Netilmicin
Encyclopedia
Netilmicin is a member of the aminoglycoside
Aminoglycoside
An aminoglycoside is a molecule or a portion of a molecule composed of amino-modifiedsugars.Several aminoglycosides function as antibiotics that are effective against certain types of bacteria...

 family of antibiotic
Antibiotic
An antibacterial is a compound or substance that kills or slows down the growth of bacteria.The term is often used synonymously with the term antibiotic; today, however, with increased knowledge of the causative agents of various infectious diseases, antibiotic has come to denote a broader range of...

s. These antibiotics have the ability to kill a wide variety of bacteria
Bacteria
Bacteria are a large domain of prokaryotic microorganisms. Typically a few micrometres in length, bacteria have a wide range of shapes, ranging from spheres to rods and spirals...

. Netilmicin is not absorbed from the gut
Gastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....

 and is therefore only given by injection or infusion. It is only used in the treatment of serious infection
Infection
An infection is the colonization of a host organism by parasite species. Infecting parasites seek to use the host's resources to reproduce, often resulting in disease...

s particularly those resistant to gentamicin
Gentamicin
Gentamicin is an aminoglycoside antibiotic, used to treat many types of bacterial infections, particularly those caused by Gram-negative organisms. However, gentamicin is not used for Neisseria gonorrhoeae, Neisseria meningitidis or Legionella pneumophila...

.

Available dosage forms

Available dosage forms include:
  • UK: netilmicin (as Sulphate):
    • 10 mg/mL (1.5 mL amp)
    • 50 mg/mL (1-mL amp)
    • 100 mg/mL(1-mL,1.5-mL & 2-mL amp)
  • France
    France
    The French Republic , The French Republic , The French Republic , (commonly known as France , is a unitary semi-presidential republic in Western Europe with several overseas territories and islands located on other continents and in the Indian, Pacific, and Atlantic oceans. Metropolitan France...

    : Nétilmicin sulfate:
    • Amp 25 mg/1 mL
    • 50 mg/2 mL
    • 100 mg/1 mL
    • 150 mg/1.5 mL

Ingredients for 100 mg/mL vial

Netilmicin (as sulphate
Sulfate
In inorganic chemistry, a sulfate is a salt of sulfuric acid.-Chemical properties:...

)
100 mg
Sodium metabisulfite
Sodium metabisulfite
Sodium metabisulfite or sodium pyrosulfite is an inorganic compound of chemical formula Na2S2O5. The substance is sometimes referred to as disodium...

2.4 mg
Sodium sulfite
Sodium sulfite
Sodium sulfite is a soluble sodium salt of sulfurous acid. It is a product of sulfur dioxide scrubbing, a part of the flue gas desulfurization process...

0.8 mg
Edetate disodium
EDTA
Ethylenediaminetetraacetic acid, widely abbreviated as EDTA , is a polyamino carboxylic acid and a colourless, water-soluble solid. Its conjugate base is named ethylenediaminetetraacetate. It is widely used to dissolve limescale. Its usefulness arises because of its role as a hexadentate ligand...

0.1 mg
Benzyl alcohol
Benzyl alcohol
Benzyl alcohol is an organic compound with the formula C6H5CH2OH. The benzyl group is often abbreviated "Bn", thus benzyl alcohol is denoted as BnOH. Benzyl alcohol is a colorless liquid with a mild pleasant aromatic odor. It is a useful solvent due to its polarity, low toxicity, and low vapor...

10 mg
Water for injection qs 1 mL

FDA approval date : February 28, 1983

Comparison with drugs of the same therapeutic category

According to the British National Formulary
British National Formulary
The British National Formulary is a medical and pharmaceutical reference book that contains a wide spectrum of information and advice on prescribing and pharmacology, along with specific facts and details about all medicines available on the National Health Service , including indication,...

 (BNF), netilmicin has similar activity to gentamicin, but less ototoxicity
Ototoxicity
Ototoxicity is damage to the ear , specifically the cochlea or auditory nerve and sometimes the vestibular system, by a toxin. It is commonly medication-induced; ototoxic drugs include antibiotics such as the aminoglycoside gentamicin, loop diuretics such as furosemide, and platinum-based...

 in those needing treatment for longer than 10 days.Netilmicin is active against a number of gentamicin-resistant Gram-negative bacilli but is less active against Ps. Aeuroginosa than gentamicin or tobramycin.

However according to the below-mentioned studies, the above advantages are somehow controversial:
  • Netilmicin (Netromycin, Schering-Plough, Netspan- Cipla):
    In summary, netilmicin has not been demonstrated to have significant advantages over other aminoglycosides (gentamicin, tobramycin, amikacin
    Amikacin
    Amikacin is an aminoglycoside antibiotic used to treat different types of bacterial infections. Amikacin works by binding to the bacterial 30S ribosomal subunit, causing misreading of mRNA and leaving the bacterium unable to synthesize proteins vital to its growth.-Administration:Amikacin may be...

