TIOCONAZOLE

Clinical safety rating: safe

Animal studies have demonstrated safety

How it works

Inhibition of fungal CYP450-dependent 14α-demethylase, blocking ergosterol synthesis and disrupting fungal cell membrane integrity.

What the body does with it

Metabolism	Minimal systemic absorption; not extensively metabolized.
Excretion	Primarily fecal (minimally absorbed; <5% absorbed dose excreted renally as metabolites); topically applied tioconazole is largely unabsorbed.
Half-life	Terminal elimination half-life is approximately 24–30 hours after topical application, reflecting slow systemic clearance of absorbed fraction.
Protein binding	Approximately 90–95% bound to plasma proteins, primarily albumin.
Volume of Distribution	Not well characterized due to minimal systemic absorption; estimated Vd <0.1 L/kg after topical application, indicating limited distribution.
Bioavailability	Topical vaginal: <5% of dose absorbed systemically; oral bioavailability negligible (<1%) due to extensive first-pass metabolism.
Onset of Action	Topical: Clinical improvement (relief of symptoms) typically begins within 24–72 hours; antifungal effect begins immediately upon contact.
Duration of Action	Topical: After single application, therapeutic concentrations persist in vaginal mucosa for 48–72 hours; clinical cure usually requires 7–14 days of daily application.

Classification & Brands

Dosing & administration

Topical: Apply 1% cream, lotion, or solution to affected area twice daily for 2-4 weeks. Vaginal: Insert 1 applicatorful of 6.5% ointment intravaginally at bedtime as a single dose.

Dosage form	OINTMENT
Renal impairment	No dose adjustment required for topical use; systemic absorption minimal. For systemic use, no specific GFR-based guidelines exist; use caution in severe renal impairment.
Liver impairment	No dose adjustment required for topical use. For systemic use, contraindicated in Child-Pugh Class C; reduce dose by 50% in Child-Pugh Class B (if oral formulation available).
Pediatric use	Topical: Apply to affected area twice daily for 2-4 weeks in children ≥2 years. Safety in infants <2 years not established.
Geriatric use	No specific dose adjustment required for topical use; monitor for local irritation. For vaginal use, same as adult dosing.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

No significant drug interactions For topical use only not for ophthalmic use.

Breastfeeding

It is unknown if tioconazole is excreted in human breast milk. Following vaginal administration, systemic absorption is minimal (<5%), making significant excretion unlikely. The M/P ratio has not been determined. Caution is advised, but use is likely compatible with breastfeeding due to low systemic exposure.

Teratogenic Risk

Tioconazole is classified as FDA Pregnancy Category C. No adequate and well-controlled studies in pregnant women. In animal studies, no teratogenic effects were observed at doses up to 20 mg/kg/day (approximately 0.2 times the human vaginal dose based on body surface area). However, increased fetal resorptions and delayed ossification occurred at maternally toxic doses. First trimester: insufficient human data. Second and third trimesters: minimal systemic absorption limits risk, but avoid unless clearly needed.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Common Effects	Vaginal burning
Serious Effects

Absolute Contraindications

["Hypersensitivity to tioconazole or any component of the formulation"]

Clinical Precautions

Precautions

["For external use only; avoid contact with eyes and mucous membranes","Discontinue if irritation or sensitivity occurs","Not for use in nail or scalp infections"]

Clinical Tips & Counseling

Drug interactions

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