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Netilmicin (1-N-ethylsisomicin) is a semisynthetic aminoglycoside
antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of ...
, and a derivative of
sisomicin Sisomicin (bactoCeaze, ensamycin, and initially antibiotic 6640 and rickamicin), is an aminoglycoside antibiotic, isolated from the fermentation broth of '' Micromonospora inositola''. It is a newer broad-spectrum aminoglycoside most structurally ...
, produced by ''
Micromonospora inyoensis ''Micromonospora'' is a genus of bacteria of the family Micromonosporaceae. They are gram-positive, spore-forming, generally aerobic, and form a branched mycelium; they occur as saprotrophic forms in soil and water. Various species are sources o ...
''. Aminoglycoside antibiotics have the ability to kill a wide variety of bacteria. Netilmicin is not absorbed from the gut and is therefore only given by injection or infusion. It is only used in the treatment of serious infections particularly those resistant to
gentamicin Gentamicin is an antibiotic used to treat several types of bacterial infections. This may include bone infections, endocarditis, pelvic inflammatory disease, meningitis, pneumonia, urinary tract infections, and sepsis among others. It is not e ...
. It was patented in 1973 and approved for medical use in 1981. It was approved for medical use in the UK in December 2019, for the treatment of external infections of the eye. It is on the World Health Organization's List of Essential Medicines.


Comparison with drugs

According to the British National Formulary (BNF), netilmicin has similar activity to gentamicin, but less ototoxicity in those needing treatment for longer than 10 days. Netilmicin is active against a number of gentamicin-resistant Gram-negative bacteria but is less active against '' Pseudomonas aeruginosa than gentamicin or tobramycin. However, according to the below-mentioned studies, the above advantages are controversial: *''Netilmicin (Netromycin, Schering-Plough, Netspan- Cipla)'':
In summary, netilmicin has not been demonstrated to have significant advantages over other aminoglycosides (gentamicin, tobramycin, amikacin), and it is more expensive; thus, its potential value is limited. ''Drug Intelligence & Clinical Pharmacy: Vol. 17, No. 2, pp. 83-91''. *''Once-daily gentamicin versus once-daily netilmicin in patients with serious infections—a randomized clinical trial'':
We conclude that with once-daily dosing no benefit of netilmicin over gentamicin regarding nephro- or ototoxicity could be demonstrated. ''
Journal of Antimicrobial Chemotherapy The ''Journal of Antimicrobial Chemotherapy'' is a peer-reviewed medical journal which covers antimicrobial chemotherapy, including laboratory aspects and clinical use of antimicrobial agents. It is published by Oxford University Press on behalf o ...
(1994) 33, 823-835''. *''Ototoxicity and nephrotoxicity of gentamicin vs netilmicin in patients with serious infections. A randomized clinical trial'':
We conclude that with once-daily treatment no benefit of netilmicin over gentamicin regarding nephro- or ototoxicity could be demonstrated. ''Clin Otolaryngol Allied Sci. 1995 Apr;20(2):118-23''. *''Relative
efficacy Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as ''effectiveness'', and it has often been used synonymously, although in pharmacology a pragmatic clinical trial#Efficacy versu ...
and toxicity of netilmicin and tobramycin in oncology patients'':
We conclude that aminoglycoside-associated ototoxicity was less severe and more often reversible with netilmicin than with tobramycin. ''Arch Intern Med. 1986 Dec;146(12):2329-34''. *''Daily single-dose aminoglycoside administration. Therapeutic and economic benefits'':
Animal studies have shown that dosing aminoglycosides once daily is more efficient and less nephrotoxic than the conventional multiple daily dosing regimens. Netilmicin and amikacin are the drugs most often used in clinical trials of once-daily dosing regimens. ''Ugeskrift for Lægerer. 1993 May 10;155(19):1436-41''. *''Comparison of Netilmicin with Gentamicin in the Therapy of Experimental Escherichia coli
Meningitis Meningitis is acute or chronic inflammation of the protective membranes covering the brain and spinal cord, collectively called the meninges. The most common symptoms are fever, headache, and neck stiffness. Other symptoms include confusion or ...
'':
Because of its reduced toxicity and greater in vivo
bactericidal A bactericide or bacteriocide, sometimes abbreviated Bcidal, is a substance which kills bacteria. Bactericides are disinfectants, antiseptics, or antibiotics. However, material surfaces can also have bactericidal properties based solely on their ...
activity, netilmicin may offer an advantage over gentamicin in the therapy of gram-negative bacillary meningitis. ''Antimicrob Agents Chemother. 1978 June; 13(6): 899-904''. *''A comparison of netilmicin and gentamicin in the treatment of pelvic infections'':
The microbacteria isolated by standard culture techniques before therapy revealed
Neisseria gonorrhoeae ''Neisseria gonorrhoeae'', also known as ''gonococcus'' (singular), or ''gonococci'' (plural), is a species of Gram-negative diplococci bacteria isolated by Albert Ludwig Sigesmund Neisser, Albert Neisser in 1879. It causes the sexually transmit ...
in 69% and 51% of the netilmicin and gentamicin groups, respectively;
anaerobic organism An anaerobic organism or anaerobe is any organism that does not require molecular oxygen for growth. It may react negatively or even die if free oxygen is present. In contrast, an aerobic organism (aerobe) is an organism that requires an oxygenate ...
s were cultured in about 75% of each group. ''Obstetrics & Gynecology 1979;54:554-557''. *''Netilmicin: a review of toxicity in laboratory animals'':
Presently available data suggest that netilmicin offers distinct advantages over older aminoglycosides. Final conclusions must await prospective randomized double-blind trials in man. ''J Int Med Res. 1978;6(4):286-99''. *''Nonparallel nephrotoxicity dose-response curves of aminoglycosides'':
Nephrotoxicity comparisons of aminoglycosides in rats, utilizing large multiples of human doses, have indicated an advantage for netilmicin. However, no nephrotoxicity advantage of netilmicin has been demonstrated at the lower doses used in clinics. ''Antimicrob Agents Chemother. 1981 June; 19(6): 1024–1028''. *''Comparative ototoxicity of netilmicin, gentamicin, and tobramycin in cats'':
Under the conditions of this study, at least a twofold (vestibular) to fourfold (cochlear) relative safety margin for ototoxicity was established in favor of netilmicin over tobramycin and gentamicin. ''Toxicol Appl Pharmacol. 1985 Mar 15;77(3):479-89''. *''Comparison of Netilmicin and Gentamicin
Pharmacokinetics Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered ...
in Humans'':
In a crossover study, single doses of netilmicin and gentamicin were administered
intramuscularly Intramuscular injection, often abbreviated IM, is the injection of a substance into a muscle. In medicine, it is one of several methods for parenteral administration of medications. Intramuscular injection may be preferred because muscles have ...
, each at 1.0 and 2.5 mg/kg. No significant differences were observed between the two drugs in disposition half-life, rate of distribution and elimination, area under the serum concentration-time curve, urinary excretion, total body clearance, and
renal clearance In pharmacology, clearance is a pharmacokinetic measurement of the volume of plasma from which a substance is completely removed per unit time. Usually, clearance is measured in L/h or mL/min. The quantity reflects the rate of drug elimination d ...
. ''Antimicrobial Agents and Chemotherapy, Feb. 1980, p. 184-187. Schering-Plough Research Division, Bloomfield, New Jersey 07003''.


References

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External links

* {{Portal bar , Medicine Aminoglycoside antibiotics Micromonosporaceae