Colistin
Colistin: 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. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Colistin
ATX code: J01XB01
Active ingredient: colistimethate sodium
Manufacturer: Kcellia Pharmaceuticals APS (Denmark)
Description and photo update: 10.07.2018
Prices in pharmacies: from 1500 rubles.
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Colistin is an antibiotic for inhalation use.
Release form and composition
Colistin dosage form - powder for preparation of a solution for inhalation: white or almost white, hygroscopic (in colorless glass vials, sealed with a rubber stopper and rolled up with an aluminum cap with first opening control, in a cardboard box 1 bottle complete with 1 ampoule of solvent; packaging for hospitals - in a box with lattices or partitions 60 or 100 vials complete with 60 or 100 ampoules of solvent, respectively).
1 vial of the drug contains the active substance: sodium colistimethate - 1 million units (80 mg).
Solvent: 0.9% sodium chloride solution (3 ml in a type I colorless glass ampoule, on which there may be a technological mark, a breaking point, as well as a double ring on the ampoule head).
Pharmacological properties
Pharmacodynamics
Sodium colistimethate is a cyclic polypeptide antibiotic produced by Bacillus polymyxa, a subspecies of colistinus. It is a derivative of methanesulfonic acid colistin.
The drug has bactericidal activity against gram-negative bacteria. The mechanism of its action is due to the ability to disrupt the processes of polarization of membrane structures and, as a result, to change the structure and disrupt the functions of the cytoplasmic and outer membranes.
When determining the susceptibility to colistimethate from the table of bacteria sensitivity to antibiotics in relation to the use of the drug by inhalation, caution is required.
The following microorganisms are usually susceptible to colistimethate sodium: Haemophilus influenzae, Citrobacter spp., Salmonella spp., Klebsiella spp., Acinetobacter spp., Shigella spp., Pseudomonas aeruginosa, Escherichia coli.
The following microorganisms may develop acquired resistance: Stenotrophomonas maltophilia, Enterobacter spp., Achromobacter xylosoxidans.
Colistimethate sodium is usually resistant to anaerobic bacteria, gram-negative cocci, gram-positive bacteria (for example, Staphylococcus aureus), Proteus mirabilis, Burkholderia cepacia, Serratia marcescens.
In severe infectious processes and the ineffectiveness of antimicrobial therapy, local geographic characteristics of the spread of resistance should be taken into account. It also requires microbiological identification of a pathogenic microorganism and testing it for sensitivity to Colistin.
Full cross-resistance is observed between colistimethate sodium and polymyxin B. This phenomenon is absent with other antibiotics.
Pharmacokinetics
After inhalation, the absorption of colistimethate sodium varies significantly depending on the individual characteristics of the patient. The registered values of the maximum concentration of the drug in the blood serum after its inhalation at a dose of 2 million units are recorded at concentrations below the detection limit of up to 0.53 mg / l. Comparing these indicators with those after parenteral administration of sodium colistimethate, we can conclude that it is absorbed slightly. This fact is also confirmed by the data that after inhalation of the drug at a dose of 2 million units, the average value of the total renal excretion is about 4%.
1–4 hours after inhalation of 1–2 million units of sodium colistimethate, its concentration in sputum is 16–180 mg / l. About 15% of the dose received is retained in the lungs.
The drug practically does not penetrate into tissues and body fluids, including cerebrospinal fluid in case of inflammation of the meninges. Compared to the serum concentration in urine, it is 20–40 times higher.
It is characterized by a low bond with plasma proteins - no more than 10%. Penetrates the placenta.
The half-life is 2-3 hours.
After intravenous administration of sodium colistimethate, about 60% of the dose is excreted unchanged by the kidneys, where the maximum concentration is observed 2–4 hours after administration. It is assumed that these data relate to the absorbed part of the drug after inhalation. Unabsorbed sodium colistimethate is thought to be excreted in sputum.
Given the low systemic bioavailability of the drug, the risk of its cumulation, including in patients with renal failure, is assessed as minimal.
Indications for use
According to the instructions, Colistin is used to treat infectious diseases of the respiratory tract caused by gram-negative bacteria sensitive to its active substance, especially Pseudomonas aeruginosa (for example, in cystic fibrosis).
Contraindications
- myasthenia gravis (myasthenia gravis);
- children under 6 years old;
- the presence of hypersensitivity to sodium colistimethate or polymyxin B.
Colistin should be used with caution in bronchial hyperreactivity, hemoptysis, porphyria, impaired renal function, concomitant use of potentially nephrotoxic or neurotoxic drugs.
Instructions for the use of Colistin: method and dosage
Colistin is administered by inhalation. A solution is prepared from the powder immediately before inhalation.
The optimal dose is determined individually, depending on the severity of the disease and the sensitivity of the pathogen.
The daily dose for children from 6 years old and adults can vary between 2-6 million units. Usually, 1 million units are prescribed twice a day at 12-hour intervals.
In the case of the development of resistance of the pathogen, it is possible to increase the dose of Colistin to 2 million IU three times a day.
In the case of primary colonization / infection with Pseudomonas aeruginosa, debridement therapy may last from 3 weeks to 3 months.
In chronic infection caused by Pseudomonas aeruginosa, there are no restrictions on the duration of use of Colistin.
For patients undergoing combination therapy, Colistin should be administered immediately after the use of a bronchodilator, as well as after physiotherapy procedures on the chest.
For aerosol antibiotic treatment, it is recommended to use spray nebulizers (ultrasonic or jet), which, when used with an appropriate compressor, create most particles for inhalation no more than 5 microns in diameter (in this case, the most effective absorption of the drug by the lungs occurs).
