| The Butenafine./
La Butenafina. ***********************************
****** DATA-MEDICOS *********
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LA BUTENAFINA / THE BUTENAFINE
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***** DERMAGIC-EXPRESS No 13 ********
****** 04 NOVIEMBRE 1.998 *******
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1.) EDITORIAL
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Amigos de la red, DERMAGIC los saluda de nuevo, hoy una revisión del nuevo antimicótico que la casa Penederm Incorporated liberó al mercado en 1.997.
Se trata de la BUTENAFINA, un producto perteneciente a las benzylaminas, derivado de las alilaminas con alta actividad fungicida. Schering Plough es el encargado de comercializarlo en Canada, nombre comercial MENTAX.
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PRODUCTO:
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Butenafina Hidrocloride al 1 %
Mentax 1% crema (Schering Plough)
Penederm Incorporated
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Hasta una proxima edición de DERMAGIC, amigos de la NET,,,
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DERMAGIC/EXPRESS(13)
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L A B U T E N A F I N A ======================================================================
1.) Treatment of interdigital tinea pedis with a 4-week once-daily regimen
of butenafine hydrochloride 1% cream.
2.) One-week therapy with twice-daily butenafine 1% cream versus vehicle
in the treatment of tinea pedis: a multicenter, double-blind trial.
3.) Butenafine 1% cream in the treatment of tinea cruris: a multicenter,
vehicle-controlled double-blind trial.
4.) Butenafine.
5.) A randomized trial to assess once-daily topical treatment of tinea
corporis with butenafine, a new antifungal agent.
6.) Topical butenafine for tinea pedis.
7.) Update on topical therapy for superficial fungal infections: focus on
butenafine.
8.) Allylamine type xanthone antimycotics.
9.) Butenafine, a fungicidal benzylamine derivative, used once daily for
the treatment of interdigital tinea pedis.
10.) Neutral red assay in minimum fungicidal concentrations of antifungal
agents.
11.) Thiophene congeners of morpholine and allylamine type
antifungals--syntheses and biological activities.
12.) LA BUTENAFINA EN LA WEB: Butenafine HCl Approved as OTC Treatment For
Athlete's Foot In Canada
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1.)Treatment of interdigital tinea pedis with a 4-week once-daily regimen
of butenafine hydrochloride 1% cream.
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Author
Tschen E; Elewski B; Gorsulowsky DC; Pariser DM
Address
Department of Dermatology, University of New Mexico School of
Medicine, Albuquerque,
USA.
Source
J Am Acad Dermatol, 36(2 Pt 1):S9-14 1997 Feb
Abstract
BACKGROUND: Butenafine hydrochloride, a potent new benzylamine with
fungicidal
activity, has been extensively studied and approved for topical use in
Japan. Results reported
here are from one of the first major North American butenafine
clinical trials. OBJECTIVE:
We evaluated butenafine in the treatment of tinea pedis in a
controlled, randomized,
double-blind trial. METHODS: Of 80 patients with positive fungal
cultures, 40 applied
butenafine 1% cream and 40 applied vehicle to the affected area once
daily for 4 weeks.
Efficacy was assessed during treatment and 4 weeks after. RESULTS:
Significantly more
patients using butenafine than using vehicle had mycologic cure
(butenafine, 88%; vehicle,
33%) and effective clinical response (butenafine, 78%; vehicle, 35%).
Differences between
treatment groups were greatest (p < 0.001) 4 weeks after treatment.
CONCLUSION:
Butenafine applied once daily for 4 weeks resulted in an effective
clinical response and
mycologic cure of tinea pedis during treatment. Patients continued to
improve for at least 4
weeks after treatment.
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2.) One-week therapy with twice-daily butenafine 1% cream versus vehicle
in the treatment of tinea pedis: a multicenter, double-blind trial.
======================================================================
Author
Savin R; De Villez RL; Elewski B; Hong S; Jones T; Lowe N; Lucky A;
Reyes B; Stewart
D; Willis I
Address
Department of Dermatology, Yale University School of Medicine, New
Haven, CT, USA.
