LOCOID LIPOCREAM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LOCOID LIPOCREAM (LOCOID LIPOCREAM).
Locoid Lipocream contains hydrocortisone butyrate, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. It acts by inducing phospholipase A2 inhibitory proteins (lipocortins), thereby inhibiting the release of arachidonic acid and subsequent synthesis of prostaglandins and leukotrienes. It also suppresses cytokine production, reduces mast cell degranulation, and decreases vascular permeability.
| Metabolism | Hydrocortisone butyrate undergoes hepatic metabolism primarily via cytochrome P450 3A4 (CYP3A4) and other esterases to inactive metabolites, including hydrocortisone and butyric acid. Subsequent glucuronidation and sulfation occur before renal excretion. |
| Excretion | Renal: ~1.5% as unchanged hydrocortisone butyrate and metabolites; Biliary/fecal: ~85% as metabolites |
| Half-life | Terminal elimination half-life: ~6-8 hours (hydrocortisone butyrate); clinical context: supports twice-daily dosing |
| Protein binding | Hydrocortisone butyrate: ~88-92% bound to corticosteroid-binding globulin (CBG) and albumin |
| Volume of Distribution | Vd: ~0.3-0.5 L/kg (estimated systemic absorption from topical application; low Vd indicates limited tissue distribution in systemic circulation) |
| Bioavailability | Topical: ~1-5% systemically absorbed through intact skin; higher (up to 10-15%) if applied to inflamed, denuded, or occluded skin |
| Onset of Action | Topical: measurable vasoconstriction within 1-2 hours; clinical effect (e.g., reduced erythema) within 3-5 days of regular use |
| Duration of Action | Topical: vasoconstriction persists 6-8 hours after single application; clinical improvement maintained with twice-daily application |
| Molecular Weight | 432.56 |
Apply a thin layer to affected area twice daily. Maximum duration of continuous treatment: 4 weeks.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required. |
| Liver impairment | No dosage adjustment required. |
| Pediatric use | Apply a thin layer to affected area once daily. Maximum treatment duration: 7 days. Avoid prolonged use and occlusive dressings. |
| Geriatric use | Apply a thin layer to affected area twice daily. Limit use to shortest duration possible due to increased risk of skin atrophy and systemic absorption. |
| 1st trimester | Topical corticosteroids should be used during the first trimester only if the potential benefit justifies the potential risk to the fetus. Avoid use on large areas, under occlusion, or for prolonged periods. |
| 2nd trimester | Use with caution. Avoid extensive application, prolonged treatment, or occlusive dressings. Consider lower potency alternatives. |
| 3rd trimester | Use with caution near term. Prolonged use or high doses may cause fetal adrenal suppression or low birth weight. Avoid application to large areas or broken skin. |
Clinical note
Comprehensive clinical and safety monograph for LOCOID LIPOCREAM (LOCOID LIPOCREAM).
| Placental transfer | Corticosteroids cross the placenta. The degree of transfer varies with potency, formulation, and application site. For hydrocortisone butyrate, systemic absorption after topical use is minimal (<1% of applied dose), so placental transfer is expected to be low with proper use. |
| Breastfeeding |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to hydrocortisone butyrate or any component of the formulationUntreated bacterial, fungal, or viral skin infections (e.g., herpes simplex, varicella, tuberculosis)
| Precautions | Systemic absorption of topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, especially in pediatric patients, patients with extensive disease, or with prolonged use on occluded areas., Local adverse reactions include skin atrophy, striae, telangiectasias, burning, itching, irritation, dryness, folliculitis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, and miliaria., Prolonged use may increase the risk of cataracts or glaucoma if applied to periorbital area., Use with caution in patients with skin atrophy, bacterial/fungal/viral infections, or impaired circulation., Not for ophthalmic, oral, or intravaginal use. |
| Food/Dietary | No known food interactions. Topical application minimizes systemic absorption, but avoid excessive intake of corticosteroids (e.g., grapefruit juice) as a general precaution. |
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| Topical application is generally considered compatible with breastfeeding. Avoid application to the breast area or use on large areas, under occlusion, or for prolonged periods to minimize infant exposure. Hydrocortisone butyrate is a mild to moderate potency corticosteroid; systemic absorption is low when used as directed. |
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Topical corticosteroids are generally considered low risk during pregnancy due to minimal systemic absorption. However, prolonged use of potent or large amounts may increase risk of low birth weight (LBW) and preterm delivery. First trimester: no evidence of teratogenicity; second/third trimester: prolonged use associated with LBW and preterm delivery. |
| Fetal Monitoring | Monitor for signs of adrenal suppression with prolonged use. No specific fetal monitoring required, but assess fetal growth if used extensively in second/third trimester. |
| Fertility Effects | No known adverse effects on fertility from topical corticosteroids. |
| Clinical Pearls | Locoid Lipocream (hydrocortisone butyrate 0.1%) is a medium-potency topical corticosteroid in a lipophilic cream base that enhances skin penetration. Use limited to 2 weeks on face or intertriginous areas due to risk of skin atrophy. Avoid occlusion unless directed, as it increases systemic absorption. Not for ophthalmic use. |
| Patient Advice | Apply a thin layer only to affected areas, usually twice daily. · Do not use on broken skin, infections, or for more than 2 weeks unless directed. · Avoid contact with eyes, mouth, and mucous membranes. · Wash hands after application unless treating hands. · Do not cover with bandages or dressings unless instructed by your doctor. |