PURIFIED CORTROPHIN GEL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PURIFIED CORTROPHIN GEL (PURIFIED CORTROPHIN GEL).
Corticotropin (ACTH) stimulates the adrenal cortex to release cortisol, corticosterone, aldosterone, and androgenic steroids. It binds to melanocortin 2 receptors (MC2R) on adrenocortical cells, activating adenylyl cyclase and increasing cAMP, leading to steroidogenesis. Immunomodulatory effects are mediated via melanocortin receptors on immune cells, reducing inflammation.
| Metabolism | Corticotropin is a polypeptide hormone. Its metabolism is primarily via proteolytic degradation in plasma and tissues. No specific cytochrome P450 enzymes are involved. Elimination occurs via renal catabolism. |
| Excretion | Renal: 50-70% as unchanged corticotropin and metabolites; biliary/fecal: minimal (<5%). |
| Half-life | Terminal elimination half-life: approximately 15-20 minutes; clinical context: requires depot formulation for sustained effect. |
| Protein binding | Approximately 15-30% bound to plasma proteins, primarily albumin and beta-globulins. |
| Volume of Distribution | Approximately 0.4-0.6 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | IM: 70-90%; SC: 60-80%; oral: negligible (<1%) due to gastrointestinal degradation. |
| Onset of Action | Intramuscular: 2-4 hours; Subcutaneous: 3-6 hours; onset of adrenal stimulation (cortisol rise) within 15-30 minutes after injection. |
| Duration of Action | 36-48 hours after single IM or SC dose in depot formulation; clinical notes: duration correlates with gel formulation's prolonged absorption. |
40 to 80 units subcutaneously or intramuscularly every 24 to 72 hours, adjusted based on clinical response.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment guidelines; use with caution in severe renal impairment due to risk of fluid retention and electrolyte disturbances. |
| Liver impairment | No specific dose adjustment guidelines; monitor for fluid retention and electrolyte imbalance in severe hepatic impairment. |
| Pediatric use | 0.5 to 1 unit/kg subcutaneously or intramuscularly every 24 hours, not to exceed 40 units daily; alternative regimens may be used per protocol. |
| Geriatric use | Use lower end of dosing range (e.g., 40 units every 48-72 hours) due to increased sensitivity to corticosteroid effects and higher risk of adverse events such as fluid retention and hypertension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PURIFIED CORTROPHIN GEL (PURIFIED CORTROPHIN GEL).
| Breastfeeding | Excretion into breast milk is unknown. Corticotropin is a peptide that is likely degraded in infant GI tract. Use with caution, especially in premature infants. M/P ratio not available. |
| Teratogenic Risk | PURIFIED CORTROPHIN GEL (corticotropin) is pregnancy category C. First trimester: No adequate human studies; animal studies show fetal abnormalities at high doses. Second and third trimesters: Corticosteroids can cause fetal growth restriction, adrenal suppression, and cleft palate; risk may be higher with prolonged use. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to corticotropin or any component of the formulation","Administration of live or live-attenuated vaccines","Scleroderma (systemic sclerosis)","Osteoporosis","Congestive heart failure","Hypertension","Primary adrenocortical insufficiency (Addison's disease)","Adrenogenital syndrome","Recent surgery","Herpes simplex keratitis","Fungal infections","Peptic ulcer disease","Psychoses","Diabetes mellitus (relative contraindication)","Cushing's syndrome (relative contraindication)"]
| Precautions | ["Hypothalamic-pituitary-adrenal (HPA) axis suppression with prolonged use","Cushing's syndrome with chronic administration","Increased susceptibility to infections","Masking signs of infection","Fluid and electrolyte disturbances (e.g., sodium retention, potassium loss)","Gastrointestinal perforation","Increased intraocular pressure and glaucoma","Behavioral and mood disturbances","Thromboembolic events","Vaccine-associated complications: do not administer live vaccines during therapy","Immunosuppression and increased risk of secondary infections"] |
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| Fetal Monitoring | Monitor maternal blood pressure, blood glucose, serum potassium, and signs of infection. Fetal monitoring: growth ultrasound and amniotic fluid assessment if prolonged use. Newborns: monitor for adrenal insufficiency if maternal treatment continued until delivery. |
| Fertility Effects | May cause menstrual irregularities, ovulatory dysfunction, and reduced fertility due to corticosteroid effects on HPA axis and gonadal function. Reversible upon discontinuation. |