Products
Lorcaserin is commercially available in the form of film-coated tablets (Belviq). It was approved in the United States on June 27, 2012. It is not currently registered in many countries.
Structure and properties
Lorcaserin (C
11
H
14
ClN, M
r
= 195.7 g/mol) is present in drugs as lorcaserin hydrochloride and hemihydrate, a white powder soluble in water. It is a benzazepine derivative and a pure -enantiomer and has structural similarities to dexfenfluramine.
Effects
Lorcaserin has an appetite-suppressing and satiating effect by selectively activating the 5-HT2C receptor on certain neurons in the hypothalamus. Other antiadiposita such as fenfluramine and dexfenfluramine also bind to this receptor but are not selective. The possible adverse cardiovascular effects of fenfluramine (valvular heart disease, pulmonary arterial hypertension) are attributed to the 5-HT2B and 5-HT2A receptors.
Indications
For the treatment of overweight and obesity in patients with a BMI of ≥ 30 kg/m.
2
Or with a BMI of ≥ 27 kg/m
2
In the presence of at least one comorbidity (e.g., high blood pressure, dyslipidemia, type 2 diabetes). In addition, a reduced-calorie diet and increased physical activity are prescribed.
Dosage
According to the SmPC. Tablets are taken twice daily with or without food. Treatment success must be evaluated after 3 months.
Contraindications
Lorcaserin is contraindicated in hypersensitivity and during pregnancy. For complete precautions, see the drug label.
Interactions
Lorcaserin inhibits CYP2D6 and thus may cause drug-drug interactions. Because of the serotonergic properties of lorcaserin and the resulting possibility of serotonin syndrome, combination with other serotonergic agents such as SSRIs, SNRIs, MAO inhibitors, triptans, bupropion, dextromethorphan, and St. John’s wort should be avoided.
Adverse effects
The most common potential adverse effects include headache, dizziness, fatigue, nausea, dry mouth, and constipation. In diabetic patients, hypoglycemia, back pain, and cough have also been observed.