Ziomycin

Ziomycin is a systemic antibacterial drug from the category of lincosamides, macrolides and streptogramins. Contains an element of azithromycin.

Indications of the ziomycin

It is used in the treatment of infectious diseases that were provoked by bacteria that are sensitive to the azithromycin component:

• ENT organs - sinusitis or otitis media, and in addition tonsillitis or pharyngitis of bacterial type;
• respiratory system - non-hospital pneumonia, and with it the bacterial form of bronchitis;
• soft tissues with skin: the initial stage of development of tick-borne borreliosis, impetigo with erysipelas, and in addition piodermatosis of secondary type;
• STDs: cervicitis caused by exposure to Chlamydia trachomatis, and in addition urethritis (with or without complications).

Release form

Release in tablet form, according to 6 or 21 pieces inside the blister pack. In the pack, there is 1 such blister.

Pharmacodynamics

Element azithromycin is a macrolide from the category of azalides. This molecule is formed after the introduction into the lactone ring of erythromycin type A nitrogen atom.

The substance acts by inhibiting the process of protein binding of bacteria as a result of synthesis with the ribosomal 50 S subunit, and in addition by suppressing the peptide translocation.

A full cross-type stability with respect to the azithromycin and erythromycin substances, and other lincosamides with macrolides, is formed among pneumococci, fecal enterococci with golden staphylococci (here, among other things, there are staphylococci with a resistance to the methicillin component), and along with this, the so-called β-hemolytic streptococcus, an element from the category A.

Acquired resistance can spread in different ways, taking into account the time, as well as places for designated categories, which is why local stability data are especially needed during the treatment of infections in the severe stage of development.

The range of antimicrobial drug activity is quite diverse.

Among sensitive microorganisms:

• Gram-positive aerobes - sensitive to methicillin, golden staphylococci, penicillin-sensitive pneumococci, and along with them pyogenic streptococcus;
• aerobes of the gram-negative type - Haemophilus parainfluenzae with Influenza rod, Moraxella cataralis with legionella pneumophile, and in addition pasturella multocid;
• anaerobes - Fusobacterium spp., clostridium perfringens, prevotella, as well as Porphyriomonas spp .;
• other bacteria - chlamydophile pneumonia with Chlamydia trachomatis, and with it mycoplasma pneumonia.

Among microorganisms that are able to acquire resistance to the drug: Gram-positive aerobes - resistant to penicillin or having an intermediate sensitivity to it pneumococci.

Bacteria possessing congenital resistance:

• Gram-positive aerobes - fecal enterococcus, as well as methicillin-sensitive staphylococci are golden;
• anaerobes are some pathogenic microorganisms from the category of bacteroidoid fragilis.

Pharmacokinetics

As a result of taking the tablet inside, the bioavailability level of the medicament is about 37%. Peak serum values of the drug are displayed after 2-3 hours after the application of the drug.

The distribution of the substance occurs throughout the body. Pharmacokinetic tests have determined that the level of the component inside tissues far exceeds its plasma values (by 50 times). This demonstrates its significant connection with tissues.

The level of protein synthesis inside the plasma varies with the existing plasma values and is at least 12% (0.5 μg / ml) and a maximum of 52% (0.05 μg / ml) within the blood serum. In this case, the equilibrium value of the distribution volume is 31.1 l / kg.

The final time of plasma half-life is similar to the half-life of Ziomycin from tissues - in the interval of 2-4 days.

About 12% of the used dose of drugs is excreted simultaneously with the urine in unchanged form - during the next 3 days. Very high indices of the unchanged component were noted inside the bile, in addition to which 10 decay products of the drug formed during the N-, as well as O-demethylation, cleavage of the cladinose element conjugate were also found, and in addition, with the hydroxylation of aglycon and, in addition, dezosamine rings.

Dosing and administration

The medicine is taken once a day, without taking into account the eating habits. It is necessary to swallow the tablets without chewing them. If the dose was missed for some reason, it should be taken as soon as possible, and all the following doses should be consumed with an interval of 24 hours.

Children weighing more than 45 kg, as well as adults.

During the treatment of infectious diseases related to the respiratory system, ENT organs, and in addition to soft tissues with skin (in addition to the migrating form of erythema of chronic nature), the total dose of azithromycin per course is 1500 mg. In this case, the daily portion of the drug is 500 mg (a single dose of 2 tablets). The course lasts for 3 days.

