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Autobiography of the topical antifungal

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Lauren Brannon

on 24 July 2016

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Transcript of Autobiography of the topical antifungal

By: Lauren Brannon, Leah Alfino, Allie herron, lucia levia, eleanor Colmenares
Autobiography of the topical antifungal
1944: The antifungal properties of azoles were first observed with benzimidazole (Maertens, 2004)
Late 1960's: First topical antifungals, including clotrimazole were developed. Clotrimazole was first introduced in Germany. (Maertens, 2004)
Clotrimazole is on the World Health Organization's Model List of Essential Medicines and is considered to be a medication needed for all basic health-care systems.

(World Health Organization, 2013)
Precautions & Contraindications:
Avoid topical corticosteroids for optimal results. If necessary, use a low-potency steroid such as an OTC hydrocortisone in cases of severe inflammation (O’Mara, 2014).
Adverse Drug Reactions:
Nystatin & Tolnaftate: may cause minor skin irritation

Azoles antifungals: may cause itching, stinging, burning, or skin irritation. Cross-sensitization may occur.
Allylamine antifungals: burning, stinging, dryness, redness, itching, irritation, and rash.

Ciclopirox olamine: itching, irritation, erythema, pain, burning,
worsening symptoms. Change in nail shape and discoloration may occur.
(Robinson & Woo, 2016)

Drug Interactions:
Minimal drug interactions exist.

§ Azole antifungal may interfere with the treatment of amphotericin
B and nystatin by depleting polyene-binding sites.
(Robinson &Woo, 2016)

§ Corticosteroids may inhibit therapeutic effects of econazole
against C.albicans.
(Robinson & Woo, 2016)
Clinical Use:
Used to treat tinea (fungal) skin infections.

Tinea infections are classified based on the location of infection:
§ Scalp: tinea capitis
§ Groin or jock itch: tinea cruris
§ Ringworm: tinea corporis
§ Athlete’s foot: tinea pedis
§ Fingernails or toenails: tinea unguium or onychomycosis
§ Skin (primarily seen on the trunk and upper arms): Tinea Versicolor
§ Mouth, esophagus, & vagina: mucocutaneous candidiasis

Topical antifungal medication can be prescribed in the following form: cream, lotion, ointment, gel, liquid spray, shampoo, foam, powder spray, and powders.

Keep in mind many of the following infections may be treated in combination with oral medication or systemic antifungal...
Tinea Capitis:
Sporicidal shampoo:

Wash with selenium sulfide 2.5% or ketoconazole 2% twice a week until no visible signs of infection.

(Woo & Robinson, 2016)
Tinea Cruris & Tinea Corporis: (Use same treatment)
Terbinafine (Lamisil, Lamisil AT): once daily for 1 week

Naftifine (Naftin), Butenafine (Mentax, Lotrimin Ultra), Clotrimazole (Lotrimin), Econazole, Ketoconazole (Nizoral), Luliconazole (Luzu), Oxiconazole (Oxistat), Tolnaftate (Tinactin): Once daily for 2 weeks

Miconazole & Ciclopirox
(Penlac, Loprox): twice a day for up to 4 weeks.

Ciclopirox (Penlac): Applied once daily to entire nail bed and surrounding tissue (about 5 mm) 8 hours before bathing. Once weeks penlac is removed with alcohol and affected nail is trimmed. Therapy may last for up to 9 months.

(Robinson & Woo, 2016)
Treatment is the same with topical agents as tinea corporis. Length of treatment is up to 4 weeks.

Tinea Pedis
(O’Mara, 2014)
Tinea Versicolor:
Selenium sulfide shampoo is applied to affected area for 10 to 15 minutes daily for one week. (Robinson & Woo, 2016)

Over the counter Miconazole, clotrimazole, and econazole (OTC azoles): twice a day for 2-4 weeks. (Robinson & Woo, 2016)

Butenafine: apply once daily for 2 weeks (O’Mara, 2014)

Mucocutaneous Candidiasis:
o OTC azoles: applied twice daily until no visible signs of infection.

o > 3 years old: Clotrimazole troche 10 mg is dissolved in mouth for 5 times a day for 2 weeks.

o Nystatin: applied 2-3 times a day until no visible signs of infection.

o Ciclopirox olamine: massaged twice a day until clear.

o Naftidine: massaged once a day in cream formula and twice a day in gel formula.

o Butenafine: For patients > 12 years old. Apply once a day until clear.

(Robinson & Woo, 2016)
Rational Drug Selection:
Are thereany guidelines that recommend one drug in the class over another?

Ø The most effective treatment for onychomycosis is an oral antifungal, terbinafine (Lamisil) (O’Mara, 2014).

