阿米卡星：修订间差异
删除的内容 添加的内容
Add 1 book for verifiability (20240917sim)) #IABot (v2.0.9.5) (GreenC bot |
|||
| （未显示6个用户的38个中间版本） | |||
第1行：
{{Infobox drug
| Watchedfields = changed
| verifiedrevid = 464364466
| image = Amikacin.svg
| width =
| alt =
| image2 = Amikacin 3D ball-and-stick 4P20.png
| width2 =
| alt2 =
| caption =
<!-- Clinical data -->
| pronounce =
| tradename = Amikin、Amiglyde-V、Arikayce及其他
| Drugs.com = {{drugs.com|monograph|amikacin-sulfate}}
| MedlinePlus = a682661
| DailyMedID = Amikacin
| pregnancy_AU = D
| pregnancy_AU_comment = <ref name="Drugs.com pregnancy">{{cite web | title=Amikacin Use During Pregnancy | website=Drugs.com | date=2019-12-02 | url=https://www.drugs.com/pregnancy/amikacin.html | access-date=2020-03-13 | archive-date=2020-07-25 | archive-url=https://web.archive.org/web/20200725052838/https://www.drugs.com/pregnancy/amikacin.html | dead-url=no }}</ref>
| pregnancy_category=
| routes_of_administration = [[肌肉注射]]、[[靜脈注射]]及口部吸入
| class = [[氨基糖苷類抗生素|胺基糖苷類抗生素]]
| ATCvet =
| ATC_prefix = D06
| ATC_suffix = AX12
| ATC_supplemental = {{ATC|J01|GB06}}, {{ATC|S01|AA21}}, {{ATC|J01|RA06}}, {{ATCvet|D06|AX12}}, {{ATCvet|J01|GB06}}, {{ATCvet|S01|AA21}}, {{ATCvet|J01|RA06}}
<!-- Legal status -->
| legal_AU = S4
| legal_AU_comment = <ref>{{cite web | title=Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017 | website=Therapeutic Goods Administration (TGA) | date=21 June 2022 | url=https://www.tga.gov.au/resources/publication/publications/prescription-medicines-registration-new-generic-medicines-and-biosimilar-medicines-2017 | access-date=2024-03-30 | archive-date=2023-07-06 | archive-url=https://web.archive.org/web/20230706023149/https://www.tga.gov.au/resources/publication/publications/prescription-medicines-registration-new-generic-medicines-and-biosimilar-medicines-2017 | dead-url=no }}</ref>
| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F-->
| legal_BR_comment =
| legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_CA_comment =
| legal_DE = <!-- Anlage I, II, III or Unscheduled-->
| legal_DE_comment =
| legal_NZ = <!-- Class A, B, C -->
| legal_NZ_comment =
| legal_UK = POM
| legal_UK_comment = <ref>{{cite web | title=Amikacin 250 mg/ml Injection - Summary of Product Characteristics (SmPC) | website=(emc) | date=16 September 2015 | url=https://www.medicines.org.uk/emc/medicine/619 | access-date=2020-03-13 | archive-date=2020-03-13 | archive-url=https://web.archive.org/web/20200313193548/https://www.medicines.org.uk/emc/medicine/619 | dead-url=no }}</ref>
| legal_US = Rx-only
| legal_US_comment = <ref name="Arikayce FDA label" />
| legal_EU = Rx-only
