Amizolid
Amizolid: 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. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Amizolid
ATX code: J01XX08
Active ingredient: linezolid (Linezolid)
Manufacturer: Pharmasintez JSC (Russia)
Description and photo update: 2019-10-07
Amizolid is an antibacterial drug of the oxazolidinone group.
Release form and composition
The drug is available in the form of film-coated tablets: from light brown to dark brown, biconvex, round (dosage 200 and 300 mg), capsular (dosage 400 mg) or oval (dosage 600 mg); the core of the tablet is white or white with a yellow tinge of color (dosages 200, 300, 400 or 600 mg: 10 pcs. in blisters, in a cardboard box 1, 2, 3, 5, 6 or 10 packages; 10, 14, 20, 24, 30, 50 or 100 pcs. In polymer cans, in a cardboard box 1 can; dosage 300 mg: 60 pcs. In polymer cans, in a cardboard box 1 can. Each pack also contains instructions for the use of Amizolid) …
Composition of 1 tablet:
- active substance: linezolid - 200, 300, 400 or 600 mg;
- auxiliary components: copovidone, betadex (beta-cyclodextrin), pregelatinized starch (for tablets with a dosage of 300 mg - pregelatinized corn starch), colloidal silicon dioxide (Aerosil A-300), sodium stearyl fumarate, magnesium hydroxycarbonate (for tablets with a dosage of magnesium carbonate 300 mg);
- water-soluble film shell: hydroxypropyl methylcellulose (hypromellose), polyethylene glycol (macrogol 6000), titanium dioxide, talc, iron dye red oxide, iron dye yellow oxide.
Pharmacological properties
Pharmacodynamics
Amizolid is an antibacterial drug of the oxazolidinone group. The antimicrobial effect of Amizolid is due to the ability of the active substance, linezolid, to inhibit protein synthesis in bacteria. As a result of binding to the 23S region located on the bacterial ribosomal RNA (ribonucleic acid) of the 50S subunit, linezolid prevents the formation of a functional 70S initiation complex, an important component of the translation process during protein synthesis. Aerobic Gram-positive bacteria, some Gram-negative bacteria, and anaerobic microorganisms exhibit sensitivity to linezolid in vitro.
Amizolid is active against the following microbes:
- gram-positive aerobes: in vitro and in vivo - Staphylococcus aureus (including methicillin-resistant strains), Enterococcus faecium (including vancomycin-resistant strains), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus pneumoniae (including multiresistant strains); in vitro - Enterococcus faecalis (including vancomycin-resistant strains), Enterococcus faecium (vancomycin-sensitive strains), Staphylococcus epidermidis (including methicillin-resistant strains), Staphylococcus haemolyticus, Streptococcus viridans;
- gram-negative aerobes: Pasteurella multocida.
Microorganisms such as Haemophilus influenzae, Neisseria speciales (spp.), Pseudomonas spp., Enterobacteriaceae spp., Moraxella catarrhalis are resistant to linezolid.
The mechanism of action of linezolid differs from that of aminoglycosides, beta-lactam antibiotics, folic acid antagonists, glycopeptides, lincosamides, quinolones, rifamycin, tetracyclines, and chloramphenicol. Therefore, with the simultaneous use of these antibacterial agents with linezolid, cross-resistance is unlikely. Amizolid is active against microorganisms sensitive and resistant to the listed antimicrobial agents. Resistance to linezolid develops very slowly through multistep mutation of 23S ribosomal RNA.
In addition to antimicrobial action, Amizolid exhibits the properties of a weak non-selective MAO (monoamine oxidase) inhibitor of types A and B.
Pharmacokinetics
After oral administration, linezolid is rapidly and intensively absorbed from the gastrointestinal tract. Simultaneous food intake does not affect the absorption of the drug. The absolute bioavailability is approximately 100%.
Against the background of a single dose of 400 mg tablets, the maximum concentration in the blood (C max) is reached after 1.52 hours and is 8.1 μg / ml. With a dosing regimen 2 times a day (800 mg), C max is reached after 1.12 hours and is 11 μg / ml. AUC (area under the curve "concentration - time") when taking Amizolid 1 time per day or 2 times a day, respectively, 55.1 or 73.4 μg / h / ml, clearance - 146 or 110 ml / min, T 1 / 2 (half-life) - 5.2 or 4.69 hours. While taking a dose of Amizolid 600 mg once a day or 2 times a day (1200 mg), the pharmacokinetic parameters of linezolid are (respectively): C max- achieved after 1.28 or 1.03 hours and is equal to 12.7 or 21.2 μg / ml, AUC - 91.4 or 138 μg / h / ml, clearance - 127 or 80 ml / min, T 1/2 - 4.26 or 5.4 hours.
Plasma protein binding, regardless of drug concentration, is 31%.
