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Unit 3 HDC > Drugs > Flashcards

Drugs Flashcards

1
Q

Beta Lactam Classes

A

Penicillin
Cephalosporins
Carbapenems
Monobactams

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2
Q

Penicillin subclasses

A

Natural Penicillin - Penicillin V and G
Anti-staphylococcal - Nafcillin, Oxacillin, Dicloxacillin
Extended Spectrum - Amoxicillin, Ampicillin
Anti-pseudomonal - Piperacillin

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3
Q

Penicillin Spectrum

A

Natural Penicillin - Gram +, non B-lactamase; some gram -
Anti staphylococcus - staphylococcus
Extended spectrum - Gram (+) and (-)
Antipseudomonal - Broadest spectrum, improved against gram -

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4
Q

Penicillin MOA

A

Bactericidal

Binds to penicillin-binding protein to inhibit transpeptidase activity and prevent cross-linking of NAG and NAM - inhibits production of cell wall

All B-lactams

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5
Q

Penicillin Resistance

A

Beta lactamase
Efflux pumps
Alterations to penicillin binding proteins

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6
Q

Penicillin Drug interaction and AE/CI

A

DI: Probenecid - competes for excretion site; indirectly effects Warfarin via diminished Vitamin K production

AE: Toxicity, rashes, nausea
CI: Hypersensitivity, renal failure, previous anaphylactic reaction

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7
Q

Natural Penicillin ADME

A

A: PCN G - IV, PCN V - oral
D: PCN G - well distributed, PCN V - low systemic levels limit widespread use
M: Both renally
E: both renally (PCN G- rapid)

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8
Q

Anti staphylococcus PCN ADME

A

A: IV, added stability to staphylococcal beta-lactamase
D: well distributed
M: biliary clearance
E: Renal

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9
Q

Extended Spectrum PCN ADME

A

A: Amoxicillin and ampicillin given orally. Ampicillin IV for serious infections
D: well distributed
M: renally eliminated
E: Renal

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10
Q

Antipseudomonal PCN ADME

A

A: IV
D: well distributed
M: renally eliminated
E: Renal

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11
Q

Cephalosporin generations

A

1st (CEFA) - Cefazolin, Cefalexin, Cefadroxil, Cefradine
2nd (FFFT) - Cefoxitin, Cefuroxime, Cefaclor, Cefotetan
3rd (FIXT) - Cefixime, Ceftriaxone, Ceftazidime, Cefotazime
4th (QUINOa PI) - Cefquinome, Cefepime, Cefpirome
5th (CEFTOL) - Ceftobiprole, Ceftaroline, Ceftolozane

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12
Q

Cephalosporin Spectrum

A

1st gen- gram (+) bacteria
2nd gen - improved against gram (-)
3rd gen - broad activity against (+) and (-); more serious infections; Ceftazidime against pseudomonas
4th gen - activity against pseudomonas
5th gen - MRSA

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13
Q

Cephalosporin MOA

A

Bactericidal

Binds to penicillin-binding protein to inhibit transpeptidase activity and prevent cross-linking of NAG and NAM - inhibits production of cell wall

All B-lactams

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14
Q

Cephalosporin Resistance

A

Beta lactamase
Efflux pumps
Alterations to penicillin binding proteins

Same as penicillin

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15
Q

Cephalosporin Drug interactions, AE/CI

A

DI: Probenecid - competes for excretion site; indirectly effects Warfarin via diminished Vitamin K production

CI/AE: Anaphylaxis of penicillin

Same as penicillin

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16
Q

Cephalosporin ADME

A

A: Oral, IV, IM
D: Well distributed, 3rd gen = CNS
M: Renal
E: Renal, Cefriaxone excreted via bile

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17
Q

Carbapenams Spectrum

A

Activity against gram (+) and (-), atypicals, not MRSA
UTI - enterobacteria, pseudomonas
Empiric therapy for serious infection

