TIOCONAZOL
DESCRIPCION Tioconazole is an imidazole antifungal agent available for intravaginal use. Tioconazole is fungicidal against Candida sp. and is used to treat vulvovaginal candidiasis. It is the only topical antifungal agent approved in the US as a single-dose treatment for vulvovaginal candidiasis. A single intravaginal dose of tioconazole is as effective as a 3 day course of terconazole.[1743] Tioconazole was approved by the FDA in 1983 and was originally available only as a prescription product. In 1996, tioconazole was reclassified as a nonprescription drug. Mechanism of Action: Tioconazole exerts its effect by disrupting normal fungal cell membrane permeability. Ergosterol is an essential component of the fungal cell membrane. Tioconazole inhibits ergosterol synthesis by interacting with 14-alpha demethylase, a cytochrome P-450 enzyme necessary for converting lanosterol to ergosterol. Inhibition of ergosterol synthesis results in increased cellular permeability, causing leakage of cellular contents such as phosphorous-containing compounds and potassium. Tioconazole has documented in vitro activity against both albicans and non-albicans Candida species, including C. albicans, C. glabrata, C. krusei, C. parapsilosis, C. pseudotropicalis, and C. tropicalis. Pharmacokinetics: Tioconazole is administered intravaginally. One dose (applicatorful) of tioconazole 6.5% provides 3 days of in vitro antifungal activity, with vaginal concentrations maintained above the MIC. Systemic absorption after a single intravaginal application in nonpregnant women is negligible. Indications...Dosage The following organisms are generally considered susceptible to tioconazole in vitro: Candida albicans; Candida glabrata; Candida krusei; Candida parapsilosis; Candida pseudotropicalis; and Candida tropicalis. For the treatment of vulvovaginal candidiasis: Intravaginal dosage (6.5% vaginal ointment): Adults and adolescents: For self-medication, insert 1 applicatorful (about 4.6 g) PV before bedtime as a single dose. Although Vagistat�-1 is a single-dose treatment, most women experience relief of symptoms within 7 days. If symptoms do not improve in three days or remain after seven days, a physician should be consulted. Patients with renal impairment: No dosage adjustment needed. Intravaginal Administration �Tioconazole is usually administered at bedtime as a single-dose treatment. CONTRAINDICACIONES Patients should not self-medicate with tioconazole in the presence of abdominal pain, fever higher than 100 degrees F, chills, vomiting, diarrhea, or foul smelling vaginal discharge. Use of tioconazole is not recommended during pregnancy (pregnancy category C). There are no adequate and well-controlled studies in pregnant women. Tioconazole did not adversely affect fetal viability or growth when administered orally to pregnant rats at doses up to 165 mg/kg/day during the period of organogenesis. However, tioconazole can cause dystocia in rats when treatment is extended through parturition; effects include prolongation of pregnancy, in utero deaths, and impaired pup survival. These effects are only observed with oral doses exceeding 20 mg/kg/day and intravaginal doses greater than 9 mg/kg/day. The single-dose treatment regimen of tioconazole is also a reason its use is not recommended in pregnant women. According to CDC guidelines, many experts recommend 7 days of therapy with a topical azole preparation for the treatment of vulvovaginal candidiasis that occurs during pregnancy. It is not known if tioconazole is excreted in human milk. Because of the potential for adverse effects of tioconazole in nursing infants, breast-feeding should be temporarily discontinued while tioconazole is administered. Tioconazole single-dose treatment for vulvovaginal candidiasis should not be used in women with human immunodeficiency virus (HIV) infection since efficacy has not been established in this patient population. Tioconazole (Vagistat�-1) is available without a prescription for self-medication. Although Vagistat�-1 is a single-dose treatment, most women experience relief of symptoms within 7 days. If symptoms do not improve in three days or remain after seven days, a physician should be consulted. A physician should also be consulted if initial treatment is effective but symptoms recur within 2 months. Recurring yeast infections may be a sign of pregnancy or a serious condition such as AIDS or diabetes. Tioconazole should not be used in patients with a history of azole hypersensitivity. The ointment base in Vagistat�-1 may interact with contraceptive devices containing rubber or latex such as condoms or vaginal contraceptive diaphragms. Patients should avoid using condoms or vaginal contraceptive diaphragms for 3 days following treatment with tioconazole. Safe and effective use of tioconazole has not been established in children less than 12 years of age. INTERACCIONES The spermicides nonoxynol-9 and octoxynol should not be administered concurrently with butoconazole, clotrimazole, econazole, miconazole, terconazole, or tioconazole intravaginal preparations. These intravaginal azole antifungals may inactivate the spermicides, leading to contraceptive failure. Also, the base ingredients of some of these azole intravaginal creams and suppositories may interact with the latex of contraceptive devices used concurrently with the spermicides, leading to breakdown of the physical barrier. Conversely, it is possible that spermicides may cause decreased effectiveness of these azole antifungals. Studies have shown that concurrent use of oral contraceptives does not affect the cure rate of tioconazole vaginal ointment. REACCIONES ADVERSAS According to the manufacturer, vaginal irritation and/or burning have been reported in 1.9�6% of patients treated with single-dose tioconazole vaginal ointment. This incidence is similar to that reported in patients treated with miconazole vaginal cream (2.4%). However, in one study of patients with vulvovaginal candidiasis, women receiving a single dose of tioconazole vaginal ointment experienced more local irritation or pruritus (30%) than patients treated with a 3-day course of 100 mg clotrimazole vaginal tablets (5%).[1744] Other adverse reactions reported in less than 1% of patients treated with tioconazole include vaginal discharge, vulvar edema and swelling, vaginal pain, dysuria, nocturia, dyspareunia, and dryness of vaginal secretions. Several cases of contact dermatitis associated with topical tioconazole have been reported in the literature. No long-term studies in animals have been conducted to evaluate the carcinogenic potential of tioconazole. When evaluated in vitro, tioconazole did not demonstrate mutagenic activity at the chromosomal or subchromosomal level. PRESENTACION Tioconazole Vagistat� |
REFERENCIAS
|