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Questions and Answers
What type of interferon is Interferon-ω (omega) closely related to?
What type of interferon is Interferon-ω (omega) closely related to?
What is the mechanism of action of Interferon-ω (omega)?
What is the mechanism of action of Interferon-ω (omega)?
What is Oseltamivir phosphate converted to by hepatic esterases?
What is Oseltamivir phosphate converted to by hepatic esterases?
What is the mechanism of action of Oseltamivir?
What is the mechanism of action of Oseltamivir?
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What is the effect of Zidovudine (AZT) on viral DNA synthesis?
What is the effect of Zidovudine (AZT) on viral DNA synthesis?
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What is the bioavailability of Zidovudine (AZT) in cats?
What is the bioavailability of Zidovudine (AZT) in cats?
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What is the half-life of Zidovudine (AZT) in cats?
What is the half-life of Zidovudine (AZT) in cats?
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What is a potential adverse effect of Zidovudine (AZT)?
What is a potential adverse effect of Zidovudine (AZT)?
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What is the drug interaction between Zidovudine (AZT) and Doxorubicin?
What is the drug interaction between Zidovudine (AZT) and Doxorubicin?
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What is the mechanism of action of Trifluorothymidine (TFT)?
What is the mechanism of action of Trifluorothymidine (TFT)?
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What is the mechanism of action of acyclovir?
What is the mechanism of action of acyclovir?
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What is the primary use of amantadine in veterinary medicine?
What is the primary use of amantadine in veterinary medicine?
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What is the contraindication for amantadine in patients with?
What is the contraindication for amantadine in patients with?
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What is the mechanism of action of famciclovir?
What is the mechanism of action of famciclovir?
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What is the adverse effect of acyclovir in cats?
What is the adverse effect of acyclovir in cats?
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What is the mechanism of action of interferons?
What is the mechanism of action of interferons?
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What is the use of interferon alfa-2a in veterinary medicine?
What is the use of interferon alfa-2a in veterinary medicine?
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What is the adverse effect of interferon alfa-2a in cats?
What is the adverse effect of interferon alfa-2a in cats?
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What is the pharmacokinetic characteristic of amantadine?
What is the pharmacokinetic characteristic of amantadine?
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What is the contraindication for famciclovir?
What is the contraindication for famciclovir?
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What is the therapeutic use of acyclovir in veterinary medicine?
What is the therapeutic use of acyclovir in veterinary medicine?
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What is a contraindication for the use of amantadine?
What is a contraindication for the use of amantadine?
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What is the pharmacokinetic characteristic of amantadine in horses?
What is the pharmacokinetic characteristic of amantadine in horses?
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What is the mechanism of action of famciclovir?
What is the mechanism of action of famciclovir?
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What is the therapeutic use of interferon alfa-2a in veterinary medicine?
What is the therapeutic use of interferon alfa-2a in veterinary medicine?
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What is a contraindication for the use of famciclovir?
What is a contraindication for the use of famciclovir?
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What is the pharmacokinetic characteristic of acyclovir?
What is the pharmacokinetic characteristic of acyclovir?
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What is the mechanism of action of amantadine?
What is the mechanism of action of amantadine?
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What is the adverse effect of amantadine in dogs?
What is the adverse effect of amantadine in dogs?
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What is the therapeutic use of amantadine in veterinary medicine?
What is the therapeutic use of amantadine in veterinary medicine?
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What is the therapeutic use of Interferon-ω (omega) in cats?
What is the therapeutic use of Interferon-ω (omega) in cats?
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What is the contraindication for Oseltamivir phosphate in veterinary medicine?
What is the contraindication for Oseltamivir phosphate in veterinary medicine?
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What is the mechanism of action of Zidovudine (AZT)?
What is the mechanism of action of Zidovudine (AZT)?
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What is the pharmacokinetic characteristic of Zidovudine (AZT) in cats?
What is the pharmacokinetic characteristic of Zidovudine (AZT) in cats?
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What is the therapeutic use of Oseltamivir phosphate in veterinary medicine?
What is the therapeutic use of Oseltamivir phosphate in veterinary medicine?
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What is the potential adverse effect of Zidovudine (AZT) in cats?
What is the potential adverse effect of Zidovudine (AZT) in cats?
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What is the mechanism of action of Trifluorothymidine (TFT)?
What is the mechanism of action of Trifluorothymidine (TFT)?
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What is the potential drug interaction between Zidovudine (AZT) and Interferon alfa?
What is the potential drug interaction between Zidovudine (AZT) and Interferon alfa?
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What is the contraindication for Zidovudine (AZT) in cats?
What is the contraindication for Zidovudine (AZT) in cats?
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What is the pharmacokinetic characteristic of Oseltamivir phosphate?
What is the pharmacokinetic characteristic of Oseltamivir phosphate?
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What is the primary therapeutic use of Interferon-ω (omega) in cats?
What is the primary therapeutic use of Interferon-ω (omega) in cats?
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What is a common adverse effect of Zidovudine (AZT) in cats?
