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Centrally acting antihypertensives and Rauwolfia alkaloids

9 articles

AYUSH-HR

AYUSH-HR is a coded Ayurvedic polyherbal formulation by India's CCRAS for pre-hypertension (JNC-VII 120-139/80-89 mmHg), tested in a double-blind randomized placebo-controlled trial at three centres, 500 mg twice daily for 12 weeks.

Bethanidine

Bethanidine (betanidine, B.W. 467C60, Esbatal) is a guanidinium sympatholytic antihypertensive, C10H15N3, half-life 9 hours, approved in the UK in 1963 and later discontinued; it resembled guanethidine but caused no diarrhea.

Deserpidine

Deserpidine, a Rauwolfia alkaloid antihypertensive related to reserpine, ATC C02AA05/C02LA03, formula C32H38N2O8, first approved 1957; brands Harmonyl, Oreticyl, Enduronyl; depletes catecholamines.

Guanabenz

Guanabenz (Wytensin) is a centrally acting alpha-2 adrenergic agonist antihypertensive, dosed 8–32 mg/day twice daily; discontinued in the US and investigated for ALS and vanishing white matter.

Guanadrel

Guanadrel (Hylorel) is a discontinued oral postganglionic sympathetic inhibitor, a guanidine analog of guanethidine, FDA-approved in 1982 for mild to moderate hypertension.

Moxonidine

Moxonidine, sold as Physiotens and Cynt, is a centrally acting antihypertensive that stimulates I1-imidazoline receptors in the brainstem; it is approved for mild to moderate hypertension.

Pentolinium

Pentolinium (Ansolysen, pentolonium) is a bisquaternary pyrrolidinium ganglionic blocking agent, a nicotinic acetylcholine receptor antagonist once used for severe hypertension, later for surgical hypotension and autonomic research.

Rescinnamine

Rescinnamine (Moderil) is a Rauwolfia serpentina indole alkaloid antihypertensive, C35H42N2O9, ATC C02AA01, described as an ACE inhibitor by DrugBank; FDA approved 1956, later discontinued.

Urapidil

Urapidil (Ebrantil, B 66256) is a piperazine antihypertensive combining peripheral alpha-1 adrenoceptor blockade with central 5-HT1A agonism, used in Europe and Asia for hypertension and hypertensive emergencies; not marketed in the United States.