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Terbinafine Hydrochloride topical

Pronunciation

Class: Allylamines
VA Class: DE102
Chemical Name: 1-Naphthalenemethanamine,N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethanamine hydrochloride
Molecular Formula: C21H25N•ClH
CAS Number: 78628-80-5
Brands: Lamisil

Introduction

Antifungal; synthetic allylamine structurally and pharmacologically related to naftifine.1 2 11 12 19

Uses for Terbinafine Hydrochloride

Dermatophytoses

Treatment of tinea corporis (body ringworm)1 2 9 10 11 19 20 21 and tinea cruris (jock itch)1 2 6 8 9 10 11 19 20 21 caused by Trichophyton mentagrophytes, T. rubrum, or Epidermophyton floccosum.

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Treatment of tinea pedis (athlete's foot) caused by T. mentagrophytes, T. rubrum, or E. floccosum1 2 3 4 5 9 10 11 14 19 20 21 and plantar tinea pedis (moccasin type) caused by T. mentagrophytes or T. rubrum.1

Pityriasis (Tinea) Versicolor

Treatment of pityriasis (tinea) versicolor caused by Malassezia furfur (Pityrosporum ovale).19

Terbinafine Hydrochloride Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a cream or solution.1 2 3 4 5 6 7 8 9 10 11 13 14 15 18 19 20 21

Do not apply to the eye or administer orally or intravaginally.1 19 20 21

Do not use on nails or scalp; avoid contact with the nose, mouth, and other mucous membranes.1 19 20 21

Do not use the solution spray on the face.21

Do not use with occlusive dressings or wrappings, unless otherwise directed by clinician.1 19 20 21

Cream or Solution

The affected skin and surrounding areas should be washed with soap and water and dried completely before the drug is applied.20 21

Apply a sufficient amount of cream or solution either once or twice daily (as directed); rub gently into affected area and surrounding skin.1 3 4 5 9 10 11 13 14 15 18

Dosage

Available as terbinafine hydrochloride; dosage expressed in terms of terbinafine.1

Pediatric Patients

Dermatophytoses
Tinea Corporis or Tinea Cruris
Topical

Children ≥12 years of age: apply cream once or twice daily for ≥1 week.1 2 6 8 9 10 11 16 17 20 21 Alternatively, apply solution once daily for 1 week.19 21

For self-medication, treatment usually is continued for 1 week.20 21 When directed by clinician, treatment is ≥1 week but should not be >4 weeks.1

Tinea Pedis
Topical

Children ≥12 years of age: apply cream or solution twice daily (morning and evening) for ≥1 week.1 3 4 5 9 10 11 13 14 15 18

For plantar/moccasin-type tinea pedis, apply cream twice daily for 2 weeks.1

For self-medication, treatment usually is continued for 1 week.20 21 When directed by clinician, treatment is ≥1 week but should not be >4 weeks.1

Pityriasis (Tinea) Versicolor
Topical

Children ≥12 years of age: apply solution twice daily for 1 week.19

Adults

Dermatophytoses
Tinea Corporis or Tinea Cruris
Topical

Apply cream once or twice daily for ≥1 week.1 2 6 8 9 10 11 16 17 20 21 Alternatively, apply solution once daily for 1 week.19 21

For self-medication, treatment usually is continued for 1 week.20 21 When directed by clinician, treatment is ≥1 week but should not be >4 weeks.1

Tinea Pedis
Topical

Apply cream or solution twice daily (morning and evening) for ≥1 week.1 3 4 5 9 10 11 13 14 15 18

For plantar/moccasin-type tinea pedis, apply cream twice daily for 2 weeks.1

For self-medication, treatment usually is continued for 1 week.20 21 When directed by clinician, treatment is ≥1 week but should not be >4 weeks.1

Pityriasis (Tinea) Versicolor
Topical

Apply solution twice daily for 1 week.19

Cautions for Terbinafine Hydrochloride

Contraindications

  • Hypersensitivity to terbinafine or any ingredient in the formulation.1 19

Warnings/Precautions

Sensitivity Reactions

If irritation or sensitivity occurs, discontinue the drug and initiate appropriate therapy.1 19

General Precautions

Selection and Use of Antifungals

Prior to administration of terbinafine for dermatophytoses or pityriasis (tinea) versicolor, diagnosis should be confirmed either by direct microscopic examination of scrapings from infected tissue mounted in potassium hydroxide (KOH) or by culture.1 19