| legal_EU_comment = <ref name="Arikayce liposomal EPAR">{{cite web | title=Arikayce liposomal EPAR | website=European Medicines Agency | date=21 July 2020 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/arikayce-liposomal | access-date=2023-03-04 | archive-date=2023-09-24 | archive-url=https://web.archive.org/web/20230924020219/https://www.ema.europa.eu/en/medicines/human/EPAR/arikayce-liposomal | dead-url=no }}</ref><ref>{{cite web | title=Arikayce liposomal Product information | website=Union Register of medicinal products | url=https://ec.europa.eu/health/documents/community-register/html/h1469.htm | access-date=2023-03-03 | archive-date=2023-03-05 | archive-url=https://web.archive.org/web/20230305062002/https://ec.europa.eu/health/documents/community-register/html/h1469.htm | dead-url=no }}</ref>
| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV-->
| legal_UN_comment =
| legal_status = <!--For countries not listed above-->
<!-- Pharmacokinetic data -->
| bioavailability = >90%<ref name="plumb"/>
| protein_bound = 0–11%
| metabolism = 幾乎不會被代謝
| metabolites =
| onset =
| elimination_half-life = 2–3小時
| duration_of_action =
| excretion = [[腎]]臟
<!-- Identifiers -->
| index2_label = as salt
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 37517-28-5
| CAS_supplemental =
| PubChem = 37768
| IUPHAR_ligand =
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00479
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 34635
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 84319SGC3C
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D02543
| KEGG2_Ref = {{keggcite|correct|kegg}}
| KEGG2 = D00865
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 2637
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 177
| NIAID_ChemDB =
| PDB_ligand =
| synonyms =
<!-- Chemical and physical data -->
| IUPAC_name = (2''S'')-4-Amino-''N''-[(2''S'',3''S'',4''R'',5''S'')-5-amino-2-[(2''S'',3''R'',4''S'',5''S'',6''R'')-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2''R'',3''R'',4''S'',5''R'',6''R'')-6-(aminomethyl)-3,4,5-trihydroxy-oxan-2-yl]oxy-3-hydroxy-cyclohexyl]-2-hydroxybutanamide
| C=22 | H=43 | N=5 | O=13
| 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
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChI_comment =
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = LKCWBDHBTVXHDL-RMDFUYIESA-N
| density =
| density_notes =
| melting_point =
| melting_high =
| melting_notes =
| boiling_point =
| boiling_notes =
| solubility =
| sol_units =
| specific_rotation =
}}
'''阿米卡星'''（{{lang-en|Amikacin}}）是一種[[抗生素]]藥物，用於治療多種[[病原細菌]][[感染]],<ref name=AHFS2016>{{cite web|url=https://www.drugs.com/monograph/amikacin-sulfate.html|title=Amikacin Sulfate|publisher=The American Society of Health-System Pharmacists|access-date=2016-12-08|url-status=live|archive-url=https://web.archive.org/web/20161220231044/https://www.drugs.com/monograph/amikacin-sulfate.html|archive-date= 2016-12-20}}</ref>包括[[敗血性關節炎]]、{{le|腹腔內感染|intra-abdominal infection}}、[[腦膜炎]]、[[肺炎]]、[[敗血症]]和[[泌尿道感染]]。