Colistinmethanesulfonic Acid

Colistinmethanesulfonic Acid Uses, Dosage, Side Effects, Food Interaction and all others data.

Each vial contains Colistinmethanesulfonic Acid Sodium 1 MIU or 34 mg Colistin.Each vial contains Colistinmethanesulfonic Acid Sodium 2 MIU or 68 mg Colistin.Each vial contains Colistinmethanesulfonic Acid Sodium 3 MIU or 102 mg Colistin.Each vial contains Colistinmethanesulfonic Acid Sodium 4.5 MIU or 150 mg Colistin.Colistinmethanesulfonic Acid sodium is a surface active agent which penetrates into and disrupts the bacterial cell membrane. It has been shown to have bactericidal activity against Aerobic gram-negative microorganisms e.g. Enterobacter aerogenes, E. coli, Klebsiella pneumoniae and PseudomonasColistinmethanesulfonic Acid is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistinmethanesulfonic Acid is polycationic and has both hydrophobic and lipophilic moieties. It interacts with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. There is also evidence that polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes.

Colistinmethanesulfonic Acid is a polymyxin antibiotic agent. Originally, colistimethate sodium was thought to be less toxic than polymyxin B; however, if the drugs are administered at comparable doses, their toxicities may be similar. Polymyxins are cationic polypeptides that disrupt the bacterial cell membrane through a detergentlike mechanism. With the development of less toxic agents, such as extended-spectrum penicillins and cephalosporins, parenteral polymyxin use was largely abandoned, except for the treatment of multidrug-resistant pulmonary infections in patients with cystic fibrosis. More recently, however, the emergence of multidrug-resistant gram-negative bacteria, such as Pseudomonas aeruginosa and Acinetobacter baumannii, and the lack of new antimicrobial agents have led to the revived use of the polymyxins.

Colistinmethanesulfonic Acid
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Colistinmethanesulfonic Acid
Availability	Prescription only
Generic	Colistimethate
Colistimethate Other Names	Colistin methanesulfonic acid, Colistin sulfomethate, Colistinmethanesulfonic acid
Related Drugs	penicillin g potassium, Pfizerpen, Coly Mycin M
Type
Formula	C₅₈H₁₀₅N₁₆O₂₈S₅
Weight	Average: 1634.87 Monoisotopic: 1633.588775306
Groups	Approved, Vet approved
Therapeutic Class	Other antibacterial preparation
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Colistinmethanesulfonic Acid is used for the treatment of acute or chronic infections caused by sensitive strains of certain gram-negative bacilli. It is particularly used for the infection caused by sensitive strains of Pseudomonas aeruginosa. Colistinmethanesulfonic Acid is not used for infections due to Proteus or Neisseria. Colistinmethanesulfonic Acid is very effective in the treatment of infections due to the following gram-negative organisms: Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa.

Colistinmethanesulfonic Acid is also used to associated treatment for these conditions: Bacterial Infections

How Colistinmethanesulfonic Acid works

Colistinmethanesulfonic Acid is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistinmethanesulfonic Acid is polycationic and has both hydrophobic and lipophilic moieties. It interacts with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. There is also evidence that polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes.

Dosage

Colistinmethanesulfonic Acid dosage

Maintenance dose: 9 MIU/day in 2-3 divided doses. In patients who are critically ill, a loading dose of 9 MIU should be administered.

Renal impairment patients: Dose adjustments in renal impairment patients are necessary. Dose reductions are recommended for patients with creatinine clearance < 50 ml/min. Twice daily dosing is recommended.

Creatinine clearance <50-30 ml/min: daily dose 5.5-7.5 MIU
Creatinine clearance <30-10 ml/min: daily dose 4.5-5.5 MIU
Creatinine clearance <10 ml/min: daily dose 3.5 MIU

Haemodialysis (HD) patients:

No-HD days: 2.25 MIU/day (2.2-2.3 MIU/day).
HD days: 3 MIU/day (Should be given after the HD session) Twice daily dosing is recommended.

Pediatric population: The dose should be based on lean body weight.

Children ≤40 kg: 75,000-150,000 IU/kg/day divided into 3 doses.
Children >40 kg: >150,000 IU/kg/day has been reported in children with cystic fibrosis.

Hepatic impairment patients: There are no data in patients with hepatic impairment. Caution is advised when administering colistimethate sodium in these patients.

