Azithromycin tabs n / 500mg film about 3 pieces bfz

Description

Composition
Active substance:
1 tablet contains: Azithromycin dihydrate (equivalent to the anhydrous azithromycin) – 524 mg (500 mg).
Excipients:
Starch pregelatinized 63 mg, giproloza 63 mg, 36 mg copovidone, crospovidone 31.5 mg Calcium hydrogen phosphate anhydrous 142 mg Talc 22.5 mg Sodium lauryl sulfate 7.2 mg, 10.8 mg Magnesium stearate Coating: Hypromellose 13.6 mg macrogol 6000 2.7 talc 15 mg titanium dioxide 3.6 mg, 0.1 mg of dimethicone.
Description:
Oval biconvex tablets, film-coated, white, with a transverse notch on one side of dividing the tablet into two equal halves. The cross-sectional view seen white tablet core and a thin white film coating.
Product form:
Tablets, film-coated 500 mg.
3 tablets in blisters of PVC film and aluminum foil printed patent. 1 contour cell package 3 tablets together with instructions for medical application is placed in a pile of cardboard.
Contraindications
– Increased sensitivity to azithromycin, erythromycin, other macrolides, ketolides, or other components of the preparation. – hepatic impairment, severe (more than 9 points on a scale Child-Pugh). – Children under 12 years of age with a body weight less than 45 kg. – The period of breastfeeding. – Simultaneous administration with ergotamine and dihydroergotamine.
Carefully.
myasthenia gravis; liver dysfunction mild and moderate severity (less than 9 points on the scale Chayld- Pyo); Terminal renal failure with GFR (glomerular filtration rate) of less than 10 ml / min; at arrhythmias 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 fluid and electrolyte balance, particularly in the case of hypokalemia and severe heart failure yu; simultaneous application ditoksina, warfarin, cyclosporine; in elderly patients; neurological or mental illness; during pregnancy.
Dosage
500 mg
Indications
Infectious and inflammatory diseases caused by microorganisms susceptible to the drug, including: upper respiratory tract infections and ENT (sinusitis, tonsillitis, pharyngitis, otitis media); lower respiratory tract infections (pneumonia, including those caused by atypical pathogens; bronchitis, including acute, exacerbation of chronic); urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis); skin and soft tissue infections (Lyme disease (initial stage – erythema migrans), erysipelas, impetigo, secondary pyoderma, acne vulgaris (acne) moderate severity).
Interaction with other drugs
Antacids (aluminum and magnesium-containing) does not affect the bioavailability of azithromycin, but decreased its maximum concentration in the blood at 30%, and the drug should be taken at least one hour before or two hours after administration of these drugs. When combined with anticoagulants indirect coumarin (warfarin) and azithromycin (in normal doses) patients requires careful monitoring of the prothrombin time. When simultaneous administration of fluconazole reduces the maximum azithromycin blood concentration of 18%, which has no clinical significance.
While the use of cyclosporin required dosage adjustment and monitoring of cyclosporin blood levels.
When co-administered azithromycin and digoxin is necessary to control the concentration of digoxin in the blood, as many macrolides increase the absorption of digoxin in the intestine, thereby increasing its maximum concentration in the blood.
When simultaneous administration of macrolides with ergotamine and dihydroergotamine can manifest their toxic action (vasospasm, dysesthesia) – the simultaneous use contraindicated.
Care must be taken with co-administration of terfenadine and azithromycin, since it has been found that simultaneous reception of terfenadine, and cisapride or macrolide antibiotics class causes arrhythmia and QT interval elongation. On this basis, we can not exclude the above-mentioned complications during coadministration of terfenadine and azithromycin.
At the same time taking azithromycin and rifabutin in rare cases may develop neutropenia, developing a mechanism which, as well as the existence of a causal connection with the admission of the drug have not been established.
When co-administered azithromycin and zidovudine, azithromycin had little effect on the pharmacokinetics, including the allocation of kidneys of zidovudine or its glucuronide metabolite. Increasing the concentration of the active metabolite – phosphorylated AZT in peripheral blood mononuclear cells. The clinical significance of this fact has not been determined.
The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase of the equilibrium concentration of azithromycin in plasma. No clinically significant side effects were observed and correction dose of azithromycin when applied simultaneously with nelfinavir not required.
Azithromycin has no effect on the concentration of carbamazepine, cimetidine (subject to application of cimetidine after 2 hours before azithromycin), didanosine, efavirenz, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin and blood methylprednisolone while applying .
some were reported cases of rhabdomyolysis in patients receiving both azithromycin and statins.
Azithromycin weakly interacts with the cytochrome P450 isozymes. Not found that azithromycin is involved in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inducer and an inhibitor of cytochrome P450 isoenzymes.