<ref name=AHFS2016/>它也用於治療{{le|多重抗藥性結核病|Multidrug-resistant tuberculosis}}。<ref name=WHO2008>{{cite book | title = WHO Model Formulary 2008 | url = https://archive.org/details/whomodelformular00unse | year = 2009 | isbn = 9789241547659 | vauthors = ((World Health Organization)) | veditors = Stuart MC, Kouimtzi M, Hill SR | hdl = 10665/44053 | author-link = World Health Organization | publisher = World Health Organization | hdl-access=free |page=[https://archive.org/details/whomodelformular00unse/page/137 137]}}</ref>此藥物經由[[靜脈注射]]、[[肌肉注射]]及口部吸入方式使用。<ref name=AHFS2016/>
阿米卡星與其他[[氨基糖苷类抗生素|胺基糖苷類藥物]]一樣，會導致聽力損失、身體平衡問題和[[腎功能衰竭]]。<ref name=AHFS2016/>其他的副作用有[[癱瘓]]（導致無法呼吸）。<ref name=AHFS2016/>如果個體在[[姙娠|懷孕]]期間使用，出生的後代可能會永久性失聰。<ref name=AHFS2016/><ref name="Drugs.com pregnancy" />阿米卡星是透過阻斷細菌[[30S核糖體亞基]]的功能，使其無法產生蛋白質而發揮作用。<ref name=AHFS2016/>
==醫療用途==
阿米卡星最常用於治療嚴重性多重抗藥性與需氧[[革蘭氏陰性菌]]的感染，後者細菌特別指[[假單胞菌屬]]、[[不動桿菌屬]]、[[腸桿菌屬]]、[[大腸桿菌]]、[[變形桿菌屬]]、[[克雷伯氏菌屬]]和[[沙雷氏菌屬]]。<ref name="Amikacin sulfate FDA label">{{cite web | title=Amikacin sulfate injection, solution | website=DailyMed | date=2019-4-10 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c0f57839-1c9b-49e5-8c7a-708e2d16495d | access-date=2020-05-13 | archive-date=2020-03-13 | archive-url=https://web.archive.org/web/20200313193145/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c0f57839-1c9b-49e5-8c7a-708e2d16495d | dead-url=no }}</ref>少數會受阿米卡星強烈影響的[[革蘭氏陽性菌]]有[[葡萄球菌屬]]<ref name="Amikacin sulfate FDA label" />及[[諾卡氏菌屬]]兩種。 <ref>{{cite book | vauthors = Scholar EM, Pratt WB | title=The Antimicrobial Drugs | date=2000-05-22 | pages=15–19 | url=https://books.google.com/books?id=gACeB8XCnpgC&pg=PA15 | edition=2nd | publisher=Oxford University Press, USA | isbn=978-0-19-975971-2 | url-status=live | archive-url=https://web.archive.org/web/20170910172330/https://books.google.com/books?id=gACeB8XCnpgC&pg=PA15 | archive-date=2017-09-10 }}</ref>在第一線藥物無法控制非結核[[分枝桿菌屬]]感染和[[結核病]]感染（且如果是對阿米卡星效力敏感的菌株所引起）時，也可使用阿米卡星治療。<ref name=AHFS2016 />此種藥物在治療時很少會單獨使用。<ref name=cunha>{{cite journal | vauthors = Cunha BA | title = New uses for older antibiotics: nitrofurantoin, amikacin, colistin, polymyxin B, doxycycline, and minocycline revisited | url = https://archive.org/details/sim_medical-clinics-of-north-america_2006-11_90_6/page/1089 | journal = The Medical Clinics of North America | volume = 90 | issue = 6 | pages = 1089–1107 | date = November 2006 | pmid = 17116438 | doi = 10.1016/j.mcna.2006.07.006 | series = Antimicrobial Therapy | s2cid = 30373734 }}</ref>
阿米卡星常用於治療下述疾病：<ref name=AHFS2016 />
*[[支氣管擴張]]<ref name=medscape>{{cite web | work=Medscape | title=amikacin (Rx) | publisher=WebMD | access-date=2017-08-09 | url=http://reference.medscape.com/drug/amikin-amikacin-342516#0 | url-status=live | archive-url=https://web.archive.org/web/20170809083119/http://reference.medscape.com/drug/amikin-amikacin-342516 | archive-date=2017-08-09 }}</ref>
