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Azimed
Azimed is an antimicrobial drug for systemic use. Included in the category of lincosamides, macrolides, as well as streptogramins.
Indications of the azimede
It is used to eliminate infections caused by bacteria sensitive to the substance azithromycin:
- diseases of the ENT organs (such as tonsillitis or pharyngitis of bacterial type, inflammation of the middle ear and sinusitis);
- infections in the respiratory tract (such as bacterial type bronchitis and non-hospital pneumonia);
- infectious diseases in the soft tissue and skin: migratory erythema (early stage of tick borreliosis), impetigo and erysipelas, as well as secondary pyodermatosis;
- STDs: cervicitis or urethritis of a complicated / uncomplicated type.
Pharmacodynamics
Azithromycin is azalide (a new category from the macrolide group) and has a large range of antimicrobial effects. It is synthesized with the ribosomal (70S) 50S subunit of sensitive bacteria and suppresses the RNA-dependent protein binding. As a result of this process, the multiplication and growth of microbes slow down. At high concentrations of the drug in the body, its bactericidal properties may manifest.
Azithromycin has a fairly large spectrum of effects and actively affects the following pathogenic microorganisms:
- separate germs of Gram-positive type: pneumococcus, streptococcus pyogenes, streptococcus agalactia, streptococci types C, F, and also G, Staphylococcus aureus and S. Viridans;
- germs of gram-negative type: Influenza rod, H. Parainfluenzae, Ducrea's stick, Moraxella cataralis, Pertussis stick, Paracolitus stick, Gonococcus and Gardnerella vaginalis;
- sensitive to the substance anaerobes: peptostreptococci and peptococci, Bacteroides bivius and clostridia perfringence;
- effectively affects intracellular and other bacteria, among them: legionella pneumophila, Chlamydia trachomatis, mycoplasma pneumonia, ureaplasma urealiticum, pale treponema and Borrelia Burgdorfer.
Has no effect on germs of gram positive type, resistant to erythromycin.
Pharmacokinetics
The bioavailability level for internal drug intake is approximately 37% (with the effect of the "first hepatic transmission"). Inside the serum, the peak concentration reaches 2-3.5 hours after the oral administration and amounts to 0.4 mg / l (after oral administration of 500 mg LS). The medicine quickly penetrates into the tissues and organs of the genitourinary system (among them the prostate), as well as respiratory organs, soft tissues and skin. Inside the cells with tissues, the indicator of the substance is higher than inside the serum (10-100 times). The equilibrium plasma parameters reach 5-7 days later. The substance in large quantities cumulates inside the phagocytes, transferring it to the site of inflammation or infection. There it is gradually released by phagocytosis.
Synthesis with proteins has a level inversely proportional to the value of the substance inside the blood (7-50% of the drug). Approximately 35% of the dose is exposed to hepatic metabolism (dimethylation process), as a result of which the substance loses its activity. Approximately 50% of the drug is excreted unchanged with bile, and another 4.5% - with urine, within 72 hours.
The half-life of the plasma is approximately 14-20 hours (the interval is within 8-24 hours after the drug is consumed) and the 41st hour (interval within 24-72 hours). Pharmacokinetic properties of drugs significantly change when it is taken with food.
In elderly men (age 65-85 years), there is no change in the pharmacokinetics of drugs, but in women, the peak rate rises by 30-50%. In young children (age 1-5 years), the AUC, peak concentration and half-life of the substance decrease.
Side effects of the azimede
Often the substance of azithromycin is tolerated fairly well, but in some cases, when it is administered, there may be such side effects:
- reactions from the CCC: there have been cases of arrhythmias such as pirouette (this includes also ventricular tachycardia), palpitations, as well as lowering blood pressure;
- manifestations of the gastrointestinal tract: diarrhea, bloating, nausea, changes in the shade of the tongue, abdominal pain, indigestion, constipation and vomiting, as well as the development of pancreatitis, gastritis and pseudomembranous form of colitis;
- organs of the hepatobiliary system: the development of hepatitis (also necrotic and fulminant of its form), intrahepatic cholestasis and kidney insufficiency (occasionally can lead to death), and in addition disorders in the liver;
- neurological disorders: the appearance of paresthesias, seizures, headaches and dizziness. In addition, the development of hypoesthesia, agesia and dysgeusia, parosmia, myasthenia gravis and anosmia. There are fainting, psychomotor agitation, as well as a feeling of drowsiness or vice versa insomnia;
- mental disorders: a sense of aggressiveness, nervousness, anxiety or anxiety;
- reactions of the vestibular apparatus and auditory organs: curable deafness, vertigo, and also ear ringing;
- visual disorders: visual impairment;
- reaction of lymph and hematopoietic system: development of hemolytic form of anemia, and also leuko-, thrombocytopenic or neutropenia;
- subcutaneous tissue and skin: itching, photosensitization and eruptions, development of urticaria, Lyell's syndrome or Stevens-Johnson, multiform erythema or edema Quincke;
- manifestations of connective tissues and organs of the OA: development of arthralgia;
- organs of the urination system: development of kidney failure in acute form or tubulointerstitial nephritis;
- invasive or infectious diseases: the appearance of candidiasis (also in the mouth), vaginal infection;
- allergic disorders: anaphylactic manifestations, hypersensitivity;
- general reactions: the development of anorexia, asthenia, severe fatigue, the appearance of pain in the sternum, malaises and edemas;
- change in the results of laboratory studies: the development of eosinophilia or lymphocytopenia, an increase in creatinine, AST, ALT and bilirubin, a decrease in the level of blood bicarbonates, prolongation of the QT-interval on the ECG and changes in potassium.
