pharmachologic effect
Polypeptide cyclic antibiotic. Sodium colistimethate is produced by Bacillus polymyxa, subspecies colistinus. Colistimethate is colistin methanesulfonate. Sodium colistimethate has a bactericidal effect on gram-negative microorganisms that are in the stage of division and dormancy, by changing the structure and function of the outer and cytoplasmic membrane.
The drug is active against Pseudomonas aeruginosa, Haemophilus influenzae, Acinetobacter spp., Citrobacter spp., Enterobacter spp., Klebsiella spp., Salmonella spp., Shigella spp.
Not active against Burkholderia cepacia and Staphylococcus aureus.
Caution is required when determining the sensitivity or resistance of pathogens when using colistimethate sodium by inhalation.
Overdose
Symptoms: from the central nervous system and peripheral nervous system - dizziness, paresthesia, diplopia (due to paresis of the eye muscles), ptosis, general weakness, speech impairment, areflexia, visual impairment, dysphagia, convulsions and coma; neuromuscular blockade can cause death due to respiratory paralysis; from the urinary system - damage to the epithelial cells of the renal tubules and necrosis of the tubules.
Treatment: symptomatic therapy, peritoneal dialysis (or hemodialysis) is advisable; Ventilation Calcium gluconate and neostigmine do not relieve neuromuscular blockade.
Directions for use and doses
The drug is used by inhalation.
For adults and children over 6 years of age, the daily dose of the drug ranges from 2 million units to 6 million units, depending on the severity of the disease. As a rule, 1 million units are prescribed 2 times a day with an interval of 12 hours.
The duration of rehabilitation therapy for primary colonization/infection caused by Pseudomonas aeruginosa ranges from 3 weeks to 3 months. There is no time limit on the duration of therapy for chronic infection caused by Pseudomonas aeruginosa.
In patients with impaired renal function, the dose of the drug does not need to be reduced.
Pharmacokinetics
Suction
Absorption of colistimethate sodium after inhalation is characterized by pronounced individual differences. Cmax of colistimethate sodium in serum after inhalation at a dose of 2 million units ranges from an undetectable level to 280 mcg/l. When comparing these values with the serum concentration of the drug after parenteral administration, it can be concluded that absorption is less than 2%.
Distribution
1 hour and 4 hours after inhalation of the drug at a dose of 1 million units, the concentration of sodium colistimethate in sputum is 183.6 mg/l and 22.8 mg/l, respectively. About 15% of the administered dose accumulates in the lungs.
Colistimethate sodium penetrates the placental barrier and is excreted in breast milk.
Removal
Colistimethate sodium is excreted in expectorated sputum. A small part of the drug that enters the systemic circulation is eliminated primarily by glomerular filtration. Within 8 hours, about 60% of the ingested dose is excreted unchanged by the kidneys.
After inhalation of the drug at a dose of 2 million units, the average cumulative rate of renal excretion is approximately 1%.
Pharmacokinetics in special clinical situations
The pharmacokinetics of colistimethate sodium in patients with renal failure have not been studied. However, due to the low systemic bioavailability of the drug, the risk of adverse reactions is low.
special instructions
Inhaled drugs, incl. Colistin may cause acute bronchoconstriction in sensitive patients. Therefore, the use of the first dose of Colistin for inhalation should be carried out under the supervision of experienced medical personnel, and inhalation should be preceded by the use of a bronchodilator, if it is included in the treatment regimen of this patient. Before and after inhalation of Colistin, FEV should be measured in 1 second. If a patient not receiving bronchodilators has signs of drug-induced bronchial obstruction, the next time Colistin is used, the test should be repeated by adding a bronchodilator.
The first use of Colistin should be carried out under the supervision of medical personnel experienced in working with patients suffering from cystic fibrosis.
Patients with impaired renal function should be closely monitored for the possibility of side effects from the nervous system and renal function should be regularly monitored.
It is necessary to take a break between dornase alfa inhalation and Colistin inhalation.
In rare cases, treatment with Colistin may result in the emergence of resistant strains of Pseudomonas aeruginosa. After discontinuation and/or modification of therapy, the effectiveness of the drug may be restored.
During treatment with the drug, the patient should refrain from drinking alcohol.
Colistin
Stylab / Catalog / Antibacterial drugs / Colistin
STYLAB offers test systems for the determination of colistin in meat, fat, liver, as well as in fish, milk, eggs and animal feed using the ELISA method.
| Enzyme-linked immunosorbent assay (ELISA), strip plate | 5151COL Colistin ELISA |
Colistin, or polymyxin E, is a mixture of polymyxins E1 and E2, a narrow-spectrum antibiotic. Like other polymyxins, colistin is a cyclic polypeptide. It was first isolated in 1949 in Japan from a culture of the soil nitrogen-fixing bacterium Bacillus polymyxa.
