Netilmicin

Netilmicin belongs to the pharmacological class of Aminoglycoside antibiotics.

Netilmicin has been approved to relieve symptoms and also for treating and maintaining Severe systemic infections, Respiratory tract infections, Urinary tract infections, and Eye infections.

Netilmicin exhibits rapid and complete absorption following intramuscular administration, leading to peak serum levels within 30-60 minutes. However, its oral absorption is limited, and topical absorption is generally inadequate unless there is significant skin damage. The precise volume of distribution for netilmicin is not available. Protein binding of netilmicin is low, and the degree of binding may vary depending on the test conditions, particularly the concentration of cations in the test medium. Netilmicin does not undergo metabolic transformation, and approximately 80% of the administered dose is excreted unchanged in the urine within 24 hours.

The common side effects involved in using Netilmicin are Nausea, Vomiting, Diarrhea, Abdominal cramps or discomfort, Loss of appetite, Skin rash or irritation, and Itching.

Netilmicin is available in the form of Injectables.

Netilmicin is approved in Germany, Japan, Malaysia, India, the U.K., the U.S., and China.

Netilmicin belongs to the pharmacological class of Aminoglycoside antibiotics.

Aminoglycosides, including netilmicin, bind irreversibly to specific proteins of the 30S subunit and 16S rRNA, leading to significant effects. Netilmicin specifically binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This binding interferes with the decoding site near nucleotide 1400 in the 16S rRNA of the 30S subunit, and this particular region interacts with the wobble base in the anticodon of tRNA. Consequently, this interference disrupts the initiation complex, causing a misreading of mRNA. As a result, incorrect amino acids are inserted into the polypeptide chain, leading to the synthesis of nonfunctional or toxic peptides. Moreover, this disruption also causes the breakdown of polysomes into nonfunctional monosomes. Ultimately, these actions hinder the bacterium's ability to synthesize essential proteins necessary for its growth.

Netilmicin has been approved to relieve symptoms and also for treating and maintaining Severe systemic infections, Respiratory tract infections, Urinary tract infections, and Eye infections.

Netilmicin is found to be available in the form of Injectables.

Netilmicin can be used in the following treatment:

● Severe systemic infections

● Respiratory tract infections

● Urinary tract infections

● Eye infections

Netilmicin can help to relieve symptoms and also for the treatment and maintenance of Severe systemic infections, Respiratory tract infections, Urinary tract infections, and Eye infections.

Netilmicin is approved for use in the following clinical indications:

● Severe systemic infections

● Respiratory tract infections

● Urinary tract infections

● Eye Infections

● Severe systemic infections: For severe systemic infections such as sepsis or bacteremia, the typical adult dose of netilmicin is 4-6 mg/kg per day divided into two or three equal doses. The total daily dose should be at most 7.5 mg/kg.

● Respiratory tract infections: In the case of respiratory tract infections, including pneumonia and bronchitis, the recommended adult dose of netilmicin is usually 4-6 mg/kg per day divided into two or three equal doses. The total daily dose should be at most 7.5 mg/kg.

● Urinary tract infections: For urinary tract infections, including complicated infections and pyelonephritis, the typical adult dose of netilmicin is 4-6 mg/kg per day divided into two or three equal doses. The total daily dose should be at most 7.5 mg/kg.

Dosage Adjustments in Kidney Patients:

For patients with a creatinine clearance (CrCl) of 20 to 40 mL/min, the recommended frequency of the usual dose is once every 24 hours.

For patients with a CrCl of 40 to 60 mL/min, the recommended frequency of the usual dose is once every 12 hours.

Dosage Adjustments in Hepatic Impairment Patients:

No dosage adjustments are needed for hepatic impairment.

Dosage Adjustments in Pediatric Patients:

● No specific information is available

Injectables: 50 mg, 100 mg, 200 mg, and 300 mg.

