VANTRELA ER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VANTRELA ER (VANTRELA ER).
Norepinephrine reuptake inhibitor and alpha-2 adrenergic receptor agonist; increases norepinephrine and serotonin availability in the prefrontal cortex.
| Metabolism | Primarily metabolized via CYP2D6 to 4-hydroxyviloxazine; also minor pathways via CYP3A4 and CYP2C19. |
| Excretion | Primarily renal (70-80% as unchanged drug) with 10-15% biliary/fecal elimination. |
| Half-life | Approximately 24 hours (range 20-30 hours) allowing once-daily dosing; steady state reached in 5-7 days. |
| Protein binding | Approximately 90% bound to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | 0.2 L/kg (low Vd indicating limited tissue distribution and high plasma protein binding). |
| Bioavailability | Oral: 85-95% due to extended-release formulation; absolute bioavailability not established for IV route. |
| Onset of Action | Oral: 30-60 minutes for peak effect; therapeutic levels achieved within 2-4 hours. |
| Duration of Action | 24 hours due to extended-release formulation; clinical effect maintained over dosing interval with consistent plasma levels. |
VANTRELA ER (cialoxine sodium) 250 mg orally once daily with evening meal; maximum dose 500 mg per day.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 50% (max 250 mg/day). GFR <30 mL/min: not recommended (no data). |
| Liver impairment | Child-Pugh Class B or C: contraindicated (no safety data). Class A: use normal dosing with caution. |
| Pediatric use | Not approved for patients under 18 years (safety and efficacy not established). |
| Geriatric use | No specific dose adjustment; monitor renal function due to age-related decline; initiate at 125 mg daily if CrCl <60 mL/min. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VANTRELA ER (VANTRELA ER).
| Breastfeeding | Excreted into human milk; M/P ratio unknown. Infants exposed via breast milk may experience sedation and respiratory depression. Discontinue breastfeeding or drug, considering importance of drug to mother. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Risk of major malformations not established but animal studies show increased fetal loss and reduced fetal weight. Second/third trimester: Potential for neonatal opioid withdrawal syndrome with chronic use. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
May increase the risk of suicidal ideation/suicidal behavior in pediatric/adolescent patients with ADHD; monitor closely for worsening of depression, suicidal thoughts/behaviors, or unusual changes in mood/behavior.
| Serious Effects |
Concomitant use with MAOIs or within 14 days of MAOI discontinuation; uncontrolled hypertension; hypersensitivity to viloxazine or any excipients.
| Precautions | Increased blood pressure and heart rate; suicidal thoughts/behaviors in children/adolescents; activation of mania in patients with bipolar disorder; cardiovascular effects including hypertension, tachycardia, and QT prolongation; priapism; glaucoma; urinary retention; hepatic impairment. |
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| Fetal Monitoring |
| Monitor maternal respiratory status, sedation level, and bowel function. Assess fetal growth and well-being via ultrasound if chronic use. Monitor neonatal for withdrawal symptoms if used near term. |
| Fertility Effects | Animal studies show decreased fertility and increased preimplantation loss at high doses. Human data insufficient; potential for hormonal disruption due to opioid receptor interaction. |