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Host Defense Drugs
N/A
30
Science
Pre-School
03/29/2014

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Term
Penicillin
Definition
Penicillin G: acid labile, highly potent
Penicillin V: acid stable, low potency
Beta lactam ring + thiazolidine ring (1 R group)
Narrow spectrum: Gram + bacilli/cocci, Gram – cocci and spirochetes
Term
Cephalosporin
Definition
Beta lactam ring + dihydrothiazine ring (2 R groups)
Wider spectrum
Term
Beta lactamase inhibitors
Definition
Clavulanic acid
Sulbactam
Tazobactam
Term
Vancomycin
Definition
Inhibits cell wall synthesis
Bactericidal
Narrow spectrum (only gram +)
Used primarily in treatment of clostridium dificile
Term
Bacitracin
Definition
Inhibits cell wall synthesis
Bactericidal
Very nephrotoxic (DON’T GIVE IV)
Primarily in topical ointments and bowel sterilization
Term
Mycobacterial infection drugs
Definition
All inhibit cell wall synthesis
Isoniazid
Ethionamid
Ethambutol
Cycloserine
Term
Antibiotics that inhibit protein synthesis
Definition
Aminoglycosides
Tetracyclines
Chloramphenicol
Macrolides
Lincosamides
Streptogramins
Oxazolidinones
Term
Antibiotics that inhibit folic acid synthesis
Definition
Sulfonamides
Dapsone and Para-aminosalicyclyic acid
Trimethoprim
Cotrimoxazole
Term
Antibiotics that inhibit nucleic acid function
Definition
Metronidazole
Rifampin
Nalidixic acid
Quinolones
Term
Antibiotics that interact with cytoplasmic membrane
Definition
Polymixin
Daptomycin
Term
Other beta lactam antibiotics
Definition
Carbapenems (broad spectrum)
Monobactam (narrow spectrum)
Term
Aminoglycosides (Streptomycin)
Definition
Taken up via O2 dependent process (doesn’t work in aneorobic conditions)
Bactericidal: irreversible binding to ribosomal subunit
Poorly absorbed (give IV), and has narrow spectrum (Gram -)
Side effects: ototoxic and nephrotoxic
Resistance mechs:
Enzyme modification: antibiotic specific (can use diff aminoglycoside)
Decreased uptake/increased expulsion/mutation of binding site
These mechs result in cross resistance for all aminoglycosides
Term
Tetracyclines (-cyclines)
Definition
(From streptomyces)
Bacteriostatic: reversible binding to ribosomal subunit
Broad spectrum, oral absorption
Side effects: discoloration of teeth and GI effects
If resistant to one, the bacteria is resistanct to all
Mechs of resistance: less permeable, active efflux, alteration of ribosomal binding site, and enzymatic modification
Term
Chloramphenicol
Definition
Bacteriostatic: reversible binding to ribosomal subunit
Broad spectrum, oral absorption
Side effects: Bone marrow depression [dose dependent] (anemia, leukopenia, thrombocytopenia) and aplastic anemia (dose independent)
Mechs of resistance: acetyl transferase and mutation of OMPs
Term
Macrolides (Erythromycin, azithromycin)
Definition
Bacteriostatic, binds to ribosomal subunit
Broad spectrum
Mechs of resistance: alteration of ribosomal subunit; esterase
Term
Lincosamides (Clindamycin)
Definition
Mostly for anaerobic bacteria; important in MRSA
Bacteriostatic: binds to ribosomal subunit
Mechs of resistance: alteration of ribosomal subunit
High incidence of GI effects and causing c. dificile
Term
Streptogramins (Synercid)
Definition
Bactericidal: inhibits protein synthesis by binding ribosomal subunit and prematurely releasing the growing peptide
For use in Gram + bacteria: imp in Vancomycin-resistant Enterococcus
Hepatotoxic side effects
Term
Oxazolidinones (Linezolid)
Definition
Bacteriostatic: inhibits protein synthesis at ribosome
Useful for VREF and MRSA
Side effects: interaction with OTC cold meds
Term
Sulfonamides
Definition
Bacteriostatic, broad spectrum, competitive inhibitor for PABA
Used in UTI’s, GI infections, and topical applications
Side effects: hypersensitivity and blood abnormalities
Mechs of resistance
Overproduction of PABA
Alteration of tetrahydropteroic acid synthetase
Folic acid dependency
Decreased permeability
Term
Dapsone and Para-aminosalicyclic acid
Definition
Structure, mechanism of action and resistance similar to sulfonamides
Narrow spectrum: mycobacteria
Term
Trimethoprim
Definition
Structure: 2,4-diaminopyrimidine
Bacteriostatic: inhibitor of DHF reductase
Used for UTI’s and traveler’s diarrhea
Pharmacology is same as sulfonamides
Side effects: hypersensitivity and blood abnormalities
Mech of resistance:
Overproduction of DHF acid
Alteration of DHF reductase
Folic acid dependency
Decreased permeability
Term
Cotrimoxazole
Definition
Trimethoprim + sulfamethoxazole
When combined with the other folic acid synthesis inhibitor, it becomes bactericidal since you’ve inhibited 2 steps
Term
Metronidazole
Definition
Bactericidal, narrow spectrum (anaerobic bacteria and anaerobic protozoa) Trichomonas vaginalis
Breaks down DNA, RNA, protein
Side effects: alcohol interaction
Term
Rifampin
Definition
Broad spectrum, inhibits DNA-dependent RNA polymerase
Useful for mycobacterium tuberculosis; resistance develops fairly quickly
Side effects: skin rashes and thrombocytopenia
Mech of resistance: alteration of RNA polymerase
Term
Nalidixic acid
Definition
Inhibits bacterial DNA gyrases and topoisomerases
Narrow spectrum (Gram -), not very potent; usually for UTI’s
Term
Quinolones
Definition
Broad spectrum (+ and -) , oral administration
Inhibits bacterial DNA dependent gyrase and topoisomerases
GI side effects
Mechs of resistance:
Alteration of bacterial DNA gyrase/topoisomerases
Alteration of outer membrane proteins
Export of antimicrobial agent through efflux pumps
Term
Polymixin
Definition
Polymixin E = colistin
Bactericidal, cationic detergent, disrupts cell membrane
Narrow spectrum (Gram – bacilli)
Used in topical ointments + bacitracin, neomycin
Used orally for gut sterilization
Used in systemic infections (acinetobacter and pseudomonas)
Side effects: neurotoxic and nephrotoxic
Mech of resistance: alteration of LPS
Term
Daptomycin
Definition
Mech of action: membrane depolarization and disruption of ionic gradients
Narrow spectrum (Gram + bacteria)
Term
Clofazimine
Definition
Lipophilic antibiotic binding to DNA
Treatment of leprosy
Term
Pyrazinamide
Definition
Mech unknown
Treats tuberculosis
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