Direct Intermittent Administration- Slowly inject one-half of the total daily dose over a period of 3 to 5 minutes every 12 hours.

Continuous Infusion- Slowly inject one-half of the total daily dose over 3 to 5 minutes. Add the remaining half of the total daily dose of Colistinmethanesulfonic Acid for injection to one of the following:

0.9% NaCl
5% dextrose in 0.9% NaCl
5% dextrose in water
5% dextrose in 0.45% NaCl
5% dextrose in 0.225% NaCl
Lactated Ringer's solution

There are not sufficient data to recommend usage of Colistinmethanesulfonic Acid for injection with other drugs or other than the above listed infusion solutions. Administer the second half of the total daily dose by slow intravenous infusion, starting 1 to 2 hours after the initial dose, over the next 22 to 23 hours. In the presence of impaired renal function, reduce the infusion rate depending on the degree of renal impairment. The choice of intravenous solution and the volume to be employed are dictated by the requirements of fluid and electrolyte management. Any infusion solution containing Colistinmethanesulfonic Acid sodium should be freshly prepared and used for no longer than 24 hours.

Alternative method- As per specialized references for intermittent infusion: Prescribed dose can be diluted in 50-100 ml 0.9% NaCl and administer over 30-60 minutes in IV route.

Side Effects

The following adverse reactions have been reported: gastrointestinal upset, tingling of extremities and tongue, slurred speech, dizziness, vertigo and paresthesia, generalized itching, urticaria and rash, fever, increased blood urea nitrogen (BUN), elevated creatinine and decreased creatinine clearance, respiratory distress and apnea, nephrotoxicity and decreased urine output.

Toxicity

Oral LD₅₀ in rats is 5450 mg/kg. Overdosage with colistimethate can cause neuromuscular blockade characterized by paresthesia, lethargy, confusion, dizziness, ataxia, nystagmus, disorders of speech and apnea. Respiratory muscle paralysis may lead to apnea, respiratory arrest and death.

Precaution

Colistinmethanesulfonic Acid should be used with caution in patient with impaired renal function. When actual renal impairment is present, Colistinmethanesulfonic Acid may be used, but the greatest caution should be exercised and the dosage should be reduced in proportion to the extent of the impairment. Colistinmethanesulfonic Acid should be used with caution in neonates, infants and children.

Interaction

Colistinmethanesulfonic Acid should not be given with certain antibiotics like- aminoglycosides and polymyxin due to report of interfere with the nerve transmission at the neuromuscular junction. It should not be given with muscle relaxants e.g., tubocurarine and other drugs including ether, succinylcholine, gallamine, decamethonium and sodium citrate. The concomitant use of Sodium Cephalothin and Colistinmethanesulfonic Acid should be avoided.

Food Interaction

No interactions found.

Colistinmethanesulfonic Acid Drug Interaction

Moderate: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprimUnknown: pancrelipase, pancrelipase, heparin, heparin, acetaminophen, acetaminophen, budesonide, budesonide, dornase alfa, dornase alfa, montelukast, montelukast, valproic acid, valproic acid, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Colistinmethanesulfonic Acid Disease Interaction

Major: colitisModerate: renal dysfunction

Elimination Route

Very poor absorption from gastrointestinal tract.

Half Life

2-3 hours following either intravenous or intramuscular administration in adults and in the pediatric population, including premature infants.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies about the use of Colistinmethanesulfonic Acid in pregnant women. Since colistimethate is transferred across the placental barrier in humans, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Colistinmethanesulfonic Acid is excreted in human breast milk. Therefore, caution should be exercised when administered to nursing women.

Contraindication

The use of Colistinmethanesulfonic Acid Sodium Parenteral is contraindicated for patients with a history of sensitivity to the drug or any of its components.

Acute Overdose

Overdosage with colistimethate sodium can cause neuromuscular blockade characterized by paresthesia, lethargy, confusion, dizziness, ataxia, nystagmus, disorders of speech and apnea. Respiratory muscle paralysis may lead to apnea, respiratory arrest and death. Overdosage with the drug can also cause acute renal failure, manifested as decreased urine output and increases in serum concentrations of B.U.N and creatinine. As in any case of overdose, Colistinmethanesulfonic Acid Sodium therapy should be discontinued and general supportive measures should be utilized.