ANUSOL HC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANUSOL HC (ANUSOL HC).
Hydrocortisone, a corticosteroid, binds to glucocorticoid receptors, inhibiting phospholipase A2 activity and reducing prostaglandin and leukotriene synthesis. It also suppresses cytokine production and inflammatory cell migration, leading to decreased edema, erythema, and pruritus in anorectal tissues.
| Metabolism | Hydrocortisone is primarily metabolized in the liver via CYP3A4 to inactive metabolites, including tetrahydrocortisone and tetrahydrocortisol, which are conjugated with glucuronic acid and excreted renally. |
| Excretion | Renal (primarily as metabolites) >80%; fecal ~15%; <2% unchanged in urine due to extensive hepatic metabolism. Biliary excretion is negligible. |
| Half-life | Terminal elimination half-life of hydrocortisone is approximately 1.5-2 hours (range 1-3 h) in adults; clinical effect outlasts half-life due to intracellular receptor-mediated action. |
| Protein binding | Hydrocortisone: 90-95% bound to corticosteroid-binding globulin (CBG) and albumin. Pramoxine: ~85% bound to plasma proteins. |
| Volume of Distribution | Hydrocortisone: Vd approximately 0.3-0.5 L/kg (confined to extracellular fluid); pramoxine: Vd ~4-6 L/kg (extensive tissue distribution). |
| Bioavailability | Rectal bioavailability of hydrocortisone from suppository/cream is approximately 10-30% due to first-pass metabolism and local retention; systemic absorption is low but sufficient for local effect. |
| Onset of Action | Rectal administration: relief of itching and discomfort within 24-72 hours; full therapeutic effect may take several days. |
| Duration of Action | Duration of anti-inflammatory effect is 4-6 hours after topical application, but pruritus relief may persist 12-24 hours due to anesthetic component (pramoxine has duration ~4-6 h). |
Apply a thin layer to the affected area rectally 2 to 4 times daily, or after each bowel movement, for up to 7 days. Each application should not exceed 1 gram.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Children ≥12 years: same as adult. Children <12 years: not recommended without physician consultation. |
| Geriatric use | Use with caution due to potential for skin atrophy and systemic absorption; limit use to shortest duration necessary. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANUSOL HC (ANUSOL HC).
| Breastfeeding | Topical hydrocortisone excretion into breast milk is negligible due to low systemic absorption. M/P ratio not established for topical use. Oral corticosteroids are excreted in low amounts. Use with caution; avoid application to nipples. The American Academy of Pediatrics considers topical corticosteroids compatible with breastfeeding. |
| Teratogenic Risk | Anusol HC (hydrocortisone acetate 1%) is a topical corticosteroid. Systemic absorption is minimal with recommended use. However, prolonged or excessive use may lead to systemic effects. Corticosteroids cross the placenta. Animal studies show corticosteroids are teratogenic (cleft palate). First trimester: Theoretical risk; avoid. Second/third trimester: Use only if clearly needed; prolonged use may cause fetal adrenal suppression. No adequate human studies. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to hydrocortisone or any component of the formulation","Uncontrolled anorectal infection (bacterial, fungal, viral, including herpes simplex or tuberculous)","Fungal infections (except with concomitant antifungal therapy if indicated)","Viral infections (e.g., vaccinia, varicella, herpes simplex) in the area of application","Perforated anus or fistula (relative contraindication due to risk of systemic absorption and infection)"]
| Precautions | ["Systemic absorption may cause reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome, hyperglycemia, or glucosuria, especially with prolonged use, large body surface area application, or occlusive dressings.","Local adverse reactions including skin atrophy, telangiectasias, hypopigmentation, and secondary infection may occur.","Use with caution in patients with pre-existing skin atrophy, or infections (avoid if active untreated bacterial, fungal, or viral infection is present in the application area).","Discontinue if irritation or sensitization develops; appropriate antifungal or antibacterial therapy should be instituted if needed.","Pediatric patients may absorb proportionally larger amounts due to higher skin-to-body mass ratio, increasing susceptibility to systemic toxicity and HPA axis suppression.","Rectal administration may cause burning, itching, or discomfort; discontinue if severe."] |
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| Fetal Monitoring | No specific monitoring required for topical use. If used long-term or on large areas, monitor for maternal adrenal suppression and fetal growth restriction. In neonates, monitor for signs of adrenal suppression if maternal prolonged high-dose use. |
| Fertility Effects | No known adverse effects on fertility from topical hydrocortisone. Systemic corticosteroids may cause menstrual irregularities; topical use unlikely to affect fertility. |
| Food/Dietary | No clinically relevant food interactions. Avoid spicy or greasy foods if they exacerbate symptoms, but no specific dietary restrictions required. |
| Clinical Pearls | Anusol HC is a combination product containing hydrocortisone, a corticosteroid, and pramoxine, a local anesthetic. It is used for relief of hemorrhoidal and perianal inflammation and pruritus. Limit use to 7 days to avoid skin atrophy and systemic absorption. Do not apply to infected areas without concomitant antifungal/antibacterial therapy. |
| Patient Advice | Apply a small amount to the affected area 3-4 times daily, or after each bowel movement. · Do not use for more than 7 days unless directed by a doctor. · Avoid contact with eyes; if contact occurs, rinse thoroughly with water. · Inform your doctor if symptoms persist or worsen after 7 days, or if rectal bleeding occurs. · Do not share this medication with others; it is for external use only. · Store at room temperature away from moisture and heat. |