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Lamisil Review Article

 

TextLamisil is the first oral antimycotic of the allylamine class of antifungals. It possesses a broad spectrum of antifungal activity, with proven activity against dermatophytes, molds, and some yeasts and dimorphic fungi. Lamisil (Terbinafine) used to treat infections caused by fungus and affect the toenails and fingernails. Also, the lamisil oral granules are used in treating children under four years with fungal infections of scalp hair follicles and for the treatment of superficial fungal infections, particularly onychomycosis of the nails.

Fungal Infections: Onychomycosis

Fungal infections may be classified as systemic mycoses or superficial infections. The former is a more serious condition wherein the fungi invades the body and enters the general circulation, whereas the latter involves infection of the external structures such as the skin.

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Superficial infections of the skin are referred to as dermatophytoses, or more commonly, ringworm or tinea. These are caused by fungi called dermatophytes, which are soil-dwelling organisms that consist of the genera Trichophyton, Epidermophyton, or Microsporum. Because of the fungi’s ability to penetrate and proliferate in keratinous structures of the body, different areas of the body may be affected such as the hands, hair, and foot. Dermatophytoses of the fingernails or toenails are referred to as onychomycosis or tinea unguium.
Onychomycosis is one of the most common dermatological conditions, with an estimated prevalence of seven to ten percent. It affects the toenails around four times more commonly than the fingernails, and in most cases are caused by the organism Trichophyton rubrum. It can be precipitated by certain risk factors such as increasing age, genetic predisposition, immunodeficient state, diabetes mellitus, peripheral vascular disease, smoking, and frequent nail trauma. It usually manifests as a chalky or dull yellow nail which may eventually become brittle and crumbly. Onychomycosis is classified clinically as distal and lateral subungual onychomycosis (DLSO), superficial white onychomycosis (SWO), proximal subungual onychomycosis (PSO), candidal onychomycosis and total dystrophic onychomycosis. (Roberts, Taylor, and Boyle, 2003) Continue reading...

Although it may be perceived as a trivial problem which does not require medical attention, Onychomycosis is actually a progressive, possibly debilitating disease which may pose a negative impact on one’s health and quality of life if not properly treated. It can proceed to complications such as cellulitis, which reduces mobility and affect blood circulation in diabetes or peripheral vascular disease patients. As the disease is also infectious, untreated persons can transmit the fungi to other areas of the body or to other people. (Roberts, Taylor, and Boyle, 2003)

Prior to treatment, a confirmed diagnosis of onychomycosis should be made through laboratory testing of nail specimens.


Mechanism of Action

As a member of the allylamine class of antifungal agents, Lamisil exerts its action by inhibiting the enzyme squalene epoxidase, which is responsible for the conversion of squalene to ergosterol. The fungicidal action is a result of the accumulation of intracellular squalene, which interferes with fungal membrane function and cell wall synthesis. Aside from this, there is also a deficiency of ergosterol, an integral component of the fungal cell wall. Lamisil is a potent non-competitive squalene epoxidase inhibitor in fungi such as Candida, but a much higher drug concentration is required for inhibition of rat squalene epoxidase. This inhibition is also reversible, thereby causing Lamisil to have no effect on mammalian cholesterol biosynthesis. Lamisil also has no inhibitory effect on the cytochrome P-450 enzyme system. (Ryder, 1992)

Lamisil possesses a very low minimum inhibitory concentration (MIC) of 0.004 mcg/mL., which is also equivalent to its minimal fungicidal concentration (MFC). It is currently the most active antifungal agent against dermatophytes in-vitro. (Ryder and Leitner, 1998)


Pharmacokinetics and Clinical Efficacy

Lamisil is well absorbed from the gastrointestinal tract, with an oral bioavailability of around 40%. It is extensively bound to plasma proteins and is highly distributed into areas such as the stratum corneum of the skin, the nails, and hair. Lamisil concentrations in keratinous tissues are significantly higher compared to plasma concentrations, and fungicidal concentrations in nails are still found after weeks of stopping therapy. All of these factors contribute to Lamisil’s high efficacy against superficial infections such as onychomycosis. (Sweetman, 2009)

In vitro, Lamisil has been found to exert excellent activity against a great number of dermatophyte species, including Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. The clinical efficacy of Lamisil against dermatophyte infections has also been found to exceed that of the gold standard of therapy, griseofulvin. Thus, it may be recommended as an alternative drug for cases of superficial infections which respond poorly to griseofulvin. Lamisil, however, does not appear to be as effective in the treatment of nondermatophyte infections. (Abdel-Rahman and Nahata, 1997)

