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Tioconazole

Pronunciation

(tye oh KONE a zole)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Ointment, Vaginal:

Vagistat-1: 6.5% (4.6 g [DSC])

Brand Names: U.S.

  • Vagistat-1 [OTC] [DSC]

Pharmacologic Category

  • Antifungal Agent, Imidazole Derivative
  • Antifungal Agent, Vaginal

Pharmacology

A 1-substituted imidazole derivative with a broad antifungal spectrum against a wide variety of dermatophytes and yeasts, including Trichophyton mentagrophytes, T. rubrum, T. erinacei, T. tonsurans, Microsporum canis, Microsporum gypseum, and Candida albicans. Both agents appear to be similarly effective against Epidermophyton floccosum.

Absorption

Intravaginal: Systemic 10.6 to 35.8 ng/mL at 8 hours postdose; none detectable at 24 hours (Houang 1985)

Distribution

Vaginal fluid: 24 to 72 hours (Jones 1993)

Onset of Action

Onset of action: Some improvement: Within 24 hours; Complete relief: Within 7 days

Use: Labeled Indications

Candidiasis, vulvovaginal: Local treatment of vulvovaginal candidiasis

Contraindications

Hypersensitivity to tioconazole or any component of the formulation

Dosing: Adult

Candidiasis, vulvovaginal: Intravaginal: Insert 1 applicatorful in vagina as a single dose at bedtime

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Children ≥12 years and Adolescents: Refer to adult dosing

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Administration

Intravaginal: For vaginal use only. Administer 1 applicatorful (prefilled) intravaginally. Applicator may be inserted in any comfortable position. Hold the applicator by the barrel, insert gently into the vagina as far as possible without causing discomfort. Press the plunger until it stops and withdraw the applicator. Patients should not use intravaginal products (eg, tampons, douches) or engage in vaginal intercourse for the duration of treatment. Discard applicator after use.

Storage

Store at 20°C to 25°C (68°F to 77°F).

Drug Interactions

CloZAPine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of CloZAPine. Monitor therapy

Progesterone: Antifungal Agents (Vaginal) may diminish the therapeutic effect of Progesterone. Avoid combination

TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use cannot be avoided, initiate tizanidine at an adult dose of 2 mg and increase in 2-4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification

Adverse Reactions

Frequency not defined.

Central nervous system: Headache

Gastrointestinal: Abdominal pain

Dermatologic: Burning sensation of skin, exfoliation of skin

Genitourinary: Dyspareunia, dysuria, nocturia, vaginal discharge, vaginal pain, vaginitis, vulvar swelling, vulvovaginal irritation, vulvovaginal pruritus

Warnings/Precautions

Concerns related to adverse effects:

• Irritation: If irritation or sensitization occurs, discontinue use.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Pediatric: Vaginal products are not for OTC use in children <12 years of age.

Dosage form specific issues:

• Formulation: Petrolatum-based vaginal products may damage rubber or latex condoms or diaphragms; separate use by 3 days.

• Vaginal product: Consult with health care provider prior to self-medication (OTC use) if experiencing vaginal itching/discomfort, lower abdominal pain, back or shoulder pain, chills, nausea, vomiting, foul-smelling discharge, if this is the first vaginal yeast infection, or if exposed to HIV. Contact health care provider if symptoms do not begin to improve after 3 days or last longer than 7 days. May damage condoms or diaphragms.

Pregnancy Considerations

Following vaginal administration, small amounts of imidazoles are absorbed systemically. Single dose, topical azole regimens are not recommended for the treatment of vulvovaginal candidiasis; only topical azole products with 7-day regimens are recommended in pregnant women with vulvovaginal candidiasis. This product may weaken latex condoms and diaphragms (CDC [Workowski 2015]).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience itching or burning. Have patient report immediately to prescriber abdominal pain, chills, nausea, vomiting, severe vaginal irritation, or foul smelling vaginal discharge (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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