Products
Lisdexamphetamine (LDX) was approved in many countries in March 2014 in capsule form (Elvanse). It has been available in the United States since 2007 (Vyvanse). The dosage form is non-retarded, unlike other ADHD medications. Continuous release is achieved with the conversion of the prodrug. Lisdexamphetamine is legally classified as a narcotic and therefore requires an aggravated prescription.
Structure and properties
Lisdexamphetamine (C15H25N3O, Mr = 263.8 g/mol) consists of the enantiomerically pure dexamphetamine covalently bound to the amino acid lysine via a peptide bond. It is a prodrug that is continuously hydrolyzed enzymatically in the blood in erythrocytes to the active drug D-amphetamine. Lysine does not contribute to the therapeutic effect. Lisdexamphetamine exists as lisdexamphetamine dimesilate, a white powder that is soluble in water.
Effects
Lisdexamfetamine (ATC N06BA12) is effective against ADHD symptomatology. The mechanism of action is not fully understood. Dexamphetamine inhibits the reuptake of norepinephrine and dopamine into the presynaptic neuron and increases the concentration of monoamines in the synaptic cleft. In addition, it promotes the release of neurotransmitters from the presynapse.
Indications
- As a second-line agent for the treatment of attention-deficit/hyperactivity disorder ADHD.
- Binge eating (initial U.S. approval in 2015).
Dosage
According to the professional information. The capsules are taken once a day in the morning and independently of meals. The contents of the capsules can also be used to prepare a drink to be consumed immediately.
Abuse
Like other amphetamines, lisdexamphetamine can be abused as a stimulant intoxicant and become addictive. However, it has a lower potential for abuse because the active ingredient is released continuously and more slowly.
Contraindications
Numerous precautions must be observed during use. Full details can be found in the drug label.
Adverse effects
Possible adverse effects include lack of appetite, weight loss, diarrhea, dry mouth, nausea, abdominal pain, vomiting, anxiety, dizziness, headache, irritability, and insomnia. The drug may rarely cause serious side effects such as cardiovascular disease (including sudden cardiac death), hypertension, psychiatric disorders, and convulsions.
