antimicrobials

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Table 1 INHIBIT CLASSIFICATION ANTIBIOTICS Cell Wall S y n t h e s i s 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 Ticarcillin Carbenicillin Ureidopenicillins Piperacillin Azlocillin Mezlocillin Cephalosporins Not effective for the LAME bacterias Listeria (Amoxicillin often in combination w/ Aminoglycosides) Atypicals (Macrolides, Tetracyclins) MRSA (Vancomycin) Enterococci (Amoxicillin often in combination w/ Aminoglycosides) 1 st Generation (long t1/2 , surgical prophylaxis) Cefazolin Cephalexin Cefadroxil Cephalotin Cephadrine 2 nd Generation (Better G -ve coverage) Cefuroxime (1 st to cross BBB) Cefoxitin Cefotetan Cefaclor Cefonicid Cefamandole Cefmetazole Cefprozil 3 rd Generation (Empirical Rx of Sepsis & Meningitis, except Cefoperazone) Cefoperazone Ceftriaxone Ceftazidime Cefpodoxime Ceftizoxime Cefotaxime Cefixime Ceftibuten Cefdinir Cefditoren 4 th Generation Cefepime (Beta-lactamase resistant) 5 th 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 topoisomerases BC Floroquinolones G(-) Osteo: Pseudo A. UTI, STDs, travellers diarrhoea. Tendonitis; tendon rupture. CI; pregnancy & children Ciprofloxacin (2 nd ) Norfloxacin (2 nd ) Ofloxacin (2 nd ) Enofloxacin (2 nd ) Levofloxacin (3 rd ) Sparfloxacin (3 rd ) Moxifloxacin (4 th ) Gemifloxacin (4 th ) Quinolones Nalidixic acid (1 st ) 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

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Schema of antimicrobials

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Page 1: Antimicrobials

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