Source
J Am Acad Dermatol, 36(2 Pt 1):S15-9 1997 Feb
Abstract
BACKGROUND: Butenafine hydrochloride, a benzylamine derivative with
potent
antifungal activity, has been used in Japan to treat superficial
fungal diseases. OBJECTIVE:
We evaluated the safety and efficacy of twice-daily butenafine versus
its vehicle in the
treatment of interdigital tinea pedis in a multicenter, randomized,
double-blind, parallel-group
trial. METHODS: A total of 402 patients with interdigital tinea pedis
and a positive potassium
hydroxide examination were enrolled. Of the 271 patients who had
culture-confirmed tinea
pedis and were assessed for efficacy, 132 applied butenafine and 139
applied vehicle twice
daily for 1 week. Patients were assessed for mycologic cure, effective
treatment, overall cure,
and mycologic/clinical cure. RESULTS: The rates of all four end points
were significantly
higher with butenafine than with vehicle 5 weeks after treatment
ended. Rates of mycologic
cure and effective treatment with butenafine were significantly higher
than with vehicle at
cessation of treatment. Adverse events to treatment occurred in less
than 1% of patients
treated with butenafine and 2% of patients who applied vehicle.
CONCLUSION:
Butenafine applied twice daily for 1 week is highly effective in
treating interdigital tinea
pedis.
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3.) Butenafine 1% cream in the treatment of tinea cruris: a multicenter,
vehicle-controlled double-blind trial.
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Author
Lesher JL Jr; Babel DE; Stewart DM; Jones TM; Kaminester L; Goldman M;
Weintraub JS
Address
Department of Medicine, Medical College of Georgia, Augusta
30912-3190, USA.
Source
J Am Acad Dermatol, 36(2 Pt 1):S20-4 1997 Feb
Abstract
BACKGROUND: Butenafine hydrochloride, a potent antifungal agent
related to the
allylamines, has been used in Japan for treating various cutaneous
mycoses including tinea
cruris. OBJECTIVE: We compared the safety and efficacy of butenafine
hydrochloride and
its vehicle when used once daily for 2 weeks to treat tinea cruris.
METHODS: Patients (n =
93) with tinea cruris and a positive potassium hydroxide examination
and mycologic culture
were enrolled. Of the 76 patients assessed for efficacy, 37 applied
butenafine and 39 applied
vehicle once daily for 2 weeks. Assessments were made at the end of
the 2-week treatment
period and 4 weeks after the end of treatment. RESULTS: Patients in
the butenafine group
had a higher mycologic cure rate by day 7 (66% vs 13%, p < 0.0001),
with marked
improvement 4 weeks after the end of treatment (81% vs 13%, p <
0.0001). They also had
a higher rate of effective treatment at day 7 (29% vs 5%, p < 0.01)
and at 4 weeks after
treatment (73% vs 5%, p < 0.0001). Adverse events definitely related
to butenafine
treatment were limited to one case of burning sensation after
application. CONCLUSION:
Butenafine applied once daily for 2 weeks is effective in treating
tinea cruris. The
proportion of patients cured increased between the end of treatment
and 4 weeks after
treatment.
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4.) Butenafine.
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Author
McNeely W; Spencer CM
Address
Adis International Limited, Auckland, New Zealand. [email protected]
Source
Drugs, 55(3):405-12; discussion 413 1998 Mar
Abstract
Butenafine is a new antifungal agent with primary fungicidal activity
against dermatophytes
such as Trichophyton mentagrophytes, Microsporum canis and
Trichophyton rubrum which
cause tinea infections. 14C-labelled butenafine (approximately 30
micrograms/g tissue) was
found within guinea-pig dorsal skin 24 hours after topical
application. Most of the drug was
distributed into the epidermis including the horny layer. Small
amounts were found in the
dermis, probably transported via sebaceous glands and hair follicles.
In vitro, the minimum
concentration that completely inhibited growth of dermatophytes (MIC)
and the minimum
fungicidal concentrations (MFC) for butenafine against T.
mentagrophytes and M. canis
were similar (0.012 to 0.05 mg/L) and were 4 to 130 times lower than
those for naftifine,
tolnaftate, clotrimazole and bifonazole. It also has greater activity
against T. rubrum, M.
gypseum and Epidermophyton floccosum when compared with naftifine,
tolnaftate and
clotrimazole; comparisons with bifonazole against these strains were
not available.
Assessment after 1 week's treatment in patients with tinea pedis
revealed that mycological
cure rates were greater in those who received twice-daily butenafine
for 1 week or
once-daily butenafine for 4 weeks than in placebo recipients.
Mycological and overall cure
rates were either further increased or maintained up to 5 weeks after
treatment cessation
compared with end-of-treatment values. In patients with tinea cruris
or tinea corporis who
received once-daily butenafine 1% for 2 weeks, the mycological and
overall cure rates
continued to increase for up to 4 weeks after treatment cessation.
=====================================================================
5.) A randomized trial to assess once-daily topical treatment of tinea
corporis with butenafine, a new antifungal agent.
=====================================================================
Author
Greer DL; Weiss J; Rodriguez DA; Hebert AA; Swinehart JM
Address
Department of Dermatology, Louisiana State University Medical Center,
New Orleans
70112, USA.
