Table 1
INHIBIT
CLASSIFICATION
ANTIBIOTICS Beta-lactamase Beta-lactamase sensitive Natural Penicillins (narrow spectrum)
Penicillin G (Benzylpenicillin): (Benzylpenicillin): Procainic ( !pain w/ IM), Benzathine ( depot IM) Penicillin V (Phenoxymethylpenicillin): (Phenoxymethylpenicillin): PO
Aminopenicillins (broad spectrum)
Ampicillin (IM/IV (IM/IV - poorly absorbed orally; hence, risk for C. Difficile) Amoxicillin (PO) Positively charged amino group enhances their uptake through bacterial porin (G -ve) channels. Change in Porin Structure -> Pseudomonas becoming resistant. resistant.
Beta-lactamase Beta-lactamase resistant (very narrow spectrum) Staphylococc Staphylococcus us aureus
change in PBPs -> MRSA
Penicillins Methicillin (no longer made)
Nafcillin
Oxacillin
Antipseudomonal (extended spectrum) Antipseudomonal Carboxypenicillins
Cell Wall S y n t h e s i s
Ureidopenicillins
Beta Lactams
1st Generation (long t1/2 , surgicalprophylaxis)
Cephalosporins Not effective for the LAME bacterias Listeria (Amoxicillin often in combination w/
2nd Generation
Atypicals (Macrolides, Tetracyclins) MRSA (Vancomycin) Enterococci (Amoxicillin often in combination
3rd Generation
(Empirical Rx of Sepsis & Meningitis, except Cefoperazone)
w/ Aminoglycosides)
Carbapenems (Beta-lactamaseresistant)
Monobactams
beta-lactamase sensitive
Ticarcillin Carbenicillin Piperacillin Azlocillin Mezlocillin Cefazolin
Cephalexin
Cefadroxil
Cephalotin
Cefuroxime (1st to cross BBB)
Cefoxitin
Cefotetan
Cefaclor
Cefonicid
Cefamandole
Cefmetazole
Cefprozil
Cefoperazone
Ceftriaxone
Ceftazidime
Cefpodoxime
Ceftizoxime
Cefotaxime
Cefixime
Ceftibuten
Cefdinir
Cefditoren
Ertapenem
Doripenem
Cephadrine
4th Generation
Cefepime (Beta-lactamase resistant)
5th Generation
Ceftaroline
Meropenem
Imipenem (1 in q 2 pts suffer a seizure w/ use) + Cilastatin (dehydropeptidase inhibitor)
Aztreonam (alternative Aztreonam (alternative for persons allergic to cephalosporins and infected with a G -ve rod) rod ) (Beta-lactamase
Beta-lactamase Beta-lactamase inhib.
Sulbactam
Tazobactam
Clavulonic Acid
Glycopeptides
Vancomycin
(Red man syndromehistamine induced vasodilation, ototoxicity, nephrotoxicity)
Bacitracin
Teicoplanin
Polymyxin B
Gentamycin
Amikacin
Neomycin
Tobramycin
Not a ! Lactam
Aminoglycosides BC
Flucloxacillin
(Better G -ve
coverage)
Aminoglycosides)
BC
Dicloxacillin
(contact dermatitis)
resistant)
use O2 dependent uptake system anaerobes innately resistant. Nephrotoxicity, Ototoxicity, NeuromuscularBlockade: ! Ach release. Resistance: conjugating enzymes (acetyltransferases)
30S
Tetracyclins
DOC for Rickettsia,Borrelia burgdorferi. Chelators. Resistance: PUMPS. CI; pregnancy & children
Streptomycin (DOC for Bubonic plague, Tularemia) a)
Doxycycline DOC for Borrelia
Tetracyclin Tetracyclin
burgdorferi (Lyme Disease)
Demeclocyclin Demeclocyclin Blocks
Minocyclin Minocyclin Dentistry
Tigecyclin Tigecyclin
ADH receptor; Rx for SIADH
Chloram phenicol phen icol Phenyl group; lipid soluble. Neonates; Grey baby syndrome, Kernicterus. Dose-dependent bone marrow suppression
Protein Synthesis
Macrolide DOC: Legionella.
Erythromycin Erythromycin
Azithromycin Azithromycin
Clindamycin S. Aureus,
Lincomycin
Clarithromycin Clarithromycin
Telithromycin
Also used for: Atypicals, C. jejuni, MAC, H. pylori. Stim. motilin recep. Resistance:Methylated binding site
50S
Lincosamides
Ketolide: macrolide-resistant Strep. pneumonia
Anaerobes. Conc in Bone (Rx Osteo.) Strong link w/ pseudo. colitis
Linezolid VRSA, VRE. Bone marrow suppression (thrombocytopenia) Streptogramins
Quinupristin Quinu pristin/Dalfo /Dalfopristin pristin VRSA, VRE
Floroquinolones G(-) Osteo: Pseudo A. DNA topoisomerases topoisomerases BC
UTI, STDs, travellers diarrhoea. Tendonitis; tendon rupture. CI; pregnancy & children
Ciprofloxacin Ciprofloxacin (2 (2nd)
Norfloxacin floxacin (2 (2nd)
Ofloxacin floxacin (2 (2nd)
Enofloxacin floxacin (2 (2nd)
Levofloxacin Levo floxacin (3 (3rd)
floxacin (3 Sparfloxacin (3rd)
floxacin (4 Moxifloxacin (4th)
Gemi floxacin (4th)
Ag Sulfadiazi Sulfadiazine ne (burns) (burns)
Sulfasalazine (UC, RA)
Sulfisoxazole
Pirymethamine-sulfadiazine: Cerebral Toxoplasmosis
Prodrug; 5-aminosalicylic acid (UC) & sulfapyridine (RA)
(1st)
Quinolones
Nalidixic acid
Sulfonamides Dihydropteroate
Sulfametho Sulfamethoxazol xazole e (SMX)
synthetase (not found in humans) inhibitor. neonate; Kernicterus. Steven-Johnson syndrome
Folic acid synthesis TMP/SMX: Nocardia (DOC), Travellers Diarrhoea, P. Jiroveci
Sulfone
Dapsone (Diaminodiphenyl sufone, DDS) Competitive inhibitor of Dihydropteroate synthetase. SLE-like syndrome w/ slow acetylators. Used in combination with CLOFAZIMINE (binds to the guanine bases of bacterial DNA, thereby blocking the template function of the DNA and inhibiting bacterial proliferation) &/orRIFAMPIN &/orRIFAMPIN for for Leprosy Rx. DERMATITIS HERPETIFORMIS Rx. HERPETIFORMIS Rx.
DHFR inhibitors DNA (damage) BC
Metronidazole (free radicals)
mRNA synthesis BC
Rifampin
Tr im im et et ho ho pr pr im im ( TM TM P) P)
P irir ym ym et et ha ha mi mi ne ne
DOC: C. Difficile; Pseudo. Colitis. Anaerobes. Antiprotozoal: Giardia, Trichomonas, Entamoeba.
