Drug therapies are considered a desirable alternative to surgical treatments or other weight loss solutions whenever possible because of the cost and time savings involved. The mechanisms of drug treatment for weight loss include inhibiting appetite, increasing energy expenditure, stimulating fat movement, lowering triacylglycerol synthesis, and inhibiting fat absorption. Examples of weight loss drugs are phenylpropanolamine (PPA), orlistat, and sibutramine. There are three main ways for the pharmaceutical treatment of overweight and they’re inhibition of absorption of nutrition in the intestine; modulation of the activities of the metabolic and central nervous system (hypothalamic) satiety and food consumption signals; and induction of energy dissipation in tissues, especially adipose tissue (thermogenesis). The drugs used to promote weight loss are anorexiants or appetite suppressants.

Various pharmaceutical compositions have been developed with the purpose of stimulating thermogenesis and thereby inducing weight loss. In general, weight loss medications used to treat or prevent obesity are directed at the adipocyte compartment of the tissue and work by either decreasing energy availability or increasing energy output. These pharmaceutical agents can be placed into three categories based on mechanism. For example, some weight loss drugs act by mimicking the effects of endogenous neurotransmitters, and are capable of directly replacing these neurotransmitters in their actions on receptors. Which, in turn, results in increased activity of the cells which possess the receptors. Where these receptors are typically responsive to the endogenous hormones adrenaline (epinephrine) and noradrenaline (norepinephrine). Adrenaline (epinephrine) and noradrenaline (norepinephrine) mediate the activities of the sympathetic nervous system, such substances are termed direct-acting sympathicomimetic agents.

Another major class of weight control medications are drugs which promote malabsorption of nutrients through suppression of digestive enzymes. Acarbose is a bacterial inhibitor of amylase and brushborder glycosidases. Another similar agent is tetrahydrolipostatin which is a fungal inhibitor of lipases. These weight control agents act by preventing digestion of carbohydrates or fats, and in this way create an effective reduction in the quantity of calories absorbed, despite continued food consumption. One drawback is that virtually complete inhibition of the respective enzymes must be maintained throughout the digestive period, a situation that can be rarely achieved.

Weight loss drugs approved by the FDA for long-term use may be effective as an adjunct to weight loss diet and physical activity for obese patients. Orlistat and sibutramine are two Food and Drug Administration (FDA) approved anti-obesity drugs. Orlistat works by inhibiting pancreatic lipase activity in the small intestine. Pancreatic lipase breaks down triglycerides into fatty acids and monoglycerides which are subsequently absorbed into the body. Thus inhibition of lipase activity may effective reduces fat absorption from food. Sibutramine is a serotonin and norepinephrine reuptake inhibitor and reduces body weight by suppressing appetite. FDA has approved it for the treatment of obesity for up to 2 years.

Phentermine has been used as oral monotherapy for weight loss since about 1970. Phentermine monotherapy can increase weight loss when used in combination with diet and exercise, as compared to diet and exercise alone. Phentermine acts on the cerebral appetite center to reduce appetite, and is effective for about two weeks, but then quickly loses effect. Phentermine is not approved by the FDA. for use beyond six weeks for this reason. Moreover, phenterrine monotherapy is associated with side effects, including nervousness, insomnia and constipation. People have also taken prescription stimulants and thyroid medications. These can only be used temporarily and have many side effects. Thermogenic drugs are also sometimes used for promoting weight loss. The catecholamine medications have some thermogenic activity, in addition to their suppression of appetite.

Drug therapy for weight reduction has undergone radical changes over the past decades. Various weight loss drugs have been used to treat obesity, but all have been inadequate because they are either dangerous, ineffective, or quickly lose their effect. Currently, no single drug regimen has been reported as superior in either promoting or sustaining weight loss. Pharmaceutical compositions designed for weight loss and fat loss, more or less, carry considerable side effects. In the face of the increasing needs for physical slimness and the high prevalence of obesity and overweight, there is a need for new pharmaceutical solutions and compositions to promote and maintain weight loss with long term effects and free of serious complications.

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