*骨骼和關節感染
*與[[替卡西林]]共同使用，治療[[癌症]]患者的[[粒細胞]]減少症<ref name="aronson">{{cite book |editor=Aronson J. K.| title=Meyler's Side Effects of Drugs | chapter=Amikacin | location=Oxford | date=2016 | edition=16th | publisher=Elsevier | isbn=978-0-444-53716-4 | pages=207–209}}</ref>
*作為其他藥物（如[[克林黴素]]、[[甲硝唑]]、{{le|哌拉西林/他唑巴坦|piperacillin/tazobactam}}或{{le|氨芐西林/舒巴坦|ampicillin/sulbactam}}）的輔助藥物，用於治療腹腔內感染（如[[腹膜炎]]）
*腦膜炎
*分枝桿菌屬感染，包括用作治療活動性結核病的二線藥物。<ref>{{cite book | vauthors = Vardanyan R, Hruby V | title=Synthesis of Best-Seller Drugs | chapter=Chapter 32: Antimicobacterial Drugs | location=Boston| date=2016| publisher=Academic Press | isbn=978-0-12-411492-0 | pages=669–675}}</ref>它也用於治療由{{le|鳥分枝菌群|Mycobacterium avium complex}}、{{le|膿腫分枝桿菌|Mycobacteroides abscessus}}、{{le|龜分枝菌群|Mycobacteroides chelonae}}和{{le|偶發分枝菌群|Mycobacterium fortuitum}}的感染。
*{{le|玫瑰紅球菌|Rhodococcus equi }}所引起類似結核病的感染
*呼吸道感染，包括作為[[β-內醯胺]]類或[[碳青黴烯]]類藥物的輔助藥物，用以治療{{le|院內型肺炎|hospital-acquired pneumonia}}
*敗血症，包括新生兒敗血症，<ref name="Amikacin sulfate FDA label" />作為β-內酰胺類或碳青黴烯類藥物的輔助藥物
*皮膚和手術縫合部位感染<ref name="Amikacin sulfate FDA label" />
*對毒性較低藥物具有抗藥性的細菌所引起的泌尿道感染（通常是[[腸桿菌科]]細菌或[[綠膿桿菌]]）
阿米卡星可與β-內酰胺類抗生素聯合針對[[嗜中性白血球低下]]和[[發燒]]患者進行{{le|經驗治療|empiric therapy}}。<ref name=AHFS2016 />
===懸浮液吸入劑===
[[美國]]<ref name="FDA PR">{{cite press release |title=FDA approves a new antibacterial drug to treat a serious lung disease using a novel pathway to spur innovation |url=https://www.fda.gov/news-events/press-announcements/fda-approves-new-antibacterial-drug-treat-serious-lung-disease-using-novel-pathway-spur-innovation |website=U.S. [[Food and Drug Administration]] (FDA) |access-date=2018-11-12 |archive-date=2019-10-01 |archive-url=https://web.archive.org/web/20191001182321/https://www.fda.gov/news-events/press-announcements/fda-approves-new-antibacterial-drug-treat-serious-lung-disease-using-novel-pathway-spur-innovation |dead-url=no }} {{PD-notice}}</ref><ref name="Arikayce FDA label">{{cite web | title=Arikayce- amikacin suspension | website=DailyMed | date=2018-09-30 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=499ab990-2b21-474f-aaba-d86388965f40 | access-date=2020-03-13 | archive-date=2020-03-13 | archive-url=https://web.archive.org/web/20200313194403/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=499ab990-2b21-474f-aaba-d86388965f40 | dead-url=no }}</ref>和[[歐盟]]<ref name="Arikayce liposomal EPAR" />也批准使用含阿米卡星的[[脂質體]]懸浮液吸入劑，用於治療鳥分枝菌群感染。
===特定人口群組===
對於老年人和兒童，由於老年人通常會出現隨年齡增長而有的腎功能下降，而兒童則為腎臟尚未發育完全，而應採小劑量治療方式。此藥物在美國和[[澳大利亞]]被歸類為妊娠類別D，表示有可能會傷害胎兒。<ref name="FDA PR" />
阿米卡星於人體內的分布容積、清除率以及對特殊人群的影響如下述：
