Lorcaserin (Belviq)

A selective agonist of the serotonin 5-hydroxytryptamine 2c receptor.

A selective serotonin receptor agonist that works specifically on appetite signals in the brain.

A serotonin 2C receptor agonist.

A serotonin 2C receptor agonist, was approved at a dosage of 20 mg once daily for use with a reduced-calorie diet and increased physical activity as a means to improve weight loss in adults who are obese or overweight and have at least one weight-related medical problem, such as such as hypertension, type 2 diabetes, or dyslipidemia.

Thought to reduce food consumption and promote satiety by selectively activating serotonin 2 C receptors on anorexigenic proopiomelanocortin neurons in the hypothalamus.

Does not activate serotonin 2B receptors, the action associated with heart valve damage associated with fenfluramine and dexfenfluramine.

Indicated as an adjunct to a reduced calorie diet and increased physical activity for weight management in adults with initial body mass index of 30 or greater, or 27 or greater in the presence of at least one weight-related comorbid conditions, such as hypertension, dyslipidemia, or type two diabetes.

In a study evaluating 604 obese and overweight participants with type 2 diabetes in a double-blind placebo-controlled randomized trial over a one-year treatment period: those on the medication lost 4.5 – 5.0% of their initial bodyweight compared to a loss of 1.5% by patients on the inactive placebo.

Decreases body weight in non-diabetic overweight and obese individuals.

Weight losses of 5-10% can significantly improve glycemic control in diabetics as well as other weight-related comorbid conditions.

A serotoninergic drug and is therefore associated with the risk of life-threatening serotonin syndrome or neuroleptic malignant syndrome-like reactions.

The risk of serotonin syndrome increased with the concurrent use of drugs with serotonergic activity: selective serotonin reuptake inhibitors such as fluoxetine, serotonin norepinephrine reuptake inhibitors such as venlafaxine, tricyclic antidepressants, monamine oxidase inhibitors, lithium, triptans, tramadol, tryptophan, bupropion, dextromethorphan and St. John’s wort.

Concurrent use of lorcaserin and any of the above drugs is best avoided, but if used patients should be much more closely for symptoms and signs of serotonin syndrome.

Approximate 2% of patients treated with this agent for at least a year have impaired attention in memory compared to 0.5% among those receiving placebo.

May be associated with confusion fatigue, and somnolence.

FDA Warns About Possible Cancer Risk With Lorcaserin, without any specific evidence.

FDA concludes benefit therapy with this drug does not outweigh the risk for cancers.

In patients without diabetes adverse reactions include headache, dizziness, nausea, fatigue, constipation, and dry mouth.

In diabetics adverse reactions include hypoglycemia, headache, back pain, cough, and fatigue.

Classified as a Schedule IV controlled substance, as in greater than recommended doses can cause euphoria, hallucinations and dissociation in some patients.

Contraindicated for concurrent use with serotoninergic and dopaminergic drugs that are potent serotonin 2B receptor agonists and can increase the risk of cardiac valve damage such as cabergoline.

Depression and suicidal ideation may be related.

Activation of serotonin 2C receptors may increase the possibility of priapism in the drug should be used caution in patients with sickle cell anemia or leukemia and those using erectile dysfunction drugs.

Should be used in caution with patients with use of hazardous machinery because of potential for cognitive impairment and disturbances in attention and memory.

Should be used with caution among psychiatric patients including those with euphoria, disassociation and those predisposed to depression should be monitored for suicidal thoughts.

Metabolized in the liver and metabolites are excreted in the urine.

Dosage is 10 mg twice a day.

The Food and Drug Administration asked Eisai to voluntary withdraw the weight-loss drug lorcaserin (Belviq and Belviq XR) on Feb. 13 2020.

FDA asked drug company to remove drug from market.

A post-marketing trial with more than 12,000 subjects revealed an increased occurrence of cancer.

There was one additional cancer observed for every 470 patients treated for 1 year.

Pancreatic, colorectal, and lung cancers were among those diagnosed.

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