Is this drug class recommended over another drug class for a specific condition and if so what evidenced based resource/guidelines make/support the recommendation?

Ø The first line of treatment are OTC azoles. However, if infection is not resolved, broader spectrum antifungal may be prescribed (Robinson & Woo, 2016).
Ø Allylamine antifungal may be more effective and require less time for treatment than imidazole agents (O’Mara, 2014).
Ø If itching does not resolve after antifungal treatment, non-steroid antipruritic such as Sarna Sensitive (pramoxine) is recommended (O’Mara, 2014).
Pediatric Considerations:
The use of topical antifungals in children greater than two years, apply to affected area, gently massage sufficient medication into affected and surrounding area q12 hours. If no improvement after four weeks reevaluate diagnosis (Medscape, 2015).
Poor oral bioavailability, unlikely to have any adverse effects in nursing children, including application to nipples. Any excess cream or ointment should be removed from nipples before nursing. Only water miscible cream or gel products should be applied to nipples d/t ointments may expose infants to excessive levels of mineral paraffins (Lactmed, 2013).

Antifungals in lactation are considered a Category L3, which is limited data but probably compatible (Hale & Rowe, 2014).
Pregnancy Considerations:
NYSTATIN is the antifungal of choice;this topical antifungal has the most data collected. There are no teratogenic effects associated with it and it is poorly absorbed from intact skin and mucosal membranes (Prescriber’s Letter, 2014 ). Nystatin is considered category A by the FDA (Pilmis et al., 2015).

CLOTRIMAZOLE is the prototype and has minimal absorption from skin and vagina. There is no association with teratogenic effects to the fetus ( Prescriber’s Letter, 2014).

MICANAZOLE has small amounts absorbed from vagina and has no documented teratogenic effects (Prescriber’s Letter, 2014 ). Miconazole is rated category C during pregnancy (Pilmis et al., 2015).

TERBINAFINE has no human data recorded. Minimal systemic absorption and no teratogenic effects in animals (Prescriber’s Letter, 2014).

CICLOPIROX has no human data. Has minimal systemic absorption with no teratogenic effects in animals (Prescriber’s Letter, 2014).

CICLOPIROXALAMINE displays a poor systemic absorption and is rated category B during pregnancy (Pilmis et al., 2015).

SELENIUM SULFIDE recommended for short term use only (Prescriber’s Letter, 2014)

The CDC recommends the seven-day treatment plan of topical azole for pregnant women with vulvovaginal candidiasis (Prescriber’s Letter, 2014). Topical antifungals all display a small and limited absorption of medication (Pilmis et al., 2015).
Vaginal azoles are first-line for vaginal yeast during pregnancy. The inconvenience of using this product for a week may cause patients to request oral medication. Now new evidence suggests that just 1 or 2 doses of Fluconazole during the first or second trimester is linked to miscarriage and long term use is associated with birth defects (Prescriber’s Letter, 2016).
Elderly Considerations:
There is data indicating that intravaginal and topical miconazole can lead to an increased INR, it can be increased significantly with single doses of fluconazole. It is recommended to monitor the INR when therapy is started, stopped, and/or dosage change occurs. Some clinicians consider decreasing the warfarin dose by about 25% (Prescriber’s Letter, 2012). Elderly patients treated for Pityriasis Versicolor, were found to have a less therapeutic effect of Imidazolium topical therapy, as the patient population increased in age (Balestri et al., 2012).
Hepatic & Renal Insufficiency Considerations:
Frequency not reported - elevated serum AST (SGOT) concentrations (15%) have been documented (Medscape, 2015).

Many patients cannot tolerate systemic antifungals because of the potential liver toxicity. Topical antifungals are a great option because there is minimal systemic absorption with most topical agents (Woo & Robinson, 2016).

There are times when a topical agent can be harmful and should always be researched. The treatment of tinea capitis may need prolonged treatment. Two examples of topical medications are griseofulvin, and ketoconazole may require liver, renal, and hematopoietic test prior to beginning and throughout treatment (Woo & Robinson, 2016)
The prototype for topical antifungals is
Over the counter butenafine ( Lotrimin Ultra) and terbinafine (Lamisil AT) cost approximately $16 for 30 grams (Prescriber’s Letter, 2014).