C ss (equilibrium concentration) in the blood is reached after 48–72 hours of therapy. Linezolid is rapidly distributed in tissues with good perfusion. When C ss is reached, the volume of distribution averages 40–50 liters.
As a result of metabolic oxidation, 2 inactive metabolites are formed. The main metabolite of linezolid, hydroxyethylglycine, is formed as a result of a non-enzymatic process. The second metabolite, aminoethoxyacetic acid, is formed in smaller quantities. In addition, other "small" inactive metabolites have been identified.
It was established in vitro that cytochrome P 450 isoenzymes do not participate in the metabolism of linezolid. The active substance does not inhibit or potentiate the activity of such clinically important cytochrome P 450 isozymes as CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6, CYP2E1.
The main part of the dose taken is excreted through the kidneys (30–35% - in the form of unchanged linezolid, 40% - in the form of hydroxyethylglycine, 10% - in the form of aminoethoxyacetic acid). Through the intestines in the form of hydroxyethylglycine, 6% of the dose taken is excreted, in the form of aminoethoxyacetic acid - 3%.
In children, the clearance of linezolid is higher, it decreases with increasing age of the patient.
It should be borne in mind that in women the volume of distribution is lower, the clearance is 20% less, the concentration in the plasma is higher than in men.
T 1/2 does not differ significantly in women and men, therefore, there is no need to adjust the dosage regimen related to the patient's gender.
In chronic renal failure, no dosage adjustment is required.
Patients on hemodialysis should take Amizolid after the procedure, since 30% of the drug dose is excreted within three hours of dialysis.
With moderate or moderate hepatic impairment, the pharmacokinetics of linezolid does not change, therefore, dose adjustment of Amizolid is not required.
Indications for use
The use of Amizolid is indicated for the treatment of the following infectious and inflammatory diseases caused by microorganisms sensitive to linezolid:
- community-acquired and hospital-acquired pneumonia;
- enterococcal infections, including those caused by strains of Enterococcus faecalis and Enterococcus faecium, which are resistant to vancomycin;
- infections of the skin and soft tissues.
Contraindications
Absolute:
- uncontrolled arterial hypertension, thyrotoxicosis, pheochromocytoma and / or the simultaneous use of adrenergic agonists (including pseudoephedrine, epinephrine, phenylpropanolamine, dobutamine, norepinephrine), dopamine and other dopaminomimetics - in the absence of blood pressure (BP) monitoring; and monitoring of the patient;
- concomitant therapy with serotonin reuptake inhibitors, tricyclic antidepressants, triptans (5-HT 1 receptor agonists), meperidine or buspirone and / or carcinoid syndrome - in the absence of careful monitoring in patients at increased risk of developing serotonin syndrome;
- simultaneous administration with phenelzine, isocarboxazid and other drugs, monoamine oxidase A and B inhibitors, or within 14 days after stopping their use;
- period of breastfeeding;
- age up to 12 years and body weight less than 40 kg;
- hypersensitivity to the components of the drug.
With caution, it is recommended to prescribe Amizolid during pregnancy, with hepatic failure, severe renal failure.
Amizolid, instructions for use: method and dosage
Amizolid tablets are taken orally, regardless of food intake.
Dose selection is not required when switching to the oral form of linezolid after pretreatment with the dosage form of the drug for intravenous administration.
The doctor prescribes the duration of the course of treatment individually, taking into account the pathogen, localization, severity of the infection and clinical efficacy.
The recommended dosage of Amizolid for adults and children aged 12 years and older (with a body weight of at least 40 kg):
- community-acquired pneumonia caused by Streptococcus pneumoniae (including multi-resistant strains), including infections accompanied by bacteremia, or methicillin-susceptible strains of Staphylococcus aureus: 600 mg 2 times a day with an interval of 12 hours between doses. Duration of the course - 10-14 days;
- hospital pneumonia caused by Streptococcus pneumoniae (including multidrug-resistant strains) or Staphylococcus aureus (including methicillin-sensitive and resistant strains): 600 mg 2 times a day every 12 hours for 10-14 days;
- complicated infections of the skin and soft tissues (including infections in diabetic foot syndrome, not accompanied by osteomyelitis) caused by Streptococcus pyogenes, Streptococcus agalactiae, or Staphylococcus aureus (including strains sensitive and resistant to methicillin): Amizolid 600 mg 2 times a day with an interval … The duration of treatment is from 10 to 14 days;
- infections caused by Enterococcus faecium resistant to vancomycin, including cases accompanied by bacteremia: 600 mg 2 times a day every 12 hours. The course of therapy is from 14 to 28 days.
For elderly patients, dose adjustment is not required.
Patients with renal or hepatic insufficiency do not need dose adjustment of Amizolid.
