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Manufacturer
TARO PHARM USA
SKU
51672130200

terconazole 0.8% cream

Generic
$58.66 / tube/kit
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Uses

Vulvovaginal Candidiasis

Uncomplicated Vulvovaginal Candidiasis

Terconazole is used intravaginally for the treatment of vulvovaginal candidiasis. Prior to initial use of miconazole in a woman who has signs and symptoms of uncomplicated vulvovaginal candidiasis, the diagnosis should be confirmed either by demonstrating yeast or pseudohyphae with direct microscopic examination of vaginal discharge (saline or 10% potassium hydroxide [KOH] wet mount or Gram stain) or by culture; identifying Candida by culture in the absence of symptoms is not an indication for antifungal treatment since approximately 10-20% of women harbor Candida or other yeasts in the vagina. When an adequate response is not achieved following a course of terconazole therapy for vulvovaginal candidiasis or if there is recurrence of symptoms within 2 months, appropriate microbiologic studies should be performed to confirm the diagnosis and identify unusual Candida species (e.g., C. glabrata).

Up to 75% of women reportedly have at least one episode of vulvovaginal candidiasis and 40-45% have 2 or more episodes during their lifetime, but a small percentage of women (up to 5%) have recurrent vulvovaginal candidiasis (i.e., 4 or more episodes of symptomatic vulvovaginal candidiasis in a year). While certain factors may precipitate a sporadic attack of vulvovaginal candidiasis and have been associated with an increased risk for recurrent vulvovaginal candidiasis (e.g., uncontrolled diabetes mellitus, pregnancy, oral contraceptive use, corticosteroid or other immunosuppressive therapy, immunodeficiency, use of intravaginal sponges or devices, repeated courses of topical or systemic antibacterial agents), these factors are not present in most women who have recurrent episodes.

Azole antifungals (imidazole and triazole derivatives) are considered the drugs of choice for the treatment of vulvovaginal candidiasis. The US Centers for Disease Control and Prevention (CDC) and other clinicians generally recommend that uncomplicated vulvovaginal candidiasis (defined as vulvovaginal candidiasis that is mild to moderate, sporadic or infrequent, most likely caused by Candida albicans, and occurring in immunocompetent women) should be treated with an intravaginal azole antifungal (e.g., butoconazole, clotrimazole, miconazole, terconazole, tioconazole) given in appropriate single-dose or short-course regimens or, alternatively, oral fluconazole given in a single-dose regimen. These regimens generally have been associated with clinical and mycologic cure rates of 80-90% in otherwise healthy, nonpregnant women with uncomplicated infections, and there is no clear evidence that any one intravaginal azole antifungal regimen is superior to any other intravaginal azole regimen available for the treatment of these infections. While intravaginal nystatin also can be used for the treatment of uncomplicated vulvovaginal candidiasis, it generally is less effective than intravaginal azole antifungals. A longer duration of therapy (i.e., 7-14 days) with an intravaginal or oral azole antifungal generally is necessary for the treatment of complicated vulvovaginal candidiasis, including recurrent and severe disease. Complicated vulvovaginal candidiasis is defined as infections that are recurrent or severe, caused by Candida other than C. albicans, or occurring in women who have underlying medical conditions such as pregnancy, uncontrolled diabetes, debilitation, or immunosuppression.(See Complicated and Recurrent Vulvovaginal Candidiasis under Uses: Vulvovaginal Candidiasis.)

Vulvovaginal candidiasis usually is not acquired through sexual activity, and treatment of sexual partner(s) is not recommended but may be considered in women who have recurrent infections. However, male sexual partners who have symptomatic balanitis or penile dermatitis may benefit from treatment with a topical antifungal to relieve symptoms.

