Block 4

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ssbhat
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184945
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Block 4
Updated:
2012-11-23 16:30:26
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Pharmacology
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Antibacterials, thyroid, and more
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  1. Bactericidal
    kills bacteria
  2. Bacteriostatic
    stops active growth of bacteria but they remain viable - host defenses important to eliminate pathogens
  3. MBC
    minimal bactericidal concentration, kills 99.9% bacteria
  4. MIC
    minimal inhibitory (static) concentration
  5. Time-dependent killing
    amount of time above MIC, best clinical effect whe 4-fold above MIC for >50% of total time
  6. Concentration-dependent killing
    maximize peak concentration, Cmax/MIC ratio greater than 8 is best
  7. Killing dependent on concetration X time
    area under the curve

    AUC24/MIC greater than 125
  8. Penicillin G & V
    • V: oral
    • G: injection

    • Use: gram-pos.
    • anaerobes
    • non-beta lactamase producing
    • strep throat
    • limited gram-neg.
    • syphilis

    • Mechanism:
    • inhibit transpeptidases (penicillin-binding proteins) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • anaphylaxis
    • rash, fever
    • diarrhea, enterocolitis
    • increased liver enzymes
    • hemolytic anemia
    • seizures
  9. Oxacillin
    Use: beta-lactamase producing staph (MSSA)

    • Mechanism: inhibit transpeptidases (penicillin-binding proteins) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE: 
    • allergic rxn
    • anaphylaxis
    • rash, fever
    • diarrhea, enterocolitis
    • increased liver enzymes
    • hemolytic anemia
    • seizures
  10. Ampicillin
    • Use:
    • gram +
    • expanded gram -
    • meningitis
    • GI infections

    • Mechanism:
    • inhibit transpeptidases (penicillin-binding proteins) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • anaphylaxis
    • rash, fever
    • diarrhea, entercolitis
    • increased liver enzymes
    • hemolytic anemia
    • seizures
  11. Amoxicillin
    • Use:
    • gram +
    • expanded gram -
    • otitis media

    • Mechanism:
    • inhibit transpeptidases (penicillin-binding proteins) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • anaphylaxis
    • rash, fever
    • diarrhea, enterocolitis
    • increased liver enzymes
    • hemolytic anemia
    • seizures
  12. Ticarcillin
    Use: extended gram(-) spectrum

    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • anaphylaxis
    • rash, fever
    • diarrhea, enterocolitis
    • increased liver enzymes
    • hemolytic anemia
    • seizures
  13. Piperacillin
    Use: extended gram(-) spectrum

    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • anaphylaxis
    • rash, fever
    • diarrhea, enterocolitis
    • increased liver enzymes
    • hemolytic anemia
    • seizures
  14. Clavulanic Acid
    beta-lactam analog, acts as suicide inhibitor (binds irreversibly to beta-lactamase)
  15. Sulbactam
    beta-lactam analog that acts as suicide inhibitor (binds irreversibly to beta-lactamase)
  16. Cefazolin
    • 1st generation cephalosporin
    • best gram + activity of cephalosporins
    • some use for some gram (-)
    • IV/IM

    • uncomplicated skin infections
    • surgical prophylaxis (skin flora)
    • not for meningitis

    • Mechanism: 
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE: 
    • allergic rxns
    • nausea, vomiting, diarrhea, enterocolitis
    • hepatocellular damage
  17. Cephalexin
    • 1st generation cephalosporin
    • gram+
    • some use for some gram(-)
    • oral

    • uncomlicated skin infections
    • surgical prophylaxis (skin flora)
    • not for meningitis

    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • nausea, vomiting, diarrhea, enterocolitis
    • hepatocellular damage
  18. Cefuroxime
    • 2nd generation cephalosporin
    • increased gram(-) activity
    • less active against some gram-pos

    only 2nd generation to penetrate CSF

    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE: 
    • allergic rxn
    • nausea, vomiting, diarrhea, enterocolitis
    • hepatocellular damage
  19. Cefotetan
    • 2nd generation cephalosporin
    • increased gram(-) activity
    • less active against some gram+
    • also good for anaerobes

    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks 
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • nausea, vomiting, diarrhea, eneterocolitis
    • hepatocellular damage
  20. Ceftriaxone
    • 3rd generation cephalosporin
    • more active against gram-
    • used for Klebsiella, Enterobacter, Proteus

    • use: gonorrhea, empiric therapy for meningitis
    • long T1/2


    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE: 
    • allergic rxn
    • nausea, vomiting, diarrhea, enterocolitis
    • hepatocellular damage
  21. Ceftazidime
    • 3rd generation cephalosporin
    • more active against gram-
    • used for Klebsiella, Enterobacter, Proteus

    use: effective against many strains of Ps. aeruginosa, short T1/2, poorest 3rd gen. for gram+

    • Mechanism:
    • inhibit transpeptidases (PBD)s which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • nausea, vomiting, diarrhea, enterocolitis
    • hepatocellular damage
  22. Cefepime
    • 4th generation cephalosporin
    • similar to ceftazidime, except more resistant to type I beta-lactamases

    use:broad gram(-), empircal tx of serious inpatient infections

    • Mechanism:
    • inhibit transpeptidases (PBPs) which catalyze cell wall crosslinks
    • murein hydrolases
    • analog of D-Ala-D-Ala linkage

    • SE:
    • allergic rxn
    • nausea, vomiting, diarrhea, enterocolitis
    • hepatocellular damage
  23. Imipenem
    • broad spectrum beta-lactam
    • resistant to many beta-lactamases, including ESBLs (extended spectrum beta-lactamases)
    • not effective against MRSA
    • given with cilastatin (to extend T1/2)

    • use:
    • mixed or ill-defined infection, those not responsive to resistant to other drugs

    • SE:
    • hypersensitivity; some cross-allergies with penicillins/cephalosporins
    • seizures, dizziness, confusion
    • nausea, vomiting, diarrhea, pseudomembranous colitis; superinfection
  24. Aztreonam
    beta-lactam, used against gram-neg aerobic rods

    not useful against gram+ & anaerobes, not indicated for meningitis

    resistant to many beta-lactamases

    can be used in those w/ known hypersensitivities to penicillins

    • SE:
    • seizures
    • cramps, nausea, vomiting, enterocolitis
    • anaphylaxis, transient EKG changes
  25. Vancomycin
    not beta-lactam

    • mechanism:
    • bactericidal
    • inhibits cell wall synthesis: binds to free carboxyl end (D-Ala-D-Ala) of the pentapeptide; interferes with transpeptidation (crosslinking) and transglycosylation (elongation of the peptidoglycan chains)

    • use: 
    • gram+ only
    • MRSA
    • C. difficile enterocolitis (2nd choice)

    • administration:
    • IV for systemic infections
    • oral for C. difficile enterocolitis

    • SE:
    • red man/red neck syndrome
    • nephrotoxicity
    • phlebitis
    • ototoxicity
  26. Fosfomycin
    Mechanism: inhibits peptidoglycan synthesis by inactivating enolpyruvyl transferase, an early-stage cell wall synthesis enzyme

    Use: uncomplicated UTIs caused by E. Coli, Enterococcus

    SE: headache, diarrhea, nausea, vaginitis
  27. Bacitracin
    not a beta-lactam

    mechanism: interferes with cell wall synthesis by interfering with carrier that moves early wall components through the cell membrane

    Use: topical only, gram+

    SE: allergic dermatitis
  28. Polymyxin B
    Mechanism: cationic detergents that disrupt the bacterial membranes

    • Use: 
    • topical for Pseudomonas and other gram(-) infections
    • systemic use - causes potential serious nephrotoxicity & neurotoxicity
  29. Daptomycin
    Mechanism: binds bacterial membranes, causing rapid membrane depolarization

    • Use:
    • uncomplicated skin and skin structure infections
    • MSSA, MRSA
    • Streptococcus
    • Enterococcus
    • Bactermia
    • Not pneumonia

    • SE:
    • nausea, diarrhea, GI flora alterations
    • muscle pai and weakness
  30. Norfloxacin
    Fluorinated quinolone, well distributed, oral administration

    Mechanism: inhibits DNA gyrase, interfering with control of bacterial DNA supercoiling; bactericidal; killing dependent on AUC24hr/MIC (area under curve)

    Resistance: altered DNA gyrase, decreased permeability

    Use: urinary tract infection

    • SE:
    • nausea, vomiting, abdominal pain, enterocolitis
    • dizziness, headache, restlessness, depression
    • seizures
    • peripheral neuropathy
    • arthropathy, tendon rupture
    • rashes
    • EKG irregularities

    CI: seizure disorder, pregnancy, children
  31. Ciprofloxacin
    Fluorinated quinolone, well distributed, oral administration

    • mechanism: inhibits DNA gyrase, interfering with control of bacterial DNA supercoiling; bactericidal; killing dependent on AUC24hr/MIC (area under curve)
    • Resistance: altered DNA gyrase, decreased permeability

    • Use:
    • urinary tract infections
    • infectious diarrhea
    • skin infections
    • bone and joint infections
    • anthrax

    • SE:
    • nausea, vomiting, abdominal pain, enterocolitis
    • dizziness, headache, restlessness, depression
    • seizures
    • peripheral neuropathy
    • arthropathy, tendon rupture
    • rashes
    • EKG irregularities

    CI: seizure disorder, pregnancy, children
  32. Moxifloxacin
    Fluorinated quinolone, well distributed, oral administration

    mechanism: inhibits DNA gyrase, interfering with control of bacterial DNA supercoiling; bactericidal; killing dependent on AUC24hr/MIC (area under curve)

    Resistance: altered DNA gyrase, decreased permeability

    • Use:
    • better gram+ activity than many quinolones
    • respiratory infections, NOT strep throat
    • community acquired pneumonia, bacterial bronchitis

    • SE:
    • nausea, vomiting, abdominal pain, enterocolitis
    • dizziness, headache, restlessness, depression
    • seizures
    • peripheral neuropathy
    • arthropathy, tendon rupture
    • rashes 
    • EKG irregularities

    CI: seizure disorder, pregnancy, children
  33. Nitrofurantoin
    Mechanism: nitroreductase enzyme converts drug to reactive compound (incl. free radicals) which can damage DNA

    Use: urinary tract infections

    • SE: 
    • nausea, vomiting, diarrhea
    • peripheral neuropathy
    • pulmonary rxns (fibrosis)
    • liver damage
    • granulocytopenia, leukopenia, megaloblastic anemia
    • acute hemolytic anemia
  34. Rifampin
    Mechanism: inhibits bacterial RNA synthesis by binding RNA polymerase B

    Use: pulmonary tuberculosis, prophylaxis meningococcal meningitis, prophylaxis of Haemophilus influenza type b meningitis

    • SE:
    • serious hepatoxicity
    • CYP inducer (inactivates other drugs)
    • Orange color to urine, saliva, sweat, tears
  35. Fidaxomicin
    Mechanism: inhibitor of RNA polymerase, inhibits RNA synthesis, bactericidal

    Use: C. difficile infection

    Administration: oral, poorly absorbed

    • SE:
    • GI upset, GI bleeding
  36. Metronidazole
    Mechanism: anaerobes reduce nitro group, resulting product disrupts DNA

    USE: anaerobes, C. difficile enterocolitis, combination therapy for H. pylori, Gardnerella vaginalis

    • SE:
    • nausea, vomiting, anorexia, diarrhea
    • transiet leukopenia, neutropenia
    • thrombophlebitis after IV infusion
    • bacterial and fungal superinfections
  37. Gentamicin
    aminoglycoside, bactericidal, glomerular filtration, IV/IM

    • Mechanism:
    • transported into cell by an energy-requiring aerobic process, binds to several ribosomal sites, stops initiaion, causes mRNA misreading
    • post-antibiotic effect
    • concentration-dependent killing

    Resistance: enzymatic modification of the aminoglycosides

    • Use:
    • most effective against gram(-) (gram- aerobic bacilli)
    • ineffective against anaerobes
    • use restricted to serious infections
    • streptomycin

    • SE:
    • nephrotoxicity
    • ototoxicity
    • neuromuscular blockade
  38. Tobramycin
    aminoglycoside, bactericidal, glomerular filtration, IV/IM

    • Mechanism:
    • transported into cell by an energy-requiring aerobic process, binds to several ribosomal sites, stops initiation, causes mRNA misreading
    • post-antibiotic effect
    • concentration-dependent killing

    Resistance: enzymatic modification of the aminoglycosides

    • Use:
    • most effective against gram (-) (gram- aerobic bacilli)
    • ineffective against anaerobes
    • use restricted to serious infections
    • streptomycin
    • covers those resistant to gentamicin

    • SE:
    • nephrotoxicity
    • ototoxicity
    • neuromuscular blockade
  39. Amikacin
    aminoglycoside, bactericidal, glomerular filtration, IV/IM

    • Mechanism:
    • transported into cell by an energy-requiring aerobic process, binds to several ribosomal sites, stops initiation, causes mRNA misreading
    • post-antibiotic effect
    • concentration-dependent killing

    Resistance: enzymatic modification of the aminoglycosides

    • Use: 
    • most effective against gram (-) (gram- aerobic bacilli)
    • ineffective against anaerobes
    • use restricted to serious infections
    • streptomycin
    • covers those resistant to gentamicin & tobramycin

    • SE:
    • nephrotoxicity
    • ototoxicity
    • neuromuscular blockade
  40. Doxycycline
    Tetracycline, bacteriostatic, least affinity for Ca2+

    Mechanism: transported into cells, binds to 30S ribosomal subunits; prevent attachment of aminoacyl-tRNA to the acceptor site

    Resistance: increased transport of the drugs out of the bacterial cells, resistance to one tetracycline often implies resistance to them all

    • Use: were once broad spectrum
    • preferred agents for unusual organisms: rickettsia, chlamydia, etc.

    • SE:
    • GI disturbances
    • Candida superinfection in colon
    • photosensitization with rash
    • teeth discolorization

    • Administration:
    • oral
    • food and milk decrease absorption
  41. Minocycline
    Tetracycline, bacteriostatic

    Mechanism: transported into cells, binds to 30S ribosomal subunits; prevent attachment of aminoacyl-tRNA to the acceptor site

    Resistance: increased transport of the drugs out of the bacterial cells, resistance to one tetracycline often implies resistance to them all

    • Use: were once broad spectrum
    • preferred agents for unusual organisms: rickettsia, chlamydia, etc.

    • SE:
    • GI disturbances
    • Candida superinfection in colon
    • photosensitization with rash
    • teeth discolorization

    • Administration:
    • oral
    • food & milk decrease absorption
  42. Tigecycline
    Mechanism: binds 30S ribosomal subunit and blocks aminoacyl-tRNA entry, also binds additional unique sites in the ribosomes

    • Use:
    • skin/skin structure infections
    • complicated intraabdominal infections
    • community acquired pneumonia
    • E, Coli, Citrobacter, Klebsiella, Enterobacter, NOT Pseudomonas
    • Enterococcus faecalis
    • MSSA, MRSA
    • Bacteroides
    • Clostridium perfringens
    • S. pneumoniae, Haemophilus

    • SE:
    • nausea, vomiting
    • caclium binding
    • increased risk of death
  43. Chloramphenicol
    Mechanism: binds 50S ribosomal subunit, interferes with binding of aminoacyl-tRNA, inhibits peptide bond formation

    Resistance: acetylated by chloramphenicol acetyltransferase

    • Use: 
    • broad spectrum of activity (but SE limit)
    • alternate agent for meningitis
    • brain abscesses
    • severe Salmonella
    • secondary agents for ricketssial diseases, brucellosis

    • SE:
    • bone marrow depression, can progress to fatal aplastic anemia
    • Grey baby syndrome
    • optic neuritis and blindness
  44. Erythromycin
    Mechanism: binds 50S ribosomal subunit, blocks translocation step

    Resistance: plasmid-mediated methylation of 23S rRNA of 50S subunit

    Use: primarily against gram+, also effective against typical bugs

    • SE:
    • nausea/vomiting
    • inhibits CYP3A4
    • increases risk of arrhythmias and cardiac arrest
  45. Clarithromycin
    Mechanism: Bind to 50S ribosomal subunit

    • Use:
    • alternatives to erythromycin 
    • pharyngitis, respiratory infections, soft tissue infections, sinusitis
    • H. pylori
    • atypical myobacterial infections in AIDS patients
  46. Azithromycin
    Mechanism: bind to 50S ribosomal subunit

    Use: respiratory and genital infections

    • SE: 
    • fewer GI disturbances than erythromycin
    • few drug interactions
  47. Clindamycin
    Mechanism: binds to 50S ribosomal subunit, blocks translocation step

    Resistance: plasmid-mediated methylation of 23S rRNA of 50S subunit

    Use: most gram+ cocci and many anaerobes incl. Bacteroides fragilis; not for MRSA

    • SE:
    • serious antibiotic associated enterocolitis
    • GI irritation diarrhea
    • hepatotoxicity
  48. Linezolid
    Mechanism: interferes with translation: binds 50S ribosomal subunit, interfering with formation of 70S initiation complex; bacteriostatic

    • Use: 
    • VRE: vancomycin-resistant Enterococcus faecium
    • MRSA and MSSA
    • Streptococcus
    • Streptococcus pneumoniae


    • SE:
    • non-selective MAOI (avoid tyramine)
    • diarrhea, headache, nausea/vomit, superinfection, enterocolitis
    • bone marrow supression
  49. Sulfamethoxazole
    Mechanism: inhibit folate synthesis by inhibiting dihydropteroate synthase

    Resistance: reduced uptake of drug, mutation in dihydropteroate synthase

    • Use: 
    • given with trimethoprim
    • urinary tract infections
    • bacillary dysentery
    • typhoid fever

    • SE:
    • hypersensitivity 
    • rashes, serum sickness
    • GI disturbances
    • renal damage from crystalluria
    • potentiate action of other drugs (CYP2C( inhibitor)
  50. Silver Sulfadiazine
    Mechanism: inhibit folate synthesis by inhibiting dihydropteroate synthase

    Resistance: reduced uptake of drug, mutation in dihydropteroate synthase

    • Use:
    • urinary tract infections
    • bacillary dysentery
    • typhoid fever
    • topically in burns

    • SE: hypersensitivity
    • rashes, serum sickness
    • GI disturbances
    • renal damage from crystalluria
    • potentiate action of other drugs (inhibit CYP2C9)
  51. Trimethoprim
    Mechanism: inhibit folate synthesis by competitively inhibiting dihydrofolate reductase

    Resistance: mutated dihydrofolate reductase, decreased permeability

    • Use: most often in conjunction with sulfamethoxazole (TMP/SMX)
    • urinary infections
    • upper respiratory tract and ear infections
    • Pneumocystis jiroveci, Salmonella, Shigella

    • SE:
    • nausea, vomiting, diarrhea, rashes
    • eosinophilia, neutropenia, bone marrow supression

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