Tìm theo
Lorcaserin
Thuốc Gốc
Small Molecule
CAS: 616202-92-7
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ hòa tan
Water solubility is greater than 400 mg/mL.
Dược Lực Học : Lorcaserin produced a dose-dependent weight loss over a 12-week period by promoting satiety and decreasing food consumption.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ Absorption :
Lorcaserin has a peak plasma concentration of about 1.5 - 2 hours, but the bioavailability was not determined.
▧ Volume of Distribution :
The volume of distribution was not determined, but lorcaserin distributes to the central nervous system and cerebrospinal fluid.
▧ Protein binding :
Lorcaserin hydrochloride has a plasma protein binding of approximately 70%.
▧ Metabolism :
Lorcaserin has extensive hepatic metabolism producing inactive compounds. Lorcaserin sulfamate (M1) is the major metabolite circulating in the plasma, and N-carbamoyl glucuronide lorcaserin (M5) is the major metabolite in urine. Other minor metabolites that are both excreted in urine are glucuronide or sulfate conjugates.
▧ Route of Elimination :
Lorcaserin is eliminated by hepatic metabolism, and the metabolites are eliminated mostly in the urine (92.3%) and some through feces (2.2%).
▧ Half Life :
The plasma half life is approximately 11 hours.
▧ Clearance :
The clearance value was not determined.
Độc Tính : 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.
Chỉ Định : For the treatment of obesity, as an adjunct to a reduced-calorie diet and increased physical activity.
Tương Tác Thuốc :
  • Ergotamine Avoid all combinations with any ergot derivative such as ergotamine. The combination can increase the risk of developing serotonin syndrome and/or valvular heart disease.
  • Thioridazine Avoid combination.The combination is likely to reduce the metabolism of Thioridazine.
Liều Lượng & Cách Dùng : Tablet - Oral - 10 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : EISAI INC
    Sản phẩm biệt dược : Belviq
  • Công ty :
    Sản phẩm biệt dược : Lorqess
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04871
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06613
Wikipedia
http://en.wikipedia.org/wiki/Lorcaserin
RxList
http://www.rxlist.com/belviq-drug.htm
Drugs.com
http://www.drugs.com/mtm/lorcaserin.html
... loading
... loading