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Asit
Asit is an antibacterial systemic drug. Contains the active ingredient azithromycin. Included in the category of lincomycins, streptogramins and macrolide antibiotics.
Indications of the azita
It is used for the treatment of infectious pathologies, provoked by bacteria sensitive to azithromycin:
- diseases of ENT organs (sinusitis, inflammation of the middle ear, as well as tonsillitis or bacterial pharyngitis);
- pathology in the respiratory system (community-acquired pneumonia, as well as bacterial-type bronchitis);
- infectious processes in soft tissues and skin (erysipelas, migratory erythema (the initial stage of tick borreliosis), as well as piodermatosis of secondary type and impetigo);
- STDs: cervicitis or urethritis of a complicated or uncomplicated type, provoked by Chlamydia trachomatis.
Pharmacodynamics
Azithromycin is included in the category of macrolides - azalides, which have a large range of antimicrobial effects. The properties of the substance are due to the inhibition of the binding processes of bacterial proteins (in this case, synthesis occurs with the ribosomal 50 S subunit), as well as inhibiting peptide migration in the absence of effect on the binding of polynucleotides.
Resistance to azithromycin is both acquired and congenital. Full cross resistance is observed in pneumococci, β-hemolytic streptococci from category A, enterococci of fecal and golden staphylococci (here also includes methicillin-resistant staphylococcus aureus) - with respect to azithromycin with erythromycin, as well as other linkomycins and macrolides.
The range of antimicrobial activity of the active drug component includes:
- Gram-positive aerobes: methicillin-sensitive Staphylococcus aureus, penicillin-sensitive pneumococcus, and streptococcus pyogenic (from category A);
- Gram-negative aerobes: hemophilic rod, Haemophilus parainfluenzae, pneumonophil legionella, moraxella cataralis and multicid pasteurella;
- anaerobes: clostridium perfringens, Fusobacterium spp., prevotella and Porphyromonas spp .;
- other microbes: Chlamydia trachomatis.
Among the bacteria (anaerobes) inherent resistance to the drug possess bacteroid fragigis.
Pharmacokinetics
With the internal use of drugs, the bioavailability index is approximately 37%. The peak serum level reaches 2-3 hours after the use of the tablet.
After taking the pill, the active substance is distributed inside all tissues and organs. Pharmacokinetic tests demonstrated that the azithromycin index in tissues is higher than its analogous plasma value (by 50 times). This is a confirmation that the drug has a powerful synthesis with tissues.
The synthesis index with a plasma protein varies depending on the level of the substance inside the plasma and can range from 12% (in the case of 0.5 μg / ml intake) to 52% (in the case of 0.05 μg / ml) inside the blood serum. The equilibrium distribution volume (VVss) is 31.1 l / kg.
The final half-life from the plasma completely corresponds to the half-life of the tissues over a period of 2-4 days.
Approximately 12% of the dosage of azithromycin is excreted unchanged together with the urine during the subsequent 3 days. The highest values of unchanged substance were observed inside bile. In addition, 10 decay products formed by N-processes as well as O-demethylation, as well as hydroxylation of aglycone and dezosamine rings, were found in the bile. Also, the cleavage conjugate was cleaved.
Use of the azita during pregnancy
Azithromycin is able to pass through the placental barrier, but there was no adverse effect of this substance on the fetus. Comprehensive and carefully controlled testing of drug exposure to pregnant women has not been carried out, and therefore it is recommended to use Azit exclusively in cases when there is no adequate alternative to this drug.
Tests that can determine the passage of the substance into the mother's milk have not been carried out, so use azithromycin during lactation is required only in the absence of other similar drugs.
Contraindications
- intolerance of the active component of the drug or other of its constituent elements and other macrolides;
- since in theory, if iazitromycin is combined with ergot derivatives, ergotism can develop, these drugs can not be used in combination;
- if the liver is not deficient, the drug is not used, since the active component of Azith passes the metabolism inside the liver and is excreted with bile;
- Also, do not prescribe drugs in the form of tablets to children weighing less than 45 kg (in this case it is better to use a suspension).
