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 今天學妹問我,學長,有第五代頭孢子菌素嗎?

當然是有啦!時代一直進步,細菌也會跟著進步,所以我們也要有新的武器才能與之抗衡。

Ceftobiprole(Zeftera

 

這是繼Vancomycin失效之後,人類從開發Zyvox、Daptomycin、synercid(quinupristin/dalfopristin)這些之後,繼續開發出的新抗生素,

目前研究對於VRSA非常有效果,

 

2010年10月美國 FDA 核准 ceftobiprole 用來治療 MRSA、MSSA、enterococci 感染等抗藥性細菌

 

 

tefl400b  

Ceftaroline fosamil

Ceftaroline_fosamil2DCSD.svg  

ceftaroline 為原形藥物 (prodrug),當在體內代謝為 ceftaroline-M1 方有抗菌活性,1,2,4-thiadiazole:對格蘭氏陽性菌具有穿透力,且包含 transpeptidase活性。

位於1,2,4-thiadiazole 上的磷酸基,不僅增加了 prodrug 的水溶性,在固態時也有穩定的效果。

Oxime group (C=N-O-CH3) 提高對 β-lactamase 的抗性。(4) 1,3-thiazole 環,大幅提高對 MRSA 的滅菌效果。

兩性離子 (zwitterions) 的特性,增加對格蘭氏陰性菌的穿透力。

不過,如果人類還是繼續浮濫使用抗生素的話,就很難保他的效果可以維持多久了。

 

來複習一下前面1~4代吧

 

Generation

Members

1

Cefacetrile (cephacetrile), Cefadroxil (cefadroxyl; Duricef), Cephalexin (cefalexin; Keflex), Cefaloglycin (cephaloglycin), Cefalonium (cephalonium), Cefaloridine (cephaloradine), Cefalotin (cephalothin; Keflin), Cefapirin (cephapirin; Cefadryl), Cefatrizine, Cefazaflur, Cefazedone, Cefazolin (cephazolin; Ancef, Kefzol), Cefradine (cephradine; Velosef), Cefroxadine, Ceftezole

描述

Gram-positive: Activity against penicillinase-producing, methicillin-susceptible staphylococci and streptococci (though they are not the drugs of choice for such infections). No activity against methicillin-resistant staphylococci or enterococci.

Gram-negative: Activity against Proteus mirabilis, some Escherichia coli, and Klebsiella pneumoniae ("PEcK"), but have no activity against Bacteroides fragilis, Pseudomonas, Acinetobacter, Enterobacter, indole-positive Proteus, or Serratia

2

Cefaclor (Ceclor, Distaclor, Keflor, Raniclor), Cefonicid (Monocid), Cefprozil (cefproxil; Cefzil), Cefuroxime (Zefu, Zinnat, Zinacef, Ceftin, Biofuroksym,[13] Xorimax), Cefuzonam, second-generation cephalosporins with antianaerobe activity: Cefmetazole, Cefotetan, Cefoxitin. The following cephems are also sometimes grouped with second-generation cephalosporins: Carbacephems: loracarbef (Lorabid); Cephamycins: cefbuperazone, cefmetazole (Zefazone), cefminox, cefotetan (Cefotan), cefoxitin (Mefoxin), Cefotiam (Pansporin).

描述

Gram-positive: Less than first-generation.

Gram-negative: Greater than first-generation: HEN (Haemophilus influenzae, Enterobacter aerogenes and some Neisseria + the PEcK described above

3

Cefcapene, Cefdaloxime, Cefdinir (Sefdin, Zinir, Omnicef, Kefnir), Cefditoren, Cefetamet, Cefixime (Fixx, Zifi, Suprax), Cefmenoxime, Cefodizime, Cefotaxime (Claforan), Cefovecin (Convenia), Cefpimizole, Cefpodoxime (Vantin, PECEF), Cefteram, Ceftamere (Enshort), Ceftibuten (Cedax), Ceftiofur, Ceftiolene, Ceftizoxime (Cefizox), Ceftriaxone (Rocephin).

Third-generation cephalosporins with antipseudomonal activity: Cefoperazone (Cefobid), Ceftazidime (Meezat,Fortum, Fortaz).

These cephems are also sometimes grouped with third-generation cephalosporins: Oxacephems: latamoxef (moxalactam).

描述

Gram-positive: Some members of this group (in particular, those available in an oral formulation, and those with antipseudomonal activity) have decreased activity against gram-positive organisms.

Gram-negative: Third-generation cephalosporins have a broad spectrum of activity and further increased activity against gram-negative organisms. They may be particularly useful in treating hospital-acquired infections, although increasing levels of extended-spectrum beta-lactamases are reducing the clinical utility of this class of antibiotics. They are also able to penetrate the central nervous system, making them useful against meningitis caused by pneumococci, meningococci, H. influenzae, and susceptible E. coli, Klebsiella, and penicillin-resistant N. gonorrhoeae. Since August 2012, the third-generation cephalosporin, ceftriaxone, is the only recommended treatment for gonorrhea in the United States (in addition to azithromycin or doxycycline for concurrent Chlamydia treatment). Cefixime is no longer recommended as a first-line treatment due to evidence of decreasing susceptibility.[14] Activity against staphylococci and streptococci is less with the third-generation compounds than with the first- and second-generation compounds.[15]

4

Cefclidine, cefepime (Maxipime), cefluprenam, cefoselis, cefozopran, cefpirome (Cefrom), cefquinome These cephems are also sometimes grouped with fourth-generation cephalosporins: Oxacephems: flomoxef

Note:Cefquinome is not approved for human use. It is for veterinary medicine.

描述

Gram-positive: They are extended-spectrum agents with similar activity against Gram-positive organisms as first-generation cephalosporins.

Gram-negative: Fourth-generation cephalosporins are zwitterions that can penetrate the outer membrane of Gram-negative bacteria.[16] They also have a greater resistance to β-lactamases than the third-generation cephalosporins. Many can cross the blood–brain barrier and are effective in meningitis. They are also used against Pseudomonas aeruginosa.

5

Ceftobiprole, ceftaroline, ceftolozane

 

Ceftobiprole has been described as "fifth-generation" cephalosporin,[17][18] though acceptance for this terminology is not universal. Ceftobiprole has powerful antipseudomonal characteristics and appears to be less susceptible to development of resistance. Ceftaroline has also been described as "fifth-generation" cephalosporin, but does not have the antipseudomonal or VRE coverage of ceftobiprole.[19] Ceftolozane is a new option for treatment of Complicated Intra-abdominal Infections (cIAI), and Complicated Urinary Tract Infections (cUTI). Ceftolozane is combined with the β-lactamase inhibitor tazobactam, as multi-drug resistant bacterial infections will generally show resistance to all β-lactam antibiotics unless this enzyme is inhibited.

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