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Pharmacology (2014-2018) > Anti-fungal drugs > Flashcards

Anti-fungal drugs Flashcards

1
Q

True of amphotericin B EXCEPT
A. It is the most potent among all the anti-fungals
B. It is a polyene antifungal
C. It creates pores in the fungal membrane
D. It can cause gynecomastia

A

D. Antifungals trans. Amphotericin B is a polyene macrolide (others are nystatin and natamycin) whose MOA is interaction with sterols in cell membranes to form channels or pores through the membrane (consequence is leakage of intracellular ions like K+). It is the gold standard and has the broadest spectrum for yeasts, and is reserved for treatment of life-threatening fungal infections

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2
Q

True of ketoconazole
A. Is a polyene antifungal
B. Has good CNS penetration
C. Inhibits ergosterol formation by inhibiting fungal cytochrome P450 enzymes
D. Has no effect on testosterone synthesis

A

C. Antifungals trans. Azoles are fungistatic drugs, divided into 2 classes: imidazoles or triazoles (Ketoconazole is an imidazole.) Its MOA is reduction of ergosterol synthesis by inhibiting cytochrome P450 enzymes. It has poor CNS penetration and it interferes with synthesis of adrenal hormones (may cause Cushing’s; would also affect DHEAS production by the zona reticularis, and DHEAS is an intermediate in the synthesis of androgens)

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3
Q

True of fluconazole
A. Has numerous infusion-related adverse effects
B. is the most potent of all azoles
C. Has poor CNS penetration
D. May be used for the treatment of Cryptococcus neoformans and Candida infections

A

D. Antifungals trans. “Azole of choice in treatment and secondary prophylaxis of cryptococcal meningitis…IV fluconazole has equivalent efficacy to amphotericin B in treatment of candidemia in ICU patients…”

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4
Q

Itraconazole
A. Inhibits DNA synthesis
B. Treatment of histoplasmosis, aspergillosis, blastomycosis, cryptococcosis (not CNS) and coccidiomycosis
1C. Is a polyene antifungal
D. May be used to treat Cryptococcus neoformans meningitis

A

B. Antifungals trans. MOA of azoles is interruption of ergosterol synthesis, and it cannot cross the BBB, thus, it cannot be used to treat C. neoformans meningitis.

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5
Q 
Adverse effects of amphotericin B includes the following EXCEPT
A. Azotemia
B. Potassium loss
C. Anemia
D. SLE
A

D. Antifungals trans. “K+ loss due to pores in membranes…variable azotemia…anemia due to reduced erythropoietin production…”

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6
Q 
Adverse effects of voriconazole include the following EXCEPT
A. Visual disturbances 
B. Nephrotoxicity 
C. Fever
D. Rash
A

B. From Katzung: “Observed toxicities include rash, elevated hepatic enzymes…Visual disturbances are common…Photosensitivity dermatitis is commonly observed in patients receiving chronic therapy…”
No mention of fever or nephrotoxicity explicitly, but azoles are relatively safe drugs. Fever is a common ADR, but nephrotoxicity is a notable ADR, so it should have been stated if ever it were observed.

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7
Q

The mechanism of action of caspofungin is by
A. Creation of pores in the fungal membrane
B. Inhibits ergosterol synthesis
C. Inhibits synthesis of beta glucan synthase
D. Inhibits peptidoglycan synthesis

A

C. Caspofungin is an echinocandin. MOA: inhibit cell wall synthesis by inhibiting β-(1,3)-glucan synthase.

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8
Q 
The appropriate treatment of Cryptococcus neoformans meningitis is
A. Itraconazole
B. Amphotericin B with flucytosine
C. Voriconazole
D. Ketoconazole
A

B. “Often used as initial induction regimen for serious fungal infections, then replaced by one of the newer azole drugs for chronic therapy or prevention of relapse (e.g. for cryptococcosis: amphotericin B = initial tx, flucystosine = adjuvant tx, fluconazole = completetion tx)

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9
Q 
Drug class that inhibits the P450-dependent enzymes involved in the biosynthesis of fungal ergosterol:
	A. Polyenes
	B. Azoles
	C. Echinocandins
	D. Allylamine
A

B

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10
Q 
The following is a triazole which is considered to be relatively less toxic and with greater specificity:
	A. Imidazole
	B. Ketoconazole
	C. Clotrimazole
	D. Fluconazole
A

D

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11
Q 
Drug that has the broadest spectrum among the antifungals:
A.     Amphotericin B
B.     Ketoconazole
C.      Flucytosine
D.     Griseofulvin
A

A

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12
Q 
Which of the following drugs is almost exclusively used for candidiasis (especially oropharyngeal candidiasis)?
	A. Griseofulvin
	B. Nystatin
	C. Flucytosine
	D. Fluconazole
A

B

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13
Q 
Anti-fungal drug that acts by interrupting DNA and RNA synthesis in the fungal cell:
A. Polyenes
B. Azoles
C. Flucytosine
D. Echinocandins
A

C

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14
Q 
The following drugs are fungistatic EXCEPT:
	A. Polyenes
	B. Azoles
	C. Antimetabolite (Flucystosine)
D. Allylamines
A

A

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15
Q

The following is a characteristic typical of the imidazoles (versus triazoles):
A. The imidazoles are more selective for fungal cytochrome P450 than for the human enzyme
B. Ketoconazole is an example that is used for systemic fungal infections
C. Has replaced amphotericin B for serious fungal infections
D. Has poor CNS penetration

A

D

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16
Q

The following are correct ways to address cryptococcal meningitis:
A. IV Amphotericin B as monotherapy
B. IV Amphotericin B plus Flucytosine
C. Intrathecal Amphotericin B then fluconazole oral or IV
D. Intrathecal Amphotericin B then IV Ketoconazole

A

C

17
Q

The mechanism of action of the allylamine Terbinafine:
A. Inhibition of cytochrome P450 enzyme
B. Creation of a pore which cause extrusion of the protoplasm and egress of
C. Inhibition of DNA and RNA synthesis
D. Inhibition of enzyme squalene 2,3-epoxidase causing accumulation of squalene

A

D

18
Q

The most specific of all the azoles in terms of favoring inhibition of the fungal enzyme rather than human microsomal liver enzymes:

a. Ketoconazole
b. Fluconazole
c. Itraconazole
d. Miconazole

A

B

19
Q 
The following systemically administered antifungals are indicated for systemic mycoses: 
A. Griseofulvin
B. Allylamine (Terbinafine)
C. Clotrimoxazole
D. Amphotericin B
A

D

20
Q 
Drug of choice for onychomycosis:
A. Terbinafine
B. Amorolfine
C. Griseofulvin
D. Clotrimoxazole
A

D

21
Q 
You have a diabetic patient with vulvovaginal candidiasis. She is up and about but complaining of severe pruritus in the genital area and vaginal discharge. She is also on statins, a drug known to be metabolized by the liver miicrosomal enzymes (CYP450). Which of the following drugs should be avoided?
	A. Terbinafine
	B. Ketoconazole
	C. Flucytosine
	D. Griseofulvin
A

B

22
Q 
The following may be given for tinea corporis (an-an/hadhad) in the skin of the arm EXCEPT:
	A. Terbinafine cream
	B. Clotrimazole cream	
	C. Topical amphotericin B
	D. Topical miconazole
A

C

Pharmacology (2014-2018) (23 decks)

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