Source
J Am Acad Dermatol, 37(2 Pt 1):231-5 1997 Aug
Abstract
BACKGROUND: Tinea corporis treatment usually requires topical
application of an
antifungal agent for 2 to 3 weeks. OBJECTIVE: We evaluated short-term
treatment of tinea
corporis with butenafine hydrochloride, a new benzylamine with in
vitro fungicidal activity.
METHODS: Patients (n = 78) were randomly selected to apply butenafine
or its cream
vehicle alone once daily for 14 days and were periodically assessed
until day 42. RESULTS:
Butenafine recipients had significantly higher rates of mycologic cure
beginning at day 7
(64% vs 9%) with continued improvements through day 42 (88% vs 17%).
They also had
higher rates of effective treatment (mycologic cure and 90% to 100%
symptom
improvement) at day 7 (33% vs 0%) with increasing rates through day 42
(81% vs 14%).
CONCLUSION: Butenafine provides rapid and persistent antifungal
activity and symptom
relief in patients with tinea corporis. Significant effects were
observed within 7 days of
therapy initiation, and increasing effectiveness was observed 4 weeks
after therapy.
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6.) Topical butenafine for tinea pedis.
Source
Med Lett Drugs Ther, 39(1004):63-4 1997 Jul 4
=====================================================================
=====================================================================
7.) Update on topical therapy for superficial fungal infections: focus on
butenafine.
=====================================================================
Author
Odom RB
Address
University of California at San Francisco, USA.
Source
J Am Acad Dermatol, 36(2 Pt 1):S1-2 1997 Feb
=====================================================================
8.) Allylamine type xanthone antimycotics.
=====================================================================
Author
Salmoiraghi I; Rossi M; Valenti P; Da Re P
Address
Institute of Pharmaceutical Chemistry, University of Milan, Italy.
Source
Arch Pharm (Weinheim), 331(6):225-7 1998 Jun
Abstract
A number of xanthone derivatives bearing the basic chain of naftifine
and butenafine
antimycotics in 1, 2, 3, and 4 nuclear positions are described. The in
vitro antifungal activity
against representative strains of molds and yeasts is reported. Only
butenafine xanthone
analogues show significant activity against Cryptococcus neoformans,
in particular the
regioisomer 4d (1.5 micrograms/ml).
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9.) Butenafine, a fungicidal benzylamine derivative, used once daily for
the treatment of interdigital tinea pedis.
=====================================================================
Author
Reyes BA; Beutner KR; Cullen SI; Rosen T; Shupack JL; Weinstein MB
Address
International Dermatology Research, Inc. Miami, Florida, USA.
Source
Int J Dermatol, 37(6):450-3 1998 Jun
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10.) Neutral red assay in minimum fungicidal concentrations of antifungal
agents.
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Author
Fukuda T; Naka W; Tajima S; Nishikawa T
Address
Department of Dermatology, Keio University School of Medicine, Tokyo,
Japan.
Source
J Med Vet Mycol, 34(5):353-6 1996 Sep-Oct
Abstract
We assayed the fungicidal effects of antifungal agents using neutral
red staining. Fungal
elements of Trichophyton mentagrophytes and T. rubrum were treated
with various
concentrations of antifungal agents in 96-well filtration plates and
then stained with neutral
red. The amount of neutral red incorporated by the surviving viable
cells was determined
from the automated spectrophotometric readings at 550 nm. The minimum
fungicidal
concentrations (MFCs) of antifungal agents determined by this assay
correlated well with
those determined by conventional assay. This newly developed procedure
should provide a
rapid, reproducible, quantitative, qualitative and semi-automated
susceptibility test for
determination of the MFCs of the fungicidal agents.
Title
An overview of topical antifungal therapy in dermatomycoses. A North
American
perspective.
Author
Gupta AK; Einarson TR; Summerbell RC; Shear NH
Address
Department of Medicine, Sunnybrook Health Science Center, Toronto,
Ontario, Canada.
[email protected]
Source
Drugs, 55(5):645-74 1998 May
Abstract
Dermatophytes cause fungal infections of keratinised tissues, e.g.
skin, hair and nails. The
organisms belong to 3 genera, Trichophyton, Epidermophyton and
Microsporum.
