Azithromycin Ecomed pills 250 mg, 6 pcs.

Composition

Composition per tablet:

Active ingredient, mg:

azithromycin dihydrate 262.03 (based on azithromycin) 250.00

Excipients, mg:

lactitol 300.00

croscarmellose sodium 35.00

hyprolose 35.00

pregelatinized starch 20.00

magnesium stearate 14.00

sodium lauryl sulfate 3.50

colloidal silicon dioxide 3.50

microcrystalline cellulose 102 to obtain a tablet without a shell weighing: 700,00

Shell composition, mg:

hypromellose 9.49

titanium dioxide 5.20

macrogol-4000 3.74

talc 1.12

povidone K-17 0.42

quinoline yellow dye 0.03.

Pharmacological action

Pharmacodynamics

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of macrolides-azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. Binding to the 50S subunit of the ribosome, it inhibits peptidtranslase at the translation stage and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations, it has a bactericidal effect.

It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms. Microorganisms can initially be resistant to the action of an antibiotic or acquire resistance to it.

Scale of sensitivity of microorganisms to azithromycin (minimum inhibitory concentration (MIC), mg / ml)

Microorganisms MICK, mg/Sensitive – Sustainable Staphylococcus ≤ 1 > 2Streptococcus A, B, C, G ≤ 0,25 > 0,5 Streptococcus pneumoniae ≤ 0,25 > 0,5 Haemophilus influenzae ≤ 0,12 > 4Moraxella catarrhalis ≤ 0,5 > 0,5 Neisseria gonorrhoeae ≤ 0,25 > 0,5

In most cases, sensitive microorganisms: 1. Gram-positive aerobes:Staphylococcus aureus (methicillin-sensitive)Streptococcus pneumoniae (penicillin-sensitive)Streptococcus pyogenes2. Gram-negative aerobes:Haemophilus influenzaeHaemophilus parainfluenzaeLegionella pneumophilaMoraxella catarrhalisPasteurella multocidaNeisseria gonorrhoeae3. Anaerobes:Clostridium perfringensFusobacterium spp. Prevotella spp. Porphyromonas spp.4. Other microorganisms:Chlamydia trachomatisChlamydia pneumoniaeChlamydia psittaciMycoplasma pneumoniaeMycoplasma hominisBorrelia burgdorferi

Microorganisms capable of developing resistance to azithromycin:gram-positive aerobes:Streptococcus pneumoniae (penicillin – resistant)

Initially resistant microorganisms:gram-positive aerobes:Enterococcus faecalis staphylococcus (methicillin-resistant staphylococci exhibit a very high degree of macrolide resistance)gram-positive bacteria resistant to erythromycin

anaerobesBacteroides fragilis

PharmacokineticsAfter oral administration, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single 500 mg dose is 37% (the ‘first pass ” effect), the maximum concentration (0.4 mg/l) in the blood is created after 2-3 hours, the apparent volume of distribution is 31.1 l / kg, binding to plasma proteins is inversely proportional to the concentration in the blood is 7-50%. Penetrates cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. It easily passes through histohematic barriers and enters the tissues. The concentration in tissues is 10-50 times higher than in plasma, and in the focus of infection-24-34% higher than in healthy tissues. Azithromycin has a very long half-life of 35-50 hours. The tissue half-life is significantly longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged-50% by the intestines,6% by the kidneys. In the liver, it is demethylated, losing its activity.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin: 

• infections of the upper respiratory tract and respiratory tract: pharyngitis, tonsillitis, sinusitis, otitis media;
• infections of the lower respiratory tract: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, incl. caused by atypical pathogens;
• infections of skin and soft tissues: acne vulgaris moderate, erysipelas, impetigo, secondarily infected dermatoses;
• the initial stage of Lyme disease (borreliosis) is a migratory erythema (erythema migrans);
• urinary tract infection caused by Chlamydia trachomatis (urethritis, cervicitis).

Use during pregnancy and lactation

Azithromycin during pregnancy is recommended to be prescribed only in cases where the expected benefit of taking it for the mother exceeds the potential risk to the fetus. During treatment with azithromycin, breastfeeding is suspended.

