Irreversible VMAT2 inhibitor
- Monoamines cannot be packaged → cytoplasmic degradation → profound depletion
- Recovery needs new transporter synthesis — days to weeks
- Depression, parkinsonism, orthostatic hypotension
- 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.
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