Dermatophytes may be grouped into 3 categories based on host
preference and natural
habitat. Anthropophilic species predominantly infect humans, geophilic
species are soil based
and may infect both humans and animals, zoophilic species generally
infect non-human
mammals. It is important to confirm mycologically the clinical
diagnosis of onychomycosis and
other tinea infections prior to commencing therapy. The identity of
the fungal organism may
provide guidance about the appropriateness of a given topical
antifungal agent. Special
techniques may be required to obtain the best yield of fungal
organisms from a given site,
especially the scalp and nails. It is also important to realise the
limitations of certain diagnostic
aids e.g., Wood's light examination is positive in tinea capitis due
to M. canis and M.
audouinii (ectothrix organisms); however, Wood's light examination is
negative in T. tonsurans
(endothrix organism). Similarly, it is important to be aware that
cicloheximide in culture
medium will inhibit growth of non-dermatophytes. Appropriate media are
therefore required
to evaluate the growth of some significant non-dermatophyte moulds.
For tinea infections
other than tinea capitis and tinea unguium, topical antifungals may be
considered. For
effective therapy of tinea capitis an oral antifungal is generally
necessary. Similarly, oral
antifungals are the therapy of choice, especially if onychomycosis is
moderate to severe.
Furthermore, where the tinea infection involves a large area, in an
immunocompromised host
or if infection is recurrent with poor response to topical agents,
then oral antifungal therapy
may be necessary. Topical antifungal agents may be broadly divided
into specific and
nonspecific agents. The former group includes the polyenes, azoles,
allylamines, amorolfine,
ciclopirox and butenafine. Generally the topical agent is available as
a cream, sometimes for
use intravaginally. Less commonly, the formulation may be in the form
of a powder, lacquer,
spray, gel or solution. Many of these agents have a broad spectrum of
activity, being effective
against dermatophytes, yeasts and Malassezia furfur. For the treatment
of tinea corporis,
tinea cruris tinea versicolor and cutaneous candidosis, once or twice
daily application may be
required, the most common duration of therapy being 2 to 4 weeks. For
tinea pedis the most
common treatment duration is 4 to 6 weeks.
=====================================================================
11.) Thiophene congeners of morpholine and allylamine type
antifungals--syntheses and biological activities.
=====================================================================
Author
Bracher F; Papke T
Address
Institut f¨ur Pharmazeutische Chemie, Technische Universit¨at
Braunschweig.
Source
Pharmazie, 50(8):525-7 1995 Aug
Abstract
A thiophene analogue 8 of the antifungal drug amorolfine (1) was
prepared starting from the
alcohol 5. In addition, congeners of naftifine, terbinafine and
butenafine, in which the
naphthalene ring is replaced by a branched thienylalkyl group, wee
synthesized. Of the four
drug analogues only compound 9, related to terbinafine, showed
significant antifungal activity.
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12.) Butenafine HCl Approved as OTC Treatment For
Athlete's Foot In Canada
=====================================================================
FOSTER CITY, Calif. -- May 8, 1997 -- Penederm Incorporated today
announced that its topical antifungal compound, butenafine HCl 1% cream, has
received regulatory approval as an over-the-counter (OTC) tinea pedis
(athlete's foot) medication from the Health Protection Branch of Health
Canada.
Butenafine HCl was recently approved by the United States Food and Drug
Administration as a prescription drug for three indications, tinea pedis
(athlete'sfoot), tinea corporis (ringworm), and tinea cruris (groin
fungus), and is being marketed under the trade name Mentax(tm)
(butenafine HCl cream) cream 1% in the United States.
Schering-Plough Healthcare, Products Inc.will market the butenafine cream in
Canada under its own brand names.
"This is the first OTC approval of our lead topical antifungal," stated
Lloyd H. Malchow, President and CEO of Penederm. "We launched Mentax
in the US
market early in 1997, along with our co-promotion partner, Schering-Plough
Healthcare, Inc. Five papers in the February Journal of the American
Academy of Dermatology were recently published in conjunction with our
product launch, thereby making available the excellent comprehensive clinical
data for this product."
Malchow went on to say, "We believe that the strong brand franchise
Schering-Plough Corporation's subsidiaries hold in OTC antifungals make them
an excellent marketing partner for this product."
Butenafine is the first of a new class of antifungal agents known as the
benzylamines, which are chemically and pharmacologically related to the
allylamine antifungal drugs. Japan-based Kaken Pharmaceutical Co., Ltd.,
developed the active compound and markets the drug in Japan, where it has
become one of the leading topical antifungals. Penederm acquired exclusive
rights to the active compound in Mentax in North, Central and South America
for topical use against skin and nail fungus.
Penederm Incorporated is a specialty pharmaceutical company located in
Foster City, California, which focuses on the commercialization of dermatology
products.
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DATA-MEDICOS/DERMAGIC-EXPRESS No (13) 04/11/98 DR. JOSE LAPENTA R.
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Dr. Jose Lapenta R.
Maracay, Venezuela
[email protected]
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