EXXUA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EXXUA (EXXUA).
Selective allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), reducing glutamate signaling.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2C8. |
| Excretion | Renal (approximately 30% unchanged) and biliary (approximately 70% as metabolites). |
| Half-life | Terminal elimination half-life of 24-30 hours, allowing once-daily dosing. Steady-state reached within 5-7 days. |
| Protein binding | 99.5% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.2 L/kg (range 0.8-1.6 L/kg), indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is approximately 40-50% due to first-pass metabolism. |
| Onset of Action | Oral: 2-4 hours; time to peak effect may take several days for full therapeutic benefit. |
| Duration of Action | Approximately 24 hours, supporting once-daily dosing regimen. Clinical effects persist for duration of dosing interval. |
5 mg orally once daily. If needed, may increase to 10 mg once daily after 4 weeks based on tolerability and response.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | No dose adjustment required for GFR >=30 mL/min. For GFR <30 mL/min or on dialysis, use is not recommended due to lack of data. |
| Liver impairment | Child-Pugh A: No dose adjustment. Child-Pugh B: 2.5 mg once daily. Child-Pugh C: contraindicated. |
| Pediatric use | Not indicated in patients <18 years; safety and efficacy not established. |
| Geriatric use | Start at 2.5 mg once daily; increase cautiously due to potential for decreased renal function and increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EXXUA (EXXUA).
| Breastfeeding | Unknown if excreated in breast milk; risk to infant cannot be excluded. M/P ratio not established. |
| Teratogenic Risk | Teratogenic risk unknown; no human data available. In animal studies, no evidence of harm at clinically relevant doses. |
| Fetal Monitoring | Monitor fetal development via ultrasound; assess neonatal adaptation in third trimester. |
■ FDA Black Box Warning
Increased risk of suicidal thoughts and behaviors in pediatric patients with MDD.
| Serious Effects |
["Concomitant use with MAOIs or within 14 days of MAOI discontinuation","Hypersensitivity to axomadol (EXXUA)"]
| Precautions | ["Suicidal thoughts/behaviors in young adults","Hepatotoxicity","Psychotic symptoms/mania","Seizures","Urinary retention"] |
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| Fertility Effects | No data on fertility impairment in humans; animal studies show no effect on fertility. |