VYKAT XR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VYKAT XR (VYKAT XR).
VYKAT XR is a fixed-dose combination of amphetamine and dextroamphetamine, which are central nervous system (CNS) stimulants. They increase the synaptic concentrations of norepinephrine and dopamine by blocking their reuptake and promoting their release from presynaptic neurons.
| Metabolism | Amphetamine and dextroamphetamine are primarily metabolized by cytochrome P450 (CYP) isoenzymes, including CYP2D6, and also undergo deamination and oxidation. |
| Excretion | Primarily renal elimination as unchanged drug and metabolites; approximately 65% of the dose is excreted in urine and 35% in feces via biliary secretion. |
| Half-life | The terminal elimination half-life is approximately 20-22 hours in steady state, allowing for once-daily dosing. Half-life may be prolonged in patients with renal impairment. |
| Protein binding | Approximately 95-99% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 2-4 L/kg, indicating extensive extravascular distribution and tissue binding. |
| Bioavailability | Oral bioavailability is approximately 60-70% for the extended-release formulation, with food slightly increasing absorption (AUC increase by 10-20%). |
| Onset of Action | Oral (extended-release): Onset of therapeutic effect is typically observed within 2-4 hours after the first dose, with steady-state efficacy achieved by day 3-5. |
| Duration of Action | Duration of action is approximately 24 hours, supporting once-daily dosing. The extended-release formulation maintains therapeutic plasma concentrations over the dosing interval. |
| Molecular Weight | 291.36 |
100 mg orally once daily with or without food, administered in the morning.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | eGFR 30-89 mL/min/1.73m²: no adjustment. eGFR 15-29 mL/min/1.73m²: dose reduction to 50 mg once daily. eGFR <15 mL/min/1.73m² or dialysis: not recommended. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce to 50 mg once daily. Child-Pugh Class C: not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients under 18 years. |
| Geriatric use | For patients >65 years, start at 50 mg once daily; titrate to 100 mg once daily based on tolerability. |
| 1st trimester | Avoid use in first trimester unless clearly indicated. Limited human data; animal studies show reproductive toxicity. |
| 2nd trimester | Use only if potential benefit justifies risk. Consider alternatives. |
| 3rd trimester | Use only if potential benefit outweighs risk. May cause adverse effects in fetus. |
Clinical note
Comprehensive clinical and safety monograph for VYKAT XR (VYKAT XR).
| Placental transfer | Crosses placenta in animal studies. Likely crosses in humans. |
| Breastfeeding | Present in breast milk. Not recommended during breastfeeding due to potential for adverse effects in infant. |
| Lactation Rating |
■ FDA Black Box Warning
WARNING: ABUSE AND DEPENDENCE. CNS stimulants, including VYKAT XR, have a high potential for abuse and dependence. Assess the risk of abuse prior to prescribing and monitor for signs of abuse and dependence while on therapy.
| Serious Effects |
Hypersensitivity to active substance or excipientsConcomitant use with MAOIsSevere cerebrovascular disease
| Precautions | Serious cardiovascular events including sudden death, stroke, and myocardial infarction in patients with pre-existing structural cardiac abnormalities or other serious heart problems, Blood pressure and heart rate increases, Psychiatric adverse events including exacerbation of pre-existing psychosis, mania, and new-onset aggressive behavior or hostility, Seizures in patients with a history of seizures, Serotonin syndrome when co-administered with serotonergic drugs, Suppression of growth in pediatric patients requiring regular monitoring, Peripheral vasculopathy including Raynaud's phenomenon, Long-term suppression of growth in children |
| Food/Dietary | Avoid high-fat meals close to dosing; may delay absorption. No specific food restrictions otherwise. |
Loading safety data…
| L5 |
| Teratogenic Risk | First trimester: Amphetamines are associated with increased risk of major congenital anomalies, including cardiac malformations (e.g., septal defects). Second and third trimesters: Risk of preterm delivery, low birth weight, and neonatal withdrawal syndrome (irritability, poor feeding, hyperactivity). Use only if benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of central nervous system stimulation. Assess fetal growth via ultrasound and monitor for preterm labor. Evaluate neonate for withdrawal symptoms after delivery. |
| Fertility Effects | Amphetamines may impair fertility in females via disruption of hypothalamic-pituitary-ovarian axis and in males via decreased sperm count and motility. Reversible upon discontinuation. |
| Clinical Pearls | VYKAT XR (viloxazine extended-release) is a norepinephrine reuptake inhibitor approved for ADHD. Monitor for increased blood pressure and heart rate; consider baseline and periodic cardiovascular assessment. Do not administer with or within 14 days of MAOIs. Avoid use in patients with severe hypertension, tachyarrhythmias, or recent MI. Titrate slowly to reduce side effects; common adverse effects include insomnia, decreased appetite, and nausea. |
| Patient Advice | Take VYKAT XR exactly as prescribed, once daily in the morning with or without food. · Swallow the capsule whole; do not crush, chew, or open. · Avoid alcohol while taking this medication. · Report any chest pain, shortness of breath, or fainting to your doctor immediately. · Do not stop abruptly; may cause withdrawal symptoms. Follow your doctor's plan to taper off. · Keep out of reach of children; store at room temperature. |