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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/10 22:38:06」(JST)

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Aztreonam (trade names Azactam injection, Cayston inhalation) is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration (FDA) in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases.

Mechanism of action

Aztreonam is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking. It has a very high affinity for penicillin-binding protein-3 and mild affinity for penicillin-binding protein-1a. Aztreonam binds the penicillin-binding proteins of Gram-positive and anaerobic bacteria very poorly and is largely ineffective against them.^[1] Aztreonam is bactericidal, but less so than some of the cephalosporins.

Spectrum of bacterial susceptibility and resistance

Acinetobacter anitratus, Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis are generally susceptible to aztreonam, while some staphylococci, Staphylococcus aureus, Staphylococcus hemolyticus and Xanthomonas maltophilia are resistant to it. Furthermore, Aeromonas hydrophila, Citrobacter diversus, Enterobacter agglomerans, Haemophilus spp. and Streptococcus pyogenes have developed resistance to aztreonam to varying degrees.^[2]

Indications and spectrum of activity

Aztreonam has strong activity against susceptible Gram-negative bacteria, including Pseudomonas aeruginosa. It has no useful activity against Gram-positive bacteria or anaerobes. It is known to be effective against a wide range of bacteria including Citrobacter, Enterobacter, E. coli, Haemophilus, Klebsiella, Proteus, and Serratia species.^[3] The following represents MIC susceptibility data for a few medically significant microorganisms.

Staphylococcus aureus 8 - >128 μg/ml
Staphylococcus epidermidis 8 - 32 μg/ml
Streptococcus pyogenes 8 - ≥128 μg/ml

^[4]

Synergism between aztreonam and arbekacin or tobramycin against P. aeruginosa has been suggested.^[5]

Aztreonam is often used in patients who are penicillin allergic or who cannot tolerate aminoglycosides.

Administration

Aztreonam is poorly absorbed when given orally, so it must be administered as an intravenous or intramuscular injection (trade name Azactam ), or inhaled (trade name Cayston) using an ultrasonic nebulizer. In the United States, the FDA approved the inhalation form on February 22, 2010, for the suppression of P. aeruginosa infections in patients with cystic fibrosis.^[6] It received conditional approval for administration in Canada and the European Union in September 2009,^[6] and has been fully approved in Australia.^[7]

Common adverse effects

Reported side effects include injection site reactions, rash, and rarely toxic epidermal necrolysis. Gastrointestinal side effects generally include diarrhea and nausea and vomiting. There may be drug-induced eosinophilia. Because of the unfused beta-lactam ring unique to aztreonam, there is somewhat lower cross-reactivity between aztreonam and many other beta-lactam antibiotics, and it may be safe to administer aztreonam to many patients with hypersensitivity (allergies) to penicillins and nearly all cephalosporins. ^[1] However, like other beta lactams, there is a risk of very serious allergic reactions, including anaphylaxis. The aztreonam label directs physicians to be aware of the possibility of these severe adverse reactions. This is more likely if the patient is allergic to a certain cephalosporin known as ceftazidime. Azetreonam exhibits cross-reactivity with this cephalosporin due to a similar side chain. Physicians should evaluate prior allergy history when prescribing this medicine.

Special caution is warranted in patients who are allergic to ceftazidime and are subsequently placed on aztreonam therapy.

References

^ ^a ^b AHFS DRUG INFORMATION 2006 (2006 ed.). American Society of Health-System Pharmacists. 2006.
^ "Aztreonam spectrum of bacterial susceptibility and Resistance" (PDF). Retrieved 15 May 2012.
^ Mosby's Drug Consult 2006 (16 ed.). Mosby, Inc. 2006.
^ http://www.toku-e.com/Assets/MIC/Aztreonam.pdf
^ Kobayashi, Y., Uchida, H., Kawakami Y. (1992). "Synergy with aztreonam and arbekacin or tobramycin against Pseudomonas aeruginosa isolated from blood". J Antimicrob Chemother 30 (6): 871–872. doi:10.1093/jac/30.6.871. PMID 1289363.
^ ^a ^b Larkin, Catherine (February 22, 2010). "Gilead’s Inhaled Antibiotic for Lungs Wins Approval". BusinessWeek. Retrieved 2010-03-05.
^ "FDA approves Gilead cystic fibrosis drug Cayston". BusinessWeek. February 23, 2010. Retrieved 2010-03-05.

