Central Alpha-2 Agonists
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Overview
Central alpha-2 agonists are antihypertensive medications that work in the brain to reduce sympathetic nervous system outflow. By stimulating alpha-2 adrenergic receptors in the brainstem, they decrease the signals that cause blood vessels to constrict and the heart to beat faster. They are used for hypertension, ADHD, opioid withdrawal, and certain pain conditions.
How do central alpha-2 agonists work?
Central alpha-2 agonists bind to presynaptic alpha-2 adrenergic receptors in the brainstem vasomotor center (particularly the nucleus tractus solitarius and locus coeruleus). This stimulation reduces sympathetic outflow from the central nervous system, resulting in decreased peripheral vascular resistance, heart rate, and blood pressure. The net effect is reduced norepinephrine release from sympathetic nerve terminals throughout the body.
Drugs in this class
- Clonidine (Catapres, Catapres-TTS, Kapvay)