Side effects of the azita
Taking tablets can cause the following side effects:
- lymphatic and blood flow reactions: thrombocytopenia develops occasionally. Clinical tests alone provided information on the development of periods of transient neutropenia (mild severity), but it was not possible to find a relationship with the use of azithromycin in this case;
- mental manifestations: occasionally there are feelings of anxiety, aggressiveness, nervousness and anxiety;
- reactions from the NA: in some cases, a feeling of drowsiness, syncope, headache and dizziness or vertigo develop, and convulsions also appear (it was possible to reveal that they are capable of provoking other macrolides) and there is a breakdown in the olfactory and taste buds. Occasionally there is insomnia, asthenia and paresthesia;
- disorders in the work of auditory organs: occasionally appeared information about hearing damage when using macrolides. Individual patients who used azithromycin developed auditory disorders - ear ringing, the appearance of deafness. Basically, such cases were recorded in experimental tests, when the drug was used in high doses for a long time. Existing reports of follow-up medical examination confirm that often these disorders are curable;
- manifestations on the part of the CCC: occasionally there was information about the development of the heartbeat, as well as arrhythmias due to ventricular tachycardia (it turned out that it can cause other macrolides). Rarely, prolongation of QT-interval, decrease in blood pressure level, and also ventricular fibrillation was reported;
- reactions of the digestive tract: often there is diarrhea, vomiting, abdominal cramps or abdominal pain, and nausea. Rarely, bloating, loose stools, anorexia, digestive upset, and dyspepsia may develop. Occasionally there is pancreatitis and constipation or a change in the shade of the tongue. There is evidence of the appearance of a pseudomembranous form of colitis;
- gallbladder and liver: occasionally intrahepatic cholestasis or hepatitis developed, and pathological values were also observed when taking a functional liver test. Rarely there was hepatic dysfunction (sometimes resulting in death) and hepatitis of necrotic type;
- reactions of the skin: in some cases, there were manifestations of allergies, among which rash and itching. Occasionally developed urticaria, edema Quincke and photophobia. There is information about the development of serious skin manifestations - such as erythema multiforme, as well as Stevens-Johnson or Lyell syndromes;
- disorders in the work of muscles and bones: sometimes arthralgia arose;
- disorders in the work of the urethra and kidneys: occasionally there was an acute form of kidney failure and tubulointerstitial nephritis;
- reactions of the reproductive organs: in some cases, vaginitis appeared;
- general disorders: occasionally there was anaphylaxis (with edemas that single-handedly caused death), and in addition candidiasis.
Dosing and administration
Tablets should be consumed 1 hour before meals or 2 hours after eating. Such a regimen is necessary, because a combined intake of azithromycin with food leads to a violation of the absorption of the substance. The medicine is consumed once a day - the pill should be swallowed without chewing.
For adults and teenagers weighing more than 45 kg:
- to eliminate infectious diseases in the respiratory system, ENT organs, and in addition soft tissue and skin (excluding migrating erythema): 500 mg once a day for a period of 3 days;
- for the treatment of migratory erythema: take the medicine once a day during a period of 5 days. In this case, 1 g should be taken on the first day, and in the following days the dose should be reduced to 500 mg;
- to eliminate STDs: with cervicitis or urethritis uncomplicated type requires taking once 1 g of the drug.
If one of the techniques was missed, you need to use the dose as quickly as possible, and then use tablets with an interval of 24 hours.
Interactions with other drugs
Azithromycin is used with caution in combination with other drugs that can prolong the QT-interval.
During the study of the effect of antacid drugs on the pharmacokinetic properties of azithromycin, their combined administration did not generally change the bioavailability, but a decrease in the peak plasma values of azithromycin (by 30%) was observed. As a result, it is required to use azithromycin at least 1 hour before taking antacid medicines or 2 hours afterwards.
Certain related macrolides affect the metabolic processes of the substance cyclosporin. Since clinical and pharmacokinetic tests for possible interaction with combined use of azithromycin with cyclosporine have not been performed, the clinical picture before the appointment of combined therapy using these agents must be carefully evaluated. If the doctor found this combination to be justified, careful regular monitoring of the cyclosporine values would be necessary in order to adjust its dose as necessary.
There is evidence of increased rates of bleeding in the case of concomitant medication with warfarin or oral anticoagulants coumarinovogo number. Because of this, while simultaneously receiving such drugs it is required to constantly monitor the level of the PTV.
In some patients, the development of the effect of certain macrolides on intestinal metabolism of digoxin has been observed. Therefore, when digoxin is combined with Azith, it is required to constantly monitor digoxin digestion in the body, since its level may increase.
Azithromycin had no effect on the pharmacokinetic properties of theophylline in the case of concomitant use of these drugs by volunteers. In the period of simultaneous administration of theophylline with other macrolides, the serum values of this substance sometimes increased.
The combination of zidovudine (a single dose of 1000 mg) with azithromycin (a reusable dose of 600 or 1200 mg) did not lead to a change in the pharmacokinetics of zidovudine within the plasma, and in addition excretion of this substance or its glucuronic degradation products along with urine. But the use of azithromycin led to an increase in the level of phosphorylated zidovudine (a drug-active product of disintegration inside peripheral blood mononuclear cells). The medicinal value of this information is not known.
The combined use of daily doses of azithromycin (1200 mg) with didanosine in 6 people did not lead to a change in the pharmacokinetic characteristics of the latter (in comparison with placebo).
The combined use of the drug with rifabutin had no effect on the indices of these drugs inside the plasma. Some patients sometimes develop neutropenia, but its appearance is associated with the use of rifabutin, and the association with the combined use of azithromycin has not been established.