ANTIFUNGAL

An antifungal is a medication that inhibits the growth of fungus, kills it or prevents it from forming. A common example of such a fungus would be yeast. antifungal works by attacking the cells of the fungus, either killing it or preventing it from reproducing. One drug in particular is called flucytosine, which acts by directly penetrating the cells of the fungus and slowing down reproduction and growth rates. Another drug, called clotrimazole acts by punching holes in the cell walls of the fungus, causing important components to fall out. Without these components, the cells cannot reproduce, and therefore the fungus dies. Fungal infections are fairly common and with antifungal medication, many people report relief of uncomfortable symptoms caused by the fungi growth. Antifungal medications come in a variety of forms for a variety of fungal ailments including:

  • Topical: These antifungal medications are typically in cream form and are applied directly to the affected area. Such antifungals are commonly used to treat nail fungal infections and similar ailments.
  • Oral: People who suffer from a yeast infection of the mouth will often be required to take oral medication to treat the fungus.
  • Suppositories: Vaginal yeast infections are commonly treated by way of suppositories, which dissolve and release a topical cream that eliminates the fungus by killing it.

Indications:
> systemic fungal infections (candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis) - these occur when fungi get into the bloodstream and generally cause more serious diseases. Systemic fungal infections may be caused either by an opportunistic organism that attacks a person with a weakened immune system, or by an invasive organism that is common in a specific geographic area, such as cocci and histoplasma. Unlike superficial infections, systemic fungal infections can be life-threatening.

> tinea infections of the skin, hair, nail unresponsive to topical - ringworm, which isn't a worm at all, is a fungus infection that can affect the skin, nails, or scalp. Tinea fungi can infect the skin and related tissues of the body. The medical name for ringworm of the scalp is tinea capitis; ringworm of the body is called tinea corporis; and ringworm of the nails is called tinea unguium. With tinea corporis, the fungi can cause scaly, ring-like lesions anywhere on the body.

> cryptococcal meningitis - is a brain infection caused by a fungus called cryptococcus neoformans, which is found mainly in dirt and bird droppings.
> severe recalcitrant dermatophyte infections unresponsive to topical
> onychomycosis - fungal infection of the finger or toe nails which is very difficult to cure

1. G.N:Clotrimazole

Brand Name:

  • Canesten* Bayer
  • Mycelex* Bayer
  • Desenex* Novartis

Dosage Forms:

  • Lozenges: Clotrimazole 10 mg Mycelex*
  • Topical: Cream: Clotrimazole 1% Desenex* Lotrimin*
    - Lotion: Clotrimazole 1% Desenex* Lotrimin*
    - Solution: Clotrimazole 1% Desenex*

Used for:

  • Tinea corporis
  • Tinea cruris
  • Tinea pedis
  • Pityriasis versicolor
  • Cutaneous candidiasis
  • Nail and skin infections, fungal or gram positive

Therapuetic regimen:

Adult
Pediatric
Dermatomycoses

Clotrimazole 1% cream, solution, or lotion bid x14-28d, apply in a thin layer to the affected area and surrounding skin.

  • Topical preparations should not be used in children < 2 years old
  • Vaginal preparations are not recommended for children < 12 years old
  • Lozenges should not be used in children < 5 years old

Adverse Effect:Local cutaneous effects may include irritation, hypersensitivity, burning, pruritus, erythema, fissuring, or swelling. FDA Pregnancy Category C Oral formulation shows toxicity in animal trials. Use is not recommended during pregnancy or lactation. 2.G.N:Ciclopirox

Trade Name:

  • Penlac* Dermik
  • Loprox* Dermik

Dosage Forms:

  • Nail lacquer solution: Ciclopirox olamine 8% Penlac Nail Lacquer*
  • Topical Gel: Ciclopirox olamine 1% Loprox*
  • Cream: Ciclopirox olamine 1% Loprox*
  • Lotion: Ciclopirox olamine 1% Loprox*
The topical application of this drug was one of the first effective antifungals for superficial dermatophyte, yeast, and fungal infections. The most recent formulation, a lacquer, has made ciclopirox convenient in the treatment of nail infections.

Used for

  • Tinea corporis
  • Tinea cruris
  • Tinea pedis
  • Tinea versicolor
  • Candidiasis, cutaneous
  • Nail lacquer-
  • Onychomycosis

Therapeutic Regimen

Adult
Pediatric
Ciclopirox 1% lotion, gel or cream applied to the affected areas twice a day.

