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Pharm Spring 2023 > Antifungal Pharmacology > Flashcards

Antifungal Pharmacology Flashcards

1
Q

What is the overall function of the fungal cell membrane/wall

A

To control cellular permeability and protects cell from stress

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2
Q

What does ergosterol do?

A

Maintains cell membrane integrity

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3
Q

What does squalene expoxidase do?

A

Catalyzes first oxygenation step in sterol biosynthesis
*rate limiting step
*if this is targeted then there will be no fungal cell membrane

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4
Q

What is Chitin?

A

Base polysaccharide creating durability for the cell wall
*it is a bridge between the cell membrane and cell wall

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5
Q

What is B-glucan synthase?

A

A complex that synthesizes beta glucans

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6
Q

What is a B-glucan?

A

The most important structural polysaccharide
*B-1,3-D are the most important

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7
Q

What are Azoles?

A
  1. Most commonly used anti fungal agents
  2. The agents are available in large number of formulations
  3. A variety of routes are used
  4. Known for the strong inhibition of many cytochrome P-450 enzymes
    *the Azoles have the potential to result in many serious life-threatening drug interactions
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8
Q

What will CYP inhibitors do? (AZOLES)

A

The CYP inhibitors will allow a certain drug to stay in the body for a prolonged time which increases the drugs potency
*causing serious life threatening interactions

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9
Q

What will CYP inducers do?

A

They will increase metabolism of drugs
*EX: Being on a CYP inducer and warfarin will decrease the warfarin potency making the drug less effective

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10
Q

What is the MOA of Azoles?

A
  1. Will inhibit the synthesis of ergosterol (which helps maintain cell membrane integrity)
  2. The result will be cell death
  3. Azoles inhibit P-450 enzymes midway in the ergosterol pathway
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11
Q

What does Fluconazole (Diflucan) cover?

A

It is the most used Azoles
1. Candidia species
*except C. Glabrata and C. Krusei

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12
Q

What does Fluconazole NOT cover?

A
  1. C. Glabrata
  2. C. Krusei
  3. Aspergillus species
  4. Fusarium species
  5. Zygomycetes
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13
Q

What are the common uses of Fluconazole?

A
  1. Candidiasis
  2. Cryptococcal meningitis
    *has excellent CNS penetration
  3. Prophylaxis against candida (trying to prevent candida infection before it happens)
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14
Q

What is the most common dose of Fluconazole?

A

Vaginal 150mg X 1 dose

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15
Q

What are the SE or ADRs of Fluconazole?

A

Generally well-tolerated
1. GI” distress
2. Rash
3. Hepatic toxicity

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16
Q

What are the drug interaction of Fluconazole?

A
  1. Inhibits CYP3A4 and CYP2C9
    *be careful with lovastatin, simvastatin and warfarin
  2. QT prolongation
  3. Lower likelihood of serious drug interactions vs other Azoles
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17
Q

What dosing adjustments should be made with Fluconazole?

A
  1. Decrease dose by 50%
  2. It is the only Azoles that is cleared renally
    *adjust for renal clearance
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18
Q

What is the common use for Miconazole?

A
  1. Vulvovaginal candidiasis
  2. In many OTC creams, powders, and gel
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19
Q

What is a common drug form of clotrimazole?

A
  1. Creams, ointments, for topical applications
  2. Available in a 10mg troche (cough drop) used 5 times a day for 7-14 days oropharyngeal candidas
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20
Q

What WAS ketoconazole made into?

A
  1. An oral formulation
    *no longer used due to the potentially fatal liver and adrenal complications
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21
Q

What are the common forms of Ketoconazole?

A

Creams, gels, shampoo

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22
Q

What are the ADRs of ketoconazole?

A
  1. Hepatoxicity
  2. QTc prolongation (which happens for all Azoles)
23
Q

What does Itraconazole cover?

A
  1. Adds sensitivity to what Fluconazole did not
    *aspergillosis
    *C. Glabrata
    *C. Krusei
24
Q

What is the correct way to take the solution formulation of Itraconazole?

A

*Preferred for systemic infections
1. Has better bioavailability (more stays in our system)
2. Take on an empty stomach

25
Q

What is the correct way to take he capsule formulation of Itraconazole?

A
  1. Taken with a full meal (to increase absorption)
26
Q

What is the common use of Itraconazole?

A
  1. Treat fungal infections in both immunocompromised and immunocompetent hosts
27
Q

When will Itraconazole will used when a patient is refractory to amphotericin B?

