VYKAT XR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VYKAT XR (VYKAT XR).

How it works

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.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for VYKAT XR (VYKAT XR).

Breastfeeding	Amphetamines are excreted in human milk. M/P ratio not established. Potential for adverse effects in breastfed infant (irritability, poor weight gain). Decision to breastfeed should consider importance of drug to mother and potential infant risks.
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.

Warnings & precautions

■ 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.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to amphetamine or other components","Concurrent use or within 14 days of discontinuing monoamine oxidase inhibitors (MAOIs)","Advanced arteriosclerosis","Symptomatic cardiovascular disease","Moderate to severe hypertension","Hyperthyroidism","Glaucoma","Agitated states","History of drug abuse"]

Clinical Precautions

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"]

Clinical Tips & Counseling

Drug interactions

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VYKAT XR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VYKAT XR (VYKAT XR).

How it works

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for VYKAT XR (VYKAT XR).

Breastfeeding	Amphetamines are excreted in human milk. M/P ratio not established. Potential for adverse effects in breastfed infant (irritability, poor weight gain). Decision to breastfeed should consider importance of drug to mother and potential infant risks.
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.