Diet pills are not health products, as a drug, it has certain side effects and adverse reactions, expect to achieve slimming through diet pills must be taken for a long time in order to produce a slimming effect, but long-term consumption of diet pills will make the human body's gastrointestinal function disorders, the lesser will have indigestion, the heavier may cause a series of gastrointestinal diseases, some diet pills are even harmful to the human body, such as diuretics in the weight loss pills. Some diet pills are even harmful to the human body, such as diuretics in diet pills, if taken for a long time, it will lead to kidney function degradation, which will lead to a variety of diseases. Women eating diet pills will also lead to infertility, which is very bad for every woman and will become a lifetime of regret. In fact, the most important thing to lose weight is still to eat a normal diet, a balanced diet, and more importantly, exercise, which is the best way to lose weight, so, for the sake of the general health of women, you still need to lose weight scientifically ah.
If you take diet pills after the symptoms of excessive excitement, can not sleep at night, then you have to be alert to your medicine may contain amphetamine. At the beginning of taking this kind of drug, the weight loss effect may be very obvious, but as the body resistance to the drug, there will be emotional instability, delusions, hallucinations, sleep disorders and other symptoms. Bupropion is also addictive like drugs. Once addicted, the process of quitting is very painful, and symptoms such as anxiety, depression, fatigue, drowsiness and overeating may even occur. Experts suggest that this drug should never be taken easily.
Status and safety of diet pills Editorial Podcasts
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The approval of new diet pills must adhere to both efficacy and safety. In terms of efficacy, the listed diet pills all meet the FDA's efficacy evaluation standards for diet pills: (1) After 1 year of taking diet pills and placebo, the difference in weight loss between the 2 groups of subjects should be no less than 5%. (2) The proportion of subjects who lost at least 5% of their body weight in the drug treatment group should be not less than 35%, and the proportion should be twice as high as that in the placebo group. However, weight-loss drugs have serious safety problems while delivering good weight-loss efficacy. The most notorious of these are the appetite suppressant amphetamine analogues fenfluramine and phentermine, which were widely used in the 1990s for their appetite-suppressing effects but had to be withdrawn from the market because of the risk of pulmonary hypertension and heart valve disease. Other amphetamine analogues and sympathomimetics also carry serious risks of addiction, cardiotoxicity and sudden death. Chronic pulmonary hypertension caused by aminorex has a mortality rate of 50 per cent. Phenylpro-panolamine can cause intracranial haemorrhage and stroke. Ephedrine can cause heart disease, high blood pressure, palpitations, stroke and sudden death. Sibutramine can cause an increase in cardiovascular disease.
Rimonabant, an endogenous cannabinoid receptor CBL antagonist, can cause an increase in depression and suicide. All of these unsafe drugs have been withdrawn from the market. Currently, there are five diet pills still in clinical use, including orlistat (orlistat) capsules approved in 1999, lorcaserin (lorcaserin) and phenylbutazone and topiramate (qsymia) extended-release capsules approved in 2012, and naltrexone hydrochloride and bupropion hydrochloride combination extended-release tablets (contrave) approved in 2014 and liraglutide (liraglutide) injections.
Diet pills in clinical use Editorial Podcast
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1. orlistat
In 1987, the pancreatic lipase inhibitor lipstatin was isolated from Streptomyces sp. However, due to the presence of two unstable cis-double bonds in its structure, Roche obtained a more stable orlistat by hydrogenation reduction while retaining its basic structure, which was approved by the US FDA in 1999 for the treatment of obesity. In addition to its good weight loss effect, it can also improve the blood pressure of patients with hypertension, which is difficult to be controlled by conventional antihypertensive drugs. In addition, orlistat can control blood glucose and reduce the incidence of diabetes mellitus at the same time of weight loss. orlistat, as a gastrointestinal esterase inhibitor, partially inhibits gastric lipase, pancreatic lipase and carboxylester lipase, and hinders the absorption of fatty acids and glycerol monostearate by mucosal cells of gastrointestinal tract, which reduces the absorption of 30% of the ingested fats, and increases the excretion of fecal matter, and thus achieves the purpose of weight loss. Since orlistat at a high dose of 800mg-d (normal dose of 360mg-d) does not have systemic effects, its main manifestation is adverse effects on the intestinal tract, such as diarrhoea, flatulence, urgency and urinary incontinence, which can be reduced by lowering the fat content of the diet. orlistat reduces the absorption of fat while also reducing fat-soluble vitamins (vitamins A/D). absorption of fat-soluble vitamins (vitamins A/D/E), minerals (calcium and potassium), and certain medications [warfarin, amiodarone, ciclosporin, lamotrigine, valproic acid, vigabatrin, gabapentin vigabatrin), gabapentin, thyroxine, etc.]. In addition, orlistat has been documented in 2010 to cause severe liver damage, acute pancreatitis, acute kidney injury, and precancerous colon cancer. In conclusion, the limited weight loss efficacy and serious adverse effects highlight the shortcomings of orlistat. Therefore, there is still an urgent need to develop new weight loss drugs with high efficiency and low toxicity.
2. lorcaserin
Dexfenfluramine, the first weight-loss drug approved by the FDA in 1996 for the long-term treatment of obesity, has good weight-loss efficacy, but due to its lack of selectivity for 5-HT2B and 5-HT2C receptors, resulting in serious heart valve lesions, was withdrawn from the market in 1997. In order to avoid the adverse heart valve reactions caused by agonism of 5-HT2B, Arena Pharmaceuticals modified the structure of fenfluramine by combining the C-1 and C-6 positions of the benzene ring to form a phenylpropanazepine nucleus, and then substituted chlorine for trifluoromethyl group at the C-3 position to increase the selectivity of fenfluramine for 5-HT2C, and obtained lorcaserin. Iorcaserin was approved by the US FDA in June 2012 for the adjunctive treatment of overweight or obese patients with a body mass index (BMI) ≥27 and at least one obesity complication.Iorcaserin selectively activates 5-HT2C receptors in the hypothalamus to reduce appetite and increase satiety, avoiding the adverse effects of agonistic 5-HT2B on heart valves, and enhancing the safety of administration. Safety of medication. When used alone, the most common adverse effects in non-diabetic patients were headache, dizziness, fatigue, nausea, dry heaves and constipation; the most common adverse effects in diabetic patients included hypoglycaemia, headache, back pain, cough and fatigue.
3、 qsymia
Phentermine (phentermine) was first approved for short-term weight management in 1956. It is an amphetamine analogue, which is mainly used to suppress appetite and reduce food intake by inducing the release of central nervous norepinephrine, thereby achieving weight loss. The most common adverse effects include insomnia, dry mouth and constipation. Also, its stimulant nature makes it contraindicated for cardiovascular disease, hyperthyroidism, glaucoma, irritability, and substance abuse. Studies have found that topiramate, which was first approved for the treatment of epilepsy in 1996, increases satiety and reduces energy intake, but the mechanism of weight loss is unclear. Its most common adverse effects are sensory abnormalities (tingling in the legs and feet) and taste disturbances. Because topiramate is primarily metabolised by the kidneys, it has been associated with kidney stones, metabolic acidosis and acute angle-closure glaucoma in some patients.Vivus has used phentermine in combination with topiramate and found it to be more effective for weight loss, with lower dosages for the same therapeutic effect, and fewer adverse effects, but with an increase in patient tolerance to the drug. Tolerance of the drug was increased. The US FDA approved qsymia in 2012 as a new combination weight-loss drug in the appetite suppressant class, and concluded that the benefits of the drug outweigh the drawbacks in long-term use in overweight and obese populations.
4. contrave
Bupropion is a selective norepinephrine and dopamine reuptake inhibitor used clinically as an antidepressant and smoking cessation drug. It has been found that bupropion has appetite suppressant activity that is associated with stimulation of opioid-opioid-opiomelanocortinogen (POMC)-releasing neurons (opiomelanocortinogens) in the hypothalamus. These neurons release a-melanocyte stimulating hormone (a-MSH), which reduces food intake while increasing energy expenditure. However, the weight loss efficacy of bupropion alone in clinical studies has been less than significant. As a result, the FDA has not approved it to be marketed as a weight loss drug on its own. It was also found that taking naltrexone (naltrexone) along with bupropion enhanced appetite-suppressing activity and strengthened weight-loss efficacy. As a result, the US FDA approved the marketing of contrave, a combination weight loss drug developed by Takeda and Orexigen, in October 2014 for obese adult patients with a BMI ≥30kg-m, or adult patients with a BMI ≥27kg-m and at least one comorbid condition such as high blood pressure, type 2 diabetes, or high cholesterol (dyslipidaemia). Because contrave contains bupropion, the combination drug has a black box warning alerting health care professionals and patients that this drug can increase suicidal thoughts and behaviour associated with antidepressants.
5. liraglutide
liraglutide is a human glucagon-like peptide-1 (GLP-1) analogue developed by Novo Nordisk and first marketed in the European Union in July 2009 and in China in October 2011 for the treatment of type 2 diabetes. in December 2014, liraglutide was approved by the US FDA to be marketed in the United States as a long-term weight loss drug for for adult obese patients with a BMI ≥ 30 kg-m or a BMI ≥ 27 kg-m with obesity-related complications such as diabetes mellitus or hypertension. liraglutide carries a black box warning that studies have shown liraglutide to increase the risk of thyroid C-cell tumours in rodents, and that the above risk is uncertain in humans. Therefore, liraglutide should not be used in patients with a family or personal history of medullary thyroid carcinoma (MTC) and in patients with multiple endocrine neoplasia syndrome type 2 (disease combining more than one type of adenoma that predisposes to MTC). Serious adverse reactions reported with liraglutide therapy include pancreatitis, gallbladder disease, renal dysfunction, and suicidal ideation. liraglutide also accelerates the heart rate, and should be discontinued if a patient has a persistently accelerated resting heart rate. In clinical trials, the most common adverse reactions in liraglutide-treated patients included nausea, diarrhoea, constipation, vomiting, hypoglycaemia and decreased appetite. This product is available as a subcutaneous injection.