Ciclopirox 8% nail lacquer to be applied daily as directed and removed once a week. Continue up to 48 weeks if necessary.

PediatricSafety and efficacy have not been established for children < 10 years of age.

Safety Information

Adverse Effects
Cutaneous effects may include local irritation or burning when first applied.

FDA Pregnancy Category B Adequate human studies have not been completed. Animal studies have not shown adverse fetal effects. It is not known if ciclopirox is distributed in breast milk.


3.G.N:Ketoconazole

Trade Name:

  • Nizoral* Janssen

Dosage Forms:

  • Topical: Cream: Ketoconazole cream 2% Nizoral*
  • Shampoo: Ketoconazole shampoo 1% and 2% Nizoral Shampoo*
  • Oral: Tablets: Ketoconazole tablets 200 mg
  • Suspension: Ketoconazole oral suspension 100mg/5mL Nizoral*

Uses

Labeled Indications
Off-Label Uses
Topical
  • Tinea corporis, cruris, pedis
  • Pityriasis versicolor
  • Cutaneous candidiasis
  • Seborrehic dermatitis
  • Dandruff
Systemic Tinea corporis, cruris, pedis, severe and unresponsive to Griseofulvin therapy * Chromomycosis
  • Chronic mucoutaneous candidiasis
  • Candidiasis, oropharyngeal
Other (selection)* Paracoccidiomycosis
  • Candidiasis, systemic
Systemic* OnychomycosisParonychia #
  • Leishmaniasis, cutaneous #
  • Candidiasis, vulvo-vaginal #

# - not included in Canadian product labeling

Therapeutic Regimen

Adult
Pediatric
Systemic
  • Pityriasis versicolor
  • Ketoconazole 200mg po daily x5-10d
Other antifungal indications Ketoconazole 200-400mg po daily. * Therapy to be continued for 1-2 weeks in candidal infections; for 1- 8 weeks in dermatophytes; and for 6 months or longer in systemic mycoses
Topical* Dandruff

  • Ketoconazole 1% shampoo every 3-4 days for up to 8 weeks
Seborrehic dermatitis* Ketoconazole 2% shampoo or cream twice a week for 2-4 weeks. Apply to the hair and scalp, leave for 5 minutes and wash off
Pityriasis versicolor* Ketoconazole 2% shampoo single application to the affected areas and surrounding skin. Leave for 5 minutes and rinse.
Tinea corporis, cruris, pedis and cutaneous candidiasis* Ketoconazole 2% cream applied to the affected areas, and surrounding skin once a day until clear.

Systemic* Safety and efficacy have not been established for systemic use in children < 2 years of age
  • 2 years of age * Ketoconazole 3.3-6.6 mg/kg po daily
Vulvovaginal candidiasis * Ketoconazole 5-10 mg/kg po daily yx5d
Paronychia * Ketoconazole 5-10 mg/kg po daily
Topical* Safety and efficacy have not been established for topical use

Side Effects:

  • Local cutaneous effects may include itching, stinging, irritation or contact dermatitis.
  • Cutaneous effects may include hypersensitivity reactions including exfoliative dermatitis and Stevens-Johnson syndrome
  • Gastrointestinal effects may include nausea, abdominal pain, diarrhea, constipation, loss of appetite and rarely, hepatotoxicity.
  • Hematologic effects may include agranulocytosis or thrombocytopenia.
  • Other effects may include headache, dizziness and drowsiness. Azospermia, impotence, decreased libido in menstrual irregularities may occur as a result of corticosteroid and testosterone suppression.
FDA Pregnancy Category C
Animal studies have shown teratogenicity and embryonic toxicity when given very high oral doses. Use of ketoconazole is not recommended during pregnancy or lactation.

