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Luliconazole

Class: Azoles
VA Class: DE102
Chemical Name: (2E)-2-[(4R)-4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-imidazol-1-ylacetonitrile
Molecular Formula: C14H9Cl2N3S2
CAS Number: 187164-19-8
Brands: Luzu

Introduction

Antifungal; azole (imidazole derivative).1 2 17

Uses for Luliconazole

Dermatophytoses

Treatment of tinea corporis (body ringworm) and tinea cruris (jock itch, groin ringworm) caused by Epidermophyton floccosum or Trichophyton rubrum.1 2 5

Treatment of interdigital tinea pedis (athlete’s foot, foot ringworm) caused by E. floccosum or T. rubrum.1 2 4

Topical antifungals usually effective for treatment of tinea corporis and tinea cruris.7 8 9 10 14 An oral antifungal may be necessary if tinea corporis or tinea cruris is extensive, dermatophyte folliculitis is present, the infection is chronic or does not respond to topical therapy, or patient is immunocompromised because of coexisting disease or concomitant therapy.7 8 9 10 14

Topical antifungals usually effective for treatment of uncomplicated tinea pedis.7 8 9 10 14 An oral antifungal usually necessary if tinea pedis is extensive, the infection is chronic or does not respond to topical therapy, patient is immunocompromised because of coexisting disease or concomitant therapy, or the infection involves hyperkeratotic areas on palms and soles or chronic moccasin-type (dry-type) tinea pedis.7 8 9 10 14

Luliconazole Dosage and Administration

Administration

Topical Administration

Apply topically to skin as a 1% cream.1

Do not administer orally or intravaginally;1 do not apply topically to eyes.1

Apply sufficient amount of cream to cover affected areas and approximately 1 inch of surrounding healthy skin.1

Wash hands after applying the cream.1

Dosage

Adults

Dermatophytoses
Tinea Corporis or Tinea Cruris
Topical

Apply 1% cream once daily for 1 week.1 Use amount sufficient to cover affected area and approximately 1 inch of surrounding healthy skin.1

Tinea Pedis (Interdigital)
Topical

Apply 1% cream once daily for 2 weeks.1 Use amount sufficient to cover affected area and approximately 1 inch of surrounding healthy skin.1

Special Populations

No special population dosage recommendations.1

Cautions for Luliconazole

Contraindications

  • Manufacturer states none.1

Warnings/Precautions

Sensitivity Reactions

Contact dermatitis reported following topical application of 1% cream.1 13 Cross-sensitivity to both luliconazole and lanoconazole (not commercially available in US) reported.13

Local irritation may occur.1

Administration Precautions

For topical use only.1 Do not use orally or intravaginally;1 do not apply to eyes.1

Selection and Use of Antifungals

Prior to initiation of treatment of dermatophytoses, confirm diagnosis by direct microscopic examination of scrapings from infected tissue mounted in potassium hydroxide (KOH) or by culture.7 9 14

Specific Populations

Pregnancy

Category C.1

Lactation

Not known whether distributed into milk following topical application of 1% cream.1 Use with caution in nursing women.1

Pediatric Use

Safety and efficacy not established in children.1

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.1

Common Adverse Effects

Application site reactions, including pruritus and pain.1

Interactions for Luliconazole

May inhibit CYP2C19 and 3A4;1 2 clinically important interactions with CYP2C19 and 3A4 substrates unlikely because systemic exposure is low following topical application of luliconazole to skin.2 Inhibition of CYP1A2, 2C9, and 2D6 not expected.1

No formal drug interaction studies to date.1

Luliconazole Pharmacokinetics

Absorption

Bioavailability

Following topical application of luliconazole 1% cream to skin, low concentrations are absorbed systemically.1 6

Adults with moderate to severe tinea cruris: Once-daily application of 1% cream to affected and surrounding areas of skin (approximately 3.5 g daily) for 15 days resulted in mean peak plasma concentrations of 4.91 ng/mL after first dose and 7.36 ng/mL after final dose; time to peak concentrations was 21 and 6.5 hours, respectively.1 6

Adults with moderate to severe tinea pedis: Once-daily application of 1% cream to affected and surrounding areas of skin (approximately 3.5 g daily) for 15 days resulted in mean peak plasma concentrations of 0.4 ng/mL after first dose and 0.93 ng/mL after final dose; time to peak concentrations was 16.9 and 5.8 hours, respectively.1 6

Distribution

Extent

Not known whether distributed into milk following topical application of 1% cream.1

Plasma Protein Binding

>99%.1

Elimination

Metabolism

In vitro studies suggest systemically absorbed luliconazole may be metabolized by CYP2D6 and 3A4.6

Half-life

Mean plasma half-life was 21.1 or 32.4 hours on day 15 of once-daily topical application of 1% cream in adults with tinea cruris or tinea pedis, respectively.6

Stability

Storage

Topical

Cream

20–25°C (may be exposed to 15–30°C).1

Actions and Spectrum

  • Imidazole-derivative azole antifungal.1 2 17

  • Exact mechanism of action not fully determined.1 2 3 12 Antifungal activity appears to result from interference with ergosterol synthesis via inhibition of C-14 demethylation of sterol intermediates (e.g., lanosterol).1 2 3 12 This results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and accumulation of lanosterol.1

