Overview Of Drugs For Treating Fungus, Yeast, And Candida Infections

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Fluconazole (Diflucan)

(a triazole )

IV, Oral Fungistatic against Candida, not fungicidal.
Well tolerated.
15%C. glabrata completely resistant to fluconazole
C. krusei is intrinsically resistant to fluconazole.
Std dose = 400mg/d; if C glabrata, dose should be 800 mg/d
Doses can be as high as 12 mg/kg — for a 150 lb. person
(70 kg)  = 840 mg/d)
For vulvovaginal candidiasis 150 mg single dose therapy
Only azole to cross blood-brain barrier to treat central nervous
system infections

Voriconazole (Vfend)

(a triazole )

IV, Oral New, structurally similar to fluconazole
Fungistatic against Candida, not fungicidal
Enhanced activity against fluconazole-resistant C. Glabrata
Dose at 200 mg/twice day

Itraconazole (Sporanox)

(a triazole )

IV, Oral (Capsules & Oral Solution) Fungistatic against Candida, not fungicidal
Highly lipophilic – poor penetration into aqueous fluids
Capsule form has unpredictable absorption
— Oral Solution preferred
Dose at 100-400 mg/d. For 400 mg/d take 200 mg/twice/day

CCWS Candida Cleanser

(lufenuron)

Topical, oral  more info

Clotrimazole

(Mycelex)

(an imidazole)

Oral Fungicidal against Candida.
Available as a troche (lozenge) for oropharyngeal Candidiasis
Dosage: 10 mg five times per day

Miconazole (Monistat)

(an imidazole)

Topical, oral gel Effective against Candida – fungicidal at
higher dosages.

Widely used topically for skin and vaginal yeast infections
Oral gel used for oral Candidiasis in some countries.
Not absorbed well orally — not generally available in this form.
No hormonal side effects.
No hepatoxicity (liver)
Frequent hypersensitivity – fever and chills, skin rash or itching

Flucytosine
(5-F)

(Ancobon)

Oral Fungistatic, not fungicidal
Transports in aqueous media. Complements lipophilic drugs.
Use in combination with another drug to avoid building
resistance.
Resistance by Candida is possible.
Dose at 25-37.5 mg/kg four times daily (100-150 mg/kg/day).

Nystatin (Mycostatin, Nilstat)

(a polyene)

Oral tablets, powder, solution Not absorbed. Useful for GI infections only.
Fungicidal
4 tabs (500,000 IU’s each) four times daily or equivalent oral
suspension (500,000 IU’s per 5 ml)

Amphotericin-B

(Fungizone)

(a polyene)

IV Fungicidal
High toxicity to liver – most toxic anti-microbial in clinical use
AmB is the most potent antifungal available.
AmB Not absorbed by GI tract — must use IV formulation for
systemic treatment

Amphotericin-B

(lipids)

(a polyene)

IV Fungicidal
Lipid formulation of AmB
Can deliver higher concentrations with lower toxicity than
Amphotericin-B

Amphotericin-B

(a polyene)

Oral solution, Capsule Fungicidal
No longer available in capsule & suspension forms in US
except from compounding pharmacies
Oral AmB absorption is negligible, not for systemic use
— for GI infections only.
AmB is the most potent antifungal available.
Safe: Oral formulation for GI infections avoids toxicity
of IV formulation.
Dosages:
Oral suspension: 100 mg (1 ml) four times daily
Capsule: 250 – 500 mg four times daily

Caspofungin (Cancidas)

IV Recently approved, esp. for life-threatening fungal infections.
Fungicidal for Candida spp.

Terbinafine (Lamisil)

Oral, Topical Mainly effective on dermatophytes (skin fungi)
Active against Candida in vitro.
Highly lipophilic – poor penetration into aqueous fluids
Has been combined with fluconazole to treat
fluconazole-resistant Candida
Typical dose 250 mg/d, systemic dose 250-500 mg once daily

Ketoconazole (Nizoral)

(an imidazole)

 Oral  Fungistatic against Candida, may be fungicidal
at high doses

Highly lipophilic – poor penetration into aqueous fluids
Stronger liver toxicity than for fluconazole or itraconazole.
Less toxic than amphotericin-B; used for similar fungal
infections.
May decrease testosterone and cortisol levels
Dose at 200-400 mg once/day. Can increase to 600-800
mg/day with increased risk of toxicity

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