Clinical improvement usually is evident within the first week of therapy, and patients treated for 1–2 weeks usually show continued improvement for several weeks after completion of treatment.1 2 4 6 8 11 14 18 If clinical improvement is not evidence within 2–6 weeks after completion of topical therapy, the diagnosis should be reevaluated.1

Local Effects

The solution contains 28.7% alcohol which may be irritating or drying.19

Possible Prescribing and Dispensing Errors

Ensure accuracy of prescription; similarity in spelling of lamotrigine (Lamictal) and terbinafine (Lamisil) may result in errors.22 23

Specific Populations

Pregnancy

Category B.1 19

Lactation

Distributed into milk following oral administration.1 19 Discontinue nursing or the drug.1 19

Pediatric Use

Safety and efficacy not established in children <12 years of age.1 19 20 21

Common Adverse Effects

Irritation, burning/tingling, pruritus, dryness, skin exfoliation, erythematous rash.1 19

Terbinafine Hydrochloride Pharmacokinetics

Absorption

Percutaneous absorption occurs following topical application of the cream or solution to intact skin.1 19

Distribution

Extent

Penetration into stratum corneum is similar following topical application of the cream or solution.1 19

Distributed into milk following oral administration.1 19

Elimination

Metabolism

Systemically absorbed drug is extensively metabolized.1 19

Elimination Route

Approximately 75% of cutaneously absorbed drug is eliminated in urine, principally as metabolites.1 19

Half-life

Half-life when absorbed through the skin is approximately 21 hours.19

Stability

Storage

Topical

Cream

20–25°C;20 may be stored at 5–30°C.1

Solution

8–25°C;21 do not refrigerate.19

Actions and Spectrum

  • May be fungicidal or fungistatic in action, depending on concentration of the drug and specific fungus tested.1 2 3 4 11 15 19

  • Appears to interfere with sterol biosynthesis in susceptible fungi by inhibiting the enzyme squalene monooxygenase (squalene 2,3-epoxidase).1 2 19 The resulting accumulation of squalene (the usual substrate of the enzyme) in the cells and decreased amounts of sterols, especially ergosterol,1 2 19 may contribute to the antifungal effects.2

  • Active against many fungi, including dermatophytes (Trichophyton, Microsporum, Epidermophyton), filamentous (e.g. Aspergillus), dimorphic (e.g., Blastomyces), and dematiaceous fungi and yeasts.1 2

  • Dermatophytes: active in vitro and in clinical infections against T. rubrum, T. mentagrophytes, and E. floccosum.1 19 Also active in vitro against M. canis, M. gypseum, M. nanum, and T. verrucosum.1 19 More active than azole antifungals (e.g., fluconazole, itraconazole, ketoconazole) against dermatophytes.5 8 15

  • Other fungi: active in vitro and in clinical infections against Malassezia furfur.19 Also active in vitro against some Candida, including C. albicans and C. parapsilosis.2 3 4 11 15 Less active than azole antifungals against Candida.2 9 11

Advice to Patients

  • Importance of applying to affected areas as directed and avoiding contact with eyes, nose, mouth, or other mucous membranes.1 19 20 21 Importance of not using occlusive dressings, unless otherwise directed by clinician.1 19

  • Advise patient not to use spray solution on the face.19 If accidental contact with eyes occurs, importance of rinsing eyes thoroughly with running water and consulting a clinician if symptoms persist.19 20 21

  • Advise patients to wash their hands after touching the affected areas so that the infection is not spread to other areas of the body or to other individuals.20 21

  • For patients with tinea pedis (athlete's foot), importance of wearing well-fitting, ventilated shoes and changing socks at least once daily.20 21

  • Importance of completing full course of therapy, even if symptoms improve.1 19

  • Importance of notifying clinician if improvement does not occur after 1 week of treatment.19

  • Importance of consulting clinician if treated area becomes irritated (e.g., erythema, pruritus, burning, blistering, swelling, oozing).1 19 20 21

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs.

