Diprolene - Drug Monograph

Introduction

Diprolene (betamethasone dipropionate) is a high-potency topical corticosteroid indicated for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. It belongs to the class of synthetic glucocorticoids and is available in various formulations including cream, ointment, and lotion.

Mechanism of Action

Betamethasone dipropionate exerts its anti-inflammatory, antipruritic, and vasoconstrictive effects through multiple mechanisms. The drug diffuses across cell membranes and forms complexes with cytoplasmic glucocorticoid receptors. These complexes migrate to the cell nucleus, bind to glucocorticoid response elements in DNA, and modify transcription of certain genes. This results in:

• Inhibition of inflammatory cytokine production
• Decreased vasodilation and permeability
• Suppression of migration of polymorphonuclear leukocytes
• Reduction in fibroblast proliferation
• Decreased collagen synthesis

Indications

FDA-approved indications:

• Relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses including:

- Atopic dermatitis - Contact dermatitis - Eczema - Psoriasis - Lichen planus - Lichen simplex chronicus

Off-label uses (should be used with caution and under specialist supervision):

• Discoid lupus erythematosus
• Granuloma annulare
• Alopecia areata

Dosage and Administration

• Apply a thin film to affected areas twice daily (morning and evening)
• Duration of treatment should be limited to 2 weeks
• Total dosage should not exceed 50 g/week

• Pediatric patients: Use should be limited and duration minimized due to increased systemic absorption risk
• Geriatric patients: May require monitoring for increased skin atrophy risk
• Hepatic impairment: No specific dosage adjustment recommended
• Renal impairment: No specific dosage adjustment recommended

• Gently cleanse and dry area before application
• Use sparingly and rub in gently
• Do not use with occlusive dressings unless directed by physician
• Avoid application near eyes, mouth, or mucous membranes

Pharmacokinetics

• Topical absorption varies based on vehicle, skin integrity, and use of occlusive dressings
• Greater absorption occurs through inflamed skin, denuded skin, or under occlusion
• Systemic absorption can occur, especially with prolonged use or large surface area application

• Distributed throughout local skin tissues
• Minimal systemic distribution when used appropriately

• Primarily metabolized in the liver via CYP3A4
• Converted to active and inactive metabolites

• Renal excretion of metabolites
• Elimination half-life approximately 6-8 hours

Contraindications

• Hypersensitivity to betamethasone dipropionate or any component of the formulation
• Viral skin infections (herpes simplex, varicella)
• Fungal infections
• Bacterial skin infections without appropriate antimicrobial therapy
• Perioral dermatitis
• Acne rosacea
• Tuberculosis of the skin

Warnings and Precautions

• Not for ophthalmic use
• May cause HPA axis suppression and Cushing's syndrome with prolonged use

• Use with caution in patients with liver impairment
• Avoid use on face, groin, or axillae due to increased absorption risk
• Discontinue if irritation develops
• Pregnancy Category C: Use only if potential benefit justifies potential risk
• Pediatric patients are more susceptible to systemic toxicity
• May mask symptoms of infection
• Prolonged use may result in skin atrophy, striae, and telangiectasias

Drug Interactions

• No clinically significant pharmacokinetic drug interactions documented
• Theoretical increased risk of HPA axis suppression when used with other systemic corticosteroids
• Caution advised when using with other potentially hepatotoxic drugs

Adverse Effects

• Burning sensation
• Pruritus
• Irritation
• Dryness
• Folliculitis
• Hypertrichosis

• Hypothalamic-pituitary-adrenal (HPA) axis suppression
• Cushing's syndrome
• Glaucoma (with periocular use)
• Secondary infections
• Skin atrophy
• Striae
• Contact dermatitis
• Hypopigmentation

Monitoring Parameters

• Clinical response to therapy
• Signs of skin irritation or infection
• Signs of systemic absorption (especially in pediatric patients):

- Linear growth retardation - Weight gain - Cushingoid features - Hyperglycemia

• For long-term use: periodic adrenal function tests
• Ophthalmic examination if used near eyes

Patient Education

• Use only as directed by healthcare provider
• Apply thin film to affected areas only
• Wash hands after application unless hands are treatment area
• Do not use occlusive dressings unless instructed
• Avoid contact with eyes, mouth, and mucous membranes
• Report any signs of skin irritation, infection, or lack of improvement
• Do not use longer than prescribed duration
• Inform all healthcare providers about all medications being used
• Store at room temperature, away from excessive heat or moisture

References

1. FDA Prescribing Information: Diprolene (betamethasone dipropionate) 2. Wolverton SE. Comprehensive Dermatologic Drug Therapy. 4th ed. Elsevier; 2021. 3. Bolognia JL, Schaffer JV, Cerroni L. Dermatology. 4th ed. Elsevier; 2018. 4. Habif TP. Clinical Dermatology: A Color Guide to Diagnosis and Therapy. 7th ed. Elsevier; 2021. 5. American Academy of Dermatology Guidelines for Topical Corticosteroid Use (2020) 6. Katzung BG, Vanderah TW. Basic & Clinical Pharmacology. 15th ed. McGraw Hill; 2021. 7. ClinicalTrials.gov database for post-marketing surveillance data 8. Micromedex® Drug Information: Betamethasone dipropionate