Azithromycin capsules. 250mg 6 vertex units

Description

Composition
Active substance:
1 capsule contains: azithromycin dihydrate – 262.02 mg (in terms of azithromycin – 250.00 mg) ;.
Excipients:
Lactose monohydrate – 61.98 mg; microcrystalline cellulose – 40.60 mg; magnesium stearate – 3.70 mg; povidone K-17 (polyvinylpyrrolidone, low molecular weight) – 1.00 mg; Sodium lauryl sulfate – 0.70 mg; hard gelatin capsules: titanium dioxide – 2.0% gelatin – up to 100%.
Description:
Hard gelatin capsules № 0 white. Contents of capsules – powder white or white with a light yellow color. Presence of conglomerates, which when pressed with a glass rod are readily converted to free-flowing powder.
Product form:
Capsules 250 mg. 6 or 10 capsules in blisters of PVC film and aluminum foil. 6 capsules a bank of high-density polyethylene. 1 blisters of 6 capsules 1 blisters 10 capsules or one bank, along with instructions for medical use in a stack of cardboard.
Contraindications
Hypersensitivity to azithromycin, erythromycin, other macrolides, ketolides, or other components of the formulation; – violation of severe liver function (class C by Child-Pugh classification); – violation severe renal impairment (creatinine clearance (CC) of less than 40 ml / min); – Children under 12 years old with a body weight less than 45 kg (500 mg tablet); – children up to 3 years (for 125 mg tablets); – the period of breast-feeding; – Simultaneous reception with ergotamine and dihydroergotamine; – lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Carefully:
myasthenia gravis; human liver mild or moderate (grades A and B according to the classification Child-Pugh); renal dysfunction and mild to moderate severity (CC 40 ml / min); elderly patients; patients with presence proaritmogennoe factors (especially in elderly patients) with congenital or acquired lengthening the interval QT, in patients receiving antiarrhythmic drug therapy class IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin, levofloxacin), impaired with fluid and electrolyte balance, particularly in the case of hypokalemia or hypomagnesemia with clinically significant radikardiey, cardiac arrhythmia or heart failure, severe; concurrent use of digoxin, warfarin, cyclosporine.
Dosage
250 mg
Indications
Infectious and inflammatory diseases caused by microorganisms susceptible to azithromycin: -infektsii upper respiratory and ENT (sinusitis, tonsillitis, pharyngitis, otitis media); – lower respiratory tract infections (acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including those caused by atypical pathogens); – skin and soft tissue infections (erysipelas, impetigo, secondarily infected dermatoses, acne vulgaris moderate); – urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis); – the initial stage of Lyme disease (borreliosis) – erythema migrans (erythema migrans).
Interaction with other drugs
antacids
Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration of 30%, and the drug should be taken at least one hour before or two hours after taking these drugs or food intake.
cetirizine
Simultaneous application for 5 days in healthy volunteers azithromycin with cetirizine (20 mg) did not result in a substantial pharmacokinetic interaction and change interval QT.
DdI (dideoxyinosine)
The simultaneous use of azithromycin (1200 mg / day) and didanosine (400 mg / day) in 6 HIV-infected patients revealed no changes in readings pharmacokinetic ddI compared to the placebo group.
Digoxin (P-glycoprotein substrates)
The simultaneous use of macrolide antibiotics, including azithromycin with substrates of P-glycoprotein, such as digoxin, increases the concentration of substrate of P-glycoprotein in the blood plasma. Thus, while the use of azithromycin and digoxin is necessary to consider the possibility of increasing the concentration of digoxin in plasma.
zidovudine
The simultaneous use of azithromycin (1000 mg single dose and multiple dose of 600 mg or 1200) has little effect on the pharmacokinetics, including the renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated AZT, clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this is unclear. Pharmacokinetic studies were conducted simultaneously azithromycin and preparations which metabolism occurs with the participation of cytochrome P450 isoenzymes. Azithromycin weakly interacts with the cytochrome P450 isozymes system. Not found that azithromycin is involved in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor and inducer of cytochrome P450 isoenzymes.
atorvastatin
Simultaneous use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes atorvastatin concentrations in plasma (based inhibition assay MMC-CoA reductase). However, sporadic reports of cases of rhabdomyolysis in patients receiving both azithromycin and statins were obtained.
carbamazepine
In pharmacokinetic studies in healthy volunteers revealed no significant effect on the concentration of carbamazepine and its active metabolite in the blood plasma of patients treated with azithromycin at the same time.
cimetidine
The pharmacokinetic studies influence of single dose azithromycin pharmacokinetics cimetidine revealed no changes in the pharmacokinetics of azithromycin, cimetidine, subject to application of 2 hours prior to the azithromycin.
