Drug intelligence / Profile preview

zimelidine

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Zimelidine is a selective serotonin reuptake inhibitor (SSRI) and was one of the first drugs in this class to be marketed as an antidepressant. Structurally distinct from tricyclic and tetracyclic antidepressants, it is a pyridylallylamine derivative of brompheniramine. Zimelidine acts by strongly inhibiting the reuptake of serotonin at the presynaptic neuronal membrane, thereby increasing serotonergic neurotransmission in the central nervous system. Its main active metabolite is norzimelidine. Developed by Astra AB in Sweden in the late 1970s and early 1980s under Arvid Carlsson’s leadership, it was introduced to market in 1982 for depression but was withdrawn worldwide within two years due to rare cases of Guillain–Barré syndrome and hypersensitivity reactions[1][2][5]. It showed efficacy comparable to tricyclic antidepressants but with fewer anticholinergic or sedative side effects[3].

Brand names
ZelmidNormudZimeldine
Other names
zimelidineZimeldine
02

Targets

SERT (Sodium-dependent serotonin transporter)

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