antimicrobials
DESCRIPTION
Schema of antimicrobialsTRANSCRIPT
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Table 1
INHIBIT CLASSIFICATION ANTIBIOTICS
Cell
Wall
Synthesis
BC
Beta Lactams
Penicillins
Beta-lactamase sensitive
Natural Penicillins (narrow spectrum)
Penicillin G (Benzylpenicillin): Procainic (↓pain w/ IM), Benzathine ( depot IM) Penicillin V (Phenoxymethylpenicillin): PO
Aminopenicillins (broad spectrum)
Ampicillin (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.
Beta-lactamase resistant (very narrow spectrum) Staphylococcus aureus change in PBPs -> MRSA
Methicillin (no longer made) Nafcillin Oxacillin Dicloxacillin Flucloxacillin
Antipseudomonal (extended spectrum) beta-lactamase sensitive
Carboxypenicillins TicarcillinCarbenicillin
UreidopenicillinsPiperacillinAzlocillinMezlocillin
CephalosporinsNot effective for the LAME
bacterias Listeria (Amoxicillin often in combination w/
Aminoglycosides)
Atypicals (Macrolides, Tetracyclins)
MRSA (Vancomycin)
Enterococci (Amoxicillin often in combination w/ Aminoglycosides)
1st Generation (long t1/2 , surgical prophylaxis)
Cefazolin Cephalexin Cefadroxil Cephalotin
Cephadrine
2nd Generation (Better G -ve coverage)
Cefuroxime (1st to cross BBB) Cefoxitin Cefotetan Cefaclor
Cefonicid Cefamandole Cefmetazole Cefprozil
3rd Generation (Empirical Rx of Sepsis & Meningitis, except
Cefoperazone)
Cefoperazone Ceftriaxone Ceftazidime Cefpodoxime
Ceftizoxime Cefotaxime Cefixime Ceftibuten
Cefdinir Cefditoren
4th Generation Cefepime (Beta-lactamase resistant)
5th Generation Ceftaroline
Carbapenems (Beta-lactamase resistant) Meropenem Imipenem (1 in q 2 pts suffer a seizure w/ use) + Cilastatin (dehydropeptidase inhibitor)
Ertapenem Doripenem
Monobactams Aztreonam (alternative for persons allergic to cephalosporins and infected with a G -ve rod) (Beta-lactamase resistant)
Beta-lactamase inhib. Sulbactam Tazobactam Clavulonic Acid
Not a β Lactam
Glycopeptides Vancomycin (Red man syndrome- histamine induced vasodilation, ototoxicity, nephrotoxicity)
Bacitracin Teicoplanin Polymyxin B
Protein Synthesis
30S
Aminoglycosides BC use O2 dependent uptake system - anaerobes innately resistant. Nephrotoxicity, Ototoxicity, Neuromuscular Blockade: ↓ Ach release. Resistance: conjugating enzymes (acetyltransferases)
Gentamycin Amikacin Neomycin (contact dermatitis) Tobramycin Streptomycin (DOC for Bubonic plague, Tularemia)
Tetracyclins DOC for Rickettsia, Borrelia burgdorferi. Chelators. Resistance: PUMPS. CI; pregnancy & children
Doxycycline DOC for Borrelia burgdorferi (Lyme Disease)
Tetracyclin Demeclocyclin Blocks ADH receptor; Rx for SIADH
Minocyclin Dentistry Tigecyclin
50S
Chloramphenicol Phenyl group; lipid soluble. Neonates; Grey baby syndrome, Kernicterus. Dose-dependent bone marrow suppression
Macrolide DOC: Legionella. Also used for: Atypicals, C. jejuni, MAC, H. pylori. Stim. motilin recep.Resistance:Methylated binding site
Erythromycin Azithromycin Clarithromycin Telithromycin Ketolide: macrolide-resistant Strep. pneumonia
Lincosamides Clindamycin S. Aureus, Anaerobes. Conc in Bone (Rx Osteo.) Strong link w/ pseudo. colitis
Lincomycin
Linezolid VRSA, VRE. Bone marrow suppression (thrombocytopenia)
Streptogramins Quinupristin/Dalfopristin VRSA, VRE
DNA topoisomerasesBC
Floroquinolones G(-) Osteo: Pseudo A. UTI, STDs, travellers diarrhoea. Tendonitis; tendon rupture. CI; pregnancy & children
Ciprofloxacin (2nd) Norfloxacin (2nd) Ofloxacin (2nd) Enofloxacin (2nd)
Levofloxacin (3rd) Sparfloxacin (3rd) Moxifloxacin (4th) Gemifloxacin (4th)
Quinolones Nalidixic acid (1st)
Folic acid synthesis TMP/SMX: Nocardia (DOC), Travellers Diarrhoea, P. Jiroveci
Sulfonamides Dihydropteroate synthetase (not found in humans) inhibitor. neonate; Kernicterus. Steven-Johnson syndrome
Sulfamethoxazole (SMX) Ag Sulfadiazine (burns) Pirymethamine-sulfadiazine: Cerebral Toxoplasmosis
Sulfasalazine (UC, RA) Prodrug; 5-aminosalicylic acid (UC) & sulfapyridine (RA)
Sulfisoxazole
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) &/or RIFAMPIN for Leprosy Rx. DERMATITIS HERPETIFORMIS Rx.
DHFR inhibitors Trimethoprim (TMP) Pirymethamine
DNA (damage) BC Metronidazole (free radicals) DOC: C. Difficile; Pseudo. Colitis. Anaerobes. Antiprotozoal: Giardia, Trichomonas, Entamoeba.
mRNA synthesis BC Rifampin