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Classifications of Antifungal Agents: Systemic Antifungal Drugs for Systemic Infections

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What is the main mechanism of action of Amphotericin B?

Disrupting fungal membrane permeability and transport properties

How is Amphotericin B usually administered for systemic infections?

Intravenously as a nonlipid colloidal suspension or in a liposomal formulation

What is the bioavailability of oral Amphotericin B for systemic disease treatment?

Effective only on fungi within the gastrointestinal tract lumen

Why is Amphotericin B not suitable for treatment of central nervous system (CNS) fungal infections?

It cannot penetrate the blood-brain barrier effectively

How is Amphotericin B primarily eliminated from the body?

Renal excretion

What percentage of Amphotericin B is bound by serum proteins in the bloodstream?

More than 90%

What is the main mechanism of action of amphotericin B?

Binding to ergosterol and causing pore formation

Why does resistance to amphotericin B arise?

Decrease in ergosterol membrane concentration

Which fungal infection is NOT commonly treated with amphotericin B?

Streptococcus

What is a common toxic effect associated with amphotericin B colloidal formulations?

Nephrotoxicity

How can infusion-related toxicity with amphotericin B be reduced?

AOTA

What is the reason for using lipid formulations of amphotericin B?

To decrease toxicity to mammalian cells

What is the mechanism by which flucytosine exerts its antifungal activity?

It inhibits fungal DNA and RNA synthesis

What is the primary reason for combining flucytosine with amphotericin B during initiation treatment?

To reduce the risk of resistance developing to flucytosine

How is flucytosine primarily excreted from the body?

Unchanged in the urine

What is the mechanism of resistance to flucytosine?

Altered metabolism of the drug

Which of the following is NOT a potential toxicity associated with flucytosine?

Nephrotoxicity

For which fungal infection is flucytosine commonly used in combination with other antifungal agents?

Cryptococcal meningitis

Which class of azoles includes fluconazole?

Triazoles

What is a characteristic feature of fluconazole's bioavailability?

High bioavailability

For which fungal infection is fluconazole NOT effective according to the text?

Aspergillosis

What makes fluconazole the azole of choice for Cryptococcal meningitis and mucocutaneous candidiasis?

High degree of water solubility

Which fungal infection can high doses of fluconazole help obviate the need for intrathecal amphotericin B?

Cryptococcal meningitis

What is a distinguishing factor of fluconazole's effect on hepatic microsomal enzymes compared to other azoles?

No effect

Which of the following statements about voriconazole is correct?

It has a broader spectrum than fluconazole.

Which of the following is NOT a potential toxicity associated with voriconazole?

Nephrotoxicity

Which of the following statements about itraconazole is correct?

It does not affect mammalian steroid synthesis.

Which of the following statements about posaconazole is correct?

It is effective against mucormycosis.

Which of the following statements about isavuconazole is correct?

It is licensed for treatment of invasive mucormycosis and invasive aspergillosis.

Which of the following statements about ketoconazole is correct?

It is too toxic for systemic use, so it is only available as topical preparations.

Which of the following is a characteristic of echinocandins?

They inhibit the synthesis of β(1-3)glucan, a critical component of fungal cell walls

Which of the following is a potential toxicity associated with caspofungin?

Infusion-related effects like headache and flushing

What is a distinguishing characteristic of micafungin compared to caspofungin?

It increases the levels of cyclosporine and sirolimus

Which echinocandin has the longest half-life?

Anidulafungin

Which echinocandin is used for the treatment of esophageal and invasive candidiasis?

Anidulafungin

Which of the following statements about echinocandins is correct?

They have minimal drug interactions

Which antifungal drug is keratophilic and requires administration for 2-6 weeks for skin and hair infections?

Griseofulvin

Which toxicity is specifically associated with griseofulvin use?

AOTA

Why must griseofulvin be administered for months in the case of nail infections?

To allow regrowth of the new protective nail

Which drug has an unclear mechanism of action at the cellular level but binds to newly forming skin?

Griseofulvin

What is the mechanism of action of griseofulvin?

It binds to keratin in newly forming skin, protecting it from infection

Which of the following statements is true regarding the absorption of griseofulvin?

It is improved when taken with fatty foods

What is the mechanism of action of terbinafine at the cellular level?

Inhibits squalene epoxidase

Which of the following statements about terbinafine is true?

It is a keratophilic drug, effective for dermatophytosis

How does terbinafine exert its antifungal effect?

By inhibiting the fungal enzyme squalene epoxidase

What is a potential adverse effect associated with terbinafine?

Gastrointestinal upset

What is the mechanism of action of nystatin?

It binds to ergosterol, disrupting fungal membranes

Which of the following is an advantage of nystatin?

It has low toxicity when used topically

Which of the following is a common indication for nystatin?

Oropharyngeal thrush

Which of the following statements about clotrimazole and miconazole is correct?

They can be used over-the-counter for vulvovaginal candidiasis

What is a common use of topical ketoconazole?

Treatment of seborrheic dermatitis

Which of the following statements about the absorption of topical antifungals is correct?

Absorption of these agents from the skin and mucous membranes is negligible

What is the most common indication for the use of nystatin?

Oral thrush

Which antifungal agent is used as a pleasant-tasting alternative to nystatin for the treatment of oral thrush?

Clotrimazole

Which topical antifungal is effective against tinea cruris and tinea corporis?

Terbinafine

Which topical antifungal is specifically useful for dermatophytic infections?

Clotrimazole

Which topical antifungal is most commonly used for intertriginous candidal infections?

Nystatin

This quiz covers the classifications of systemic antifungal drugs, focusing on Amphotericin B as a fungicidal drug with a broad spectrum. It discusses its administration, resistance, and effectiveness. Test your knowledge on systemic antifungal agents with this quiz!

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