What is a common adverse effect of Zidovudine (AZT) in cats?
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What is a contraindication for the use of Oseltamivir phosphate in veterinary medicine?
What is a contraindication for the use of Oseltamivir phosphate in veterinary medicine?
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What is the mechanism of action of Oseltamivir phosphate?
What is the mechanism of action of Oseltamivir phosphate?
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What is the pharmacokinetic characteristic of Zidovudine (AZT) in cats?
What is the pharmacokinetic characteristic of Zidovudine (AZT) in cats?
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What is the therapeutic use of Trifluorothymidine (TFT) in veterinary medicine?
What is the therapeutic use of Trifluorothymidine (TFT) in veterinary medicine?
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What is a potential adverse effect of Interferon-ω (omega) in cats?
What is a potential adverse effect of Interferon-ω (omega) in cats?
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What is the mechanism of action of Zidovudine (AZT) in cats?
What is the mechanism of action of Zidovudine (AZT) in cats?
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What is a contraindication for the use of Zidovudine (AZT) in cats?
What is a contraindication for the use of Zidovudine (AZT) in cats?
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What is the pharmacokinetic characteristic of Oseltamivir phosphate?
What is the pharmacokinetic characteristic of Oseltamivir phosphate?
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What is the primary therapeutic use of amantadine in veterinary medicine?
What is the primary therapeutic use of amantadine in veterinary medicine?
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What is a potential adverse effect of acyclovir in cats?
What is a potential adverse effect of acyclovir in cats?
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What is a contraindication for the use of amantadine in veterinary medicine?
What is a contraindication for the use of amantadine in veterinary medicine?
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What is the mechanism of action of famciclovir?
What is the mechanism of action of famciclovir?
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What is the pharmacokinetic characteristic of acyclovir?
What is the pharmacokinetic characteristic of acyclovir?
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What is a potential adverse effect of interferon alfa-2a in cats?
What is a potential adverse effect of interferon alfa-2a in cats?
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What is the therapeutic use of famciclovir in veterinary medicine?
What is the therapeutic use of famciclovir in veterinary medicine?
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What is a contraindication for the use of famciclovir in veterinary medicine?
What is a contraindication for the use of famciclovir in veterinary medicine?
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What is the pharmacokinetic characteristic of amantadine in horses?
What is the pharmacokinetic characteristic of amantadine in horses?
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What is the mechanism of action of acyclovir?
What is the mechanism of action of acyclovir?
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What is the primary mechanism of action of Amphotericin B?
What is the primary mechanism of action of Amphotericin B?
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What is the primary indication for the use of Itraconazole?
What is the primary indication for the use of Itraconazole?
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What is a common adverse effect of Amphotericin B?
What is a common adverse effect of Amphotericin B?
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What is the primary mechanism of action of Polyene macrolides?
What is the primary mechanism of action of Polyene macrolides?
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What is the primary indication for the use of Nystatin?
What is the primary indication for the use of Nystatin?
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What is a common use of Natamycin?
What is a common use of Natamycin?
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What is the primary mechanism of action of Fluconazole?
What is the primary mechanism of action of Fluconazole?
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What is a common adverse effect of Itraconazole?
What is a common adverse effect of Itraconazole?
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What is the primary indication for the use of Amphotericin B?
What is the primary indication for the use of Amphotericin B?
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What is the primary mechanism of action of Polyene macrolides?
What is the primary mechanism of action of Polyene macrolides?
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What is the primary difference between ketoconazole and fluconazole?
What is the primary difference between ketoconazole and fluconazole?
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What is the mechanism of action of fluconazole?
What is the mechanism of action of fluconazole?
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What is a common adverse effect of ketoconazole?
What is a common adverse effect of ketoconazole?
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What is the primary therapeutic use of miconazole?
What is the primary therapeutic use of miconazole?
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What is a contraindication for the use of fluconazole?
What is a contraindication for the use of fluconazole?
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What is the difference in the metabolism of ketoconazole and fluconazole?
What is the difference in the metabolism of ketoconazole and fluconazole?
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What is the primary therapeutic use of ketoconazole?
What is the primary therapeutic use of ketoconazole?
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What is the primary advantage of fluconazole over ketoconazole?
What is the primary advantage of fluconazole over ketoconazole?
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What is the primary therapeutic use of miconazole in horses?
What is the primary therapeutic use of miconazole in horses?
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What is the effect of ketoconazole on adrenal or gonadal steroids?
What is the effect of ketoconazole on adrenal or gonadal steroids?
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What is the mechanism of action of Flucytosine?
What is the mechanism of action of Flucytosine?
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What is the therapeutic use of Flucytosine in dogs and cats?
What is the therapeutic use of Flucytosine in dogs and cats?
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What is the adverse effect of Flucytosine?
What is the adverse effect of Flucytosine?
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What is the mechanism of action of Terbinafine?
What is the mechanism of action of Terbinafine?
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What is the therapeutic use of Terbinafine?
What is the therapeutic use of Terbinafine?
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What is the pharmacokinetic characteristic of Flucytosine?
