Zimelidine | Genelabs.com

Zimelidine has been banned worldwide due to serious, sometimes fatal, cases of central and/or peripheral neuropathy known as Guillain-Barré syndrome and due to a peculiar hypersensitivity reaction involving many organs including skin exanthema, flu-like symptoms, arthralgias, and sometimes eosinophilia. Additionally, zimelidine was charged to cause an increase in suicidal ideation and/or attempts among depressive patients. After its ban, it was succeeded by fluvoxamine and fluoxetine (derived from the antihistamine diphenhydramine) in that order, and the other SSRIs.
Categories	Selective Serotonin Reuptake Inhibitors (SSRIs) Antidepressive Agents Serotonin Uptake Inhibitors
Synonyms	(Z)-3-(4'-Bromophenyl)-3-(3''-pyridyl)dimethylallylamine (Z)-3-[1-(p-Bromophenyl)-3-(dimethylamino)propenyl]pyridine (z)-zimelidine Cis-zimelidine Zimeldine

indication

For the treatment of depression.

pharmacology

Zimelidine was the first marketed selective serotonin reuptake inhibitor (SSRI) antidepressant. It is a pyridylallylamine, structurally different from other antidepressants.

mechanism of action

The antidepressant actions of zimelidine are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Zimelidine blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.

half life

8.4 +/- 2.0 hours for the parent compound and 19.4 +/- 3.6 hours for norzimelidine.

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