Irreversible VMAT2 inhibitor
- Monoamines cannot be packaged → cytoplasmic degradation → profound depletion
- Binds VMAT2 essentially permanently
- Recovery needs new transporter synthesis — days to weeks
- ⚑ Cannot be titrated off, unlike reversible VMAT2 inhibitors
- Depression, parkinsonism, orthostatic hypotension
- Sedation
Drugs with this mechanism (1)
- Reserpine — Historic VMAT2-depleting antihypertensive; caused depression, now rare.
Self-check
- What is needed to recover from irreversible VMAT2 inhibition?
New transporter synthesis, over days to weeks. - Which blood-pressure adverse effect accompanies profound depletion?
Orthostatic hypotension.
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