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# Amfetamine

A stimulant that releases dopamine and noradrenaline from nerve endings. Used for ADHD and narcolepsy; high abuse potential.

Updated 2026-11-01

- Class: [ADHD medicines](https://durgical.com/en/pharmacology/classes/adhd-medicines/)
- Transporter: Vesicular monoamine transporter 2 (VMAT2) and the dopamine and noradrenaline transporters
- ATC code: N06BA01

Also called: Amphetamine

⇄**Vesicular monoamine transporter 2 (VMAT2) and the dopamine and noradrenaline transporters**Amfetamine

ⓘ The figure shows dextroamphetamine (the S-enantiomer) bound to the human vesicular monoamine transporter VMAT2.

**Target in 3D:** Vesicular monoamine transporter 2 (VMAT2) and the dopamine and noradrenaline transporters. PDB structure 9W8F (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/9W8F) · Drag to rotate · pinch to zoom

## 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 →](https://durgical.com/en/conditions/obesity/)

## Adverse effects

### Common

- Reduced appetite and weight loss
- Insomnia
- Dry mouth
- Nervousness and irritability
- Faster heart rate and higher blood pressure

### Serious (rare, important)

- Abuse, misuse and addiction (boxed warning; controlled substance)
- Sudden death in people with structural heart disease; raised blood pressure and heart rate
- New psychosis or mania, or worsening of existing psychosis
- Peripheral vasculopathy including Raynaud's phenomenon
- Slowed growth in children
- Serotonin syndrome with serotonergic drugs or CYP2D6 inhibitors

## 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.

## Memory aid

Methylphenidate closes the drain; amphetamine also opens the tap (vesicle release and reverse transport).

## 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.

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## Related drugs

- [Methylphenidate](https://durgical.com/en/pharmacology/methylphenidate/)
- [Atomoxetine](https://durgical.com/en/pharmacology/atomoxetine/)

## Related conditions

- [Obesity](https://durgical.com/en/conditions/obesity/)

[← Back to the class: ADHD medicines](https://durgical.com/en/pharmacology/classes/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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=20735c2e-6304-425f-a4e4-584f6f90d6a0) (DailyMed (U.S. National Library of Medicine), 2026); [Amphetamine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a616004.html) (MedlinePlus (U.S. National Library of Medicine), 2026).

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Representative model, for educational purposes only.

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