What is the pharmacokinetic characteristic of Flucytosine?
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What is the therapeutic use of Flucytosine in birds?
What is the therapeutic use of Flucytosine in birds?
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What is the mechanism of action of other antifungals?
What is the mechanism of action of other antifungals?
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What is the therapeutic use of Terbinafine in birds?
What is the therapeutic use of Terbinafine in birds?
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What is the pharmacokinetic characteristic of Terbinafine?
What is the pharmacokinetic characteristic of Terbinafine?
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What is the mechanism of action of Griseofulvin?
What is the mechanism of action of Griseofulvin?
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Which of the following is a characteristic of Griseofulvin?
Which of the following is a characteristic of Griseofulvin?
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What is the effect of Griseofulvin on infected cells?
What is the effect of Griseofulvin on infected cells?
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Which of the following is a type of Azole antifungal drug?
Which of the following is a type of Azole antifungal drug?
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What is the mechanism of action of Azole antifungal drugs?
What is the mechanism of action of Azole antifungal drugs?
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What is the effect of Ketoconazole on mammalian steroid synthesis?
What is the effect of Ketoconazole on mammalian steroid synthesis?
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What is the mechanism of action of Ketoconazole?
What is the mechanism of action of Ketoconazole?
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Which of the following is a characteristic of Ketoconazole?
Which of the following is a characteristic of Ketoconazole?
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What is the use of Ketoconazole?
What is the use of Ketoconazole?
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What is a potential adverse effect of Ketoconazole?
What is a potential adverse effect of Ketoconazole?
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What is the mechanism of action of Flucytosine?
What is the mechanism of action of Flucytosine?
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What is the therapeutic use of Flucytosine in dogs and cats?
What is the therapeutic use of Flucytosine in dogs and cats?
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What is the adverse effect of Flucytosine?
What is the adverse effect of Flucytosine?
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What is the mechanism of action of Terbinafine?
What is the mechanism of action of Terbinafine?
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What is the pharmacokinetic characteristic of Terbinafine?
What is the pharmacokinetic characteristic of Terbinafine?
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What is the therapeutic use of Terbinafine in animals?
What is the therapeutic use of Terbinafine in animals?
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What is the therapeutic use of Flucytosine in psittacine birds?
What is the therapeutic use of Flucytosine in psittacine birds?
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What is the mechanism of action of amphotericin B?
What is the mechanism of action of amphotericin B?
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What is the therapeutic use of Flucytosine in combination with amphotericin B?
What is the therapeutic use of Flucytosine in combination with amphotericin B?
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What is the therapeutic use of Terbinafine in birds?
What is the therapeutic use of Terbinafine in birds?
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Which of the following antifungal drugs is water soluble?
Which of the following antifungal drugs is water soluble?
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What is the primary indication for Ketoconazole?
What is the primary indication for Ketoconazole?
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Which of the following antifungal drugs is contraindicated in patients with hepatic diseases?
Which of the following antifungal drugs is contraindicated in patients with hepatic diseases?
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What is the mechanism of action of Fluconazole?
What is the mechanism of action of Fluconazole?
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Which of the following antifungal drugs is used to treat fungal keratitis in horses?
Which of the following antifungal drugs is used to treat fungal keratitis in horses?
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What is the route of excretion for Ketoconazole?
What is the route of excretion for Ketoconazole?
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Which of the following antifungal drugs is effective against Microsporum canis?
Which of the following antifungal drugs is effective against Microsporum canis?
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What is a common adverse effect of Ketoconazole?
What is a common adverse effect of Ketoconazole?
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Which of the following antifungal drugs is used to treat systemic mycoses?
Which of the following antifungal drugs is used to treat systemic mycoses?
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What is a contraindication for the use of Fluconazole?
What is a contraindication for the use of Fluconazole?
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What is the mechanism of action of Amphotericin B?
What is the mechanism of action of Amphotericin B?
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What is the main use of Nystatin?
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What is the adverse effect of Amphotericin B?
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What is the fungicidal or fungistatic activity of Flucytosine?
What is the fungicidal or fungistatic activity of Flucytosine?
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What is the indication for Natamycin?
What is the indication for Natamycin?
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What is the pharmacokinetic characteristic of Amphotericin B?
What is the pharmacokinetic characteristic of Amphotericin B?
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What is the combination therapy with Amphotericin B?
What is the combination therapy with Amphotericin B?
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What is the mechanism of action of Flucytosine?
What is the mechanism of action of Flucytosine?
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What is the indication for Nystatin?
What is the indication for Nystatin?
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What is the adverse effect of Flucytosine?
What is the adverse effect of Flucytosine?
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Which type of microorganisms is fungi classified as?
Which type of microorganisms is fungi classified as?
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What is the mechanism of action of Griseofulvin?
What is the mechanism of action of Griseofulvin?
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What is the effect of Griseofulvin on infected cells?
What is the effect of Griseofulvin on infected cells?
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How is Griseofulvin administered?
How is Griseofulvin administered?