Side effects
Side effects of linezolid are mild to moderate. The most common adverse events are nausea, diarrhea, and headache.
Possible side effects during therapy with Amizolid:
- skin and subcutaneous tissues: often (≥ 1% and <10%) - rash, itching; infrequently (≥ 0.1% and <1%) - urticaria, dermatitis, excessive sweating; the frequency is unknown (it is impossible to determine the frequency of occurrence of adverse reactions based on the available data) - alopecia, bullous skin lesions, for example, toxic epidermal necrolysis;
- heart and blood vessels: often - increased blood pressure; infrequently - transient ischemic attack, tachycardia (arrhythmia), thrombophlebitis, phlebitis;
- blood and lymphatic system: infrequently - neutropenia, eosinophilia; frequency unknown - sideroblastic anemia;
- metabolism and nutrition: infrequently - hyponatremia;
- digestive system: often - nausea, vomiting, colic, local and generalized abdominal pain, diarrhea, constipation, dyspepsia, candidiasis of the oral mucosa, flatulence and / or convulsions; in addition, in children (aged 12 to 17) - loose stools; infrequently - discoloration of the mucous membrane of the tongue and other disorders of the tongue, dry mouth, stomatitis, glossitis, gastritis, pancreatitis, abdominal distension;
- respiratory system: often (in children) - pharyngitis, upper respiratory tract infections, cough;
- nervous system: often - headache, insomnia, dizziness, taste perversion (presence of a "metallic" taste in the mouth); in addition, in children - vertigo; infrequently - paresthesia, hypesthesia; frequency unknown - serotonin syndrome;
- immune system: frequency unknown - anaphylaxis;
- genitals and mammary gland: infrequently - disorders of the vagina and vulva;
- liver and biliary tract: often - increased activity of liver enzymes [including aspartate aminotransferase (ACT), alanine aminotransferase (ALT), alkaline phosphatase (ALP), amylase, lactate dehydrogenase (LDH)], change in the results of liver function tests; infrequently - an increase in the concentration of total bilirubin;
- kidneys and urinary tract: often - an increase in the level of urea in the blood; infrequently - polyuria, renal failure, increased plasma creatinine levels;
- organ of hearing and labyrinthine disorders: infrequently - ringing in the ears;
- organ of vision: infrequently - blurred vision; rarely - the appearance of visual field defects; frequency unknown - change in color vision, change in visual acuity, optic neuritis;
- infectious and parasitic diseases: often - fungal infections, candidiasis, including vaginal candidiasis and oral candidiasis; infrequently - vaginitis; rarely - colitis that occurs while taking antibiotics, including pseudomembranous colitis;
- laboratory parameters: often - an increase / decrease in platelets / leukocytes, an increase in glucose concentration (not on an empty stomach), the number of eosinophils, neutrophils, the activity of creatine kinase / amylase / lipase / lactate dehydrogenase, a decrease in sodium / calcium, the number of erythrocytes, hematocrit, hemoglobin, albumin, total protein, increase / decrease in potassium / bicarbonates; infrequently - an increase in the concentration of triglycerides in the blood, an increase in the number of reticulocytes, sodium / calcium, prolactin levels, a decrease in glucose concentration (not on an empty stomach), the number of neutrophils, an increase / decrease in blood chlorides;
- others: often - fever; in addition, in children - pain of unspecified localization; infrequently - opportunistic fungal infection, dyspepsia, weakness, thirst.
According to the results of post-marketing studies, the following undesirable effects of Amizolid were recorded:
- digestive system: discoloration of tooth enamel;
- nervous system: peripheral neuropathy, seizures;
- senses: neuropathy of the optic nerve (including cases leading to loss of vision);
- skin: skin rash, bullous skin lesions (Stevens-Johnson syndrome), angioedema;
- metabolism: lactic acidosis;
- allergic reactions: anaphylactic shock;
- laboratory parameters: reversible myelosuppression (anemia, leukopenia, thrombocytopenia, pancytopenia);
- others: increased fatigue, chills.
Overdose
Symptoms of an overdose of Amizolid have not been established.
Treatment: the appointment of symptomatic therapy, measures to restore and maintain the level of glomerular filtration. The use of hemodialysis for 3 hours allows you to withdraw 30% of the dose taken.
special instructions
In cases when, along with the established infection, a concomitant infection caused by gram-negative microorganisms occurs, an additional appointment of agents active against gram-negative flora is shown.
Due to the existing risk of developing reversible myelosuppression, accompanied by anemia, leukopenia, pancytopenia or thrombocytopenia, with prolonged use (more than 2 weeks) of Amizolid, it is necessary to control the number of platelets and hemoglobin in the blood. Patients with a history of myelosuppression or those who are prone to bleeding, as well as those on concomitant therapy with drugs that cause a decrease in the hemoglobin content or the number of platelets and / or their functional properties, require special attention.
