Imipramine Hydrochloride

Imipramine hydrochloride, 5-[3-(dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine monohydrochloride (Tofranil), is the lead compound of the TCAs. It is also a close relative of the antipsychotic phenothiazines (replace the 10-11 bridge with sulfur, and the compound is the antipsychotic agent promazine). It has weaker D2 postsynaptic blocking activity than promazine and mainly affects amines (5-HT, NE, and DA) via the transporters. As is typical of dimethyl-amino compounds, anticholinergic and sedative (central H1 block) effects tend to be marked. The compound per se has a tendency toward a high 5-HT-to-NE uptake block ratio and probably can be called a serotonin transport inhibitor (SERTI). Metabolic inactivation proceeds mainly by oxidative hydroxylation in the 2-position, followed by conjugation with glucuronic acid of the conjugate. Urinary excretion predominates (about 75%), but some biliary excretion (up to 25%) can occur, probably because of the large nonpolar grouping. Oxidative hydroxylation is not as rapid or complete as that of the more nucleophilic ring phenothiazine antipsychotics; consequently, appreciable N-demethylation occurs, with a buildup of norimipramine (or desimipramine).

Was this article helpful?

0 0
Peripheral Neuropathy Natural Treatment Options

Peripheral Neuropathy Natural Treatment Options

This guide will help millions of people understand this condition so that they can take control of their lives and make informed decisions. The ebook covers information on a vast number of different types of neuropathy. In addition, it will be a useful resource for their families, caregivers, and health care providers.

Get My Free Ebook

Post a comment