CLOCORTOLONE PIVALATE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for CLOCORTOLONE PIVALATE (CLOCORTOLONE PIVALATE).

How it works

Clocortolone pivalate is a corticosteroid that exerts anti-inflammatory, antipruritic, and vasoconstrictive actions. It binds to glucocorticoid receptors, modulating gene expression to inhibit phospholipase A2, reduce prostaglandin and leukotriene synthesis, and suppress cytokine release.

What the body does with it

Metabolism	Clocortolone pivalate is primarily metabolized in the skin; systemic metabolism is minimal after topical application. Specific enzymes have not been well characterized.
Excretion	Primarily renal (approximately 80%) as glucuronide and sulfate conjugates; minor biliary/fecal excretion (20%).
Half-life	Terminal elimination half-life is approximately 2.5 hours (range 1-4 hours), reflecting rapid clearance; clinical duration exceeds half-life due to tissue binding.
Protein binding	Approximately 90-95% bound to albumin and corticosteroid-binding globulin (CBG).
Volume of Distribution	Apparent volume of distribution is approximately 0.3-0.5 L/kg, suggesting distribution primarily into extracellular fluid and tissues.
Bioavailability	Topical: Systemic bioavailability is extremely low (<1%) when applied to intact skin; increased with damaged skin or occlusion.
Onset of Action	Topical: Onset of anti-inflammatory effect within hours of application, with maximal effect observed after 24-48 hours of regular use.
Duration of Action	Duration of anti-inflammatory effect after single topical dose is 12-24 hours; clinical recommendations typically advise twice-daily application to maintain effect.

Classification & Brands

Dosing & administration

Topical: Apply a thin film to affected area once or twice daily. Not for ophthalmic use. Maximum duration of 2 weeks per course.

Dosage form	CREAM
Renal impairment	No adjustment required for topical use due to negligible systemic absorption.
Liver impairment	No adjustment required for topical use due to negligible systemic absorption.
Pediatric use	Children ≥ 3 months: Apply a thin film to affected area once or twice daily for no more than 7 days. Use lowest potency and smallest amount possible. Not recommended for diaper dermatitis or under occlusive dressings in children.
Geriatric use	Use with caution due to increased risk of skin atrophy and systemic absorption from thinner skin. Apply lowest effective amount, avoid prolonged use, and monitor for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for CLOCORTOLONE PIVALATE (CLOCORTOLONE PIVALATE).

Breastfeeding	Excreted in breast milk? Unknown, but systemic absorption minimal with topical use. Caution advised; M/P ratio not established. Use only if essential; monitor infant for adrenal suppression.
Teratogenic Risk	Category C: No adequate human studies; animal studies show fetal abnormalities at high doses. Risk cannot be ruled out. First trimester: Avoid unless benefit outweighs risk. Corticosteroids may increase risk of cleft palate (2-3 per 1000). Second/third trimester: Use only if clearly needed; may cause fetal adrenal suppression.

Warnings & precautions

■ FDA Black Box Warning

No FDA boxed warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to clocortolone pivalate or any component of the formulation.","Untreated bacterial, fungal, viral, or parasitic skin infections."]

Clinical Precautions

Precautions

["Topical corticosteroids may cause reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome, hyperglycemia, and glucosuria.","Systemic absorption is increased with prolonged use, use over large body surface areas, use under occlusion, or use in children.","Children may be more susceptible to systemic toxicity due to higher skin surface-to-body mass ratio.","Local adverse reactions include skin atrophy, striae, telangiectasias, burning, itching, irritation, dryness, folliculitis, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, and miliaria."]

Clinical Tips & Counseling

Drug interactions

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CLOCORTOLONE PIVALATE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for CLOCORTOLONE PIVALATE (CLOCORTOLONE PIVALATE).

How it works

What the body does with it

Metabolism	Clocortolone pivalate is primarily metabolized in the skin; systemic metabolism is minimal after topical application. Specific enzymes have not been well characterized.
Excretion	Primarily renal (approximately 80%) as glucuronide and sulfate conjugates; minor biliary/fecal excretion (20%).
Half-life	Terminal elimination half-life is approximately 2.5 hours (range 1-4 hours), reflecting rapid clearance; clinical duration exceeds half-life due to tissue binding.
Protein binding	Approximately 90-95% bound to albumin and corticosteroid-binding globulin (CBG).
Volume of Distribution	Apparent volume of distribution is approximately 0.3-0.5 L/kg, suggesting distribution primarily into extracellular fluid and tissues.
Bioavailability	Topical: Systemic bioavailability is extremely low (<1%) when applied to intact skin; increased with damaged skin or occlusion.
Onset of Action	Topical: Onset of anti-inflammatory effect within hours of application, with maximal effect observed after 24-48 hours of regular use.
Duration of Action	Duration of anti-inflammatory effect after single topical dose is 12-24 hours; clinical recommendations typically advise twice-daily application to maintain effect.

Classification & Brands

Dosing & administration

Topical: Apply a thin film to affected area once or twice daily. Not for ophthalmic use. Maximum duration of 2 weeks per course.

Dosage form	CREAM
Renal impairment	No adjustment required for topical use due to negligible systemic absorption.
Liver impairment	No adjustment required for topical use due to negligible systemic absorption.
Pediatric use	Children ≥ 3 months: Apply a thin film to affected area once or twice daily for no more than 7 days. Use lowest potency and smallest amount possible. Not recommended for diaper dermatitis or under occlusive dressings in children.
Geriatric use	Use with caution due to increased risk of skin atrophy and systemic absorption from thinner skin. Apply lowest effective amount, avoid prolonged use, and monitor for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for CLOCORTOLONE PIVALATE (CLOCORTOLONE PIVALATE).

Breastfeeding	Excreted in breast milk? Unknown, but systemic absorption minimal with topical use. Caution advised; M/P ratio not established. Use only if essential; monitor infant for adrenal suppression.
Teratogenic Risk	Category C: No adequate human studies; animal studies show fetal abnormalities at high doses. Risk cannot be ruled out. First trimester: Avoid unless benefit outweighs risk. Corticosteroids may increase risk of cleft palate (2-3 per 1000). Second/third trimester: Use only if clearly needed; may cause fetal adrenal suppression.

Warnings & precautions

■ FDA Black Box Warning

No FDA boxed warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to clocortolone pivalate or any component of the formulation.","Untreated bacterial, fungal, viral, or parasitic skin infections."]