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What is a rare adverse effect of Griseofulvin in kittens?
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What is the mechanism of action of Azoles?
What is the mechanism of action of Azoles?
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Which of the following is a characteristic of Ketoconazole?
Which of the following is a characteristic of Ketoconazole?
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What is the mechanism of action of Ketoconazole?
What is the mechanism of action of Ketoconazole?
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What is the pharmacokinetic characteristic of Ketoconazole?
What is the pharmacokinetic characteristic of Ketoconazole?
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What is the effect of high doses of Azoles on mammalian systems?
What is the effect of high doses of Azoles on mammalian systems?
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What is the mechanism of action of Griseofulvin?
What is the mechanism of action of Griseofulvin?
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What type of fungi is Griseofulvin effective against?
What type of fungi is Griseofulvin effective against?
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What is the absorption of Griseofulvin affected by?
What is the absorption of Griseofulvin affected by?
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What is the mechanism of action of Azoles?
What is the mechanism of action of Azoles?
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What is the effect of high doses of Azoles?
What is the effect of high doses of Azoles?
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What is the mechanism of action of Ketoconazole?
What is the mechanism of action of Ketoconazole?
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What is the administration route of Ketoconazole?
What is the administration route of Ketoconazole?
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What is the distribution of Griseofulvin?
What is the distribution of Griseofulvin?
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What is the metabolism of Griseofulvin?
What is the metabolism of Griseofulvin?
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What is the excretion route of Griseofulvin?
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What is the unique property of fluconazole?
What is the unique property of fluconazole?
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What is ketoconazole used to treat in dogs and cats?
What is ketoconazole used to treat in dogs and cats?
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What is the effect of fluconazole on fungal cells?
What is the effect of fluconazole on fungal cells?
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What is miconazole effective against?
What is miconazole effective against?
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What is a contraindication for fluconazole?
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What is a common adverse effect of ketoconazole?
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How is fluconazole excreted?
How is fluconazole excreted?
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What is miconazole used for in horses?
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What is ketoconazole metabolized in?
What is ketoconazole metabolized in?
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What can happen to patients with impaired renal function taking ketoconazole?
What can happen to patients with impaired renal function taking ketoconazole?
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What is the primary mechanism of action of Flucytosine?
What is the primary mechanism of action of Flucytosine?
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What is the therapeutic use of Flucytosine in psittacine birds?
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What is the characteristic of Flucytosine in terms of toxicity?
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What is the mechanism of action of Terbinafine?
What is the mechanism of action of Terbinafine?
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What is the therapeutic use of Terbinafine in dogs and cats?
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What is the characteristic of Terbinafine in terms of its effect on dermatophytes?
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What is the route of administration for Terbinafine?
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What is the pharmacokinetic characteristic of Terbinafine?
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What is the therapeutic use of Flucytosine in combination with amphotericin B?
What is the therapeutic use of Flucytosine in combination with amphotericin B?
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What is the effect of Flucytosine on the synthesis of DNA and RNA in susceptible fungi?
What is the effect of Flucytosine on the synthesis of DNA and RNA in susceptible fungi?
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What is the mechanism of action of Amphotericin B?
What is the mechanism of action of Amphotericin B?
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What is the primary use of Nystatin?
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What is the unique characteristic of Natamycin?
What is the unique characteristic of Natamycin?
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What is the mechanism of action of Flucytosine?
What is the mechanism of action of Flucytosine?
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What is the common adverse effect of Amphotericin B?
What is the common adverse effect of Amphotericin B?
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What is the primary advantage of Itraconazole over Ketoconazole?
What is the primary advantage of Itraconazole over Ketoconazole?
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What is the unique characteristic of Polyene macrolides?
What is the unique characteristic of Polyene macrolides?
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What is the primary indication for using Flucytosine in combination with Amphotericin B?
What is the primary indication for using Flucytosine in combination with Amphotericin B?
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What is the unique characteristic of Nystatin?
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What is the primary advantage of using Amphotericin B in combination with other antifungals?
