Anti-microbials IIa/b Flashcards

1
Q

Cell Wall Synthesis Inhibitor Drug CLASSES (8)

A
Penicillins
Cephalosporins
Monobactams
Glycopeptides
Polypeptides
Carbapenems
Phosphoenolpyruvate
Beta-lactamase inhibitor
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2
Q

Cell Membrane Targeting Drug CLASSES (2)

A

Lipopeptides

Detergents

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3
Q

Protein Synthesis Inhibitor Drug CLASSES (4)

A

Tetracyclines
Aminoglycosides
Macrolides
Others (clindamycin, chloramphenicol, linezolid)

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4
Q

DNA/RNA Synthesis Inhibitor drug CLASSES (4)

A

Sulfonamides
Trimethoprims
Fluoroquinolones
Metronidazole

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5
Q

Main components of bacterial cell wall

A

peptidoglycan

NAM-NAG-Pentapeptide repeating monomers

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6
Q

Penicillin Binding Proteins important for

A

LINKING PENTAPEPTIDE TO FORM PEPTIDOGLYCAN cell wall

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7
Q

Beta lactam compounds (4)

A

PENICILLINS
CEPHALOSPORINS
MONOBACTAMS
CARBAPENEMS

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8
Q

Cell wall synthesis inhibitors generally are ________

A

bactericidal

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9
Q

Penicillins MOA

Adverse effect?

A

bind and inhibit PBP enzymes

HYPERSENSITIVITY RXN - rash to anaphylaxis range

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10
Q

With hypersensitivity and penicillins, if someone has anaphylaxis hypersensitivity, what do you need to consider?

A

CROSS REACTIVITY with similar compounds (beta-lactam ring)

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11
Q

Narrow Spectrum Penicillin (2)

beta-lactamase sensisity?

A

Penicillin G and V

sensitive

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12
Q

Very narrow spectrum Penicillin (3)

beta-lactamase sensisity?

A

Methicillin
Nafcillin
Oxacillin

resistant

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13
Q

Broad spectrum Penicillins (2)

beta-lactamase sensisity?

A

Ampicillin
Amoxicillin

sensitive

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14
Q

Extended spectrum Penicillins (3)

beta-lactamase sensisity?

A

Piperacillin
Ticarcillin
Azlocillin

sensitive

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15
Q

Beta-lactamase inhibitor?

Adverse effects associated with?

A

CLAVULANIC ACID

Augmentin (amoxicillin + clavulanic acid)

Adverse effects are associated with whatever drug clavulanic acid is combined with

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16
Q

Cephalosporins MOA

Adverse effect?

A

Bind and inhibit PBP’s

HYPERSENSITIVITY

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17
Q

Changes from generation to generation of cephalosporins

A

INCREASE SPECTRUM OF ACTIVITY FROM 1ST TO 4TH

starts with gram positive and mores to include more gram negative

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18
Q

1st generation Cephalosporins (2)

beta lactamase sensitivity?

enter CNS?

A

Cefazolin
Cephalexin

sensitive

do not enter CNS

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19
Q

2nd Generation cephalosporins (3)

beta lactamase sensitivity?

enter CNS?

A

Cefotetan
Cefaclor
Cefuroxime

Sensitive

only cefuroxime enters CNS

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20
Q

3rd Generation cephalosporins (4)

beta lactamase sensitivity?

enter CNS?

A

Ceftriaxone
Cefotaxime
Cefdinir
Cefixime

sensitive

MOST ENTER CNS

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21
Q

4th Generation cephalosporins (1)

beta lactamase sensitivity?

enter CNS?

A

Cefepime

resistant

ENTER CNS

22
Q

Monobactam MOA

Drug?

Specific for what type of bacteria?

Adverse reaction

CNS penetration?

A

binds to and inhibits PBP

Aztreonam

GRAM NEGATIVE

HYPERSENSITIVITY

Passes into CNS easily

23
Q

Carbipenems (4)

Which is co-administered with cilastatin?

A

Doripenem
Imipenem*** (co-administered)
Ertapenem
Meropenem

24
Q

Carbipenems MOA

Adverse reaction

beta lactamase sensitivity?

CNS penetration?

A

bind to and inhibit PBP’s

GI UPSET

RESISTANCE

Penetrates CNS relatively well

25
Q

Glycopeptide drug?

MOA?

Adverse effect?

Good for treatment of?

Penetrate CNS?

A

Vancomycin

PREVENTS ELONGATION OF PEPTIDOGLYCAN CELL WALL –> binds D-ala-D-ala pentapeptide

FLUSHING - red man syndrome

resistant strains of bacteria (MRSA, enterococci, C. difficile)

does not have good CNS penetration

26
Q

Polypeptide drug?

MOA?

Commonly found in?

A

bacitracin

blocks incorporation of amino acids and nucleic acids into cell wall

TOPICAL OINTMENTS

27
Q

Phosphoenolpyruvate drug?