A

When a patient has Aspergillosis
*Itraconazole is commonly used

28
Q

If a patient is using Itraconazole and has onychomycosis of the toenails and fingernails how long is the tretment?

A

12 weeks

29
Q

What are the ADR/ SE of Itraconazole?

A
  1. Nausea
  2. CHF exacerbation (do not use in heart failure patients)
30
Q

What are the drug interactions of Itraconazole?

A
  1. Strong inhibitor of CYP3A4
    *should not be used with many other drugs
31
Q

What does Voriconazole have better activity against?

A

Improved activity against: Aspergillosis (first line agent for this infection)
More reliable activity: C. Glabrata and C. Krusei

32
Q

What do Echinocandins have the most activity against?

A
  1. Candida species
    *including C. Krusei and C. Glabrata
  2. Aspergillus
33
Q

What is the problem with using Echinocandins?

A
  1. Only available for IV administration
  2. Very expensive
34
Q

When would Echinocandins generally be used?

A
  1. Esophageal candidiasis
  2. Systemic Candida infections
  3. Empiric treatment of presumed fungal infections
    *Used as a last resort
35
Q

What is the MOA of Echinocandins?

A
  1. Inhibit the synthesis of B (1-3) D-glucagan
    *It is an essential component of the fungal cell membrane
36
Q

What is the ADR risk of Echinocandins?

A
  1. Low risk of SE
37
Q

What are the common Echinocandins?

A
  1. Caspofungin (cancidas)
  2. Micafungin (mycamine)
    *Histamine-like effects
  3. Anidulafungin (Eraxis)
38
Q

What is the most commonly used Echinocandins?

A

Caspofungin
*have dosing adjustments

39
Q

What are the common CYP inducers?

A
  1. Phenytoin
  2. Rifampin
  3. Carbamazepine
    *These will reduce the drug substrate
    *The drug will be less effective
40
Q

What are the characteristics of the Amphotericin B products?

A
  1. Have the BROADEST activity of all anti fungal agents
41
Q

What is the MOA of Amphotericin B?

A
  1. The polyene structure
    *it binds to ergosterol IN the fungal cell membrane and leads to loss of membrane integrity and cell death
42
Q

What is conventional amphotericin B?

A

Deoxycholate
*not used as much bc of the development of several effective and less toxic agents
*least expensive

43
Q

What are some of the ADRs of deoxycholate?

A
  1. Infusion reactions
    *Fever
    *chills
    *headaches
  2. Nephrotoxicity
44
Q

What are the characteristics of Lipid-base Amphotericin B?

A
  1. Can be prescribe 2 times the does as conventional Amphotericin B
    *Conventional cannot exceed 1.5mg/kg/day (will lead to cardiopulmonary arrest)
  2. Expensive
45
Q

What are the different types of lipid-base amphotericin B

A
  1. Abelcef
  2. AmBisome
  3. Amphotec
46
Q

What are the ADRs of lipid-base Amphotericin B

A
  1. Much less likely to result in nephrotoxicity/electrolyte disorders vs conventional
  2. Infusion reactions are less likely
  3. Liver toxicities appear more likely with lipid-based products bs conventional
47
Q

What is the MOA of Nystatin?

A

Similar to Amphotericin
*Will bind to ergosterol IN fungal cell membrane and leads to loss of membrane integrity and cell death

48
Q

What are some formulations of Nystain?

A
  1. Topical products (creams, ointments, powders, vaginal suppositories)
  2. Suspension that is used for thrush
49
Q

What is the typical dosage for Nystatin?

A
  1. 5ml 4 times a day for 7-14 days
  2. Swish and spit / swish and swallow (if thrush has spread to throat)
50
Q

What is the mechanism of flucytosine (Ancoban)

A
  1. Interferes with fungal DNA synthesis (works inside the cell)
51
Q

What is Flucytosine (Ancoban) most commonly used for?

A
  1. Cryptococcal meningitis
    *will always be used in COMBO with another drug
    *Amphotericin B
52
Q

What should happen to the dosage of Flucytosine (Ancoban) if a patient has renal failure?

A

Decrease the dosage

53
Q

What are the ADRs of Flucytosine (Ancoban)?

A
  1. Can result in life-threatening bone marrow toxicity
    *monitor CBC with diff
54
Q

What is Terbinafine available as?

A
  1. Cream for topical applications (skin, hair, nails)
  2. Tablet for nail infections
    *250mg QD for at least 6 weeks

Pharm Spring 2023 (27 decks)

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