, bromocriptine, theophylline and other xanthine derivatives, oral hypoglycemic agents. Incompatible with heparin.
Azithromycin precautionary measures.
Observe break 2 hours, while the use of antacids. To use caution when expressed in human liver, kidney, cardiac arrhythmias (ventricular arrhythmias and prolongation of QT interval). After discontinuation of treatment hypersensitivity reactions in some patients may persist, which requires specific therapy under medical supervision.
Azithromycin product form:
Tablets to 0,125 g of azithromycin dihydrate in a package of 6 pieces; 0.5 grams of pills azitromiiina dihydrate in a package of 3 pieces; Capsules of 0.5 g of azithromycin dihydrate in a package of 6 pieces; Syrup in bottles; forte syrup in bottles.
Sumamed: tablets 125 mg and 500 mg; 250 mg capsules; powder for oral suspension 100 mg / 5 mL and 200 mg / 5 ml in 20 ml vials.
Azithromycin storage conditions:
List B. In a dry, dark place at a temperature of 15-25 ° C. Keep out of the reach of children.
Shelf life: 2 years. Do not use after the expiration date.
Dispensed by prescription.
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