Zitrolide forte
Zitrolide forte: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Zitrolid forte
ATX code: J01FA10
Active ingredient: azithromycin (azithromycin)
Producer: VALENTA PHARMACEVTIKA, JSC (Russia)
Description and photo updated: 2018-23-11
Prices in pharmacies: from 153 rubles.
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Zitrolide forte is an antimicrobial drug with a broad spectrum of bacteriostatic action for systemic use.
Release form and composition
Dosage form Zitrolide forte - capsules: No. 00, gelatinous solid, with a white body and an orange lid, filled with a powder prone to clumping from white with a yellowish tinge to white (3 pcs. In blisters made of PVC film and foil, in a pack from cardboard 1 or 2 packs).
The composition of 1 capsule contains:
- active substance: azithromycin dihydrate (in terms of azithromycin) - 500 mg;
- auxiliary components: microcrystalline cellulose, magnesium stearate;
- capsule: titanium dioxide (E171), sunset yellow dye (E110), gelatin.
Pharmacological properties
Pharmacodynamics
The active component of Zitrolide forte is azithromycin, an antibiotic with antimicrobial bacteriostatic efficacy, belongs to the macrolide group, azalide. Its mechanism of action is associated with inhibition of protein synthesis of the microbial cell. Binding reversibly to the 50S-subunit of the ribosome, azalide inhibits peptide translocase at the stage of translation and inhibits protein biosynthesis, thereby slowing down the growth of bacteria and their reproduction. Azithromycin, used in high concentrations, is bactericidal.
Zitrolide forte is active against a number of aerobic (both gram-positive and gram-negative), anaerobic, intracellular and other microorganisms.
Microorganisms can show initial resistance to antibiotic action or become resistant during therapy.
Microflora, in most cases sensitive to azithromycin:
- gram-positive [Gram (+)] aerobic bacteria: methicillin-sensitive Staphylococcus aureus, Streptococcus pyogenes, penicillin-sensitive Streptococcus pneumoniae;
- gram-negative [Gram (-)] aerobic bacteria: Haemophilus influenzae, Legionella pneumophila, Haemophilus parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Pasteurella multocida;
- anaerobic bacteria: Clostridium perfringens, Prevotella spp., Fusobacterium spp., Porphyromonas spp.;
- other microorganisms: Chlamydia pneumoniae, Chlamydia trachomatis, Borrelia burgdorferi, Mycoplasma pneumoniae, Chlamydia psittaci, Mycoplasma hominis.
Penicillin-resistant gram-positive aerobes Streptococcus pneumoniae are capable of developing resistance to azithromycin.
Microorganisms initially resistant to Zitrolide forte: gram-positive aerobic bacteria [Enterococcus faecalis, Staphylococcus spp. (staphylococci resistant to methicillin show increased resistance to macrolides)], anaerobic bacteria (Bacteroides fragilis), gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
The main pharmacokinetic characteristics of azithromycin:
- absorption: absorption of azithromycin is high, it is lipophilic and acid-resistant; after a single dose of 500 mg, bioavailability is 37%, the maximum concentration (C max) in the blood serum is 0.4 mg / l, the time to reach C max (T max) is 2.5–2.9 hours;
- distribution to organs and tissues: volume of distribution (V d) - 31.1 l / kg, the concentration in tissues and cells is 10-50 times higher than serum. Azithromycin easily penetrates the histohematogenous barriers, passes well into the urogenital organs (including the prostate gland), respiratory tract, soft tissues, skin, accumulates in an environment with low pH, in lysosomes (which is of great importance for the eradication of pathogens located inside cells). The substance is transported by polymorphonuclear leukocytes, phagocytes and macrophages; penetrates through cell membranes, creating high concentrations in them. In the foci of infection, the level of azithromycin is significantly higher (by 24–34%) than in healthy tissues, and shows a direct relationship with the severity of the inflammatory process, while maintaining therapeutically effective concentrations from 5 to 7 days after the last dose. The connection of a substance with blood plasma proteins is 7–50% and is inversely proportional to its concentration in the blood;
- metabolism: azithromycin undergoes intense demethylation in the liver with the formation of inactive metabolites. The process involves isozymes of cytochrome P 450 CYP3A4, CYP3A5, CYP3A7, in relation to which azithromycin is an inhibitor;
- excretion: plasma clearance of azithromycin - 630 ml / min; its half-life (T 1/2) after taking 500 mg of the substance: in the interval from 8 to 24 hours - 14–20 hours, in the interval 24–72 hours - 41 hours. In unchanged form, up to 50% of the substance is excreted in the bile, about 6% - by the kidneys.
The pharmacokinetic characteristics are significantly affected by the simultaneous administration of the drug with food: the C max decreases by 52%, the area under the concentration-time curve (AUC) decreases by 43%.
In elderly men (from 65 to 85 years), the pharmacokinetic parameters of azithromycin remain unchanged, in elderly women, C max increases by 30-50%.
