Pulmonary Infections- Pharm Flashcards

1
Q

Are macrolides bacteriocidal or bacteriostatic?

A

Bacteriostatic

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2
Q

Targeting the 23s rRNA on the 50s subunit does what from macrolides?

A

block translation and prevents exit

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3
Q

Why are macrolides really good for lung infections?

A

They can penetrate lung tissue really well.

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4
Q

Which bug do macrolids have intracellular activity against?

A

Legionella

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5
Q

Which subunit again do macrolides act upon?

A

23s rRNA of the 50s subunit

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6
Q

Which enzyme is produced by gram + organisms to cause resistance against macrolides?

A

Methylase

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7
Q

What does methylase do to bacteria to cause the resistance to macrolides?

A

it modifies the ribosomal target of macrolides, leading to ↓ drug binding

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8
Q

What is the #1 reason to discontinue erythromycin?

think side effects

A

GI intolerance

cuz it stimualtes gut motility –> N/V, diarrhea, anorexia

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9
Q

What are the 2 mechanisms for quinolones as an antibiotic?

A
  1. inhibits topoisomerases

2. coverts these enzymes into DNA-damaging agents

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10
Q

Which type of isomerases do quinolones act upon?

A

Type II topoisomerases (topoisomerase II and IV)

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11
Q

What are the 3 types of infections do u use fluoroquinolones?

A
  1. Urogenital
  2. Respiratory
  3. GI
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12
Q

Which gram stain bacteria do u use fluoroquinolones for?

A

Gram -

like E. coli, Neisseria gonorrhoeae, Enterobacter, Salmonella, and Shigella

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13
Q

What are the 3 mechanisms to cause resistance to quinolones?

A
  1. chromosomal mutations in the genes that encode type II topoisomerases
  2. alterations in the expression of membrane porins
  3. alterations in the expression of efflux pumps
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14
Q

What is the mechanism of topisomerase II, which is inhibited by quinolones?

A

DNA gyrase

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15
Q

Which gram stain bacteria use topisomerase IV, which is inhibited by quinolones?

A

Gram +

like S. aureus

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16
Q

What are the 2 main species of mycobacteria?

A

M. TB

M. leprae

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17
Q

What are the 2 targets for antimycobacterials?

A
  1. synthesis of NAG-arabinogalactan

2. early reactions of mycolic acid synthesis

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18
Q

What is it about the mycobacterial cell envelope that makes it hard to have antimycobacterials treat the infection?

A

It’s thick, asymmetric, and highly impermeable to hydrophobinand hydrophilic substances.

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19
Q

Why are antimyobacterials that target cell growth ineffective?

A

Myobacteria are very slow growers

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20
Q

What are the 5 drugs that are first-line agents for TB?

A

Ethambutol, pyrazinamide, isoniazid, rifampin, and streptomycin

SPIRE

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21
Q

What are the indications for the 4-drug regimen for TB (isonazid, refampin, pyrazinamide, and either Ethambutol or Streptomycin)?

4-RIP(E/S)

A

pt with active TB and w/o a Hx of prior therapy

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22
Q

What are teh indications for the 3-drug regimen for TB (isonazid, refampin, pyrazinamide)?

3-RIP

A

if isonazid resistance is rare

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23
Q

Is ethambutol bacteriocidal or bacteriostatic?

A

bacteriostatic

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24
Q

What enzyme does ethambutol target to decrease arabinogalactan synthesis?

A

Arabinosyl transferase

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25
Q

Is isonazid a bacteriocidal or bacteriostatic?

A

bacteriocidal

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26
Q

Which enzyme does isonazid target to inhibit mycolic acid synthesis?

A

FAS2

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27
Q

What do u use a lotta drugs for TB?

A

TB has a high frequency of mutations –> resistances.

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28
Q

What can isonazid do to cytochrome P450?

A

inhibit or induce it

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29
Q

What 5 drugs can be affected by isonazid action on cytochrome P450?

A

Rifampin, Carbamazepine, Phenytoin, Azole-type antifungals, and alcohol

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30
Q

Why is selectivity harder for antifungals than antibacterials?

A

fungi cell structure is similiar to animal cells.

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31
Q

In humans, we have cholesterol in our cell membranes, but what is it in fungi that does the same thing?

A

Ergosterol

32
Q

Imidazole and triazole inhibits which enzyme?

A

14a sterol demethylase

33
Q

14a sterol demethylase is used by fungi to do what?

A

converts Lanosterol –> ergosterol

34
Q

Which enzyme do echinocandins act on to inhibit cell wall biosynthesis in fungi?

A

beta-(1,3)-D-glucan synthase

35
Q

What is the fxn of beta-(1,3)-D-glucan synthase for the cell wall?

A

It adds glucose residues from UDP-glucose to the growing polysaccharide chain

36
Q

So are echinocandins fungicidal or fungistatic?

