Antifungal Drugs
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Questions and Answers

What is the main target for chemotherapeutic agents in fungi?

  • Eukaryotic cell wall (correct)
  • Prokaryotic cell wall
  • Mitochondria
  • Nucleus

Why are antibiotics ineffective against fungi?

  • Fungi are resistant to all antibiotics
  • Fungi reproduce asexually
  • Fungi lack a cell membrane
  • Fungi have a different cell wall composition (correct)

What has led to an increased incidence of mycoses?

  • Improved sanitation
  • Cancer chemotherapy (correct)
  • Vaccination programs
  • Antibiotic use

What is the main component of the fungal cell membrane?

<p>Ergosterol (B)</p> Signup and view all the answers

Which type of infections are caused by fungi extending into the epidermis?

<p>Cutaneous mycoses (A)</p> Signup and view all the answers

What is the role of organ transplantation in the increased incidence of mycoses?

<p>It leads to immune suppression (B)</p> Signup and view all the answers

Why are mycotic infections difficult to treat in patients undergoing cancer chemotherapy?

<p>Due to immune suppression (A)</p> Signup and view all the answers

Which antifungal drug is considered the drug of choice for onychomycosis?

<p>Terbinafine (C)</p> Signup and view all the answers

Which antifungal drug is known for causing taste and visual disturbances as adverse effects?

<p>Terbinafine (C)</p> Signup and view all the answers

Which antifungal drug is contraindicated in pregnancy and patients with porphyria?

<p>Griseofulvin (D)</p> Signup and view all the answers

Which antifungal drug is used for the treatment of cutaneous and oral Candida infections?

<p>Nystatin (A)</p> Signup and view all the answers

Which antifungal drug is rarely used today due to the risk for severe liver injury, adrenal insufficiency, and adverse drug interactions?

<p>Ketoconazole (B)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor?

<p>Terbinafine (D)</p> Signup and view all the answers

Which antifungal drug is highly protein-bound and deposited in skin, nails, and adipose tissue?

<p>Terbinafine (A)</p> Signup and view all the answers

Which antifungal drug is metabolized in the liver and excreted in the urine, and should be avoided in patients with moderate to severe renal impairment or hepatic dysfunction?

<p>Terbinafine (B)</p> Signup and view all the answers

Which antifungal drug is used for tinea corporis, tinea cruris, tinea pedis, and oropharyngeal and vulvovaginal candidiasis?

<p>Ketoconazole (C)</p> Signup and view all the answers

What is the mechanism of action of Amphotericin B?

<p>Binding to ergosterol, forming pores, disrupting membrane function, and causing cell death (C)</p> Signup and view all the answers

What is the main route of administration for Amphotericin B?

<p>Slow IV infusion (B)</p> Signup and view all the answers

What is the primary adverse effect of Flucytosine (5-FC)?

<p>Bone marrow toxicity (B)</p> Signup and view all the answers

What is the reason Flucytosine is not used alone?

<p>High susceptibility of resistance (B)</p> Signup and view all the answers

What is the mechanism of action of Azole antifungals?

<p>Reducing ergosterol synthesis and inhibiting 14 α-demethylase (B)</p> Signup and view all the answers

What is the primary resistance mechanism related to Amphotericin B?

<p>Ergosterol content and structure (B)</p> Signup and view all the answers

What is the main reason for the slow IV infusion of Amphotericin B?

<p>Water insolubility (B)</p> Signup and view all the answers

Which class of antifungal agents acts on the cell wall and has potent activity against Aspergillus and most Candida species?

<p>Echinocandins (C)</p> Signup and view all the answers

Which antifungal drug is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis?

<p>Caspofungin (C)</p> Signup and view all the answers

Which antifungal drug has a broad spectrum of activity and is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses?

<p>Voriconazole (D)</p> Signup and view all the answers

Which antifungal drug is the least active triazole with a spectrum limited to yeast and some dimorphic fungi?

<p>Fluconazole (B)</p> Signup and view all the answers

Which enzyme do azole antifungals inhibit, leading to drug interactions with medications metabolized by the same enzyme?

<p>Hepatic CYP450 3A4 isoenzyme (B)</p> Signup and view all the answers

Which class of antifungal agents is teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to the fetus?

<p>Azole antifungals (B)</p> Signup and view all the answers

Which squalene epoxidase inhibitor is commonly used to treat cutaneous mycotic infections caused by mold-like fungi?

