DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Butenafine
Butenafine hydrochloride (MENTAX, LOTRIMIN ULTRA) is a benzylamine
derivative with a mechanism of action similar to that of
terbinafine and naftifine. Its spectrum of antifungal activity and use
also are similar to those of the allylamines.
Polyene Antifungal Antibiotics
Nystatin. Nystatin was discovered in the New York State Health
Laboratory and was named accordingly; it is a tetraene macrolide
produced by Streptomyces noursei, is structurally similar to amphotericin
B, and has the same mechanism of action. The drug is not
absorbed from the GI tract, skin, or vagina. A liposomal formulation
(NYOTRAN) is in clinical trials for candidemia.
Nystatin (MYCOSTATIN, NILSTAT, others) is useful only for candidiasis
and is supplied in preparations intended for cutaneous, vaginal,
or oral administration for this purpose. Infections of the nails
and hyperkeratinized or crusted skin lesions do not respond. Powders
are preferred for moist lesions and are applied two to three times
daily. Creams or ointments are used twice daily. Combinations of
nystatin with antibacterial agents or corticosteroids also are available.
Allergic reactions to nystatin are very uncommon. Although
vaginal tablets of nystatin are well tolerated, imidazoles or triazoles
are more effective agents than nystatin for vaginal candidiasis.
Nystatin suspension is usually effective for oral candidiasis of
the immunocompetent host. Patients should be instructed to swish
the drug around in the mouth and then swallow; otherwise, the
patient may expectorate the bitter liquid and fail to treat the infected
mucosa in the posterior pharynx or esophagus. Other than the bitter
taste and occasional complaints of nausea, adverse effects are
uncommon.
Miscellaneous Antifungal Agents
Undecylenic Acid. Undecylenic acid is 10-undecenoic acid, an
11-carbon unsaturated compound. It is a yellow liquid with a characteristic
rancid odor. It is primarily fungistatic, although fungicidal
activity may be observed with long exposure to high concentrations
of the agent. The drug is active against a variety of fungi, including
those that cause ringworm. Undecylenic acid (DESENEX, others) is
available in a cream, powder, spray powder, soap, and liquid. Zinc
undecylenate is marketed in combination with other ingredients. The
zinc provides an astringent action that aids in the suppression of
inflammation. Compound undecylenic acid ointment contains both
undecylenic acid (~5%) and zinc undecylenate (~20%). Calcium
undecylenate (CALDESENE, CRUEX) is available as a powder.
Undecylenic acid preparations are used in the treatment of
various dermatomycoses, especially tinea pedis. Concentrations of
the acid as high as 10%, as well as those of the acid and salt in the
compound ointment, may be applied to the skin. The preparations as
formulated are usually not irritating to tissue, and sensitization to
them is uncommon. It is of undoubted benefit in retarding fungal
growth in tinea pedis, but the infection frequently persists despite
intensive treatment with preparations of the acid and the zinc salt. At
best, the clinical “cure” rate is ~50%, which is much lower than that
obtained with the imidazoles, haloprogin, or tolnaftate. Efficacy in
the treatment of tinea capitis is marginal, and the drug is no longer
used for that purpose. Undecylenic acid preparations also are
approved for use in the treatment of diaper rash, tinea cruris, and
other minor dermatologic conditions.
Benzoic Acid and Salicylic Acid. An ointment containing benzoic and
salicylic acids is known as Whitfield’s ointment. It combines the
fungistatic action of benzoate with the keratolytic action of salicylate.
It contains benzoic acid and salicylic acid in a ratio of 2:1 (usually
6-3%) and is used mainly in the treatment of tinea pedis.
Because benzoic acid is only fungistatic, eradication of the infection
occurs only after the infected stratum corneum is shed, and continuous
medication is required for several weeks to months. The salicylic
acid accelerates the desquamation. The ointment also is
sometimes used to treat tinea capitis. Mild irritation may occur at
the site of application.
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CHAPTER 57
ANTIFUNGAL AGENTS