Clinical Research Progress Of Tablets To Suppress Appetite

The tablets to suppress appetitehas always been a research hotspot for weight loss drugs. As early as 1962, theFDA approved amoxazoline for clinical use as an appetite suppressant. Afterthat, fenfluramine, fenfluramine/phentermine compound preparation, sibutramine,ephedrine, phenylpropanolamine hydrochloride, rimonabant and other tablets tosuppress appetite have been used in clinic successively. However, due toadverse reactions, they have withdrawn from the market. Nonetheless, researchon tablets to suppress appetite has not stopped, and new drugs continue toemerge.

Phentermine/Topiramate ExtendedRelease

In 2012, the FDA approved theappetite suppressant compound phentermine/topiramate for clinical use as aweight loss drug. The trade name is Qsymia, each tablet contains 15mg ofphentermine and 92mg of topiramate, the usual dose is 1 tablet/time, orallyonce a day. Phentermine is a sympathomimetic agent that promotes energyexpenditure; topiramate is a monosaccharide-based dextrose derivative used inthe treatment of epilepsy. The two work together on the hypothalamus, which notonly suppresses appetite, enhances satiety, but also reduces adverse drugreactions and improves safety and tolerance. The main adverse reactions ofQsymia are fetal toxicity, increased heart rate, suicidal tendency, acuteangle-closure glaucoma, affective and sleep disturbances, cognitive impairmentand metabolic acidosis, and paresthesia. Therefore, Qsymia is contraindicatedin hyperthyroidism, glaucoma, concomitant use of monoamine oxidase inhibitors,pregnant and lactating women.

Naltrexone/Bupropion

In 2014, the FDA approved theappetite suppressant naltrexone/bupropion compound sustained-releasepreparation (Naltrexone-bupropion, NB) as a new type of tablets to suppressappetite for clinical use. Each tablet contains 8 mg of naltrexonehydrochloride and 90 mg of bupropion hydrochloride under the brand nameContrave. As an extended-release dosage form, this medicine cannot be dividedor chewed. Naltrexone and bupropion act on the centers of the hypothalamus anddopamine circuits, respectively, to reduce food intake. The most common adversereactions during treatment were nausea, vomiting, abdominal pain, blood in the stooland other digestive system abnormalities, and occasionallytachycardia/myocardial infarction, dehydration, depression, and suicide.

lorcaserin hydrochloride

In 2012, the FDA approvedlorcaserin hydrochloride (Lorcaserin) as an appetite suppressant to treatobesity. The trade name is Belviq, the specification is 10mg per tablet, andthe approved regimen is 2 times a day, 1 tablet each time. Belviq is aselective serotonin (5-HT) receptor agonist that specifically stimulates thecentral 5-HT2C receptor to suppress appetite and induce satiety. In clinicalapplication, Belviq is mainly used for obese or overweight persons with BMI ≥27kg/m² and a combination of weight-related diseases (such ashypertension, type 2 diabetes mellitus or hyperlipidemia). In obese oroverweight patients without type 2 diabetes, the most common adverse reactionswere headache, dizziness, fatigue, nausea, dry mouth, and constipation. Inobese patients with type 2 diabetes, the most common adverse reactions werehypoglycemia, headache, low back pain, cough and fatigue.

Liraglutide

Glucagon-like peptide-1(glucagon-likepeptide-1, GLP-1) can promote insulin release, inhibitpostprandial glucagon secretion, increase hepatic glycogen storage, and inhibitβ-cell apoptosis. GLP-1 is also an anorexia signal peptide, which can besynthesized in the central nervous system, acting on the central nervoussystem, suppressing appetite, increasing satiety, and delaying gastricemptying; Liraglutide belongs to GLP-1 receptor Body agonist, FDA approvedliraglutide (3.0mg/d) as a drug for the treatment of obesity. The most commonadverse reactions of liraglutide are gastrointestinal reactions, risk ofpancreatitis, and allergies.

Drugs under development

Pramlintide is an amylin analog,trade name Symlin, its main function is to inhibit glucagon, it is used for theadjuvant treatment of type 1 and type 2 diabetes mellitus, and it should beused with caution when liver and kidney dysfunction occurs. A meta-analysisshowed that Symlin reduced body weight as an adjunct to obese diabeticpatients; subgroup analyses suggested that the trend of Symlin weight loss wasconsistent with the duration of treatment. However, there is uncertainty aboutthe security of Symlin. In clinical studies, patients experienced symptoms suchas nausea, vomiting and anorexia, but fortunately these reactions were onlymild to moderate and lessened over time. This finding suggests that Pramlintidehas the effect of delaying gastric emptying and weight loss, but the specificmechanism of action is unclear, and more research is needed to confirm theweight loss effect and safety of Pramlint-ide.

Although reducing caloric intakeand increasing energy consumption are the cornerstones of obesity treatment,considering the current trend of chronic obesity and the severity ofcomplications, consumption of tablets to suppress appetite is still the bestoption for obesity prevention and treatment. The treatment of obesity bytargeting appetite suppression has always been a hot research topic at home andabroad.