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Pharmacology II Antibacterial Agents
Pharmacology II Antibacterial Agents
79
Pharmacology
Professional
02/20/2012

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Term
Penicillins
Definition
β-lactam antibiotics; ADRs: GI (N/V/D); nephritis, cation toxicity, neurotoxicity (seizures) at high levels
Term
Cephalosporins
Definition
β-lactam antibiotics; can cause severe pain at I.M. site, thrombophlebitis with I.V., intestinal nephritis and tubular necrosis; never give to anyone that has had an anaphylactic reaction to penicillin
Term
Carbapenems
Definition
β-lactam antibiotics; broadest spectrum; more affinity for PBP; β-lactamase resistant; can cause N/V/D, hypersensitivity rxns, local rxns, seizures; drugs of choice for extended spectrum β-lactamase infections; TREAT P. AERUGINOSA w/o aminoglycoside
Term
Monobactams
Definition
β-lactam antibiotics
Term
Fosfomycin
Definition
Non-β-lactam Cell Wall Synthesis Inhibitor; oral; broad spectrum; inhibits enol pyruvate transferase preventing the conversion of NAG to NAM stopping the crosslinking of peptide and glycan
Term
Cycloserine (no longer on market)
Definition
Non-β-lactam Cell Wall Synthesis Inhibitor
Term
Bacitracin
Definition
Non-β-lactam Cell Wall Synthesis Inhibitor; topical; prevents the dephosphorylation of isoprenyl pyrophosphate, a lipid that transports peptidoglycan building blocks across the plasma membrane; Gram +; Neisseria, T. Pallidum
Term
Vancomycin
Definition
Non-β-lactam Cell Wall Synthesis Inhibitor; Slow I.V. infusion only; D-Ala - D-Ala terminus preventing elongation and cross-linking of the peptidoglycan layers; only active against G+; ACTIVE AGAINST MRSA & MRSE; can cause red man syndrome, ototoxicity, nephrotoxicity, phlebitis
Term
β-lactams
Definition
Cell wall synthesis inhibitors; inhibit PBP and prevent the crosslinking of peptidoglycan layers
Term
Penicillin G (benzylpenicillin)
Definition
Natural Penicillin; mostly used for g+ streptococci, meningococci, and T.Pallidum (syphilis); Parenteral (acid labile)
Term
Penicillin V
Definition
Natural Penicillin; indicated for minor infections due to poor oral bioavailability and reduced activity; also requires qid dosing; (oral)
Term
Methicillin (withdrawn from market)
Definition
Antistaphylococcal Penicillin
Term
Nafcillin
Definition
Antistaphylococcal Penicillin; IV
Term
Oxacillin
Definition
Antistaphylococcal Penicillin; oral but IV if serious staph infection; biliary and renal elimination; no dosing adjustment in renal failure
Term
Dicloxacillin
Definition
Antistaphylococcal Penicillin; oral; renally and biliary elimination but no dose adjustment required
Term
Ampicillin, Amoxicillin
Definition
Aminopenicillins - extended spectrum penicillins; only ones that are orally administered but ampicillin is also given IV; haemophilus, proteus, e.coli
Term
Ticarcillin
Definition
Carboxypenicillins; extended spectrum penicillins; I.V.; pseudomonas, proteus, H. influenzae, E.coli; can cause platelet dysfunction
Term
Piperacillin
Definition
Ureidopenicillins; extended spectrum penicillins; I.M.; effective against PSEUDOMONAS AERUGINOSA (usually with aminoglycoside)
Term
Natural Penicillins
Definition
Narrow spectrum, active only against G+ (aerobes and some anaerobes), staphylococci are resistant (β lactamase producing bacteria); some bacilli; drug of choice against spriochetes (T. Pallidum); bacterial resistance = β-lactamase
Term
Clavulanate
Definition
β-lactamase inhibitor given with amoxicillin (Augmentin) and with Ticarcillin (Timentin)
Term
Sulbactam
Definition
β-lactamase inhibitor given with ampicillin (Unasyn)
Term
Tazobactam
Definition
β-lactamase inhibitor given with piperacillin
Term
Cefadroxil
Definition
First generation cephalosporin; oral
Term
Cefazolin
Definition
First generation cephalosporin; I.V.