Indications for use
According to the instructions, Zitrolide forte is recommended for the treatment of infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:
- pneumonia, including atypical and exacerbation of chronic, bronchitis, including acute and exacerbation of chronic, other infections of the lower respiratory tract;
- sinusitis, otitis media, tonsillitis, pharyngitis, other infections of the ENT organs and upper respiratory tract;
- cervicitis, gonorrheal / non-gonorrheal urethritis, other urinary tract infections;
- acne vulgaris of moderate severity, erysipelas, secondarily infected dermatoses, impetigo, other infections of the skin and soft tissues;
- borreliosis (the initial stage of Lyme disease), erythema migrans, infectious diseases transmitted through the bite of the Ixodidae tick.
Contraindications
Absolute:
- severe renal failure with creatinine clearance less than 40 ml / min;
- severe hepatic impairment (on the Child-Pugh scale, class B and higher);
- lactation period;
- children under 12 years old;
- body weight up to 45 kg;
- combined therapy with ergotamine and dihydroergotamine;
- individual hypersensitivity to azithromycin and other macrolides, as well as to any components of the drug.
Relative contraindications for which Zitrolide forte should be used with caution: pregnancy, renal failure with creatinine clearance greater than 40 ml / min, mild and moderate hepatic failure (on the Child-Pugh scale below class B), myasthenia gravis, the presence of arrhythmias and a predisposition to the development of arrhythmias with prolongation of the QT interval (risk of ventricular arrhythmias / prolongation of the QT interval), as well as simultaneous use with terfenadine, warfarin and digoxin.
Instructions for the use of Zitrolide forte: method and dosage
Zitrolide forte capsules are taken orally, 1 time per day, one hour before or two hours after a meal.
The recommended dosage according to indications for adult patients and children over 12 years old with a body weight of 45 kg or more:
- infectious lesions of the ENT organs, upper / lower respiratory tract, skin and soft tissues: 500 mg per day for three days; course dose - 1500 mg;
- acne vulgaris (acne vulgaris): 500 mg per day for three days, then 500 mg per day 1 time per week for nine weeks. The first weekly dose is taken seven days after the first daily dose, on the eighth day from the beginning of the course, the next 8 weekly doses are taken at intervals of seven days;
- acute infections of the genitourinary organs (uncomplicated urethritis / cervicitis): 1000 mg once;
- borreliosis, or Lyme disease (for the treatment of stage I - erythema migrans): 1000 mg on the first day and 500 mg per day from the second to the fifth day; course dose - 3000 mg;
- pneumonia: 500 mg per day for 7-10 days; taking the capsules begins immediately after the end of the intravenous administration of the antibiotic.
Side effects
- digestive system: nausea, vomiting, abdominal pain, diarrhea, flatulence, melena, anorexia, constipation, gastritis, oral mucosa candidiasis, dyspepsia, increased activity of liver enzymes, hyperbilirubinemia, hepatitis, cholestatic jaundice, pseudomembranous colitis, hepatic pancreatitis (in exceptional cases with a fatal outcome, mainly against the background of hepatic dysfunction), fulminant hepatitis, liver necrosis;
- cardiovascular system: chest pain, palpitations, decreased blood pressure (BP), increased QT interval, ventricular tachycardia (arrhythmia of the "pirouette" type);
- nervous system: headache, dizziness, drowsiness, vertigo, paresthesia, dysgeusia / ageusia, hypesthesia, convulsions, aggression, psychomotor hyperactivity, fainting, myasthenia gravis, loss of smell / taste; in children - anxiety, neurosis, insomnia, hyperkinesia; in the treatment of otitis media - headache;
- senses: conjunctivitis, impaired clarity and acuity of visual perception, tinnitus, deafness;
- genitourinary system: an increase in the plasma concentration of creatinine, an increase in the level of residual nitrogen in urea, vaginal candidiasis, interstitial nephritis, acute renal failure;
- organs of hematopoiesis: neutropenia, leukopenia, thrombocytopenia, eosinophilia, lymphopenia, hemolytic anemia;
- hypersensitivity reactions: urticaria, rash, pruritus, angioedema, Stevens-Johnson syndrome (malignant exudative erythema), erythema multiforme, Lyell's syndrome (toxic epidermal necrolysis), anaphylactic reaction;
- other: arthralgia, hyperglycemia, asthenia, photosensitivity reactions, peripheral edema, weakness, malaise.
Overdose
Symptoms of an azithromycin overdose are: severe nausea, diarrhea, vomiting, temporary hearing loss.
Immediate withdrawal of Zitrolide forte, gastric lavage, intake of activated charcoal and, if necessary, symptomatic therapy is recommended.
special instructions
Zitrolide forte is taken one hour before or two hours after antacid medicines.
If the next daily dose is missed, the capsule should be taken as soon as it is remembered, and the subsequent ones should be taken at intervals of 24 hours from this time.
The presence of symptoms of impaired hepatic function, such as a tendency to bleeding, rapidly increasing asthenia, dark urine, jaundice, hepatic encephalopathy, requires discontinuation of azithromycin therapy and a study of the functional state of the liver.
Due to the possible development of ergotism, the simultaneous administration of ergotamine and dihydroergotamine derivatives with azithromycin is contraindicated.
