CORTICOTROPIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CORTICOTROPIN (CORTICOTROPIN).
Corticotropin (ACTH) stimulates the adrenal cortex to release cortisol, corticosterone, aldosterone, and androgens via activation of melanocortin 2 receptor (MC2R) in the zona fasciculata and reticularis.
| Metabolism | Metabolized by tissue peptidases; half-life approximately 15-20 minutes (intramuscular). |
| Excretion | Primarily metabolized in tissues via proteolysis; negligible renal excretion of intact hormone (<5%); urinary metabolites include small peptide fragments. |
| Half-life | 15-30 minutes (intravenous); clinically, duration of action (via adrenal stimulation) exceeds half-life due to sustained cAMP-mediated effects. |
| Protein binding | Negligible (<10%); primarily bound to albumin with low affinity. |
| Volume of Distribution | 0.4-0.6 L/kg; distributes primarily into extracellular fluid. |
| Bioavailability | Intramuscular: ~70%; Subcutaneous: ~60%; Oral: <1% (not clinically used). |
| Onset of Action | Intravenous: 15 minutes; Intramuscular: 30 minutes; Subcutaneous: 30-60 minutes. |
| Duration of Action | Intravenous: 2-4 hours; Intramuscular: 4-6 hours; Subcutaneous: 4-6 hours; effects on cortisol secretion last longer due to delayed feedback. |
40-80 units IM or SC every 24-72 hours; dose adjusted based on response.
| Dosage form | INJECTABLE |
| Renal impairment | No specific guidelines; use caution in severe renal impairment due to fluid/electrolyte disturbances. |
| Liver impairment | No specific guidelines; use caution in severe hepatic impairment. |
| Pediatric use | 0.2-0.4 units/kg IM or SC every 24-72 hours; maximum 80 units/day. |
| Geriatric use | Initiate at lower end of dosing range; monitor for fluid retention and electrolyte imbalance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CORTICOTROPIN (CORTICOTROPIN).
| Breastfeeding | Corticotropin is not detected in breast milk in significant amounts; M/P ratio is unknown. However, caution is advised due to potential effects on maternal adrenal function and infant cortisol levels. Use only if clearly needed and monitor infant for signs of adrenal suppression. |
| Teratogenic Risk | Corticotropin (ACTH) is generally not associated with major teratogenicity in humans, but animal studies show increased risk of cleft palate and placental insufficiency. First trimester: theoretical risk of cleft palate (low incidence). Second/third trimesters: risk of fetal adrenal suppression, intrauterine growth restriction (IUGR), and preterm birth due to maternal hypertension/hyperglycemia. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to corticotropin or porcine-derived proteins; scleroderma; osteoporosis; systemic fungal infections; ocular herpes simplex; recent surgery; history of peptic ulcer; congestive heart failure; hypertension; tuberculosis (active or latent); diabetes mellitus; psychoses; vaccinia or exanthematous diseases; uncontrolled infections.
| Precautions | May cause suppression of hypothalamic-pituitary-adrenal (HPA) axis with prolonged use; increased risk of infections; masking of signs of infection; gastrointestinal perforation; hypersensitivity reactions; edema due to mineralocorticoid effects; behavioral/mood changes; osteoporosis; growth suppression in children. |
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| Fetal Monitoring | Monitor maternal blood pressure, blood glucose, and electrolytes. Assess for signs of infection or adrenal suppression. Fetal monitoring includes serial growth ultrasound (every 4-6 weeks for IUGR), and consider nonstress testing or biophysical profile in third trimester if placental insufficiency suspected. |
| Fertility Effects | Corticotropin may disrupt hypothalamic-pituitary-adrenal axis and gonadotropin secretion, potentially causing anovulation, menstrual irregularities, and reduced fertility. Reversible upon discontinuation. |