Zithrolex

Zitrolex is a macrolide antibiotic with a wide range of activity against pathogenic microbes.

Indications Zithrolex

The medicine is used to eliminate pathologies of an infectious nature - caused by bacteria that are sensitive to the active component of the drug:

• respiratory system (upper and lower sections), as well as ENT organs: acute diseases such as pharyngitis, sinusitis with tonsillitis, bronchitis and otitis media. In addition, pneumonia and chronic bronchitis in the acute stage;
• subcutaneous tissues and skin surface: erysipelas or impetigo;
• urinary organs and genitals: non-specific acute forms or gonococcal/chlamydial cervicitis, colpitis or urethritis.

Release form

Release in capsules: volume 250 mg (6 such capsules inside a blister) or 500 mg (3 such capsules inside a blister). In the package - 1-2 blister plates with capsules.

Pharmacodynamics

Azithromycin is a new macrolide subcategory – it is an azalide agent. It is synthesized with the bacterial ribosome type 70S – more specifically, with its 50S subunit. As a result, protein synthesis dependent on RNA is suppressed and the processes of reproduction and growth of pathogenic microorganisms are inhibited. High concentrations of the drug are capable of providing a bactericidal effect.

Among the bacteria sensitive to the drug:

• Gram-positive cocci - penicillin-sensitive pneumococci, methicillin-sensitive Staphylococcus aureus, as well as pyogenic streptococci from subgroup A;
• gram-negative microbes - Moraxella catarrhalis, gonococci, Haemophilus influenzae and Haemophilus parainfluenzae, Legionella pneumophila, Gardnerella vaginalis, ureaplasma and Pasteurella multocida with Chlamydia trachomatis;
• individual anaerobes – part of the bacteroides subgroup fragilis, prevotella, some species of fusobacteria, and also Peptostreptococcus species, Clostridium perfringens and Porphyromonas spp.;
• aerobes of the gram-positive group - fecal enterococci.

Pharmacokinetics

The drug is absorbed inside the gastrointestinal tract and is carried out quite quickly - due to the fact that azithromycin is lipophilic, and in addition, it is stable in acidic conditions. It is necessary to take into account that food weakens the absorption of the substance. The plasma maximum of the drug is observed after 2-3 hours after taking the capsule. The bioavailability index is 37%.

Distribution within the body occurs quickly. The accumulation of the drug within tissues is very high – it is approximately 50 times higher than the existing plasma values of the main component of the drug. This allows us to conclude that azithromycin has a high level of synthesis with tissues.

The level of protein binding inside the plasma changes in accordance with the plasma indices of the substance – within 12-52% with the corresponding level of serum concentration of 0.5-0.05 μg/ml. The average value of the distribution volume under conditions of the drug equilibrium level is 31.1 l/kg.

Plasma elimination of the drug occurs in 2 stages: the half-life is 14-20 hours with an interval of 8-24 hours after the use of the medicinal capsule, and 41 hours with an interval of 24-72 hours. Such indicators allow one-time (per day) use of the drug.

Excretion occurs predominantly with bile – the drug is excreted mainly unchanged. During the first week, about 6% of the dose taken is excreted unchanged in the urine.

Dosing and administration

Zitrolex capsules are taken either 1 hour before eating or at least 120 minutes after eating. A single dose of the drug is required per day.

When treating infectious diseases affecting the respiratory system with ENT organs, or penetrating into soft tissues with the surface of the skin (excluding migratory erythema), it is necessary to take 0.5 g of the drug (3-day cycle of administration) per treatment course.

To eliminate the migratory form of erythema, the medicine is taken for 5 days (daily single dose): on the 1st day - 1 g of the drug, and then 0.5 g during the period of 2-5 days.

When treating infectious STIs, a single dose of 1 g of the drug is required.

To eliminate certain diseases developing in the duodenum and stomach, the medicine is used in combination with other drugs and taken 1 g per day during a 3-day cycle.