A

Fungicidal

37
Q

What are in the fungal membranes that takes up Flucytosin?

A

Cytosine-specific permeases

38
Q

Once inside the fungal cells, which enzyme converts flucytosin –> 5-FU?

A

Cytosine deaminase

39
Q

5-FU then is converted to 5dUMP, which inhibits which enzyme?

A

Thymidylate synthase

40
Q

Inhibition of thymidylate synthase causes inhibition of what cellular process, thus resulting in inhbiition of cell division?

A

DNA synthesis

41
Q

What are the 3 fungi that flucytosine works upon?

A

Candidiasis
Cryptococcosis
Chromomycosis

CCC

42
Q

Griseofulvin inhibits fungal mitosis by binding to what cellular structure?

A

Tubulin

43
Q

Binding of tubulin by griseofulvin causes what to be inhibited in the fungal cell?

A

assembly of the mitotic spindle

44
Q

Griseofulvin accumulated in which cells?

A

Keratin precursor cells

45
Q

Accumulation of griseofulvin in keratin precursor cells causes growth of which structures to be free of dermatophyte infection?

A

skin, hair, and nails

46
Q

Is griseofulvin fungistatic or fungicidal?

A

Fungistatic

47
Q

Squalene epoxidase converts squalene into what?

A

Lanosterol

48
Q

What are the 3 drugs that inhibit squalene epoxidase to be fungicidal from the prevention of ergosterol formation?

A

Terbinafine (allyamines)
Naftifine (allylamines)
Butenafine (benzylamines)

“squalene are -fine”

49
Q

Which 3 pts are condraindications for terbinafine?

A

Renal failure
Hepatic failure
Pregnant women

50
Q

Again, which enzyme is inhibited by azoles?

A

14a steroid demethylase

51
Q

Why is ketoconazole limited by oral intake if the pt has low stomach acid?

A

It has to be converted to a salt by stomach acid.

52
Q

What has replaced ketoconazole?

A

Itraconazole

53
Q

What 2 conditions do u use topical ketoconazole?

A

Common dermatophyte infection

Seborrheic dermatitis

54
Q

Why is fluconazole used for cryptococcal meningitis?

A

free diffusion into CSF

55
Q

What does polyenes bind directly to inhibit the fungal membrane?

A

Ergosterol

56
Q

Binding and inhibition of ergosterol by polyenes causes pores, which does what to the cell?

A

Cause leaking of essential cellular contents, leading to cell death.

57
Q

Why are polyenes selective for fungi than animal cells?

A

it has a 500x stronger affinity for ergosterol than cholesterol

58
Q

What are the 2 polyenes?

A

Amphotericin B

Nystatins

59
Q

IV administration of amphotericin B causes a cytokine storm by the relase of what 2 factors from cells of the host immune system?

A

TNFa and IL-1

60
Q

What are the 5 Sx to amphoteticin B after administration?

A

fever, chills, hypoTN, renal toxicity and anemia

61
Q

What are the 3 echnocandins?

A

Capsofungin
Anidulafungin
Micofungin

“Fungin CAM!”

62
Q

What is the mechanism of adamantane?

A

inhibits viral uncoating

63
Q

Adamantane works only against which 1 specific virus?

A

Influenza A

64
Q

What is the channel on the viral envelope to move H+ protons into the viral envelope?

A

M2 proton channel

65
Q

Movement of protons into the viral envelope, which is inside the acidic endosome, causes what to happen?

A

Viral uncoating and release of viral RNP into the hsot cell cytosol

66
Q

Which drug has largely replaced the adamantanes?

A

Neuraminidase inhibitors

67
Q

What action do neuraminidase inhbitors block for viral infetions?

A

they block viral relase from the host cell

68
Q

Neruaminidase inhibitors are analogues of which host protein?

A

sialic acid

69
Q

Neuraminidase usually does what to sialic acid in the host cell to cause it’s release?

A

it cleaves sialic acid

70
Q

This is a neuraminidase inhibitor and is active against influenza A and B.

A

Zanamavir

71
Q

Since zanamavir has poor oral availability, what is the route of administration?

A

Inhaler

72
Q

Which neuraminidase inhibitor has a better oral bioavailability than zanamavir?

A

Oseltamavir

73
Q

Oseltamavir is used as a prophylactic for what 2 serious viral infections?

A

H5N1 (bird flu)

H1N1 (swine flu)

74
Q

What is the route of administration for ribavirin?

A

Aerosol

75
Q

Ribavarin is used as a Tx for what condition?

A

RSV

76
Q

Ribavirin can also be used in combination with an interferon (like INFa) for what condition?

A

chronic hep C infection

77
Q

Palivizumab is used to prevent what illness in high-risk children?

A

RSV

this was an LDP test question