Ziromine

Ziromin is a systemic antimicrobial drug from the group of lincosamides and macrolides, as well as streptogramins.

Mga pahiwatig Ziromina

It is used for pathologies of infectious origin, which were provoked by certain bacteria sensitive to the substance azithromycin:

• in the upper respiratory tract, as well as inside the ENT organs: sinusitis with tonsillitis, and also pharyngitis with otitis media (both diseases are in acute form);
• in the lower respiratory tract: pneumonia (atypical or bacterial form) and exacerbated chronic bronchitis;
• subcutaneous layer and skin: the first stage of Lyme borreliosis, various secondary pyodermatoses, and also impetigo or erysipelas. Along with this, it can be prescribed for the elimination of common acne in a mild form;
• STDs: pathologies such as cervicitis or urethritis (with or without complications), caused by the pathogenic microbe Chlamydia trachomatis.

Paglabas ng form

Release in tablet form - 3 pieces inside a separate blister pack. The pack of the drug contains 1 blister plate.

Pharmacodynamics

The component azithromycin is an azalide, a representative of the macrolide subcategory. It has a wide range of activity against pathogenic microbes. The substance is synthesized with ribosomes (specifically, with their 50S subunit), which allows it to inhibit the process of protein binding inside bacterial cells, without affecting the binding of polynucleotides.

The drug actively affects these pathogenic microbes both in vitro tests and in the case of clinical infectious processes:

• gram-positive form of aerobes: pneumococci with pyogenic streptococcus and Staphylococcus aureus;
• gram-negative aerobes: Haemophilus influenzae and Haemophilus parainfluenzae, as well as Moraxella catarrhalis with gonococcus and Listeria monocytogenes with whooping cough bacillus;
• other bacteria: Chlamydophila pneumoniae with Chlamydia trachomatis and Legionella pneumophila, as well as Ureaplasma urealyticum with Mycoplasma pneumoniae, as well as the causative agent of tick-borne borreliosis (Borrelia burgdorferi bacteria) and Mycobacterium avium.

Azithromycin has high activity against the microorganism Toxoplasma gondii.

The activity of the component is not weakened in the presence of microbes that produce β-lactamase.

Resistance to the action of the drug is found in gram-positive microbes (fecal enterococci), as well as in most strains of staphylococci (sensitive to the activity of the substance methicillin) and anaerobes such as Bacteroides fragilis.

Pharmacokinetics

The medicinal component easily passes through the hematoparenchymatous barrier and then gets inside the tissues. At the same time, inside the tissues of the urogenital (this includes the prostate) and respiratory system, and at the same time inside the lungs and soft tissues with the skin, increased drug levels are observed compared to plasma (10-50 times), and inside the infectious focus this figure is 24-34% higher than inside the tissues in healthy areas.

The substance penetrates into the cell membranes (therefore the drug is very effective in treating infections caused by pathogens inside the cells). It moves to the site of infection with the help of phagocytes, macrophages, and polymorphonuclear leukocytes, and is then released there in the process of phagocytosis.

The active component is very quickly absorbed from the plasma into the tissues with cells, passes into the phagocyte cells and then moves to the area where the infectious focus is located, creating high and stable drug concentrations inside the affected tissues (they persist for 5-7 days after the end of drug use).

The substance is stable in an acidic environment and is also lipophilic. The bioavailability level of the drug is 34%.

The peak value (0.4 mg/l) is formed after 2-3 hours, and the distribution volume is 31.1 l/kg. Protein synthesis is inversely proportional to the element values in the blood and reaches 7-50%. Taking the tablet with food increases peak values by 23%, but the AUC level remains unchanged.

Azithromycin is excreted mainly in unchanged form - 50% with bile, and another 6% with urine. In the liver, the substance is demethylated, losing its activity.

The clearance of the substance in plasma is 630 ml/min. The drug has a long half-life - within 34-68 hours. In elderly men (within 65-85 years), the pharmacokinetic characteristics remain unchanged. In women, the peak indicator of the drug increases (by 30-50%). But in children aged 1-5 years, the half-life, peak values and AUC level of the drug are lower than in adults.

Dosing at pangangasiwa

The tablets of the medicine must be taken before a daily meal (approximately 60 minutes) or after (after 120 minutes), because taking it with food disrupts the absorption process of the drug. The medicine is taken once a day, the tablet must be swallowed without chewing.

Dose sizes for adults, children weighing over 45 kg and the elderly:

• for the treatment of ENT disorders: 1 tablet (0.5 g) every day for 3 days;
• disorders of the respiratory system: take 1 tablet (0.5 g) every day for 3 days;
• lesions of soft tissues together with the skin surface: take 1 tablet (0.5 g) of the medicine daily for 3 days;
• at the initial stage of tick-borne borreliosis: for adults - on the 1st day, take 2 tablets (1 g) of Ziromin, and then over the course of 2-5 days - 1 tablet (0.5 g). The entire course lasts 5 days;
• to eliminate common acne: a total of 6 g of the medicine is required for the course. The standard treatment regimen is to take 1 tablet per day (0.5 g/day) for the first 3 days, and then take the medicine at a rate of 0.5 g/week for the next 9 weeks;
• uncomplicated urethritis or cervicitis caused by the activity of the bacterium Chlamydia trachomatis: it is necessary to take 2 tablets of the drug (1 g of the substance) once.

In case of kidney failure.

The drug's effect on people with CC values <40 ml/minute has not been tested, so this category of patients should use the drug with special caution.

For liver failure.

Due to the fact that the metabolism of the active component of Ziromin occurs in the liver, and its excretion occurs with bile, it is prohibited to prescribe the drug to people suffering from severe liver diseases.