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18
Q

Carbapenams MOA

A

Bactericidal

Bind to penicillin binding protein to inhibit transpeptidation (prevent cross-linking of NAG and NAM) to prevent the production of a the bacterial cell wall

All B-lactams

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19
Q

Carbapenams Resistance

A

B-lactamases

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20
Q

Carbapenams DI, CI/AE

A

CI: pts with penicillin allergy

Imipenem rapidly degraded by renal enzyme dehydropepridase 1 when administered alone, so always coadministered with cilastatin

AE: N/V/D/Rash, Renal failure from dehydropeptidase

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21
Q

Carbapenams ADME

A

A: IV
D: Well distributed, no CNS
M: renal
E: renal

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22
Q

Monobactam Spectrum

A

Only effective against gram (-)

Pseudomonas, E.coli, Haemophilus, Moraxella

Aztreonam

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23
Q

Monobactam MOA

Aztreonam

A

Bactericidal

Prevents bacterial cell wall synthesis by binding to and inhibiting cell wall transpeptidases

All B-lactams

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24
Q

Monobactam Resistance

Aztreonam

A

B-lactamases, not effective against gram (+)

25
Q

Monobactam DI, CI/AE

Aztreonam

A

DI: Cross reaction with Ceftazidime (3rd gen Cephalosporin)

AE: skin rash, safe for PCN allergy

26
Q

Monobactam ADME

Aztreonam

A

A: IV, IM, inhalation
D: penetrates CSF
M: renal
E: renal

27
Q

Vancomycin Spectrum

Glycopeptide

A

Gram (+) only
MRSA
C. diff

28
Q

Vancomycin MOA

A

Bactericidal

Inhibits cell wall synthesis by blocking peptidoglycan polyermization by binding to terminal d-Ala-d-Ala residues on NAM/NAG - prevents cross linking

Cell Wall inhibitor

29
Q

Vancomycin Resistance

A

Modification of D-ala-D-ala binding site of peptidoglycan in which terminal D-ala is replaced with D-lactate

30
Q

Vancomycin DI, CI/AE

A

AE: Nephrotoxicity, monitoring of weekly creatine phosphokinase recommended
Red Man Syndrome: Flushing/Shock due to histamine release after rapid infusion

Used for pts that are allergic to B-lactams

31
Q

Vancomycin ADME

A

A: IV, Oral only for gut infections - does not absorb systemically through gut
D: Wide distribution, crosses BBB
M: Renal
E: Renal

32
Q

Tetracycline Drugs

A

Tetracycline
Doxycycline
Minocyclin
Tegecyclin
Eravacycline
Omadacycline

33
Q

Tetracyclines Spectrum

A

Broad Spectrum abx, Gram (+) and Gram (-), anaerobes, and atypical infections

Doxycycline - R. rickettsia
Tetracycline - H. pylori

34
Q

Tetracyclines MOA

A

Bacteriostatic

Binds to bacterial ribosomal 30S subunit –> blocks tRNA from binding to acceptor site –> inhibits protein synthesis

35
Q

Tetracyclines Resistance

A

PCN-ase producing Staph
Efflux pumps
Protection proteins - proteins that cover active site to prevent abx from binding

36
Q

Tetracyclines DI, CI/AE

A

CI: Pregnancy, children <8 - Teratogenic - binds to cations on bone –> causes malformation of bone, discoloration of teeth

AE: N/V/D, binds to calcified tissues, fetal hepatotocivity, phototoxicity/sensitivity, vestibular issues, superinfections

DI: Divalent cations (Ca2+, Mg2+, etc)

37
Q

Tetracycline ADME

A

A: Oral, reduced ~20% with dairy or high fat meal; Tega - IV only
D: Well distributed
M: Liver - then secreted into bile, reabsorbed in intestines
E: Renal, except Doxy and Tega - not reabsorbed by intestines and excreted in feces

38
Q

B-Lactamase inhibitors

A

Clavulanic Acid
Sulbactam
Tazobactam

39
Q

B-Lactamase inhibitor Spectrum

A

Effective against B-lactamase producing bacteria
S. pneumoniae, H. influenzae, N. Gonorrhoea, Intra-abdominal abscess anaerobes

