OBESITY AND ITS PHARMACOTHERAPY: AN UPDATE

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Gangwal et al. World Journal of Pharmacy and Pharmaceutical Sciences
OBESITY AND ITS PHARMACOTHERAPY: AN UPDATE
Amit Gangwal*, Deep Yadav, Nidhi S Nair, Sanjay Jain
Smriti College of Pharmaceutical Education, Indore, India.
ABSTRACT
Obesity is recognized as a social problem, associated with serious
health risks and increased mortality. It is defined as excessive
accumulation of body fat that may impair health. It has become a
worldwide epidemic. WHO has cited obesity as a global epidemic.
Close to half of the adult population in OECD countries is overweight
(body mass index ≥ 25 Kg/m2
). Obesity is known to be related to
increased risks of coronary heart diseases, hypertension, non-insulin-
dependent diabetes mellitus and certain type of cancer. Many synthetic
drug therapies are available for the treatment of obesity, but they are
not devoid of side effects and not recommended for long term therapy
plus their long term efficacy is not established satisfactorily, e. g.
Orlisat (Xenical®
), Sibutramine (Reductil®
). Sibutramine and orlistat
possess the risk of some side effects like depression, anxiety, gallbladder diseases, liver
damage, allergic reaction, gastro intestinal diseases. Phentermine and Topiramate (Qsymia®
)
combination is also used in management of obesity. These drugs help in reducing 3-4% of the
body weight. Plentiful trials have been conducted to find and develop new anti-obesity drugs
through herbal sources and conventional options, but still outcome is not encouraging and
promising. The major factor contributing to obesity is imbalance between energy intake and
expenditure. One most important approach in the treatment of obesity includes the
development of nutrient digestion and absorption inhibitors, in an attempt to reduce the
energy intake through gastrointestinal mechanisms without altering any central mechanisms.
Inhibition of digestive enzymes is one of the most widely studied mechanisms used to
determine the potential efficacy of natural products as anti-obesity agents. In this article an
attempt has been made to crawl highly relevant information pertaining to current option and
ongoing research to manage and treat obesity.
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Article Received on
28 August 2013,
Revised on 19 Sept 2013,
Accepted on 24 November
2013
*Correspondence for
Author:
*Dr. Amit Gangwal
Smriti College of
Pharmaceutical Education,
Indore, India.
gangwal.amit@gmail.com

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Gangwal et al. World Journal of Pharmacy and Pharmaceutical Sciences
Key words: Obesity, Sibutramine, Orlisat, Phentermine, Topiramate.
INTRODUCTION
Obesity is defined as BMI (body mass index) 30kgm2
or more. A person with a BMI
between 25 and 29.9 are considered over weight but not obese. BMI is a simple index of
weight-for-height that is commonly used to classify overweight and obesity in humans. It is
also defined as a person’s weight in kilograms divided by the square of his height in meters
(kgm2). As per world health organization (WHO), BMI greater than or equal to 25 is
overweight and BMI greater than or equal to 30 is obese. Obesity is a foremost health
problem not only in developed nations but also in developing countries. It increases the risk
of other diseases like diabetes, cardiovascular ailments, fatty liver and some forms of cancer1
.
Obesity is now so common in various geographies that it is beginning to replace conditions
arising from malnutrition and infectious diseases as the most significant contributor to ill
health. Obesity is measured using BMI and further evaluated in terms of fat distribution via
the waist–hip ratio and total cardiovascular risk factors2
. BMI is closely related to
both percentage body fat and total body fat3
. The global epidemic of obesity results from an
amalgamation of such factors as genetic susceptibility, increased availability of high-energy
foods and diminished need of physical activity in prevailing situation in modern society.
Obesity is no more a cosmetic issue affecting certain individuals, but a pandemic threatening
global well being because it exacerbates a large number of health-related problems, both
independently and in association with other ailments4,5
. Present article describes
pharmacotherapy and ongoing research to address this menace.
Pathophysiology
Insufficient expenditure of calorie leads to storage of extra calories as fat in body. A calorie is
a unit of energy that body gets from food. Eating too many calories and not being physically
active increases one’s risk for obesity. Aged people are more prone to weight gain, owing to
age related changes in body. Some medicines may also cause weight gain. One may also be at
a higher risk if she has a family member who is obese. Being overweight as a child makes
you more likely to be obese. Some causes of weight gain include: poor diet: A person has a
poor diet if he eats too many foods that are high in fat and sugar. Examples are hamburgers,
french-fries, donuts, potato chips, and sugar-sweetened soda. Eating these foods often can
cause one to consume more calories than his body needs. Other factors are sedentary life
style: A person may not undergo exercise, if he is a couch potato, plays video games and