External links

MedlinePlus DrugInfo uspdi-202078

UpToDate Contents

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1. ペニシリン-アレルギー患者：セフェム系、カルバペネム系、およびモノバクタム系の使用 penicillin allergic patients use of cephalosporins carbapenems and monobactams
2. グラム陰性桿菌性髄膜炎：治療 gram negative bacillary meningitis treatment
3. β-ラクタマーゼ阻害剤、カルバペネム系、およびモノバクタム系抗菌薬の併用 combination beta lactamase inhibitors carbapenems and monobactams
4. セファロスポリン-アレルギー患者：セファロスポリンおよび関連抗菌薬のその後の使用 cephalosporin allergic patients subsequent use of cephalosporins and related antibiotics
5. β-ラクタム系抗生物質：作用機序、耐性および有害作用 beta lactam antibiotics mechanisms of action and resistance and adverse effects

English Journal

Prevalence, antimicrobial susceptibility, and genetic diversity of Pseudomonas aeruginosa as intestinal colonizer in the community.

Valenza G1, Tuschak C, Nickel S, Krupa E, Lehner-Reindl V, Höller C.
Infectious diseases (London, England).Infect Dis (Lond).2015 Sep;47(9):654-7. doi: 10.3109/23744235.2015.1031171. Epub 2015 Apr 2.
In this study we determined the prevalence of intestinal carriage, the antimicrobial susceptibility rates, and the genetic diversity of Pseudomonas aeruginosa in the community. From July 2010 to December 2011, a total of 2110 nonreplicate fecal samples from individuals living in Bavaria were collect
PMID 25832457

Antimicrobial Disk Susceptibility Testing of Leptospira spp. Using Leptospira Vanaporn Wuthiekanun (LVW) Agar.

Wuthiekanun V1, Amornchai P2, Langla S2, White NJ2, Day NP2, Limmathurotsakul D1, Peacock SJ2.
The American journal of tropical medicine and hygiene.Am J Trop Med Hyg.2015 Aug 5;93(2):241-3. doi: 10.4269/ajtmh.15-0180. Epub 2015 Jun 8.
Leptospira Vanaporn Wuthiekanun (LVW) agar was used to develop a disk diffusion assay for Leptospira spp. Ten pathogenic Leptospira isolates were tested, all of which were susceptible to 17 antimicrobial agents (amoxicillin/clavulanic acid, amoxicillin, azithromycin, cefoxitin, ceftazidime, ceftriax
PMID 26055750

Pseudomonas aeruginosa Infection after Pancreatoduodenectomy: Risk Factors and Clinic Impacts.

Zhang JF1, Zhu HY2, Sun YW1, Liu W1, Huo YM1, Liu DJ1, Li J1, Hua R1.
Surgical infections.Surg Infect (Larchmt).2015 Aug 3. [Epub ahead of print]
BACKGROUND: Pseudomonas aeruginosa (P. aeruginosa) is a leading cause of nosocomial infections, which is difficult to treat because of limited susceptibility to antimicrobial agents. In China, isolation rates of P. aeruginosa were observed to increase by year. The incidence of infectious complicatio
PMID 26237502