Term
Cephalexin
Definition
First generation cephalosporin; oral
Term
Cefaclor
Definition
Second generation cephalosporin; oral only
Term
Cefprozil
Definition
Second generation cephalosporin; oral only
Term
Cefuroxime
Definition
Second generation cephalosporin; I.V. and I.M.
Term
Cefoxitin
Definition
Second generation cephalosporin; a cephamycin; the only lone I.V. 2nd gen cephalosporin
Term
Cefotetan
Definition
Second generation cephalosporin; a cephamycin; I.V. and I.M.
Term
Cefixime
Definition
Third generation cephalosporin; oral only
Term
Cefdinir
Definition
Third generation cephalosporin; oral only
Term
Cefpodoxime
Definition
Third generation cephalosporin; oral only
Term
Ceftibuten
Definition
Third generation cephalosporin; oral only
Term
Cefotaxime
Definition
Third generation cephalosporin; I.V. only
Term
Ceftazidime
Definition
Third generation cephalosporin; I.V. and I.M.
Term
Ceftizoxime
Definition
Third generation cephalosporin; I.V.
Term
Ceftriaxone
Definition
Third generation cephalosporin; I.V. and I.M.
Term
Cefepime
Definition
Fourth generation cephalosporin; I.V. and I.M.; better against G+ than 3rd gen; better against β-lactamases (enterobacter); ACTIVE AGAINST P. AERUNGINOSA
Term
Ceftaroline
Definition
Fifth generation cephalosporin; I.V. only; ACTIVE AGAINST MRSA
Term
Imipenem
Definition
Carbapenem; I.V.; must be administered with cilastain to prevent deactivation by dehydropeptidases in renal tubule
Term
Tetracyclines
Definition
Bacterial protein synthesis inhibitors at the ribosomal 30S subunit; block tRNA from entering the A site of the ribosome; broad spectrum more against G+ and atypical bacteria; ACTIVE AGAINST MRSA; don't take with dairy, iron, ca, multivitamin, or antacids; can accumulate in forming bone or teeth, N/V/D, SUPERINFECTIONS, photosensitivity, hepatotoxicity renal toxicity, teeth discoloration; bacterial resistance through efflux, ribosomal protection (protein prevents binding), enzyme inactivation
Term
Aminoglycosides
Definition
Bacterial protein synthesis inhibitors at the ribosomal 30S subunit (bactericidal); they interfere with the initiation complex, cause misreading of mRNA, and block movement of the ribosome on the mRNA; significant PAE and concentration dependent; G- aerobes including P.AERUGINOSA but not active against anaerobes; bacterial resistance through enzymatic deactivation, ribosome mutation, and decreased cell entry; can cause ototoxicity, renal toxicity, muscular block, and should not be given in pregnancy
Term
Spectinomycin
Definition
Bacterial protein synthesis inhibitors at the ribosomal 30S subunit; like aminoglycosides but not all 3 MOAs; mostly active against G-; can cause nephrotoxicity and anemia rarely
Term
Macrolides
Definition
Bacterial protein synthesis inhibitors at the ribosomal 50S subunit; block movement of the ribosome on the mRNA and bind close to the same sites as clindomycin and streptogramins; can stimulate GI motility leading to ab pain, cramping, N/V/D, QT prolongation, and ototoxicity; CYP34A inhibitors and can interact with theophylline, warfarin, cyclosporine, and methylprednisolone; bacterial resistance through efflux pump and MLSb
Term
Lincosamides
Definition
Clindamycin; Bacterial protein synthesis inhibitors at the ribosomal 50S subunit with same MOA as macrolides
Term
Streptogramins
Definition
Bacterial protein synthesis inhibitors at the ribosomal 50S subunit; Qunuprustin same MOA as macrolides and Dalfoprisin binds nearby synergistically; mostly active against G+ and VRSA AND VRE; bacterial resistance through MLSb and enzymatic inactivation; can cause pain and phlebitis at inj. site; also a CYP3A4 inhibitor
Term
Chloramphenicol
Definition
Bacterial protein synthesis inhibitors at the ribosomal 50S subunit; prevents tranpeptidation (handing off of peptide from site A to B); broad spectrum against G+/- , rickettsia, and anaerobes; can cause GRAY BABY SYNDROME, N/V/D, bone marro disturbances (lowered RBC count and AA); BBW for aplastic anemia
Term
Oxazolidinones
Definition
Bacterial protein synthesis inhibitors at the ribosomal 50S subunit and prevents the formation of the ribosome complex; mostly G+ and VRSA and VRE; bacterial resistance through mutation of the binding site; can cause serotonin syndrome with other serotonergic drugs; hematologic disturbances (thrombocytopenia, anemia, neutropenia)
Term
Demeclocycline
Definition
Tetracycline; Oral only
Term
Doxycycline
Definition
Tetracycline; Oral only
Term
Minocycline
Definition
Tetracycline; Oral, I.V.