<p>Terbinafine (D)</p> Signup and view all the answers

Which antifungal drug is associated with the adverse effect of hepatotoxicity and requires monitoring of liver function tests during therapy?

<p>Ketoconazole (C)</p> Signup and view all the answers

Which antifungal drug is a prodrug that is converted to 5-fluorouracil by cytosine deaminase in susceptible fungi?

<p>Flucytosine (A)</p> Signup and view all the answers

Which antifungal drug has the potential to cause QT interval prolongation and visual disturbances as adverse effects?

<p>Voriconazole (C)</p> Signup and view all the answers

Which antifungal drug acts by binding to the fungal cell membrane ergosterol, resulting in the formation of pores and leakage of intracellular components?

<p>Nystatin (A)</p> Signup and view all the answers

Which antifungal drug is associated with the adverse effect of skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis?

<p>Voriconazole (A)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor used for the treatment of dermatophyte infections such as tinea pedis and tinea corporis?

<p>Terbinafine (D)</p> Signup and view all the answers

Which antifungal drug is contraindicated in pregnancy due to its association with skeletal abnormalities and embryotoxicity in animal studies?

<p>Griseofulvin (A)</p> Signup and view all the answers

Which adverse effect is specifically associated with Flucytosine (5-FC)?

<p>Bone marrow toxicity (D)</p> Signup and view all the answers

What is the primary mechanism of action of Azole antifungals?

<p>Reducing ergosterol synthesis and inhibiting 14 α-demethylase (A)</p> Signup and view all the answers

What is the main reason for the restricted antifungal spectrum of Flucytosine (5-FC)?

<p>High susceptibility of resistance (C)</p> Signup and view all the answers

Which antifungal drug is administered parenterally through slow IV infusion due to its water insolubility?

<p>Amphotericin B (C)</p> Signup and view all the answers

What is the main factor related to Amphotericin B resistance?

<p>Ergosterol content and structure (A)</p> Signup and view all the answers

Which antifungal drug is well-absorbed orally and penetrates the CSF?

<p>Itraconazole (D)</p> Signup and view all the answers

What is the primary mechanism of action of Amphotericin B?

<p>Binding to ergosterol, forming pores, disrupting membrane function, and causing cell death (A)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor commonly used to treat cutaneous mycotic infections caused by mold-like fungi?

<p>Terbinafine (D)</p> Signup and view all the answers

Which antifungal drug is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis?

<p>Caspofungin (A)</p> Signup and view all the answers

Which antifungal drug has a broad spectrum of activity and is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses?

<p>Voriconazole (A)</p> Signup and view all the answers

Which antifungal drug is highly protein-bound and deposited in skin, nails, and adipose tissue?

<p>Itraconazole (B)</p> Signup and view all the answers

Which class of antifungal agents acts on the cell wall and has potent activity against Aspergillus and most Candida species?

<p>Echinocandins (C)</p> Signup and view all the answers

Which antifungal drug is metabolized in the liver and excreted in the urine, and should be avoided in patients with moderate to severe renal impairment or hepatic dysfunction?

<p>Itraconazole (D)</p> Signup and view all the answers

Which antifungal drug is the least active triazole with a spectrum limited to yeast and some dimorphic fungi?

<p>Fluconazole (A)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor and is the drug of choice for onychomycosis?

<p>Terbinafine (C)</p> Signup and view all the answers

Which antifungal drug causes disruption of mitotic spindle, is deposited in newly forming skin, and used for dermatophytosis of the scalp and hair?

<p>Griseofulvin (D)</p> Signup and view all the answers

Which antifungal drug is used for the treatment of cutaneous and oral Candida infections and is not absorbed from the GI tract?

<p>Nystatin (B)</p> Signup and view all the answers

Which antifungal drug is known for causing taste and visual disturbances as adverse effects, and is an inhibitor of CYP450 2D6 isoenzyme?

<p>Terbinafine (B)</p> Signup and view all the answers

Which antifungal drug has historically been used for the treatment of systemic fungal infections but is rarely used today due to the risk for severe liver injury, adrenal insufficiency, and adverse drug interactions?

<p>Ketoconazole (A)</p> Signup and view all the answers

Which antifungal drug is used for tinea corporis, tinea cruris, tinea pedis, and oropharyngeal and vulvovaginal candidiasis?

<p>Miconazole (A)</p> Signup and view all the answers

Which antifungal drug has a prolonged half-life of 200 to 400 hours and is highly protein-bound and deposited in skin, nails, and adipose tissue?