Over the counter products are more affordable than prescription medications. Clotrimazole and miconazole are often a first choice for purchase d/t the lower price range. Generic products are less expensive than the brand name of the drug (Woo & Robinson, 2016)
Monitoring Needs:
Topical antifungals generally do not require any additional monitoring beyond what the disease process being treated needs monitoring. ( & (Woo & Robinson, 2016).
Griseofulvin, and ketoconazole may require liver, renal, and hematopoietic test prior to beginning and throughout treatment (Woo & Robinson, 2016)
Patient Education:
-clean and dry the area before applying medication
-do not cover the area with a bandage or wrap
-wash your hands after administration
-do not get this message in eyes, nose, mouth, nose, vagina or on healthy area of skin.
-Use the medication regularly as directed for best results.
-Continue to use the medication for the whole time you have been prescribed even if the symptoms improve.
(Medscape, 2015)

Adverse Reactions
-Typically minimal-mild skin irritation, itching, burning, stinging.
-cross reaction between topical azoles is common
(Robinson & Woo, 2016)
Rx Examples:
Inscription: Econazole topical 1% cream
Sig: apply topically to affected area BID for 2 weeks
Disp: #1
Refills: 0
Inscription: Nystatin topical ointment 100,000 unit/g
Sig: apply topically to affected area every 12 hours for 2 weeks.
Disp: #1
Overview of Drug Class:
 Topical antifungal medications are used to treat superficial fungal and yeast infections (Woo & Robinson, 2016).

 There are four categories of topical antifungal medications:

 1. Allylamine/benzylamine –examples Lamisil, Naftin, and Menatax

 2. Imidazole-examples Lotrimin, Nizoral, Extina, Monistat,

 3. Polyene-example is nystatin

 4. Other-Loprox broad spectrum antifungal (a benzylamine), Spectazole, Ertaczo, Oxistat,
Topical antifungal treatments come in a
variety of forms
such as cream, gel, liquid spray, powder spray, and powder. It is important to consider cost, infection location, and patient preference when choosing a topical antifungal treatment.

It is important that the patient understand correct application of topical antifungals. Application of the topical antifungal should be to the lesion itself as well as two inches around the lesion to prevent the spread of infection to surrounding skin.

(Prescribers Letter, 2014)
(American Academy of Family Physicians, 2002)
Topical nystatin and azole antifungals alter the fungal cell membrane by inhibiting synthesis of ergosterol. This causes permeability and leaking of fungal cell contents.

Allymine antifungals prevent sterol biosynthesis in fungi by inhibiting squalene epoxidase.

Benzylamines inhibit normal cell growth by hindering the production of squalene monooxygenase by fungal cell membranes.

(Woo & Robinson, 2016)
Absorption & Distribution:
Metabolism & Excretion:
Topical antifungals are not absorbed or minimally absorbed systemically. Less than one percent of an applied dose is recovered in the urine and feces.

(Woo & Robinson, 2016)

Check out Prescriber's Letter Table of Topical Antifungal Agents for Tinea Infections here:
(Crowley & Gallagher, 2014)
Chemical structure of clotrimazole
Image retrieved from: https://kaiserhealthnews.files.wordpress.com/2014/11/drug-cost-ben-570.jpg
Image retrieved from: https://www.bestonlinemd.com/what-is-topical-antibiotics/
Image retrieved from: http://img.aws.livestrongcdn.com/ls-1200x630/cme/cme_public_images/www_livestrong_com/photos.demandstudios.com/getty/article/83/28/177875275_XS.jpg
The two main groups of topical antifungal drugs are the azoles and allylamines. Each topical antifungal preparation comes in a variety of strengths with the same active ingredients and different vehicles for application.

A topical treatment ideally should have a high cure rate with a short duration of action and minimal to no adverse effects.

Topical antifungal treatment for fungal infections are well-tolerated and tend not to cause adverse effects in patients.

Most topical antifungal treatments work to disrupt ergosterol synthesis. When ergosterol is interrupted in the cell membrane of a fungus it causes inhibition of fungal growth.

Azole antifungals are fungistatic and can also at high concentrations be fungicidal.
a few things to get us started...
(El-Gohary, et al., 2014)
Based on four clinical trials conducted by Austin, Cleminson, Darlow, and McGuire (2015), prophylactic oral/topical non-absorbed antifungal therapy may reduce the rate of invasive fungal infection in very preterm or very low birth weight infants. However, procedural weaknesses exist, indicating more research is needed to determine its efficiency.
Preterm & Low Birth Weight Use:
Image retrieved from: https://colonialnuggets.wikispaces.com/file/view/super%20fungi.jpg/457024272/976x703/super%20fungi.jpg
Image retrieved from: http://image.shutterstock.com/z/stock-vector-cartoon-man-scratching-all-over-192469196.jpg
New Frontiers in Antifungals!
It has been hypothesized that fungi is a possible pathogenesis of chronic rhinosinusitis (CRS), but little research has been done to support antifungal agents for management of CRS. A 2016 double-blind RCT found that there was no significant difference between treatment of CRS with fluconazole nasal drop 0.2% and placebo treatment. More study is needed to arrive at a clinical consensus on this emerging topic.
(Hashemian, F. et al, 2016)
(Magellan Rx Management, 2015)
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