Indirect anticoagulants (coumarin derivatives)
In pharmacokinetic studies of azithromycin had no effect on the anticoagulant effect of a single dose of 15 mg of warfarin in healthy volunteers received.
It has been reported to potentiate the anticoagulant effect after simultaneous application of azithromycin and indirect anticoagulants (coumarin derivatives). Despite the fact that a causal link has not been established, it is necessary to take into account the need for frequent monitoring of prothrombin time when azithromycin in patients who receive oral anticoagulants of indirect action (coumarin derivatives).
cyclosporine
In a pharmacokinetic study in healthy volunteers for three days ingested azithromycin (500 mg / day one), and then the cyclosporin (10 mg / kg / day once) revealed a significant increase in the maximum plasma concentration (Cmax) and area under the curve “concentration-time» (AUC0-5) cyclosporin. Caution must be exercised while the use of these drugs. If necessary, the simultaneous use of these drugs, it is necessary to control the concentration of cyclosporine in the blood plasma and adjust the dose.
efavirenz
The simultaneous use of azithromycin (600 mg / day one) and efavirenz (400 mg / day) daily for 7 days did not cause any clinically significant pharmacokinetic interactions.
fluconazole
The simultaneous use of azithromycin (1200 mg single dose) did not alter the pharmacokinetics of fluconazole (800 mg dose). Total exposure and half-life of azithromycin is not changed while the application of fluconazole, however, the observed reduction in Cmax of azithromycin (18%), which had no clinical significance.
indinavir
The simultaneous use of azithromycin (1200 mg single dose) caused no statistically significant effect on the pharmacokinetics of indinavir (800 mg three times a day for 5 days).
methylprednisolone
Azithromycin has no significant effect on the pharmacokinetics of methylprednisolone.
nelfinavir
The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg tid) causes an increase of the equilibrium concentration of azithromycin in plasma. No clinically significant adverse effects were observed. Correction dose of azithromycin when applied simultaneously with nelfinavir not required.
rifabutin
The simultaneous use of azithromycin and rifabutin did not affect the concentration of each drug in the blood plasma. With simultaneous use of azithromycin and rifabutin sometimes observed neutropenia. Despite the fact that neutropenia associated with the use of rifabutin, a causal relationship between the use of a combination of azithromycin and rifabutin and neutropenia has not been established.
sildenafil
When applied in healthy volunteers received no evidence for an effect of azithromycin (500 mg / day, daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.
terfenadine
The pharmacokinetic studies have not shown evidence of interaction between azithromycin and terfenadine. It reported a few cases, when the possibility of such an interaction could not be excluded completely, but there was no specific evidence that such an interaction has taken place. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and lengthening the interval QT.
theophylline
Revealed no interaction between azithromycin and theophylline.
Triazolam / midazolam
Significant changes pharmacokinetic parameters, while the application of azithromycin with midazolam or triazolam in therapeutic doses have been identified.
Trimethoprim / sulfamethoxazole
The simultaneous use of trimethoprim / sulfamethoxazole with azithromycin showed no significant effect on the Cmax, the overall exposure or excretion by the kidneys trimethoprim or sulfamethoxazole. The concentration of azithromycin in plasma corresponded detectable in other studies.
ergot alkaloids
Given the theoretical possibility of ergotism, the simultaneous use of azithromycin derivatives of ergot alkaloids is not recommended.
Overdose
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: symptomatic.
pharmachologic effect
Pharmacological group:
Antibiotic-azalide.
Pharmacodynamics:
Azithromycin -bakteriostatichesky broad-spectrum antibiotic from macrolide-azalides. It has a broad spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with suppression of the synthesis of microbial cell protein.
Communicating with the 50S-ribosomal subunit, inhibits peptidtranslokazu step of broadcasting and inhibits protein synthesis by slowing 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 organisms. Microorganisms can initially be resistant to the antibiotic, or may acquire resistance to it.
In most cases are sensitive to azithromycin: – gram-positive aerobic bacteria: Staphylococcus aureus (methicillin sensitive), Streptococcus pneumoniae (penicillin sensitive),
Streptococcus pyogenes, Streptococcus group A, B, C, G; – aerobic gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida,
Neisseria gonorrhoeae; – anaerobic bacteria: Clostridium perfringens, Fusobacterium spp,.
Prevotella spp., Porphyromonas spp .; – other micro-organisms: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.
Microorganisms capable of developing resistance to azithromycin: -Streptococcus pneumoniae (penicillin resistant).
Microorganisms, initially resistant to azithromycin: -aerobnye Gram-positive microorganisms: Enterococcus faecalis,
Staphylococcus spp. (Methicillin-resistant staphylococci very high frequency have acquired resistance to macrolides); – Gram-positive bacteria resistant to erythromycin; – anaerobic bacteria: Bacteroides fragilis.
