DEXTROSTAT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DEXTROSTAT (DEXTROSTAT).
Dextroamphetamine is a central nervous system stimulant that promotes release of dopamine and norepinephrine from presynaptic neurons, and inhibits their reuptake, thereby increasing synaptic concentrations of these neurotransmitters.
| Metabolism | Primarily metabolized by hepatic CYP2D6 enzymes to inactive metabolites; also undergoes deamination and oxidation. |
| Excretion | Primarily renal (approximately 90% as unchanged drug and metabolites); minor biliary/fecal elimination (<10%). |
| Half-life | Terminal elimination half-life is approximately 10-13 hours in adults, 6-8 hours in children. Extended duration allows once-daily dosing in some patients. |
| Protein binding | 15-40% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 3-4 L/kg, suggesting extensive tissue distribution. |
| Bioavailability | Oral: approximately 60-70% due to first-pass metabolism; extended-release formulations have comparable bioavailability. |
| Onset of Action | Oral immediate-release: 30-60 minutes; oral extended-release: 1-2 hours. |
| Duration of Action | Immediate-release: 4-6 hours; extended-release: 8-12 hours. Duration varies with individual metabolism and formulation. |
5-60 mg orally per day in divided doses, typically 5-10 mg 2-3 times daily, maximum 60 mg/day.
| Dosage form | TABLET |
| Renal impairment | No specific guideline; use with caution and monitor for adverse effects in severe renal impairment (eGFR <30 mL/min/1.73m²). |
| Liver impairment | No specific guideline; use with caution in severe hepatic impairment (Child-Pugh C) due to increased risk of toxicity. |
| Pediatric use | For ADHD: Children 6 years and older, start with 5 mg once or twice daily, increase by 5 mg weekly as tolerated; maximum 40 mg/day. Weight-based: 0.3-0.6 mg/kg/day. |
| Geriatric use | Start at lower doses, e.g., 2.5 mg once or twice daily, due to increased sensitivity and risk of side effects; monitor blood pressure and cardiac status. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DEXTROSTAT (DEXTROSTAT).
| Breastfeeding | Amphetamines are excreted in human milk. M/P ratio not established. Breastfeeding not recommended due to potential adverse effects in infants including irritability, poor feeding, and growth suppression. |
| Teratogenic Risk | First trimester: Limited data, but amphetamine use is associated with increased risk of premature delivery and low birth weight. Second and third trimesters: Risk of fetal growth restriction, increased neonatal heart rate, and neonatal withdrawal syndrome. Avoid use during pregnancy unless potential benefit justifies risk. |
■ FDA Black Box Warning
High potential for abuse and dependence. Prolonged use may lead to drug dependence. Misuse may cause sudden death or serious cardiovascular events.
| Serious Effects |
["Hypersensitivity to amphetamines or any component of the formulation.","Concurrent use or within 14 days of monoamine oxidase inhibitors (MAOIs) due to hypertensive crisis.","Advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, glaucoma, agitated states, history of drug abuse."]
| Precautions | ["Serious cardiovascular events including sudden death in patients with pre-existing structural cardiac abnormalities.","Blood pressure and heart rate increase; monitor for hypertension and tachycardia.","Psychiatric adverse events including exacerbation of pre-existing psychosis, mania, or aggression.","Seizures: may lower seizure threshold.","Peripheral vasculopathy including Raynaud's phenomenon.","Serotonin syndrome risk if used with serotonergic drugs.","Growth suppression in children; monitor growth during long-term use."] |
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| Fetal Monitoring |
| Monitor for fetal growth and development via serial ultrasound; assess for signs of prematurity and low birth weight. Monitor maternal blood pressure and heart rate. |
| Fertility Effects | May impair fertility in animal studies; human data insufficient. Potential for anovulation or menstrual irregularities. |