4.G.N: Terbinafine hydrochloride

Trade Name:

  • Lamisil* Novartis
  • Lamisil DermGel* Novartis
  • Lamisil AT* Novartis

Dosage Types;

  • Topical: Cream: Terbinafine hydrochloride 1% *
    Lamisil* and Lamisil AT
  • Solution: Terbinafine hydrochloride Lamisil
  • Oral: Tablets: Terbinafine hydrochloride tablets 250 mg Lamisil*

Therapeutic Regimen

Adult
Pediatric
Oral
Onychomycosis

  • Lamisil 250 mg po daily x6 weeks for the fingernails, and x12 weeks for the toenails.
Tinea cruris, corporis and pedis * Lamisil 250 mg po daily x2-6 weeks
Topical
Tinea corporis and cruris* Lamisil 1% 1-2x/d x1 week until significant improvement shows.

  • Treatment should not be continued after 4 weeks.
Tinea pedis* Lamisil 1% 2x/d x2 weeks until significant improvement shows.
  • Treatment should not be continued after 4 weeks.
Tinea versicolor.* Lamisil 1% 1-2x/d x2 weeks until significant improvement shows.
  • Treatment should not be continued after 4 weeks.
Cutaneous candidiasis * Lamisil 1% 1-2x/d x1-2 weeks until significant improvement shows.
  • Treatment should not be continued after 4 weeks.
Oral* Safety and efficacy have not been established
Topical* Safety and efficacy have not been established in children < 12 years of


Adverse Effects
  • Local cutaneous effects may include mild burning, irritation, and erythema.
  • Cutaneous effects may include hypersensitivity reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.
  • Gastrointestinal effects may include nausea, dyspepsia, stomach pain, reversible loss of taste and hepatitis.
  • Hematologic effects may include neutropenia and pancytopenia.

FDA Pregnancy Category B

Human tests have not been completed, but animal testing has not shown any adverse fetal effects. Terbinafine is distributed in the breast milk. Treatment during pregnancy and lactation is not recommended.

5. G.N: Caspofungin

Trade Name:

  • Cancidas

Dosage Types:
  • Cancidas 50mg for i.v.-infusion (manufacturer Merck)
  • Cancidas 70mg for i.v.-infusion (manufacturer Merck)

    Therapeutic Regimen:
Adult
Pediatric
There is no sufficient clinical experience to judge the safety and efficacy in patients younger than 18 years of age.
  • Warning:
  • Hepatic Effects
The concomitant use of caspofungin and cyclosporine in healthy volunteers led to a more frequent increase of liver enzymes (ALT=SGPT and AST=SGOT) than noted with cyclosporine alone. Combination treatment is only indicated, if the potential benefit for the patient outweighs the potential risk.
Dosage reduction in patients with moderately impaired liver function is recommended. No clinical data exists regarding the use of caspofungin in patients with severely impaired liver function.

    • Sensitivity Reactions
Reactions due to histamine release (rash, facial swelling, pruritus, sensation of warmth and one case of anaphylaxis) have been seen. Those reactions should be carefully watched for.
    • Drug Resistance
In a few patients with infections caused by C. albicans mutants with reduced sensitivity to caspofungin have been noticed. Currently there is no data regarding development of resistance in other fungi than C. albicans.
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  • Side Effects:
Compared to amphotericin B, caspofungin seems to have a relatively low incidence of side-effects. In clinical studies and post-marketing reports the side-effects seen in 1% or more of the patients were as follows:
Additionally, infrequent cases of symptomatic liver damage, peripheral edema and swelling, and hypercalcemia have been seen. One case of anaphylaxis (severe allergic reaction) has also been noted.
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  • FDA Pregnancy Category C
Caspofungin has in animal studies been shown to have embroyotoxic properties and therefore has been assigned to class C. It should only be given to pregnant women, if the benefit to the mother clearly outweighs the potential risk to the unborn.
The drug is found in the milk of lactating rats; it is not known, whether this effect can be seen in women, too. Lactating women should be treated cautiously.

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  • Trade Name:

  • * Mycamine 6. Micafungin

  • Dosage Forms:

  • Mycamine 50mg for i.v.-infusion (manufacturer Astellas)
  • Mycamine 100mg for i.v.-infusion (manufacturer Astellas)

    Dosage:
For the treatment of candidemia, acute disseminated candidiasis, candida peritonitis and abscesses, the dosage of micafungin is 100 mg once daily. For the treatment of esophageal candidiasis, the dosage is 150 mg once daily. For prophylaxis of candida infections in HSCT recipients, the dosage is 50 mg once daily.
  • Contraindications:
>
Known hypersensitivity to micafungin or any other ingredient contained in the formulation.

  • FDA Pregnancy Category C