Overdose
When high doses of the drug may be increased side effects observed: temporary hearing loss, nausea, vomiting, diarrhea. In this case shows gastric lavage, symptomatic therapy.
pharmachologic effect
Pharmacological group:
Antibiotic-azalide.
Pharmacodynamics:
Broad-spectrum antibiotic. It is a representative subgroup of macrolide antibiotics – azalides. Communicating with the 50S ribosomal subunit, inhibits peptidtranslokazu step of broadcasting, inhibits protein synthesis, inhibits the growth and reproduction of bacteria, acts bacteriostatically, at higher concentrations it has a bactericidal effect. It acts on the extra- and intracellular pathogens.
It is active against gram-positive aerobic microorganisms: Streptococcus spp. (Groups A, B, C, G), Streptococcus pneumoniae (penitsillinchuvstvitelny), Streptococcus pyogenes, Staphylococcus aureus (metitsillinchuvstvitelny); Gram-negative aerobic organisms: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Legionella pneumophila, Neisseria gonorrhoeae, Pasteurella multocida; Some anaerobes: Prevotella spp, Clostridium perfringens, Fusobacterium spp, Porphyriomonas spp .;.. and Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.
Microorganisms capable of developing resistance to azithromycin: Gram-positive aerobes (Streptococcus pneumoniae (penitsillinustoychivy).
Initially resistant microorganisms: Gram-positive aerobes (. Enterococcus faecalis, Staphylococcus spp (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolide), Gram-positive bacteria resistant to erythromycin); anaerobic bacteria (Bacteroides fragilis).
Pharmacokinetics:
Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic medium and lipophilicity. After oral administration of 500 mg of azithromycin maximum concentration in plasma is reached after 2 – 3 hours, and 0.4 mg / l. Bioavailability is 37%.
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (in particular in the prostate gland), in skin and soft tissue. The high concentration in tissues (10-50 times higher than in blood plasma) and a long half-life of azithromycin due to low binding to plasma proteins as well as its ability to penetrate into eukaryotic cells and concentrated in a low pH environment surrounding the lysosomes. This, in turn, defines a large apparent volume of distribution (31.1 l / kg) and high plasma clearance. The ability of azithromycin accumulate mainly in lysosomes, particularly important for the elimination of intracellular pathogens. It is shown that phagocytes deliver azithromycin localization of infection in places where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissue (on average 24-34%) and correlated with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin did not significantly affect their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.
In the liver demetiliruetsa formed metabolites are inactive. Excretion of azithromycin from plasma takes place in 2 stages: half-life of 14-20 hours in the range of from 8 to 24 hours after drug administration and 41 hours – in the range from 24 to 72 hours, which allows the use of drug 1 time / day.
Azithromycin is derived mainly as unchanged – 50% of the intestines, the kidneys of 6%.
Pregnancy and breast-feeding
Use of the drug during pregnancy is possible only when the intended benefits for a mother than the potential risk to the fetus.
If necessary, the appointment during lactation should stop breastfeeding.
Conditions of supply of pharmacies
On prescription.
side effects
Most celebrated of adverse reactions are reversible after treatment or discontinuation of the drug. Classification incidence of side effects (WHO): very often (with a frequency of more than 1/10), often (with a frequency not less than 1/100 but less than 1/10) infrequently (at a frequency of at least 1 / 1000th and less than 1 / 100), rare (with a frequency of not less than 1/10000 and less than 1/1000), very rare (with a frequency of less than 1/10 000), including isolated reports. On the part of the circulatory and lymphatic systems: common – lymphocytopenia, eosinophilia; rarely – leukopenia, neutropenia; rarely – thrombocytopenia, hemolytic anemia.
Central nervous system: often – dizziness, headache, paresthesia, impaired perception of taste, anorexia; rare – anxiety, nervousness, gipostezii, insomnia, somnolence; seldom – agitation, delirium, hallucinations; very rarely – fainting, seizures, psychomotor hyperactivity, aggression, anosmia, loss of taste, parosmiya, exacerbation of myasthenia gravis, a distortion of the sense of smell.
From the sensory organs: rarely – hearing disorders, vertigo, blurred vision; unknown frequency – hearing impairment, including deafness and / or tinnitus.
The respiratory system and ENT organs: rarely – shortness of breath, nasal bleeding.
Cardio-vascular system: rarely – palpitations, “tides” of blood to the face; very rarely – lowering blood pressure, arrhythmia, ventricular tachycardia, increased QT interval, arrhythmia type “pirouette”.
Infectious diseases: infrequently – rhinitis, respiratory disease, pharyngitis, pneumonia, candidiasis, including oral and genital mucosa gastroenteritis.
From the digestive system: very often – nausea, diarrhea, abdominal pain, flatulence (bloating), often – vomiting; infrequently – regurgitation, dysphagia, gastritis, constipation, dryness of the oral mucosa, ulceration of the oral mucosa, increased secretion of the salivary glands; very rarely – to change the language of color, pseudomembranous colitis, pancreatitis.
