Azitrox capsules 250 mg, 6 pcs. (Azithromycin)

Release form

capsules

Packing

6 pcs.

Pharmacological action

Pharmacotherapeutic group:

antibiotic-azalide

ATX code: [J01FA10]

Pharmacological properties of

Pharmacodynamics

Broad-spectrum antibiotic. It is a representative of the subgroup of macrolide antibiotics - azalides. By binding to the 50S subunit of ribosomes, it inhibits the peptide translocase at the translation stage, inhibits protein synthesis, slows the growth and reproduction of bacteria, acts bacteriostatically, and has a bactericidal effect in high concentrations.

Acts on extra- and intracellular pathogens.

Active against gram-positive aerobic microorganisms: Streptococcus spp. (groups A, B, C, G), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Staphylococcus aureus (methicillin-sensitive) gram-negative aerobic microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella legarhella Neisseria gonorrhoeae, Pasteurella multocida of some anaerobic microorganisms: Prevotella spp., Clostridium perfringens, Fusobacterium spp., Porphyriomonas spp. as well as Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Microorganisms capable of developing resistance to azithromycin: gram-positive aerobes (Streptococcus pneumoniae (penicillin-resistant)). Initially resistant microorganisms: gram-positive aerobes (Enterococcus faecalis, Staphylococcus spp. (Methicillin-resistant staphylococci show a very high degree of resistance to macrolides), gram-positive bacteria resistant to erythromycin) anaerobes (Bacteroides fragilis).

Pharmacokinetics

Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. After oral administration of 500 mg, the maximum concentration of azithromycin in blood plasma is reached after 2.5-3.0 hours and is 0.4 mg / L. Bioavailability is 37%.

Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate gland), into the skin and soft tissues. A high concentration in tissues (10-50 times higher than in blood plasma) and a long half-life are due to the low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding lysosomes.

This, in turn, determines the large apparent volume of distribution (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate primarily in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to the sites of localization of the infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function.

Azithromycin persists in bactericidal concentrations in the focus of inflammation for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.

In the liver, demethylates, the resulting metabolites are inactive.

Excretion of azithromycin from blood plasma takes place in 2 stages: The half-life is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours, which allows you to use the drug 1 time / day.

Azithromycin is excreted mainly unchanged - 50% by the intestines, 12% by the kidneys.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug, including:

infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media)

infections of the lower respiratory tract (pneumonia including bronchitis caused by atypical pathogens, including acute, exacerbation of chronic)

infections of the urogenital tract (urethritis, cervicitis)

infections of the skin and soft tissues (Lyme disease (initial stage - erythema migrans), erysipelas, impetigo, secondary pyodermatosis, acne ordinary (acne) moderate).

Contraindications

Hypersensitivity to azithromycin (including other macrolides), the components of the drug severe liver failure: more than 9 points on the Child-Pugh scale (no data on efficacy and safety) severe renal failure: creatinine clearance (QC) less than 40 ml / min (there is no data on efficacy and safety) children under the age of 12 years with a body weight of less than 25 kg (for this dosage form) are taking ergotamine and dihydroergotamine simultaneously.

With caution

With moderate hepatic impairment (7-9 Child-Pugh score) of chronic renal failure (CC more than 40 ml / min), arrhythmias or a predisposition to arrhythmias and lengthening of the QT interval while taking terfenadine, warfarin, digoxin with myasthenia gravis during pregnancy.

Use during pregnancy and lactation

Use of the drug during pregnancy is only possible if the intended benefit to the mother outweighs the potential risk to the fetus.

Case reports and observational studies have shown that the use of azithromycin during pregnancy does not increase the frequency of adverse pregnancy outcomes and is not associated with the occurrence of any specific malformations in the child.

If necessary, the appointment of the drug during lactation should stop breastfeeding.

Special instructions

If you miss one dose of the drug, you should take the missed dose as soon as possible, and the subsequent ones at 24-hour intervals. Azithromycin should be taken at least 1 hour before or 2 hours after taking antacid drugs.

Azithromycin should be used with caution in patients with moderate hepatic impairment due to the possibility of developing fulminant hepatitis and severe liver failure in such patients. If there are symptoms of impaired liver function (rapidly increasing asthenia, jaundice, dark urine, a tendency to bleed, hepatic encephalopathy), azithromycin therapy should be discontinued and a study of the functional state of the liver should be carried out.

