Antibacterial Agents (excluding J04 antimycobacterials)

Antibacterial classes and individual agents within classes are displayed below, as well as a brief outline of activity and mode of action. For each class and agent the corresponding anatomical therapeutic chemical (ATC) classification is added in brackets. The ATC is the internationally recognised and World Health Organisation endorsed drug classification system.

ANTIBACTERIAL CLASS
(ATC pharmacological subgroup & chemical subgroup where relevant)

AGENTS WITHIN CLASS

(ATC chemical substance)

Aminoglycosides(J01G) (J01GB) Active against a broad spectrum of Gramnegative organisms, including Pseudomonas aeruginosa. Gentamicin is the agent of choice in most cases. Sometimes used in combination with a beta-lactam or glycopeptide for the treatment of enterococcal infections. Mode of action: Inhibit protein synthesis causing disruption of bacterial cell wall.

amikacin (J01GB06) gentamicin (J01GB03) neomycin (J01GB05) netilmicin (J01GB07) (discontinued 2004) tobramycin (J01GB01)
(Also includes streptomycin - available through the Special Access Scheme.).

Cephalosporins (beta-lactam bicyclic structure)(J01D) st 1. 1 generation (J01DB) cephalexin (J01DB01) (moderate spectrum mainly Gram +ve cephalothin (J01DB03) activity, also some Gram-ve e.g. E. coli, cephazolin (J01DB04) Klebsiella species)
2.

2nd generation (J01DC) (moderate spectrum with activity against Haemophilus influenzae) 2nd generation-cephamycins (J01DC) (moderate spectrum with activity against anaerobes) 3rd generation (J01DD) (broad spectrum active against most enteric Gram-ve rods, but less active against staphylococci than 1 or 2nd generation) 3rd generation (J01DD) (broad spectrum with anti-pseudomonal activity) 4th generation (J01DE) (broad spectrum with anti-pseudomonal activity greater activity against Gram +ve organism than 3rd generation)

cefaclor (J01DC04) cefuroxime (J01DC02) cefotetan (J01DC05) (discontinued 2004) cefoxitin (J01DC01)

3.

4.

cefotaxime (J01DD01) ceftriaxone (J01DD04)

5.

ceftazidime (J01DD02)

6.

cefepime (J01DE01) cefpirome (J01DE02) (discontinued 2006)

As a class, cephalosporins have no useful activity against enterococci or MRSA. Cephalosporins are rarely the drugs of first choice for treatment. Exceptions include cefotaxime or ceftriaxone for empiric therapy of bacterial meningitis. First generation agents are often appropriate for surgical prophylaxis. Mode of action: Interfere with bacterial cell wall peptidoglycan synthesis.


Carbapenems (beta-lactam group bicyclic structure) (J01D) (J01DH) Broadest antimicrobial spectrum of all ertapenem (J01DH03) antimicrobial classes. Have good activity imipenem / cilastatin (J01DH51) against Gram-negative and Gram-positive meropenem (J01DH02) organisms and anaerobes. Meropenem attains doripenem (J01DH04) better levels in the CSF than imipenem and has a lower incidence of seizures; ertapenem is not active against Pseudomonas aeruginosa and Acinetobacter. These drugs are expensive and should be regarded as reserve agents. Mode of action: Inhibit bacterial cell wall synthesis. Penicillins (beta-lactam group bicyclic structure) (J01C) 1. narrow spectrum (lactamase sensitive penicillins) (J01CE) benzylpenicillin (J01CE01) phenoxymethylpenicillin (J01CE02) benzathine benzylpenicillin (J01CE08) procaine benzylpenicillin (J01CE09) dicloxacillin (J01CF01) flucloxacillin (J01CF05) amoxycillin (J01CA04) ampicillin (J01CA01) piperacillin (J01CA12) amoxycillin/clavulanate (J01CR02) piperacillin/tazobactam (J01CR05) ticarcillin/clavulanate (J01CR03)

2. narrow spectrum, anti-staphylococcal (lactamase resistant penicillins) (J01CF) 3. Extended spectrum (J01CA)

4. penicillin/-lactamase inhibitor combinations (broad spectrum +/- antipseudomonal activity) (J01CR)

Narrow spectrum penicillins are active mainly against Gram-positive organisms. Extended, broad spectrum or broad spectrum with anti-pseudomonal activity have additional and increasing activity against Gram-negative organisms. Addition of a -lactamase inhibitor extends the spectrum of activity to cover many -lactamase-producing Gram-positive and Gram-negative organisms, including Gram-negative anaerobes. Monobactams (beta-lactam group monocyclic structure) (J01D) (J01DF) Active against Gram-negative aerobic organisms eg Pseudomonas aeruginosa. Gram-positive organisms and anaerobes are resistant. Mainly used in the treatment of serious Gram-negative infections where there is a history of severe allergic reaction to other -lactam antibiotics. Caution should be used as cross-allergenicity is rare but may occur. Mode of action: Inhibit bacterial cell wall synthesis. Fluoroquinolones (J01M) (J01MA) Have excellent activity against Gram-negative bacteria and some activity against grampositive bacteria. There is increasing resistance to quinolones therefore should be reserved for proven or suspected infections where alternative agents are ineffective or contraindicated. Mode of action: Inhibit bacterial DNA synthesis. ciprofloxacin (J01MA02) gatifloxacin (J01MA16) (discontinued 2006) moxifloxacin (J01MA14) norfloxacin (J01MA06) ofloxacin (J01MA01) aztreonam (J01DF01)


