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Respiratory Exam 2 > Anti-Fungal Drugs > Flashcards

Anti-Fungal Drugs Flashcards

1
Q 
Fluconazole
Itraconazole
Posaconazole
Voriconazole 
Amphotericin B used to treat
A
  • Blastomyces
  • Histoplasma
  • Coccidioides
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2
Q

Sulfamethoxazole/Trimethoprim used to treat

A
  • Pneumocystis jirovecii
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3
Q

what is ergosterol

A
  • a crucial component of the fungal cell membrane
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4
Q

Azole antifungals MOA

which one

A
  • inhibition of enzymes involved in ergosterol synthesis

- lanosterol demethylase

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5
Q

Azole antifungals selectivities

A
  • highly selective for the fungal enzymes
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6
Q

Azole antifungal toxicities

A
  • Prolonged QT
  • drug interactions
  • hormonal effects
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7
Q

are Azole antifungals safe to use during pregnancy

A
  • potential teratogen
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8
Q

which azole antifungals cause prolonged QT

A
  • fluconazole, posaconazole
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9
Q

drug interactions with azole antifungals

A
  • inhibit CYP enzymes

- slow metabolism of drugs and elevate their plasma concentration

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10
Q

what is an important cytochrome that azole antifungals inhibit?

A
  • CYP3A4
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11
Q

what azole drug causes hormonal effects

which effects?

A
  • ketoconazole

- gynecomastia, decreased libido, impotence

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12
Q

MOA of polyenes

A
  • ergosterol binding agents
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13
Q

amphotericin B structures

A
  • hydrophobic and hydrophilic face
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14
Q

MOA of amphotericin B

selective for

A
  • binds ergosterol and forms pores in fungal cell membrane

- selective for ergosterol only

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15
Q

which part of amphotericin B associates with ergosterol

A
  • hydrophobic face
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16
Q

resistance mechanism to amphotericin B

A
  • reduced concentration of ergosterol in the membrane

- modification of ergosterol to a form with reduced amphotericin B binding

17
Q

how is amphotericin B administered

why?

A
  • IV

- poor GI tract absorption

18
Q

what is one condition in which we may orally administer amphotericin B?

A
  • luminal GI tract infections
19
Q

amphotericin B distribution

A
  • aqueous insolubility requires formulation with lipids
20
Q

immediate toxicities of amphotericin B

how frequently do these symptoms occur?

A
  • fever
  • chills
  • muscle spasms
  • occur in nearly 100% of patients
21
Q

when do immediate amphotericin toxicities abate

A
  • 30-45 minutes
22
Q

cumulative toxicities of amphotericin B

A
  • nephrotoxicity/acute tubular damage
  • leads to loss of Na+/K+/Mg2+
  • Azotemia
23
Q

amphotericin B cumulative toxicities, effect is _____

A
  • dose dependent
24
Q

what is the safest anti fungal drug used during pregnancy

A
  • amphotericin B
25
Q

Importance of pneumocystis jirovecii in pharmacology

A
  • naturally resistant to almost all anti-fungals
26
Q

how is pneumocystis jirovecii resistant to azoles

A
  • uses cholesterol from host, not ergosterol

- contains natural resistance mutations

27
Q

how is pneumocystis jirovecii resistant to polyenes (amphotericin B)

A
  • lacks ergosterol so amphotericin can’t bind to it
28
Q

sulfonamides MOA

A
  • inhibit pteroate synthase in folic acid biosynthesis pathway
29
Q

trimethoprim MOA

A
  • inhibit DHFR in folic acid biosynthesis pathway
30
Q

how pneumocystis jirovecii can become resistant to SMX/TMP

A
  • mutations in target enzymes (pteroate synthase and DHFR) confer resistance
  • overproduction of PABA may overwhelm drug
31
Q

what is PABA

A
  • early compound in folic acid biosynthesis pathway
32
Q

sulfamethoxazole toxicities

A
  • fever
  • rash
  • photosensitivity
  • urticaria
  • nausea/vomiting
  • Steven’s Johnson syndrome
33
Q

steven’s Johnson syndrome a side effect of

A
  • all sulfonamide drugs
34
Q

trimethoprim side effects

A
  • folate deficiency effects
  • megaloblastic anemia
  • leukopenia
  • granulocytopenia
35
Q

SMX category in pregnancy

A
  • B
36
Q

TMP category in pregnancy

A
  • C
37
Q

When is Amphotericin B used for fungal pneumonia

A

First-line for severe systemic infections
and/or
Immunocompromised patients

38
Q

When are Azoles used for fungal pneumonia

A

Less severe infections, in immunocompetent patients, for prophylaxis or for maintenance following initial amph B

39
Q

risky during pregnancy

A

Azoles and SMZ/TMP

Respiratory Exam 2 (18 decks)

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