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Study Notes
Antiviral Drugs
Acyclovir
- Guanosine derivative, selective for herpesviruses
- Metabolized to monophosphate via thymidine kinase, then converted to triphosphate, which inhibits viral DNA polymerase
- Widely distributed throughout body tissues and fluids, including the brain, semen, and CSF
- Excreted by kidneys through glomerular filtration and tubular secretion
- Used to treat ocular and respiratory infections of herpes virus 1 in cats, and active against equine herpes virus type-1 in vitro
- Adverse effects: low WBC, leukopenia, anemia in cats, and necrosis at injection site in birds
Amantadine
- 1-aminoadamantane, binds to M2 protein and blocks its ion channel activity, inhibiting viral uncoating and replication
- N-methyl-D-aspartate (NMDA) receptor antagonist, important in pain sensation
- Used to treat influenza viruses, replicate within host cells, and M2 protein
- Therapeutic use: adjunct treatment to chronic pain in dogs and cats, and treatment of equine-2 influenza via IV
- Pharmacokinetics: variable absorption, bioavailability 40-60%, excretion renal, half-life ~3.5 hours
- Adverse effects: agitation, loose stools, flatulence, diarrhea, contraindications: hypersensitivity, untreated angle-closure glaucoma, liver and renal diseases, CHF, active psychoses, eczematoid dermatitis, seizure disorders
- Drug interactions: anticholinergics, CNS stimulants, urinary acidifiers, TMPS
Famciclovir
- Converted to penciclovir, which is phosphorylated to penciclovir monophosphate, then triphosphate, inhibiting herpes virus DNA polymerase
- Used to treat feline herpes (FHV-1), and active against varicella zoster virus
- Pharmacokinetics: cats require higher doses due to poor conversion to penciclovir
- Contraindications: hypersensitivity, patients with renal problems
- Adverse effects: not well documented, but well tolerated when used up to three weeks
Interferons
- Human recombinant IFN-α, feline recombinant IFN-ω
- MOA: released by host cells in response to viral infection, attached to receptors on adjacent cells, increasing transcription of host cell DNA and activating endonuclease, increasing cell resistance to virus infection
- Used to treat non-neoplastic Feline Leukemia (FeLV) disease, and oral administration for ocular herpes infection
- Effects: antiviral, antiproliferative, immunomodulating, well distributed throughout the body except in CNS
- Adverse effects: dose-related, malaise, fever, allergic reactions, myelotoxicity, myalgia, hyperthermia, vomiting, decrease RBCs, platelets, WBCs, increase ALT, soft feces, mild diarrhea, transient fatigue, anorexia, and weight loss
Oseltamivir phosphate
- Ester prodrug converted to its active metabolite, oseltamivir carboxylate, by hepatic esterases
- Competitive inhibitor of the enzyme neuraminidase, used by influenza viruses for budding of replicative viral particles from infected cells
- May be effective for parvovirus infections in dogs, and mixed bacterial/viral infections
- Public health issues: prohibited by the FDA for extralabel drug use in poultry due to fear of resistance that avian influenza virus would develop against oseltamivir
Zidovudine (AZT)
- Analog of thymidine, phosphorylated by host cell enzymes to AZT 5-triphosphate, which competes with host 5-thymidine, essential for proviral DNA formation by reverse transcriptase of the virus
- Antiretroviral agent, virustatic effect, converted to active metabolite- triphosphate, inhibiting viral RNA-directed DNA polymerase
- Used to treat FIV, and as adjunct treatment for FeLV
- Pharmacokinetics: well absorbed orally, 90% bioavailability in cats, widely distributed including the CSF, metabolized in liver by glucuronide conjugation, excreted in urine, t ½ = 1.5 hours
- Adverse effects: anemia, reduction in hemoglobin, diarrhea, weakness, bone marrow, renal or hepatic dysfunction
- Drug interactions: antifungals, azole, atovaquone, doxorubicin, interferon alfa, probenecid, rifampin, myelo-/cytotoxic drugs
Other Antiviral Agents
- Trifluorothymidine (TFT): thought to have higher affinity for viral DNA than mammalian, and is more potent
- Idoxuridine: thymidine analogs active against DNA viruses, herpesvirus, and poxvirus
Interferon-ω (Omega) / Cat Omega Interferon
- Produced by genetic engineering, type 1 interferon closely related to alpha interferon
- Half-life: 1-2 hours in dogs and cats
- Mechanism of action: Acts on virus-infected cells by inhibiting mRNA synthesis and translation proteins, leading to inhibition of viral replication
- Used to treat cat viral infections, including calici virus, FeLV, FIV, and others, as well as canine parvovirus
- Adverse effects: Hyperthermia, vomiting, decrease in RBCs, platelets, and WBCs (myelotoxicity), increase in ALT, soft feces/mild diarrhea, transient fatigue, anorexia, and weight loss
Oseltamivir Phosphate
- Ester prodrug converted to active metabolite, oseltamivir carboxylate by hepatic esterases
- Mechanism of action: Competitive inhibitor of the enzyme neuraminidase, which influenza viruses use for budding and release of viral particles
- May be effective for parvovirus infections in dogs and other mixed bacterial/viral infections
- Public health controversy: use in veterinary medicine may lead to resistance in avian influenza virus
Zidovudine (AZT)
- Analog of thymidine, phosphorylated by host cell enzymes to AZT 5-triphosphate, which competes with host 5-thymidine for proviral DNA formation by reverse transcriptase
