Sibutramine

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Introduction[edit | edit source]

Sibutramine is a pharmacological agent that functions as a serotonin and norepinephrine reuptake inhibitor. Originally designed for the treatment of depression, it was later repurposed and used primarily for the short- and long-term management of obesity. However, in 2010, its usage was withdrawn due to an observed increased risk of cardiovascular events.

Chemical structure of sibutramine.

Mechanism of Action[edit | edit source]

Sibutramine, chemically referred to as si bue' tra meen, belongs to the beta-phenylethylamine class of compounds. It acts by inhibiting the reuptake of two neurotransmitters in the brain: serotonin and norepinephrine. While it was initially developed to act as an antidepressant, sibutramine exhibited a minimal therapeutic effect on depression. However, an unintended consequence of its administration was weight loss, which researchers linked to decreased appetite and a subsequent reduction in caloric intake.

Relationship with Liver Toxicity[edit | edit source]

In comprehensive clinical trials, the administration of sibutramine did not correlate with elevated serum enzyme levels, indicating a low risk of liver-related side effects. However, on rare occasions, sibutramine has been connected to cases of clinically significant acute liver injury.

FDA Approval and Subsequent Withdrawal[edit | edit source]

The FDA granted approval for sibutramine as an obesity treatment in the United States in 1997. The drug enjoyed widespread prescription until 2010 when emerging research studies demonstrated a concerning association between sibutramine usage and an increased likelihood of experiencing myocardial infarction and stroke. In light of these findings, the drug was officially withdrawn from the market.

Conclusion[edit | edit source]

While sibutramine once showed promise as a treatment for obesity, concerns about its safety profile, particularly regarding cardiovascular events, led to its removal from clinical use. Its history underscores the importance of continued post-market surveillance for all approved medications.

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