In moderate renal failure (CC greater than 40 ml / min), azithromycin should be administered under the control of renal function.

Concomitant use of azithromycin with ergotamine and dihydroergotamine derivatives is contraindicated due to the possible development of ergotism.

When using the drug, both on the background of taking it, and 2-3 weeks after stopping treatment, diarrhea caused by Clostridium difficile (pseudomemranous colitis) may develop. In mild cases, discontinuation of treatment and the use of ion-exchange resins (colestyramine, colestipol) is sufficient, in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole are indicated. Do not use drugs that inhibit intestinal motility.

Since QT interval prolongation is possible in patients receiving macrolides, including azithromycin, when using azithromycin, caution should be exercised in patients with known risk factors for lengthening the QT interval: old age electrolyte imbalance (hypokalemia, hypomagnesemia) syndrome of congenital lengthening of the QT interval of heart disease (heart failure, myocardial infarction, bradycardia) while taking medications that can extend the interval QT (including antiarrhythmic drugs of classes IA and III, tricyclic and tetracyclic antidepressants, antipsychotics, fluoroquinolones).

Azithromycin can provoke the development of myasthenic syndrome or cause exacerbation of myasthenia gravis.

WHO Europe recommends azithromycin as the drug of choice for treating chlamydial infections in pregnant women. Azithromycin at risk of use in pregnant women, according to the FDA classification, it belongs to category B (animal reproduction studies did not reveal fetal damage due to azithromycin, but controlled studies in pregnant women were not conducted).

Composition

Active ingredient:

azithromycin dihydrate in terms of azithromycin - 250 mg.

Excipients:

mannitol (mannitol) - 54.58 mg,

corn starch - 13.10 mg,

magnesium stearate - 2.0 mg,

sodium lauryl sulfate - 0.32 mg

Capsules, hard gelatin capsule composition:

body and cap - titanium dioxide (E 171),

gelatin (medical gelatin).

Dosage and administration

Inside, 1 hour before or 2 hours after meals, 1 time per day.

Adults with infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues (except for the initial stage of Lyme disease (erythema migrans) and moderate acne) - 500 mg (2 capsules) per day for 1 dose for 3 days (course dose - 1.5 g).

At the initial stage of Lyme disease (erythema migrans) - 1000 mg (4 capsules) per day on the first day at a time, then 500 mg (2 capsules) per day daily from 2 to 5 days (course dose - 3 g).

When acne is indicated, ordinary (acne) of moderate severity on the 1st, 2nd and 3rd day of treatment, take 500 mg (2 capsules) once a day, then take a break from the fourth to the seventh day, from the eighth day of treatment, take 500 mg (2 capsules) once a week for 9 weeks (course dose of 6 g)

For infections of the urogenital tract (urethritis, cervicitis), 1 g (4 capsules) is crushed once for the treatment of uncomplicated urethritis or cervicitis .

For children with a body weight of 25 to 45 kg for infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 250 mg / day for 3 days in the treatment of the initial stage of Lyme disease (erythema migrans) - 500 mg (2 capsules) on the first day and 250 mg daily from 2 to 5 days (course dose - 1.5 g).

Children weighing more than 45 kg with infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 500 mg (2 capsules) per day for 1 dose for 3 days in the treatment of the initial stage of Lyme disease (erythema migrans) - 1000 mg (4 capsules) on the first day and 500 mg (2 capsules) daily from 2 5 days each (course dose - 3 g).

Side effects

Most of the reported adverse reactions are reversible after the end of treatment or drug withdrawal.

Classification of the incidence of side effects (WHO): very often (with a frequency of more than 1/10), often (with a frequency of at least 1/100, but less than 1/10), infrequently (with a frequency of at least 1/1000, but less 1/100), rarely (with a frequency of at least 1/10000, but less than 1/1000), very rarely (with a frequency of less than 1/10000), (including individual messages).

From the circulatory and lymphatic systems: often - lymphocytopenia, eosinophilia infrequently - leukopenia, neutropenia very rarely - thrombocytopenia, hemolytic anemia.