- Antiretroviral agent with virustatic effect, inhibiting viral RNA-directed DNA polymerase
- Used to treat FIV, with clinical improvement seen 14 days after treatment
- Pharmacokinetics: Well absorbed orally, widely distributed, metabolized in liver, and excreted in urine, with a half-life of 1.5 hours
- Adverse effects: Non-regenerative anemia, diarrhea, and weakness
Other Antiviral Agents
- Trifluorothymidine (TFT): Thought to have higher affinity for viral DNA than mammalian DNA, making it more potent
- Idoxuridine: Thymidine analog active against DNA viruses, including herpesvirus and poxvirus
Acyclovir
- Guanosine derivative selective for herpesviruses
- Metabolized to monophosphate via thymidine kinase, then converted to triphosphate, which inhibits viral DNA polymerase
- Used to treat ocular and respiratory infections of herpes virus 1 in cats
- Adverse effects: Low WBC, leukopenia, and anemia in cats; necrosis at injection site in birds
Amantadine
- 1-aminoadamantane, binds to M2 protein, and blocks its ion channel activity, inhibiting viral uncoating and replication
- Used as an adjunct treatment for chronic pain in dogs and cats, and for equine-2 influenza via IV
- Pharmacokinetics: Not described in dogs and cats, but has variable absorption and bioavailability of 40-60% in horses
- Adverse effects: Agitation, loose stools, flatulence, and diarrhea
Famciclovir
- For feline herpes (FHV-1), converted into penciclovir, which inhibits herpes virus DNA polymerase
- Pharmacokinetics: Cats require higher doses due to poor conversion to penciclovir
- Contraindication: Hypersensitivity
- Adverse effects: Not well documented, but well-tolerated when used up to three weeks
Interferon-ω (Omega) / Cat Omega Interferon
- Produced by genetic engineering, type 1 interferon closely related to alpha interferon
- Half-life: 1-2 hours in dogs and cats
- Mechanism of action: Acts on virus-infected cells by inhibiting mRNA synthesis and translation proteins, leading to inhibition of viral replication
- Used to treat cat viral infections, including calici virus, FeLV, FIV, and others, as well as canine parvovirus
- Adverse effects: Hyperthermia, vomiting, decrease in RBCs, platelets, and WBCs (myelotoxicity), increase in ALT, soft feces/mild diarrhea, transient fatigue, anorexia, and weight loss
Oseltamivir Phosphate
- Ester prodrug converted to active metabolite, oseltamivir carboxylate by hepatic esterases
- Mechanism of action: Competitive inhibitor of the enzyme neuraminidase, which influenza viruses use for budding and release of viral particles
- May be effective for parvovirus infections in dogs and other mixed bacterial/viral infections
- Public health controversy: use in veterinary medicine may lead to resistance in avian influenza virus
Zidovudine (AZT)
- Analog of thymidine, phosphorylated by host cell enzymes to AZT 5-triphosphate, which competes with host 5-thymidine for proviral DNA formation by reverse transcriptase
- Antiretroviral agent with virustatic effect, inhibiting viral RNA-directed DNA polymerase
- Used to treat FIV, with clinical improvement seen 14 days after treatment
- Pharmacokinetics: Well absorbed orally, widely distributed, metabolized in liver, and excreted in urine, with a half-life of 1.5 hours
- Adverse effects: Non-regenerative anemia, diarrhea, and weakness
Other Antiviral Agents
- Trifluorothymidine (TFT): Thought to have higher affinity for viral DNA than mammalian DNA, making it more potent
- Idoxuridine: Thymidine analog active against DNA viruses, including herpesvirus and poxvirus
Acyclovir
- Guanosine derivative selective for herpesviruses
- Metabolized to monophosphate via thymidine kinase, then converted to triphosphate, which inhibits viral DNA polymerase
- Used to treat ocular and respiratory infections of herpes virus 1 in cats
- Adverse effects: Low WBC, leukopenia, and anemia in cats; necrosis at injection site in birds
Amantadine
- 1-aminoadamantane, binds to M2 protein, and blocks its ion channel activity, inhibiting viral uncoating and replication
- Used as an adjunct treatment for chronic pain in dogs and cats, and for equine-2 influenza via IV
- Pharmacokinetics: Not described in dogs and cats, but has variable absorption and bioavailability of 40-60% in horses
- Adverse effects: Agitation, loose stools, flatulence, and diarrhea
Famciclovir
- For feline herpes (FHV-1), converted into penciclovir, which inhibits herpes virus DNA polymerase
- Pharmacokinetics: Cats require higher doses due to poor conversion to penciclovir
- Contraindication: Hypersensitivity
- Adverse effects: Not well documented, but well-tolerated when used up to three weeks
Antifungal Drugs
- Antifungal drugs are used to treat fungal infections in animals.
- Fungi can be unicellular or multicellular, and are classified into molds, mushrooms, and yeasts.
Azoles
- Azoles are a group of antifungal drugs that include imidazoles and triazoles.
- Azoles have antibacterial, antifungal, antiprotozoal, and anthelmintic activity.
- Azoles are poorly water-soluble, except for fluconazole.
- Azoles can be divided into imidazoles (e.g., clotrimazole, miconazole, econazole) and triazoles (e.g., ketoconazole, itraconazole, fluconazole).
Ketoconazole
- Ketoconazole is an imidazole antifungal drug used for systemic fungal infections.
- Mechanism of action: inhibits synthesis of ergosterol in fungal cytoplasmic membranes by blocking cytochrome P-450 enzymes.
- Pharmacokinetics: well-absorbed orally, widely distributed, and metabolized in the liver.
