Threohydrobupropion

Threohydrobupropion

Threohydrobupropion is a metabolite of the antidepressant and smoking cessation aid bupropion. It is formed in the body through the reduction of bupropion by the enzyme carbonyl reductase. Threohydrobupropion, along with other metabolites such as hydroxybupropion and erythrohydrobupropion, contributes to the pharmacological effects of bupropion.

Pharmacology

Threohydrobupropion is known to inhibit the reuptake of the neurotransmitters dopamine and norepinephrine, similar to its parent compound bupropion. This inhibition increases the levels of these neurotransmitters in the brain, which is believed to contribute to its antidepressant and smoking cessation properties.

Metabolism

Bupropion is metabolized in the liver primarily by the enzyme cytochrome P450 2B6 (CYP2B6) to form hydroxybupropion. Threohydrobupropion is formed through the reduction of bupropion by carbonyl reductase. The pharmacokinetics of threohydrobupropion, including its half-life and bioavailability, are important for understanding the overall effects of bupropion therapy.

Clinical Significance

The presence of threohydrobupropion and its activity is significant in the clinical use of bupropion. The metabolite's ability to inhibit dopamine and norepinephrine reuptake supports the therapeutic effects of bupropion in treating depression and aiding in smoking cessation. Understanding the role of threohydrobupropion can help in optimizing bupropion dosing and managing potential side effects.

See Also

• Bupropion
• Hydroxybupropion
• Erythrohydrobupropion
• Dopamine
• Norepinephrine
• Cytochrome P450 2B6

References

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