ACTHREL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACTHREL (ACTHREL).
ACTHREL (corticorelin ovine triflutate) is a synthetic analog of corticotropin-releasing hormone (CRH). It binds to CRH receptors in the anterior pituitary, stimulating the secretion of adrenocorticotropic hormone (ACTH). ACTH then acts on the adrenal cortex to release cortisol and other corticosteroids.
| Metabolism | Metabolized by peptidases in plasma and tissues; not primarily hepatic or renal. |
| Excretion | Primarily renal elimination of intact peptide; <5% biliary/fecal. |
| Half-life | 2.0–3.0 hours; correlates with duration of cortisol stimulation. |
| Protein binding | ~25% bound to albumin; negligible to other proteins. |
| Volume of Distribution | 0.4–0.5 L/kg; reflects distribution primarily into extracellular fluid. |
| Bioavailability | IM: ~100% (comparable to IV); not administered orally. |
| Onset of Action | Bolus IV: 5–15 minutes; 10–20 minutes after IM administration. |
| Duration of Action | Cortisol elevation persists 2–3 hours post-IV; up to 4 hours after IM. |
1 mcg/kg IV bolus over 1-2 minutes, followed by a 2-mcg/kg IV infusion over 15 minutes. Alternatively, 1 mcg/kg IV bolus over 1-2 minutes for cosyntropin stimulation test.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required; use caution in severe renal impairment (eGFR <30 mL/min/1.73 m²) due to limited data. |
| Liver impairment | No dose adjustment for Child-Pugh A or B; not studied in Child-Pugh C. |
| Pediatric use | Not approved for use in pediatric patients; efficacy and safety not established. |
| Geriatric use | No specific dose adjustment; consider lower initial doses due to potential increased sensitivity and comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ACTHREL (ACTHREL).
| Breastfeeding | It is not known whether corticorelin ovine is excreted in human milk. Due to the short half-life (approximately 15 minutes) and diagnostic single-dose use, significant excretion is unlikely. However, caution is advised. M/P ratio is not available. The American Academy of Pediatrics considers corticorelin's structural analog CRH as likely compatible with breastfeeding, but no specific data exist. |
| Teratogenic Risk | ACTHREL (corticorelin ovine triflutate) is a synthetic corticotropin-releasing hormone (CRH) used for diagnostic purposes. There are no adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. As a CRH analog, it may theoretically affect fetal hypothalamic-pituitary-adrenal axis development. Risk cannot be ruled out; use only if clearly needed. First trimester: Potential unknown effects on organogenesis. Second and third trimesters: Possible influence on fetal stress response and parturition timing. Post-marketing data insufficient. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to corticorelin or any component of the formulation"]
| Precautions | ["May cause anaphylaxis or hypersensitivity reactions","Use with caution in patients with asthma or other allergic conditions","False positive/negative results may occur; consider other diagnostic tests","Not for therapeutic use; diagnostic only"] |
| Food/Dietary | No specific food interactions. However, advise patient to fast for 8-12 hours before the test as per clinical protocol to avoid interference with cortisol measurement. |
| Clinical Pearls |
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| Fetal Monitoring | Monitor maternal vital signs (blood pressure, heart rate) during and after administration due to potential flushing, hypotension, or tachycardia. Fetal heart rate monitoring is not routinely required but may be considered in high-risk pregnancies. No specific fetal monitoring guidelines exist for diagnostic use. |
| Fertility Effects | No studies have assessed the effect of corticorelin ovine on fertility. As a CRH analog, it may transiently alter pituitary gonadotropin secretion, but single diagnostic doses are unlikely to have lasting effects on fertility. No data on male or female fertility impairment. |
| Administer ACTHREL as a single IV or IM injection. Monitor cortisol levels at 30 and 60 minutes post-injection. Avoid in patients with recent pituitary surgery or known hypersensitivity. False positives may occur with concurrent use of corticosteroids or estrogen. |
| Patient Advice | This test measures how well your pituitary gland and adrenal glands respond to stress. · You may experience temporary redness, swelling, or pain at the injection site. · Report any signs of allergic reaction such as hives, difficulty breathing, or swelling of the face or throat. · Inform your healthcare provider if you have had a recent pituitary surgery or are taking any corticosteroid medications. |