Azole derivatives Flashcards

1
Q

Azole derivatives (2 groups)

A

Diazole compounds

Triazole compounds

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2
Q

Diazole compounds (3 drugs)

A

Clotrimazole
Econazole
Ketoconazole

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3
Q

Triazole compounds (4 drugs)

A

Fluconazole
Itraconazole
Posaconazole
Voriconazole

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4
Q

Azole derivatives that can be adm IV (2 drugs)

A

Fluconazole

Voriconazole

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5
Q

Azole drugs that cannot be used with drugs that decrease gastric acid (3 drugs)

A

Ketoconazole
Itraconazole
Posaconazole

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6
Q

Only azole drug used for fungal meningitis

A

Fluconazole (both prophylaxis and treatment)

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7
Q

Azole drugs - adverse effects

A

Birth defects

Systemic adm: Hepatic injury, hematopoietic toxicity

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8
Q

Azole drugs - interactions

A
Inhibits metabolism of:
HMG-CoA reductase inhibitors
Some benzodiazepines 
Quinidine
Warfarin
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9
Q

Azole drugs - contraindications

A

Pregnancy (Cat D for longterm, high doses. Cat C for short term, vaginal)

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10
Q

Itraconazole - indications

A

Systemic mycoses: Blastomycosis, histoplasmosis.

Superficial mycoses: onychomycosis (nails)

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11
Q

Itraconazole - amdinistration

A

Orally in pulse dosing

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12
Q

Fluconazole - indications

A

Cryptococcal meningitis in AIDS
Mucocutaneous and disseminated candidiasis
UTI by candida

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13
Q

Azole drug for single dose adm for acute vaginal candidiasis (1 drug)

A

Fluconazole

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14
Q

Second generation triazoles (2 drugs)

A

Voriconazole

Posaconazole

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15
Q

Voriconazole - indications

A

Invasive aspergillosis
Esophageal candidiasis
Invasive candidiasis

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16
Q

Voriconazole - interactions

A

Additive activity with caspofungin (used for treatment of invasive aspergillosis)

17
Q

Voriconazole - adverse effects

A
Visual disturbances (altered light perception, chromatopsia, photophobia).
Increased liver enzymes, liver failure (with death sometimes)
18
Q

Posaconazole - indications

A

Systemic infections not responding to other agents (aspergillus, fusarium, rhizopus, mucormycosis)

19
Q

Which azole drug has higher incidence of drug interactions

A

Ketoconazole

20
Q

Ketoconazole - indications and adm

A

Adm topical for seborrheic dermatitis

21
Q

Clotrimazole and econazole - indications

A

Candida (mouth, throat, vagina, vulva)
Tinea versicolor
Tinea pedis, tinea cruris

22
Q

Clotrimazole and econazole (+other topicals) are not effective for…

A

Tinea capitis

Tinea unguium/onychomycosis

23
Q

Azole drugs - MOA

A

Inhibits 14α-demethylase, and conversion of lanosterol to ergosterol