Diet Drugs

We all belong to one of two groups. We either burn as many calories as we eat or we don't.

Those that don't burn enough, gain weight.

 

As a consequence of inactivity Americans have gotten soft and fat.

 

Losing weight is much harder to do than not gaining it in the first place is. That is why it is extremely difficult to not gain weight, at some point in life.

With the need to lose so high, the number of nutritional gurus with gimmicks and potions, preaching pie-in-the sky answers has grown with it.

 

 

Americans, spend much of their day studying, reading, speaking, computing, and playing video games. Highly inactive activities.

No disrespect to the sedentary, but while these activities keep the world afloat, they don't make physical demands on mitochondria.

They are stressful as well.

But cognition is not the type of work that burns calories.

 

Intellectual work challenges nervous tissue, not striated muscles.

 

 

Good health requires active muscles not sedentary ones.

 

With over half the American population considered overweight or fa there is no shortage of desperate disciples and no shortage of miracle solutions.

In considering our preoccupation and obsession with losing weight, it is worth remembering the words of the noted critic of the American middle class, Henry Lewis Mencken, who said, ‘no one ever went broke underestimating the intelligence of the American people'.

 

As the waistlines of Americans continue to swell, a plethora of books, seminars, programs, and organizations have been developed to reverse one's personal expansion. This, in addition to the pharmaceutical drugs, natural herbs, and weight loss drinks, purported to help lose weight, stock the shelves of the new comfort stations, Walgreens, CVS, ad nusaseum. 

This simplest way to lose weight or more precisely to lose body fat is to exercise more.

 

Meridia

Meridia (sibutramine), manufactured by Abbott Laboratories was approved by the Federal Drug Administration in 1997, as an oral treatment for obesity. Sibutramine is known as Reductil in Europe. Meridia (sibutramine) is an expensive drug and chemical cousin of amphetamine.

 

Meridia is similar to amphetamines in structure and effect and binds to the same receptors. Sibutramine affects the brain's appetite control centers without completely suppressing appetite.

 

Meridia represses appetite and enhances satiety by preventing the breakdown and reuptake of the three main neurotransmitters involved with appetite and mood, serotonin, norepinephine, and dopamine.

Despite prolonging the action of these neurotransmitters, sibutramine does not provide any antidepressant activity.

 

Meridia causes an increase in pulse rate and blood pressure. Since Meridia was introduced at least thirty patients have died due to cardiac arrest and studies have been undertaken regarding reports of  heart and kidney failure.

The FDA has made no attempts to withdraw the drug despite Dr. David Graham’s testimony before Congress that sibutramine may be more dangerous to health than the conditions it is intended to treat (obesity).

 

Side effects of Meridia include dry mouth, headache, constipation, insomnia, and increased blood pressure.

Meridia is only recommended to the serious obese because their excess weight pose more of a threat to their health than the harmful side effects of the drug.

 

Rimonabant

Rimonabant (Acomplia) is a new diet drug developed by the French pharma firm, Sanofi-Aventis. It has been available in Europe since 2006 for use as an adjunct to diet and exercise to help obese patients lose weight.Despite the approval by the FDA in February 2006 for its obesity indication and its non-approvable or its use as a smoking cessation aid, the drug did not enter appear in the US market  Sanofi-Aventis response tto the FDA’s actionb triggered a review process.

In 2007, the FDA's Endocrine and Metabolic Drugs Advisory Committee (EMDAC) concluded that Sanofi-Aventis had failed to demonstrate the safety of rimonabant and voted against recommending the anti-obesity treatment for approval

 

 

Rimonabant is a endocannabinoid receptor antagonist, which binds to cannabinoid receptors in the brain.

 

Rimonabant works by blocking the naturally produced or endogenous cannabinoid from binding to its neuronal receptor in the brain by occupying its binding site. These are the same receptors that the active ingredient in marijuana, THC or tetrahydrocannabinol binds to.

 

Activation of these receptors by endogenous cannabinoids, such as anandamide, or exogenous ones like THC, increases appetite. This explains the munchies phenomena of marijuana.

 

This endocannabinoid receptor antagonist offers a novel therapeutic approach to appetite control and weight reduction.

Rimonabant was originally intended to help smokers repress the urge to smoke smoking because the endocannabinoid system is involved in the body's response to tobacco dependence.

Orlistat

Orlistat (Xenical) is a new expensive drug developed to fight the war on obesity. It was  approved by the FDA in 1999 to treat obesity. Xenical is supposed to be prescribed to individuals who maintain a body mass index over 30. Orlistat acts by decreasing the intestinal absorption of fat.

Xenical is a much safer alternative to Meridia. Xenical neither mimics nor inhibits nerve transmissions. Instead it targets the digestive tract and blocks the absorption of fats.

Roche Holding AG is the manufacturer of the drug and granted exclusive rights to GlaxoSmithKline of Great Britain.

In its short history, Orlistat has become the most widely prescribed weight loss drug on the planet. It sales are over $500 million a year with no limit to its growth. Orlistat is only the second drug prescribed for long term use, Meridia is the other.

Orlistat is known to cause gastrointestinal side effects including diarrhea and flatulence as well as prevent the absorption of fat soluble vitamins.

Xenical is available by prescription in 120 mg doses. Xenical is taken three times a day for the purpose of inducing artificial fat maldigestion. It is claimed that patients on Xenical have lost an average of 13 pounds in one year.

Orlistat (tetrahydrolipstatin or THL) is a specific lipase inhibitor derived from lipstatin, a lipid produced by the bacteria Streptomyces toxytricini.  Lipase is an enzyme that aids in the absorption of lipids in the small intestine.  By interfering with the lipase enzyme, the amount of fat absorbed in the small intestine is reduced. The less fat absorbed in the gut, the more that will be excreted along with its high calorie content.

Early in 2007, this miracle weight loss drug was approved by the FDA as an OTC (over-the-counter) drug. The dosage in the OTC version is half (60mg) that of the prescription only drug(120mg).

Studies have failed to demonstrate any benefit from six months use at this low dose so it may not even be effective. Of course one could always take two pills instead, but that was supposed to require a prescription.

The OTC version is known as Alli (pronounced ally).  Alli is manufactured by GlaxoSmithKine, the same people who brought us the dangerous diabetic drug, Avandia.  Alli was approved by the FDA despite concerns of causing pre-cancerous lesions in the colon. The media treated its approval as a fantastic development and shinning example of how modern medicine can respond to our national crisis with this miracle drug. The debate over whether the risks posed by teenage abuse of orlistat warrants its inclusion as an OTC drug never materialized.

In June of 2007, Alli was launched along with diet program promoting it as the no-brainer way to lose weight. There are many non-obese dieters who will be using this drug despite its marginal benefits and common gastrointestinal disturbances. Furthermore, because it prevents proper fat absorption, there is a significant reduction in the absorption of fat soluble vitamins (vitamins A, D, K and E) putting its users at risk for other diseases.

 

Obesity med use will surely rise as as this ‘treatment’ makes its way into more and more American lives.

A botanical version of Xenical utilizes the herb panax japonicus. The rhizome of the plant is high in a triterpenoid  saponin (chikusetsusaponin). Saponins are the active agents of plants. Their structure, chemistry and solubility are similar to steroids and other lipids. They interact with many of the same receptors as hormones and drugs.

Panax japonicus is often used as a substitute for ginseng but is quite diiferent. This species contains a unique compound called chiku-setsu saponin. Chiku-setsu saponin inhibits the same lipase enzyme as the pharmaceutical drug, orlistat.

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