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

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

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

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