Azit

Azit is an antibacterial systemic drug. Contains the active ingredient azithromycin. It belongs to the category of lincomycins, streptogramins and macrolide antibiotics.

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Indications Azita

It is used to treat infectious pathologies caused by bacteria sensitive to azithromycin:

• ENT diseases (sinusitis, inflammation of the middle ear, as well as tonsillitis or bacterial pharyngitis);
• pathologies in the respiratory system (community-acquired pneumonia, as well as bacterial bronchitis);
• infectious processes in soft tissues and skin (erysipelas, erythema migrans (initial stage of tick-borne borreliosis), as well as secondary pyodermatoses and impetigo);
• STD: cervicitis or urethritis, complicated or uncomplicated, caused by Chlamydia trachomatis.

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Release form

Release in tablets: volume 250 mg - 6 pieces in a blister. Inside the package there is 1 blister plate. Volume 500 mg - 3 pieces in a blister. Inside a separate pack - 1 blister plate.

Pharmacodynamics

Azithromycin belongs to the category of macrolides - azalides, which have a wide range of antimicrobial action. The properties of the substance are due to the inhibition of bacterial protein binding processes (in this case, synthesis with the ribosomal 50 S-subunit occurs), as well as the prevention of peptide movement in the absence of an effect on the process of polynucleotide binding.

Resistance to azithromycin can be either acquired or congenital. Complete cross-resistance is observed in pneumococci, β-hemolytic streptococci of category A, enterococci faecalis and Staphylococcus aureus (this also includes methicillin-resistant Staphylococcus aureus) – against azithromycin with erythromycin, as well as other lincomycins and macrolides.

The range of antimicrobial action of the active component of the drug includes:

• Gram-positive aerobes: methicillin-sensitive Staphylococcus aureus, penicillin-sensitive Streptococcus pneumoniae, and Streptococcus pyogenes (from category A);
• Gram-negative aerobes: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis and Pasteurella multocida;
• anaerobes: Clostridium perfringens, Fusobacterium spp., Prevotella and Porphyromonas spp.;
• other microbes: Chlamydia trachomatis.

Among bacteria (anaerobes), Bacteroides fragilis has an innate resistance to the drug.

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Pharmacokinetics

When taken orally, the bioavailability index is approximately 37%. The peak serum level is reached 2-3 hours after taking the tablet.

After taking the tablet, the active substance is distributed within all tissues and organs. Pharmacokinetic tests have shown that the azithromycin index within tissues is higher than its similar plasma value (50 times). This confirms that the drug has a powerful synthesis with tissues.

The plasma protein synthesis rate varies depending on the plasma level of the substance and can be from 12% (in the case of 0.5 μg/ml) to 52% (in the case of 0.05 μg/ml) in the blood serum. The equilibrium distribution volume (VVss) is 31.1 L/kg.

The terminal half-life from plasma is fully consistent with the half-life from tissues over a period of 2-4 days.

About 12% of the azithromycin dose is excreted unchanged in the urine over the next 3 days. The highest levels of unchanged substance were observed in the bile. In addition, 10 breakdown products were found in the bile, formed by N- and O-demethylation processes, as well as hydroxylation of aglycone and desosamine rings. Cladinose conjugate cleavage was also observed.

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Dosing and administration

The tablets should be taken 1 hour before or 2 hours after meals. This regimen is necessary because taking azithromycin in combination with food leads to impaired absorption of the substance. The medicine is taken once a day - the tablet should be swallowed without chewing.

For adults and teenagers weighing more than 45 kg:

• to eliminate infectious diseases in the respiratory system, ENT organs, as well as soft tissues and skin (excluding erythema migrans): 500 mg once a day for 3 days;
• for the treatment of erythema migrans: take the medicine once a day for 5 days. In this case, on the 1st day, you should take 1 g of the drug, and on the following days, reduce the dose to 500 mg;
• to eliminate STIs: for cervicitis or uncomplicated urethritis, you need to take 1 g of the medicine once.

If one of the doses is missed, it is necessary to take the dose as quickly as possible, and then take the tablets at intervals of 24 hours.

Use Azita during pregnancy

Azithromycin is able to pass through the placental barrier, but no negative impact of this substance on the fetus has been identified. Full and carefully controlled tests of the drug's effect on pregnant women have not been conducted, therefore it is recommended to use Azit only in cases where there is no adequate alternative to this drug.

Tests capable of determining the passage of the substance into breast milk have not been conducted, therefore, the use of azithromycin during lactation is required only in the absence of other similar drugs.

Contraindications

• intolerance to the active component of the drug or its other components and other macrolides;
• since, in theory, ergotism may develop when combining azithromycin with ergot derivatives, these drugs cannot be used in combination;
• in case of liver failure, the drug is not used, since the active component of Azit is metabolized in the liver and excreted with bile;
• Also, the medicine should not be prescribed in tablet form to children weighing less than 45 kg (in this case, it is better to use a suspension).

