GYNE-LOTRIMIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for GYNE-LOTRIMIN (GYNE-LOTRIMIN).

How it works

Clotrimazole, an imidazole antifungal, inhibits fungal cytochrome P450 14α-demethylase, thereby blocking the conversion of lanosterol to ergosterol, an essential component of the fungal cell membrane. This disrupts membrane integrity and function, leading to fungal cell death.

What the body does with it

Metabolism	Clotrimazole is primarily metabolized in the liver via oxidative metabolism; no specific cytochrome P450 enzymes have been identified. Following vaginal administration, systemic absorption is minimal, and the small amount absorbed is metabolized and excreted in bile and feces.
Excretion	Primarily fecal (approx. 90%) as unchanged drug and metabolites; renal excretion accounts for <1% of absorbed dose.
Half-life	The terminal elimination half-life of clotrimazole is approximately 3.5-4.9 hours. However, after topical application, systemic absorption is minimal, and local concentrations persist for hours to days at the site of action.
Protein binding	Clotrimazole is highly protein-bound, approximately 90-95%, primarily to albumin.
Volume of Distribution	Due to minimal systemic absorption after topical use, the volume of distribution is not well defined; however, after oral administration (not indicated), the Vd is approximately 10-20 L/kg, indicating extensive tissue distribution.
Bioavailability	After intravaginal or topical application, systemic bioavailability is extremely low (<0.5% of the applied dose).
Onset of Action	For intravaginal administration: onset of symptomatic relief begins within 24-72 hours after the first dose.
Duration of Action	With intravaginal use, clinical effects persist for 3-7 days. However, the drug is typically administered as a 1-day, 3-day, or 7-day regimen depending on formulation.

Classification & Brands

Dosing & administration

Intravaginal: clotrimazole 500 mg vaginal tablet once or 200 mg vaginal tablet daily for 3 days or 1% vaginal cream 5 g daily for 7–14 days. Topical: clotrimazole 1% cream applied to affected area twice daily for 2–4 weeks.

Dosage form	TABLET
Renal impairment	No dose adjustment required for renal impairment.
Liver impairment	No dose adjustment required for hepatic impairment.
Pediatric use	Children ≥12 years: same as adult dosing. Children <12 years: not recommended without physician guidance; topical formulations may be used with caution as directed.
Geriatric use	Same as adult dosing. No specific adjustments needed; consider potential for decreased mucosal integrity and increased sensitivity to local irritation.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for GYNE-LOTRIMIN (GYNE-LOTRIMIN).

Breastfeeding	Clotrimazole is poorly absorbed systemically after intravaginal administration, with estimated absorption <1%. Excretion into breast milk is minimal; M/P ratio is unknown. It is considered compatible with breastfeeding. No adverse effects on nursing infants have been reported.
Teratogenic Risk	Clotrimazole (GYNE-LOTRIMIN) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, and there are no adequate controlled studies in pregnant women. Intravaginal use is considered safe in all trimesters, with no increased risk of major malformations or adverse fetal outcomes reported.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to clotrimazole or any component of the formulation. Not for use in patients with known history of hypersensitivity to imidazole antifungals.

Clinical Precautions

Precautions

Do not use if abdominal pain, fever, or foul-smelling discharge is present. Discontinue if irritation or hypersensitivity occurs. Recurrent infections may indicate underlying conditions such as diabetes or HIV. Avoid contact with eyes. For topical use only; not for ophthalmic, oral, or intravaginal use in products intended for external use.

Clinical Tips & Counseling

Drug interactions

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GYNE-LOTRIMIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for GYNE-LOTRIMIN (GYNE-LOTRIMIN).

How it works

What the body does with it

Metabolism	Clotrimazole is primarily metabolized in the liver via oxidative metabolism; no specific cytochrome P450 enzymes have been identified. Following vaginal administration, systemic absorption is minimal, and the small amount absorbed is metabolized and excreted in bile and feces.
Excretion	Primarily fecal (approx. 90%) as unchanged drug and metabolites; renal excretion accounts for <1% of absorbed dose.
Half-life	The terminal elimination half-life of clotrimazole is approximately 3.5-4.9 hours. However, after topical application, systemic absorption is minimal, and local concentrations persist for hours to days at the site of action.
Protein binding	Clotrimazole is highly protein-bound, approximately 90-95%, primarily to albumin.
Volume of Distribution	Due to minimal systemic absorption after topical use, the volume of distribution is not well defined; however, after oral administration (not indicated), the Vd is approximately 10-20 L/kg, indicating extensive tissue distribution.
Bioavailability	After intravaginal or topical application, systemic bioavailability is extremely low (<0.5% of the applied dose).
Onset of Action	For intravaginal administration: onset of symptomatic relief begins within 24-72 hours after the first dose.
Duration of Action	With intravaginal use, clinical effects persist for 3-7 days. However, the drug is typically administered as a 1-day, 3-day, or 7-day regimen depending on formulation.

Classification & Brands

Dosing & administration

Dosage form	TABLET
Renal impairment	No dose adjustment required for renal impairment.
Liver impairment	No dose adjustment required for hepatic impairment.
Pediatric use	Children ≥12 years: same as adult dosing. Children <12 years: not recommended without physician guidance; topical formulations may be used with caution as directed.
Geriatric use	Same as adult dosing. No specific adjustments needed; consider potential for decreased mucosal integrity and increased sensitivity to local irritation.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for GYNE-LOTRIMIN (GYNE-LOTRIMIN).

Breastfeeding	Clotrimazole is poorly absorbed systemically after intravaginal administration, with estimated absorption <1%. Excretion into breast milk is minimal; M/P ratio is unknown. It is considered compatible with breastfeeding. No adverse effects on nursing infants have been reported.
Teratogenic Risk	Clotrimazole (GYNE-LOTRIMIN) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, and there are no adequate controlled studies in pregnant women. Intravaginal use is considered safe in all trimesters, with no increased risk of major malformations or adverse fetal outcomes reported.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to clotrimazole or any component of the formulation. Not for use in patients with known history of hypersensitivity to imidazole antifungals.