Zitrolide
Zitrolide: 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
ATX code: J01FA10
Active ingredient: azithromycin (azithromycin)
Producer: Valenta Pharmaceuticals, PJSC (Russia)
Description and photo update: 2019-20-08
Prices in pharmacies: from 153 rubles.
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Zitrolide is an antibiotic of the macrolide group, which is a representative of the azalide subgroup.
Release form and composition
Zitrolide dosage form - capsules: size No. 0, with a white body and a yellow or orange-yellow cap; content - powder from white to white with a creamy shade of color (6 pcs. in blister strip packs, 1 pack in a cardboard box; 10 pcs. in blister strip packs, 10 packs in a cardboard box).
Active ingredient: azithromycin, in 1 capsule - 250 mg.
Additional substances: microcrystalline cellulose, magnesium stearate.
Shell composition: gelatin, azorubin, titanium dioxide, ponceau 4R, quinoline yellow.
Pharmacological properties
Pharmacodynamics
Azithromycin is a broad-spectrum bacteriostatic antibiotic, belongs to the group of macrolides (azalides). Has a wide spectrum of antimicrobial action.
The pharmacological effect of azithromycin is based on the suppression of microbial cell protein synthesis. It binds to the 50S-subunit of the ribosome, resulting in inhibition of peptide translocase at the translation stage and inhibition of protein synthesis, which leads to a slowdown in the reproduction and growth of bacteria. When used in high concentrations, it has a bactericidal effect. It is active against a number of gram-positive / gram-negative aerobes, anaerobes, intracellular and other microorganisms.
Resistance to the action of azithromycin can be initial or acquired.
In most cases, sensitivity to azithromycin is manifested by:
- gram-positive / gram-negative aerobes: Streptococcus pneumoniae penicillin-susceptible, Staphylococcus aureus methicillin-susceptible, Streptococcus pyogenes, Neisseria gonorrhoeae, Haemophilus parainfluenzae, Haemophilus influenza, Pasteraxella multocida;
- anaerobes: Fusobacterium spp., Clostridium perfringens, Porphyromonas spp., Prevotella spp.,
- other microorganisms: Borrelia burgdorferi, Chlamydia psittaci, Chlamydia pneumonia, Chlamydia trachomatis, Mycoplasma hominis, Mycoplasma pneumonia.
Microorganisms initially resistant to the action of Zitrolide: Enterococcus faecalis, Staphylococci (methicillin-resistant staphylococci have very high resistance to macrolides), Bacteroides fragilis, erythromycin-resistant gram-positive bacteria.
Streptococcus pneumoniae penicillin-resistant can develop resistance to azithromycin.
Pharmacokinetics
Azithromycin has a high absorption, lipophilic, acid-resistant.
After a single dose of 500 mg, bioavailability is 37% (due to the effect of the first passage through the liver). C max (maximum concentration of the substance) after oral administration of the specified dose is 0.4 mg / l, this figure is achieved in 2.5–2.9 hours. The concentration of the substance in cells and tissues is 10-50 times higher than the serum concentration.
The volume of distribution is 31.1 l / kg, the substance easily penetrates the histohematogenous barriers. There is a good penetration of azithromycin into the prostate gland, urogenital tissues and organs, soft tissues, skin, respiratory tract.
Accumulation is observed in an environment with low pH, in lysosomes (this is especially important for the eradication of intracellular pathogens). It is also transported by phagocytes, macrophages and polymorphonuclear leukocytes. Penetrates through cell membranes, where it creates high concentrations.
In the foci of infection, the concentration of azithromycin significantly exceeds that in healthy tissues (by 24–34%) and correlates with the severity of inflammatory edema. In the focus of inflammation, after taking the last dose, the effective concentrations of the substance remain for 5 to 7 days. The connection with plasma proteins is in the range from 7 to 50% (it is inversely proportional to the concentration in the blood).
Demethylated in the liver with the formation of inactive metabolites. Isoenzymes CYP3A4, CYP3A5, CYP3A7 are involved in the metabolism of azithromycin (it is their inhibitor). Plasma clearance is 630 ml / min.
T 1/2 (half-life) between 8 and 24 hours after administration is approximately 14–20 hours, between 24 and 72 hours - 41 hours. 50% of the substance is excreted unchanged in the bile, 6% - by the kidneys.
Food intake has a significant effect on pharmacokinetic parameters: C max decreases by 52%, AUC (area under the concentration-time curve) - by 43%.
In elderly women, C max values increase by 30-50%.
Indications for use
According to the instructions, Zitrolide is a drug for the treatment of infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:
- Infections of the upper and lower respiratory tract and ENT organs, including tonsillitis, pharyngitis, otitis media, tonsillitis, sinusitis, bronchitis, bacterial and atypical pneumonia;
- Infections of the genitourinary system, including cervicitis, uncomplicated urethritis;
- Diseases of the stomach and duodenum associated with Helicobacter pylori (complex therapy);
- Infections of the skin and soft tissues, including impetigo, erysipelas, secondarily infected dermatoses;
- Scarlet fever;
- The initial stage of Lyme disease (borreliosis) is erythema creeping (erythema migrans).
Contraindications
Absolute:
- renal failure in severe degree (with creatinine clearance less than 40 ml / min);
- severe hepatic impairment (on the Child-Pugh scale, class B and higher);
- lactation period;
- age up to 12 years with a body weight of up to 45 kg;
- combined therapy with ergotamine and dihydroergotamine;
- individual intolerance to the components of the drug, as well as other macrolides.