40
Q

B-Lactamase inhibitor MOA

A

No ABX properties
Binds to B-lactamases to allow B-lactams abx to work

41
Q

B-Lactam/B-Lactamase Inhibitor combos

A

Augmentin - Amoxicillin + Clavulanate
Zosyn - Piperacillin + Tazobactam
Unasyn - Ampicillin + Sulbactam

42
Q

Macrolides Drugs

A

Erythromycin
Clarithromycin
Azithromycin (Z-pack)

43
Q

Macrolides Spectrum

A

Broad spectrum, gram (+) and (-), atypicals
Not MRSA
Clarithromycin - increased activity vs intracellular pathogens
Azithromycin - decreased activity vs strep/staph

44
Q

Macrolides MOA

A

Bacteriostatic (Bactericidal at high concentrations)

Inhibits bacterial protein synthesis by binding to 50S subunit and preventing aminoacyl translocation

45
Q

Macrolides Resistance

A

Common, gram (+) more resistance
Altered target 50S site

46
Q

Macrolides DI, CI/AE

A

DI: Interference w/ cytochrome P450 enzymes - any drugs that are broken down with CP450 would see an increase in concentration.
Erythromycin and clarithromycin > azithromycin

AE: QT prolongation, N/V/D

47
Q

Macrolides ADME

A

A: Oral, IV - Erythromycin broken down by gastric pH, coating needed; food decreases absorption for A&E, increases for C
D: everywhere but CNS
M: metabolized in liver
E: Hepatic clearance, Clarithromycin excreted via renal and liver.

48
Q

TMP-SMX Spectrum

A

Broader than each on their own
Broad spectrum, gram (-) and (+), not anaerobes, some MRSA

49
Q

TMP-SMX MOA

A

Synergistic effect makes them bactericidal

SMX inhibits dihydroperoic synthase –> no dihydropteroic acid –> inhibits incorporation of PABA –> no folic acid or THF synthesis
TMP inhibits dihydrofolate reductase –> prevents reduction of DHF to THF –> no folic acid or THF synthesis

50
Q

TMP-SMX Resistance

A

Bacterial overproduction of PABA
Overproduction of targeted enzymes
Decreased permeability to drug

Overall rare, needs concurrent resistance to both drugs

51
Q

TMP-SMX DI, CI/AE

A

AE: Cross reacivity to host dihydrofolate reductase, megaloblastic anemia and teratogenic from folate deficiency, skin reactions
DI: can kick off other drugs from albumin
CI: pregnancy

52
Q

TMP-SMX ADME

A

A: IV, usually Oral
D: Well distributed including CNS
E: Renal

53
Q

Fluoroquinolones generations

A

2nd - Ciprofloxacin - better against gram (-)
3rd - Livofloxicin, Moxifloxicin - better against S. pneumoniae
4th - Delafloxicin

54
Q

Fluoroquinolones Spectrum

A

Broad spectrum, gram (-) and (+), atypicals
Pseudomonas
Delafloxacin only - MRSA

55
Q

Fluoroquinolones MOA

A

Bactericidal

Inhibits topoisomerase II (all gens) and IV (3rd and 4th gen) –> prevents bacteria from using DNA for replication and transcription

56
Q

Fluoroquinolones Resistance

A

Chromosomal mutations that alter target sites to prevent binding
Decreased accumulation due to decreased permeability or increased efflux

57
Q

Fluoroquinolones DI, CI/AE

A

DI: Divalent cations
CI: Pregnancy, <18 - teratogenic
AE: tendinitis/tendon rupture, prolongs QT interval (arrythmia), CNS issues, peripheral neuropathy

58
Q

Fluoroquinolones ADME

A

A: Orally, dairy interferes with absorption
D: widely distributed including CNS
M: moxifloxicin - hepatically metabolized
E: renal

Unit 3 HDC (8 decks)

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