Lorcaserin
Lorcaserin Uses, Dosage, Side Effects, Food Interaction and all others data.
Lorcaserin (previously APD-356), a highly selective 5HT2C receptor agonist, is used for the treatment of obesity. It has been shown to reduce body weight and food intake in animal models of obesity, and it is thought that targeting the 5HT2C receptor may alter body weight by regulating satiety. Lorcaserin is marketed as a salt form called Belviq, which is lorcaserin hydrochloride.
Lorcaserin produced a dose-dependent weight loss over a 12-week period by promoting satiety and decreasing food consumption.
| Trade Name | Lorcaserin |
| Availability | Discontinued |
| Generic | Lorcaserin |
| Lorcaserin Other Names | Lorcaserin, Lorqess |
| Related Drugs | phentermine, Victoza, semaglutide, Wegovy, Saxenda, liraglutide, Contrave, Qsymia, Alli |
| Type | Oral |
| Formula | C11H14ClN |
| Weight | Average: 195.69 Monoisotopic: 195.0814772 |
| Protein binding | Lorcaserin hydrochloride has a plasma protein binding of approximately 70%. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lorcaserin is a serotonin 2C receptor agonist used in conjunction with physical activity and calorie restriction for weight loss in obese patients with a body mass index (BMI) of 30 and above, and in overweight patients with weight-related comorbidities.
For the treatment of obesity, as an adjunct to a reduced-calorie diet and increased physical activity.
Lorcaserin is also used to associated treatment for these conditions: BMI >30 kg/m2
How Lorcaserin works
Although the exact mechanism is unknown, it is believed to involve the selective activation of 5-HT2C receptors in the anorexigenic pro-opiomelanocortin neurons in the arcuate nucleus of the hypothalamus. This results in decreased food intake and satiety by promoting the release of alpha-melanocortin stimulating hormone, which acts on melanocortin-4 receptors.
Toxicity
Most common adverse reactions include hypoglycemia (diabetic patients), headache, back pain,fatigue, decrease in lymphocytes,upper respiratory tract infection, and nasopharyngitis. Moreover, the safety and efficacy of coadministration with other weight loss products has not been established, and cardiovascular effects on mortality and morbidity have not been established.
Food Interaction
- Take with or without food.
[Minor] Food does not appear to significantly affect the absorption and oral bioavailability of lurasidone.
In twelve adult volunteers (6 men and 6 women), administration of a single 10 mg oral dose of lorcaserin following a high-fat (approximately 50% of total caloric content of the meal) and high-calorie (approximately 800 to 1000 calories) meal resulted in less than 10% increases in lorcaserin peak plasma concentration (Cmax) and systemic exposure (AUC) compared to administration in the fasted state.
The time to reach peak concentration (Tmax) was delayed by approximately 1 hour in the fed state.
Lorcaserin may be administered with or without food.
Lorcaserin Drug Interaction
Major: duloxetineModerate: amphetamine / dextroamphetamine, lurasidone, semaglutide, dulaglutideUnknown: aspirin, aspirin, lorazepam, buprenorphine, ubiquinone, azelastine / fluticasone nasal, omega-3 polyunsaturated fatty acids, sulfacetamide sodium topical, metronidazole topical, acetaminophen, hydroxychloroquine, omeprazole, budesonide / formoterol, levothyroxine, cholecalciferol
Lorcaserin Disease Interaction
Major: valvulopathyModerate: bradycardia, breast cancer, depression, hematological abnormalities, liver disease, priapism, pulmonary hypertension, renal dysfunction, diabetics
Volume of Distribution
The volume of distribution was not determined, but lorcaserin distributes to the central nervous system and cerebrospinal fluid.
Elimination Route
Lorcaserin has a peak plasma concentration of about 1.5 - 2 hours, but the bioavailability was not determined.
Half Life
The plasma half life is approximately 11 hours.
Clearance
The clearance value was not determined.
Elimination Route
Lorcaserin is eliminated by hepatic metabolism, and the metabolites are eliminated mostly in the urine (92.3%) and some through feces (2.2%).
Innovators Monograph
You find simplified version here Lorcaserin