Itraconazole
- Itraconazole is a triazole antifungal drug used for systemic fungal infections.
- Mechanism of action: inhibits synthesis of ergesterol in fungal cytoplasmic membranes.
- Indications: systemic mycoses, including aspergillosis, blastomycosis, and histoplasmosis.
- Adverse effects: fewer side effects than ketoconazole, but can cause hepatic toxicity, anorexia, weight loss, and vomiting.
Fluconazole
- Fluconazole is a triazole antifungal drug used for systemic fungal infections.
- Mechanism of action: inhibits synthesis of ergosterol in fungal cytoplasmic membranes.
- Indications: systemic mycoses, including cryptococcal meningitis, blastomycosis, and histoplasmosis.
- Pharmacokinetics: well-absorbed orally, widely distributed, and excreted in the urine.
Miconazole
- Miconazole is an imidazole antifungal drug used topically or orally for fungal infections.
- Indications: fungal keratitis in horses, canine and feline dermatophytoses.
Polyene Macrolides
- Polyene macrolides are a group of antifungal drugs that include amphotericin B, nystatin, and natamycin.
- Mechanism of action: binds to ergosterol in fungal membranes, forming pores and causing leakage of cellular contents.
Amphotericin B
- Amphotericin B is a polyene macrolide antifungal drug used for systemic fungal infections.
- Mechanism of action: binds to ergosterol in fungal membranes, forming pores and causing leakage of cellular contents.
- Pharmacokinetics: not absorbed orally, distributed to most tissues except CNS, eye, and bone, and excreted in the urine.
- Adverse effects: renal toxicity, renal vasoconstriction, and decreased renal glomerular filtration.
Nystatin
- Nystatin is a polyene macrolide antifungal drug used topically or orally for fungal infections.
- Indications: candidiasis, dermatophytosis, and gastrointestinal fungal infections.
Natamycin
- Natamycin is a polyene macrolide antifungal drug used topically for fungal eye infections.
- Indications: fungal keratitis in horses and humans.
Flucytosine
- Flucytosine is a fluorinated pyrimidine antifungal drug used orally for systemic fungal infections.
- Mechanism of action: inhibits synthesis of DNA and RNA in susceptible fungi.
- Indications: cryptococcosis, aspergillosis, and candidiasis.
- Pharmacokinetics: well-absorbed orally, widely distributed, and excreted in the urine.
Griseofulvin
- Griseofulvin is a benzofuran antifungal drug used orally for dermatophytic infections.
- Mechanism of action: binds to microtubules, inhibiting spindle formation and mitosis in dermatophytes.
- Pharmacokinetics: absorbed orally, distributed to keratin precursor cells, and metabolized in the liver.
Terbinafine
- Terbinafine is an allylamine derivative antifungal drug used orally or topically for fungal infections.
- Mechanism of action: inhibits synthesis of ergosterol by blocking the enzyme squalene monooxygenase.
- Indications: dermatophytic infections in dogs and cats, and aspergillosis in birds.
Other Antifungals
- Chlorhexidine, iodine, tolnaftate, benzoic acid, salicylic acid, and thiabendazole are other antifungal drugs used topically or orally for various fungal infections.
Antifungal Drugs
-
Itraconazole: Delivered by subconjunctival route, used for systemic mycoses (Aspergillosis, Cryptococcal meningitis, Blastomycosis, Histoplasmosis), no effects on hormone synthesis.
- Can cause hepatic toxicity, anorexia, weight loss, and vomiting.
Polyene Macrolides
-
Amphotericin B: Mechanism of action: binds to ergosterol of fungal membrane, forming pores or channels that result in leakage of cellular contents, fungicidal or fungistatic.
- Used for systemic mycoses in dogs, cats, horses, and birds.
- Can be combined with ketoconazole, fluconazole, or itraconazole to reduce toxicity.
- Adverse effects: renal toxicity, renal vasoconstriction, decreased renal glomerular filtration, and damage to tubular epithelium.
-
Nystatin: Fungistatic or fungicidal, used for candidiasis in small animals and birds.
- Combined with other drugs: neomycin, thiostrepton, and triamcinolone acetonide.
- Natamycin: Ophthalmic preparation approved as an antifungal for eyes, used for fungal dermatitis (Fusarium keratomycosis) in horses.
Other Antifungals
-
Flucytosine: Fluorinated pyrimidine, mechanism of action: inhibits thymidylate synthetase, inhibits DNA and RNA synthesis in susceptible fungi.
- Well absorbed orally, widely distributed, and excreted unchanged in the urine.
- Effective against Cryptococcus, Candida, and Aspergillus spp.
- Adverse side effects: low toxicity, mild gastrointestinal disturbances, and rare bone marrow depression.
-
Terbinafine: Allylamine derivative, mechanism of action: inhibits the synthesis of ergosterol by blocking the enzyme squalene monooxygenase.
- Fungicidal vs. dermatophytes, fungistatic vs. yeast.
- Can be administered orally or topically, useful for treating dermatophytic infections in dogs and cats.