From the side of the central nervous system: often - dizziness, headache, paresthesia, violation of the perception of taste sensations, anorexia infrequently - anxiety, nervousness, hyposthesia, insomnia, drowsiness rarely - agitation very rarely - fainting, cramps, psychomotor hyperactivity, anosmia, loss of taste, parosmia, aggravation of myasthenia gravis.

On the part of the sensory organs: infrequently - decreased hearing acuity, tinnitus rarely - vertigo, decreased visual acuity, deafness.

From the cardiovascular system: infrequently - sensation of a heartbeat is rare - decrease in blood pressure is very rare - arrhythmia, including: ventricular tachycardia, increased QT interval, pirouette type arrhythmia.

From the digestive system: very often - nausea, diarrhea, abdominal pain, flatulence often - vomiting infrequently - gastritis, constipation, melena very rarely - discoloration of the tongue, pseudomembranous colitis, pancreatitis

From the side of the liver and biliary tract: infrequently - hepatitis, hyperbilirubinemia, increased activity of “liver” transaminases very rarely - cholestatic jaundice, liver failure (in rare cases with fatal outcome, mainly due to impaired liver function), fulminant hepatitis, liver necrosis .

Allergic reactions: often - itching, rash not often - Stevens-Johnson syndrome, photosensitivity, urticaria very rarely - anaphylactic reactions (including angioedema) in rare cases with fatal outcome, toxic epidermal necrolysis, erythema multiforme.

From the musculoskeletal system: often - arthralgia.

From the genitourinary system: infrequently - an increase in residual urea nitrogen and plasma creatinine concentration is very rare - interstitial nephritis, acute renal failure.

Other: often - weakness infrequently - chest pain, peripheral edema, asthenia, hyperglycemia, conjunctivitis.

Infections and infestations: infrequently - vaginitis, candidiasis of various localizations.

Any side effect should be reported to your healthcare provider.

Drug interactions

Antacids (aluminum and magnesium) do not affect the bioavailability of azithromycin, but reduce its maximum concentration in the blood by 30%, so the interval between their intake should be at least 1 hour before or 2 hours after taking these drugs. With the simultaneous administration of ergotamine and dihydroergotamine derivatives, it is possible to increase their toxic effect (vasospasm, dysesthesia).

When combined with indirect anticoagulants, coumarin (warfarin) and azithromycin (in usual doses), patients need careful monitoring of prothrombin time.

Caution should be exercised when co-administering terfenadine and azithromycin, since it has been established that the simultaneous administration of terfenadine and macrolides can cause arrhythmia and lengthening of the QT interval. Based on this, the above complications cannot be excluded with the combined use of terfenadine and azithromycin.

When used simultaneously with cyclosporine, it is necessary to control the concentration of cyclosporin in the blood.

With the combined use of digoxin and azithromycin, it is necessary to control the concentration of digoxin in the blood, since many macrolides increase the absorption of digoxin in the intestine.

With simultaneous use with nelfinavir, an increase in the frequency of adverse reactions of azithromycin is possible (hearing loss, increased activity of “liver” transaminases).

When co-administered with azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or the excretion of glucuronide and its metabolite by the kidneys, but the concentration of the active metabolite, phosphorylated zidovudine in mononuclear peripheral blood cells, increases. The clinical significance of this fact is not defined.

With the simultaneous administration of azithromycin and rifabutin in rare cases, the development of neutropenia is possible, the development mechanism of which, as well as the presence of a causal relationship with the drug has not been established.

With concomitant use, fluconazole reduces Cmax of azithromycin by 18%.

Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine, sildenafil, atorvastatin and blood rifabredin.

Consideration should be given to the possibility of inhibition of the CYP3A4 isoenzyme by macrolide drugs while it is used with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism involves this enzyme, however, when using this type of azithromycin noted.

Overdose

When taking high doses of the drug, there may be an increase in side effects: temporary hearing loss, severe nausea, vomiting, diarrhea.

In this case, gastric lavage, activated charcoal administration, symptomatic therapy are shown.

Storage conditions

Do not store above 25 ° C, out of the reach of children.

Shelf life

3 years.

Deystvuyushtee substance

Azithromycin

prescription drugstore holiday

pharmacy terms

drugstore recipe

dosage form

capsules

Prescribing

Prescribing for

Children over 12 years old, Children as prescribed by a doctor, For adults as prescribed by doctor

Pharmstandard-Leksredstva, Russia



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