Amfetamine !
A stimulant that releases dopamine and noradrenaline from nerve endings. Used for ADHD and narcolepsy; high abuse potential.
Updated 2026-11-01
Also called: Amphetamine
The figure shows dextroamphetamine (the S-enantiomer) bound to the human vesicular monoamine transporter VMAT2.
Mechanism of action
Amphetamine is carried into the nerve terminal by the dopamine and noradrenaline transporters. Inside, it empties the vesicles through VMAT2 and makes the transporters run in reverse, so dopamine and noradrenaline flood the synapse. This gives a stronger stimulant effect than reuptake blockers and a high abuse potential.
- Amphetamine enters the neuron through DAT and NET
- It empties vesicles via VMAT2 into the cytoplasm
- Transporters run in reverse: dopamine and noradrenaline flood out
- More attention and wakefulness; less appetite
Pharmacokinetics
- Absorption
- Taken by mouth
- Metabolism
- Partly by CYP2D6; MAO inhibitors slow its breakdown
Indications
- Attention-deficit/hyperactivity disorder (ADHD)
- Narcolepsy
- Short-term adjunct in obesity that has not responded to other measures (an older labelled use) Obesity →
Adverse effects
Common
- Reduced appetite and weight loss
- Insomnia
- Dry mouth
- Nervousness and irritability
- Faster heart rate and higher blood pressure
Contraindications
- Use of an MAO inhibitor now or within the previous 14 days
- Pheochromocytoma
- Hypersensitivity to amphetamines
Key interactions
- MAO inhibitors (including linezolid)
- Hypertensive crisis: contraindicated
- CYP2D6 inhibitors (fluoxetine, paroxetine)
- Higher amphetamine exposure and serotonin syndrome risk
- Lithium
- May blunt amphetamine's stimulant and appetite effects
What is monitored
- Blood pressure and heart rate
- Height and weight in children
- Signs of abuse or diversion
- Mood, psychotic or manic symptoms
Administration and safety
- Different amphetamine salts and mixtures are not interchangeable one-for-one
- Controlled substance: counted, stored securely and documented
Nursing care
- Measures blood pressure, heart rate, height and weight before starting and during treatment
- Asks about heart disease, fainting and family history of sudden death before starting
- Teaches safe storage and disposal and warns against sharing the medicine
- Teaches to report cold, pale or bluish fingers or toes
Pregnancy and breastfeeding
Human data are limited; use in pregnancy weighs the benefit for the mother against possible risks to the fetus.
Test yourself
Think of the answer, then tap the question to see it.
How does amphetamine increase synaptic dopamine?
It enters the neuron, releases dopamine from vesicles via VMAT2 and reverses the dopamine transporter.
Why is amphetamine contraindicated in pheochromocytoma?
It adds catecholamine release to a tumour that already secretes them, with severe hypertension and arrhythmias.
Which antibiotic, acting as an MAO inhibitor, must not be combined with amphetamine?
Linezolid.
Related drugs
Related conditions
← Back to the class: ADHD medicines
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - AMPHETAMINE SULFATE tablet (DailyMed (U.S. National Library of Medicine), 2026); Amphetamine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026).
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Representative model, for educational purposes only.