Antifungal drugs Flashcards

1
Q

What are anti fungal drugs used for?

A

Used to treat/prevent fungal disease

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2
Q

What are fungal diseases known as?

A

Mycoses - Superficial: nail, scalp, mucous membranes. Systemic: affect internal organs - fatal.

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3
Q

What are fungal pathogens?

A

Eukaryotes an opportunistic pathogens.

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4
Q

What are the most common opportunistic fungal pathogens?

A

Candida albicans, aspergilus fumigatus, cryptococcus neofromans.

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5
Q

What puts patients at higher risk of developing fungal infections?

A

Impaired immune system - HIV/AIDS, organ transplantation, long-term abx, cancer. Menstrual cycle in women - 70% experience one episode of vaginitis caused by C.albicans.

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6
Q

What are the targets for anti fungal drugs?

A

Cell wall, plasma membrane, nucleus - DNA and RNA synthesis.

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7
Q

What does the fungal cell wall consist of?

A

Skeletal components - Glucan and Chitin.
Matrix components.
B1,3-Glucan - anti fungal targets.

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8
Q

What drugs inhibit the enzyme and synthesis of B1,3-Glucan?

A

Echinocandins: Caspofungin and Micafungin.

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9
Q

What is the difference between fungal plasma membranes and human plasma membranes?

A

Fungal cells contain ergosterol whereas human cells contain cholesterol. Fungal cells cannot grow and survive without ergosterol.

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10
Q

What is the action of antifungals that target ergosterol?

A

Either bind to resident ergosterol in the PM or inhibit different ergosterol biosynthetic enzymes and block synthesis of ergosterol.

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11
Q

What are the drugs called that bind to resident ergosterol?

A

Polyene Antifungals

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12
Q

How to Polyene Antifungals work?

A

Bind to ergosterol and form pores in the PM. The pores disrupt the membrane integrity causing leakage of cell contents.

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13
Q

What are the names of some polyene antifungals?

A

Amphotericin B.

Nystatin - used in oral and GI fungal infections.

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14
Q

What are the side effects of polyene antifungals?

A

Prolonged use has severe side effects such as kidney failure.

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15
Q

What are the drugs called that inhibit ergosterol biosynthesis?

A

Azoles.

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16
Q

How do Azoles work?

A

Inhibit the enzyme Lanosterol C-14 demethylase. This blocks ergosterol synthesis and leads to accumulation of toxic intermediates.

17
Q

What are the two types of azoles?

A

Imidazoles and Triazoles.

18
Q

Examples of Imidazoles?

A

Miconazole, Clotrimazole, Ketconazole.

19
Q

Examples of triazoles?

A

Fluconazole, Voriconazole, Itraconazole.

20
Q

What do Allylamines do?

A

Inhibit squalene to prevent the synthesis of ergosterol.

21
Q

Examples of Allylamines?

A

Terbinafine, Amorolfine.

22
Q

What drug targets RNA and DNA synthesis?

A

Flucytosine.

23
Q

What is resistance to antifungals caused by?

A

Decreased accumulation of the drug, inactivation of the drug, mutations in drug target-encoding genes.