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Bupropion Hydrochloride

Bupropion Hydrochloride

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Zyban 150
GlaxoSmithKline (GSK)
Substance Overview and History

Bupropion hydrochloride, a norepinephrine and dopamine reuptake inhibitor, is a highly permeable and soluble compound primarily used for major depressive disorder (MDD) treatment and smoking cessation. Metabolized in the liver via CYP2B6, it forms 6-hydroxybupropion, the major active metabolite, along with 4′-hydroxybupropion, threohydrobupropion, and erythrohydrobupropion. These metabolites play vital roles in its therapeutic effects. Marketed under various brands and generics, bioequivalence for these products is assessed using FDA-recommended pharmacokinetic (PK) studies. Innovations like PBPK modeling integrate drug properties, patient physiology, and metabolism to predict performance, supporting drug development and regulatory decisions.

References:

Hsieh, N.-H., Bois, F.Y., Tsakalozou, E., Ni, Z., Yoon, M., Sun, W., Klein, M., Reisfeld, B., & Chiu, W.A. (2021) A Bayesian Population Physiologically Based Pharmacokinetic Absorption Modeling Approach to Support Generic Drug Development: Application to Bupropion Hydrochloride Oral Dosage Forms, J Pharmacokinet Pharmacodyn.

Disclaimer: Information provided it this page is for general information only and does not substitute for professional medical advice.

For more details consult with your doctor or healthcare professional.

FAQ
What is Bupropion Hydrochloride used for?
Bupropion Hydrochloride is primarily used to treat major depressive disorder (MDD) and to aid in smoking cessation.
References:

Hsieh, N.-H., Bois, F.Y., Tsakalozou, E., Ni, Z., Yoon, M., Sun, W., Klein, M., Reisfeld, B., & Chiu, W.A. (2021) A Bayesian Population Physiologically Based Pharmacokinetic Absorption Modeling Approach to Support Generic Drug Development: Application to Bupropion Hydrochloride Oral Dosage Forms, J Pharmacokinet Pharmacodyn.

How does Bupropion Hydrochloride work?
It acts as a norepinephrine and dopamine reuptake inhibitor, increasing the availability of these neurotransmitters in the brain to enhance mood and reduce cravings.
References:

Hsieh, N.-H., Bois, F.Y., Tsakalozou, E., Ni, Z., Yoon, M., Sun, W., Klein, M., Reisfeld, B., & Chiu, W.A. (2021) A Bayesian Population Physiologically Based Pharmacokinetic Absorption Modeling Approach to Support Generic Drug Development: Application to Bupropion Hydrochloride Oral Dosage Forms, J Pharmacokinet Pharmacodyn.

What are the main metabolites of Bupropion Hydrochloride?
The main metabolites include 6-hydroxybupropion, 4′-hydroxybupropion, threohydrobupropion, and erythrohydrobupropion, with 6-hydroxybupropion being the most active.
References:

Hsieh, N.-H., Bois, F.Y., Tsakalozou, E., Ni, Z., Yoon, M., Sun, W., Klein, M., Reisfeld, B., & Chiu, W.A. (2021) A Bayesian Population Physiologically Based Pharmacokinetic Absorption Modeling Approach to Support Generic Drug Development: Application to Bupropion Hydrochloride Oral Dosage Forms, J Pharmacokinet Pharmacodyn.