Tioconazole (Topical)


VA CLASSIFICATION
Primary: DE102

Commonly used brand name(s): Trosyd AF; Trosyd J.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

*Not commercially available in the U.S.



Category:


Antifungal (topical).{01}

Indications

Accepted

Candidiasis, cutaneous (treatment)—Tioconazole is indicated in the topical treatment of cutaneous candidiasis caused by Candida albicans.{01}

Tinea corporis (treatment) or
Tinea cruris (treatment) or
Tinea pedis (treatment)—Tioconazole is indicated in the topical treatment of tinea corporis (ringworm of the body), tinea cruris (ringworm of the groin; jock itch), and tinea pedis (ringworm of the foot; athlete's foot) caused by Trichophyton rubrum, Trichophyton mentagrophytes, or Epidermophyton floccosum.{01}

Tinea versicolor (treatment)—Tioconazole is indicated in the topical treatment of tinea versicolor (pityriasis versicolor; ”sun fungus”) caused by Malassezia furfur (Pityrosporon orbiculare).{01}


Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Imidazole class of antifungals.{01}
Molecular weight—
    387.7{01}

Solubility
    Virtually insoluble in water; moderately soluble in chloroform, methanol, ethanol, and ethyl acetate.{01}

Mechanism of action/Effect:

Fungistatic; may be fungicidal, depending on concentration; inhibits biosynthesis of ergosterol or other sterols by blocking C-14 demethylation, damaging the fungal cell wall membrane and altering its permeability; as a result, loss of essential intracellular elements may occur.{01}

Absorption:

Tioconazole was not detectable in plasma after patients made repeated applications of tioconazole 2% cream to single or multiple superficial fungal infection sites on the skin through 28 days of treatment (detection limit 100 micrograms/liter [mcg/L]). Plasma concentrations of less than 10 mcg/L occurred after tioconazole 2% cream at a nominal dose of 40 mg per day was applied to the skin of the abdomen of normal subjects for 14 days.{01}

Biotransformation:

Orally administered tioconazole is extensively metabolized; the major metabolites are glucuronide conjugates.{01}


Time to peak concentration:

5.2 and 8 hours, following vaginal application of a single 300–mg ovule or a single dose of 6.5% ointment, respectively.{01}

1 to 3 hours, following oral administration of single doses of 250 mg to 1 g or multiple doses of up to 3.5 g over 4 days.{01}

Peak serum concentration:

24.7 mcg/L and 18 mcg/L, following vaginal application of a single 300–mg ovule or a single dose of 6.5% ointment, respectively.{01}

Elimination:
    Fecal—Primary route of excretion, following oral administration.{01}
    Renal—No unchanged drug; metabolites only, following oral administration.{01}


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other forms of tioconazole or other imidazole antifungal agents may be sensitive to this medication also.{01}

Carcinogenicity

Studies to evaluate the long-term carcinogenic potential of tioconazole have not been done.{01}

Mutagenicity

No mutagenic or cytogenic effects of tioconazole were observed in animal studies.{01}

Pregnancy/Reproduction
Fertility—
Spermatogenic arrest occurred in 2 out of 5 male rabbits after 30 daily applications of tioconazole 2% cream 1 milliliter/kilogram (mL/kg) per day to shaven but not abraded skin.{01}

Pregnancy—
Adequate and well controlled studies of topical tioconazole in humans have not been done.{01} In limited uncontrolled clinical use, tioconazole vaginal ointment and suppositories, applied as a single dose to approximately 20 patients during various stages of pregnancy, did not appear to interfere with the normal progress of the pregnancy or delivery.{01}

Local and systemic administration in rats produced adverse effects related to parturition and/or fetal development.{01} An increased incidence of stillbirths (range 37% to 100%) was observed on post-mating days 24 or 25 in rats given oral doses up to 150 milligrams/kilogram (mg/kg) per day or subcutaneous doses up to 20 mg/kg/day throughout gestation or during the last third of gestation .{01}

Breast-feeding

It not known whether tioconazole applied topically is distributed into human breast milk. However, problems in humans have not been documented. {01}

Pediatrics

Appropriate studies on the relationship of age to the effects of topical tioconazole have not been performed in the pediatric population. Limited clinical experiences have not demonstrated pediatrics-specific problems that would limit the usefulness of topical tioconazole in children.{01} Use of topical tioconazole in children less than 2 years of age should be under the direction of a physician; use in children under 12 years of age should be supervised by an adult. {01}


Geriatrics


Appropriate studies on the relationship of age to the effects of topical tioconazole have not been performed in the geriatric population. However, no geriatric-specific problems have been documented to date.{01}

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
Sensitivity to topical tioconazole{01}


Side/Adverse Effects

Note: In human studies, tioconazole applied topically showed no evidence of sensitization, skin irritation, or local or systemic side effects.{01}
No evidence of photo-irritation was seen when tioconazole 2% cream was applied to the upper back of healthy volunteers for 72 hours (under occlusion), with subsequent exposure of the treated area to sunlight or longwave ultraviolet light.{01}

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Less common
    
Burning, itching, redness, skin rash, swelling, or other signs of skin irritation not present before therapy {01}





Overdose
For more information on the management of overdose or unintentional ingestion, contact a poison control center (see Poison Control Center Listing).


Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Tioconazole (Topical).
In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to topical tioconazole or other imidazole derivatives such as miconazole or econazole

Proper use of this medication
Applying sufficient medication to cover affected and surrounding areas, and rubbing in gently

» Avoiding contact with the eyes

» Not applying occlusive dressing over this medication unless directed to do so by physician

» Compliance with full course of therapy; fungal infections may require prolonged therapy

» Proper dosing
Missed dose: Applying as soon as possible; not applying if almost time for next dose

Proper storage

Precautions while using this medication
Checking with physician if condition becomes worse or if it does not improve within: 2 weeks for tinea cruris; 2 to 4 weeks for cutaneous candidiasis or tinea corporis; 1 to 4 weeks for tinea versicolor; 6 weeks for tinea pedis

» Using hygienic measures to help cure infection or to help prevent reinfection

For tinea cruris
Avoiding underwear that is tight-fitting or made from synthetic materials; wearing loose-fitting cotton underwear instead

Using a bland, absorbent powder or an antifungal powder on the skin; not using cream and powder concurrently

For tinea pedis
Carefully drying feet, especially between toes, after bathing

Avoiding socks made from wool or synthetic materials; wearing clean, cotton socks and changing them daily or more often if feet perspire excessively

Wearing well-ventilated shoes or sandals

Using a bland, absorbent powder or an antifungal powder between toes, on feet, and in socks and shoes liberally once or twice daily; not using cream and powder concurrently


Side/adverse effects
Signs of potential side effects, especially burning, itching, redness, rash, swelling, or other signs of irritation not present before therapy


General Dosing Information
To reduce the possibility of recurrence, Candida infections and tinea corporis should be treated for 2 to 4 weeks, tinea cruris should be treated for up to 2 weeks, tinea pedis should be treated for up to 6 weeks, and tinea versicolor should be treated for 1 to 4 weeks.{01}


Topical Dosage Forms

TIOCONAZOLE CREAM USP

Usual Adult and adolescent dose
Candidiasis, cutaneous or
Tinea corporis
Topical, to the skin two times a day, morning and evening, for 2 to 4 weeks.{01}

Tinea cruris
Topical, to the skin two times a day, morning and evening, for up to 14 days.{01}

Tinea pedis
Topical, to the skin two times a day, morning and evening, for up to 6 weeks.{01}

Tinea versicolor
Topical, to the skin two times a day, morning and evening, for 7 to 28 days.{01}


Note: For infection in intertriginous areas, tioconazole cream should be applied sparingly and smoothed in well to avoid macerating effects.{01}


Usual Pediatric Dose
For children 2 to 12 years of age
See Usual adult and adolescent dose.

For children up to 2 years of age
Dosage has not been established.


Note: Tioconazole use in children under 2 years of age should be under the direction of a physician; use in children under 12 years of age should be supervised by an adult.{01}


Strength(s) usually available
U.S.—
Not commercially available.

Canada—


1% w/w (Rx) [Trosyd AF ( 10 mg of tioconazole per gram of vanishing cream base) ( benzyl alcohol) ( ethoxylated cetostearyl alcohol ) ( mineral oil) ( white petrolatum) ( propylene glycol) ( stearic acid) ( stearyl alcohol) ( purified water)]{01} [Trosyd J (10 mg of tioconazole per gram of vanishing cream base) (benzyl alcohol) ( ethoxylated cetostearyl alcohol) ( mineral oil) ( white petrolatum) ( propylene glycol) ( stearic acid) ( stearyl alcohol) ( purified water)]{01}

Packaging and storage:
Store between 15 and 30 °C (59 and 86 °F). Avoid freezing.{01}

Auxiliary labeling:
   • For external use only.
   • Continue medicine for full time of treatment.



Developed: 06/12/2000



References
  1. Product Information: Trosyd™ AF and Trosyd™ J, tioconazole 1% cream. Pfizer Canada, Kirkland, Quebec, Canada, (PI revised 10/1995) reviewed 5/2000.
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