Dosing and administration
The medication is taken orally, once a day (before meals for 1 hour or 2 hours after it - it is necessary, as combined use with food affects the absorption of azithromycin). Capsules can not be opened or divided into halves.
For teenagers weighing from 45 kg, adults and elderly people:
- to eliminate infections in the respiratory tract and ENT organs, as well as soft tissues and skin (excluding migratory erythema of a chronic type) - daily dosage is 500 mg (for 1 drink 2 capsules). Take in the period of 3 days;
- to eliminate migrating erythema to take capsules should be given once a day for 5 days. At the same time on the 1st day, the dose size is 1 g (taking 4 capsules LS), and during the 2-5th days - 500 mg (taking 2 capsules of the drug);
- for the treatment of STDs: a single dose of 1 g of medication (4 capsules).
If you miss the use of drugs you need to quickly take the missed capsule, and all subsequent techniques should be done at intervals of 24 hours.
Interactions with other drugs
With caution, it is necessary to take azithromycin in case of simultaneous use of other drugs that can prolong the QT-interval.
During the study of the drug-antacid interaction, there was no change in the level of bioavailability, although peak plasma levels were reduced by about 25%. Therefore, it is recommended to use azithromycin before taking antacid drugs (for 1 hour) or after it (after 2 hours).
Derivatives of ergot in combination with azithromycin in theory can provoke the emergence of ergotism.
Some representatives of related macrolides affect the metabolism of cyclosporine. Since clinical and pharmacokinetic tests for possible interaction in the case of concomitant reception of Azimed with cyclosporine have not been performed, it is necessary to carefully evaluate the clinical picture before the appointment of a complex reception of drug data. If combined therapy is considered justified, during the course it will be necessary to carefully monitor the parameters of cyclosporine and adjust the dose according to them.
Azithromycin does not affect the anticoagulant properties of a single dose (15 mg) of warfarin, although there is evidence of an increase in these properties with the simultaneous use of coumarinic anticoagulants (orally) with azithromycin. It was not possible to identify the cause of such an impact, but it is necessary to take this fact into account. Therefore, it is recommended to constantly monitor the rate of PTV in individuals treated with these drugs.
In some treated individual macrolides may affect the process of intestinal metabolism of digoxin. Therefore, when a combination of azithromycin with this drug is required to remember the possible increase in digoxin indicators and monitor their changes during the treatment period.
There is no information on the interaction of azithromycin and terfenadine. Simultaneous reception of these drugs should be done with caution.
Combination with theophylline does not lead to a change in the pharmacokinetic characteristics of this substance. However, the combined use of theophylline with other macrolides in certain cases may cause an increase in its serum levels.
One-time use of 1000 mg of zidovudine in combination with repeated administration of azithromycin in doses of 600 or 1200 mg does not lead to a change in the plasma pharmacokinetics of zidovudine, as well as its (together with glucuronide degradation products) urinary excretion. However, azithromycin increases the phosphorylated zidovudine (a drug-active degradation product inside mononuclear cells in the peripheral blood stream).
Combined use of the drug with rifabutin does not affect their plasma performance. As a result of this combination, neutropenia may develop (although in this case, the reason is most likely the reception of rifabutin, because it was not possible to connect the development of this disorder with the use of this substance in combination with azithromycin).
As a result of taking nelfinavir, the serum level of azithromycin rises. Correct the dosage of the drug when combined with nelfinavir is not needed, but it is required to monitor the patient's condition for the occurrence of side effects of azithromycin.
Medical expert editor
Portnov Alexey Alexandrovich
Education: Kiev National Medical University. A.A. Bogomolets, Specialty - "General Medicine"
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Attention!
To simplify the perception of information, this instruction for use of the drug "Azimed" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.