netilmicin

Action and Spectrum

Actions and spectrum: 

Action: 

• Bactericidal: netilmicin is a bactericidal antibiotic, meaning it kills bacteria rather than just inhibiting their growth. 
• Protein Synthesis Inhibition: netilmicin works by inhibiting protein synthesis in bacteria. It binds to the bacterial ribosome, specifically the 30S subunit, disrupting the reading of the genetic code and preventing the production of essential proteins. This disruption leads to bacterial cell death. 

Spectrum: netilmicin has a broad spectrum of activity against bacteria, both Gram-positive and Gram-negative. Its effectiveness may vary based on the specific bacterial strains and local resistance patterns. It is used to treat bacterial infections that are resistant to other classes of antibiotics. netilmicin has limited activity against some Gram-positive bacteria, such as Staphylococcus aureus, but its main strength lies in treating Gram-negative infections. netilmicin is most effective against aerobic bacteria, which require oxygen to grow and thrive. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Headache 

visual disturbances 

tachycardia 

palpitations 

paraesthesia 

Chills 

fluid retention 

diarrhea 

increased alkaline phosphatase 

anaemia 

malaise 

disorientation 

Hypotension 

thrombocytosis 

rash 

fever 

vomiting 

Increased blood sugar 

increased liver enzymes 

decreased haemoglobin 

increased prothrombin time 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with netilmicin 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: netilmicin should not be used in individuals with known hypersensitivity or allergic reactions to netilmicin or any other aminoglycoside antibiotics. 
• Pre-existing Hearing or Balance Issues: Individuals with pre-existing hearing impairment or balance disturbances might be at an increased risk of experiencing worsened auditory or vestibular symptoms when using netilmicin. 
• Pregnancy: netilmicin is avoided during pregnancy unless the potential benefits outweigh the risks. There is a potential for harm to the developing fetus. 
• Breastfeeding: netilmicin can be excreted in breast milk, and its use during breastfeeding should be approached with caution.  
• Renal Impairment: netilmicin is primarily excreted through the kidneys, so individuals with severe renal impairment might require dosage adjustments or alternative treatments to prevent potential toxicity.

Caution: 

• Nephrotoxicity: Aminoglycosides, including netilmicin, can be nephrotoxic, meaning they have the potential to cause kidney damage. This risk is higher when these antibiotics are used at high doses or for extended periods. Patients with pre-existing kidney conditions or those who are receiving other nephrotoxic medications might require careful monitoring of kidney function. 
• Ototoxicity: One of the most significant concerns with aminoglycosides is their potential to cause ototoxicity, which is damage to the auditory and vestibular (balance-related) systems. This can lead to hearing loss or balance disturbances. The risk is higher with prolonged or high-dose use. Patients with pre-existing auditory or vestibular issues are at greater risk. 
• Neuromuscular Disorders: Patients with neuromuscular disorders, such as myasthenia gravis, should be cautious when using netilmicin, as these conditions can increase sensitivity to the neuromuscular effects of aminoglycosides.

Comorbidities: 

• Kidney Dysfunction: netilmicin is primarily eliminated through the kidneys, and individuals with pre-existing kidney dysfunction are at an increased risk of experiencing kidney damage due to the potential nephrotoxicity of aminoglycoside antibiotics. Dosing adjustments might be necessary to prevent further kidney impairment. 
• Hearing Impairment: Patients with existing hearing impairment might be at an increased risk of worsening hearing loss when using netilmicin, as aminoglycosides are known to have ototoxic effects. 
• Balance Disorders: Individuals with balance disorders or vestibular issues should be cautious when using netilmicin due to the risk of balance disturbances caused by ototoxicity. 
• Pre-existing Infections: If the patient has other infections or illnesses that might interact with or exacerbate the primary infection being treated with netilmicin, the healthcare provider should carefully assess the overall health status. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: D 

Lactation: excreted into breast milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

netilmicin is an antibiotic belonging to the aminoglycoside class. netilmicin’s primary mechanism of action is inhibition of bacterial protein synthesis. It binds irreversibly to 30S ribosomal subunit in the bacterial cell, disrupting the reading of genetic code and leading to the misreading of mRNA. This interference prevents the proper assembly of protein chains, causing bacterial cell death. Its effectiveness varies depending on the specific bacterial strain and local resistance patterns. It is commonly used for infections caused by bacteria that are resistant to other antibiotics.  

