Lisdexamfetamine dimesylate

Lisdexamfetamine dimesylate (IUPAC name: (2S)-2,6-diamino-N-[(1S)-1-methyl-2-phenylethyl]hexanamide dimethanesulfonate), commonly known by its brand name Vyvanse, is a prodrug of the central nervous system (CNS) stimulant dextroamphetamine. It is used primarily in the treatment of attention deficit hyperactivity disorder (ADHD) and binge eating disorder (BED). Unlike dextroamphetamine, lisdexamfetamine is designed to provide a pharmacokinetic profile that reduces the potential for abuse and provides a prolonged duration of effect, which is beneficial for the treatment of ADHD.

Medical Uses

Lisdexamfetamine is approved for the treatment of ADHD in adults and children over the age of six years. It is also approved for the treatment of moderate to severe binge eating disorder in adults. The effectiveness of lisdexamfetamine in treating ADHD is attributed to its action on the neurotransmitters dopamine and norepinephrine, which are believed to play key roles in attention and behavior regulation.

Pharmacology

Mechanism of Action

Lisdexamfetamine is a prodrug, meaning it is biologically inactive until it is metabolized in the body to produce the active agent, dextroamphetamine. This conversion occurs primarily through hydrolysis in the blood. The active dextroamphetamine then exerts its effects by increasing the concentrations of dopamine and norepinephrine in the brain, which are associated with attention and alertness.

Pharmacokinetics

The pharmacokinetic profile of lisdexamfetamine is characterized by a slow and consistent release of dextroamphetamine into the bloodstream, leading to a prolonged duration of action compared to immediate-release dextroamphetamine formulations. This profile helps to mitigate the potential for abuse and reduces the need for multiple doses throughout the day.

Adverse Effects

Common adverse effects of lisdexamfetamine include dry mouth, insomnia, decreased appetite, weight loss, increased heart rate, and anxiety. It also carries a risk of more serious side effects, such as cardiovascular events, psychiatric disorders, and dependence. Due to these risks, it is classified as a Schedule II controlled substance in the United States.

Contraindications

Lisdexamfetamine is contraindicated in individuals with a history of hypersensitivity to amphetamines or other ingredients in the formulation, as well as in patients with advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, glaucoma, agitated states, or a history of drug abuse.

Interactions

Lisdexamfetamine may interact with monoamine oxidase inhibitors (MAOIs), as well as other drugs that affect neurotransmitter levels in the brain, such as antidepressants and antipsychotics. These interactions can increase the risk of serotonin syndrome, hypertensive crisis, or other adverse effects.

Society and Culture

Legal Status

Lisdexamfetamine is classified as a Schedule II controlled substance in the United States, indicating a high potential for abuse and dependence. Its legal status varies by country, but it is generally subject to strict regulations.

See Also

• Amphetamine
• Attention deficit hyperactivity disorder
• Binge eating disorder
• Central nervous system stimulants