Japanese Journal

複雑性尿路感染症に対するAztreonam (AZT)の臨床的検討

水谷修太郎,岩尾典夫,三好進,矢野久雄,岸本知巳,桜井勗,若月晶,中村隆幸,本多正人,小田昌良,清原久和,高栄哲,佐川史郎,伊藤喜一郎,古武敏彦,細木茂,藤岡秀樹,高羽津,松宮清美,細見昌弘,三宅修,板谷宏彬,高寺博史,新武三,武本征人,岩松克彦,永野俊介,市川靖二,野島道生,長船匡男,客野宮治,山口誓司,多田安温,園田孝夫,松田稔,瀬ロ利信
泌尿器科紀要 35(12), 2155-2161, 1989-12
… Aztreonam (AZT, Azactam) was given to 176 patients with complicated urinary tract infections (UTI), of whom 110 cases satisfied with the "Criteria of UTI Committee for the Evaluation of Drug Efficacy in the UTI (3rd Ed.)", which was modified by adopting the midstream urine data in cases of women. …
NAID 120002157536

Related Pictures

AZACTAM 2 GM VIAL Azactam in dextrose (iso-osmotic Azactam (Aztreonam) Azactam Azactam 1 gram Solution for AZACTAM. 1 g. 1 flacon AZACTAM Azactam 1gm , Side Effects & Interactions for Azactam

★リンクテーブル★

リンク元

「アズトレオナム」

Aztreonam
Systematic (IUPAC) name
	2-({[(1Z)-1-(2-amino-1,3-thiazol-4-yl) -2- {[(2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl]amino} -2- oxoethylidene]amino}oxy)-2-methylpropanoic acid
Clinical data
Trade names	Azactam
AHFS/Drugs.com	monograph
Pregnancy; category	B1 (Au), B (U.S.);
Legal status	UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	Intravenous, intramuscular, inhalation
Pharmacokinetic data
Bioavailability	100% (IM) 0.1% (Oral in Rats) Unknown (Oral in humans)
Protein binding	56%
Metabolism	hepatic (minor %)
Biological half-life	1.7 hours
Excretion	Renal
Identifiers
CAS Registry Number	78110-38-0
ATC code	J01DF01
PubChem	CID: 54116
DrugBank	DB00355
ChemSpider	4674940
UNII	G2B4VE5GH8
KEGG	D00240
ChEBI	CHEBI:161680
ChEMBL	CHEMBL158
Chemical data
Formula	C13H17N5O8S2
Molecular mass	435.433 g/mol
	SMILES O=S(=O)(O)N2C(=O)[C@@H](NC(=O)C(=N\OC(C(=O)O)(C)C)/c1nc(sc1)N)[C@@H]2C ;
	InChI InChI=1S/C13H17N5O8S2/c1-5-7(10(20)18(5)28(23,24)25)16-9(19)8(6-4-27-12(14)15-6)17-26-13(2,3)11(21)22/h4-5,7H,1-3H3,(H2,14,15)(H,16,19)(H,21,22)(H,23,24,25)/b17-8-/t5-,7-/m0/s1 ; Key:WZPBZJONDBGPKJ-VEHQQRBSSA-N ;
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　　[★]

英: aztreonam、AZT
商: アザクタム, Azactam
関: 抗菌薬

[AHFS-1] AHFS DRUG INFORMATION 2006 (2006 ed.). American Society of Health-System Pharmacists. 2006.

[2] "Aztreonam spectrum of bacterial susceptibility and Resistance" (PDF). Retrieved 15 May 2012.

[Mosby-3] Mosby's Drug Consult 2006 (16 ed.). Mosby, Inc. 2006.

[4] ttp://www.toku-e.com/Assets/MIC/Aztreonam.pdf

[5] Kobayashi, Y., Uchida, H., Kawakami Y. (1992). "Synergy with aztreonam and arbekacin or tobramycin against Pseudomonas aeruginosa isolated from blood". J Antimicrob Chemother 30 (6): 871–872. doi:10.1093/jac/30.6.871. PMID 1289363.

[BW1-6] Larkin, Catherine (February 22, 2010). "Gilead’s Inhaled Antibiotic for Lungs Wins Approval". BusinessWeek. Retrieved 2010-03-05.

[7] "FDA approves Gilead cystic fibrosis drug Cayston". BusinessWeek. February 23, 2010. Retrieved 2010-03-05.

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Azactam