When using the nebulizer and compressor, follow the manufacturer's instructions. Standard nebulizers create a continuous aerosol stream, so drug particles can evaporate into the environment. To avoid this, doctors advise using such devices in a well-ventilated area. The use of appropriate filters / valves will help to minimize drug evaporation.
Method of using Colistin:
- Open the bottle with the powder by removing the aluminum cap and opening the rubber stopper.
- Open the supplied solvent ampoule.
- Pour the solvent into a vial of powder and shake it until the powder dissolves. Avoid vigorous agitation as excessive foam formation is possible.
- Pour the solution into a nebulizer and inhale in accordance with the instructions for the inhalation device. One inhalation dose corresponds to the use of 3 ml of solution.
- Rinse and disinfect the nebulizer mouthpiece as directed in the manufacturer's instructions.
The inhalation procedure should be carried out in an upright position (sitting or standing), in a calm state, taking as deep breaths as possible through the mouthpiece. The nose clip makes it easier to inhale the drug through the mouth.
The prepared solution must not be mixed with other medicines.
Side effects
Side effects from the respiratory system are very common (> 1/10): increased sputum production, pharyngitis, increased cough, shortness of breath, bronchospasm, respiratory mucositis.
The frequency of the following adverse reactions could not be estimated based on the available data:
- infections and invasions: oral candidiasis; with long-term treatment - the proliferation of resistant microorganisms;
- from the gastrointestinal tract: unpleasant taste, burning sensation of the tongue, nausea;
- from the genitourinary system: acute renal failure;
- from the nervous system: dizziness, paresthesia;
- from the immune system: hypersensitivity reactions (itching, skin rash, angioedema).
Overdose
Considering the inhalation method of using Colistin, the intake of colistimethate sodium into the systemic circulation is insignificant, therefore the probability of an overdose is extremely low. To date, no such cases have been reported.
After accidental ingestion of the drug, it is unlikely that any toxic effects will occur, since sodium colistimethate is practically not absorbed from the gastrointestinal tract.
special instructions
Prepare a solution from a powder immediately before inhalation.
The contents of one bottle can be used only once, the unused drug must be disposed of.
With an exacerbation of a chronic infection caused by Pseudomonas aeruginosa, Colistin should not be used as a monopreparation.
The likelihood of developing resistant strains of microorganisms should be considered. After canceling and / or replacing Colistin, its effectiveness may be restored.
In patients with hypersensitivity, the drug can cause acute bronchospasm, therefore, the introduction of the first dose should be carried out under the supervision of a medical specialist with experience in the treatment of cystic fibrosis. In this case, inhalation should be done after the use of a bronchodilator, if it is included in the patient's therapeutic regimen. Before and after inhalation of Colistin, the forced expiratory volume is measured in the first second (FEV1). If a patient who does not receive a bronchodilator has signs of drug-induced bronchial obstruction, the FEV1 test should be repeated with the next inhalation of Colistin, adding a bronchodilator.
With porphyria, it should be borne in mind that the drug can enhance its clinical manifestations.
In the case of combined use with nephrotoxic agents, it is necessary to monitor renal function.
With hemoptysis, sodium colistimethate can aggravate the cough, so its use is possible only after assessing the balance of benefits and risks.
With the simultaneous use of recombinant human DNase (dornase alpha), a break should be taken between inhalations of drugs.
During treatment, you should not drink alcoholic beverages.
Influence on the ability to drive vehicles and complex mechanisms
The antibiotic Colistin can affect the rate of reactions (for example, due to the occurrence of dizziness), therefore, during its use, it is recommended to refrain from driving vehicles and performing potentially dangerous types of work that require the speed of psychophysical reactions.
Application during pregnancy and lactation
Colistimethate sodium crosses the placental barrier. Due to the risk of developing neuro- and nephrotoxic reactions in the fetus, during pregnancy, Colistin is allowed to be used only in cases where the expected benefit of therapy is definitely higher than all possible risks.
Colistimethate sodium passes into breast milk. May cause an imbalance in the intestinal microflora in the child, leading to diarrhea and colonization of the intestine by Blastomyces spp. Development of sensitization is possible. If treatment is required during lactation, breastfeeding should be discontinued.
Pediatric use
The antibiotic Colistin is not indicated for the treatment of children under 6 years of age.
With impaired renal function
In case of impaired renal function, Colistin should be used with caution, under the control of renal function. The patient should be monitored for the development of adverse reactions from the nervous system.
Drug interactions
With caution, colistimethate sodium should be used simultaneously with potentially nephrotoxic agents (loop diuretics, cephalosporins, cyclosporins, aminoglycosides), since there is a risk of increased nephrotoxicity.
When using Colistin in combination with aminoglycosides, muscle relaxants of central and peripheral action, inhalation anesthesia, the likelihood of blockade of neuromuscular transmission increases.
Analogs
The analogue of Colistin is Colomycin.
Terms and conditions of storage
Store in its original packaging at temperatures up to 25 ° C in a place protected from light, out of reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Kolistin
Most of the reviews about Kolistin are positive. Colistimethate sodium is one of the few drugs that are highly effective in cystic fibrosis.
Negative reviews contain complaints about the development of side effects.
The price of Colistin in pharmacies
The price of Colistin powder for a solution for inhalation of 80 mg 1 million units averages 1,350 rubles. for 1 bottle of the drug with an ampoule of solvent (isotonic NaCl solution).
Colistin: prices in online pharmacies
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Drug name Price Pharmacy |
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Colistin 80 mg (1 million IU) powder for solution for inhalation 1 pc. RUB 1,500 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!