    ), 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 (1994) 33, 823-835.

  • Ototoxicity and nephrotoxicity
    Nephrotoxicity
    Nephrotoxicity is a poisonous effect of some substances, both toxic chemicals and medication, on the kidneys. There are various forms of toxicity. Nephrotoxicity should not be confused with the fact that some medications have a predominantly renal excretion and need their dose adjusted for the...

     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
    Efficacy is the capacity to produce an effect. It has different specific meanings in different fields. In medicine, it is the ability of an intervention or drug to reproduce a desired effect in expert hands and under ideal circumstances.- Healthcare :...

     and toxicity
    Toxicity
    Toxicity is the degree to which a substance can damage a living or non-living organisms. Toxicity can refer to the effect on a whole organism, such as an animal, bacterium, or plant, as well as the effect on a substructure of the organism, such as a cell or an organ , such as the liver...

     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
    Animal testing
    Animal testing, also known as animal experimentation, animal research, and in vivo testing, is the use of non-human animals in experiments. Worldwide it is estimated that the number of vertebrate animals—from zebrafish to non-human primates—ranges from the tens of millions to more than 100 million...

     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. Ugeskr Laeger. 1993 May 10;155(19):1436-41.

  • Comparison of Netilmicin with Gentamicin in the Therapy of Experimental Escherichia coli
    Escherichia coli
    Escherichia coli is a Gram-negative, rod-shaped bacterium that is commonly found in the lower intestine of warm-blooded organisms . Most E. coli strains are harmless, but some serotypes can cause serious food poisoning in humans, and are occasionally responsible for product recalls...

     Meningitis
    Meningitis
    Meningitis is inflammation of the protective membranes covering the brain and spinal cord, known collectively as the meninges. The inflammation may be caused by infection with viruses, bacteria, or other microorganisms, and less commonly by certain drugs...

    :
    Because of its reduced toxicity and greater in vivo
    In vivo
    In vivo is experimentation using a whole, living organism as opposed to a partial or dead organism, or an in vitro controlled environment. Animal testing and clinical trials are two forms of in vivo research...

     bactericidal 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
    Sexually transmitted disease
    Sexually transmitted disease , also known as a sexually transmitted infection or venereal disease , is an illness that has a significant probability of transmission between humans by means of human sexual behavior, including vaginal intercourse, oral sex, and anal sex...

    :
    The microbacteria isolated by standard culture techniques
    Microbiological culture
    A microbiological culture, or microbial culture, is a method of multiplying microbial organisms by letting them reproduce in predetermined culture media under controlled laboratory conditions. Microbial cultures are used to determine the type of organism, its abundance in the sample being tested,...

     before therapy revealed Neisseria gonorrhoeae
    Neisseria gonorrhoeae
    Neisseria gonorrhoeae, also known as gonococci , or gonococcus , is a species of Gram-negative coffee bean-shaped diplococci bacteria responsible for the sexually transmitted infection gonorrhea.N...

     in 69% and 51% of the netilmicin and gentamicin groups, respectively; anaerobic organism
    Anaerobic organism
    An anaerobic organism or anaerobe is any organism that does not require oxygen for growth. It could possibly react negatively and may even die if oxygen is present...

    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
    Dose-response relationship
    The dose-response relationship, or exposure-response relationship, describes the change in effect on an organism caused by differing levels of exposure to a stressor after a certain exposure time...

     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
    Pharmacokinetics, sometimes abbreviated as PK, is a branch of pharmacology dedicated to the determination of the fate of substances administered externally to a living organism...

     in Humans
    :
    In a crossover study
    Crossover study
    A crossover study is a longitudinal study in which subjects receive a sequence of different treatments . While crossover studies can be observational studies, many important crossover studies are controlled experiments, which are discussed in this article...

    , single doses of netilmicin and gentamicin were administered intramuscularly
    Intramuscular injection
    Intramuscular injection is the injection of a substance directly into a muscle. In medicine, it is one of several alternative methods for the administration of medications . It is used for particular forms of medication that are administered in small amounts...

    , 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
    Clearance (medicine)
    In medicine, the clearance is a measurement of the renal excretion ability. Although clearance may also involve other organs than the kidney, it is almost synonymous with renal clearance or renal plasma clearance. Each substance has a specific clearance that depends on its filtration characteristics...

    . ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, Feb. 1980, p. 184-187. Schering-Plough Research Division, Bloomfield, New Jersey 07003.
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