  • Spectrum of activity includes dermatophytes, yeasts, and some other fungi.1 3 11 12 16 18

  • Dermatophytes: Active in vitro against Epidermophyton floccosum,1 3 11 Trichophyton mentagrophytes,3 11 12 16 T. rubrum,1 3 11 12 16 T. tonsurans,11 12 T. verrucosum,11 T. violaceum,11 Microsporum canis,11 and M. gypseum.11

  • Other fungi: Active in vitro against Candida albicans,3 11 12 Malassezia furfur,3 18 M. restricta,12 M. slooffiae,18 and M. sympodialis.18

  • Some evidence that luliconazole may be more active than terbinafine against dermatophytes and C. albicans in vitro.3 11 12

Advice to Patients

Importance of using luliconazole cream only for the condition prescribed.1

Advise patients that the cream is for external use only and to avoid contact with eyes, mouth, or vagina.1

Advise patients to wash their hands after applying the cream to affected areas.1

Advise patients that skin irritation may occur;1 importance of reporting any application site adverse reactions.1

Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1

Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Luliconazole

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

1%

Luzu

Valeant

AHFS DI Essentials. © Copyright, 2016, American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814. Review Date: September 06, 2016.

References

1. Medicis. Luzu (luliconazole) cream 1% prescribing information. Bridgewater, PA: 2013 Nov.

2. US Food and Drug Administration. Center for Drug Evaluation and Research. Application Number204153Orig1s000: Medical Review. From FDA website.

3. US Food and Drug Administration. Center for Drug Evaluation and Research. Application Number204153Orig1s000: Microbiology Review. From FDA website.

4. Jarratt M, Jones T, Adelglass J et al. Efficacy and safety of once-daily luliconazole 1% cream in patients ≥12 years of age with interdigital tinea pedis: a phase 3, randomized, double-blind, vehicle-controlled study. J Drugs Dermatol. 2014; 13:838-46. [PubMed 25007368]

5. Jones TM, Jarratt MT, Mendez-Moguel I et al. A randomized, multicenter, double-blind, vehicle-controlled study evaluating the efficacy and safety of luliconazole cream 1% once daily for 7 days in patients aged ≥ 12 years with tinea cruris. J Drugs Dermatol. 2014; 13:32-8. [PubMed 24385117]

6. US Food and Drug Administration. Center for Drug Evaluation and Research. Application Number204153Orig1s000: Clinical Pharmacology and Biopharmaceutics Review. From FDA website.

7. Hay RJ. Dermatophytosis and other superficial mycoses. In: Mandell GL, Bennett, JE, Dolin R, eds. Mandell, Douglas, and Bennett's: Principles and Practice of Infectious Diseases. Vol 2. 7th ed. Philadelphia: Elsevier; 2010: 3345-55.

8. Piérard GE, Arrese JE, Piérard-Franchimont C. Treatment and prophylaxis of tinea infections. Drugs. 1996; 52:209-24. [PubMed 8841739]

9. Drake LA, Dincehart SM, Farmer ER et al. Guidelines of care for superficial mycotic infections of the skin: tinea corporis, tinea cruris, tinea faciei, tinea manuum, and tinea pedis. J Am Acad Dermatol. 1996; 34:282-6. [IDIS 363962] [PubMed 8642094]

10. Gupta AK, Einarson TR, Summerbell RC et al. An overview of topical antifungal therapy in dermatomycoses. A North American perspective. Drugs. 1998; 55:645-74. [PubMed 9585862]

11. Uchida K, Nishiyama Y, Yamaguchi H. In vitro antifungal activity of luliconazole (NND-502), a novel imidazole antifungal agent. J Infect Chemother. 2004; 10:216-9. [PubMed 15365862]

12. Koga H, Nanjoh Y, Makimura K et al. In vitro antifungal activities of luliconazole, a new topical imidazole. Med Mycol. 2009; 47:640-7. [PubMed 19115136]

13. Tanaka T, Satoh T, Yokozeki H. Allergic contact dermatitis from luliconazole: implication of the dithioacetal structure. Acta Derm Venereol. 2007; 87:271-2. [PubMed 17533499]

14. American Academy of Pediatrics. Red Book: 2012 Report of the Committee on Infectious Diseases. 29th ed. Elk Grove Village, IL: American Academy of Pediatrics; 2012.

15. El-Gohary M, van Zuuren EJ, Fedorowicz Z et al. Topical antifungal treatments for tinea cruris and tinea corporis. Cochrane Database Syst Rev. 2014; 8:CD009992. [PubMed 25090020]

16. Niwano Y, Kuzuhara N, Kodama H et al. In vitro and in vivo antidermatophyte activities of NND-502, a novel optically active imidazole antimycotic agent. Antimicrob Agents Chemother. 1998; 42:967-70. [PubMed 9559824]

17. Khanna D, Bharti S. Luliconazole for the treatment of fungal infections: an evidence-based review. Core Evid. 2014; 9:113-24. [PubMed 25285056]

18. Uchida K, Nishiyama Y, Tanaka T et al. In vitro activity of novel imidazole antifungal agent NND-502 against Malassezia species. Int J Antimicrob Agents. 2003; 21:234-8. [PubMed 12636984]

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