Glycopeptides (J01X) (J01XA) Narrow spectrum of activity against Grampositive aerobic and Gram-positive anaerobic bacteria. Vancomycin is currently the recommended agent in this class; teicoplanin is usually reserved for those intolerant of vancomycin. Due to increasing resistance vancomycin use should be restricted. Mode of action: Preventing formation of bacterial cell wall components thereby causing inhibition of bacterial cell wall synthesis. Lincosamides (J01F) (J01FF) Active against staphylococci, streptococci, most anaerobes and some protozoa. Usually used as an alternative in patients with severe allergy to penicillins and cephalosporins. Mode of action: synthesis. Inhibit bacterial protein clindamycin (J01FF01) lincomycin (J01FF02) teicoplanin (J01XA02) vancomycin (J01XA01)

Macrolides (J01F) (J01FA) Broad spectrum of activity including Grampositive and some Gram-negative bacteria. Also active against M. pneumoniae, Treponema pallidum, Bordetella pertussis and Chlamydia, Legionella, Campylobacter, and Borrelia spp. Not active against enterococci. Mode of synthesis action: Inhibit bacterial protein azithromycin (J01FA10) clarithromycin (J01FA09) erythromycin or erythromycin ethylsuccinate (J01FA01) roxithromycin (J01FA06)

Imidazoles (J01X) (J01XD) Antimicrobial spectrum encompasses Gramnegative anaerobes, Gram-positive anaerobes and anaerobic protozoa. Mode of action: Active metabolites are thought to interfere with DNA synthesis Nitrofurans (J01X) (J01XE) Active against urinary pathogens, except Pseudomonas aeruginosa, Proteus and some Enterobacter spp. Mode of action: Inhibit bacterial protein, DNA, RNA and cell wall synthesis. Oxazolidinones (J01X) (J01XX) Active mainly against Gram-positive organisms such as staphylococci (including MRSA), streptococci and vancomycin-resistant enterococci. Indicated for use in serious infections due to these organisms where other agents are contraindicated or inappropriate. Mode of action: synthesis. Inhibit bacterial protein linezolid (J01XX08) nitrofurantoin (J01XE01) metronidazole (J01XD01) tinidazole (J01XD02)


Polymyxins (J01X) (J01XB) Prophylaxis against respiratory infection with Pseudomonas aeruginosa in cystic fibrosis (inhaled). IV form increasingly used to treat multi drug-resistant Gram-positive bacteria. Mode of action: Bind to phospholipids in bacterial cell wall and modify cell wall permeability. colistin (J01XB01)

Rifamycins (miscellaneous) Active against most Mycobacteria, most Grampositive bacteria and some Gram-negative bacteria. Reserved for treating MRSA and mycobacterial infections, and for prophylaxis of meningitis and epiglottitis. Mode of action: polymerase. Inhibit bacterial RNA rifampicin (J04AB03)

Steroids (J01X) (J01XC) Used for serious infections caused by S. aureus, usually restricted to MRSA in combination regimens after initial IV treatment. Resistance develops rapidly if used alone; always combine with another antimicrobial eg rifampicin. Mode of action: synthesis. Inhibit bacterial protein fusidic acid (sodium fusidate) (J01XC01)

Streptogramins (J01F) (J01FG) For severe MRSA or vancomycinresistant Enterococcus faecium infections when other antibiotics are inappropriate. Mode of action: In combination, quinupristin and dalfopristin work synergistically to inhibit bacterial protein synthesis. quinupristin/dalfopristin (J01FG02) pristinamycin (J01FG01) (available
SAS)

through

Tetracyclines (J01A) (J01AA) Have a broad spectrum of activity which includes Gram-positive and Gram-negative bacteria, Chlamydia, Rickettsia, Mycoplasma, spirochetes, some non-tuberculous mycobacteria and some protozoa. Doxycycline is the preferred choice in most situations. Tigecycline is a glycylcycline (tetracycline derivative) which may be administered intravenously. Mode of synthesis action: Inhibit bacterial protein doxycycline (J01AA02) minocycline (J01AA08) tetracycline (J01AA07) tigecycline (J01AA12)


Miscellaneous Sulphonamides and trimethoprim (J01E) (J01EA,J01EE) trimethoprim (J01EA01) trimethoprim/sulfamethoxazole (J01EE01) chloramphenicol (J01BA01) Other (J01X) (J01XX) daptomycin (J01XX09)

Amphenicols (J01B) (J01BA)

Further information relating to the antimicrobial spectrum of particular agents is available in a number of texts, including the latest versions of the Therapeutic Guidelines Antibiotic and the Australian Medicines Handbook.

Version2 January2010