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Gangwal et al. World Journal of Pharmacy and Pharmaceutical Sciences
spends a major chunk of time on digital stuff and does not come out of digital world owing to
professional or personal reasons. Certain medicines and diseases can cause weight gain, or
make it more likely that person will be obese.
Genetic influences: The genetic makeup plays a significant role in the chances of becoming
obese. However, person still maintain most of the control when it comes to the weight. Some
rare genetic diseases make it almost impossible to avoid obesity. Physiological influences:
Some researchers are of the opinion that every person has a predetermined weight that the
body resists moving away from. Also, people of the same age, sex and body type often have
different metabolic rates. It indicates that their body burn food differently in different
individuals. Someone with a low metabolic rate may require fewer calories to maintain
approximately the same weight as someone whose metabolic rate is high. Food intake and
eating disorders: Binge consumption in depression and some eating disorders may lead to
obesity11
.
Pharmacotherapy of obesity
Obesity treatments include physical activity, changes in eating behavior, pharmacotherapy,
weight reducing medicinal plants, acupuncture etc. Antiobesity drugs may be taken to reduce
appetite or inhibit fat absorption together with a suitable diet. If diet, exercise and medication
are not successful, other options are available. A gastric balloon may assist with weight loss,
or surgery may be performed to condense stomach volume and/or bowel length, leading to
earlier feeling of satiety and reduced ability to absorb nutrients from food6
. Many synthetic
drug therapies are available for the treatment of obesity e. g. orlisat (Xenical®
): a pancreatic
lipase inhibitor which can block 30% of triglyceride hydrolysis in subjects eating a 30% fat
diet7
, sibutramine (Reductil®
): neurotransmitter reuptake inhibitor, rimonabant (Acomplia®
):
cannabinoid-1 receptors blocker. Sibutramine showed increased incidence of serious, non
fatal cardiovascular events and rimonabant has been shown to possess risk of depression and
anxiety. The relatively safer orlistat also possesses several side effects like signs of liver
damage, allergic reaction, gallbladder disease etc. Orlistat’s use is associated with high rates
of gastrointestinal side effects8
. Weight loss caused by these synthetic drugs however is
modest with an average of 2.9 kg at 1 to 4 years and there is scarcity of data on how these
drugs influence longer-term complications of obesity. A combination of phentermine and
topiramate (Qsymia®
) is also fairly effective in treatment of obesity9
. Recently USFDA has
given consent to a pill (lorcaserin under the trade name Belviq®
) that could help to treat

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Gangwal et al. World Journal of Pharmacy and Pharmaceutical Sciences
obesity. It can help people to lose about 3–4% of their body weight when combined with
other classical way to combat obesity like a healthy diet and exercise. The drug has been
approved for use by obese people with a BMI greater than 30, and for a subset of overweight
people (BMI > 27) who have health conditions such as high blood pressure, elevated
cholesterol and type 2 diabetes. In the past two years, the USFDA has rejected around 3
obesity drugs because of safety concerns or lack of efficacy. The USFDA advisory committee
recommended in March 2012 that all antiobesity drug candidates should pass cardiovascular
risks assessing tests10
.
DISCUSSION AND CONCLUSION
Obesity threat is replacing morbidity and mortality arising from malnutrition and infectious
disease as most significant contributor to ill health. The rising incidence and prevalence of
obesity, especially in developing countries will warrant involvement of governments and
individuals. Plant treatments may be more culturally acceptable for some people and
exploiting foodstuffs as obesity treatments may be easier to incorporate into a lifestyle than
taking a tablet or injections. Obesity is often a lifelong problem. Many of the currently
available treatments for obesity aim to reduce body weight or manage obesity for
impermanent period; there is a need for some solution which can address obesity in a longer
lasting or permanent way. Once excess weight is gained, it is not easy to lose. Once lost, you
will have to work at maintaining your healthier weight. The continuing rise in occurrence of
obesity worldwide will require new solutions to be found for treatment, management and
prevention of obesity. Because humanity does not appear inclined to take more exercise or
avoid opulent life style, the emphasis over the next few decades is likely to be on treating
obesity and might be possible that next Lipitor®
will be again from metabolic therapy. There
is an urgent need of exploring all the available options to address the menace of this
metabolic disorder.
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