H.P. ACTHAR GEL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for H.P. ACTHAR GEL (H.P. ACTHAR GEL).
Adrenocorticotropic hormone (ACTH) analog that stimulates adrenal cortex to release cortisol, corticosterone, and aldosterone. Also exerts anti-inflammatory and immunomodulatory effects via melanocortin receptors.
| Metabolism | ACTH is a polypeptide; metabolism primarily by proteolytic degradation in plasma and tissues. Half-life of corticotropin is approximately 15 minutes; prolonged effect due to gel formulation. |
| Excretion | Primarily renal (<5% unchanged; metabolites excreted in urine). Biliary/fecal excretion is negligible. |
| Half-life | Terminal elimination half-life is approximately 15-20 hours for cortisol suppression effect; repository formulation prolongs absorption. |
| Protein binding | ~90-95%, primarily to corticosteroid-binding globulin (CBG) and albumin. |
| Volume of Distribution | Vd ~0.5-1.5 L/kg (wide tissue distribution, including CNS). |
| Bioavailability | IM/SC: ~100% (repository formulation); intra-articular: locally high, systemic absorption negligible. |
| Onset of Action | IM/SC: clinical effect within 6-12 hours (corticosteroid response); intra-articular: 24-48 hours. |
| Duration of Action | Single dose: 24-72 hours (corticosteroid effect); repository effect can last up to 1-3 weeks depending on dose and route. |
80 units subcutaneously or intramuscularly once daily for 2-3 weeks, then taper as per clinical response for infantile spasms; for multiple sclerosis exacerbations, 80-120 units intramuscularly daily for 2-3 weeks.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment guidelines available; use with caution in severe renal impairment due to potential for edema and hypertension. |
| Liver impairment | No specific dose adjustment guidelines available; use with caution in hepatic impairment due to potential for fluid retention. |
| Pediatric use | Infantile spasms: 150 units/m² intramuscularly twice daily for 2 weeks, then taper; other indications: dosing not well-established, use per adult guidelines with caution. |
| Geriatric use | No specific adjustment; monitor for fluid retention, hypertension, and glucocorticoid effects; initiate at lower end of dosing range due to increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for H.P. ACTHAR GEL (H.P. ACTHAR GEL).
| Breastfeeding | Corticosteroids are excreted in breast milk in low concentrations. M/P ratio unknown for ACTH gel. Use caution; consider risk-benefit, especially with high doses. Monitor infant for growth and adrenal function. |
| Teratogenic Risk | Corticosteroids, including ACTH, are associated with increased risk of cleft palate and intrauterine growth restriction, especially during first trimester. Extended use in third trimester may cause fetal adrenal suppression, hypoadrenalism, and transient neonatal adrenal insufficiency. |
■ FDA Black Box Warning
Because of its action, H.P. Acthar Gel may mask signs and symptoms of infection. The use of H.P. Acthar Gel in patients with systemic fungal infection is contraindicated. Immunization procedures should not be undertaken in patients receiving H.P. Acthar Gel, especially high doses, because of possible hazards of neurological complications and lack of antibody response.
| Serious Effects |
Systemic fungal infection; known hypersensitivity to ACTH or porcine proteins; administration of live or live attenuated vaccines in patients receiving immunosuppressive doses; scleroderma; osteoporosis; peptic ulcer disease; congestive heart failure; hypertension; thromboembolic disorders; recent surgery; primary adrenocortical insufficiency; adrenogenital syndrome; vaccinia and exanthematous diseases.
| Precautions | May increase risk of infection; may mask signs of infection; may cause immunosuppression; may cause adrenal insufficiency with prolonged use; may cause Cushing's syndrome; may cause behavioral and mood disturbances; may cause gastrointestinal perforation; may increase cardiovascular risk; may cause osteoporosis; may cause growth suppression in children; may cause electrolyte disturbances; may cause increased intraocular pressure; may cause hypersensitivity reactions; use caution in patients with diabetes, hypertension, renal impairment, myasthenia gravis, or history of tuberculosis. |
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| Fetal Monitoring |
| Monitor maternal blood pressure, glucose levels, weight, and signs of infection. Perform fetal growth ultrasounds if prolonged use. Assess neonatal adrenal function at birth if used near term. |
| Fertility Effects | High-dose corticosteroids may disrupt menstrual cycles and inhibit ovulation. Long-term use may impair fertility. Effects are typically reversible upon dose reduction or discontinuation. |