Colistin and colistin sodium have been used in medicine since 1959. It is effective against gram-negative bacteria, including Pseudomonas aeruginosa , Klebsiella, Acinetobacter, Enterobacter. In the 1980s, the use of colistin was stopped due to severe side effects, including nephrotoxicity, ototoxicity and neurotoxicity. They are especially pronounced with intravenous administration of colistin. Colistin sodium is able to penetrate the placenta into the fetus, causing nephrotoxic and neurotoxic effects on the embryo.
A common side effect of inhaled colistin is bronchospasm. In addition, like other antibiotics, colistin inhibits microflora, which can lead to candidiasis or bacterial lesions of the oral cavity and gastrointestinal tract.
The use of colistin in medicine resumed in the 1990s due to the spread of bacteria resistant to other antibiotics. However, in 2015, data were published on the presence of the MCR-1 gene Escherichia coli , Klebsiella and Salmonella This gene is located in plasmids, which means resistance spreads quickly to other bacteria. This gene has been found in both pig intestinal bacteria and human microorganisms. Resistance to colistin is completely cross-resistance with other polymyxins. However, it does not mean that the microorganism is resistant to antibiotics of other groups.
Colistin is currently used to treat infections caused by bacteria resistant to other antibiotics. Colistin is used intravenously or in forms for external use: in the form of creams, ointments, ear rinsing solutions, etc. In addition, colistin is used for inhalation for antibacterial therapy for cystic fibrosis and respiratory diseases. In some countries, including the Russian Federation, colistin is allowed to be used in veterinary medicine. It is used to treat bacterial diarrhea, including salmonellosis in poultry, calves, pigs and rabbits. For these purposes, colistin is mixed into the feed.
Both in the Russian Federation and in the countries of the European Union the following maximum permissible levels of colistin in food products have been adopted: in meat, fish and fat - 0.15 mg/kg, in liver and kidneys - 0.2 mg/kg, in milk - 0 .05 mg/kg, in egg – 0.3 mg/kg. For screening colistin in food and animal feed, it is convenient to use ELISA test systems. They allow you to quickly process a large number of samples and obtain quantitative results.
Literature
- Colistin: instructions, application and formula. Radar website.
- Sachin Gupta, Deepak Govil, Prem N. Kakar, Om Prakash, Deep Arora, Shibani Das, Pradeep Govil, and Ashima Malhotra. Colistin and polymyxin B: A re-emergence Indian J Crit Care Med. 2009 Apr-Jun; 13(2): 49–53.
- Roger L Nation and Jian Li. Colistin in the 21st Century. Curr Opin Infect Dis. 2009 Dec; 22(6): 535–543.
- Yi-Yun Liu, Yang Wang, Timothy R Walsh, Ling-Xian Yi, Rong Zhang, James Spencer, Yohei Doi, Guobao Tian, Baolei Dong, Xianhui Huang, Lin-Feng Yu, Danxia Gu, Hongwei Ren, Xiaojie Chen, Luchao Lv, Dandan He, Hongwei Zhou, Zisen Liang, Jian-Hua Liu, Jianzhong Shen. Emergence of plasmid-mediated colistin resistance mechanism MCR-1 in animals and human beings in China: a microbiological and molecular biological study. Lancet Infect Dis 2016; 16: 161–68. Published Online November 18, 2015
- The European Agency for the Evaluation of Medical Products Veterinary Medicines and Inspections. Committee for Veterinary Medical Products. Colistin. Summary Report. (1)EMEA/MRL/016/95-FINAL
- The European Agency for the Evaluation of Medical Products Veterinary Medicines and Inspections. Committee for Veterinary Medical Products. Colistin. Summary Report. (2). EMEA/MRL/815/02-FINAL January 2002
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Conditions for dispensing from pharmacies
The drug is available with a prescription.
Attention!
The description of the drug "Colistin" on this page is a simplified and expanded version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the instructions approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Colistin 1 million unit 3ml 10 pcs. powder for solution for inhalation
pharmachologic effect
Cyclic polypeptide antibiotic produced by Bacillus polymyxa, subspecies colistinus.
It has a bactericidal effect on gram-negative microorganisms that are in the stage of division and dormancy, by changing the structure and function of the outer and cytoplasmic membrane. In vitro, Pseudomonas aeruginosa and Hemophilus influenza are sensitive to the drug; Burkholderia cepacia and Staphylococcus aureus are not sensitive.
Composition and release form Colistin 1 million. unit 3ml 10 pcs. powder for solution for inhalation
Colistimethate sodium - 1 million units (80 mg).
Solvent: sodium chloride solution 0.9% - 3 ml.
Description of the dosage form
Powder for preparing a solution for inhalation, white or almost white, hygroscopic.
