Irreversible VMAT2 inhibitor
- Binds VMAT2 essentially permanently
- ➔ recovery waits on synthesis of new transporter — days to weeks
- ⚑ Cannot be titrated off, unlike reversible VMAT2 inhibitors
- Profound depletion; depression and sedation
Drugs with this mechanism (1)
- Reserpine — Historic VMAT2-depleting antihypertensive; caused depression, now rare.