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NEUROLOGY 1988;38:1095
© 1988 American Academy of Neurology

Treatment of neurogenic orthostatic hypotension with amezinium metilsulfate, a new indirect sympathomimetic drug

Kohei Kita, MD and Keizo Hirayama, MD

From the Department of Neurology, Brain Research Institute, Chiba University School of Medicine, Chiba, Japan.

Amezinium metilsulfate is a new, indirectly acting sympathomimetic drug which exclusively affects postganglionic sympathetic neurons and inhibits both intraneuronal monoamine oxidase and norepinephrine reuptake. We examined the short-term effects of amezinium in five patients with severe neurogenic orthostatic hypotension. Single-dose administration of amezinium (10 mg) raised both the supine and sitting mean blood pressures by 15 to 45 mm Hg for 8 hours, with a slight increase in the plasma norepinephrine level. Repeated administration of amezinium (10 to 40 mg/d) produced an increase in sitting blood pressure in three patients and improvement of the orthostatic symptoms in all patients without remarkable recumbent hypertension. The heart rate was increased in two patients. The results indicate that amezinium is of therapeutic value for the treatment of neurogenic orthostatic hypotension. The adrenergic effect of amezinium on the blood pressure and heart rate apparently was related to a slight increase in endogenous norepinephrine in the presence of {alpha}- and ß-adrenoreceptor supersensitivity.

Address correspondence and reprint requests to Dr. Kita, Department of Neurology, Brain Research Institute, Chiba University School of Medicine, 1–8–1 Inohana, Chiba City, Chiba, 280 Japan.

Received September 1,1987. Accepted for publication in final form November 13,1987.

Supported by the grant-in-aid from the Kashiwado Memorial Foundation in Japan.