LOCOID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LOCOID (LOCOID).
Topical corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Binds to glucocorticoid receptors, modulating gene expression to inhibit phospholipase A2, reduce prostaglandin and leukotriene synthesis, and suppress cytokine production.
| Metabolism | Primarily metabolized in the liver via CYP3A4 to inactive metabolites. Systemically absorbed amount is minimal with topical use. |
| Excretion | Renal (approximately 60-70%) as conjugated metabolites; biliary/fecal (approximately 20-30%) |
| Half-life | Terminal elimination half-life: 30-40 hours; clinically significant for once-daily dosing and prolonged action |
| Protein binding | Highly protein-bound (96-99%), primarily to albumin and corticosteroid-binding globulin |
| Volume of Distribution | Vd approximately 0.3-0.5 L/kg, indicating predominant distribution into extracellular fluid |
| Bioavailability | Topical: negligible systemic absorption (<1% on intact skin, up to 5-10% on damaged skin). Oral: not applicable; parenteral: 100% |
| Onset of Action | Topical: relief of pruritus within 24-48 hours; intralesional: within 6-12 hours |
| Duration of Action | Topical: anti-inflammatory effect persists for 12-24 hours after single application; duration may extend with occlusion |
Topical: Apply a thin layer to affected area once or twice daily. Maximum: 30-60 g per week. Not for use >2 consecutive weeks or on >50% of body surface.
| Dosage form | OINTMENT |
| Renal impairment | No adjustment needed for topical use; negligible systemic absorption. |
| Liver impairment | No adjustment needed for topical use; negligible systemic absorption. |
| Pediatric use | Topical: Apply a thin layer once or twice daily. Use lowest potency and shortest duration; avoid occlusive dressings. Maximum 2 weeks. |
| Geriatric use | Use with caution; thinner skin increases risk of atrophy. Limit to short-term, low-potency application. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LOCOID (LOCOID).
| Breastfeeding | Locoid is likely compatible with breastfeeding when used topically in limited areas for short duration. The M/P ratio is unknown. To minimize infant exposure, avoid application to breast area and wash off before nursing. High doses or prolonged use could theoretically cause systemic effects in the infant |
| Teratogenic Risk | Topical corticosteroids like Locoid (hydrocortisone butyrate) are generally considered low risk for teratogenicity when used at recommended doses. Systemic absorption is minimal with topical application, but high-potency or prolonged use may increase risk. In the first trimester, avoid extensive use; there is no clear evidence of major malformations. Second and third trimesters: risk of intrauterine growth restriction and adrenal suppression in the fetus with prolonged high-dose application |
■ FDA Black Box Warning
None
| Common Effects | Eye irritation Burning eyes Eye discomfort Eye itching Eye pain |
| Serious Effects |
["Hypersensitivity to hydrocortisone butyrate or any component of the formulation","Untreated bacterial, fungal, or viral skin lesions","Perioral dermatitis","Rosacea"]
| Precautions | ["Systemic absorption may produce HPA axis suppression, especially in children and with prolonged use.","Topical use may cause local skin reactions including atrophy, striae, and telangiectasias.","Avoid use on face, groin, and axillae unless directed.","Prolonged use may lead to contact dermatitis or secondary infection.","Use with caution in patients with impaired skin barrier or widespread disease."] |
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| Fetal Monitoring | Monitor maternal adrenal function if used extensively or for prolonged periods. Assess fetal growth via ultrasound if high-potency or large quantities are used in pregnancy. Monitor newborn for signs of adrenal suppression (e.g., hypoglycemia, lethargy) if maternal use was high-dose or long-term near term |
| Fertility Effects | No significant effects on fertility have been reported with topical corticosteroid use. Systemic corticosteroids may affect ovulation, but topical Locoid at typical doses does not alter fertility |