<p>Terbinafine (C)</p> Signup and view all the answers

Which antifungal drug is contraindicated in pregnancy and patients with porphyria, and induces hepatic CYP450 leading to drug-drug interactions?

<p>Griseofulvin (C)</p> Signup and view all the answers

Which antifungal drug is used for the treatment of tinea capitis and requires oral formulation?

<p>Terbinafine (A)</p> Signup and view all the answers

Which class of antifungal agents acts on the cell wall and has potent activity against Aspergillus and most Candida species?

<p>Echinocandins (C)</p> Signup and view all the answers

Which antifungal drug is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses?

<p>Voriconazole (A)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor commonly used to treat cutaneous mycotic infections caused by mold-like fungi?

<p>Terbinafine (B)</p> Signup and view all the answers

Which antifungal drug is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis?

<p>Caspofungin (B)</p> Signup and view all the answers

Which antifungal drug is a prodrug that is converted to 5-fluorouracil by cytosine deaminase in susceptible fungi?

<p>Flucytosine (A)</p> Signup and view all the answers

Which antifungal drug is used for tinea corporis, tinea cruris, tinea pedis, and oropharyngeal and vulvovaginal candidiasis?

<p>Fluconazole (C)</p> Signup and view all the answers

Which antifungal drug is the least active triazole with a spectrum limited to yeast and some dimorphic fungi?

<p>Fluconazole (B)</p> Signup and view all the answers

Which antifungal drug is associated with the adverse effect of skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis?

<p>Fluconazole (C)</p> Signup and view all the answers

What is the main factor related to Amphotericin B resistance?

<p>Altered cell membrane composition (C)</p> Signup and view all the answers

What is the primary resistance mechanism related to Amphotericin B?

<p>Altered cell membrane composition (B)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor commonly used to treat cutaneous mycotic infections caused by mold-like fungi?

<p>Terbinafine (D)</p> Signup and view all the answers

What is the main target for chemotherapeutic agents in fungi?

<p>Ergosterol (B)</p> Signup and view all the answers

Which antifungal drug is metabolized in the liver and excreted in the urine, and should be avoided in patients with moderate to severe renal impairment or hepatic dysfunction?

<p>Itraconazole (B)</p> Signup and view all the answers

What is the main route of administration for Amphotericin B?

<p>Intravenous (D)</p> Signup and view all the answers

What is the mechanism of action of Amphotericin B?

<p>Binding to ergosterol, forming pores, disrupting membrane function, and causing cell death (B)</p> Signup and view all the answers

What is the primary resistance mechanism related to Amphotericin B?

<p>Increased ergosterol content and structure (C)</p> Signup and view all the answers

What is the primary adverse effect of Flucytosine (5-FC)?

<p>Bone marrow toxicity (D)</p> Signup and view all the answers

What is the main factor related to Amphotericin B resistance?

<p>Ergosterol content and structure (B)</p> Signup and view all the answers

What is the primary mechanism of action of Azole antifungals?

<p>Inhibiting ergosterol synthesis (B)</p> Signup and view all the answers

Why is Flucytosine (5-FC) not used alone?

<p>High susceptibility of resistance (B)</p> Signup and view all the answers

How are Azole antifungals administered for the treatment or prophylaxis of cutaneous and systemic mycoses?

<p>Orally (B)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor and is the drug of choice for onychomycosis?

<p>Terbinafine (A)</p> Signup and view all the answers

Which antifungal drug has a prolonged half-life of 200 to 400 hours and is highly protein-bound and deposited in skin, nails, and adipose tissue?

<p>Terbinafine (D)</p> Signup and view all the answers

Which antifungal drug is used for tinea corporis, tinea cruris, tinea pedis, and oropharyngeal and vulvovaginal candidiasis?

<p>Fluconazole (B)</p> Signup and view all the answers

Which antifungal drug is metabolized in the liver and excreted in the urine, and should be avoided in patients with moderate to severe renal impairment or hepatic dysfunction?

<p>Terbinafine (C)</p> Signup and view all the answers

Which antifungal drug resembles amphotericin B and is used for the treatment of cutaneous and oral Candida infections?

<p>Nystatin (A)</p> Signup and view all the answers

Which antifungal drug is a prodrug that is converted to 5-fluorouracil by cytosine deaminase in susceptible fungi?

<p>Flucytosine (C)</p> Signup and view all the answers

Which antifungal drug has historically been used for the treatment of systemic fungal infections but is rarely used today due to the risk for severe liver injury, adrenal insufficiency, and adverse drug interactions?

