Antifungal agents Flashcards
Bind to fungal cell membrane ergosterol and increase membrane permeability
Amphotericin B (AMB), Nystatin
Inhibition of ergosterol synthesis
Clotrimazole, econazole, miconazole, ketoconazole, fluconazole, itraconazole, voriconazole
Inhibition of ergosterol + lanosterol synthesis
Terbinafine
Inhibition of fungal cell wall synthesis
Echinocandins – Caspofungin,
micafungin
Inhibition of nucleic acid synthesis
5-flucytosine
Inhibition of fungal mitosis
Griseofulvin
MOA AMB
N
Adverse effects of amphotericin-B
Nephrotoxicity
* Haemolytic anaemia (hypochromic normocytic
anemia)
* Hepatic impairment
* Infusion related toxicity – hypotension, fever,
chills, tachypnea
* Intrathecal administration – seizures
AMB Therapeutic uses
Invasive aspergillosis
* Mucormycosis
* Disseminated histoplasmosis
Slow i.v. infusion
* Topical AMB: Oropharyngeal and cutaneous candidiasis
* Cryptococcal meningitis – intrathecal injection
* Reserve drug – resistant cases of Kala azar, mucocutaneous leishmaniasis (slow i.v. infusion)
Mechanism of flucytosine and amphotericin-B
AMB increases the entry of flucytosine into the cell by creating pores in the cell membrane
* Flucytosine acts inside the fungal cell by inhibiting thymidylate synthetase thereby inhibiting fungal DNA synthesis.
* Enhances the activity of flucytosine,
* of development of resistance
* decreases the dose requirement of AMB
Used in cryptococcosis and candidiasis
Therapeutic uses of Nystatin
Topical:
Oropharyngeal, corneal, conjunctival, cutaneous candidiasis
Oral:
Intestinal candidiasis and superinfection due to candida
Vaginal :vaginal candidiasis
Systemic (oral/IV) AZOLE
Fluconazole, Itraconazole, Voriconazole ,Ketoconazole
Topical AZOLE
Clotrimazole, Miconazole, Econazole, Ketoconazole
Mechanism of action AZOLE
N
Ketoconazole USES
Oropharyngeal candidiasis
Seborrheic dermatitis Dermatophytosis Candidiasis
Kala-azar
Dermal leishmaniasis Cushing’s syndrome Prostatic carcinoma