Clinical Experience

Terconazole given once daily for 7 days as a 0.4% vaginal cream or once daily for 3 days as a 0.8% vaginal cream or as 80-mg vaginal suppositories produces clinical cures (i.e., complete absence of vulvovaginal burning, itching, swelling, erythema, excoriation, and/or ulceration and substantial decreases in vaginal discharge) in approximately 84-96% and mycologic cures in 79-97% of nonpregnant and pregnant patients with vulvovaginal candidiasis 7 days after completion of therapy. The relapse rate 3-4 weeks after therapy is 3-15%.

Terconazole has been used with good results in women with vulvovaginal candidiasis during oral contraceptive use. Although oral contraceptive use has been associated with an increased incidence of vulvovaginal candidiasis and frequently recurring infection, cure rates reported with terconazole in patients using oral contraceptive agents concomitantly do not differ substantially from those in women using other methods of contraception or not practicing contraception. Because vulvovaginal candidiasis may be more difficult to cure during pregnancy, many experts prefer the use of 7-day regimens in pregnant patients. However, terconazole has been used with good results in pregnant women when given as a 3-day regimen using 80-mg vaginal suppositories or as a 7-day regimen using the 0.4% vaginal cream.

Intravaginal terconazole appears to be at least as effective as intravaginal clotrimazole or miconazole in the treatment of vulvovaginal candidiasis. In several studies, 7 days of therapy with terconazole 0.4% vaginal cream given once daily or 3 days of therapy with terconazole 80-mg vaginal suppositories given once daily was as effective as 3 days of therapy with clotrimazole 200-mg vaginal tablets given once daily. In studies in pregnant and nonpregnant women who received 7 days of therapy with terconazole 0.4% vaginal cream or clotrimazole 1% vaginal cream, mycologic cure rates 1 week after therapy were 90-94.6 and 84.4-95%, respectively, and relapse rates 4 weeks later were 3.3 and 16.7%, respectively. In controlled studies comparing terconazole 0.4% vaginal cream and miconazole 2% vaginal cream applied once daily for 7 days, clinical cure rates 7-10 days after therapy were 92 and 91%, respectively, and mycologic cure rates were 86 and 83%, respectively.

Complicated and Recurrent Vulvovaginal Candidiasis

Optimum regimens for the treatment of recurrent vulvovaginal candidiasis (usually defined as 4 or more episodes of symptomatic vulvovaginal candidiasis in a year) have not been established. Although each individual episode caused by C. albicans may respond to usual short-course intravaginal antifungal regimens or a single-dose of oral fluconazole, a longer duration of initial therapy may be necessary to achieve mycologic remission and chronic maintenance therapy may be necessary to prevent relapse. The CDC recommends use of an initial intensive regimen consisting of 7-14 days of an intravaginal azole antifungal or a 3-dose regimen of oral fluconazole (100-, 150-, or 200-mg doses given every third day for a total of 3 doses) followed by a maintenance antifungal regimen (given for 6 months). For the maintenance regimen, the CDC recommends oral fluconazole (100-, 150-, or 200-mg doses once weekly). If this oral regimen cannot be used, some clinicians recommend intravaginal clotrimazole (200 mg twice weekly or 500 mg once weekly) or other intravaginal treatments used intermittently. These maintenance regimens can be effective in reducing recurrent infections; however, 30-50% of women will have recurrent disease once maintenance therapy is discontinued.

The response rate to short-course antifungal regimens is lower in patients with severe vulvovaginal candidiasis (i.e., extensive vulvar erythema, edema, excoriation, and fissure formation) and either a 2-dose regimen of oral fluconazole (150 mg repeated 3 days later) or 7-14 days therapy with an intravaginal azole antifungal is recommended for these infections. These more prolonged regimens may also be necessary for the treatment of vulvovaginal candidiasis in women with underlying debilitating medical conditions (e.g., those with uncontrolled diabetes or those receiving corticosteroid therapy).

For the treatment of vulvovaginal candidiasis during pregnancy, the CDC recommends use of a 7-day regimen of an intravaginal azole antifungal.