<p>Ketoconazole (D)</p> Signup and view all the answers

Which antifungal drug is a squalene epoxidase inhibitor commonly used to treat cutaneous mycotic infections caused by mold-like fungi?

<p>Terbinafine (A)</p> Signup and view all the answers

Which antifungal drug is highly protein-bound and deposited in skin, nails, and adipose tissue?

<p>Terbinafine (C)</p> Signup and view all the answers

Antifungal drugs are effective in treating viral infections

<p>False (B)</p> Signup and view all the answers

Fungi have a eukaryotic cellular structure

<p>True (A)</p> Signup and view all the answers

Amphotericin B is administered parenterally through slow IV infusion due to its water solubility

<p>False (B)</p> Signup and view all the answers

Increased incidence of mycoses is related to factors such as cancer chemotherapy and organ transplantation

<p>True (A)</p> Signup and view all the answers

Antifungal drugs are not selective and can also act as antibiotics

<p>False (B)</p> Signup and view all the answers

Mycotic infections can be classified as cutaneous, subcutaneous, or systemic infections

<p>True (A)</p> Signup and view all the answers

Antifungal drugs target the rigid cell wall and cell membrane of fungi

<p>True (A)</p> Signup and view all the answers

Terbinafine is the drug of choice for onychomycosis, and it is better tolerated, with a shorter duration of therapy, and more effective compared to itraconazole or griseofulvin.

<p>True (A)</p> Signup and view all the answers

Terbinafine has a prolonged half-life of 200 to 400 hours.

<p>True (A)</p> Signup and view all the answers

Griseofulvin is still used for dermatophytosis of the scalp and hair and is taken with high-fat meals.

<p>True (A)</p> Signup and view all the answers

Nystatin is absorbed from the gastrointestinal tract and can cause systemic toxicity if given parenterally.

<p>False (B)</p> Signup and view all the answers

Oral ketoconazole is commonly used for the treatment of systemic fungal infections.

<p>False (B)</p> Signup and view all the answers

Imidazoles, such as ketoconazole, are rarely used today due to the risk for severe liver injury, adrenal insufficiency, and adverse drug interactions.

<p>True (A)</p> Signup and view all the answers

Griseofulvin is a squalene epoxidase inhibitor.

<p>False (B)</p> Signup and view all the answers

Flucytosine (5-FC) is used alone for the treatment of systemic fungal infections.

<p>False (B)</p> Signup and view all the answers

Terbinafine is contraindicated in patients with moderate to severe renal impairment or hepatic dysfunction.

<p>True (A)</p> Signup and view all the answers

Amphotericin B is water soluble and can be administered orally.

<p>False (B)</p> Signup and view all the answers

Azole antifungals have different mechanisms of action and similar pharmacokinetic properties.

<p>False (B)</p> Signup and view all the answers

Flucytosine has a broad spectrum of antifungal activity.

<p>False (B)</p> Signup and view all the answers

Amphotericin B resistance is not related to ergosterol content and structure.

<p>False (B)</p> Signup and view all the answers

Flucytosine is well-absorbed orally and penetrates the CSF.

<p>True (A)</p> Signup and view all the answers

Triazoles are only administered topically for the treatment of cutaneous mycoses.

<p>False (B)</p> Signup and view all the answers

The primary mechanism of action of Azole antifungals involves reducing ergosterol synthesis.

<p>True (A)</p> Signup and view all the answers

Fluconazole is the most active triazole with a broad spectrum of activity, including Aspergillus and most Candida species.

<p>False (B)</p> Signup and view all the answers

Voriconazole is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis.

<p>False (B)</p> Signup and view all the answers

Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species.

<p>True (A)</p> Signup and view all the answers

Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine.

<p>True (A)</p> Signup and view all the answers

Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to decreased membrane permeability and cell death.

<p>False (B)</p> Signup and view all the answers

The majority of dermatophytosis is caused by Trichophyton, Microsporum, and Epidermophyton fungi.

<p>True (A)</p> Signup and view all the answers

Micafungin and anidulafungin are substrates for CYP450 enzymes, thus having potential drug-drug interactions.