*一般來說，應避免將阿米卡星用於嬰兒身上。<ref name=ettinger>{{cite book | vauthors = Ettinger SJ, Feldman EC | title=Textbook of Veterinary Internal Medicine | date=2009-12-24 | pages=1976, 523 | url=https://books.google.com/books?id=4Qzau1jagOYC&pg=PA1976 | publisher=Elsevier Health Sciences | isbn=978-1-4377-0282-8 | url-status=live | archive-url=https://web.archive.org/web/20170910172330/https://books.google.com/books?id=4Qzau1jagOYC&pg=PA1976 | archive-date=2017-09-10 }}</ref>嬰兒由於細胞外液濃度較高，其藥物分布容積也往往更大，會含有更多胺基糖苷類藥物。<ref name="plumb" >{{cite book | vauthors = Plumb DC | title=Plumb's Veterinary Drug Handbook | url = https://archive.org/details/plumbsveterinary0000plum_o2u8 | chapter=Amikacin Sulfate | location=Stockholm, Wisconsin; Ames, Iowa | date=2011 | edition=7th | publisher=Wiley | isbn=978-0-470-95964-0 | pages=[https://archive.org/details/plumbsveterinary0000plum_o2u8/page/39 39]–43}}</ref>
*阿米卡星於老年人體內的停留時間往往更長。 20歲患者的阿米卡星平均清除率為每小時6升，而80歲患者則為每小時3升。<ref name=maire>{{cite book | vauthors = Maire P, Bourguignon L, Goutelle S, Ducher M, Jelliffe R | chapter=Chapter 20 – Individualizing Drug Therapy in the Elderly | veditors = Jelliffe RW, Neely M | title=Individualized Drug Therapy for Patients | location=Boston | date=2017 | publisher=Academic Press | isbn=978-0-12-803348-7 | pages=373–382}}</ref>
*[[囊腫性纖維化]]患者的清除率則更高。<ref name="eghianruwa">{{cite book | vauthors = Eghianruwa K | title=Essential Drug Data for Rational Therapy in Veterinary Practice | date=2014 | page=16 | url=https://books.google.com/books?id=h4zCAgAAQBAJ&pg=PA16 | publisher=Author House | isbn=978-1-4918-0000-3 | url-status=live | archive-url=https://web.archive.org/web/20170910172330/https://books.google.com/books?id=h4zCAgAAQBAJ&pg=PA16 | archive-date= 2017-09-10 }}</ref>
*對於患有肌肉疾患，如[[重症肌無力症]]或[[帕金森氏症]]等的患者，阿米卡星的神經肌肉銜接阻滯作用可能會加劇肌肉無力症状。<ref name=AHFS2016/>
==不良影響==
阿米卡星的副作用與其他胺基糖苷類藥物相似。{{le|腎毒性|Nephrotoxicity}}和{{le|耳毒性|ototoxicity }}（可導致聽力損失）是最重要的影響，會發生在1-10%的使用者身上。<ref name=medscape />腎毒性和耳毒性被認為是由於胺基糖苷類藥物容易在腎臟和[[內耳]]中累積所致。<ref name=plumb />
[[File:Gray920.png|thumb|人類內耳圖，阿卡米星會對[[耳蝸]]及[[耳前庭]]造成損害。|300x300px]]
如果使用較高劑量或使用時間超過建議時，可能會導致神經毒性。
含阿米卡星脂質體懸浮液吸入劑的處方資訊中列有[[黑框警告]]，指出使用將涉及有關呼吸系統疾病風險增加，包括過敏性肺炎、支氣管痙攣、潛在肺部疾病惡化和[[咳血]]，且在某些情況下需住院治療。<ref name="FDA PR" /><ref name="Arikayce FDA label" />使用此類吸入劑的患者的其他常見副作用有[[聲音嘶啞]]、[[咳嗽]]、耳毒性、上呼吸道不適、肌肉骨骼疼痛、疲勞、[[腹瀉]]和[[噁心]]。<ref name="FDA PR" /><ref name="Arikayce FDA label" />
==禁忌症==
對任何胺基糖苷類藥物敏感的患者應避免使用，因為阿米卡星會引發交叉過敏性。對[[亞硫酸鹽]]敏感的人也應避免使用（在氣喘患者中更為常見），<ref name="Amikacin sulfate FDA label" />因為大多數阿米卡星通常含有[[焦亞硫酸鈉]]，可能會引起過敏反應。<ref name=AHFS2016 />
一般來說，阿米卡星不應與另一種可引起神經毒性、耳毒性或腎毒性的藥物一起使用，或在其之前/之後使用。此類藥物包括其他胺基糖苷類藥物、[[阿昔洛韋]]（抗病毒）、[[兩性黴素B]]（抗真菌）、[[桿菌肽]]（抗生素）、{{le|捲曲黴素|capreomycin}}、[[粘菌素]]、[[多粘菌素B]]和[[萬古黴素]]，以及用於[[化學療法]]的[[順鉑]]。<ref name=AHFS2016 />
阿米卡星不應與[[神經肌肉阻滯藥]]一起使用，因為它們會加劇肌肉無力和癱瘓。<ref name=AHFS2016 />
==藥物交互作用==
阿米卡星可被其他β-內酰胺類藥物滅活，但程度不如其他胺基糖苷類藥物，而仍經常與[[青黴素]]（一種β-內酰胺類藥物）和碳青黴烯類藥物一起使用，以產生針對某些細菌的附加作用。已知抗生素[[氯黴素]]、克林黴素和[[四環黴素]]通常透過藥理拮抗作用讓胺基糖苷類藥物失去活性。<ref name=AHFS2016 />