Vulvovaginal candidiasis may occur more frequently and may be more severe in women with human immunodeficiency virus (HIV) infection than in women without HIV infection and these infections have been recognized as an early manifestation of acquired immunodeficiency syndrome (AIDS) in women. While optimum therapy for recurrent vulvovaginal candidiasis in HIV-infected women has not been established, there is no evidence to date that these women have a lower response rate to the intravaginal or oral antifungal regimens usually recommended for the treatment of vulvovaginal candidiasis. Therefore, the CDC and other clinicians recommend that treatment of vulvovaginal candidiasis in HIV-infected women be the same as that in women without HIV infection.

Recurrent vulvovaginal candidiasis rarely may be caused by resistant strains of C. albicans or, more commonly, by other Candida with reduced susceptibility to azole antifungals (e.g., C. glabrata). It has been suggested that repeated treatment of recurrent vulvovaginal candidiasis with intravaginal azole antifungals and widespread and/or injudicious use of these agents for self-medication of vulvovaginal candidiasis may favor the selection of Candida resistant to azole antifungals. Optimum therapy for the treatment of vulvovaginal candidiasis caused by Candida with reduced susceptibility to azole antifungals has not been determined to date. For the treatment of vulvovaginal candidiasis caused by Candida other than C. albicans, the CDC and other clinicians recommend 7-14 days of therapy with an antifungal agent other than fluconazole; if recurrence occurs, a 14-day regimen of intravaginal boric acid (not commercially available in the US) is recommended. Referral to a specialist is advised.

Dosage and Administration

Administration

Terconazole is administered intravaginally as a cream or suppository.

Dosage

Uncomplicated Vulvovaginal Candidiasis

Vaginal Cream

For the treatment of vulvovaginal candidiasis, one applicatorful of terconazole 0.4% cream is administered intravaginally once daily at bedtime for 7 consecutive days or, alternatively, one applicatorful of terconazole 0.8% cream is administered intravaginally once daily at bedtime for 3 consecutive days.

Vaginal Suppositories

For the treatment of vulvovaginal candidiasis, one vaginal suppository containing 80 mg of terconazole is administered intravaginally once daily at bedtime for 3 consecutive days.

Single-dose regimens using a vaginal suppository containing 180- or 240-mg of terconazole (not commercially available in the US) also have been used for the treatment of vulvovaginal candidiasis.

Complicated Vulvovaginal Candidiasis

For the treatment of recurrent vulvovaginal candidiasis caused by Candida albicans, the CDC and other clinicians recommend an initial intensive regimen (7-14 days of an intravaginal azole or 3-dose regimen of oral fluconazole) to achieve mycologic remission, followed by an appropriate maintenance regimen (6-month regimen of once-weekly oral fluconazole or, alternatively, an intravaginal azole given intermittently).

For the treatment of vulvovaginal candidiasis that is severe, caused by Candida other than C. albicans, or occurring in women with underlying medical conditions, the CDC and other clinicians recommend 7-14 days of an intravaginal azole.

HIV-infected Individuals

HIV-infected patients with vulvovaginal candidiasis generally should receive the same regimen recommended for other patients. Some experts recommend a treatment duration of 3-7 days for uncomplicated infections in such patients.

Although a maintenance regimen of an intravaginal azole can be considered for those with recurrent episodes,routine primary or secondary prophylaxis (long-term suppressive or chronic maintenance therapy) is not usually recommended.

Cautions

Adverse Effects

Terconazole for intravaginal use generally is well tolerated, and adverse effects have required discontinuance of the drug in about 2-4% of patients.

Vulvovaginal burning, pruritus, or irritation have occurred in about 2-5% of patients receiving terconazole 0.4 or 0.8% vaginal cream and in up to 15% of patients receiving terconazole 80-mg vaginal suppositories during clinical studies. Vulvovaginal itching was the adverse effect most frequently requiring discontinuance of terconazole 0.4 or 0.8% vaginal cream. Burning and itching were the adverse effects most frequently requiring discontinuance of terconazole vaginal suppositories.