<p>False (B)</p> Signup and view all the answers

Antifungal drugs are effective in treating viral infections

<p>False (B)</p> Signup and view all the answers

Increased incidence of mycoses can be related to factors such as cancer chemotherapy and organ transplantation

<p>True (A)</p> Signup and view all the answers

Amphotericin B is water soluble and can be administered orally

<p>False (B)</p> Signup and view all the answers

Azole antifungals have different mechanisms of action and similar pharmacokinetic properties

<p>False (B)</p> Signup and view all the answers

Terbinafine is contraindicated in patients with moderate to severe renal impairment or hepatic dysfunction

<p>True (A)</p> Signup and view all the answers

Flucytosine (5-FC) is commonly used alone for the treatment of mycoses

<p>False (B)</p> Signup and view all the answers

Antifungal drugs target the rigid cell wall and cell membrane of fungi

<p>True (A)</p> Signup and view all the answers

Amphotericin B is the drug of choice for life-threatening mycoses.

<p>True (A)</p> Signup and view all the answers

Flucytosine (5-FC) is a synthetic pyrimidine with selective toxicity and is used alone for antifungal treatment.

<p>False (B)</p> Signup and view all the answers

Azole antifungals, including imidazoles and triazoles, share a similar mechanism of action and PK properties.

<p>False (B)</p> Signup and view all the answers

Triazoles are only administered topically for the treatment of cutaneous mycoses.

<p>False (B)</p> Signup and view all the answers

The primary mechanism of action of Azole antifungals involves reducing ergosterol synthesis.

<p>True (A)</p> Signup and view all the answers

Flucytosine adverse effects include bone marrow toxicity, nausea, and vomiting.

<p>True (A)</p> Signup and view all the answers

Amphotericin B resistance is related to ergosterol content and structure.

<p>True (A)</p> Signup and view all the answers

Terbinafine is the drug of choice for onychomycosis and is better tolerated, with a shorter duration of therapy compared to itraconazole or griseofulvin.

<p>True (A)</p> Signup and view all the answers

Oral terbinafine is metabolized in the liver and excreted in the urine, making it safe for patients with moderate to severe renal impairment or hepatic dysfunction.

<p>False (B)</p> Signup and view all the answers

Griseofulvin is still used for onychomycosis and requires 6-12 months of treatment.

<p>False (B)</p> Signup and view all the answers

Nystatin is absorbed from the gastrointestinal tract and can cause systemic toxicity if given parenterally.

<p>False (B)</p> Signup and view all the answers

Imidazoles, such as ketoconazole, are rarely used today due to the risk for severe liver injury, adrenal insufficiency, and adverse drug interactions.

<p>True (A)</p> Signup and view all the answers

Flucytosine is well-absorbed orally and penetrates the central nervous system.

<p>False (B)</p> Signup and view all the answers

Squalene epoxidase inhibitors, such as terbinafine, block the synthesis of ergosterol, leading to decreased membrane permeability and cell death.

<p>True (A)</p> Signup and view all the answers

Oral ketoconazole is commonly used for the treatment of systemic fungal infections.

<p>False (B)</p> Signup and view all the answers

Amphotericin B resistance is related to ergosterol content and structure.

<p>False (B)</p> Signup and view all the answers

Fluconazole is the least active triazole with a spectrum limited to yeast and some dimorphic fungi.

<p>True (A)</p> Signup and view all the answers

Azole antifungals inhibit hepatic CYP450 3A4 isoenzyme, leading to drug interactions with medications metabolized by the same enzyme.

<p>True (A)</p> Signup and view all the answers

Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions.

<p>True (A)</p> Signup and view all the answers

Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death.

<p>True (A)</p> Signup and view all the answers

Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis.

<p>True (A)</p> Signup and view all the answers

Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species.

<p>True (A)</p> Signup and view all the answers

Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine.

<p>True (A)</p> Signup and view all the answers

Antifungal drugs target the rigid cell wall and cell membrane of fungi

<p>True (A)</p> Signup and view all the answers

Azole antifungals, including imidazoles and triazoles, share a similar mechanism of action and PK properties

<p>True (A)</p> Signup and view all the answers

Echinocandins are the newest class of antifungal agents

<p>True (A)</p> Signup and view all the answers

Flucytosine (5-FC) is commonly used alone for the treatment of mycoses

<p>False (B)</p> Signup and view all the answers

Amphotericin B is administered parenterally through slow IV infusion due to its water solubility

