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Rilmenidine
- Development stage
- Phase 4
- Lead developer
- Servier
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Rilmenidine is an oxazoline compound and imidazoline analog that functions as a centrally-acting antihypertensive medication. It is primarily used for the treatment of hypertension. Its mechanism of action involves selective binding to I1 imidazoline receptors in the brainstem, which reduces systemic sympathetic tone and peripheral vascular resistance. Rilmenidine also exhibits a mild agonistic effect on alpha-2 adrenergic receptors. This dual action contributes to its blood pressure-lowering effects while offering a favorable side effect profile compared to less selective alpha-2 agonists. The drug is administered orally. Developed by Servier, Rilmenidine is also being investigated for potential benefits in metabolic syndrome, other cardiovascular-related conditions, chronic kidney disease, and longevity research.
- Brand names
- AlbarelHyperiumIteriumTenaxum
- Other names
- oxaminozolinerilmenidenerilmenidine phosphaterilmenidine dihydrogen phosphate
02
Targets
mAChR (Muscarinic acetylcholine receptors)I1R (Nischarin)Nicotinic Acetylcholine ReceptorI2R (Imidazoline I2 receptor)ADRA2A (α2A)
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