Contraindications

• hypersensitivity to macrolide antibiotics;
• hypersensitivity to other components of the drug;
• severe hepatic insufficiency
• severe renal insufficiency (creatinine clearance below 40 ml / min);
• children under 12 years of age with a body weight of less than 45 kg (for this dosage form);
• breastfeeding;
• simultaneous administration with ergotamine and dihydroergotamine.

With caution• Myasthenia gravis;• mild to moderate hepatic impairment;• mild to moderate renal impairment (creatinine clearance greater than 40 ml / min); * in patients with proarrhythmogenic factors (especially in elderly patients): patients with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with impaired water-electrolyte balance balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure;• concomitant use of terfenadine, warfarin, digoxin, cyclosporine.

Side effects

the Frequency of side effects is classified in accordance with who recommendations: very often – at least 10%; often – not less than 1% but < 10%; infrequently – no more than 0.1% but < 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely – less than 0.01%; frequency unknown — cannot be estimated from available data. Infectious diseases:infrequently-candidiasis, including oral and genital mucosa, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; unknown frequency-pseudomembranous colitis. From the blood and lymphatic system: infrequently-leukopenia, neutropenia, eosinophilia; very rarely-thrombocytopenia, hemolytic anemia. From the side of metabolism and nutrition: infrequently — anorexia. Allergic reactions:infrequently-angioedema, hypersensitivity reaction; unknown frequency — anaphylactic reaction. From the nervous system: often — headache; infrequently — dizziness, a violation of taste sensations, paresthesia, somnolence, insomnia, nervousness; rarely — agitation; unknown frequency — hypoesthesia, anxiety, aggression, fainting, seizures, psychomotor hyperactivity, loss of smell, a perversion of the sense of smell, loss of taste, myasthenia gravis, delirium, hallucinations. From the side of the organ of vision: infrequently-visual impairment. Hearing disorders and labyrinth disorders: infrequently-hearing disorders, vertigo; unknown frequency-hearing disorders, including deafness and / or tinnitus. From the cardiovascular system: infrequently-palpitations, flushes of blood to the face; unknown frequency-decrease in blood pressure, increase in the QT interval on the ECG, arrhythmia of the “pirouette” type, ventricular tachycardia. Respiratory system disorders:infrequently-shortness of breath, nosebleeds.

From the gastrointestinal tract: very often-diarrhea; often-nausea, vomiting, abdominal pain; infrequently-flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased salivary gland secretion; very rarely — discoloration of the tongue, pancreatitis. From the liver and biliary tract: infrequently-hepatitis; rarely-impaired liver function, cholestatic jaundice; unknown frequency-liver failure (in rare cases with a fatal outcome, mainly against the background of severe liver dysfunction); liver necrosis, fulminant hepatitis. From the skin and subcutaneous tissues: infrequently-skin rash, pruritus, urticaria, dermatitis, dry skin, sweating; rarely-photosensitization reaction; unknown frequency-Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme. Musculoskeletal disorders: infrequently-osteoarthritis, myalgia, back pain, neck pain; unknown frequency-arthralgia. From the side of the kidneys and urinary tract: infrequently-dysuria, pain in the kidney area; unknown frequency-interstitial nephritis, acute renal failure. From the genitals and breast: infrequently — metrorrhagia, testicular dysfunction. Others: infrequently-asthenia, malaise, fatigue, facial swelling, chest pain, fever, peripheral edema. Laboratory data: often, a decrease in the number of lymphocytes, increase in the number of eosinophils, increased number of basophils, increased number of monocytes, increasing the number of neutrophils, reducing the concentration of bicarbonate in the blood plasma; rarely — increased activity of AST, ALT, increasing the concentration of bilirubin in blood plasma, increasing the concentration of urea in blood plasma, increasing the concentration of creatinine in the blood plasma, a change in the content of potassium in the blood plasma, increased the activity of alkaline phosphatase in blood plasma, increasing chlorine content in blood plasma, increasing the concentration of glucose in the blood, increasing the number of platelets, increased hematocrit, increasing the concentration of bicarbonate in the blood plasma, a change in the content of sodium in the blood plasma.