Directions for use and doses
Inhalation (via nebulizer). The daily dose for adults and children over 6 years of age is 2-6 million units, depending on the severity of the disease. The average dose is 1 million units 2 times a day with an interval of 12 hours.
The duration of sanitation therapy for primary colonization/infection caused by Pseudomonas aeruginosa is from 3 weeks to 3 months.
Pharmacokinetics
Suction:
Absorption of colistimethate sodium after inhalation is characterized by pronounced individual differences. Cmax of colistimethate sodium in serum after inhalation at a dose of 2 million units ranges from an undetectable level to 280 mcg/l. When comparing these values with the serum concentration of the drug after parenteral administration, it can be concluded that absorption is less than 2%.
Distribution:
1 hour and 4 hours after inhalation of the drug at a dose of 1 million units, the concentration of sodium colistimethate in sputum is 183.6 mg/l and 22.8 mg/l, respectively. About 15% of the administered dose accumulates in the lungs.
Colistimethate sodium penetrates the placental barrier and is excreted in breast milk.
Removal:
Colistimethate sodium is excreted in expectorated sputum. A small part of the drug that enters the systemic circulation is eliminated primarily by glomerular filtration. Within 8 hours, about 60% of the ingested dose is excreted unchanged by the kidneys.
After inhalation of the drug at a dose of 2 million units, the average cumulative rate of renal excretion is approximately 1%.
Pharmacokinetics in special clinical situations:
The pharmacokinetics of colistimethate sodium in patients with renal failure have not been studied. However, due to the low systemic bioavailability of the drug, the risk of adverse reactions is low.
Indications for use Colistin 1 million. unit 3ml 10 pcs. powder for solution for inhalation
Treatment of respiratory tract infections in cystic fibrosis caused by Pseudomonas aeruginosa.
Contraindications
Hypersensitivity (including to polymyxin B), children's age (up to 6 years), lactation period.
Application of Colistin 1 million. unit 3ml 10 pcs. powder for preparing a solution for inhalation during pregnancy and breastfeeding
During pregnancy, due to the risk of developing nephro- and neurotoxic reactions in the fetus, the drug should be used only for health reasons.
Children's age up to 6 years.
special instructions
Inhaled drugs, incl. Colistin may cause acute bronchoconstriction in sensitive patients. Therefore, the use of the first dose of Colistin for inhalation should be carried out under the supervision of experienced medical personnel, and inhalation should be preceded by the use of a bronchodilator, if it is included in the treatment regimen of this patient. Before and after inhalation of Colistin, FEV should be measured in 1 second. If a patient not receiving bronchodilators has signs of drug-induced bronchial obstruction, the next time Colistin is used, the test should be repeated by adding a bronchodilator.
The first use of Colistin should be carried out under the supervision of medical personnel experienced in working with patients suffering from cystic fibrosis.
Patients with impaired renal function should be closely monitored for the possibility of side effects from the nervous system and renal function should be regularly monitored.
It is necessary to take a break between dornase alfa inhalation and Colistin inhalation.
In rare cases, treatment with Colistin may result in the emergence of resistant strains of Pseudomonas aeruginosa. After discontinuation and/or modification of therapy, the effectiveness of the drug may be restored.
During treatment with the drug, the patient should refrain from drinking alcohol.
Impact on the ability to drive vehicles and operate machinery:
During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms: from the central nervous system and peripheral nervous system - dizziness, paresthesia, diplopia (due to paresis of the eye muscles), ptosis, general weakness, speech impairment, areflexia, visual impairment, dysphagia, convulsions and coma; neuromuscular blockade can cause death due to respiratory paralysis; from the urinary system - damage to the epithelial cells of the renal tubules and necrosis of the tubules.
Treatment: symptomatic therapy, peritoneal dialysis (or hemodialysis) is advisable; Ventilation Calcium gluconate and neostigmine do not relieve neuromuscular blockade.
Side effects Colistin 1 million. unit 3ml 10 pcs. powder for solution for inhalation
Allergic reactions: angioedema.
From the nervous system: dizziness, paresthesia.
From the respiratory system: bronchospasm (more than 10%), increased cough, increased sputum production, mucositis, pharyngitis, shortness of breath.
From the digestive system: nausea, heartburn.
From the genitourinary system: acute renal failure.
Drug interactions
The prepared solution should not be mixed with other drug solutions.
Agents for general inhalation anesthesia (diethyl ether, halothane), muscle relaxants (tubocurarine chloride, suxamethonium), aminoglycosides - the risk of developing neurotoxic reactions.
Potentially nephrotoxic drugs (aminoglycosides, cephalosporins, cyclosporine) - increased nephrotoxicity.
If simultaneous use of dornase alfa is necessary, a break must be taken between inhalations of dornase alfa and inhalation of the drug.