<p>True (A)</p> Signup and view all the answers

Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death

<p>False (B)</p> Signup and view all the answers

Triazoles are only administered topically for the treatment of cutaneous mycoses

<p>False (B)</p> Signup and view all the answers

Amphotericin B is the drug of choice for life-threatening mycoses

<p>True (A)</p> Signup and view all the answers

Flucytosine is commonly used alone for the treatment of mycoses

<p>False (B)</p> Signup and view all the answers

Azole antifungals reduce ergosterol synthesis and inhibit 14 α-demethylase

<p>True (A)</p> Signup and view all the answers

Flucytosine is well-absorbed orally and penetrates the CSF

<p>True (A)</p> Signup and view all the answers

Triazoles are only administered topically for the treatment of cutaneous mycoses

<p>False (B)</p> Signup and view all the answers

Nystatin is absorbed from the gastrointestinal tract and can cause systemic toxicity if given parenterally

<p>True (A)</p> Signup and view all the answers

Antifungal drugs are effective in treating viral infections

<p>False (B)</p> Signup and view all the answers

Terbinafine is better tolerated and has a shorter duration of therapy compared to itraconazole or griseofulvin.

<p>True (A)</p> Signup and view all the answers

Oral terbinafine is metabolized in the liver and excreted in the urine, making it suitable for patients with moderate to severe renal impairment or hepatic dysfunction.

<p>False (B)</p> Signup and view all the answers

Griseofulvin is still used for onychomycosis and requires 6-12 months of treatment.

<p>False (B)</p> Signup and view all the answers

Nystatin can be absorbed from the gastrointestinal (GI) tract, leading to systemic toxicity if given parenterally.

<p>False (B)</p> Signup and view all the answers

Oral ketoconazole is widely used for the treatment of systemic fungal infections due to its low risk of severe liver injury and adverse drug interactions.

<p>False (B)</p> Signup and view all the answers

Imidazoles, such as ketoconazole, are commonly used for the treatment of tinea capitis.

<p>False (B)</p> Signup and view all the answers

Flucytosine (5-FC) is used alone for the treatment of systemic fungal infections.

<p>False (B)</p> Signup and view all the answers

Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions.

<p>True (A)</p> Signup and view all the answers

Squalene epoxidase inhibitors, such as terbinafine, block the synthesis of ergosterol, leading to decreased membrane permeability and cell death.

<p>True (A)</p> Signup and view all the answers

Fluconazole is the most active triazole with a broad spectrum of activity, including Aspergillus and most Candida species.

<p>False (B)</p> Signup and view all the answers

Voriconazole is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses.

<p>True (A)</p> Signup and view all the answers

Echinocandins act on the cell wall and have potent activity against Aspergillus and most Candida species.

<p>True (A)</p> Signup and view all the answers

Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis.

<p>True (A)</p> Signup and view all the answers

Micafungin and anidulafungin are substrates for CYP450 enzymes, thus having potential drug-drug interactions.

<p>False (B)</p> Signup and view all the answers

Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death.

<p>True (A)</p> Signup and view all the answers

The majority of dermatophytosis is caused by Trichophyton, Microsporum, and Epidermophyton fungi.

<p>True (A)</p> Signup and view all the answers

Flashcards

Azole Antifungals

A class of antifungal drugs that inhibit the synthesis of ergosterol, a vital component of fungal cell membranes.

How do Azoles affect drug interactions?

Inhibits the CYP450 3A4 isoenzyme in the liver, leading to potential interactions with other medications metabolized by the same enzyme.

Are azoles safe during pregnancy?

They are categorized as teratogens and should be avoided during pregnancy unless the potential benefits outweigh the risks to the fetus.

Fluconazole

The least active triazole, primarily effective against yeast and some dimorphic fungi. It has a narrow spectrum of activity.

Signup and view all the flashcards

Itraconazole

A broader-spectrum triazole than fluconazole, often used for infections that require a wider antifungal coverage.

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Voriconazole

A triazole with the broadest spectrum of activity, making it a preferred choice for invasive aspergillosis. However, high doses can lead to visual and auditory hallucinations.

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Echinocandins

The newest class of antifungal agents that target the fungal cell wall, disrupting its structure and ultimately leading to cell death.

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What are some side effects of Echinocandins?

Echinocandins can cause adverse effects like fever and rash. They should be administered slowly intravenously to prevent histamine-like reactions.

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Caspofungin

The first-line option for patients with invasive candidiasis and a second-line choice for invasive aspergillosis.

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Micafungin and Anidulafungin

First-line agents for invasive candidiasis, they have an advantage of not being metabolized by CYP450 enzymes, minimizing drug interactions.

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Cutaneous Mycotic Infections

These infections are caused by mold-like fungi and commonly treated with squalene epoxidase inhibitors.

