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Pharm 225B > Anti-Microbials > Flashcards

Anti-Microbials Flashcards

1
Q

What does selective toxicity mean in respects to anti-microbial?

A

anti-microbials’ MoA do not harm the host (us), only do damage to bacteria, ex.:
- disrupt cell wall of BacT
- inhibit an enzyme unique to BacT
- disrupt bacterial protein synthesis

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2
Q

Antimicrobial Classes (5)

A

Narrow-spectrum (active against few bugs)
Broad spectrum (active against a variety of bugs)
Virus (antiviral)
Fungus (antifungal)
Protozoa (antiprotozoal)

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3
Q

Beta-Lactam Anti-microbials MoA/classes

A

MoA: inhibit bacterial growth by interfering with a specific step in bacterial cell wall synthesis
BACTERICIDAL
classes: penicillins, cephalosporins, monobactams, carbapenems

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4
Q

Narrow spectrum penicillins & route

A
  • penicillin G - IV
  • penicillin VK- PO
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5
Q

Narrow spectrum penicillins (anti-staphylococcal)

A
  • nafcillin
  • oxacillin
  • cloxacillin (PO)
  • dicloxacillin
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6
Q

Broad spectrum penicillins & route

A

(aminopenicillins)
- ampicillin- IV, PO
- amoxicillin- PO

*improved activity against gram -, but destroyed by B-lactamases

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7
Q

Extended-spectrum penicillins & route

A

(anti-pseudomonal)
- Piperacillin (IV)
- Ticarcillin (IV)

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8
Q

bacterial mechanisms of resistance to B-lactams

A
  1. Inactivation of antibiotic by B- lactamase
  2. Modification of target PBP’s
  3. Presence of efflux pump
  4. Impaired penetration of drug to target PBP’s
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9
Q

Penicillin AEs

A

very safe, least toxic; AEs due to hypersensitivity
- rash most common

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10
Q

Penicillin anaphylaxis

A
  • Immediate: urticartia, anaphylaxis, laryngeal edema
  • accelerated: urticartia, less severe
  • Late: maculopapular rash, drug fever, hemolytic anemia, thrombocytopenia, interstitial nephritis

**avoid all other B-Lactams

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11
Q

Cephalosporin changes with generation

A

The higher up in generation
- increasing ability to reach CSF
- increasing resistance to destruction by B-lactamases
- increasing activity against gram - bacteria and anaerobes

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12
Q

1st generation Cephalosporins/spectrum/use

A

Cefadroxil - PO
Cefazolin - IV
Cephalexin - PO

  • active against gram + cocci
  • for UTI, minor staph lesions, cellulitis
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13
Q

2nd Generation Cephalosporins/spectrum/use

A

Cefoxitin - IV
Cefotetan - IV
Cefuroxime - PO and IV
Cefaclor

  • less active against gram -; more against gram +
  • for sinusitis, otitis, and lower respiratory infections
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14
Q

Cephamycins drugs (sub group of 2nd gen)

A

Cefocitin
Cefotetan

  • active against anaerobes
  • for diverticulitis, peritonitis, abdominal/colorectal surgical prophylaxis
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15
Q

3rd Generation Cephalosporins/spectrum/use

A

Cefotaxime- IV
Ceftrazidime - IV
Ceftriaxone - IV/IM

  • more active against gram -; crosses BBB, used in HAIs
  • for complicated CAIs of resp. tract, blood, intra-abdominal, skin/soft tissue, and UTI
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16
Q

4th Generation Cephalosporins/spectrum

A

Cefepime - IV/IM

  • good gram - & + coverage, with activity against Pseudomonas
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17
Q

5th Generation Cephalosporins/spectrum

A

Ceftaroline - IV

  • broad gram-positive and gram-negative organism coverage, including MRSA; does not cover Pseudomonas
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18
Q

“6th” Generation Cephalosporin/use

A

Cefiderocol - IV

Clinical Uses: hospital acquired pneumonia, complicated UTI

19
Q

AE of Cephalosporins

A

patients with anaphylaxis, hives, angioedema, to penicillins should not get cephalosporins
- opportunistic infections with broader spectrum
- hypoprothrombinemia if on warfarin

20
Q

Carbapenems drug/class

A

*drugs in this class end in -penem
- Imipenem
BACTERICIDAL

21
Q

AE of Carbapenems

A

HA
Seizures
Nausea
Lowers valproic acid concentrations

22
Q

Monobactam drug

A

Aztreonam (Azactam)

23
Q

Other B-lactam drugs/use

A
  • Clavulanic acid
  • Sulbactam
  • Tazobactam
  • inhibit B-lactamases protecting penicillins from inactivation; used only in combo with PCNs
24
Q

Glycopeptides drug, moa, use

A
  • Vancomycin - IV (targets gram + bacteria)
  • moa: inhibit cell wall
  • use: sepsis or endocarditis caused by MRSA, meningitis with highly penicillin resistant pneumococcus
25
Q