To eliminate common acne, it is necessary to take a total of 6 g of the drug per course of treatment. The scheme usually looks like this: during the first 3 days, 0.5 g should be taken once a day. Then, during the next 9 weeks, 0.5 g of the drug should be taken once a week.

If a dose is missed, take the missed capsule as soon as possible and take subsequent doses at 24-hour intervals.

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Use Zithrolex during pregnancy

Pregnant women are not prescribed Zitrolex. The exception may be situations when the use of the drug is dictated by vital indications.

If the medicine needs to be taken during lactation, it is necessary to stop breastfeeding for this period of time.

Contraindications

Main contraindications:

• hypersensitivity to azithromycin, as well as other components of the drug or any antibiotic from the category of ketolides with macrolides;
• Do not combine with ergot alkaloids;
• use in severe forms of kidney or liver dysfunction;
• It is prohibited to prescribe to children whose weight is less than 45 kg.

Side effects Zithrolex

Taking capsules sometimes causes various side effects:

• systemic circulation: mild transient neutropenia, and also thrombocytopenia;
• CNS damage: headaches, fainting, vertigo, insomnia or a feeling of drowsiness. In addition, the appearance of paresthesia, olfactory or gustatory disorders, as well as asthenia;
• mental manifestations: occasionally there are feelings of strong anxiety, as well as aggressiveness, nervousness or restlessness, and in addition hyperactivity;
• hearing disorders: tinnitus, noticeable hearing loss or complete deafness (most of these disorders can be cured);
• problems with the functioning of the cardiovascular system: heart rhythm disturbance or arrhythmia due to the development of ventricular tachycardia. In addition, ventricular fibrillation, prolongation of the QT interval, and also chest pain and decreased blood pressure are occasionally observed;
• Gastrointestinal tract lesions: abdominal cramps or pain, nausea, loose stools and diarrhea, as well as dyspeptic symptoms, vomiting or constipation. Anorexia, gastritis with pancreatitis may also occur, as well as bloating, loss of appetite and a change in the color of the tongue. Pseudomembranous colitis is occasionally observed;
• liver disorders: rarely, patients develop hepatitis or intrahepatic cholestasis or moderately increase the activity of liver transaminases (treatable disorder). Hepatic dysfunction (rarely causes death) or necrotic hepatitis are noted in isolated cases;
• skin lesions: rashes with urticaria and itching, photosensitivity, Quincke's edema, TEN, erythema multiforme and Stevens-Johnson syndrome;
• reactions of the musculoskeletal system: development of arthralgia;
• lesions of the urinary organs: acute stage of renal failure, and in addition tubulointerstitial nephritis;
• reproductive disorders: the appearance of vaginitis;
• Others: development of anaphylaxis (this includes swelling, which occasionally leads to death) or candidiasis.

Overdose

Symptoms of intoxication include nausea, transient hearing loss, diarrhea, or severe vomiting.

If an overdose occurs, it is necessary to take activated charcoal and also perform standard symptomatic therapy procedures.

Interactions with other drugs

Antacids (containing aluminum, magnesium and calcium), ethyl alcohol and food weaken the degree and decrease the rate of absorption of the drug, so it is necessary to take these drugs separately - 1 hour before or 2 hours after.

Lincosamides reduce, and chloramphenicol with tetracycline increase the effect of Zitrolex.

The drug is not pharmaceutically compatible with the substance heparin.

The drug should be used with caution in people who are already using other drugs that can prolong the QT interval.

It is necessary to monitor the patient's condition in case of taking drugs with cyclosporine, ergot derivatives, terfenadine, as well as with carbamazepine and theophylline with digoxin. This is necessary due to the fact that macrolides can potentiate the effect of the above-described medications.

Azithromycin reduces the rate of excretion and increases the toxic properties and plasma values of indirect anticoagulants.

The drug should be combined with zidovudine and nelfinavir with caution, because macrolides enhance the properties of these substances.

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Storage conditions

Zitrolex should be stored in places inaccessible to small children. The temperature in the storage room is a maximum of 25°C.

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Shelf life

Zitrolex can be used for a period of 3 years from the date of manufacture of this medication.