Pharmacokinetics:
After oral administration, azithromycin is well absorbed and rapidly distributed in the body. After a single dose of 500 mg bioavailability -37% (the effect of “first pass”), the maximum blood concentration (0.4 mg / L) is reached after 2-3 hours, the apparent volume of distribution – 31,1 l / kg, protein binding blood plasma is inversely proportional to the concentration in the blood and is 7-50%. Penetrates through the cell membrane (effective against infections caused by intracellular pathogens).
Phagocytes transported to the site of infection, where the presence of released bacteria. Easily it passes through the blood-tissue barriers and into the tissue. Concentration in the tissues and cells in a 10-50 times higher than in blood plasma, and the source of infection – by 24-34% higher than in healthy tissues. We azithromycin very long half-life -30-50 hours. The half-life of the tissues is much greater. Therapeutic concentrations of azithromycin remains until 5-7 days after the last dose. Azithromycin is derived mainly as unchanged – 50% of the intestines, the kidneys of 6%. The liver is demethylated, losing activity.
Pregnancy and breast-feeding
Pregnancy: Pregnancy drug Azithromycin is used only if the expected benefit to the mother outweighs the potential risk to the fetus.
Lactation: the need for the drug during breastfeeding recommended suspend breastfeeding.
Conditions of supply of pharmacies
Prescription.
side effects
Classification incidence of side effects according to the recommendations
World Health Organization (WHO): very common> 1/10; often> 1/100, 1/1000, 1/10000,
Infectious diseases: infrequently – candidiasis, including oral and genital mucosa, pneumonia, pharyngitis, gastroenteritis, respiratory infections, rhinitis; the frequency is unknown – pseudomembranous colitis.
On the part of metabolism and nutrition: rarely – anorexia.
Allergic reactions: infrequently – angioneurotic edema, hypersensitivity reactions; frequency neizvestna- anaphylactic reaction.
From the blood and lymphatic system: nechasto- leukopenia, neutropenia, eosinophilia; very rare-thrombocytopenia, hemolytic anemia.
The respiratory system: rarely – shortness of breath, nasal bleeding.
From the nervous system: often – headache; nechasto- dizziness, paresthesia, impaired taste, somnolence, insomnia, nervousness; seldom – agitation; the frequency is unknown – hypoesthesia, anxiety, aggression, fainting, seizures, psychomotor hyperactivity, loss of smell, sense of smell distortion, loss of taste, myasthenia gravis, delirium, hallucinations.
From a sight organ: nechasto- blurred vision.
On the part of the ear and labyrinth disorders: rarely – a disorder of hearing, vertigo; the frequency is unknown – hearing impairment, including deafness and / or tinnitus.
Cardio-vascular system: rarely – palpitations, “tides” of blood to the facial skin; frequency is unknown – blood pressure, an increase in QT interval on the electrocardiogram, arrhythmia type “pirouette”, ventricular tachycardia.
Gastro-intestinal tract: often – diarrhea; often – nausea, vomiting, abdominal pain; -meteorizm infrequently, dyspepsia, constipation, gastritis, dysphagia, abdominal distension, dryness of the oral mucosa, increased secretion of the salivary glands, belching, ulcers of the oral mucosa; very rarely – to change the language of color, pancreatitis.
Of the liver and biliary tract: rarely – hepatitis; rarely -Violation liver function, cholestatic jaundice; the frequency is unknown – hepatic insufficiency (in rare cases with fatal consequences mainly on the background of the liver, severe), liver necrosis, fulminant hepatitis.
For the skin: rare – skin rash, itching, hives, dermatitis, dry skin, increased sweating; rarely – photosensitivity reactions; frequency is unknown – Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.
On the part of the musculoskeletal system and connective tissue disorders: uncommon – osteoarthritis, myalgia, back pain, neck pain; the frequency is unknown – arthralgia.
With the genitourinary system: rarely – dysuria, pain in the kidneys, metrorrhagia, impaired testicular function; the frequency is unknown – interstitial nephritis, acute renal failure.
Laboratory parameters: often – a reduction in the number of lymphocytes, increase in the number of eosinophils, basophils increase in the number, increase in the number of monocytes, increased neutrophil count, decreased bicarbonate concentration in the blood plasma; infrequently – increase of aspartate aminotransferase activity, alanine, increasing the concentration of bilirubin in plasma creatinine concentration in blood plasma, the potassium content variation in the blood plasma, increased alkaline phosphatase activity in plasma, increasing chlorine content in the plasma, increasing the concentration of blood glucose, increasing the number of platelets, increasing hematocrit, increasing the bicarbonate concentration in the blood plasma, a change in the sodium content in the blood plasma, increasing conc tion of urea in the blood plasma.
