Anti-obesity drugs or weight-loss drugs are pharmacological agents that reduce or control weight. These medicines change one of the fundamental processes of the human body, regulating weight, by changing appetite, or caloric absorption. The main modality of treatment for overweight and obese individuals remains diet and physical exercise.
In the United States orlistat (Xenical) is currently approved by the FDA for long-term use. It reduces intestinal fat absorption by inhibiting pancreatic lipase. Rimonabant (Acomplia), a second drug, works through a specific blockade of the endocannabinoid system. It has been developed from the knowledge that marijuana smokers often experience hunger, often referred to as "snacks". It has been approved in Europe for the treatment of obesity but has not received approval in the United States or Canada due to security concerns. The European Medicines Agency in October 2008 recommended the suspension of rimonabant sales because the risk appeared to outweigh the benefits. Sibutramine (Meridia), which acts in the brain to inhibit the deactivation of neurotransmitters, thus reducing appetite withdrawn from the United States and the Canadian market in October 2010 due to cardiovascular concerns.
Because of potential side effects, and limited evidence of small benefits in weight loss especially in obese children and adolescents, it is recommended that anti-obesity drugs be prescribed only for obesity where it is expected that the benefits of treatment outweigh the risks.
Video Anti-obesity medication
Mekanisme aksi
Current and potential anti-obesity drugs can operate through one or more of the following mechanisms:
- Catecholamine release drugs such as amphetamines, phentermines, and associated substituted amphetamines (eg bupropion) that act as appetite suppressants are the primary means used for the treatment of obesity.
- Increased metabolism.
- Interference with the body's ability to absorb certain nutrients in food. For example, Orlistat (also known as Xenical and Alli) blocks fat breaking and thereby prevents fat absorption. OTC glucomannan and guar gum fiber supplements have been used for the purpose of inhibiting digestion and decreasing the absorption of calories
Anorectrics are primarily intended to suppress appetite, but most drugs in this class also act as stimulants (eg, amphetamines), and patients have abused "label" drugs to suppress appetite (eg digoxin).
Maps Anti-obesity medication
History
The first attempt described to produce weight loss was from Soranus of Ephesus, a Greek physician, in the second century AD. He prescribed a laxative and laxative, as well as heat, massage, and exercise. It remains a mainstay of care for over a thousand years. It was not until the 1920s and 1930s that new treatments began to emerge. Based on its effectiveness for hypothyroidism, thyroid hormone becomes a popular treatment for obesity in euthyroid people. It has a simple effect but produces symptoms of hyperthyroidism as a side effect, such as palpitations and difficulty sleeping. 2,4-Dinitrophenol (DNP) was introduced in 1933; this works by releasing the biological processes of oxidative phosphorylation in the mitochondria, causing them to produce heat instead of ATP. The most significant side effects are warm sensation, often with sweating. Overdose, though rare, causes an increase in body temperature and, eventually, a fatal hyperthermia. By the end of 1938 DNP was no longer in use because the FDA had been empowered to put pressure on producers, who voluntarily withdrew it from the market.
Amphetamine (marketed as Benzedrine) became popular for weight loss during the late 1930s. They work primarily by suppressing appetite, and have other beneficial effects such as increased alertness. The use of amphetamine increased over the next several decades, including Obetrol and culminated in the "rainbow pill regime". It is a combination of many pills, all of which help lose weight, taken throughout the day. Typical regimens include stimulants, such as amphetamines, and thyroid hormones, diuretics, digitalis, laxatives, and often barbiturates to suppress the stimulant side effects. In 1967/1968 a number of deaths attributed to diet pills sparked a Senate inquiry and gradual implementation of the larger restrictions on the market.
Meanwhile, phentermine was approved by the FDA in 1959 and fenfluramine in 1973. Both were no more popular than other drugs until in 1992 a researcher reported that when combined both led to a 10% weight loss that was maintained for more than two years. Fen-phen was born and quickly became the most commonly prescribed diet drug. Dexfenfluramine (Redux) was developed in the mid-1990s as an alternative to fenfluramine with fewer side effects, and received regulatory approval in 1996. However, this coincides with the growing evidence that this combination can cause heart valve disease by up to 30% of those which has taken it, led to the withdrawal of phen-phen and dexfenfluramine from the market in September 1997.
Ephedra was removed from the US market in 2004 due to concerns that it increases blood pressure and can lead to stroke and death.
Drug
Some patients find that diet and exercise are not a viable option; For these patients, anti-obesity drugs can be the last resort. Some prescription drugs for weight loss are stimulants, which are recommended only for short-term use, and thus have limited utility for very obese patients, who may need to lose weight for months or years.
Orlistat
Orlistat (Xenical) reduces intestinal fat absorption by inhibiting pancreatic lipase. Some of the side effects of Orlistat use include frequent, greasy bowel movements (steatorrhea). But if the fat in the diet is reduced, symptoms often improve. Initially available only by prescription, it was approved by the FDA for over-the-counter sales in February 2007. On May 26, 2010, the US Food and Drug Administration (FDA) approved a revised label for Xenical to include new safety information about the case severe liver injury that is rarely reported with the use of this drug. Of the 40 million Orlistat users worldwide, 13 cases of severe liver damage have been reported.
Lorcaserin
Lorcaserin (Belviq) approved June 28, 2012 for obesity with other comorbidities. The average weight loss by study participants was simple, but the most common side effects of the drug were considered benign. This reduces appetite by activating a type of serotonin receptor known as the 5-HT 2C recipe in the area of ​​the brain called the hypothalamus, which is known to control appetite. Sibutramine
Sibutramine (Reductil or Meridia) is anorectic or appetite suppressor, reducing the desire to eat. Sibutramine can increase blood pressure and can cause dry mouth, constipation, headache, and insomnia.
In the past, it was noted by the US that Meridia is a harmless drug to combat obesity. The US District Court in the Northern District of Ohio rejected 113 cases complaining about the drug's negative effects, stating that the client has no supporting facts and that the representatives involved are not sufficiently qualified.
Sibutramine has been withdrawn from markets in the United States, Britain, the European Union, Australia, Canada, Hong Kong, and Colombia. The risks (non-life threatening myocardial infarction and stroke) have been shown to outweigh the benefits.
Rimonabant
Rimonabant (also known as SR141716, the trade name Acomplia and Zimulti) is an anorectical antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States. Rimonabant is an inverse agonist for CB1 cannabinoid receptors and is the first approved drug in that class.
Metformin
In people with type 2 Diabetes mellitus, metformin drugs (Glucophage) can lose weight. Metformin limits the amount of glucose produced by the liver and increases the consumption of muscle glucose. It also helps increase the body's response to insulin.
Exenatide/Liraglutide
Exenatide (Byetta) is a long-acting analog of the GLP-1 hormone, secreted by the intestine in response to the presence of food. Among other effects, GLP-1 delayed gastric emptying and increased satiety. Some obese people lack GLP-1, and the diet reduces GLP-1 further. Byetta is currently available as a treatment for type 2 Diabetes mellitus. Some, but not all, patients find that they lose considerable weight while taking Byetta. The weakness of Byetta includes that it should be injected subcutaneously twice daily, and it causes severe nausea in some patients, especially when therapy begins. Byetta is recommended only for patients with Type 2 Diabetes. A somewhat similar drug, pramlintide, is currently available to treat diabetes and is under testing to treat obesity in non-diabetic patients.
Liraglutide (Saxenda) adalah analog GLP-1 lainnya.
Phentermine/topiramate
The combination of phentermine and topiramate, the brand name Qsymia (formerly Qnexa) is approved by the US FDA on July 17, 2012, as an obesity treatment that complements diet and exercise. The European Medicines Agency, in contrast, rejected the combination as a treatment for obesity, citing concerns about the long-term effects on heart and blood vessels, mental health and cognitive side effects.
Bupropion/naltrexone
Bupropion/naltrexone is a combination drug used to lose weight in those who are obese or overweight with some weight-related illnesses It combines low-dose bupropion and naltrexone. Both drugs individually show some evidence of effectiveness in weight loss, and this combination is shown to have some synergistic effect on weight. In September 2014, a sustained release formulation of the drug was approved for marketing in the United States under the Contrave brand name. This combination is then approved in the EU in spring 2015, where it will be sold under the name Mysimba.
Other drugs
Other weight-loss drugs have also been associated with medical complications, such as fatal pulmonary hypertension and heart valve damage due to Redux and Phen-phen, and hemorrhagic stroke due to phenylpropanolamine. Many of these substances are associated with amphetamines.
Tesofensine (NS2330) is a serotonin-noradrenaline-dopamine reuptake inhibitor of the phenyltropane family of drugs, which is being developed for the treatment of obesity. Tesofensine was originally developed by the Danish biotechnology company, NeuroSearch, which transfers rights to Saniona by 2014. Tesofensine has been evaluated in Phase 1 and Phase 2 of human clinical studies with the aim of investigating the potential of treatment related to obesity.
Nonprescription products or programs that have not been prescribed for weight loss are greatly promoted through letters and print ads and on the internet. The US Food and Drug Administration recommends caution with the use of these products, as many security claims and effectiveness are not proven. Individuals with anorexia nervosa and some athletes try to control weight with laxatives, diet pills or diuretic medications, although these generally have no impact on body fat. Products that work as laxatives can cause blood potassium levels to drop, which can cause heart and/or muscle problems. Pyruvate is a popular product that can produce a slight weight loss. However, pyruvate, which is found in red, cheese, and red wine apples, has not been fully studied and its weight loss potential has not been scientifically established.
Herbs and alternative medicine
Canada's clinical practice guidelines state that there is insufficient evidence to recommend supporting or opposing the use of herbal medicines, dietary supplements or homeopathy against obesity.
Conjugated linoleic acid is claimed to help reduce obesity but is not effective for this use.
ECA stacks can not be marketed in most developed countries but are used to be marketed as weight loss; it provides short-term weight loss that is simple but ineffective in the long run and has adverse effects on the cardiovascular system, mental, digestive, and nervous.
Side effects
Some anti-obesity drugs can have severe, even lethal side effects, phen-phen being a well-known example. Phen-phen is reported through the FDA to cause abnormal echocardiogram, heart valve problems, and rare valvular disease. One, if not the first, to sound an alarm is Sir Arthur MacNalty, Chief Medical Officer (UK). In the early 1930s, he warned the use of dinitrophenol as an anti-obesity drug and the use of unattended and/or unattended thyroid hormones to achieve weight reduction. Side effects are often associated with the mechanism of action of the drug. In general, stimulants carry the risk of high blood pressure, faster heart rate, palpitations, closed-angle glaucoma, drug addiction, anxiety, agitation, and insomnia.
Other drugs, orlistat, block the absorption of dietary fat, and as a result can cause gastrointestinal bowel movement (steatorrhea), oily stools, abdominal pain, and flatulence. A similar drug designed for patients with type 2 diabetes is Acarbose; which partially inhibits the absorption of carbohydrates in the small intestine, and produces the same side effects including abdominal pain and flatulence.
Research
Other classes of drugs in development include lipase inhibitors, similar to orlistat. Another lipase inhibitor, called GT 389-255, is being developed by Peptimmune (licensed from Genzyme). This is a new combination of inhibitors and polymers designed to bind undigested triglycerides to allow increased fatigue removal without side effects such as oily stools that occur with orlistat. Development stalled because Phase 1 trials were conducted in 2004 and no subsequent clinical human developments thereafter. In 2011, Peptimmune filed Liquidation Chapter 7.
See also
- The effect of weight loss from water
References
Further reading
Boss, Olivier; Karl G. Hofbauer (2004). Obesity pharmacotherapy: options and alternatives . Boca Raton: CRC Press. ISBNÃ, 0-415-30321-4.
External links
- Prescription Drugs for Obesity Treatment
Source of the article : Wikipedia
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