During the period of treatment with Amizolid, the risk of developing pseudomembranous colitis of varying severity increases, this should be taken into account when diagnosing abdominal pain in a patient.
During treatment with linezolid, the normal intestinal microflora is disturbed, this leads to an increased growth of Clostridium difficile, which produces toxins A and B and causes the development of diarrhea. Diarrhea associated with Clostridium difficile can often be severe and accompanied by excess toxins. Infections caused by Clostridium difficile strains are highly resistant to antimicrobial therapy and can be fatal.
The risk of developing diarrhea associated with Clostridium difficile exists in all patients who have experienced diarrhea while taking Amizolid. Patients who have experienced Clostridium difficile-associated diarrhea while taking an antibacterial drug should be closely monitored for the next 8 weeks.
If visual acuity and color perception change, blurred vision, visual field defects or other symptoms indicating deterioration of visual function, it is recommended to urgently consult an ophthalmologist. Monitoring visual function is most important with prolonged (more than 12 weeks) intake of Amizolid. When neuropathy of the optic nerve and peripheral neuropathy occurs, it is necessary to decide whether to continue therapy, comparing the risks and benefits of treatment with linezolid.
Consideration should be given to the possibility of developing lactic acidosis. Therefore, if repeated nausea or vomiting, unexplained acidosis, a decrease in the concentration of bicarbonate anions occur while taking Amizolid, the condition of patients should be carefully monitored by a doctor.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment with Amizolid, patients are not recommended to engage in potentially hazardous activities, the implementation of which requires an increased concentration of attention and a high speed of psychomotor reactions, including driving and complex mechanisms.
Application during pregnancy and lactation
The use of Amizolid during gestation is possible only in cases where, in the opinion of the doctor, the expected therapeutic effect for the mother outweighs the potential risk to the fetus.
The use of linezolid during lactation is contraindicated. If it is necessary to prescribe the drug, breastfeeding should be discontinued.
Pediatric use
The appointment of Amizolid tablets is contraindicated for the treatment of patients under the age of 12 years and with a body weight of less than 40 kg.
With impaired renal function
Amizolid should be used with caution to treat patients with severe renal failure.
For violations of liver function
Amizolid should be used with caution to treat patients with hepatic insufficiency.
Use in the elderly
No dose adjustment is required when treating elderly patients.
Drug interactions
- adrenergic agonists (including epinephrine, pseudoephedrine, phenylpropanolamine, dobutamine, norepinephrine), dopaminomimetics (dopamine): linezolid can contribute to a moderate reversible increase in their pressor action, therefore it is recommended to reduce the initial doses of the listed drugs and carry out further dose selection by titration;
- antidepressants - selective serotonin reuptake inhibitors: the risk of developing serotonin syndrome increases;
- aztreonam, gentamicin: do not cause disturbance of linezolid pharmacokinetics;
- rifampicin: helps to reduce the C max of linezolid by an average of 21%, and the AUC by 32%.
Analogs
Amizolid analogs are: Bactolin, Zenix, Zivox, Infilinez, Linegen, Linezolid, Linezolid Canon, Linezolid-Acri, Linezolid-Vial, Linezolid-CRKA, Linezolid-Teva, Rowlin-Routek, Selezolid.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Amizolid
There are no reviews of Amizolid in social networks.
Price for Amizolid in pharmacies
The price of Amizolid can be:
- dosage 200 mg: 10 pcs. in the package - from 5100 rubles., 14 pcs. - from 7140 rubles., 20 pcs. - from 10 200 rubles, 24 pcs. - from 12 240 rubles., 30 pcs. - from 15 300 rubles., 50 pcs. - from 25 504 rubles., 60 pcs. - from 30 605 rubles., 100 pcs. - from 51,008 rubles;
- dosage 300 mg: 10 pcs. in the package - from 6300 rubles., 14 pcs. - from 8820 rubles, 20 pcs. - from 12 600 rubles;
- dosage 400 mg: 10 pcs. in the package - from 10 200 rubles., 20 pcs. - from 20 400 rubles., 24 pcs. - from 24 484 rubles., 30 pcs. - from 30 605 rubles., 50 pcs. - from 51,000 rubles., 60 pcs. - from 61 200 rubles, 100 pcs. - from 102,017 rubles;
- dosage 600 mg: 10 pcs. in the package - from 15 302 rubles., 14 pcs. - from RUB 21,423, 20 pcs. - from 30 605 rubles., 24 pcs. - from 36 726 rubles., 30 pcs. - from RUB 45,907, 50 pcs. - from RUB 76,513, 60 pcs. - from 91 815 rubles., 100 pcs. - from 153,026 rubles.
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!