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Squalene Epoxidase Inhibitors

Inhibit the enzyme squalene epoxidase, disrupting ergosterol synthesis, leading to increased fungal membrane permeability and cell death.

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Examples of Squalene Epoxidase Inhibitors

Terbinafine, Naftifine, and Butenafine are common examples of squalene epoxidase inhibitors used for treating cutaneous mycotic infections.

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Dermatophytosis

A type of cutaneous infection primarily caused by Trichophyton, Microsporum, and Epidermophyton, all fungal species.

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Amphotericin B

A naturally occurring polyene macrolide antifungals with a broad antifungal activity, particularly effective against life-threatening fungal infections.

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How does Amphotericin B work?

Amphotericin B binds to ergosterol present in the fungal cell membrane, forming pores, disrupting its function, and ultimately causing cell death.

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What leads to Amphotericin B resistance?

Amphotericin B resistance can arise due to alterations in the ergosterol content and structure of fungal cells.

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How is Amphotericin B administered?

Due to its water insolubility, Amphotericin B is administered intravenously through a slow intravenous infusion.

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What are some side effects of Amphotericin B?

Common adverse effects of Amphotericin B include fever, chills, kidney failure, hypotension, anemia, and thrombophlebitis.

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Flucytosine

A synthetic antifungal agent that interferes with fungal DNA synthesis by mimicking cytosine.

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Is Flucytosine selective?

Flucytosine exhibits selectivity meaning it primarily targets fungal cells rather than mammalian cells, making it safe for humans.

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How is Flucytosine administered?

Flucytosine is primarily administered orally for systemic infections because it's well absorbed in the digestive tract and can easily penetrate the brain through the cerebrospinal fluid.

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Is Flucytosine used alone?

Flucytosine is often used in combination with other antifungal agents, like Amphotericin B, to enhance therapeutic efficacy.

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What are some side effects of Flucytosine?

Despite its selective toxicity, Flucytosine can cause adverse effects such as bone marrow toxicity, nausea, vomiting, diarrhea, and potentially reversible liver damage.

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How do Azoles work?

They work by inhibiting the enzyme 14α-demethylase, which is essential for ergosterol biosynthesis, leading to disrupted fungal cell membrane structure.

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Azoles: What are their limitations?

The spectrum of antifungal activity varies across different azoles. Some azoles are effective against yeast infections, while others are broader spectrum, targeting a wider range of fungi.

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Study Notes

Antifungal Drugs: Pharmacological Overview

  • Azole antifungals inhibit hepatic CYP450 3A4 isoenzyme, leading to drug interactions with medications metabolized by the same enzyme
  • Azoles are teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to the fetus
  • Fluconazole is the least active triazole with a spectrum limited to yeast and some dimorphic fungi
  • Itraconazole has a broader spectrum than fluconazole and is the drug of choice for certain fungal infections
  • Voriconazole, with a broad spectrum of activity, is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses
  • Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species
  • Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions
  • Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis
  • Micafungin and anidulafungin are first-line options for the treatment of invasive candidiasis and are not substrates for CYP450 enzymes, thus having no drug-drug interactions
  • Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine
  • Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death
  • The majority of dermatophytosis, a type of cutaneous infection, is caused by Trichophyton, Microsporum, and Epidermophyton fungi

Antifungal Drugs: Pharmacological Overview

  • Azole antifungals inhibit hepatic CYP450 3A4 isoenzyme, leading to drug interactions with medications metabolized by the same enzyme
  • Azoles are teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to the fetus
  • Fluconazole is the least active triazole with a spectrum limited to yeast and some dimorphic fungi
  • Itraconazole has a broader spectrum than fluconazole and is the drug of choice for certain fungal infections
  • Voriconazole, with a broad spectrum of activity, is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses
  • Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species
  • Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions
  • Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis
  • Micafungin and anidulafungin are first-line options for the treatment of invasive candidiasis and are not substrates for CYP450 enzymes, thus having no drug-drug interactions
  • Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine
  • Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death
  • The majority of dermatophytosis, a type of cutaneous infection, is caused by Trichophyton, Microsporum, and Epidermophyton fungi