MOA?

Commonly used in treatment of?

A

Fosfomycin

blocks early step in cell wall synthesis by preventing synthesis of UDP-NAM

UTI’s

28
Q

Protein synthesis inhibitors are typically _______

A

bacteriostatic

29
Q

Steps of Prokaryotic Translation

A

1 - tRNA binds to A site
2 - peptide bond formed
3 - newly uncharged tRNA exits
4 - now longer chain translocates to P site

30
Q

Aminoglycosides (6)

A
streptomycin
gentamicin
kanamycin
amikacin
tobramycin
neomycin
31
Q

Aminoglycosides MOA?

Key adverse effects?

typically bacteriostatic or cidal?

A

binds to 30S RIBOSOMAL SUBUNIT - blocks formation of INITIATION COMPLEX

NEPHROTOXIC
OTOTOXIC

typically bacteriocidal

32
Q

Macrolides (3)

A

erythromycin
clarithromycin
azithromycin

33
Q

Macrolides MOA?

Key adverse effect?

typically bacteriostatic or cidal?

A

BINDS 50S SUBUNIT - impairs translocation of P site (step 4)

GI UPSET

bacteriocidal

34
Q

Tetracyclines (4)

A

tetracycline
minocycline
tigecycline
doxycycline

35
Q

Tetracycline MOA

key adverse effects?

typically bacteriostatic or cidal?

A

30S SUBUNIT BINDING - prevents binding of new tRNA to A site (step 1)

NUTRIENT INTERACTIONS - binds calcium - discoloration of bone/teeth
ECOLOGICAL EFFECTS
PHOTOSENSITIVITY

bacteriocidal

36
Q

Clindamycin MOA

key adverse effect?

Spectrum?

A

BINDS 50S SUBUNIT - prevents formation of initiation complex (step 1) and translocation to P site (step 4)

GI –> HIGHLY ASSOCIATED WITH C. DIFFICILE

Narrow spectrum

37
Q

Chloramphenicol MOA

Key adverse effects?

A

BINDS 50S SUBUNIT - prevents transpeptidation (step 2)

BLOOD - RBC PRODUCTION SUPPRESSION
GRAY BABY SYNDROME - glucuronic acid conjugation step inhibited

38
Q

Linezolid MOA

Key adverse effect?

Good for what type of organisms?

A

INHIBITS PROTEIN SYNTHESIS - binds to P site of 50S RIBOSOME and inhibits very first charged tRNA from coming into complex (step 1)

BLOOD - myelosuppression (pancytopenia)

RESISTANT ORGANISMS

39
Q

50 S binding drug classes (4)

A

Macrolides
Clindamycin
Chloramphenicol
Linezolid

40
Q

30 S binding drug classes (2)

A

Aminoglycosides

Tetracyclines

41
Q

Sulfonamides (3)

A

sulfadiazine
sulfamethoxazole
sulfamethizole

42
Q

Sulfonamides MOA

Key adverse effect?

A

competitively inhibits DIHYDROPTEROATE SYNTHASE

SKIN - hypersensitivty, photosensitivity, Steven-Johnson Syndrome

43
Q

Trimethoprim MOA

Key adverse effect?

Commonly used for?

A

Inhibits bacterial DIHYDROFOLATE REDUCTASE

BLOOD - bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia

UTI’s (combined with sulfonamide)

44
Q

TMP-SMX characteristic

common clinical use?

A

SYNERGISTIC ACTIVITY OF SULFONAMIDES AND TRIMETHOPRIM

UTI’s

45
Q

Fluoroquinolones Group 2

active against?

A

Ciprofloxacin
Levofloxacin
Ofloxacin

better against gram negative, some gram positive

46
Q

Fluoroquinolones MOA

Key adverse effects (3)?

clinical?

A

INHIBITS DNA TOPOISOMERASE II AND IV

GI
Drug-nutrient interactions - binds divalent cations
Cardio - QT prolongation

urinary, GI, respiratory, ANTHRAX, some STI’s

47
Q

Fluoroquinolones group 1

characteristic?

A

Norfloxacin

least activity

48
Q

Fluoroquinolones group 3

active against?

A

Gatifloxacin
Gemifloxacin
Moxifloxacin

best against gram positive

49
Q

Metronidazole MOA

Key adverse effects (2)?

Activity limited to?

A

PRODRUG - forms REACTIVE METABOLITES that bind to DNA and disrupt function

GI
Metabolism - DISULFIRAM LIKE REACTION

ANAEROBIC BACTERIA

50
Q

Daptomycin MOA

Key adverse effect(1)?

A

CAUSES DEPOLARIZATION OF BACTERIAL MEMBRANE - ultimately bactericidal

MUSCULOSKELETAL TOXICITY

51
Q

Polymyxin B MOA

A

BINDS TO PHOSPHOLIPIDS - disrupts structure - specificaly LPS BINDING

rare adverse effects

TOPICAL most often