Dexamphetamine

Products

Dexamphetamine was reapproved in many countries in 2020 in tablet form (Attentin). Dexamine tablets (5 mg, Streuli) are no longer available. Also available is the prodrug lisdexamphetamine (Elvanse). Drugs containing dexamphetamine are also prepared as an extemporaneous prescription in a pharmacy or ordered by pharmacies from specialized service providers. Dexamphetamine is a narcotic and is subject to enhanced prescription requirements.

Structure and properties

Dexamphetamine sulfate is usually present in drugs as dexamphetamine sulfate (C₁₈H₂₈N₂O₄S), M_r = 368.5), is a white crystalline powder that is readily soluble in water. It is the D- or -enantiomer of the racemate amphetamine. Dexamphetamine is structurally related to the catecholamines and belongs to the phenylethylamines.

Effects

Dextroamphetamine (ATC N06BA02) has indirect sympathomimetic, central stimulant, and appetite suppressant properties. It increases blood pressure, stimulates respiration, and dilates the bronchi. The effects are due to an enhancement of the effects of dopamine and norepinephrine in central nervous system. Dextroamphetamine increases the release and reduces the reuptake of neurotransmitters. The half-life is approximately 10 hours.

Indications for use

Attention deficit hyperactivity disorder ADHD.
Narcolepsy
Obesity (obsolete!)

Dexamphetamine is also used in the military to keep soldiers awake on long missions, especially fighter jet pilots.

Dosage

According to the prescribing information. Treatment is started gradually and the dose is adjusted individually.

Abuse

Dexamphetamine is abused as a stimulant and euphoric intoxicant, smart drug, and doping agent. Because of the health risks, abuse is strongly discouraged. Deaths have been reported.

Contraindications

Hypersensitivity
Glaucoma
Pheochromocytoma
Treatment with MAO inhibitors
Hyperthyroidism or thyrotoxicosis
Major depression, anorexia nervosa, suicidal tendencies, psychotic symptoms, major affective disorder, mania, schizophrenia, psychopathic/borderline personality disorder
Tourette syndromes or similar dystonia.
Bipolar disorders
Cardiovascular diseases, vascular diseases
Porphyria
Drug addiction or alcoholism
Pregnancy and lactation

Full precautions can be found in the drug label.

Interactions

Dexamphetamine has a high potential for drug-drug interactions, for example with MAO inhibitors (contraindicated), antidepressants, sympathomimetics, and neuroleptics.

Adverse effects

Possible adverse effects include (selection):

Cardiovascular: Palpable heartbeats, cardiac arrhythmias, rapid pulse, hypertension, cardiomyopathy with prolonged use, myocardial infarction, sudden death, stroke.
Central nervous system: psychosis, schizophrenia, hyperstimulation, restlessness, nervousness, dizziness, sleep disturbances, euphoria, movement disorders, dysphoria, tremor, headache, worsening of tics, Tourette’s syndrome
Gastrointestinal tract: dry mouth, taste disorders, diarrhea, constipation, lack of appetite, nausea, growth retardation in children.
Eyes: visual disturbances
Musculoskeletal system: joint pain

Dexamphetamine can lead to tolerance and psychological and physical dependence. Stopping too quickly leads to withdrawal symptoms.