Zyromin

Zyromin is a systemic antimicrobial drug from the group of lincosamides and macrolides, and at the same time streptogramins.

Indications of the zyromin

It is used for pathologies of an infectious origin that were provoked by some bacteria sensitive to the substance azithromycin:

• in the upper part of the respiratory tract, as well as inside the ENT organs: sinusitis with tonsillitis, and in addition pharyngitis with otitis media (both diseases - in acute form);
• in the lower part of the respiratory tract: inflammation of the lungs (atypical or bacterial form) and exacerbated chronic bronchitis;
• subcutaneous layer and skin: the first stage of Lyme borreliosis, various piodermatoses of secondary degree, and in addition impetigo or erysipelas. Together with this, it can be prescribed when ordinary acne is eliminated in an easy form;
• STDs: pathologies such as cervicitis or urethritis (with or without complications), triggered by the pathogenic microbe Chlamydia trachomatis.

Release form

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

Pharmacodynamics

The component azithromycin is azalide, a representative of the macrolide subcategory. He has a large 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 influences these pathogenic microbes both in 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 form of aerobes: haemophilus influenzae and Haemophilus parainfluenzae, and in addition moraxella cataris with gonococcus and listeria monocytogenes with a pertussis tick;
• other bacteria: chlamydophile pneumonia with Chlamydia trachomatis and legionella pneumophilia, and in addition ureaplasma urealichym with mycoplasma pneumonia, as well as the causative agent of tick borreliosis (Borrelia Burgdoria bacterium) and Mycobacterium avium.

Azithromycin has a high activity of action 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 germs of Gram-positive form (fecal enterococci), and in addition most strains of staphylococci (which have a sensitivity to the activity of the substance methicillin) and anaerobes such as phageitis bacteroids.

Pharmacokinetics

The medicinal component easily passes through the hematoparenchymal barrier, and then enters the tissues. In this case, inside the tissues of the urogenital (this includes the prostate) and the respiratory system, and at the same time, the indices of the drug (10-50 times) as compared with the plasma are observed inside the lungs and soft tissues with the skin, and within the infectious focus this figure 24-34% higher than inside tissues in healthy areas.

The substance passes inside the cells of the membranes (so the drug is very effective during the treatment of infections that were provoked by the pathogens inside the cells). Moves to the site of infection with the help of phagocytes, macrophages, as well as polymorphonuclear leukocytes, and then released there in the process of phagocytosis.

The active ingredient is absorbed very quickly from the plasma into the tissues with the cells, passes into the cells of the phagocytes 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 the application Drugs).

The substance is stable within the acid medium, and is also lipophilic. The bioavailability level of the drug is 34%.

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

Excretion of azithromycin is carried out mainly in unchanged form - 50% together with bile, and 6% more with urine. Inside the liver, the substance is dimethylated, losing its activity.

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

Dosing and administration

Tablets medicine should be consumed before daily meals (about 60 minutes) or after this (after 120 minutes), because the use of food interferes with the absorption of drugs. The medication takes place once a day, the tablet should be swallowed without chewing.

Dose sizes for adults, children weighing more than 45 kg and elderly people:

• in the treatment of violations in the field of ENT organs: according to the 1st pill (0.5 g) every day in the period of 3 days;
• disorders within the respiratory system: take each day for the first pill (0.5 g) for 3 days;
• soft tissue damage along with the skin surface: in the period of 3 days, take 1 tablet (0.5 g) daily;
• at the initial stage of tick-borne borreliosis: for adults - on the first day, taking 2 tablets (1 g) of Zyromin, and then during the 2-5th days - on the 1st tablet (0.5 g). The whole course lasts 5 days;
• to eliminate common acne: for the course you need to take in the amount of 6 g of medicine. The standard treatment regimen is to drink 1 tablet a day (0.5 g / day) during the first 3 days, and then take 0.5 g / week for the next 9 weeks;
• urethritis of uncomplicated type or cervicitis provoked by the activity of the bacterium Chlamydia trachomatis: it is necessary to take 2 tablets of medicines once (1 g of substance) once.

With kidney failure.

Testing of the effect of the drug on people with QC values <40 ml / minute was not performed, so this category of people who are being treated should be treated with extreme caution.

With liver failure.

Due to the fact that the metabolism of the active component of Zyromin occurs in the liver, and its excretion is carried out with bile, it is forbidden to prescribe medication for people suffering from hepatic diseases in a severe degree.

[1]

Use of the zyromin during pregnancy

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

In this regard, azithromycin is allowed to be prescribed to pregnant women only in situations where it can be expected that the benefit to the mother will be higher than the risk of complications, and in addition, in the absence of suitable alternative drugs.

If the medicine needs to be taken during lactation, it is required to take a decision to stop breastfeeding during this period.

