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Amikacin, sold under the brandname Amikin, 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.

Amikacin was initially sold in 1976.^[1] It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.^[2]

Medical uses

Amikacin is most often used for treating severe, hospital-acquired infections with multidrug-resistant Gram-negative bacteria such as Pseudomonas aeruginosa, Acinetobacter, and Enterobacter. Serratia marcescens and Providencia stuartii are also included in the spectrum. Amikacin can also be used to treat non-tubercular mycobacterial infections and tuberculosis (if caused by sensitive strains) when first-line drugs fail to control the infection.

Amikacin may be combined with a beta-lactam antibiotic for empiric therapy for people with neutropenia and fever.

Liposomal amikacin for inhalation is currently in late stage clinical trials for the treatment of respiratory diseases, such as cystic fibrosis,^[3] Pseudomonas aeruginosa,^[4] non-tubercular mycobacterial infections^[5] and bronchiectasis.^[6]^[7]

Bacterial susceptibility data

Amikacin is usually used as a last-resort medication against multidrug-resistant bacteria. The following represents susceptibility data on a few medically significant microorganisms.

Pseudomonas aeruginosa - 0.5 μg/mL - 32 μg/mL
Pseudomonas aeruginosa (aminoglycoside-resistant) - 32 μg/mL - 64 μg/mL
Serratia marcescens - ≤0.25 μg/mL - 8 μg/mL
Serratia marcescens (multidrug-resistant) - 32 μg/mL

^[8]

Adverse effects

Side-effects of amikacin are similar to those of other aminoglycosides. Kidney damage and hearing loss are the most important effects. Because of this potential, blood levels of the drug and markers of kidney function (creatinine) may be monitored. Moreover, doses are adjusted specifically based upon serum Creatinine clearance in clinical settings.^{[citation needed]}

Administration

Amikacin may be administered once or twice a day but must be given by the intravenous or intramuscular route or via nebulization. There is no oral form available as amikacin is not absorbed orally. In people with kidney failure, dosage must be adjusted according to the creatinine clearance, usually by reducing the dosing frequency.

Resistance

Amikacin evades attacks by most of the antibiotic-inactivating enzymes that are responsible for antibiotic resistance in bacteria. This is accomplished by the L-hydroxyaminobuteroyl amide (L-HABA) moiety attached to N-1 (compare to kanamycin), which inhibits acetylation, phosphorylation, and adenylation in the distant amino sugar ring (C-2,C-3,C-4). To prevent the development of bacterial resistance to this antibiotic, its use is tightly regulated.

References

^ Oxford Handbook of Infectious Diseases and Microbiology. OUP Oxford. 2009. p. 56. ISBN 9780191039621.
^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ "Randomized, open-label, active-controlled, multicenter study to assess the efficacy, safety and tolerability of Arikace™ in Cystic Fibrosis patients with chronic infection due to Pseudomonas aeruginosa" is a European Phase III clinical trial, being conducted across multiple sites in the EU, starting at the Royal Brompton Hospital, Department of Respiratory Medicine, in London. https://www.clinicaltrialsregister.eu/ctr-search/trial/2011-000441-20/GB
^ http://www.clinicaltrials.gov/ct2/show/NCT01315678
^ "A Randomized, Double-Blind, Placebo-Controlled Study of Liposomal Amikacin for Inhalation (Arikace™) in Patients With Recalcitrant Nontuberculous Mycobacterial Lung Disease" is a Phase II clinical trial in collaboration with the US National Institute of Allergy and Infectious Diseases. http://www.clinicaltrials.gov/ct2/show/NCT01315236
^ "A Placebo Controlled, Randomized, Parallel Cohort, Safety And Tolerability Study Of 2 Dose Levels Of Liposomal Amikacin For Inhalation (Arikace™) In Patients With Bronchiectasis Complicated By Chronic Infection Due To Pseudomonas Aeruginosa" Phase II (completed). http://www.clinicaltrials.gov/ct2/show/NCT00775138
^ "A Study to Determine the Safety and Tolerability of Arikace™ Versus Placebo in Patients Who Have Bronchiectasis" is a Phase II clinical trial (as [4]) completed in the UK. http://www.ukctg.nihr.ac.uk/trialdetails/NCT00775138
^ http://www.toku-e.com/Assets/MIC/Amikacin%20hydrate.pdf

Edson RS, Terrell CL. The aminoglycosides. Mayo Clin Proc. 1999 May;74(5):519-28. Review. PMID 10319086

UpToDate Contents

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1. 嚢胞性線維腺症：呼吸器症状が急性増悪した場合の治療 cystic fibrosis treatment of acute pulmonary exacerbations
2. アミノグリコシド（非経口）の用量および投与 dosing and administration of parenteral aminoglycosides
3. グラム陰性桿菌性髄膜炎：治療 gram negative bacillary meningitis treatment
4. アミノグリコシド aminoglycosides
5. 成人の肺MAC（マイコバクテリウム・アビウムコンプレックス）症の治療 treatment of mycobacterium avium complex lung infection in adults

English Journal

The antimicrobial activity of mecillinam, nitrofurantoin, temocillin and fosfomycin and comparative analysis of resistance patterns in a nationwide collection of ESBL-producing Escherichia coli in Norway 2010-2011.

Zykov IN1,2, Sundsfjord A1,2, Småbrekke L3, Samuelsen Ø1,3.
Infectious diseases (London, England).Infect Dis (Lond).2016 Feb;48(2):99-107. doi: 10.3109/23744235.2015.1087648. Epub 2015 Sep 28.
BACKGROUND: The prevalence of extended-spectrum β-lactamase (ESBL)-producing Escherichia coli in Norway has been steadily increasing during the last 10-15 years as part of a global pandemic. ESBL producers frequently express co-resistance to other important antimicrobial drug classes, limiting ther
PMID 26414659

Nocardia asteroides Keratitis Resistant to Amikacin.

