11
Jan 12

Drugs helping in weight loss

The medical professions use drugs to treat everything from cold to flu,cancer to AIDS.The use of drugs in weight loss are not magic, they enhance the effect of diet and exercise.

The national institute for clinical excellence and the national obesity forum both recommend pharmacotherapy or medications as a appropriate for patients who either who haven’t been successful with weight management program based around lifestyles, exercises on nutritional advice or are considered at that much risk of the co morbidity associative with obesity so that they need to lose weight more rapidly.

Many of the drugs on the market today affect the metabolic system or influence hormones and the nervous tissues. Manipulating one or all three can affect food intake or energy expenditure.

The common drugs therapies used today include:

A)     Drugs that are designed to control how much food is eaten.

B)      Drugs that stimulate the brain adding the feeling of satiety ”I’m full”

C)      Drugs that slow the food break down in the gut

D)     Drugs that interfere with nutrient absorption

E)      Drugs that increase the heat production.

F)      Drugs that increases the lean body mass

Anorectic drugs

 Anorectic drugs work by suppressing the appetite (the desire to eat). Obviously of less food is consumed then less total calories are ingested causing some type of loss in body weight.

All anorectic drugs resemble the sympathomimetic amines, sympathomimetic amines are released in the body in response to direct stimulation of the nervous system. The nervous system has 2 parts: sympathetic and parasympathetic.

At rest the parasympathetic system tends to override or dominate over the sympathetic nervous system. During exercise or periods of physical and emotional stress, the sympathetic system is activated.

The sympathetic nervous system stimulates a cascade of physical reactions that can elevate metabolism, fat breakdown and decrease the desire to consume food.

Sympathetic drugs are relative of amphetamines, amphetamines promote several effects in human including a decreased intake in food consumption, an increase in well being, an individual feels better, increased sympathetic nervous system activity, a change in brain activity and cardiovascular changes.

Some effects of amphetamines are beneficial. The decreased food intake and increased sympathetic nervous system activity lead to weight loss, but the negatives are extremely clear. Over stimulation of the brain and systemic nervous system and a constant change in mood where the user is in a state of euphoria makes amphetmaines highly addictive. And there are a lot of cardio effects as: High blood pressure and increased heart rate alone are two risk factors common to the individual prone to experience of heart attack. So, while amphetamines show tremendous promise as a weight loss aid, they are extremely dangerous. So, medicine marches on looking for products having the same effect on weight loss without the side effects.

Another example of the anorectic drugs is Sibrutramine, it is an amphetamine like drug. Also it acts on the satiety center in the brain to activate the feeling of fullness. During the first weeks the blood pressure might go higher and may need doctor supervision to make it remain under control

Another example of the anorectic drugs is Rimonabant (accomplia), it is a cannabinoid receptor antagonist (CB1) which has a great effect in reducing the appetite. It increases blood pressure but decreases cholesterol, decreases weight. It is approved in Europe at first but taken off the market and it was not approved by FDA due to its side effects such as: increased incidence of suicide attempts and depression to patients taking the drug.

orlistat (xenical)

 They are lipase inhibitors and it works by reducing the amount of fat absorbed in to your body. About one third of any fat that put into the patient’s mouth is not absorbed. The main concern side effect is the oily diarrhea that’s why those patients are instructed to eat low fat diet. Orlistat is sold in the form of 120 mg dose.

Alli

The first over the counter approved FDA approved weight loss pill. Alli is a weight loss pill that block the absorption of up to 25% percents of the fat patient consumes by attaching to the enzyme that breaks down fat preventing its digestion. Undigested fat can’t be absorbed and stored. ALLI is a lower dose of drug called orlistat (xenical). Alli is sold in 60 mg doses to the patients over 18 years old. It is contraindicated in patients who are pregnant or breast feeding, organ transplant patients, patients suffer from malabsorption, people taking cyclosporine.

Ephedrine

Ephedrine is a beta agonist and has been shown to both increase lean body weight and decrease body fat percentage. Adrenergic receptors stimulated by adrenergic agonists (like ephedrine) control the cells response to stress hormones. Ephedrine stimulates the release if catecholamines in the body. Catecholamines act on fat cells by allowing them to be broken apart to be used as fuel.

Catecholamines can be considered catalysts; they’re necessary to initiate fat cell break down. Ephedrine also stimulates the sympathetic nervous system, similar to phentermine. The result is a decrease in appetite and an increase in caloric expenditure.

Ephedrine causes calories to be burned in two ways. By stimulating the sympathetic nervous system, it promotes the release of messengers that make brown fat, the internal fat surrounding organs, more energy dependant. Since brown fat is metabolically active, it requires calories, stimulating brown fat can increase its fuel needs creating calorie expenditure without exercise.