Relative (Zitrolide is prescribed under medical supervision):
- arrhythmia, including the presence of a predisposition to the occurrence of arrhythmias and prolongation of the QT interval (associated with the risk of developing ventricular arrhythmias and prolongation of the QT interval);
- myasthenia gravis;
- liver failure (on the Child-Pugh scale below class B);
- renal failure (with creatinine clearance greater than 40 ml / min);
- combined therapy with warfarin, terfenadine, digoxin;
- pregnancy.
Instructions for the use of Zitrolide: method and dosage
Zitrolide should be taken orally 1 time per day, on an empty stomach - 1 hour before or 2 hours after meals.
Recommended daily doses for adults, depending on the indication:
- Respiratory tract infections: 500 mg, duration of treatment - 3 days (i.e., total course dose - 1500 mg);
- Infections of the skin and soft tissues, as well as stage I of Lyme disease: 1st day - 1000 mg, then 500 mg for the next 4 days (total course dose - 3000 mg);
- Acute infections of the genitourinary system: 1000 mg once;
- Peptic ulcer disease associated with Helicobacter pylori (in combination therapy): 1000 mg for 3 days.
The dose of Zitrolide for children is determined depending on the weight - at the rate of 10 mg per kilogram of body weight 1 time per day in a 3-day course or according to the following scheme: 1st day - 10 mg / kg, over the next 3-4 days - 5-10 mg / kg.
For children, for the treatment of the initial stage of Lyme disease, Zitrolide is prescribed according to the following scheme: 1st day - 20 mg / kg, during the next 4 days - 10 mg / kg.
Side effects
- From the digestive system: often (> 1%) - nausea, diarrhea, abdominal pain; rarely (≤1%) - flatulence, dyspepsia, melena, vomiting, increased activity of hepatic transaminases, cholestatic jaundice; rarely in children - anorexia, change in taste, constipation, gastritis;
- From the side of the cardiovascular system: rarely - chest pain, palpitations;
- From the side of the central nervous system: rarely - drowsiness, headache, vertigo; rarely in children - anxiety, sleep disturbance, neurosis, hyperkinesia, with otitis media - headache;
- From the genitourinary system: rarely - nephritis, vaginal candidiasis;
- Allergic reactions: photosensitivity, rash, Quincke's edema; rarely in children - urticaria, itching, conjunctivitis.
Overdose
The main symptoms: diarrhea, vomiting, severe nausea, passing hearing loss.
Therapy: Zitrolide cancellation, gastric lavage, activated charcoal intake, symptomatic treatment.
special instructions
Hypersensitivity reactions in some patients may persist even after Zitrolide is discontinued, in which case specific therapy is required.
If necessary, the simultaneous use of antacids between doses should take 2-hour breaks.
Influence on the ability to drive vehicles and complex mechanisms
Patients during the period of taking Zitrolide while driving a motor vehicle should be careful.
Application during pregnancy and lactation
- pregnancy: Zitrolide can be used only under medical supervision after evaluating the ratio of the expected benefit from therapy with the existing risk; azithromycin crosses the placenta;
- period of breastfeeding: therapy is contraindicated.
Pediatric use
Zitrolide therapy is contraindicated in patients under 12 years of age weighing up to 45 kg.
With impaired renal function
- renal failure in severe degree (with creatinine clearance less than 40 ml / min): therapy is contraindicated;
- renal failure (with creatinine clearance greater than 40 ml / min): Zitrolide should be used under medical supervision.
For violations of liver function
- severe hepatic impairment (on the Child-Pugh scale class B and higher): therapy is contraindicated;
- hepatic impairment (on the Child-Pugh scale below class B): Zitrolide should be used under medical supervision.
Drug interactions
- Digoxin: its concentration increases;
- Ergotamine, dihydroergotamine: their toxic effect increases (manifested by dysesthesia and vasospasm);
- Triazolam: its clearance decreases and its effect increases;
- Magnesium and aluminum-containing antacids, ethanol, food: absorption of azithromycin slows down and decreases;
- Warfarin: an increase in the anticoagulant effect is possible (prothrombin time must be carefully monitored);
- Lincosamines: the effectiveness of azithromycin decreases;
- Chloramphenicol, tetracycline: increases the effectiveness of azithromycin;
- Indirect anticoagulants, cycloserine, felodipine, methylprednisolone, and drugs subject to microsomal oxidation (oral hypoglycemic agents, ergot alkaloids, hexobarbital, valproic acid, cyclosporine, terfenadine, disopyramide, carbrypinephrine, biphenylamine) their excretion slows down, plasma concentration and toxicity increase.
Analogs
Zitrolide analogs are: Azithromycin, Azithromycin-OBL, Azithromycin-BHFZ, Azithromycin-KR, Azithromycin-Astrafarm, Azithromycin-Health, Azitrox, Azimed, Azine, Azicin, Zitroleks, Sumamed, Ormax.
Terms and conditions of storage
Store at temperatures up to 25 ºС. Keep out of the reach of children. Do not expose to moisture and sunlight.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Zitrolide
Reviews of Zitrolide are mostly positive. Many patients write about its high effectiveness in the treatment of various infectious and inflammatory diseases, while noting that improvement occurs in a short time. There are reports of the development of side effects, in many cases they are of a short-term nature and do not require discontinuation of therapy. The cost of the drug in comparison with analogues is estimated as high.
The price of Zitrolide in pharmacies
The approximate price for Zitrolide for 6 capsules per package is 175–348 rubles.
Zitrolide: 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!
