Stage 7: Stimulants & ADHD Medications
Concept 3 of 8
R7.3

Amphetamine Formulations

Adderall, dextroamphetamine, lisdexamfetamine — different durations, abuse-deterrent prodrug strategy.

Lisdexamfetamine prodrug: pharmacologically inactive until cleaved by red blood cell enzymes. Cannot be activated by snorting or injecting — abuse-deterrent. Steady onset, smooth duration.

Amphetamine formulations parallel the methylphenidate family but with one important pharmacologic addition: amphetamine releases dopamine and norepinephrine directly from presynaptic vesicles, on top of the reuptake inhibition shared with methylphenidate. The clinical effect is similar, but the mechanism is more aggressive.

Drug card
Class
CNS stimulant (amphetamine family)
Mechanism
DAT + NET reuptake inhibition + presynaptic vesicular release of DA/NE (via VMAT2 reversal)
Typical dose
Adderall IR 5-30 mg/day in divided doses; Adderall XR 5-30 mg daily; Vyvanse 30-70 mg daily
Half-life
IR ~10 hours; XR 10-12 hour coverage; Vyvanse 13-14 hour coverage (lisdexamfetamine converted to dextroamphetamine in blood)
FDA indications
ADHD, binge eating disorder (lisdexamfetamine specifically), narcolepsy
Key adverse effects
Appetite suppression, insomnia, irritability, BP/HR elevation, weight loss, growth slowing in children
Representative agents
Mixed amphetamine salts (Adderall IR, Adderall XR), dextroamphetamine (Dexedrine), lisdexamfetamine (Vyvanse — prodrug)

Black box: Schedule II — abuse potential. Cardiovascular events in structural heart disease.

Lisdexamfetamine (Vyvanse) is a prodrug requiring enzymatic activation by red blood cells — cannot be activated by injection or insufflation, making it abuse-deterrent. Often preferred when abuse/diversion is a concern.

Adderall — mixed amphetamine salts. The standard formulation contains 75 percent d-amphetamine and 25 percent l-amphetamine. The mixed enantiomers may produce a slightly different clinical response than pure d-amphetamine for some patients. Available as Adderall IR (4-6 hour duration) and Adderall XR (10-12 hours).

Adderall = mixed amphetamine salts (4:1 d-amphetamine to l-amphetamine). Mixed enantiomers may produce slightly different clinical response than pure d-amphetamine (Dexedrine).

Dexedrine — pure d-amphetamine. The older single-enantiomer form. Less commonly prescribed now than mixed salts but still in use.

Vyvanse (lisdexamfetamine) — the prodrug. This is the pharmacologically clever member of the family. Lisdexamfetamine is pharmacologically inactive until red blood cell enzymes cleave the L-lysine attached to dextroamphetamine. Because the activation requires enzymatic processing, lisdexamfetamine cannot be activated by snorting or injecting — abuse-deterrent by design. Onset is steady and gradual; duration is 13-14 hours. For patients with abuse risk in their history or their environment, Vyvanse is often the preferred amphetamine.

Mechanism in practice

Amphetamines differ from methylphenidate by an additional mechanism — they actively release catecholamines, not just block reuptake — giving a somewhat stronger effect.

Mechanism
Catecholamine reuptake inhibition PLUS active release from presynaptic terminals (reverses the transporter; depletes vesicles)
Effect
Higher synaptic catecholamine concentrations than reuptake blockade alone
Clinical applications
The dual mechanism gives amphetamines a modestly larger effect size than methylphenidate for many patients.
Mechanism
Lisdexamfetamine: prodrug requiring enzymatic cleavage to active dextroamphetamine
Effect
Slow, smooth conversion; consistent exposure; reduced abuse potential
Clinical applications
The prodrug design resists non-oral abuse and smooths the pharmacokinetics — a key formulation advance.
Mechanism
Mixed amphetamine salts and dextroamphetamine, immediate and extended-release
Effect
Range of onset and duration profiles
Clinical applications
Formulation chosen for coverage needs; extended-release lowers abuse liability versus immediate-release.
Mechanism
Catecholamine effects at peripheral and reward sites
Effect
Appetite suppression, insomnia, HR/BP elevation; abuse potential
Clinical applications
Same monitoring as methylphenidate; the active-release mechanism gives a somewhat higher abuse liability per formulation.

Mechanism note: Amphetamines add active catecholamine release to reuptake blockade — a modestly stronger effect than methylphenidate. Lisdexamfetamine's prodrug design is the cleanest answer to the abuse-liability problem.

Vyvanse also carries a unique FDA indication: binge eating disorder. The evidence supports specific binge-day reduction beyond what general appetite suppression would explain. For the patient with BED, Vyvanse is FDA-approved at moderate doses (typically 50-70 mg daily). This is not a weight-loss indication; it is specifically for binge eating reduction.

Lisdexamfetamine's unique indication: binge eating disorder (FDA-approved 2015). Different from appetite suppression as side effect — specific evidence for binge eating reduction beyond general appetite effect.

Side effects across the amphetamine family include appetite suppression (often significant), insomnia, irritability, increased BP and HR. Monitor growth in pediatric patients. Counsel about adequate hydration and nutrition.

The methylphenidate-vs-amphetamine choice is often empirical — try one, switch if inadequate. The Vyvanse-vs-Adderall choice within amphetamines often comes down to abuse risk and cost.

Prescribing reality
Cost
Adderall IR/XR generic ~$15-40/month. Dexedrine generic ~$30-60/month. Vyvanse generic (recent) ~$50-200/month; brand ~$400+/month.
Generic status
Adderall/Dexedrine generic for years. Vyvanse generic since 2023.
Formulary typical
Generics: Tier 1-2. Vyvanse brand: Tier 3 with PA.
Access friction
Schedule II restrictions (see methylphenidate). Stimulant shortages have particularly affected amphetamine formulations 2022-2024. Vyvanse generic supply has been variable since launch.

Prescriber tip: For abuse-deterrence concerns, lisdexamfetamine (Vyvanse) is the choice — generic now available though supply variable. For binge eating disorder, Vyvanse is the FDA-approved option.

The anchor

Amphetamines work via reuptake inhibition plus direct DA/NE release — slightly different mechanism than methylphenidate, similar clinical effect. Lisdexamfetamine prodrug strategy provides abuse deterrence; also uniquely approved for binge eating disorder.

Prove it

Why is lisdexamfetamine considered abuse-deterrent compared to other amphetamine formulations?

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