Term
Tigecycline
Definition
Glycylcycline; I.V. and the only I.M.; a tetracycline derivative
Term
Streptomycin
Definition
Aminoglycoside; I.M. only
Term
Gentamicin
Definition
Aminoglycoside, I.V and I.M.
Term
Tobramycin
Definition
Aminoglycoside; I.V. and I.M.; EFFECTIVE AGAINST P. AERUGINOSA
Term
Kanamycin
Definition
Aminoglycoside; I.V. and oral but only local effect orally
Term
Neomycin
Definition
Aminoglycoside; topical and oral but only local effect orally
Term
Amikacin
Definition
Aminoglycoside
Term
Erythromycin
Definition
Macrolide; oral and I.V.; less against anaerobes
Term
Clarithromycin
Definition
Macrolide; oral; more against anaerobes
Term
Azithromycin
Definition
Macrolide; oral and I.V.; more against anaerobes and also against chlamydia
Term
Telithromycin
Definition
Ketolide; oral; macrolide derivative BBW'd for hepatotoxicity and use in those with myasthenia gravis
Term
Clindamycin
Definition
Lincosamide; Oral and I.V.; most G+ anaerobes but not against aerobic G-; can cause N/V/D, ab pain, pseudomembraneous colitis, neutropenia, impaired hepatic function, local rxns; bacterial resistance through MLSb
Term
Quinupristin/Dalfpristin
Definition
Streptogramin
Term
Linezolid
Definition
Oxazolidinone; Oral and I.V.
Term
Probencid
Definition
gout medication that is sometimes coadministered with natural penicllins because it reduces their renal secretion and prolongs their activity
Term
Cilastatin
Definition
A dehydropeptidase inhibitor co-administered with imipenem to ensure its efficacy
Term
Antistaphylococcal Penicillins
Definition
β-lactam antibiotics; effective against G+ that produce β-lactamases but not MRSA or MRSE; bacterial resistance through PBP alteration
Term
Extended Spectrum Penicillins
Definition
β-lactam antibiotics; active against G+ and G- due to enhanced ability to penetrate outer membrane; bacterial resistance through β-lactamase; renally cleared and require dose adjustment in kidney failure
Term
First Generation Cephalosporins
Definition
cephalosporins that have the broadest spectrum of activity and are effective against G+ cocci and G- bacilli (e. coli, klebisella, proteus)
Term
Second Generation Cephalosporins
Definition
cephalosporins with activity against K. Pneumonia and increased activity against other G- and β-lactamase producing bacteria
Term
Meropenem
Definition
Carbapenem; I.V.
Term
Ertapenem
Definition
Carbapenem; only one administered I.M.
Term
Poripenem
Definition
Carbapenem; I.V.
Term
Azetreonam
Definition
Monobactam; I.V.; active against G- Aerobes including pseudomonas
Term
VRSA
Definition
Vancomycin resistance through overexpression of D-ALA termini, outcompeteing vancomycin
Term
VRE
Definition
Vancomycin resistance by changing the D-Ala - D-Ala terminus to either a D-Ala - D-Lac or D-Ser terminus, both of which have a lower affinity for vancomycin
Term
Cephamycins
Definition
second generation cephalosporins that are more active against anaerobes but can cause disulfram like rxns. and hypoprothrombopenia; cefoxitin and cefotetan
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