I1 imidazoline agonist
I1 imidazoline receptor agonist
- If BBB-crossing: medullary sympathetic inhibition → lowers blood pressure
- ↓ Sympathetic tone also improves insulin sensitivity in metabolic syndrome
- If BBB-crossing: medullary sympathetic inhibition → lowers blood pressure
- ↓ Sympathetic tone also improves insulin sensitivity in metabolic syndrome
Drugs with this mechanism (10)
- Agmatine — Endogenous polyamine; NMDA and imidazoline modulator sold as a supplement.
- Clonidine — Central alpha-2 agonist for hypertension, ADHD and withdrawal; sedation and rebound.
- Clonidine ER — Extended-release central alpha-2 agonist for ADHD; sedation and rebound hypertension limit it.
- Dexmedetomidine — Alpha-2 agonist sedative giving cooperative sedation without respiratory depression.
- Dexmedetomidine sublingual — Sublingual dexmedetomidine film for acute agitation in schizophrenia or bipolar disorder.
- Lofexidine — Alpha-2 agonist for opioid-withdrawal symptoms.
- Moxonidine — Central imidazoline I1 agonist for hypertension in some countries; dry mouth and dizziness, with avoidance in heart failure.
- Clonidine ER suspension — Extended-release clonidine liquid for ADHD; sedation and rebound hypertension shape use.
- Rilmenidine — Central imidazoline I1 agonist used for hypertension outside the U.S.; reduces sympathetic activity, with dry mouth and dizziness.
- Tizanidine — Short-acting alpha-2 agonist for spasticity; hypotension and CYP1A2 interactions.
All mechanisms · Open Imidazoline I1 agonist in the interactive console ↗