Griseofulvin
-
Griseofulvin: From Penicillium griseofulvum, actively taken up by growing dermatophytes, binds to microtubules, inhibiting spindle formation and mitosis.
- Fungistatic vs. Microsporum spp. and Trichophyton spp.
- Action is slow, infected cells shed and replaced with uninfected cells.
- Absorption: high oral absorption, high-fat foods, and preparation of micronized particles.
- Pharmacokinetics: distributed to keratin precursor cells of the skin, hair shafts, and nails, metabolized in the liver, and excreted in urine.
Azoles
-
Azoles: Have antibacterial, antifungal, antiprotozoal, and anthelmintic activity, poorly water soluble except for fluconazole.
- Divided into Imidazoles and Triazoles.
- Mechanism of action: alter cell membrane permeability of susceptible yeasts and fungi, block synthesis of ergosterol, and inhibit other enzyme systems.
-
Ketoconazole: Imidazole antifungal for systemic use, mechanism of action: inhibits synthesis of ergosterol in fungal cytoplasmic membranes by blocking cytochrome P-450 enzymes.
- Fungistatic, often given orally, and topical preparations available.
-
Fluconazole: Synthetic, water soluble, fungistatic, and excreted via kidney.
- Mechanism of action: cell membrane alteration, leakage of cellular contents, and impaired uptake of purine and pyrimidine precursors.
- Indications: systemic mycoses, cryptococcal meningitis, blastomycosis, and histoplasmosis.
Antifungal Drugs
- Flucytosine:
- Inhibits thymidylate synthetase
- Inhibits DNA and RNA synthesis in susceptible fungi
- Effective against Cryptococcus, Candida, and Aspergillus
- Well absorbed orally, widely distributed, and excreted unchanged in the urine
- Therapeutic uses: combined with amphotericin B for cryptococcosis, aspergillosis, and candidiasis
- Adverse side effects: low toxicity, mild gastrointestinal disturbances, and rare bone marrow depression
Terbinafine
- Allylamine derivative
- MOA: inhibits the synthesis of ergosterol by blocking squalene monooxygenase
- Fungicidal vs dermatophytes and fungistatic vs yeast
- Can be administered orally or topically for treating dermatophytic infections and systemic mycotic infections
Other Antifungals
- Chlorhexidine
- Iodine
- Tolnaftate
- Benzoic acid
- Salicylic acid
- Thiabendazole
Griseofulvin
- MOA: binds to microtubules, inhibiting spindle formation and mitosis
- Fungistatic against Microsporum spp. and Trichophyton spp.
- Action is slow, and infected cells shed and are replaced with uninfected cells
- Pharmacokinetics: high oral absorption, distributed to keratin precursor cells, metabolized in the liver, and excreted in the urine
- Administration and use: PO in dogs, cats, and horses for multifocal dermatophyte infections
- Adverse effects: rare, idiosyncratic reaction in kittens, leukopenia, and anemia
Azoles
- Have antibacterial, antifungal, antiprotozoal, and anthelmintic activity
- Divided into Imidazoles and Triazoles
- MOA: alter cell membrane permeability, block synthesis of ergosterol, and inhibit other enzyme systems
- Fungistatic against Blastomyces, Coccidioides, Cryptococcus, and Histoplasma spp.
Ketoconazole
- Imidazole antifungal for systemic use
- MOA: inhibits synthesis of ergosterol in fungal cytoplasmic membranes by blocking cytochrome P-450 enzymes
- Fungistatic
- Often given orally or topically
Itraconazole
- For systemic mycoses: aspergillosis, cryptococcal meningitis, blastomycosis, and histoplasmosis
- No effects on hormone synthesis
- Adverse effects: hepatic toxicity, anorexia, weight loss, and vomiting
Polyene Macrolides
- From various strains of Actinomyces
- Include Amphotericin B, Nystatin, and Pimaricin (natamycin)
- Poorly soluble in water
Amphotericin B
- Polyene macrolide
- MOA: binds to ergosterol of fungal membrane, forming pores or channels, leading to leakage of cellular contents
- Fungicidal or fungistatic
- Spectrum of activity: systemic mycoses of dog, cats, horses, and birds
- Pharmacokinetics: not absorbed in the GIT, distributed to most tissues except CNS, eye, and bone, and secreted unchanged in the urine
- Adverse effects: renal toxicity, renal vasoconstriction, and decreased renal glomerular filtration
Nystatin
- Fungistatic or fungicidal
- From Streptomyces noursei
- Combined with other drugs: Neomycin, Thiostrepton, and Triamcinolone acetonide
- For candidiasis infecting the skin, mucous membranes, and intestinal tract of small animals and birds
- Adverse side effects: rare
Natamycin
- Ophthalmic preparation: approved antifungal for eyes
- Poorly water soluble
- For fungal dermatitis and Fusarium keratomycosis in horses
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This quiz covers the properties and mechanism of action of Acyclovir, an antiviral drug used to treat herpesviruses. It also covers its distribution, excretion, and therapeutic uses.