Interaction

Antacid medicationsAntacids do not affect the bioavailability of azithromycin, but reduce its maximum concentration in the blood by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating. CetirizineConcomitant use of azithromycin with cetirizine(20 mg) for 5 days in healthy volunteers did not lead to a pharmacokinetic interaction and a significant change in the QT interval. Didanosine (dideoxyinosine)Concomitant use of azithromycin (1200 mg / day) and didanosine (400 mg / day) In 6 HIV-infected patients, there was no change in the pharmacokinetic indications of didanosine compared to the placebo group. Digoxin (P-glycoprotein substrates)Concomitant use of macrolide antibiotics, including azithromycin, with P-glycoprotein substrates, such as digoxin, leads to an increase in the concentration of the P-glycoprotein substrate in the blood serum. Thus, when azithromycin and digoxin are used simultaneously, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum. ZidovudineConcomitant administration of azithromycin (a single dose of 1000 mg and multiple doses of 1200 or 600 mg) has little effect on the pharmacokinetics, including renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear. Azithromycin weakly interacts with cytochrome P450 isoenzymes. Azithromycin was not found to be involved in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes. Ergot alkaloidsGiven the theoretical possibility of ergotism, concomitant use of azithromycin with ergot alkaloid derivatives is not recommended. Pharmacokinetic studies have been conducted on the concomitant use of azithromycin and drugs that are metabolized with the participation of cytochrome P450 isoenzymes.

AtorvastatinConcomitant administration of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in plasma concentrations of atorvastatin (based on the analysis of HMG-CoA reductase inhibition). However, in the post-marketing period, there have been isolated reports of rhabdomyolysis in patients receiving concomitant azithromycin and statins. CarbamazepinePharmacokinetic studies in healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin. CimetidinePharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin did not reveal changes in the pharmacokinetics of azithromycin, provided that cimetidine was used 2 hours before azithromycin. Indirect anticoagulants (coumarin derivatives)In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single dose of 15 mg of warfarin taken in healthy volunteers. Potentiation of the anticoagulant effect has been reported after concomitant administration of azithromycin and indirect anticoagulants (coumarin derivatives). Although no causal relationship has been established, the need for frequent monitoring of PV should be considered when using azithromycin in patients receiving oral indirect anticoagulants (coumarin derivatives). CyclosporineIn a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) and then cyclosporine (10 mg/kg/day once) orally for 3 days, a significant increase in plasma Cmax and AUC0-5 of cyclosporine was detected. Caution should be exercised when using these drugs simultaneously. If the concomitant use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly. EfavirenzConcomitant administration of azithromycin (600 mg / day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction. FluconazoleConcomitant administration of azithromycin (1200 mg once) did not alter the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1 / 2 of azithromycin did not change with concomitant use of fluconazole, but a decrease in the Cmax of azithromycin (by 18%) was observed, which was not clinically significant. IndinavirConcomitant administration of azithromycin (1200 mg once) did not have a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days). MethylprednisoloneAzithromycin does not significantly affect the pharmacokinetics of methylprednisolone. NelfinavirSimultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the Css of azithromycin in the blood serum. No clinically significant side effects were observed, and no dose adjustment of azithromycin is required when co-administered with nelfinavir. RifabutinSimultaneous use of azithromycin and rifabutin does not affect the concentration of each of the drugs in the blood serum. Neutropenia has sometimes been observed with concomitant use of azithromycin and rifabutin. Although neutropenia has been associated with rifabutin use, a causal relationship between the use of azithromycin and rifabutin combination and neutropenia has not been established. SildenafilWhen used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg / day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite. TerfenadinePharmacokinetic studies have not provided evidence for an interaction between azithromycin and terfenadine. Isolated cases were reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction took place. Concomitant use of terfenadine and macrolides has been shown to cause arrhythmia and prolongation of the QT interval. TheophyllineThere was no interaction between azithromycin and theophylline. Triazolam / midazolamNo significant changes in pharmacokinetic parameters were detected when azithromycin was co-administered with triazolam or midazolam at therapeutic doses. Trimethoprim / sulfamethoxazoleCo-administration of trimethoprim / sulfamethoxazole with azithromycin did not significantly affect Cmax, total exposure, or renal excretion of trimethoprim or sulfamethoxazole. Serum concentrations of azithromycin were consistent with those found in other studies.