Injectables

There are no specific dietary restrictions related to the use of Netilmicin. However, it is generally recommended to follow a balanced and healthy diet while undergoing treatment with any medication, including Netilmicin. Eating a nutritious diet can support overall health and aid in the recovery process.

It is important to maintain adequate hydration during treatment with Netilmicin and in general. Drinking an adequate amount of water and fluids can help support kidney function and prevent dehydration.

Netilmicin may be contraindicated under the following conditions:

Patients with a known allergy to Netilmicin or any of its components should avoid using Netilmicin Sulfate Injection USP. Additionally, suppose a patient has a history of hypersensitivity or serious toxic reactions to aminoglycosides. In that case, it may also be contraindicated to use any other aminoglycoside due to the possibility of cross-sensitivities that can occur within this class of drugs.

No specific information is available 

There is no specific alcohol warning for Netilmicin. However, it is generally advisable to avoid consuming alcohol while undergoing treatment with any medication, including Netilmicin. Alcohol can have various effects on the body and may interact with medications, potentially leading to adverse reactions or reducing the effectiveness of the treatment.

Additionally, alcohol can strain the liver and kidneys, which are organs involved in the elimination of medications from the body. Since Netilmicin can have potential side effects on these organs, alcohol consumption may exacerbate these effects.

Netilmicin is excreted in small amounts in human milk. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue breastfeeding or to discontinue netilmicin therapy, taking into account the importance of the drug to the mother.

Pregnancy Category D:

Netilmicin should be used during pregnancy only if clearly needed and when the potential benefits outweigh the risks. Limited data is available on the use of netilmicin in pregnant women, and its safety for the developing fetus has not been fully established. It is important to weigh the potential risks to the fetus against the benefits of treatment.

There are no specific food warnings related to the use of Netilmicin. However, it is generally recommended to follow a balanced and healthy diet while undergoing treatment with any medication, including Netilmicin. Eating a nutritious diet can support overall health and aid in the recovery process.

The adverse reactions related to Netilmicin can be categorized as follows:

Common :

● Nausea

● Vomiting

● Diarrhea

● Stomach pain

● Headache

● Dizziness

● Rash or itching

● Injection site reactions (e.g., redness, swelling, pain)

Less Common :

● Allergic reactions (e.g., hives, itching, swelling)

● Fever

● Changes in kidney function

● High or low blood pressure

● Abnormal liver function tests

● Abnormal blood cell counts

Rare :

● Hearing loss or ringing in the ears (ototoxicity)

● Balance problems or dizziness (vestibular toxicity)

● Severe allergic reactions (e.g., anaphylaxis)

● Neurological symptoms (e.g., seizures, confusion)

● Increased risk of infection (due to suppression of normal bacterial flora)

● Changes in blood sugar levels

● Blood disorders (e.g., thrombocytopenia, leukopenia)

The clinically relevant drug interactions of Netilmicin are briefly summarized here:

1. Loop Diuretics: Concurrent use of loop diuretics (e.g., furosemide) with netilmicin may increase the risk of nephrotoxicity.

2. Other Nephrotoxic Drugs: Concurrent use of other nephrotoxic drugs, such as vancomycin or amphotericin B, may increase the risk of kidney damage when used with netilmicin.

3. Neuromuscular Blocking Agents: Netilmicin may enhance the effects of neuromuscular blocking agents, such as tubocurarine, leading to increased muscle relaxation and respiratory paralysis.

4. Neuromuscular Blockade Antagonists: The concurrent use of netilmicin with agents that reverse neuromuscular blockade, such as calcium salts, may reduce the efficacy of these reversal agents.

5. Interactions with Other Antibiotics: Concurrent use of other antibiotics, especially those with similar mechanisms of action, may increase the risk of toxicity or reduce the effectiveness of netilmicin.