Contraindications

The main contraindications:

• the presence of hypersensitivity to the active substance, as well as all other components of drugs, or other macrolides;
• functional hepatic / renal disorders in severe degree;
• since in theory a drug can cause the development of ergotism when combined with ergot derivatives, one should abandon such a combination of drugs;
• use in children whose weight does not reach 45 kg.

Side effects of the zyromin

The taking of tablets can cause the appearance of certain side reactions:

• violations of the function of lymph and total blood flow: occasionally thrombocytopenia occurs. There are also isolated data on the periods of transient or weak neutropenia (although in this case it was not possible to identify a causal relationship with the use of Zyromin);
• mental problems: occasionally there are feelings of anxiety, increased aggressiveness or strong nervousness, and with it one can expect the development of hyperactivity;
• manifestations in the NA area: sometimes there is a feeling of drowsiness, and also fainting, dizziness, frustration of taste and olfactory receptors, and at the same time there are seizures (also can be caused by the action of other macrolides) and headaches. Occasionally, insomnia or asthenia, as well as paresthesia, are noted;
• lesions of auditory organs: occasionally there were reports that macrolides damage the auditory function. Individual people who took the medicine developed hearing disorders, ear ringing, and deafness. Most of these cases occur in experimental tests, when azithromycin has been used for a long time in high dosages. According to existing reports on follow-up medical observation, it can be concluded that most of these violations were reversible;
• problems with cardiac function: occasionally there is an increase in the rhythm of the heartbeat, and in addition, an arrhythmia, in connection with which there is a ventricular tachycardia (as it was discovered, these disturbances are caused by the remaining macrolides). There is a single ventricular fibrillation and flutter, and in addition the QT is prolonged and the blood pressure drops;
• disorders in the work of the digestive tract: often patients develop diarrhea, spasms and pains (discomfort) in the abdomen, nausea and vomiting. Sometimes, bloating, loose stools, digestive problems and anorexia are noted. Occasionally there is a change in the shade of the tongue or constipation. There is information about the occurrence of pancreatitis, melena, dyspeptic manifestations and colitis in a pseudomembranous form;
• manifestations in the area of GVP and liver: occasionally there is hepatitis and intrahepatic cholestasis. Pathological test results for hepatic function, necrotic form of hepatitis and hepatic dysfunction are also noted, which leads to death in single cases;
• skin disorders: occasionally there are symptoms of severe allergies - for example, Quincke's edema, photosensitivity and urticaria. There may be severe skin lesions (including multi-form erythema, TEN, and in addition Stevens-Johnson syndrome). Sometimes there is also a rash and itching;
• damage to the structure of muscles and bones: sometimes arthralgia develops;
• disorders of the function of urination: occasionally one can expect the development of kidney failure in the acute stage, as well as the appearance of tubulointerstitial nephritis;
• lesions of the reproductive system: sometimes there is vaginitis;
• common manifestations: occasionally, patients have anaphylaxis (this includes swelling, which can lead to death), and candidiasis;

Indicators of laboratory studies and analyzes: there may be an increase in potassium, phosphokinase, bilirubin, as well as alkaline phosphatase, serum creatinine and sugar. Thrombocytopenia, neutropenic or leukopenia occurred occasionally.

Overdose

Among the standard manifestations of an overdose: severe diarrhea or vomiting with severe nausea, and in addition to it are curable hearing problems.

When poisoning the drug, you need to give the patient activated charcoal, and then adhere to the methods of supportive and symptomatic treatment. The medicine does not have an antidote.

Interactions with other drugs

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

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

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

Individual related drugs from the category of macrolide agents have a significant effect on the metabolism of the component cyclosporin. Because drug and pharmacokinetic tests of this interaction have not been performed, before using these drugs in combination it is necessary to carefully evaluate the existing clinical picture. If a decision is made on the appropriateness of such a combination, it is required to closely monitor the parameters of cyclosporine and to change its dosages in accordance with them.

There is information about an increase in the incidence of bleeding due to drug use along with indirect anticoagulants (oral coumarin anticoagulants or warfarin medication). Therefore, with such a combination, it is strongly recommended that we constantly monitor any changes in the performance of the PTV.

There is evidence that individual drugs from the macrolide category are able to have a significant effect on the digoxin element metabolism in the intestine. Because of this, when combined taking these drugs, it is necessary to take into account the probability of increasing the level of digoxin and monitor its performance.

Caution is required if azithromycin is used together with terfenadine.

It is necessary to adhere to a minimum of 2-hour intervals between the use of Zyromin and cimetidine.

[2], [3]

Storage conditions

Zyromin is required to be kept in a place that will be inaccessible to children and closed from sunlight. Storage temperature is a maximum of 30 ° C.

[4]

Shelf life

Ziromin is allowed to be used in the period of 5 years from the date of manufacture of the medicament.