Lipoglycopeptides drug/moa/use

A
  • Telavancin
  • moa: inhibits cell wall synthesis and disrupts BacT cell membrane
  • complicated skin and skin structure infections, covers VRE, MRSA
26
Q

Tetracyclines drugs/acting time

A
  • tetracycline –> short
  • demeclocycline –> intermediate
  • doxycycline, minocycline –> long acting
27
Q

Tetracyclines spectrum/use

A
  • BACTERIOSTATIC inhibits protein synthesis
  • broad spectrum for gram + & -
  • DOC for mycoplasma pneumoniae, chlamydiae, rickettsiae
    also H pylori, acne, AECB, CAP
28
Q

Tetracylines AE

A
  • GI (N/V, diarrhea) most common reasons for D/C
  • teeth and bones: tetracyclines bind Ca+ in new bones leading to tooth discoloration or bone deformation/growth inhibition
  • Photosensitivity
29
Q

Tetracycline Resistance

A
  1. Efflux by active transport protein pump encoded on plasmid
  2. Ribosome protection by proteins that interfere with
    tetracycline binding
  3. Enzymatic inactivation
30
Q

Macrolides drugs/use

A
  • mainly BACTERIOSTATIC; -cidal in high concentrations
  • Erythromycin
  • Azithromycin
  • Clarithromycin
  • DOC in diphtheria, all Chlamydial infections, CAP; mainly against gram +
31
Q

Macrolides AE

A
  • GI: anorexia, nausea, vomiting and diarrhea most common reason for D/C
  • acute hepatitis as hypersensitivity
  • drug interactions: inhibitor of CYP3A4 (Erythromycin and Clarithromycin ONLY); can prolong QT interval & increase risk for sudden cardiac death
32
Q

Clindamycin moa/AEs/use

A

penicillin alternative, anaerobes; BACTERIOSTATIC

MOA: Penetrates saliva, sputum, pleural fluid and bone but not CSF

AE: psedomembranous colitis (suprainfection)

Clinical Use: head and neck infections

33
Q

Linezolid moa/use

A

MOA: also inhibits protein synthesis by preventing formation of the ribosome complex; BACTERIOSTATIC

Clinical Use: Vancomycin resist. enterobacteria; multiple-drug resistant organisms

34
Q

Aminoglycosides drugs/moa/use

A
  • gentamicin, streptomycin, tobramycin
  • MOA: BACTERICIDAL inhibitors of protein synthesis, against gram - enteric bacteria
  • Clinical Use: bacteriemia and sepsis
35
Q

Aminoglycosides AE

A
  • ototoxicity and nephrotoxicity
36
Q

aminoglycosides dosing

A
  • concentration dependent killing; greater conc. kill more bacteria at faster rate (once daily dosing)
  • killing also occurs for several hours after med cleared from body
37
Q

Antimetabolites MOA/spectrum

A

MOA: analogs of PABA that compete for a synthetic enzyme and block folic acid synthesis needed for DNA; BACTERIOSTATIC

  • targets both gram + & -, chlamydia, inhibits some enterics
38
Q

Trimethropim- sulfamethoxazole (Bactrim) use/AEs

A
  • anti-metabolite
  • P carinii pneumonia, shigellosis, salmonella (traveler’s diarrhea), UTI’s, prostatitis, otitis and upper resp tract infections, CAP
  • AE: frequent hypersensitivity reactions
    and rashes, photosensitivity, GI (N&V), hemolytic anemia, bone marrow depression
39
Q

Fluoroquinolones drugs/moa

A
  • Fluoroquinolones (anything ending in -floxacin, ex. ciprofloxacin)
  • MoA: block bacterial DNA synthesis by inhibiting DNA gyrase (required for DNA replication) Also inhibits topoisomerase. BACTERICIDAL
40
Q

Fluoroquinolones use/ AEs

A
  • resp., UTI’s, soft tissue bone and joint infections, gonococcal infections; newer versions better for gram +’s
  • N/V, diarrhea, may prolong QT interval, tendonitis, cipro inhibits CYP1A2- increase levels, increase toxicity, hypoglycemia (most likely to occur in pts with DM)
41
Q

Metronidalzole (Flagyl) moa/use/AEs

A

MOA: BACTERICIDAL, antiprotozoal with potent activity against anaerobes

Clinical Use: intra-abdominal infections, antibiotic associated enterocolitis, trichomonas vaginitis, giardiasis, triple therapy for H.pylori ulcer disease

AE: GI (N/V, metallic taste), CNS rxns -> seizures, peripheral neuropathy

42
Q

-Azole Antifungals moa/use/drugs

A

MOA: reduce ergosterol synthesis by inhibiting fungal CYP enzymes

Clinical Use: antifungal

drugs are anything ending in -azole, ex. fuconazole, ketoconazole

43
Q

Antimicrobials in Pregnancy

A

Avoid if possible: chloramphenicol
metronidazole
trimethoprim
sulfonamides (last trimester)

Contraindicated:
fluoroqinolones
tetracyclines

Pharm 225B (9 decks)

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