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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
Monobactam DI, CI/AE | Aztreonam
DI: Cross reaction with Ceftazidime (3rd gen Cephalosporin) AE: skin rash, safe for PCN allergy
26
Monobactam ADME | Aztreonam
A: IV, IM, inhalation D: penetrates CSF M: renal E: renal
27
Vancomycin Spectrum | Glycopeptide
Gram (+) only MRSA C. diff
28
Vancomycin MOA
**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
Vancomycin Resistance
Modification of D-ala-D-ala binding site of peptidoglycan in which terminal D-ala is replaced with D-lactate
30
Vancomycin DI, CI/AE
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
Vancomycin ADME
A: IV, Oral only for gut infections - does not absorb systemically through gut D: Wide distribution, crosses BBB M: Renal E: Renal
32
Tetracycline Drugs
Tetracycline Doxycycline Minocyclin Tegecyclin Eravacycline Omadacycline
33
Tetracyclines Spectrum
Broad Spectrum abx, Gram (+) and Gram (-), anaerobes, and atypical infections Doxycycline - R. rickettsia Tetracycline - H. pylori
34
Tetracyclines MOA
**Bacteriostatic** Binds to bacterial ribosomal 30S subunit --> blocks tRNA from binding to acceptor site --> inhibits protein synthesis
35
Tetracyclines Resistance
PCN-ase producing Staph Efflux pumps Protection proteins - proteins that cover active site to prevent abx from binding
36
Tetracyclines DI, CI/AE
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
Tetracycline ADME
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
B-Lactamase inhibitors
Clavulanic Acid Sulbactam Tazobactam
39
B-Lactamase inhibitor Spectrum
Effective against B-lactamase producing bacteria S. pneumoniae, H. influenzae, N. Gonorrhoea, Intra-abdominal abscess anaerobes
40
B-Lactamase inhibitor MOA
No ABX properties Binds to B-lactamases to allow B-lactams abx to work
41
B-Lactam/B-Lactamase Inhibitor combos
**Augmentin - Amoxicillin + Clavulanate** Zosyn - Piperacillin + Tazobactam Unasyn - Ampicillin + Sulbactam
42
Macrolides Drugs
Erythromycin Clarithromycin Azithromycin (Z-pack)
43
Macrolides Spectrum
Broad spectrum, gram (+) and (-), atypicals Not MRSA Clarithromycin - increased activity vs intracellular pathogens Azithromycin - decreased activity vs strep/staph
44
Macrolides MOA
**Bacteriostatic** (Bactericidal at high concentrations) Inhibits bacterial protein synthesis by binding to 50S subunit and preventing aminoacyl translocation
45
Macrolides Resistance
Common, gram (+) more resistance Altered target 50S site
46
Macrolides DI, CI/AE
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
Macrolides ADME
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
TMP-SMX Spectrum
Broader than each on their own Broad spectrum, gram (-) and (+), not anaerobes, some MRSA
49
TMP-SMX MOA
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
TMP-SMX Resistance
Bacterial overproduction of PABA Overproduction of targeted enzymes Decreased permeability to drug Overall rare, needs concurrent resistance to both drugs
51
TMP-SMX DI, CI/AE
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
TMP-SMX ADME
A: IV, usually Oral D: Well distributed including CNS E: Renal
53
Fluoroquinolones generations
2nd - Ciprofloxacin - better against gram (-) 3rd - Livofloxicin, Moxifloxicin - better against S. pneumoniae 4th - Delafloxicin
54
Fluoroquinolones Spectrum
Broad spectrum, gram (-) and (+), atypicals Pseudomonas ***Delafloxacin only - MRSA***
55
Fluoroquinolones MOA
**Bactericidal** Inhibits topoisomerase II (all gens) and IV (3rd and 4th gen) --> prevents bacteria from using DNA for replication and transcription
56
Fluoroquinolones Resistance
Chromosomal mutations that alter target sites to prevent binding Decreased accumulation due to decreased permeability or increased efflux
57
Fluoroquinolones DI, CI/AE
DI: Divalent cations CI: Pregnancy, <18 - **teratogenic** AE: tendinitis/tendon rupture, prolongs QT interval (arrythmia), CNS issues, peripheral neuropathy
58
Fluoroquinolones ADME
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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