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Gamitin Ziromina sa panahon ng pagbubuntis

The substance azithromycin is able to overcome the placental barrier, although no negative effect on the child is noted. But it should be noted that appropriate tests to determine the effect of the drug on pregnant women, which would be well controlled, have not yet been conducted.

In this regard, azithromycin is permitted to be prescribed to pregnant women only in situations where the benefit to the mother can be expected to outweigh the likelihood of complications, and also in the absence of suitable alternative drugs.

If the drug must be taken during lactation, a decision must be made to discontinue breastfeeding during this period.

Contraindications

Main contraindications:

• the presence of hypersensitivity to the active substance, as well as all other components of the drug, or other macrolides;
• severe functional liver/renal impairment;
• since in theory the drug can cause the development of ergotism when combined with ergot derivatives, such a combination of drugs should be avoided;
• use in children whose weight has not reached 45 kg.

Mga side effect Ziromina

Taking tablets can cause the appearance of certain side effects:

• disorders of lymphatic function and general blood flow: thrombocytopenia occurs occasionally. There are also isolated data on periods of transient or mild neutropenia (although in this case it was not possible to identify a causal relationship with the use of Ziromin);
• mental problems: occasionally there may be feelings of anxiety, increased aggressiveness or severe nervousness, and along with this, one can expect the development of hyperactivity;
• manifestations in the nervous system: sometimes there is a feeling of drowsiness, and also fainting, dizziness, disturbance of taste and olfactory receptors, and at the same time convulsions (can also be caused by the action of other macrolides) and headaches appear. Insomnia or asthenia, as well as paresthesia are occasionally noted;
• Hearing impairment: Macrolides have been reported to impair hearing in rare cases. Individuals taking the drug have developed hearing impairment, tinnitus, and deafness. Most of these cases occurred in experimental trials where azithromycin was used at high doses over a long period of time. From the available follow-up reports, most of these impairments were reversible;
• problems with cardiac function: occasionally there is an increase in heart rate, and in addition to this, arrhythmia, in connection with which ventricular tachycardia is also observed (as it turned out, these disorders are also caused by other macrolides). Ventricular fibrillation and flutter appear sporadically, and in addition, the QT index is prolonged and the blood pressure level decreases;
• gastrointestinal disorders: patients often experience diarrhea, cramps and pain (discomfort) in the abdomen, nausea and vomiting. Sometimes there is bloating, loose stools, problems with digestion and anorexia. Rarely, there is a change in the color of the tongue or constipation. There are reports of pancreatitis, melena, dyspeptic symptoms and colitis in pseudomembranous form;
• manifestations in the biliary tract and liver: hepatitis and intrahepatic cholestasis occasionally occur. Abnormal liver function tests, necrotic hepatitis and liver dysfunction, which in isolated cases leads to death, are also noted;
• Skin disorders: occasionally, severe allergy symptoms are observed, such as Quincke's edema, photosensitivity, and urticaria. Severe skin lesions may also occur (including erythema multiforme, TEN, and Stevens-Johnson syndrome). Sometimes, rashes and itching also occur;
• damage to the structure of muscles and bones: sometimes arthralgia develops;
• urinary dysfunction: occasionally, acute renal failure may develop, as well as tubulointerstitial nephritis;
• Reproductive system lesions: vaginitis is sometimes observed;
• General manifestations: occasionally, patients experience anaphylaxis (this includes swelling, which can occasionally lead to death) and candidiasis;

Laboratory tests and analysis indicators: an increase in potassium, phosphokinase, bilirubin, as well as alkaline phosphatase, serum creatinine and sugar may be observed. Thrombocyto-, neutro- or leukopenia occurred sporadically.

Labis na labis na dosis

Standard symptoms of overdose include severe diarrhea or vomiting with severe nausea, as well as treatable hearing problems.

In case of poisoning with the drug, the patient should be given activated carbon, and then adhere to supportive and symptomatic treatment methods. The drug has no antidote.

Mga pakikipag-ugnayan sa ibang mga gamot

Like other macrolides, the drug Ziromin significantly potentiates the properties of the substances triazolam, warfarin and ergotamine with phenytoin when used in combination with them.

It is necessary to prescribe the drug with great caution to people who use other drugs that have the ability to prolong QT indices.

During various tests with the combined use of Ziromin and antacids, subtle changes in the pharmacokinetic properties of azithromycin were found - the level of bioavailability remained the same, but the peak values in the plasma decreased by 30%. Therefore, it is recommended to take the drug either 1 hour before the administration of antacids, or 2 hours after their use.

Certain related drugs from the category of macrolides have a significant effect on the process of metabolism of the cyclosporine component. Since drug and pharmacokinetic tests of such interactions have not been performed, before using these drugs in combination, it is necessary to carefully evaluate the existing clinical picture. In case of a decision on the advisability of such a combination, it is necessary to very carefully monitor the cyclosporine indicators and change its dosage in accordance with them.

There is information about an increase in the incidence of bleeding due to taking the drug together with indirect anticoagulants (oral coumarin anticoagulants or warfarin). Therefore, with such a combination, it is strongly recommended to constantly monitor any changes in the PT values.

There is evidence that certain drugs from the macrolide category can have a significant impact on the metabolism of the element digoxin in the intestine. Therefore, when taking these drugs in combination, it is necessary to take into account the possibility of an increase in digoxin levels and monitor its indicators.

Caution is required when using azithromycin with terfenadine.

It is necessary to maintain at least 2-hour intervals between taking Ziromin and cimetidine.

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Mga kondisyon ng imbakan

Ziromin should be stored in a place that is inaccessible to children and protected from sunlight. Storage temperature indicators are a maximum of 30°C.

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Shelf life

Ziromin is allowed to be used for a period of 5 years from the date of manufacture of the drug.