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Side effects Azita

Taking the pills may cause the following side effects:

• Lymph and blood flow reactions: thrombocytopenia develops occasionally. Clinical tests have occasionally provided information on the development of periods of transient neutropenia (mild severity), but it was not possible to find a connection with the use of azithromycin in this case;
• mental manifestations: feelings of anxiety, aggressiveness, nervousness and restlessness are occasionally observed;
• reactions from the nervous system: in some cases, a feeling of drowsiness, syncope, headache and dizziness or vertigo develop, and in addition, convulsions appear (it was possible to establish that other macrolides can also provoke them) and a disorder of the olfactory and taste receptors is observed. Insomnia, asthenia and paresthesia occur occasionally;
• Hearing disorders: There have been rare reports of hearing damage with the use of macrolides. Some patients taking azithromycin have developed hearing disorders – tinnitus, deafness. These cases were mainly recorded in experimental tests, when the drug was used in high doses for a long time. Existing follow-up reports confirm that these disorders are often treatable;
• manifestations from the cardiovascular system: rarely, there was information about the development of palpitations, as well as arrhythmia due to ventricular tachycardia (it turned out that other macrolides can also cause it). Rarely, there were reports of prolongation of the QT interval, a decrease in blood pressure, and ventricular fibrillation;
• reactions of the gastrointestinal tract: often there is diarrhea, vomiting, abdominal cramps or abdominal pain, and nausea. Less often, bloating, loose stools, anorexia, indigestion and dyspepsia may develop. Rarely, pancreatitis and constipation occur, or the color of the tongue changes. There is information about the appearance of pseudomembranous colitis;
• Gallbladder and liver: Intrahepatic cholestasis or hepatitis have occasionally developed, and abnormal liver function tests have been observed. Rarely, liver dysfunction (sometimes leading to death) and necrotic hepatitis have been observed;
• skin reactions: in some cases, allergic reactions have occurred, including rash and itching. Urticaria, Quincke's edema, and photophobia have occasionally developed. There are reports of serious skin manifestations, such as erythema multiforme, and Stevens-Johnson or Lyell syndromes;
• disorders in the functioning of muscles and bones: sometimes arthralgia occurred;
• disorders of the urinary system and kidneys: acute renal failure and tubulointerstitial nephritis were occasionally observed;
• Reactions of the reproductive organs: in some cases, vaginitis appeared;
• General disorders: anaphylaxis (with swelling, which occasionally caused death) and candidiasis occasionally occurred.

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Overdose

Typical manifestations of overdose include: treatable hearing loss, severe diarrhea and vomiting with nausea.

To eliminate the disorders, it is necessary to take activated charcoal and perform symptomatic treatment to support the functioning of vital organs.

Interactions with other drugs

Azithromycin should be 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, when taken together, there were generally no changes in bioavailability indices, but a decrease in peak plasma values of azithromycin (by 30%) was observed. As a result, it is necessary to take azithromycin at least 1 hour before taking antacid drugs or 2 hours after it.

Certain related macrolides affect the metabolism of cyclosporine. Since clinical and pharmacokinetic tests for possible interactions with the combined use of azithromycin and cyclosporine have not been conducted, a careful clinical assessment is required before prescribing combination therapy using these agents. If the physician considers such a combination justified, careful regular monitoring of cyclosporine parameters will be required in order to adjust its dosage if necessary.

There is information about the increased incidence of bleeding in the case of combined administration of the drug with warfarin or oral coumarin anticoagulants. Because of this, when taking such drugs simultaneously, it is necessary to constantly monitor the level of PTT.

In some patients, the development of the effect of some macrolides on the intestinal metabolism of the substance digoxin is noted. Therefore, when combining digoxin with Azit, it is necessary to constantly monitor the digoxin levels in the body, since its level may increase.

Azithromycin did not affect the pharmacokinetic properties of theophylline in the case of combined use of these drugs by volunteers. During the period of simultaneous administration of theophylline with other macrolides, serum values of this substance sometimes increased.

The combination of zidovudine (single dose of 1000 mg) with azithromycin (multiple doses of 600 or 1200 mg) did not change the pharmacokinetics of zidovudine in plasma or the excretion of this substance or its glucuronic breakdown products in urine. However, the use of azithromycin led to an increase in the level of phosphorylated zidovudine (a drug-active breakdown product in mononuclear cells of the peripheral bloodstream). The medicinal significance of this information is unknown.

Combined administration of daily doses of azithromycin (1200 mg) with didanosine in 6 subjects did not result in changes in the pharmacokinetic characteristics of the latter (compared to placebo).

Concomitant use of the drug with rifabutin did not affect the plasma levels of these drugs. Neutropenia occasionally developed in individual patients, but its occurrence was associated with the use of rifabutin specifically, and a connection with the combined use of azithromycin could not be established.

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Storage conditions

The medicine must be kept in a place inaccessible to children. The temperature level should not exceed 25°C.

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Shelf life

Azit can be used for a period of 2 years from the date of manufacture of the tablets.

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