BIPHETAMINE 7.5
Clinical safety rating
cautionComprehensive clinical and safety monograph for BIPHETAMINE 7.5 (BIPHETAMINE 7.5).
Biphetamine 7.5 is a combination of amphetamine enantiomers (dextroamphetamine and levoamphetamine) that increase synaptic concentrations of dopamine and norepinephrine by inhibiting presynaptic reuptake and promoting release into the synaptic cleft.
| Metabolism | Hepatic metabolism via CYP2D6, deamination, and glucuronidation; major metabolites include 4-hydroxyamphetamine and hippuric acid. |
| Excretion | Renal: ~70-90% unchanged and as active metabolites; minor fecal elimination. Acidic urine (pH <5.6) increases excretion; alkaline urine (pH >7.0) decreases it. |
| Half-life | 6-8 hours (amphetamine moiety), 10-13 hours (dextroamphetamine); clinical effects may outlast serum levels due to accumulation. |
| Protein binding | ~16-20%; primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 4-5 L/kg; extensive tissue distribution with high CNS penetration. |
| Bioavailability | PO: 75-100% (immediate-release); food delays absorption but does not affect total AUC. |
| Onset of Action | PO: 30-60 minutes (immediate-release formulation); peak effect 1-3 hours. |
| Duration of Action | 4-6 hours (immediate-release); clinical monitoring of blood pressure and appetite suppression noted for up to 8 hours. |
| Molecular Weight | 135.21 |
Initial 7.5 mg orally once daily in the morning, titrated based on response and tolerability. Maximum daily dose is 30 mg.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | GFR 15-29 mL/min: 50% of normal dose; GFR <15 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | Children 6-17 years: initial 2.5 mg orally once daily; may increase by 2.5-5 mg weekly; maximum 30 mg daily. |
| Geriatric use | Start at 2.5 mg orally once daily; increase by 2.5 mg weekly as tolerated; monitor for cardiovascular effects and insomnia. |
| 1st trimester | Avoid: Associated with increased risk of cardiac malformations and neural tube defects. |
| 2nd trimester | Avoid: Risk of fetal growth restriction and preterm delivery. |
| 3rd trimester | Avoid: May cause neonatal withdrawal syndrome and persistent pulmonary hypertension. |
Clinical note
Comprehensive clinical and safety monograph for BIPHETAMINE 7.5 (BIPHETAMINE 7.5).
| Placental transfer | High: Readily crosses placenta via passive diffusion. |
| Breastfeeding | Contraindicated due to excretion into breast milk; may cause agitation, poor feeding, and sleep disturbances in the infant. |
| Lactation Rating | L5 |
| Teratogenic Risk | Pregnancy category C. First trimester: possible increased risk of congenital malformations (e.g., cardiac, orofacial clefts) based on limited human data and animal studies. Second and third trimesters: risk of fetal growth restriction, preterm delivery, and neonatal withdrawal symptoms (including irritability, hyperexcitability). Use only if potential benefit justifies risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of central nervous system stimulation. Fetal monitoring includes serial ultrasounds to assess growth and amniotic fluid volume, and fetal heart rate monitoring in third trimester. |
| Fertility Effects | No well-controlled studies. Theoretical possibility of reversible impairment of spermatogenesis or ovarian function based on animal studies. Clinical significance unclear. |
■ FDA Black Box Warning
WARNING: ABUSE AND DEPENDENCE. Amphetamines have a high potential for abuse; prolonged use may lead to drug dependence; misuse may cause sudden death or serious cardiovascular events.
| Serious Effects |
History of substance abuseCardiovascular disease (e.g., hypertension, arrhythmias)HyperthyroidismGlaucomaAgitated statesConcurrent use of MAOIs or within 14 daysPregnancyBreastfeeding
| Precautions | Serious cardiovascular events: sudden death, stroke, myocardial infarction in patients with structural cardiac abnormalities or other serious heart problems., Blood pressure and heart rate increase may occur; monitor for hypertension and tachycardia., Psychiatric adverse reactions: exacerbation of pre-existing psychosis, mania, aggression, or new psychotic/manic symptoms., Long-term suppression of growth in children; monitor height and weight., Seizures: may lower seizure threshold; discontinue if seizures occur., Peripheral vasculopathy: Raynaud's phenomenon; monitor for digital changes. |
| Food/Dietary | Avoid high-fat meals as they may delay absorption. Avoid excessive caffeine intake as it may potentiate stimulant effects and increase anxiety. Ensure adequate hydration to reduce the risk of dry mouth and constipation. No specific foods are contraindicated, but a balanced diet is recommended to mitigate appetite suppression. |
| Clinical Pearls | Biphetamine 7.5 is a fixed-dose combination of amphetamine and dextroamphetamine (ratio 1:1) used for ADHD. Monitor for cardiovascular adverse effects including hypertension, tachycardia, and sudden cardiac death, especially in patients with structural cardiac abnormalities. Avoid in patients with a history of drug abuse due to high abuse potential. Use with caution in patients with bipolar disorder as it may induce manic episodes. Assess for growth suppression in pediatric patients during long-term therapy. |
| Patient Advice | Take the medication exactly as prescribed; do not increase the dose or frequency without consulting your doctor. · Avoid taking this medication late in the day to prevent sleep disturbances. · Report any chest pain, shortness of breath, or fainting immediately. · Do not stop abruptly; taper under medical supervision to avoid withdrawal symptoms. · Store in a secure location away from children and others to prevent misuse. · Attend regular follow-ups for blood pressure, heart rate, and growth monitoring (in children). |
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