Headache has been reported in 21-30% of patients receiving terconazole vaginal suppositories or 0.4 or 0.8% cream; this adverse effect was reported in 16-21% of patients receiving placebo. Body pain and pain of the female genitalia occurred in 2-4% of patients receiving intravaginal terconazole suppositories or 0.4% cream.Abdominal pain and dysmenorrhea have been reported in 3.4-6% of patients receiving terconazole 0.8% vaginal cream.

Fever has occurred in 1.7 or 2.8% and chills in 0.4 or 1.8% of patients receiving terconazole 0.4% vaginal cream or 80-mg vaginal suppositories, respectively, and these effects occurred more frequently than in patients receiving placebo. Fever has been reported in 1% of patients receiving terconazole 0.8% vaginal cream. A flu-like syndrome, characterized by fever, chills, headache, and/or hypotension and occasionally by vertigo and nausea, has occurred in some patients receiving vaginal terconazole. It has been suggested that the reaction may be immunoallergenic in nature, or it may be similar to the Jarisch-Herxheimer reaction observed during penicillin therapy for syphilis, being elicited in this case as a reaction to the dying fungi.

Studies in healthy adults using topical application to the skin of various formulations of terconazole cream indicate that the drug has a low potential for contact sensitization. However, photosensitivity reactions did occur in healthy adults following exposure to filtered artificial ultraviolet light after repeated application to the skin of 0.8 or 2% terconazole cream. Photosensitivity reactions have not been reported in clinical studies to date following intravaginal administration of the drug as a 0.4 or 0.8% cream or as 80-mg suppositories.

Precautions and Contraindications

Terconazole vaginal suppositories or 0.4 or 0.8% cream are contraindicated in patients with known hypersensitivity to the drug or any ingredient in the respective formulation.

Patients should be advised against interrupting or discontinuing terconazole therapy during a prescribed regimen, even during menstruation or in response to symptomatic relief. If irritation, sensitization, fever, chills, or flu-like symptoms occur during terconazole therapy and appear to be drug related, the drug should be discontinued and not reinstituted. Appropriate microbiologic studies (e.g., potassium hydroxide smear and/or culture) should be performed to confirm the diagnosis and rule out infection caused by nonsusceptible pathogens if an adequate response is not achieved following a course of terconazole therapy.

The hydrogenated vegetable oil base contained in terconazole vaginal suppositories may interact with certain rubber or latex products such as vaginal contraceptive diaphragms, and concurrent use is not recommended; use of terconazole vaginal cream should be considered as an alternative to the suppositories in such situations.

Pediatric Precautions

Safety and efficacy of terconazole in children younger than 18 years of age have not been established.

Geriatric Precautions

Data are insufficient from clinical studies to determine whether patients 65 years of age or older respond differently than younger adults. Other clinical experience to date has not identified age-related differences in response.

Mutagenicity and Carcinogenicity

Terconazole was not mutagenic when tested in vitro for induction of microbial point mutations in the Salmonella mutagen (Ames) test with metabolic activation or for induction of cellular transformation. There was no evidence of mutagenicity when the drug was tested in vivo for chromosome breaks in the micronucleus test or for dominant lethal mutations in mouse germ cells.

The carcinogenic potential of terconazole has not been evaluated to date.

Pregnancy, Fertility, and Lactation

Pregnancy

Reproduction studies in rats using oral terconazole dosages up to 40 mg/kg daily (up to 100 times the usual recommended vaginal human dose of the 0.4% vaginal cream) or in rabbits using oral dosages up to 20 mg/kg daily have not revealed evidence of teratogenicity. In addition, there was no evidence of teratogenicity when the drug was given subcutaneously to rats in dosages up to 20 mg/kg daily. However, there was some evidence of embryotoxicity in rats and rabbits that received the drug in an oral dosage of 20-40 mg/kg daily prior to mating and throughout gestation. At this dosage in rats, there was a decreased litter size and number of viable young, reduced fetal weight, delayed ossification, and an increased incidence of skeletal variants. Terconazole does not appear to affect parturition in animals since there was no evidence of prolonged gestation or dystocia. There generally was no evidence of embryotoxicity at dosages of 10 mg/kg daily or less; however, there was a delay in fetal ossification in rats that received 10 mg/kg daily. In pregnant rats, oral administration of terconazole in a dosage 10 mg/kg daily results in mean peak plasma concentrations of 176 ng/mL which is 44 times greater than mean peak plasma concentration (4 ng/mL) attained in healthy adults following intravaginal administration of the 0.4% cream.

