Bupropion, Trazodone

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Chapter: Medicinal Chemistry : Antidepressants

Antidepressants - a. Bupropion (Zyban) b. Trazodone (Tazodac, Trazalon, Trazonil) - SYNTHESIS AND DRUG PROFILE - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE


Miscellaneous

a. Bupropion (Zyban)

Bupropion is a novel, nontricyclic antidepressant with a primary pharmacological action of monoamine uptake inhibition.


Synthesis

Route I. From: m-Chloro cyano benzene


Route II. From: 3-Chloro benzonitrile


Properties and uses: It exists as a white solid, soluble in water or ethanol. A semisynthetic centrally acting opiod analgesic derived from thebaine, it is used for the relief of moderate to severe pain particularly associated with postoperative discomfort. It is approximately 30 times as potent as morphine and exerts its analgesic effect by binding to CNS opiod receptors. Bupropion is used to treat major depression, refractory depression, and seasonal effective disorder. It is also used to help people to stop smoking and to treat bipolar depression and attention defect disorder. It does not cause sedation and has minimal cardiovascular side effects. The most frequent side effect is agitation.

Dose: Initial dosing is 75–100 mg twice or thrice a day.


b. Trazodone (Tazodac, Trazalon, Trazonil)


Synthesis

Step I. Preparation of 1, 2, 4-triazolo pyridin-3-one


Step II. Preparation of 1-(3-chloro phenyl)-4-(3-choro propyl) piperazine.


Condensation of Step I and Step II products


Properties and uses: It exists as white crystals, sparingly soluble in water or alcohol, soluble in chloroform. It is a heterocyclic with high sedative and no antimuscarnic effects. Antidepressant activity of trazodone is believed to be produced by blocking the reuptake of serotonin at the presynaptic neuronal memberane. Trazodone has no influence on the reuptake of NE or dopamine with the CNS. It has a sedative effect, which is believed to be produced by the alpha-adrenergic blocking action and modest histamine blockade.

Dose: The usual dose is 150–400 mg/day by oral.


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