阿米卡星的藥理拮抗劑作用會降低某些[[疫苗]]的效果，例如活的減毒[[卡介苗]]（用於預防結核病）、[[霍亂疫苗]]和口服減活[[傷寒疫苗]]。<ref name=medscape />
==藥理學==
===作用機制===
[[File:010 small subunit-1FKA.gif|thumb|原核生物30S核糖體亞基。圖中，橙色部分代表16S 核糖體RNA，藍色部分代表附着的各種蛋白質。]]
阿米卡星不可逆地與[[16S 核糖體RNA]]和30S核糖體亞基的RNA結合S12蛋白結合，並透過改變[[核醣體]]的形狀來抑制蛋白質合成，使其無法正確讀取[[信使核糖核酸]]的[[遺傳密碼]]。<ref name="Amikacin sulfate FDA label" /><ref name="bauman">{{cite book | vauthors = Bauman RW | title=Microbiology: with diseases by body system | url = https://archive.org/details/microbiologywith0000baum_q4z6 | location=Boston | date=2015 | edition=4th | publisher=Pearson | isbn=978-0-321-91855-0}}</ref>它也干擾與[[轉運核糖核酸]]（tRNA）反遺傳密碼[[搖擺鹼基對]]相互作用的區域。<ref name="drugbank">{{cite web|url=https://www.drugbank.ca/drugs/DB00479|title=Amikacin|date=2017-08-02|work=DrugBank|access-date=2017-08-10|url-status=live|archive-url=https://web.archive.org/web/20170816150102/https://www.drugbank.ca/drugs/DB00479|archive-date=2017-08-16}}</ref>其作用有濃度依賴性，在鹼性環境下作用較佳。<ref name="plumb" />
在正常劑量下，會在24-48小時內對具有阿米卡星敏感性的細菌發生作用。<ref name="Amikacin sulfate FDA label" />
===抗藥性===
阿米卡星可避開所有抗生素失活酶的攻擊，而這些酶會導致細菌對抗生素產生抗藥性，但氨基乙醯轉移酶和核苷酸轉移酶兩者除外。<ref name=mudd>{{cite web | vauthors = Mudd E | title=O Aminoglycosides | work=Pharmacological Sciences | access-date= 2017-08-14 | date= 2017-08-07 | url=https://www.pharmacologicalsciences.us/pharmaceutical-chemistry/o-aminoglycosides.html | url-status=live | archive-url=https://web.archive.org/web/20170816105922/https://www.pharmacologicalsciences.us/pharmaceutical-chemistry/o-aminoglycosides.html | archive-date= 2017-08-16 }}</ref>
===藥物動力學===
阿米卡星無法經由口服方式吸收，因此必須經由腸胃外給藥。於肌肉注射時，它在0.5-2小時內達到血清濃度的峰值。不到11%的阿米卡星會與血漿蛋白結合，分佈在[[心臟]]、[[膽囊]]、肺和[[骨骼]]中，以及[[膽汁]]、[[痰]]、組織液、胸膜液和[[滑液]]之中。
==化學==
阿米卡星由卡那黴素衍生而來。<ref name=kawaguchi>{{cite journal | vauthors = Kawaguchi H, Naito T, Nakagawa S, Fujisawa KI | title = BB-K 8, a new semisynthetic aminoglycoside antibiotic | journal = The Journal of Antibiotics | volume = 25 | issue = 12 | pages = 695–708 | date = December 1972 | pmid = 4568692 | doi = 10.7164/antibiotics.25.695 | url = https://www.jstage.jst.go.jp/article/antibiotics1968/25/12/25_12_695/_pdf | url-status = live | doi-access = free | archive-url = https://web.archive.org/web/20170816105728/https://www.jstage.jst.go.jp/article/antibiotics1968/25/12/25_12_695/_pdf | archive-date = 2017-08-16 }}</ref><ref name=monteleone>{{cite book | vauthors = Monteleone PM, Muhammad N, Brown RD, McGrory JP, Hanna SA | title=Amikacin Sulfate | date=1983-01-01| doi=10.1016/S0099-5428(08)60163-X | issn=0099-5428 | volume=12 | pages=37–71| series=Analytical Profiles of Drug Substances | publisher=Academic Press | isbn=9780122608124 }}</ref>
[[File:Amikacin synthesis 2.svg|center|阿米卡星由卡那黴素衍生而來的過程|800x800px]]
==社會與文化==