To eliminate erythema migratory type for the entire course of taking 3 grams of medication. The scheme of reception is as follows: the first dose of Ziomycin in the first day (for 1 consumption - 4 tablets), and then - 500 mg (for taking 2 tablets) during the 2-5th days. The total duration of therapy is 5 days.

Treatment of STDs: the size of the total portion of the drug is 1 g. It is required to consume 4 tablets of the drug once.

Elderly patients.

Because older people may be at risk of developing electrical cardiac conduction disorders, it is necessary to use the medication, taking care, because its reception increases the likelihood of pirouette tachycardia or arrhythmia of the heart.

People with kidney problems.

Azithromycin should be used with great care in individuals with functional renal impairment to a severe degree (at a glomerular filtration rate <10 ml / minute).

People with eating disorders in the liver.

Because the metabolism of azithromycin is carried out in the liver, and its excretion occurs with bile, it is forbidden to use drugs in the presence of severe disorders in hepatic work. No tests have been performed regarding the treatment of such individuals with azithromycin.

[1]

Use of the ziomycin during pregnancy

Testing for the effects of medication on the reproductive system of animals was carried out using dosages that are moderately toxic to the body of a pregnant woman. These tests did not show that azithromycin has a toxic effect on the fetus. Although it is still necessary to take into account that well-controlled adequate tests with the participation of pregnant women have not been conducted. And therefore, since testing of the impact on the reproductive activity of animals does not always show results similar to that of drugs on the human body, it is recommended to prescribe Ziomycin only in the presence of serious life indications.

There is information about the incidence of azithromycin in breast milk, although no relevant studies of this effect have been conducted. Therefore, it is possible to use the medicine during lactation only in situations where the possible benefit of taking it for a treating woman will exceed the likelihood of complications in the infant.

Fertility testing was performed in rats - the frequency of conception after the application of the active drug component decreased. But there is no evidence that such an effect substance can have on humans.

Contraindications

Among the contraindications:

• intolerance against erythromycin with azithromycin, and in addition any ketolides or macrolides, and at the same time other components of the medicament;
• because in theory when combining a medicine with ergot derivatives, it is possible to develop ergotism, it is forbidden to combine these drugs;
• children weighing less than 45 kg.

Side effects of the ziomycin

The use of tablets can cause some side reactions:

• pathology of infectious or invasive nature: candidiasis (this includes its oral form), infections in the vagina, fungal or bacterial infection, pulmonary pneumonia, runny nose with pharyngitis, and in addition gastroenteritis and pseudomembranous form of colitis;
• problems from the general blood flow and lymph: development of eosinophilia, thrombocyto-, leuko-, and also neutropenia and hemolytic form of anemia;
• immune disorders: manifestations of hypersensitivity (among them Quincke edema and anaphylactic symptoms);
• disturbances in metabolic processes: the appearance of asthenia or anorexia;
• mental disorders: sensation of nervousness, aggression, agitation, anxiety, anxiety, the appearance of hallucinations or insomnia, and with it the development of delirium;
• reactions of the organs of the National Assembly: the appearance of dizziness or headaches, seizures, paresthesias, and sensation of drowsiness. In addition, syncope, parosmia, dysgeusia with agevia and anosmia with hypesthesia and myasthenia gravis develop. There is also an increase in psychomotor activity;
• manifestations in the field of visual organs: decreased vision or its disorder;
• disturbances in the function of the auditory organs: reduction or disorder of hearing (among the manifestations - ear ringing or development of deafness);
• disorders in the heart: palpitation and change in the rhythm of the heartbeat, pirouette tachycardia, as well as arrhythmia (this list includes ventricular tachycardia) and an increase in the QT interval on the ECG;
• vascular disorders: the appearance of tides or a marked decrease in blood pressure;
• manifestations of the respiratory system: a problem with the respiratory function, dyspnea, and also bleeding from the nose;
• disorders of the gastrointestinal tract: the appearance of discomfort, vomiting, abdominal pain, diarrhea and nausea. Sometimes, too, there is frequent and loose stools, dyspepsia and bloating, constipation or gastritis, pancreatitis, anorexia and dysphagia. There may be a burp, increased salivation, dry mouth mucous membranes or ulcers in the mouth, and in addition to change the color of the tongue;
• disorders of the hepatobiliary system: liver failure develops (ends with death), functional hepatic impairment, hepatitis (among other things - necrotic and fulminant form of pathology) and intrahepatic cholestasis;
• lesions of the skin and subcutaneous layer: itching, dryness, rashes, photosensitivity, increased sweating, development of dermatitis, hives, TEN, erythema multiforme and Stevens-Johnson syndrome;
• disorders of the muscles and bones: the appearance of myalgia, pain in the neck or back, and also osteoarthritis and arthralgia;
• urinary system reaction: kidney pain, kidney failure in the acute stage, as well as dysuria and tubulointerstitial nephritis;
• problems in the operation of the breast with reproductive organs: bleeding from the uterus, vaginitis, and in addition testicular lesions;
• systemic disorders: a feeling of malaise or increased fatigue, pain in the sternum, hyperthermia or asthenia, as well as swelling (peripheral type, as well as on the face);
• the results of laboratory diagnostics: a decrease in the number of leukocytes and bicarbonate values inside the blood. In addition, an increase in the number of eosinophils, neutrophil and monocyte counts, as well as the level of ALT and AST. The values of creatinine, urea or bilirubin inside the blood, the values of sugar, alkaline phosphate, chloride, bicarbonate and chloride can also increase. It is also possible to lower hematocrit, change blood levels of potassium and deviate sodium levels;
• intoxication and lesions: the development of complications after the procedure.

