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. |
| Molecular Weight | 135.21 |
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 | Pregnancy category C. Teratogenic effects observed in animal studies; increased risk of cardiovascular anomalies and oral clefting. Use only if benefit outweighs risk. |
| 2nd trimester | Associated with preterm delivery, low birth weight, and withdrawal symptoms (hyperactivity, feeding difficulties). Use only if benefit outweighs risk. |
| 3rd trimester | Neonatal withdrawal syndrome, including irritability, hypotonia, and poor feeding. Risk of premature delivery. Avoid use during third trimester unless essential. |
Clinical note
Comprehensive clinical and safety monograph for DEXTROSTAT (DEXTROSTAT).
| Placental transfer | Dextroamphetamine crosses the placenta. Fetal/maternal ratio approximately 0.5-0.8 based on limited human data. |
| Breastfeeding | Dextroamphetamine is excreted into breast milk in low amounts. Peak milk concentration occurs 2-3 hours after dose. Relative infant dose estimated at 5-10% of maternal weight-adjusted dose. Monitor infant for irritability, poor feeding, and growth. May reduce milk production. Caution is advised; use only if clearly needed. |
■ 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 |
Advanced arteriosclerosisSymptomatic cardiovascular diseaseModerate to severe hypertensionHyperthyroidismGlaucomaAgitated statesHistory of drug abuseDuring or within 14 days of MAOI therapy
| 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. |
| Food/Dietary | Avoid acidic foods and juices (e.g., orange juice, grapefruit juice) within 1 hour of administration as they can reduce absorption. High-fat meals may delay absorption. Avoid alcohol and caffeine as they can exacerbate side effects. |
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| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
| Clinical Pearls | Dextrostat (dextroamphetamine) is a central nervous system stimulant used for ADHD and narcolepsy. Monitor for hypertension, tachycardia, and psychiatric adverse effects. Avoid in patients with structural cardiac abnormalities, cardiomyopathy, or severe anxiety. Taper to discontinue to avoid withdrawal. Use with caution in patients with a history of substance abuse. May reduce seizure threshold. |
| Patient Advice | Take exactly as prescribed; do not increase dose without consulting your doctor. · Avoid taking late in the day to prevent insomnia. · Report any chest pain, shortness of breath, or fainting immediately. · Do not crush or chew extended-release capsules. · Avoid alcohol and over-the-counter cold remedies containing decongestants. · Store in a secure place; misuse can cause serious health problems. |