There are no adequate and controlled studies to date using intravaginal terconazole in women during the first trimester of pregnancy. The drug has been used intravaginally during the second and third trimester of pregnancy in at least 100 women without adverse effects on the outcome of pregnancy. However, because small amounts of terconazole are absorbed from the vagina, the manufacturer states that terconazole should be used during the first trimester of pregnancy only when considered essential to the welfare of the patient. The CDC and others state that a 7-day regimen of an intravaginal azole antifungal can be used, if necessary, for the treatment of vulvovaginal candidiasis in pregnant women.

Fertility

It is not known whether terconazole affects fertility in humans. Studies in male and female rats using oral terconazole dosages up to 40 mg/kg daily have not revealed evidence of impaired fertility; however, weight loss did occur in both sexes of adult rats.

Lactation

It is not known whether terconazole is distributed into human milk; however, the drug is distributed into milk in rats. In a study in lactating rats receiving oral terconazole in a dosage of 40 mg/kg daily, there was decreased survival in their nursing offspring during the first few postpartum days, but overall pup weight and weight gain were comparable to or greater than controls throughout lactation. The manufacturer states that because of the potential for adverse effects of terconazole in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

Drug Interactions

Efficacy of intravaginal terconazole is not affected by concomitant use of oral contraceptives, nor does administration of intravaginal terconazole appear to affect estradiol or progesterone concentrations in women receiving low-dose oral contraceptives.

Pharmacokinetics

Absorption

Small amounts of terconazole are slowly absorbed systemically when the drug is administered intravaginally. Following intravaginal administration of a single dose of terconazole as a 0.4% cream or an 80-mg suppository in healthy hysterectomized women or nonhysterectomized women with tubal ligations, 5-16% of the dose is absorbed, with absorption appearing to be greater for the nonhysterectomized than in hysterectomized women. The amount of drug absorbed is proportional to the dose, regardless of the dosage form, and absorption is similar in women with or without vulvovaginal candidiasis. In healthy women, mean peak plasma terconazole concentrations average 4 ng/mL following administration of single or multiple doses of the 0.4% vaginal cream and 10.4 ng/mL following a single 80-mg vaginal suppository. Following daily intravaginal administration of 5 g of terconazole 0.8% cream (40 mg of terconazole) for 7 days in healthy females, mean peak plasma terconazole concentrations averaged 6 ng/mL; similar absorption characteristics were observed in pregnant and nonpregnant patients with vulvovaginal candidiasis receiving the 0.8% vaginal cream. Accumulation of the drug does not appear to occur following multiple intravaginal doses.

Distribution

Distribution of terconazole into body tissues and fluids following intravaginal administration has not been determined. It is not known whether the drug crosses the placenta or is distributed into milk in humans. The drug is distributed into milk in rats.

Elimination

The metabolic fate of terconazole following intravaginal administration has not been fully characterized, but systemically absorbed drug appears to be rapidly and extensively metabolized. Terconazole is metabolized principally by oxidative N- and O-dealkylation, dioxolane ring cleavage, and conjugation pathways.

Following oral administration of a single 30-mg dose of radiolabeled terconazole, half-life of the parent drug is 6.9 hours (range: 4-11.3 hours) and half-life of total radioactivity is 52.2 hours (range: 44-60 hours).

Following oral administration of a single 30-mg radiolabeled dose of terconazole, 32-56% of the dose is excreted in urine and 47-52% is excreted in feces within 24 hours.

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