阿米卡星於1971年由[[禮來]]公司提出申請，於1972年獲得專利，並於1976年進入商業販售。<ref>{{cite book| vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery|date=2006|publisher=John Wiley & Sons|isbn=9783527607495|page=507|url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA507|url-status=live|archive-url=https://web.archive.org/web/20161220092307/https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA507|archive-date=2016-12-20}}</ref><ref>{{cite book|title=Oxford Handbook of Infectious Diseases and Microbiology|date=2009|publisher=OUP Oxford|isbn=9780191039621|page=56|url=https://books.google.com/books?id=5W-WBQAAQBAJ&pg=PT56|url-status=live|archive-url=https://web.archive.org/web/20151124232554/https://books.google.ca/books?id=5W-WBQAAQBAJ&pg=PT56|archive-date=2015-11-24}}</ref>它已被列入[[世界衛生組織基本藥物標準清單]]之中。<ref name="WHO21st">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 21st list 2019 | year = 2019 | hdl = 10665/325771 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO | hdl-access=free }}</ref>
==
雖然阿米卡星獲得[[美國食品藥物管理局]]（FDA）批准，僅適用於治療狗和馬的子宮內感染，但它是[[獸醫學]]中最常使用的氨基糖苷類藥物之一，<ref name=forney>{{cite web | vauthors = Forney B | title=Amikacin for Veterinary Use | work=Wedgewood Pharmacy | access-date=2017-08-09 | url=http://www.wedgewoodpetrx.com/learning-center/professional-monographs/amikacin-for-veterinary-use.html | url-status=live | archive-url=https://web.archive.org/web/20170816110344/http://www.wedgewoodpetrx.com/learning-center/professional-monographs/amikacin-for-veterinary-use.html | archive-date=2017-08-16 }}</ref>並已用於狗、貓、[[豚鼠]]、[[絨鼠]]、[[倉鼠]]、{{le|小鼠|mouse}}、[[土撥鼠]]、[[家牛]]、[[鳥]]、[[蛇]]、[[龜鱉目|烏龜]]和[[陸龜]]、[[鱷魚]]、[[牛蛙]]和[[魚]]的治療。<ref name=plumb /><ref>{{cite book | vauthors = Riviere JE, Papich MG | title=Veterinary Pharmacology and Therapeutics | date=2013-05-13 | page=931 | url=https://books.google.com/books?id=xAPa4WDzAnQC&pg=PA931 | publisher=John Wiley & Sons | isbn=978-1-118-68590-7 | url-status=live | archive-url=https://web.archive.org/web/20170910172330/https://books.google.com/books?id=xAPa4WDzAnQC&pg=PA931 | archive-date=2017-09-10 }}</ref><ref>{{cite book | vauthors = Mader DR, Divers SJ | title=Current Therapy in Reptile Medicine and Surgery – E-Book | date=2013-12-12 | page=382 | url=https://books.google.com/books?id=2phWAgAAQBAJ&pg=PA382 | publisher=Elsevier Health Sciences | isbn=978-0-323-24293-6 | url-status=live | archive-url=https://web.archive.org/web/20170910172330/https://books.google.com/books?id=2phWAgAAQBAJ&pg=PA382 | archive-date=2017-09-10 }}</ref>它常用於治療蛇的呼吸道感染、烏龜的細菌性甲殼病和[[金剛鸚鵡]]的[[鼻竇炎]]。它通常禁用於家[[兔]]和野兔（但仍被使用），因為它會損害兔類[[腸道菌群]]的平衡。<ref name=plumb />
對於狗和貓，阿米卡星通常用作外用抗生素，治療[[耳炎]]和角膜潰瘍，尤其是綠膿桿菌引起的。
==
{{reflist|2}}
{{模板:皮膚病用抗生素和化療藥}}
{{模板:蛋白質合成抑制劑類抗生素}}
{{Portal bar | Medicine}}
{{Authority control}}
[[
[[分類:抗結核藥物]]
[[Category:Butyramides]]
[[分類:世界衛生組織基本藥物]]
[[分類:RTT]]
[[分類:罕用藥]]
| |||