Dextroamphetamine

Overview

• Dextroamphetamine is a potent central nervous system (CNS) stimulant.
• Used primarily to treat ADHD and narcolepsy.
• Illicit uses: cognitive and athletic performance enhancement, recreational use as an aphrodisiac and euphoriant.

Clinical Data

• Pronunciation: /dkstromftmin/
• Trade Names: Dexedrine, others.
• Pregnancy Category: AU: B3
• Dependence Liability: Physical - none; Psychological - low to moderate.
• Addiction Liability: Moderate to high.
• Routes of Administration: Oral, transdermal, intravenous, insufflation, rectal.
• Drug Class: Stimulant
• Legal Status: Varies by country.

Pharmacokinetics

• Bioavailability: ~90%
• Protein Binding: 15-40%
• Metabolism: CYP2D6, DBH, FMO3
• Onset of Action: IR dosing: 0.5-1.5 hours; XR dosing: 1.5-2 hours
• Elimination Half-life: 9-11 hours; pH-dependent: 7-34 hours
• Duration of Action: IR dosing: 3-6 hours; XR dosing: 8-12 hours
• Excretion: Mainly through kidneys; urinary pH-dependent

Uses

Medical

• Treatment for ADHD and narcolepsy.
• Occasionally used for depression and obesity.

ADHD

• Improves brain development and nerve growth in therapeutic doses.
• Long-term use of stimulants is effective and safe for ADHD treatment.
• Enhances quality of life and academic achievement.

Narcolepsy

• Effective in promoting wakefulness, especially in type 1 narcolepsy.
• Considered a third-line treatment option.

Enhancing Performance

Cognitive Performance

• Modest improvements in working memory, episodic memory, and attention.
• Enhances task saliency and arousal.

Physical Performance

• Improves muscle strength, acceleration, and endurance.
• Delays onset of fatigue and enhances reaction time.

Recreational Use

• Used for its euphoric and aphrodisiac effects.
• High potential for misuse and addiction.

Contraindications

• History of drug abuse, cardiovascular disease, severe agitation or anxiety.
• Conditions like glaucoma, hyperthyroidism, and moderate to severe hypertension.

Side Effects

Physical

• Cardiovascular issues: hypertension, tachycardia.
• Gastrointestinal issues: abdominal pain, nausea.
• Other: appetite loss, dry mouth.

Psychological

• Increased alertness, mood swings, insomnia.
• Anxiety, irritability, and potential for psychosis in high doses.

Addiction and Dependence

• High potential for addiction with recreational use.
• Chronic use can lead to significant neurobiological changes.

Pharmacological Mechanism

• Stimulates neurotransmitter release (dopamine, norepinephrine) and inhibits reuptake.
• Acts via trace amine-associated receptor 1 (TAAR1) and vesicular monoamine transporter 2 (VMAT2).

History and Culture

• First synthesized in 1887; marketed as Benzedrine inhaler in 1932.
• Used in WWII for fatigue.
• Classified as Schedule II in the U.S. in 1970.
• Widely used and prescribed in various forms around the world since.