Pharmacodynamics: 

• Bactericidal Activity: netilmicin is bactericidal, meaning it kills bacteria rather than just inhibiting their growth. Its mode of action disrupts vital bacterial processes, making it effective against a wide range of bacterial infections. 
• Post-Antibiotic Effect: A notable feature of aminoglycosides, including netilmicin, is the “post-antibiotic effect.” This effect refers to the continued suppression of bacterial growth even after the antibiotic concentration falls below the minimum inhibitory concentration for a brief period. This property contributes to the effectiveness of intermittent dosing regimens. 
• Concentration-Dependent Killing: Aminoglycosides exhibit concentration-dependent killing, which means that higher drug concentrations lead to more rapid and effective bacterial killing. This property often guides dosing strategies where higher peak concentrations are achieved through once-daily or multiple-daily dosing regimens. 
• Synergy with Other Antibiotics: netilmicin can exhibit synergistic effects when used in combination with other antibiotics. For example, it is sometimes used in combination with beta-lactam antibiotics to enhance the bacterial killing effect.

Pharmacokinetics: 

Absorption 

netilmicin is not well absorbed through the gastrointestinal tract when taken orally. Therefore, it is typically administered via intravenous (IV) or intramuscular (IM) routes to achieve therapeutic concentrations in the bloodstream. 

Distribution 

After administration, netilmicin distributes throughout the body. It can reach various tissues, extracellular fluids, and body fluids. However, its distribution into certain compartments, such as the central nervous system, is limited due to its hydrophilic nature and the presence of barriers that restrict its passage. 

Metabolism 

netilmicin is not extensively metabolized in the body. It remains unchanged in its active form. The lack of significant metabolism contributes to its potency and stability in the body. 

Elimination and excretion 

netilmicin is primarily excreted by the kidneys. The majority of the drug is eliminated from the body unchanged via glomerular filtration. This renal excretion is a significant factor in determining dosage adjustments in patients with impaired kidney function. 

Adminstartion

Administration: 

• Preparation: netilmicin is usually supplied as a sterile solution for IV/IM infusion. The medication might be available in vials or pre-filled syringes. 
• Dilution: The solution needs to be diluted according to the manufacturer’s instructions before administration. It is typically diluted in an appropriate volume of compatible IV/IM solution (e.g., normal saline). 
• Infusion: The diluted solution is then administered as a slow IV/IM infusion over a specific duration, often around 30 to 60 minutes. The infusion rate depends on the total dose and the recommended infusion time. 
• Monitoring: During IV/IM infusion, patients are closely monitored for any signs of adverse reactions or infusion-related complications. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: netilmicin 

Pronounced: (neh-TIL-mi-sin) 

Why do we use netilmicin? 

• Gram-Negative Infections: netilmicin is particularly effective against a range of Gram-negative bacteria. It is used to treat infections caused by organisms such as Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Enterobacter species. 
• Respiratory Tract Infections: netilmicin can be used to treat respiratory tract infections, including those affecting the lungs (pneumonia) or sinuses (sinusitis), caused by susceptible bacteria. 
• Urinary Tract Infections: netilmicin is used in the treatment of Gram-negative bacteria, especially when other antibiotics might not be effective due to resistance patterns. 
• Intra-abdominal Infections: It can be used to treat intra-abdominal infections caused by susceptible organisms. 
• Skin and Soft Tissue Infections: netilmicin might be used in cases of skin and soft tissue infections caused by susceptible bacteria.