Patel R1, Sise A, Al-Mohtaseb Z, Garcia N, Aziz H, Amescua G, Pantanelli SM.
Cornea.Cornea.2015 Dec;34(12):1617-9. doi: 10.1097/ICO.0000000000000634.
PURPOSE: To describe 2 cases of Nocardia keratitis resistant to topical compounded amikacin therapy.METHODS: A 24-year-old woman presented with a corneal infiltrate. Cultures were taken, and topical moxifloxacin was administered. Corneal biopsy was performed when clinical status deteriorated, which
PMID 26418432

Acinetobacter baumannii in Southern Croatia: clonal lineages, biofilm formation, and resistance patterns.

Kaliterna V1,2, Kaliterna M3, Hrenović J4, Barišić Z1, Tonkić M3,2, Goic-Barisic I3,2.
Infectious diseases (London, England).Infect Dis (Lond).2015 Dec;47(12):902-7. doi: 10.3109/23744235.2015.1078906. Epub 2015 Aug 18.
BACKGROUND: Acinetobacter baumannii is one of the most prevalent causes of severe hospital-acquired infections and is responsible for the dramatic increase in carbapenem resistance in Croatia in the last 5 years. Such data have encouraged multicenter research focused on the organism's ability to for
PMID 26365683

Related Pictures

外觀圖片2 Amikin Amikin / Bristol-Myers Squibb reference index « Amikin Pediatric Preparatul Amikin se prezinta sub forma de Drugs reference index « Amikin » AMIKIN AMIKACIN SULPHATE

★リンクテーブル★

リンク元

「アミカシン」

Amikacin
Systematic (IUPAC) name
	(2S)-4-Amino-N-[(2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5R,6R)-6-(aminomethyl)-3,4,5-trihydroxy-oxan-2-yl]oxy-3-hydroxy-cyclohexyl]-2-hydroxybutanamide
Clinical data
Trade names	Generic (formerly Amikin)
AHFS/Drugs.com	Monograph
MedlinePlus	a682661
Pregnancy; category	AU: D; US: D (Evidence of risk); ;
Routes of; administration	Intramuscular, intravenous
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Protein binding	0-11%
Biological half-life	2-3 hours
Excretion	Renal
Identifiers
CAS Number	37517-28-5
ATC code	D06AX12 (WHO) J01GB06 (WHO), S01AA21 (WHO)
PubChem	CID 37768
DrugBank	DB00479
ChemSpider	34635
UNII	84319SGC3C
KEGG	D02543
ChEBI	CHEBI:2637
ChEMBL	CHEMBL177
Chemical data
Formula	C22H43N5O13
Molar mass	585.603 g/mol
	SMILES O=C(N[C@H]3[C@H](O[C@H]1O[C@@H]([C@@H](O)[C@H](N)[C@H]1O)CO)[C@@H](O)[C@H](O[C@H]2O[C@H](CN)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](N)C3)[C@@H](O)CCN ;
	InChI InChI=1S/C22H43N5O13/c23-2-1-8(29)20(36)27-7-3-6(25)18(39-22-16(34)15(33)13(31)9(4-24)37-22)17(35)19(7)40-21-14(32)11(26)12(30)10(5-28)38-21/h6-19,21-22,28-35H,1-5,23-26H2,(H,27,36)/t6-,7+,8-,9+,10+,11-,12+,13+,14+,15-,16+,17-,18+,19-,21+,22+/m0/s1 ; Key:LKCWBDHBTVXHDL-RMDFUYIESA-N ;
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　　[★]

英: amikacin, AMK
ラ: amikacinum
化: 硫酸アミカシン amikacin sulfate
商: アミカマイシン、ビクリン、ロミカシン、カシミー、プルテツシン、ベルマトン、Amikin
関: 抗菌薬、アミノグリコシド系抗菌薬

[1] Oxford Handbook of Infectious Diseases and Microbiology. OUP Oxford. 2009. p. 56. ISBN 9780191039621.

[2] "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.

[3] "Randomized, open-label, active-controlled, multicenter study to assess the efficacy, safety and tolerability of Arikace™ in Cystic Fibrosis patients with chronic infection due to Pseudomonas aeruginosa" is a European Phase III clinical trial, being conducted across multiple sites in the EU, starting at the Royal Brompton Hospital, Department of Respiratory Medicine, in London. https://www.clinicaltrialsregister.eu/ctr-search/trial/2011-000441-20/GB

[4] ttp://www.clinicaltrials.gov/ct2/show/NCT01315678

[5] "A Randomized, Double-Blind, Placebo-Controlled Study of Liposomal Amikacin for Inhalation (Arikace™) in Patients With Recalcitrant Nontuberculous Mycobacterial Lung Disease" is a Phase II clinical trial in collaboration with the US National Institute of Allergy and Infectious Diseases. http://www.clinicaltrials.gov/ct2/show/NCT01315236

[6] "A Placebo Controlled, Randomized, Parallel Cohort, Safety And Tolerability Study Of 2 Dose Levels Of Liposomal Amikacin For Inhalation (Arikace™) In Patients With Bronchiectasis Complicated By Chronic Infection Due To Pseudomonas Aeruginosa" Phase II (completed). http://www.clinicaltrials.gov/ct2/show/NCT00775138

[7] "A Study to Determine the Safety and Tolerability of Arikace™ Versus Placebo in Patients Who Have Bronchiectasis" is a Phase II clinical trial (as [4]) completed in the UK. http://www.ukctg.nihr.ac.uk/trialdetails/NCT00775138

[8] ttp://www.toku-e.com/Assets/MIC/Amikacin%20hydrate.pdf

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Amikin