In a study by Villars and Jones (1989) of 1200 patients, complete cure has been observed in 70-90% with topical treatment of 1% Lamisil cream for tinea corporis, cutaneous candidiasis, and ptyriasis versicolor. Systemic treatment using oral Lamisil tablets resulted in a 90-100% cure rate for onychomycosis, 75-90% for tinea corporis and tinea pedis, and 60-70% for cutaneous candidiasis. Systemic therapy was found to be ineffective for ptyriasis versicolor. This study also noted a low rate of relapse of dermatophyte infections with Lamisil, a problem that is commonly associated to other antifungals.
Evidence from several studies point to Lamisil as the treatment of choice for dermatophyte onychomycosis and as a first-line treatment option, along with itraconazole, for cutaneous mycoses which require systemic therapy. (McClellan, Wiseman, Markham, et al., 1999)


Adverse Effects

The most common side effects related to the use of Lamisil are gastrointestinal disturbances such as nausea and vomiting, abdominal pain, and diarrhea. A post-marketing study of 10,000 patients using Lamisil reported that a 4.7% incidence of gastrointestinal side effects, followed by a 3.3% incidence of dermatological effects. Other less common side effects were headaches, alterations in taste, and disturbances in liver enzyme levels. Rare but serious adverse effects noted include angioedema, bronchospasm, erythema multiforme, extended stroke, and unilateral leg edema (O’Sullivan, Needham, Bangs, et al., 1996). This result was confirmed by the results from three later studies (O’Sullivan, 1999). Combined data from the 4 studies indicate that adverse effects from Lamisil use occurred in 10.5% of the patients, and serious adverse effects occurred in 0.046% (O’Sullivan, 1999).

Dermatological reactions occasionally associated with Lamisil therapy include skin rashes and urticaria, erythema multiforme, pityriasis, erythroedema, and worsening of pre-existing psoriasis (Gupta, Lynde, Lauzon, et al., 1998). It has also been suggested that patients with a history of auto-immune disease may have a predisposition to develop skin reactions with use of Lamisil (Goeteyn, Naeyaert, Lambert, et al., 2000).


Precautions and Contraindications

Lamisil is contraindicated in patients with pre-existing liver disease. Additionally, all patients planning to start on Lamisil therapy should first undergo liver function tests before initiating oral therapy. Liver enzymes should be periodically monitored in those using Lamisil and therapy should be stopped if any evidence of hepatotoxicity develops. Likewise, Lamisil should be used with caution in patients with psoriasis, and those who develop progressive skin rash during therapy should stop taking the drug. Dosage adjustments should also be observed for patients with renal impairment. As it is excreted in the breast milk, use of Lamisil should also be avoided in breastfeeding mothers. (Sweetman, 2009)
Drug Interactions

Lamisil is metabolized by the cytochrome P450 enzyme system, therefore, drugs that inhibit CYP450, such as cimetidine inhibits the metabolism of Lamisil and increases its plasma concentrations. Likewise, drugs such as rifampicin which induce CYP450 enzymes increase the metabolism of Lamisil, resulting in decreased concentrations in the plasma.

Lamisil has also been shown to inhibit the cytochrome P450 isoenzyme CYP2D6 in vitro. Thus, it may increase plasma concentrations of drugs acted upon by this enzyme system, such as many antidepressants and beta blockers. Breakthrough bleeding has been reported in some patients simultaneously taking Lamisil with oral contraceptives. (Sweetman, 2009)


Bibliography

Abdel-Rahman, S. M., and Nahata, M. C., 1997, Oral terbinafine: a new antifungal agent

Goeteyn, V., Naeyaert, J. M., Lambert, J., et al., 2000, Is systemic autoimmune disease a risk factor for terbinafine-induced erythema multiforme?

Gupta, A. K., Lynde, C. W., Lauzon, G. J., et al., 1998, Cutaneous adverse effects associated with terbinafine therapy: 10 case reports and a review of the literature

McClellan, K. J., Wiseman, L. R., Markham, A., et al., 1999, Terbinafine: an update of its use in superficial mycoses

O’Sullivan, D. P., Needham, C. A., Bangs, A., et al., 1996, Postmarketing surveillance of oral terbinafine in the UK: report of a large cohort study

O’Sullivan, D. P., 1999, Terbinafine: tolerability in general medical practice

Ryder, N. S., and Leitner, I., 1998, In vitro activity of terbinafine; an update

Ryder, N. S., 1992, Terbinafine: Mode of action and properties of the squalene epoxidase inhibition

Br_J_Dermatol_1992_Feb_126(Suppl_39)2-7.pdf
Roberts, D. T., Taylor, W. D., and Boyle, J., 2003, Guidelines for treatment of onychomycosis

Sweetman, S. C. ed., 2009, Martindale, The complete drug reference 36th ed, London: Pharmaceutical Press, 1433

Villars, V., and Jones, T. C., 1989, Clinical efficacy and tolerability of terbinafine (Lamisil)--a new topical and systemic fungicidal drug for treatment of dermatomycoses


 

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