Of the liver and biliary tract: rarely – hepatitis, hyperbilirubinemia, increased activity of “liver” transaminases; very rarely – cholestatic jaundice, hepatic failure (in rare cases with fatal outcome, mainly on the background of abnormal liver function), fulminant hepatitis, liver necrosis.
Allergic reactions: often – itching, rash; infrequently – Stevens-Johnson syndrome, photosensitivity, urticaria; rarely – anaphylactic reactions (including angioneurotic edema), in rare instances fatal, toxic epidermal necrolysis, erythema multiforme.
Skin and subcutaneous tissue disorders: dry skin, dermatitis, sweating.
On the part of the musculoskeletal system: often – arthralgia; not often – Osteoarthritis, myalgia, neck pain, back pain.
From the urogenital system: infrequently – increasing residual urea nitrogen and creatinine concentration in blood plasma, dysuria, pain in the kidneys, metrorrhagia, impaired testicular function; very rarely – interstitial nephritis, acute renal failure.
Other: often – weakness; infrequently – chest pain, peripheral edema, asthenia (unwell, fatigue); rare – swelling of the face, fever.
Laboratory data: often – increase the number of basophils, monocytes, neutrophils, decreased bicarbonate concentration in the blood plasma; infrequently – increase of alkaline phosphatase activity, increased chlorine content, increasing the glucose concentration, increasing bicarbonate concentration in the blood plasma, increasing the number of platelets, increased hematocrit, changing sodium concentration in the blood plasma, a change in the potassium concentration in the blood plasma.
On the occurrence of any side effect should be reported to your doctor.
special instructions
When you miss a single dose of the drug – the missed dose should be taken as soon as possible, and follow – at intervals of 24 hours.
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 impaired liver function and mild to moderate severity due to the possibility of development of fulminant hepatitis and severe liver disease in these patients. If symptoms of liver disease (rapidly growing fatigue, jaundice, dark urine color, a tendency to bleeding, hepatic encephalopathy) azithromycin therapy should be discontinued and a study of the functional state of the liver.
In renal failure of mild to moderate severity of azithromycin should be under the control of renal function.
Contraindicated with concomitant use of azithromycin derivatives ergotamine and dihydroergotamine because of the possible development of ergotism.
In applying the drug, both in patients receiving and 2-3 weeks after cessation of treatment may develop diarrhea caused by Clostridium difficile (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.
Drugs inhibiting peristalsis are contraindicated intestine. Since it is possible prolongation of the interval QT in patients treated with macrolides, including azithromycin, when azithromycin Caution should be exercised in patients with known risk factors for prolongation QT interval: heart disease (heart failure, myocardial infarction, bradycardia), advanced age, impaired electrolyte balance (hypokalaemia , hypomagnesaemia), congenital long QT interval syndrome, simultaneous reception of drugs capable of lengthening QT interval (including antiarrhythmics A and class III, tricyclic and tetracyclic antidepressants, neuroleptics, fluoroquinolones).
Azithromycin can trigger the development of myasthenic syndrome or aggravate myasthenia gravis.
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 should not be taken longer course than indicated in the instructions, as the pharmacokinetic properties of azithromycin can recommend short and simple dosing regimen.
In the event of adverse reactions from the central nervous system, patients are advised to refrain from road management and other activities potentially hazardous activities that require high concentration of attention, psychomotor speed and motor responses.
Storage conditions
Store at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Inside, 1 times a day, at least for 1 hour or over 2 hours after a meal. Adults (including the elderly) and children over 12 years weighing more than 45 kg.
In infections of the upper, lower respiratory tract, LOR organs, skin and soft tissue – 0.5 g / day per 1 reception for 3 days (a course dose – 1.5 g).
When erythema migrans (Lyme disease) to treat stage I – 1 times a day for 5 days: Day 1 – 1.0 g, then from the 2nd to 5th day – 0.5 g daily (course dose – 3 g).
Acne vulgaris – 6 g of course dose 0.5 g / day per 1 reception for 3 days, followed by 0.5 g / day 1 time per week for 9 weeks. The first pill to be taken weekly after 7 days after the first pill daily (day 8 from the start of treatment), the next 8 weekly tabs – with an interval of 7 days.
When urinary tract infections caused by Chlamydia trachomatis (uncomplicated urethritis, or cervicitis) – single 1 g
If the kidney functions in patients with GFR 10-80 ml / min the dose correction is not required.
That patients with impaired hepatic function: for patients with mild and moderate impaired liver function severity degree correction dose is not required.
When administered to patients of advanced age (over 65 years) No dose adjustment is required. This should take into account that in older patients may be people with the presence of arrhythmogenic factors (see. Section ”
Carefully “).
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist