PHARM_MSII_MOA_BUG_DRUGS

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soren101
ID:
97073
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PHARM_MSII_MOA_BUG_DRUGS
Updated:
2012-04-25 22:10:27
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PHARMACOLOGY MSII MOA BUG DRUGS
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PHARMACOLOGY MSII MOA BUG DRUGS
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  1. PENICILLINS
    COVALENTLY BIND TO THE ENZYMATIC SITE OF PENICILLIN-BINDING PROTEIN (A TRANSPEPTIDASE)

    -->PRODUCE AN IRREVERSIBLE INHIBITION OF PEPTIDOGLYCAN TRANSPEPTIDASE

    -->THUS PREVENT PEPTIDOGLYCAN (CELL WALL) SYNTHESIS
  2. MACROLIDES
    • BACTERIOSTATIC
    • ---------

    ERYTHRO

    CLARITHRO

    &

    AZITHROMYCIN
  3. CARBAPENEMS
    SAME AS THE PENs
  4. AZTREONAM
    SAME AS THE PENICILLANS
  5. CEPHALOSPORINS
    SAME AS THE PCNs

    BROADER SPECTRUM THAN PCN

    • GOOD CNS PENETRATION WITH
    • --*CEFTAZIDIME
    • --*CEFTRIAXONE
    • --*CEFOTAXIME
    • --^CEFEPIME

    • *3rd GEN
    • ^4th GEN
  6. VANCOMYCIN
    COVALENTLY BINDS TO THE D-ALA-D-ALA TERMINUS OF THE PEPTIDE SIDE CHAIN:

    • THIS BINDING PREVENTS THE BINDING OF THE D-ALA-D-ALA TERMINUS TO THE
    • ENZYMATIC SITE OF PEPTIDOGLYCAN TRANSPEPTIDASE.

    CELL WALL SYNTHESIS IS INHIBITED
  7. TELAVANCIN
    INHIBITS CELL WALL SYNTHESIS IN THE SAME WAY AS DOES VANCOMYCIN + RAPIDLY DEPOLARIZES THE BACTERIAL PLASMA MEMBRANE, THUS INCREASING PERMEABILITY AND CAUSING DEATH
  8. TETRACYCLINES
    BINDING TO THE A SITE OF THE 30S SUBUNIT OF THE BACTERIAL RIBOSOME

    PREVENTS THE BINDING OF THE AMINOACYL TRNA:

    PROTEIN SYNTHESIS IS INHIBITED
  9. MACROLIDES
    BINDING TO THE 50S SUBUNIT OF THE BACTERIAL RIBOSOME

    INHIBITS TRANSLOCATION OF THE MOST RECENTLY ADDED AMINO ACID FROM THE A SITE TO THE P SITE:

    PROTEIN SYNTHESIS IS INHIBITED
  10. CLINDAMYCIN
    THE SAME AS THE MACROLIDES

    BINDING TO THE 50S SUBUNIT OF THE BACTERIAL RIBOSOME

    INHIBITS TRANSLOCATION OF THE MOST RECENTLY ADDED AMINO ACID FROM THE A SITE TO THE P SITE:

    PROTEIN SYNTHESIS IS INHIBITED
  11. FLUOROQUINOLONES
    INHIBITION OF TOPOISOMERASES II (DNA GYRASE) AND IV

    • TOPO II INH:
    • PREVENTS THE RELAXATION OF (+) SUPERCOILED DNA NEEDED FOR REPLICATION

    • IV INH:
    • SEPARATION OF REPLICATED CHROMOSOMAL DNA REQUIRED FOR CELL
    • DIVISION
  12. AMINOGLYCOSIDES
    BIND TO 30S SUBUNIT TO BLOCK FORMATION OF THE INITIATION COMPLEX,

    CAUSE MISREADING OF MRNA AND BREAK POLYSOMES INTO NON-FUNCTIONAL MONOSOMES.
  13. LINEZOLID
    BLOCKS PROT SYNTH

    BINDING TO A SITE ON THE 23S RIBOSOMAL RNA OF THE 50S SUBUNIT

    • BLOCKS THE ASSEMBLY OF
    • THE 70 S BACTERIAL RIBOSOMAL COMPLEX

    CAN'T INITIATE PROTEIN SYNTHESIS

    DRUG OF LAST RESORT FOR G+ (MRSA, VRE)
  14. DAPTOMYCIN
    "ZAP-TOMYCIN"

    BINDING TO BACTERIAL MEMBRANES CAUSES DEPLOARIZATION,

    • LOSS OF MEMBRANE POTENTIAL AND
    • CELL DEATH

    MRSA & VRE
  15. FIDAXOMICIN
    INH RNA SYNTHESIS BY INH BAC RNA POLYMERASE

    NARROW SPECTRUM C. DIFF

    OTHER G+ BAC INCLUDING CLOS spp
  16. TRIMETHOPRIM
    SULFAMETHOXAZOLE INH DIHYDROPTEROATE SYNTHETASE,

    SULFAMETHOXAZOLE TRIMETHOPRIM BLOCKS DIHYDROFOLATE REDUCTASE:

    THE SYNTHESIS OF TETRAHYDROFOLATE IS BLOCKED
  17. PYRIMETHAMINE-
    SULFADIAZINE INH DIHYDROPTEROATE SYNTHETASE, AND
  18. - SULFADIAZINE PYRIMETHAMINE BLOCKS
    • DIHYDROFOLATE REDUCTASE: THE SYNTH OF TETRAHYDROFOLATE IS
    • BLOCKED
  19. NITROFURANTOIN
    • BACTERIAL ENZYMES REDUCE NITROFURANTOIN TO A HIGHLY-REACTIVE
    • INTERMEDIATE

    -->DAMAGES BACTERIAL DNA CAUSING CELL DEATH

    UTIs (e.coli)
  20. ISONIAZID
    Tx TB -- INH CELL WALL SYNTH

    • BIOACTIVATION BY MYCOBAC
    • CATALASE-PEROXIDASE,

    THE ACTIVE METABOLITE COVAL BINDS TO THE ACYL CARRIER PROTEIN AND THE b-KETOACYL CARRIER PROTEIN SYNTHETASE

    • --> PREVENT THE SYNTH OF MYCOLIC
    • ACID
  21. RIFAMPIN
    • BINDING TO THE b-SUBUNIT OF BACTERIAL
    • DNA-DEPENDENT RNA POL
  22. RIFABUTIN
    POLYMERASE PREVENTS RNA SYNTHESIS
  23. PYRAZINAMIDE
    Tx TB

    INTERFERES WITH THE SYNTHESIS OF MYCOLIC ACID

    -->AFFECTING THE GENE FOR FATTY ACID SYNTHASE I
  24. ETHAMBUTOL
    INH ARABINOSYL TRANSFERASE

    PREVENT THE POLYMERIZATION OF ARABINOGLYCAN, AN ESSENTIAL COMPONENT OF THE MYCOBACTERIAL CELL WALL
  25. STREPTOMYCIN
    BINDS TO 30S SUBUNIT TO IBLOCK FORMATION OF THE INITIATION COMPLEX

    CAUSE MISREADING OF MRNA AND BREAK POLYSOMES INTO NON-FUNCTIONAL MONOSOMES.
  26. AMPHOTERICIN B NYSTATIN
    BINDING TO ERGOSTEROL IN FUNGAL CELL MEMBRANES CREATES PORES

    -->INC THE PERM OF THE CELL WALL: LOSS OF INTRACELLULAR MACROMOLs AND IONS CAUSES CELL DEATH
  27. -AZOLES
    E.G., FLUCONAZOLE
    ANTI-FUNGAL

    INHIBITION OF CYP450 LANOSTEROL 14a-DEMETHYLASE

    BLOCKS THE SYNTHESIS OF ERGOSTEROL

    ERGO -- CELL MEM OF FUNGI & YEAST. LIKE CHOLESTEROL OF ANIMALS
  28. ECHINOCANDINS
    INHIBIT CELL WALL SYNTHESIS BY BLOCKING THE ENZYME 1,3-b-D-GLUCAN SYNTHETASE:

    CALLED "PENICILLINS FOR FUNGI"
  29. FLUCYTOSINE (5-FC)
    5-FC CONVERTED TO 5-FLUOROURACIL (5-FU) BY FUNGI;
  30. 5-FU CONVERTED TO FDUMP WHICH BLOCKS FUNGAL THYMIDYLATE SYNTHETASE;
  31. LACK OF THYMIDINE PREVENTS DNA SYNTHESIS
  32. GRISEOFULVIN
    FUNGISTATIC:
  33. BINDS TO MICROTUBULES TO PREVENT FUNGAL MITOSIS
  34. TERBENAFINE
    &
    TOLNAFTATE
    FUNGICIDAL:
  35. BLOCK SQUALENE-2,3- EPOXIDASE TO BLOCK ERGOSTEROL SYNTHESIS
  36. OSELTAMAVIR
    BLOCKS THE RELEASE OF NEW VIRAL PARTICLES FROM INFECTED CELLS

    -->INH OF VIRAL NEURAMINIDASE
  37. ACYCLOVIR
    GANCICLOVIR
    PENCICLOVIR
    ALL ARE CONVERTED TO MONOPHOSPHATES BY HSV AND CMV KINASES

    • HSV
    • --ACYCLOVIR
    • --PENCICLOVIR

    • CMV
    • --GANCICLOVIR

    -->CONVERSION TO TRIPHOSPHATES BY HOST CELL KINASES:

    TRIPHOSPHATES INHIBIT VIRAL DNA POLYMERASE
  38. FOMIVIRISEN
    Tx CMV

    ANTISENSE OLIGONUCLEOTIDE WHICH BINDS VIRAL MRNA

    -->PREVENTS TRANSLATION
  39. TRIFLURIDINE
    Tx HERPES KERATITIS

    CONVERTED TO TRIFLURIDINE TRIPHOSPHATE BY HOST-CELL KINASES:

    THE ACTIVE METABOLITE INH VIRAL DNA POLYMERASE
  40. FOSCARNET
    • Tx
    • --HSV
    • --HZV
    • --CMV

    DIRECTLY INHIBITS VIRAL DNA POLYMERASE
  41. TRIFLURIDINE
    • CONVERTED TO TRIFLURIDINE TRIPHOSPHATE BY HOST-CELL
    • KINASES:

    -->ACTIVE METABOLITE INH VIRAL DNA POL
  42. ENFUVIRTIDE
    BLOCKS THE FUSION OF THE VIRAL AND T-CELL MEMBRANES

    --> HIV CANNOT ENTER THE CD+4 CELL
  43. MARAVIROC
    HIV

    BLOCKS FUSION OF VIRAL AND T-CELL MEMs BY BINDING TO CCR5 RECEPTOR OF THE T-CELL
  44. ZIDOVUDINE
    LAMIVUDINE
    ABACAVIR
    TENOFOVIR
    EMTRICITABINE
    Tx HIV

    NRTIs - INH REVERSE TRANSCRIPTASE -- CHAIN TERMINATION BY BY NUCLEOSIDE INSERTION (HIV)


    • AFTER CONVERSION TO "FALSE" NUCLEOTIDES (TRIPHOSPHATES) BY
    • INTRACELLULAR KINASES

    -->THESE "FALSE" NUCLEOTIDES COMPETITIVELY INH HIV REVERSE TRANSCRIPTASE AND THEIR INCORPORATION INTO DNA CHAIN

    • -->CHAIN TERMINATION
    • ------------------------

    • ZIDOVUDINE
    • --AZT = AZIDOTHYMIDINE
    • --S/E BONE MARROW DEP AND ANEMIA
  45. NEVIRAPINE
    EFAVIRENZ
    Tx HIV

    NNRTIs -- DIRECTLY INHIBIT REVERSE TRANSCRIPTASE (HIV)

    -->BLOCK RNA- AND DNA-DEPENDENT POLYMERASE
  46. RALTEGRAVIR
    Tx HIV

    BLOCKADE OF THE VIRAL INTEGRASE

    -->PREVENTS THE INSERTION OF VIRAL DNA INTO HUMAN DNA
  47. RITONAVIR
    LOPINAVIR
    ATAZANAVIR
    Tx HIV

    BLOCKADE OF VIRAL PROTEASE

    • -->PREVENTS THE CLEAVAGE OF VIRAL
    • POLYPROTEINS INTO THE FUNCTIONAL SUBUNITS NEEDED TO
    • ASSEMBLE NEW FUNCTIONAL, INF VIRAL PARTICLES

    RITONAVIR INHIBITS CYP450 WHICH DEC HEPATIC CLEARANCE OF LOPINAVIR
  48. METRONIDAZOLE
    PROTOZOAL AND BACTERIAL FERREDOXINS REDUCE THE NITRO GROUP

    -->PRODUCE A HIGHLY-RECTIVE NITRO RADICAL WHICH ATTACKS DNA AND DESTROYS ITS HELICAL STRUCTURE;

    ALSO CAUSES DNA MUTATIONS
  49. NITAZOXANIDE
    ANTI-PROTOZOAL

    CRYPTOSPORIDIOSIS

    GIARDIA, BUT DOC IS METRONIDAZOLE

    • INTERFERS WITH PYRUVATE:FERRODOXIN
    • OXIDOREDUCTASE-DEPENDENT ELECTRON TRANSFER REACTION
  50. PENTAMIDINE
    MOA -- UNKNOWN

    Tx Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii SEEN WITH HIV Pt.

    ALSO Tx FOR stage I infection with Trypanosoma brucei gambiense
  51. WHAT DRUGS INHIBIT CELL WALL SYNTHESIS
    CIDAL EXCEPT ETHAMBUTOL

    "PCC-Mon VIBE"

    PCCM = b-LACs

    • PEN
    • CARBAPENEMS
    • CEPHALOSPORINS
    • MONOBACTAMS (aztreonam)
    • VANCOMYCIN
    • ISONIAZID
    • ETHAMBUTOL (static)
    • BACITRACIN
  52. WHAT DRUGS INHIBIT DNA/RNA SYNTHESIS
    CIDAL

    • FLUOROQUINOLONES (levofloxin)
    • RIFAMPIN
    • NITROFURANTOIN
  53. WHAT DRUGS INCREASE BAC MEMBRANE PERMEABILITY
    CIDAL

    POLYMIXIN b

    COLISTIN (polymixin E)
  54. WHAT DRUGS INHIBIT PROTEIN SYNTH
    INH PROT SYNTH = STATIC

    "ACCLMaTe"

    • AMINOGLYCOSIDES (exception - cidal)
    • CLINDAMYCIN
    • CHOLRAMPHENICOL
    • LINEZOLID
    • MACROLIDES (eryth)
    • TETRACYCLINES
  55. STAPH AUREUS RESISTANCE
    PROD PCNase (b-LACTAMASE) WHICH DEGRADES DRUG

    OXACILLIN AND NAFCILLIN NOT DEGRADED (MSSA)

    MRSA -- CHANGED BINDING SITE FOR b-LACTAM bc OF MUTATED BAC GENE

    CEFTAROLINE ONLY DRUG THAT KILLS MRSA
  56. STREP PNEUMO RESISTANCE TO PCN
    HIGH MOLECULAR WEIGHT PBPs WITH DECREASED AFFINITY FOR b-LACs
  57. ENTEROCOCCUS RESISTANCE TO VANCOMYCIN
    "COCKROACH OF THE ICU"

    VANC BINDS TO TERM D-ALA-D-ALA OF PEPTIDE SIDE CHAINS OF G+ CELL WALL

    VRE HAS MUTATED D-ALA-D-LAC

    RESISTANCE CARRIED BY PLASMID
  58. DRUG PUMP ON BACTERIAL MEMBRANES
    G- BUGS LIKE PSEUDOMONAS AND ACINETOBACTER PUMP DRUGS OUT

    PSEUDOMONAS MAY HAVE 20 PUMPS AND 3-4 b-LACs

    ALSO, MUTATIONS IN PORINS (channels) MAY INHIBIT ENTRY OF CARBAPENEMS IN PSEUDOMONAS

    STREP PNEUMO & STAPH AUREUS MAY PUMP OUT MACROLIDES
  59. G+ AEROBES COCCI
    • STAPH
    • --COAG+ AUREUS
    • --COAG- EPIDERMIDIS, SAPRO, other

    STREP PNEUMO & PYOGENES (A)

    ENTEROCOCCUS FAECALIS -- #3 CAUSE OF UTI, MAY CAUSE ICU INFs

    ENTEROCOCCUS FAECIUM -- ICU INF
  60. G- AEROBE COCCI
    NEISSERIA GONO

    NEISSERIA MENINGITIDIS

    MORAXELLA CATARRHALIS

    MORAXELLA -- fastidious, nonmotile, Gram-negative, aerobic, oxidase-positive diplococcus that can cause infections of the respiratory system, middle ear, eye, central nervous system and joints of humans. GROWING IMPORTANCE DUE TO RESISTANCE
  61. G+ ANAEROBE COCCI
    PEPTOCOCCUS

    PEPTOSTREPTOCOCCUS
  62. G+ AEROBE RODS
    LISTERIA MONOCYTOGENES
  63. G- AEROBE RODS
    • ENTERIC
    • --E. COLI #1 UTI
    • --KLEB PNEUMO #2 UTI
    • --PROTEUS MIRABILIS - UTI
    • --SALMONELLA
    • --SHIGELLA
    • --ENTEROBACTER - ICU
    • --CITROBACTER - ICU

    • CAP & ICU:
    • --PSEUDOMONAS
    • --H. FLU
    • --LEGIONELLA
    • --CAMPYLOBACTER
    • --ACINETOBACTER BAUMANII
    • --HELICOBACTER PYLORI
  64. G+ ANAEROBE RODS
    • --CLOS BOT
    • --CLOS DIFF
    • --CLOS TETANI
    • --CLOS PERF
  65. G- ANAEROBE RODS
    BACTEROIDES FRAGILIS
  66. IMIPENEM
    CILASTATIN
    PENs

    • IMIPENEM
    • --RESISTANT TO b-LAC
    • --METABOLIZED BY RENAL TUB DIHYDROPEPTIDASES

    • CILASTATIN
    • --INH RENAL PEPTIDASES TO DEC CLEARNACE OF IMIPENEM
  67. b-LACTAMASE INHIBITORS
    CLAVULANATE

    SULBACTAM

    TAZOBACTAM (tazo)
  68. PENICILLIN PHARMACOKINETICS
    --PROBENECID INH RENAL ACID TRANSPORT SYST --> INC T1/2

    • DISTRIBUTION
    • --GOOD IN ECF
    • --NOT GOOD IN CSF, MORE PENETRATION IF MENINGES INFLAMED
    • --POOR INTRACELLULAR; CANNOT USE FOR INTRACELLULAR BUGS

    • ELIMINATION
    • --RAPID RENAL TUBULAR SEC, PEN G T1/3 IS 30mins
    • --PROBENECID INH RENAL ACID TRANSPORT SYST --> INC T1/2
  69. 1ST GEN CEPHALOSPORINS
    • iv CEFAZOLIN - srgy prophyl, ssti mssr = oxa&naf
    • *po CEPHALEXIN - ssti; safe for pregos
    • *poCEPHRADINE

    *WEAK
  70. 2nd GEN CEPHALOSPORIN
    • *iv CEFOXITIN
    • *iv CEFOTETAN
    • ^po CEFUROXIME
    • ^po CEFACLOR

    • * only 2 cephamycins that cover anaerobes
    • ^ tx pedi and fp outpatients
  71. 3rd GEN CEPHALOSPORINS
    • iv CEFOTAXIME
    • iv CETRIAXONE - can give im
    • iv CEFTAZIDIME - kills pseudomonas
    • po CEFPODOXIME - bitter; kids spit up
    • po CEFDINIR - brick red feces in kids
    • po CEFIXIME - not good for strep pneum or mssa

    • ANTI-MRSA 3rd GEN
    • --iv CEFTAROLINE
    • covers ceftriaxone R strep pneumo also
  72. 4th GEN CEPHALOSPORINS
    iv CEFEPIME

    INC RESISTANCE TO DEGRADATION BY b-LACs

    GOOD PSEUDOMONAS COVERAGE
  73. TRENDS IN GENERATIONS OF CEPHALOSPORINS
    1st - BEST FOR G+

    2nd - G+ AND SOME G- AND ANAEROBES (only cefoxitin & cefotetan)

    3rd - INC G- AT EXPENSE OF G+ (mssa)

    4th - MODERATE G+ AND EXCELLENT G- ACTIVITY. RESEMBLES 1ST + 3rd GEN (1+3=4)
  74. IDOXURIDINE
    • RESEMBLES THYMIDINE
    • --IF RESISTANT TO ONE, ALSO THE OTHER

    TOPICAL

    TRIPHOSPHATE INH VIRAL DNA POL

    Tx HSV KERATITIS
  75. AMANTADINE
    INFLU A AND RUBELLA

    INH MEM COAT ION CHANNEL

    ALLOWS ACID-MEDIATED DISSOCIATION OF RIBONUCLEOPROTEIN COMPLEX EARLY IN REPLICAITON

    PROPHYLACTIC FOR INFLU A
  76. ZANAMIVIR
    Tx FLU

    INH VIRAL NEURAMINIDASE
  77. INTERFERONS
    ANTIVIRAL

    CAUSES PROT SYNTH

    • 2,5 ADENINE SYNTHETASE
    • --MAKES ADENYLATE OLIGOMERS
    • --ACTIVATE RNAse TO DEGRADE VIRAL RNA

    • PROT KINASE PHOSes EF2
    • --INH PEPTIDE CHAIN INITIATION

    • PDEase DEGRADES TERMINAL NUC OF tRNA
    • --INH VIRAL PEPTIDE CHAIN ELONGATION

    • NET EFFECTS
    • --INTERFERES w VIRAL PNETRATION, UNCOATING, ASSEMBLE AND RELEASE
    • --INH SYNTH OF VIRAL mRNA
    • --INH TRANSLATION OF VIRAL mRNA

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