Other: rarely – fatigue, malaise, fatigue, swelling of the face, chest pain, fever, peripheral edema.
special instructions
When you miss a single dose of azithromycin drug missed dose should be taken as soon as possible, and follow – at intervals of 24 hours. Azithromycin formulation should be taken at least one hour before or two hours after ingestion of antacids. The drug Azithromycin should not be used for the treatment of pneumonia in patients for whom it is impossible to conduct oral therapy because of the severity of the disease and / or have the following risk factors: cystic fibrosis, bacteremia or suspicion of her condition that can change the body’s response to the disease (immunodeficiency, functional asplenia et al.), patients need to be hospitalized, elderly or debilitated patients. The drug Azithromycin should be used with caution in patients with impaired liver function and mild to moderate severity due to the possibility of development of fulminant hepatitis and severe hepatic insufficiency. In the presence of liver disease symptoms, such as rapidly increasing fatigue, jaundice, dark urine, bleeding tendency, hepatic encephalopathy, therapy with azithromycin should be discontinued and a study of the functional state of the liver. When kidney function disorders of mild and moderate severity (CC 40 ml / min) therapy with azithromycin should be carried out with care under the control of renal function. In end-stage renal failure (creatinine clearance less than 10 mL / min), there is an increase in the concentration of azithromycin in blood plasma by 33%. Perhaps the development of microbial resistance non-compliance with the recommended duration of therapy courses. As with other antibacterial drugs in the treatment of drug Azithromycin should regularly examine patients for the presence of non-susceptible organisms and signs of superinfection, including fungi. The drug Azithromycin should not be used longer course than indicated in the instructions, as the pharmacokinetic properties of azithromycin can recommend short and simple dosing regimen. No data on the possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but due to the development of ergotism, while the use of macrolides derivatives with ergotamine and dihydroergotamine, this combination is contraindicated. It must be remembered that for prophylaxis of pharyngitis / tonsillitis caused by Streptococcus pyogenes, as well as for the prevention of acute rheumatic fever, the drug of choice is usually penicillin.
Chronic administration of the drug Azithromycin may develop pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea to severe colitis. With the development of antibiotic-associated diarrhea in patients receiving azithromycin drug and 2 months after completion of therapy should be excluded clostridial pseudomembranous colitis. In mild cases enough discontinuation of treatment and use of ion exchange resins (colestyramine, colestipol), in severe cases shown compensation fluid loss, electrolytes, protein, vancomycin, metronidazole or bacitracin. The use of drugs that inhibit intestinal peristalsis, are contraindicated. When treating with macrolides, including azithromycin, there was a prolongation of cardiac repolarization and the interval QT, increase the risk of cardiac arrhythmias, including arrhythmia type “pirouette”. Caution must be exercised when using the drug azithromycin in patients with presence proaritmogennoe factors (especially in the elderly): with congenital or acquired lengthening the interval QT, in patients receiving antiarrhythmic drug therapy class IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), impaired with water and electrolyte balance, wasps Aubin in the case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia or severe heart failure. The use of azithromycin drug can trigger the development of myasthenic syndrome or aggravate myasthenia gravis.
Effects on ability to drive vehicles and mechanisms:
With the development of adverse effects in the nervous system and organ of vision care should be taken while performing activities that require high concentration and psychomotor speed reactions.
Storage conditions
Store in a dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.
Dosing and Administration
Inside, once a day, at least for 1 hour before or 2 hours after eating.
Adults (including the elderly) and children over 12 years weighing more than 45 kg:
In infections of the upper and lower respiratory tract, upper respiratory tract, skin and soft tissues: 500 mg (2 capsules) once a day for 3 days (a course dose – 1.5 g).
If acne vulgaris moderate: 500 mg (2 capsules) once a day for 3 days, followed by 500 mg (2 capsules) once a week for 9 weeks (course dose 6.0 g). First weekly dose of 500 mg (2 capsules) should be taken 7 days after the first daily dose of 500 mg (2 capsules) (eighth day from the beginning of treatment), the next 8 weekly doses of 500 mg (2 capsules) – with an interval of 7 days .
When Lyme disease (borreliosis initial stage) – erythema migrans (erythema migrans): once a day for 5 days: first day – 1.0 g (4 capsules), then the second to fifth day – 500 mg (2 capsules ) (course dose – 3.0 g).
When urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): uncomplicated urethritis, or cervicitis – once 1.0 g (4 capsules).
In patients with GFR 10-80 ml / min the dose correction is not required.
In human liver mild or moderate dose adjustment is required.
Elderly patients: No dose adjustment is required. Since elderly patients may already have current proaritmogennoe state, caution should be exercised when using the drug
Azithromycin is due to the high risk of cardiac arrhythmias, including arrhythmia type “pirouette”.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist