Anorectic

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An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. [1] These substances work by affecting the central nervous system or certain neurotransmitters to create a feeling of fullness or reduce the desire to eat. The understanding of anorexiant effects is crucial in the development of interventions for weight management, eating disorders, and related health concerns. The anorexiant effect can be induced through diverse mechanisms, ranging from hormonal regulation to neural signaling. Ghrelin, leptin, and peptide YY are among the hormones involved in appetite control. Additionally, neurotransmitters such as serotonin and dopamine in the central nervous system contribute significantly to the regulation of food intake.

Contents

By contrast, an appetite stimulant is referred to as orexigenic.

The term is (from the Greek ἀν- (an-) = "without" and ὄρεξις (órexis) = "appetite"), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant.

History

Used on a short-term basis clinically to treat obesity, some appetite suppressants are also available over-the-counter. Several appetite suppressants are based on a mix of natural ingredients, mostly using green tea as its basis, in combination with other plant extracts such as fucoxanthin, found naturally in seaweed. Drugs of this class are frequently stimulants of the phenethylamine family, related to amphetamine.[ citation needed ]

The German and Finnish [2] militaries issued amphetamines (Pervitin) to soldiers commonly during the Second World War. [3] Similarly, the UK military was supplied with more than 72 million Benzedrine tablets and the US military with an approximately equal amount for situations, in which fatigue was not deemed to be an acceptable option. [4] Following the war, large amphetamine surpluses were redirected for use on the black [5] and the civilian market. Indeed, amphetamine itself was sold commercially as an appetite suppressant until it was outlawed in most parts of the world in the late 1950s because of safety issues. Many amphetamines produce side effects, including addiction, tachycardia and hypertension, [6] making prolonged unsupervised use dangerous.

Public health concerns

Epidemics of fatal pulmonary hypertension and heart valve damage associated with pharmaceutical anorectic agents have led to the withdrawal of products from the market. This was the case with aminorex in the 1960s, and again in the 1990s with fenfluramine (see: Fen-phen). [7] Likewise, association of the related appetite suppressant phenylpropanolamine with hemorrhagic stroke led the Food and Drug Administration (FDA) to request its withdrawal from the market in the United States in 2000, and similar concerns regarding ephedrine resulted in an FDA ban on its inclusion in dietary supplements in 2004. A Federal judge later overturned this ban in 2005 during a challenge by supplement maker Nutraceuticals. It is also debatable as to whether the ephedrine ban had more to do with its use as a precursor in methamphetamine manufacture rather than health concerns with the ingredient as such.[ citation needed ]

Non-pharmacological alternatives

Weight loss effects of water have been subject to some scientific research as a potential non-pharmacological approach. [8] Drinking water prior to each meal may help in appetite suppression. Consumption of 500 mL (approximately 17 fl oz) of water 30 minutes before meals has been correlated with modest weight loss (1–2 kg; 2 to 4 lb) in obese men and women over a period of 8 to 12 weeks. [9] [10]

List of anorectics

Numerous pharmaceutical compounds are marketed as appetite suppressants.

The following drugs are listed as "centrally-acting antiobesity preparations" in the Anatomical Therapeutic Chemical Classification System: [11]

The following are listed as appetite depressants by MeSH, an index of medical journal articles and books. [13]

Other compounds with known appetite suppressant activity include:

See also

Related Research Articles

<span class="mw-page-title-main">Ephedrine</span> Medication and stimulant

Ephedrine is a central nervous system (CNS) stimulant that is often used to prevent low blood pressure during anesthesia. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. It is of unclear benefit in nasal congestion. It can be taken by mouth or by injection into a muscle, vein, or just under the skin. Onset with intravenous use is fast, while injection into a muscle can take 20 minutes, and by mouth can take an hour for effect. When given by injection it lasts about an hour and when taken by mouth it can last up to four hours.

Appetite is the desire to eat food items, usually due to hunger. Appealing foods can stimulate appetite even when hunger is absent, although appetite can be greatly reduced by satiety. Appetite exists in all higher life-forms, and serves to regulate adequate energy intake to maintain metabolic needs. It is regulated by a close interplay between the digestive tract, adipose tissue and the brain. Appetite has a relationship with every individual's behavior. Appetitive behaviour also known as approach behaviour, and consummatory behaviour, are the only processes that involve energy intake, whereas all other behaviours affect the release of energy. When stressed, appetite levels may increase and result in an increase of food intake. Decreased desire to eat is termed anorexia, while polyphagia is increased eating. Dysregulation of appetite contributes to anorexia nervosa, bulimia nervosa, cachexia, overeating, and binge eating disorder.

<span class="mw-page-title-main">Benzphetamine</span> Chemical compound

Benzphetamine is a substituted amphetamine used short-term along with a doctor-approved, reduced-calorie diet, exercise, and behavioral program for weight loss. It is prescribed for obesity to people who have been unable to lose weight through exercise and dieting alone. It is a prodrug to dextroamphetamine and dextromethamphetamine.

<span class="mw-page-title-main">Fenfluramine/phentermine</span> Drug combination prescribed for weight loss; later withdrawn from market

The drug combination fenfluramine/phentermine, usually called fen-phen, was an anti-obesity treatment in the early 1990s that utilized two anorectics. Fenfluramine was marketed by American Home Products as Pondimin, but was shown to cause potentially fatal pulmonary hypertension and heart valve problems, which eventually led to its withdrawal in 1997 and legal damages of over $13 billion. Phentermine was not shown to have harmful effects.

<span class="mw-page-title-main">Fenfluramine</span> Medication used to treat seizures

Fenfluramine, sold under the brand name Fintepla, is a serotonergic medication used for the treatment of seizures associated with Dravet syndrome and Lennox–Gastaut syndrome. It was formerly used as an appetite suppressant in the treatment of obesity, but was discontinued for this use due to cardiovascular toxicity before being repurposed for new indications. Fenfluramine was used for weight loss both alone under the brand name Pondimin and in combination with phentermine commonly known as fen-phen.

<span class="mw-page-title-main">Anti-obesity medication</span> Class of pharmacological agents

Anti-obesity medication or weight loss medications are pharmacological agents that reduce or control excess body fat. These medications alter one of the fundamental processes of the human body, weight regulation, by: reducing appetite and consequently energy intake, increasing energy expenditure, redirecting nutrients from adipose to lean tissue, or interfering with the absorption of calories.

<span class="mw-page-title-main">Phentermine</span> Weight loss medication

Phentermine, sold under the brand name Ionamin among others, is a medication used together with diet and exercise to treat obesity. It is taken by mouth for up to a few weeks at a time, after which the benefits subside. It is also available as the combination phentermine/topiramate.

<span class="mw-page-title-main">Sibutramine</span> Appetite suppressant

Sibutramine, formerly sold under the brand name Meridia among others, is an appetite suppressant which has been discontinued in many countries. It works as a serotonin–norepinephrine reuptake inhibitor similar to a tricyclic antidepressant. Until 2010, it was widely marketed and prescribed as an adjunct in the treatment of obesity along with diet and exercise. It has been associated with increased cardiovascular diseases and strokes and has been withdrawn from the market in 2010 in several countries and regions including Australia, Canada, China, the European Union, Hong Kong, India, Mexico, New Zealand, the Philippines, Thailand, the United Kingdom, and the United States. However, the drug remains available in some countries.

The ECA stack is a drug combination used in weight loss and as a stimulant. ECA is an initialism for ephedrine, caffeine, and aspirin, with variants of it including the EC stack, which removes the aspirin for those who can not tolerate it. Dietary supplements based on or including elements of ECA were popular through the 1990s and early 2000s, but the marketing of ephedra- or ephedrine-containing stimulant combinations for weight loss and bodybuilding is now restricted or illegal in the United States and the Netherlands due to reports of heart attack, stroke, and death associated with these supplements.

<span class="mw-page-title-main">Amfepramone</span> Stimulant drug used as an appetite suppressant

Amfepramone, also known as diethylpropion, is a stimulant drug of the phenethylamine, amphetamine, and cathinone classes that is used as an appetite suppressant. It is used in the short-term management of obesity, along with dietary and lifestyle changes. Amfepramone has a similar chemical structure to the antidepressant and smoking cessation aid bupropion, which has also been developed as a weight-loss medicine when in a combination product with naltrexone.

<span class="mw-page-title-main">Aminorex</span> Chemical compound

Aminorex is a weight loss (anorectic) stimulant drug. It was withdrawn from the market after it was found to cause pulmonary hypertension. In the U.S., it is an illegal Schedule I drug, meaning it has high abuse potential, no accepted medical use, and a poor safety profile.

<span class="mw-page-title-main">Dexfenfluramine</span> Serotonergic anorectic medication

Dexfenfluramine, marketed as dexfenfluramine hydrochloride under the name Redux, is a serotonergic anorectic drug: it reduces appetite by increasing the amount of extracellular serotonin in the brain. It is the d-enantiomer of fenfluramine and is structurally similar to amphetamine, but lacks any psychologically stimulating effects.

<span class="mw-page-title-main">Chlorphentermine</span> Weight loss medication

Chlorphentermine is a serotonergic appetite suppressant of the amphetamine family. Developed in 1962, it is the 4-chloro derivative of the better known appetite suppressant phentermine, which is still in current use.

<span class="mw-page-title-main">Mazindol</span> Stimulant drug and appetite suppressant

Mazindol is a stimulant drug which is used as an appetite suppressant. It was developed by Sandoz-Wander in the 1960s.

Benfluorex, sold under the brand name Mediator, is an anorectic and hypolipidemic agent that is structurally related to fenfluramine. It may improve glycemic control and decrease insulin resistance in people with poorly controlled type-2 diabetes.

<span class="mw-page-title-main">Lorcaserin</span> Antiobesity drug

Lorcaserin, marketed under the brand name Belviq, was a weight-loss drug developed by Arena Pharmaceuticals. It reduces appetite by activating a type of serotonin receptor known as the 5-HT2C receptor in a region of the brain called the hypothalamus, which is known to control appetite. It was approved in 2012, and in 2020, it was removed from the market in the United States due to an increased risk of cancer detected in users of Belviq.

<span class="mw-page-title-main">Norepinephrine releasing agent</span> Catecholaminergic type of drug

A norepinephrine releasing agent (NRA), also known as an adrenergic releasing agent, is a catecholaminergic type of drug that induces the release of norepinephrine (noradrenaline) and epinephrine (adrenaline) from the pre-synaptic neuron into the synapse. This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine therefore an increase in adrenergic neurotransmission.

<span class="mw-page-title-main">Phentermine/topiramate</span> Obesity medication

Phentermine/topiramate, sold under the brand name Qsymia, is a combination drug of phentermine and topiramate used to treat obesity. It is used together with dietary changes and exercise. If less than 3% weight loss is seen after 3 months it is recommended the medication be stopped. The weight loss is modest. Effects on heart related health problems or death is unclear.

<span class="mw-page-title-main">Levofenfluramine</span> Non-marketed drug of the amphetamine class

Levofenfluramine (INN), or (−)-3-trifluoromethyl-N-ethylamphetamine, also known as (−)-fenfluramine or (R)-fenfluramine, is a drug of the amphetamine family that, itself (i.e., in enantiopure form), was never marketed. It is the levorotatory enantiomer of fenfluramine, the racemic form of the compound, whereas the dextrorotatory enantiomer is dexfenfluramine. Both fenfluramine and dexfenfluramine are anorectic agents that have been used clinically in the treatment of obesity (and hence, levofenfluramine has been as well since it is a component of fenfluramine). However, they have since been discontinued due to reports of causing cardiovascular conditions such as valvular heart disease and pulmonary hypertension, adverse effects that are likely to be caused by excessive stimulation of 5-HT2B receptors expressed on heart valves.

5-HT2C receptor agonists are a class of drugs that activate 5-HT2C receptors. They have been investigated for the treatment of a number of conditions including obesity, psychiatric disorders, sexual dysfunction and urinary incontinence.

References

  1. ↑ Lemke, Thomas L.; Williams, David A., eds. (2012). "Anorexiants as Pharmacologic Agents in the Management of Obesity". Foye's Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 1451–6. ISBN   978-1-60913-345-0.
  2. ↑ fi:Pervitiini
  3. ↑ Ulrich, Andreas (May 6, 2005). "The Nazi Death Machine: Hitler's Drugged Soldiers". Spiegel Online. Retrieved 2011-01-05.
  4. ↑ Bett, W. R. (1946-08-01). "Benzedrine Sulphate in Clinical Medicine". Postgraduate Medical Journal. 22 (250): 215. doi:10.1136/pgmj.22.250.205. ISSN   0032-5473. PMC   2478360 . PMID   20997404.
  5. ↑ Heal, David J; Smith, Sharon L; Gosden, Jane; Nutt, David J (June 2013). "Amphetamine, past and present – a pharmacological and clinical perspective". Journal of Psychopharmacology. 27 (6): 486. doi:10.1177/0269881113482532. ISSN   0269-8811. PMC   3666194 . PMID   23539642.
  6. ↑ Abenhaim, Lucien; Moride, Yola; Brenot, François; Rich, Stuart; Benichou, Jacques; Kurz, Xavier; Higenbottam, Tim; Oakley, Celia; Wouters, Emil; Aubier, Michel; Simonneau, Gérald; Bégaud, Bernard (1996). "Appetite-Suppressant Drugs and the Risk of Primary Pulmonary Hypertension". New England Journal of Medicine. 335 (9): 609–16. doi: 10.1056/NEJM199608293350901 . PMID   8692238.
  7. ↑ Fishman, A. P. (1999). "Aminorex to Fen/Phen : An Epidemic Foretold". Circulation. 99 (1): 156–61. doi: 10.1161/01.cir.99.1.156 . PMID   9884392.
  8. ↑ Handbook of Non Drug Intervention (HANDI) Project Team (2013). "Pre-meal water consumption for weight loss". Australian Family Physician. 42 (7): 478. PMID   23826600.
  9. ↑ Dennis, Elizabeth A.; Dengo, Ana Laura; Comber, Dana L.; Flack, Kyle D.; Savla, Jyoti; Davy, Kevin P.; Davy, Brenda M. (2009). "Water Consumption Increases Weight Loss During a Hypocaloric Diet Intervention in Middle-aged and Older Adults". Obesity. 18 (2): 300–7. doi:10.1038/oby.2009.235. PMC   2859815 . PMID   19661958.
  10. ↑ Vij, Vinu Ashokkumar; Joshi, Anjalis (2014). "Effect of excessive water intake on body weight, body mass index, body fat, and appetite of overweight female participants". Journal of Natural Science, Biology and Medicine. 5 (2): 340–4. doi: 10.4103/0976-9668.136180 . PMC   4121911 . PMID   25097411.
  11. ↑ ATC/DDD Index
  12. ↑ "FDA requests the withdrawal of the weight-loss drug Belviq, Belviq XR (lorcaserin) from the market". Center for Drug Evaluation and Researcher. FDA. 2020-02-13.
  13. ↑ MeSH list of agents 82001067
  14. ↑ "European Medicines Agency recommends withdrawal of benfluorex from the market in European Union". European Medicines Agency. December 12, 2009. Retrieved August 22, 2022.
  15. ↑ "Attention deficit hyperactivity disorder (ADHD) - Treatment". nhs.uk. 2018-06-01. Retrieved 2021-09-20.
  16. ↑ "Adderall Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD". www.webmd.com. Retrieved 2021-09-20.
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  18. ↑ Wood, Douglas M; Emmett-Oglesby, Michael W (1988). "Substitution and cross-tolerance profiles of anorectic drugs in rats trained to detect the discriminative stimulus properties of cocaine". Psychopharmacology. 95 (3): 364–8. doi:10.1007/BF00181948. PMID   3137623. S2CID   1105026.
  19. ↑ Schubert, Matthew M.; Irwin, Christopher; Seay, Rebekah F.; Clarke, Holly E.; Allegro, Deanne; Desbrow, Ben (December 2017). "Caffeine, coffee, and appetite control: a review". International Journal of Food Sciences and Nutrition. 68 (8): 901–912. doi:10.1080/09637486.2017.1320537. hdl:10072/345209. ISSN   1465-3478. PMID   28446037.
  20. ↑ Mohammadpour, Saba; Amini, Mohammad Reza; Shahinfar, Hossein; Tijani, Aliyu Jibril; Shahavandi, Mahshid; Ghorbaninejad, Parivash; Djafarian, Kurosh; Shab-Bidar, Sakineh (September 2020). "Effects of glucomannan supplementation on weight loss in overweight and obese adults: A systematic review and meta-analysis of randomized controlled trials". Obesity Medicine. 19: 100276. doi:10.1016/j.obmed.2020.100276. S2CID   225213522.
  21. ↑ Guo, Liping; Yokoyama, Wallace; Chen, Maoshen; Zhong, Fang (November 2021). "Konjac glucomannan molecular and rheological properties that delay gastric emptying and improve the regulation of appetite". Food Hydrocolloids. 120: 106894. doi:10.1016/j.foodhyd.2021.106894. ISSN   0268-005X.
  22. ↑ Klok, M. D.; Jakobsdottir, S.; Drent, M. L. (January 2007). "The role of leptin and ghrelin in the regulation of food intake and body weight in humans: a review". Obesity Reviews. 8 (1): 21–34. doi: 10.1111/j.1467-789X.2006.00270.x . PMID   17212793. S2CID   24266123.
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  25. ↑ "Why smoking makes you lose weight and no, it's not a good idea". The Times of India. ISSN   0971-8257 . Retrieved 2024-01-28.
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