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
Itraconazole
- Disseminated or chronic pulmonary histoplasmosis
- Non-meningeal blastomycosis
- Oropharyngeal and cutaneous candidiasis
- Ringworm infections (T. capitis & T. corporis)
- Fungal nail infections (Onychomycosis)
- Invasive aspergillosis
- Sporotrichosis
Voriconazole
- Invasive aspergillosis
- Candidiasis
Fluconazole
-Candidiasis (vulvovaginal, oropharyngeal, mucocutaneous and systemic candidiasis) -Meningeal cryptococcosis
Mechanism of action of terbinafine
N
Terbinafine
Therapeutic uses
- Onychomycosis (oral)
- Tinea infections (topical)
- Candidiasis
Terbinafine adr
Headache
Hepatic enzyme elevation
GI upset
ketoconazole, miconazole, clotrimazole
- Tinea infections (tinea corporis, tinea cruris, tinea versicolor)
- Candidiasis
- Seborrheic dermatitis – ketoconazole
Terbinafine
Tinea infections
Nystatin
Candidiasis
Tolnaftate
Tinea infections, Dermatomycosis
Ciclopirox
Tinea infections, Dermatomycosis, Candidiasis, Onychomycosis
Clioquinol
Dermatophyte infections, seborrheic dermatitis, monilial and trichomonas vaginitis, pityriasis versicolor
Therapeutic uses of echinocandins
Invasive aspergillosis
* Disseminated and mucocutaneous candidiasis