Both against the background of therapy with Zitrolide Forte, and two to three weeks after its completion, it is possible to develop pseudomembranous colitis caused by Clostridium difficile, accompanied by diarrhea. With a mild form of the disease, you should stop taking azithromycin and start using ion exchange resins (colestipol, colestyramine). In the case of a severe course of the disease, replacement of the loss of fluid, protein and electrolytes is required, as well as the use of bacitracin, vancomycin or metronidazole.
Do not use drugs that inhibit the peristalsis of the gastrointestinal tract during azithromycin therapy.
Due to the likely prolongation of the QT interval in patients receiving macrolides, including azithromycin, caution should be exercised when using it in patients with known risk factors for QT interval prolongation: in case of electrolyte imbalance (hypomagnesemia, hypokalemia), congenital prolongation of the QT interval syndrome, diseases heart (heart failure, bradycardia, myocardial infarction), while taking drugs that can lengthen the QT interval (antiarrhythmic drugs Ia and III classes, tricyclic and tetracyclic antidepressants, antipsychotics, fluoroquinolones), and in old age.
Azithromycin can cause the development of myasthenic syndrome or exacerbation of myasthenia gravis.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment with Zitrolide forte, care is required when performing potentially hazardous types of work, including driving motor vehicles, since the drug can affect concentration and the speed of psychomotor reactions.
Application during pregnancy and lactation
Due to the fact that azithromycin penetrates the placental barrier, its use during pregnancy is allowed only in the case of a clinically significant excess of the intended benefit to the mother over the potential risk to the fetus.
If Zitrolide forte must be used during lactation, breastfeeding must be discontinued.
Pediatric use
In pediatric practice, the use of Zitrolide forte 500 mg for the treatment of children under 12 years of age and / or weighing less than 45 kg is contraindicated.
With impaired renal function
Zitrolide forte is contraindicated in severe renal failure with creatinine clearance less than 40 ml / min.
With renal failure of moderate severity with a creatinine clearance of more than 40 ml / min, therapy should be carried out under the control of renal function.
For violations of liver function
Zitrolide forte is contraindicated in severe hepatic insufficiency of class B and higher on the Child-Pugh scale.
In mild and moderate hepatic insufficiency (on the Child-Pugh scale below class B), therapy should be carried out with caution because of the possibility of developing severe hepatic failure and fulminant hepatitis.
Drug interactions
- antacids (magnesium- and aluminum-containing): they do not affect the bioavailability of azithromycin, but reduce its concentration in the blood by 30%, therefore Zitrolide forte should be taken one hour before or two hours after taking them;
- derivatives of ergotamine and dihydroergotamine: their toxic effect may increase, manifested by vasospasm, dysesthesia;
- anticoagulants of indirect action of the coumarin series (warfarin): taking with azithromycin in usual doses requires careful monitoring of prothrombin time;
- terfenadine: simultaneous administration of terfenadine with macrolides can cause arrhythmia and prolongation of the QT interval, and therefore such a reaction cannot be ruled out when taken together with azithromycin, therefore, care must be taken;
- cyclosporin, digoxin: it is necessary to control their concentration in the blood (it is possible to increase the absorption of digoxin in the intestine);
- nelfinavir: may increase the incidence of azithromycin adverse reactions, such as hearing loss, increased hepatic transaminase activity;
- zidovudine: azithromycin does not affect its pharmacokinetic parameters and renal excretion of zidovudine itself and its glucuronide, but in mononuclear cells of peripheral vessels it increases the concentration of its active metabolite, phosphorylated zidovudine; at the moment, the clinical significance of this interaction has not been determined;
- cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other substances metabolized with the participation of the CYP3A4 isoenzyme: it is necessary to take into account the possibility of inhibition of this enzyme by azithromycin;
- carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin and methylprednisolone: azithromycin does not affect blood concentration.
Analogs
Analogs of Zitrolide forte are: Azibiot, Azidrop, Azitral, Azivok, AzitRus, Azitrox, Azithromycin, ZI-Factor, Zetamax retard, Zitnob, Zitrocin, Zitrolide, Sumaklid, Sumametsin, Sumamox, Sumamed, Sumatrolid, Dr Solutioncommed.
Terms and conditions of storage
Store in a dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Zitrolide forte
According to reviews, Zitrolide Forte is a potent antibiotic of a new generation that treats diseases of the upper respiratory tract well. The drug is convenient to use, but like all antibacterial agents, it can provoke various side reactions. Patients recommend taking Zitrolide forte especially carefully for asthmatics, since azithromycin worsens the respiratory state. One of the reviews states that there is a possibility of acquiring a fake of this drug in pharmacies.
The price of Zitrolide forte in pharmacies
Approximate price for Zitrolide forte 500 mg (3 capsules per package) - 266-330 rubles.
Zitrolide forte: prices in online pharmacies
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Drug name Price Pharmacy |
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Zitrolide forte 500 mg capsules 3 pcs. 153 r Buy |
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Zitrolide forte capsules 500mg 3 pcs. 330 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