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

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

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

Terbinafine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

1%

Lamisil AT (with benzyl alcohol)

Novartis

Solution

1%

Lamisil (with cetomacrogol, ethanol, and propylene glycol)

Novartis

Lamisil AT Spray Pump (with cetomacrogol, ethanol, and propylene glycol)

Novartis

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions October 1, 2005. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Novartis Pharmaceuticals Corporation. Lamisil (terbinafine hydrochloride) 1% cream prescribing information (dated 1997 Mar). In: Physicians’ desk reference. 52nd ed. Montvale, NJ: Medical Economics Company Inc; 1998;1859-61.

2. Balfour JA, Faulds D. Terbinafine: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial mycoses. Drugs. 1992; 43: 259-84.

3. Savin RC. Treatment of chronic tinea pedis (athlete’s foot type) with topical terbinafine. J Am Acad Dermatol. 1990; 23:786-9. [PubMed 2229524]

4. Berman B, Ellis C, Leyden J et al. Efficacy of a 1-week, twice-daily regimen of terbinafine 1% cream in the treatment of interdigital tinea pedis. J Am Acad Dermatol. 1992; 26:956-60. [PubMed 1607415]

5. Smith EB, Noppakun N, Newton RC. A clinical trial of topical terbinafine (a new allylamine antifungal) in the treatment of tinea pedis. J Am Acad Dermatol. 1990; 23:790-4. [PubMed 2229525]

6. Greer DL, Jolly HW Jr. Treatment of tinea cruris with topical terbinafine. J Am Acad Dermatol. 1990; 23: 800-4. [PubMed 2229527]

7. Aste N, Pau M, Pinna AL et al. Clinical efficacy and tolerability of terbinafine in patients with pityriasis versicolor. Mycoses. 1991; 34:353-7. [PubMed 1803242]

8. Millikan LE. Efficacy and tolerability of topical terbinafine in the treatment of tinea cruris. J Am Acad Dermatol. 1990; 23:795-9. [PubMed 2229526]

9. Kagawa S. Clinical efficacy of terbinafine in 629 Japanese patients with dermatomycosis. Clin Exp Dermatol. 1989; 14:114-5. [PubMed 2689013]

10. Villars V, Jones TC. Clinical efficacy and tolerability of terbinafine (Lamisil)—a new topical and systemic fungicidal drug for treatment of dermatomycoses. Clin Exp Dermatol. 1989; 14:124-7. [PubMed 2689015]

11. Shear NH, Villars VV, Marsolais C. Terbinafine: an oral and topical antifungal agent. Clin Dermatol. 1992; 9:487-95.

12. Lyman CA, Walsh TJ. Systemically administered antifungal agents: a review of their clinical pharmacology and therapeutic applications. Drugs. 1992; 44:9-35. [PubMed 1379913]

13. Anon. Topical terbinafine for tinea infections. Med Lett Drugs Ther. 1993; 35:76-8. [PubMed 8341207]

14. Bergstresser PR, Elewski B, Hanifin J et al. Topical terbinafine and clotrimazole in interdigital tinea pedis: a multicenter comparison of cure and relapse rates with 1- and 4-week treatment regimens. J Am Acad Dermatol. 1993; 28:648-51. [PubMed 8463471]

15. Smith EB. Topical antifungal drugs in the treatment of tinea pedis, tinea cruris, and tinea corporis. J Am Acad Dermatol. 1993; 28(5 Part 1):S24-8. [PubMed 8496408]

16. Sandoz Pharmaceutical Corporation, East Hanover, NJ: Personal communication.

17. Reviewers’ comments (personal observations).

18. Evans EGV, Dodman B, Williamson DM et al. Comparison of terbinafine and clotrimazole in treating tinea pedis. BMJ. 1993; 307:645-7. [IDIS 320437] [PubMed 8401048]

19. Novartis Pharmaceuticals Corporation. Lamisil (terbinafine hydrochloride) 1% solution prescribing information. East Hanover, NJ; 1999 Feb.

20. Novartis Consumer Health, Inc. Lamisil AT (terbinafine hydrochloride 1%) cream patient information. Summit, NJ; 1999.

21. Novartis Consumer Health, Inc. Lamisil AT (terbinafine hydrochloride solution 1%) Spray Pump patient information. Summit, NJ; 2000.

22. Kent RS. Dear health professional letter: Dispensing errors alert. Research Triangle Park, NC: Glaxo Wellcome, Inc; 2000 Aug.

23. Sykes NS. Dear pharmacist letter: Dispensing errors alert. Research Triangle Park, NC: Glaxo Wellcome, Inc; 2000 Jun 6.

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