Antifungal Drugs Overview

  • Amphotericin B is a naturally occurring polyene macrolide and the drug of choice for life-threatening mycoses.
  • Its mechanism of action involves binding to ergosterol, forming pores, disrupting membrane function, and causing cell death.
  • Amphotericin B resistance is related to ergosterol content and structure.
  • The drug is water insoluble and is administered parenterally through slow IV infusion.
  • Adverse effects of Amphotericin B include fever, chills, kidney failure, hypotension, anemia, and thrombophlebitis.
  • Flucytosine (5-FC) is a synthetic pyrimidine with selective toxicity and is used in combination with other antifungal agents.
  • It is well-absorbed orally, distributes throughout the body water, and penetrates the CSF.
  • Azole antifungals, including imidazoles and triazoles, share a similar mechanism of action, but differ in PK properties and therapeutic use.
  • Their mechanism of action involves reducing ergosterol synthesis and inhibiting 14 α-demethylase, leading to disrupted fungal membrane function and structure.
  • Triazoles are administered systemically for the treatment or prophylaxis of cutaneous and systemic mycoses.
  • Antifungal spectrum of Flucytosine is restricted and it is not used alone due to a high susceptibility of resistance.
  • Adverse effects of Flucytosine include bone marrow toxicity, nausea, vomiting, diarrhea, and reversible hepatic dysfunction.

Antifungal Drugs: Pharmacological Overview

  • Azole antifungals inhibit hepatic CYP450 3A4 isoenzyme, leading to drug interactions with medications metabolized by the same enzyme
  • Azoles are teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to the fetus
  • Fluconazole is the least active triazole with a spectrum limited to yeast and some dimorphic fungi
  • Itraconazole has a broader spectrum than fluconazole and is the drug of choice for certain fungal infections
  • Voriconazole, with a broad spectrum of activity, is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses
  • Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species
  • Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions
  • Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis
  • Micafungin and anidulafungin are first-line options for the treatment of invasive candidiasis and are not substrates for CYP450 enzymes, thus having no drug-drug interactions
  • Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine
  • Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death
  • The majority of dermatophytosis, a type of cutaneous infection, is caused by Trichophyton, Microsporum, and Epidermophyton fungi

Antifungal Drugs: Pharmacological Overview

  • Azole antifungals inhibit hepatic CYP450 3A4 isoenzyme, leading to drug interactions with medications metabolized by the same enzyme
  • Azoles are teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to the fetus
  • Fluconazole is the least active triazole with a spectrum limited to yeast and some dimorphic fungi
  • Itraconazole has a broader spectrum than fluconazole and is the drug of choice for certain fungal infections
  • Voriconazole, with a broad spectrum of activity, is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses
  • Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species
  • Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions
  • Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis
  • Micafungin and anidulafungin are first-line options for the treatment of invasive candidiasis and are not substrates for CYP450 enzymes, thus having no drug-drug interactions
  • Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine
  • Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death
  • The majority of dermatophytosis, a type of cutaneous infection, is caused by Trichophyton, Microsporum, and Epidermophyton fungi

Antifungal Drugs: Pharmacological Overview

  • Azole antifungals inhibit hepatic CYP450 3A4 isoenzyme, leading to drug interactions with medications metabolized by the same enzyme
  • Azoles are teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to the fetus
  • Fluconazole is the least active triazole with a spectrum limited to yeast and some dimorphic fungi
  • Itraconazole has a broader spectrum than fluconazole and is the drug of choice for certain fungal infections
  • Voriconazole, with a broad spectrum of activity, is the drug of choice for invasive aspergillosis but can cause visual and auditory hallucinations at high doses
  • Echinocandins, the newest class of antifungal agents, act on the cell wall and have potent activity against Aspergillus and most Candida species
  • Echinocandins may cause adverse effects such as fever, rash, and should be administered via a slow IV infusion to prevent histamine-like reactions
  • Caspofungin is the first-line option for patients with invasive candidiasis and second-line option for invasive aspergillosis
  • Micafungin and anidulafungin are first-line options for the treatment of invasive candidiasis and are not substrates for CYP450 enzymes, thus having no drug-drug interactions
  • Cutaneous mycotic infections, caused by mold-like fungi, are commonly treated with squalene epoxidase inhibitors such as terbinafine, naftifine, and butenafine
  • Squalene epoxidase inhibitors block the synthesis of ergosterol, leading to increased membrane permeability and cell death
  • The majority of dermatophytosis, a type of cutaneous infection, is caused by Trichophyton, Microsporum, and Epidermophyton fungi

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Antifungal Drugs PDF

Description

Test your knowledge of antifungal drugs with this pharmacological overview quiz. Learn about the spectrum of activity, drug interactions, and adverse effects of azole antifungals, echinocandins, and squalene epoxidase inhibitors. Explore the use of specific antifungal agents for different fungal infections and their impact during pregnancy.

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