The following are the side effects involving Netilmicin:

● Kidney toxicity

● Hearing loss

● Balance issues

● Nausea/vomiting

● Diarrhea

● Allergic reactions

● Neurotoxicity

● Injection site reactions

Pregnancy:

Pregnancy Category D:

Netilmicin should be used during pregnancy only if clearly needed and when the potential benefits outweigh the risks. Limited data is available on the use of netilmicin in pregnant women, and its safety for the developing fetus has not been fully established. It is important to weigh the potential risks to the fetus against the benefits of treatment.

Lactation:

Netilmicin is excreted in small amounts in human milk. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue breastfeeding or to discontinue netilmicin therapy, taking into account the importance of the drug to the mother.

Pediatric Use:

Netilmicin can be used in pediatric patients, but dosage adjustments may be necessary based on the child's age, weight, and renal function. Close monitoring of renal function and serum drug levels is important to ensure appropriate dosing and minimize the risk of toxicity.

Geriatric Use:

Elderly patients may be more susceptible to the toxic effects of netilmicin due to age-related changes in kidney function. Renal function should be closely monitored, and dosage adjustments may be required based on the individual's renal clearance. Additionally, elderly patients may have underlying conditions or be on other medications that could interact with netilmicin, so careful assessment of the overall health status is essential.

Physicians should be knowledgeable as well as vigilant about the treatment and identification of overdosage of Netilmicin.

1. In cases of overdose with netilmicin, the immediate discontinuation of the medication is recommended. As with other aminoglycoside antibiotics, the potential toxic effects of netilmicin include ototoxicity (hearing loss, tinnitus) and nephrotoxicity (kidney damage). Therefore, close monitoring of renal function and auditory status is crucial.

2. In the event of an overdose, supportive measures should be undertaken, including the maintenance of adequate hydration and diuresis to facilitate the elimination of netilmicin from the body. Hemodialysis or peritoneal dialysis may be considered to remove netilmicin, especially in cases of severe toxicity or impaired renal function.

3. There is no specific antidote for netilmicin overdose. However, symptomatic treatment can be administered as necessary to manage any complications or adverse effects that may arise.

Pharmacodynamics

Netilmicin, a water-soluble antibiotic belonging to the aminoglycoside group, is a semisynthetic compound derived from the fermentation of Micromonospora inyoensis, an actinomycete species. Aminoglycosides are primarily effective against aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. Netilmicin exhibits potent activity at low concentrations against a broad spectrum of pathogenic bacteria, including Escherichia coli, Klebsiella-Enterobacter-Serratia group bacteria, Citrobacter species, both indole-positive and indole-negative Proteus species (including Proteus mirabilis, P. morganii, P. regret, P. vulgaris), Pseudomonas aeruginosa, and Neisseria gonorrhoea. In addition, netilmicin demonstrates in vitro activity against Hemophilus influenzae, Salmonella species, Shigella species, and both penicillinase and non-penicillinase-producing strains of Staphylococcus, including methicillin-resistant strains. Certain strains of Providencia, Acinetobacter, and Aeromonas species also exhibit sensitivity to netilmicin.

Pharmacokinetics

Absorption

Netilmicin is rapidly and completely absorbed after intramuscular (IM) administration, with peak serum levels achieved within 30-60 minutes. However, oral absorption of netilmicin is poor. Topical absorption is also limited unless there is significant skin damage.

Volume of distribution

The exact volume of distribution for netilmicin is not available.

Protein binding

Netilmicin has low protein binding, and the extent of binding may vary depending on the test conditions, particularly the concentration of cations in the test medium.

Metabolism

There is no evidence of metabolic transformation of netilmicin. Typically, around 80% of the administered dose is excreted unchanged in the urine within 24 hours.

Route of elimination

Specific information regarding the route of elimination for netilmicin is not available.

1) https://go.drugbank.com/drugs/DB00955

2) https://www.drugs.com/dosage/netilmicin.html

3)https://www.hopkinsguides.com/hopkins/view/Johns_Hopkins_ABX_Guide/540382/all/Netilmicin