How to take it, course of administration and dosage

Azithromycin Ecomed® is taken orally, without chewing,1 time a day. The drug is taken at least 1 hour before or 2 hours after a meal. Adults (including the elderly) and children over 12 years of age with a body weight over 45 kg. For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 0.5 g per day for 3 days (the course dose is 1.5 g). For acne vulgaris of moderate severity: 0.5 g per day for 3 days, then 0.5 g once a week for 9 weeks. The first weekly tablet should be taken 7 days after taking the first daily tablet (the 8th day from the start of treatment), the next 8 weekly tablets – at intervals of 7 days. The course dose is 6.0 g. With erythema migrans: 1 time a day for 5 days, the 1st day 1.0 g, then from the 2nd to the 5th day 0.5 g. The course dose is 3.0 g. For urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): 1.0 g once. When used in patients with mild renal impairment: no dose adjustment is required. When used in patients with mild to moderate hepatic impairment, in elderly patients: no dose adjustment is required. Elderly patients: no dose adjustment is required. Caution should be exercised in elderly patients with persistent proarrhythmogenic factors due to the high risk of arrhythmias, including arrhythmias and pirouette type.

Overdose

Symptoms: temporary hearing loss, nausea, vomiting, diarrhea. Treatment: symptomatic.

Description

Capsule-shaped biconvex tablets covered with a yellow film coating. The cross-section shows two layers, the inner layer is white or almost white in color.

Special instructions

If one dose is missed – the missed dose should be taken as early as possible, and subsequent doses should be taken at intervals of 24 hours.

The drug should be taken at least one hour before or two hours after taking antacid medications. The drug should be used with caution in patients with mild to moderate hepatic impairment due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency. In the presence of symptoms of impaired liver function, such as rapidly increasing asthenia, jaundice, darkening of the urine, tendency to bleeding, hepatic encephalopathy, drug therapy should be discontinued and a study of the functional state of the liver should be conducted. In patients with mild to moderate renal impairment (creatinine clearance greater than 40 ml/min), azithromycin therapy should be carried out with caution under the control of renal function.

As with other antibacterial agents, patients with azithromycin should be regularly examined for the presence of non-susceptible microorganisms and signs of superinfections, including fungal infections. The drug should not be used for longer courses than indicated in the instructions, because the pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.

There are no data on possible interactions between azithromycin and ergotamine and dihydroergotamine derivatives, but due to the development of ergotism when macrolides are co-administered with ergotamine and dihydroergotamine derivatives, this combination is not recommended. With prolonged use of azithromycin, pseudomembranous colitis caused by Clostridium difficile may develop, both in the form of mild diarrhea and severe colitis. If antibiotic-associated diarrhea develops while taking the drug, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. When treated with macrolides, including azithromycin, prolongation of cardiac repolarization and QT interval was observed, which increases the risk of developing cardiac arrhythmias, including pirouette-type arrhythmias.

Caution should be exercised when using the drug in patients with proarrhythmogenic factors (especially in elderly patients). : patients with congenital or acquired prolongation of the QT interval, in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with impaired water-electrolyte balance, especially in the presence of in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia, or severe heart failure. The use of azithromycin can provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

Influence on the ability to drive vehicles and work with mechanisms. With the development of undesirable effects from the nervous system and visual organs, care should be taken when performing actions that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets,250 mg and 500 mg. 6 tablets with a dosage of 250 mg,3 tablets with a dosage of 500 mg in a contour cell package made of polyvinyl chloride/polyvinylidene chloride film and aluminum foil printed varnished.1 contour cell package together with the instructions for use is placed in a pack of cardboard.

Storage conditions

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years. Do not use after the expiration date.

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, Children over 12 years of age, Pregnant women as prescribed by a doctor, Children as prescribed by a doctor

Indications

Bronchitis, Respiratory Tract Infections, Pharyngitis, Infectious Diseases, Tonsillitis, Pneumonia, Skin Infections, Otitis Media, Sore Throat, Urethritis, Sinusitis

Weight

Weight: 15 gr.