Overdose

Among the manifestations of poisoning: the reactions that occur when taking higher dosages of drugs are similar to the side effects that occur when using standard servings - nausea, curable hearing loss, vomiting and diarrhea.

To eliminate these symptoms, it is required to take activated charcoal, and then carry out the procedures that are necessary to maintain the patient's stable condition and treatment of the disorders.

Interactions with other drugs

Caution is required when using azithromycin in people taking medications that can prolong the QT interval.

Antacid drugs.

During the study of the pharmacokinetic parameters of the active substance Ziomycin, when combined with antacids in general, no changes in its bioavailability were found, but the tests showed a decrease in the peak level of the drug within the plasma (approximately 25%). It is required to use azithromycin not less than 1 hour before the use of antacids or after a minimum of 2 hours after their use.

Digoxin.

There is evidence that the combination of macrolides (among which azithromycin) with substrates of the P-glycoprotein component (among them digoxin) causes an increase in the serum values of the substrate of the P-glycoprotein element. As a consequence, with this combination, it is always necessary to keep in mind the possibility of increasing the serum level of digoxin.

Zidovudine.

Azithromycin, used once in a dosage of 1000 and 1200 mg or repeatedly at a dosage of 600 mg, had no effect on the plasma parameters of zidovudine or urinary excretion of this element (or its glucuronic-type products). However, the use of azithromycin increased the values of zidovudine phosphorylated type (this is a drug-active decay product) in mononuclear cells within the peripheral blood flow. The significance of this information for treatment is not defined, but this information can be useful for the treated.

Azithromycin weakly interacts with the hemoprotein system P450. It is believed that this component does not have such a pharmacokinetic interaction with similar elements, which is noted in erythromycin and other macrolides. The substance azithromycin does not induce / inactivate hemoprotein P450 through hemoprotein metabolite compounds.

Tests were conducted for the interaction of the drug with individual substances that undergo significant metabolism with the help of hemoprotein P450:

• cyclosporine - some substances related to macrolides may affect the metabolism of this component. Since there is no information on the probability of interaction in the case of a combination of azithromycin with cyclosporine, it is required to carefully evaluate the drug picture before prescribing the combined treatment. If a decision is made that such therapy will be appropriate, it is required during its carrying out to closely monitor the cyclosporine parameters and change its doses in accordance with them;
• fluconazole - a combination of a single dose azithromycin (in the amount of 1200 mg) with a single dose of fluconazole 800 mg did not change the pharmacokinetic characteristics of the latter. The half-life and the level of AUC azithromycin did not change when combined with fluconazole, although a slight decrease in the peak level of azithromycin (by 18%) was observed;
• nelfinavir - azithromycin (in a dose of 1200 mg) with an equilibrium dosage of nelfinavir (a 3-fold intake of 750 mg of medication per day) increases the azithromycin values. But clinically noticeable adverse reactions were not noted, therefore, it is not necessary to change the dose size.

[2], [3]

Storage conditions

Ziomycin should be kept at temperatures not exceeding 25 ° C, inaccessible to children.

Special instructions

Reviews

Ziomycin is considered a very effective medication that helps in the treatment of diseases of an infectious origin - for example, it works very well in eliminating pathologies in the area of ENT organs.

But at the same time, the testimonies also testify to the presence of some shortcomings, among which there are many side effects, and besides this high cost. Also, when taking the drug must take into account that it is an antibiotic, so take it with caution.

Shelf life

Ziomycin can be used during the 3 years since the manufacture of the drug.