The second way ephedrine burns up calories is by increasing dietary induced thermogenesis. Foods that cause an increase in heat production in the body will create a greater increase in heat production with ephedrine use.

Caffeine prolongs the effects of ephedrine in the body. There are multiple studies showing 20 mgs a day of ephedrine combined with 200 mgs of caffeine and a reduced calorie diet causes more fat loss and greater retention of lean body mass than with the exact same diet.

So besides stimulating caloric expenditure, ephedrine and caffeine cause the body to hold ontp and retain muscle mass while dieting which keeps the metabolic rate elevated which is the most important factor in shedding body fat while decreasing calories.

This product should also be used only under close medical supervision.

Caffeine pills

Caffeine increases the body metabolic rate, also it increase in carbohydrates and fat oxidation. Caffeine increases lipolysis from the adipose tissue leading to less fat stored. If it is taken with proper quantities and proper exercise-diet program, caffeine pills will show a strong effect in weight loss.

Testosterone

Testosterone is the male hormone that dramatically increases upon puberty and declines after the age of 30. It is responsible for secondary sex characteristics of the make increased facial and body hair and a deepening of the voice.

Testosterone builds muscle.remeber, muscle builds metabolic rate. While not approved for weight control because it doesn’t work like traditional drugs(decreasing appetite or stimulating the nervous system) testosterone could be used to alter the muscle of fat ratio in the body. In a study in The New England Journal of Medecine(july 4,1996) showed that testosterone can increase the muscle mass without exercise and muscle mass is the single greatest factor that increases metabolism and caloric expenditure.

Side effects of testosterone pills include low sperm count, water retention, and change in HDL or LDL levels, possible high blood pressure and depression upon cessation.

Growth hormone

Growth hormone (GH) is released from pituitary gland within 30 to 90 minutes of dozing of to sleep. The release is greatest in teenage years and begins to decline after the mid twenties. By the time a person reaches 60, GH levels are very small compared to that of a twenty year old. GH is lipolytic( it burns fat). Declining GH levels as one age is a reason individuals gain fat and lose muscle mass. Because GH supports the immune function, prevents bone loss and supports the retention of lean body mass.

About 8 years ago, recombine GH that made in laboratory, was so expensive, only the wealthy could afford GH therapy as a means to control fat. These days, the price is radically lower and longevity clinics prescribe it like candy to anyone who walks through the front door.  Synthetic GH is injected daily, sometimes twice daily to mimic the body’s own GH. In time, GH causes a shifting effect in the metabolism where the body tries to burn a higher percentage of fatty acids than glucose. GH increases amino acid uptake by muscles and can build small amounts of lean body mass without weight training. Slight increase in lean body mass exerts metabolic boosting effects on the body. Incorporating GH with training and exercise would surely yield greater losses in body fat than exercise and diet alone

Side effects include high blood pressure, carpel tunnel syndrome and possible changes in HDL and LDL levels.

Oxandrin

Oxandrin(oxandrolone) is an anabolic hormone that increases the lean body mass with  as little influence on developing secondary male sex characteristics. Women often use oxandrin in small quantities to increase or hold onto lean body mass while dieting. Side effects include high blood pressure, water retention, potential low sperm count.

Phen-fen

It’s been off the market in the US. Both phentermine and fenfluramine were around for years before being off the market due to serious complaints of heart valve problem. That saud, both have been successful in decreasing total food consumption. While decreasing food consumption causes a caloric deficit and weight loss, phentermine also works on other mechanism outside of appetite suppression.

Fenfluramine works by altering the use of the neurotransmitter serotonin. Serotonin is a brain messenger and incrases dramatically with a high carbohydrate meal.  In lean individuals, serotonin seems to stimulate satiety causing the individual to eat less food. In the obese persons there appears to be some type of defect in serotonin’s ability to promote a feeling of being full.

Phentermine can increase the resting basal metabolism by its stimulatory effects on the nervous system similar to, though drastically stronger than, caffeine found in coffee. Being a sympathomimetic, it also causes the release of noradrenaline which promote the fight or flight resp[onse which in turn signals more fat to be broken down to be used as fuel. Due to its strong stimulatory effects, many find it undesirable reporting feelings of anxiety, restlessness and insomnia. As an appetite suppressant, it is probably the strongest product available.

Fenfluramine acts as a mild sedative by increasing the availability of serotonin. Thought not fully understood, scientists recognize the more serotonin available, the lesser the desire to eat. This product is hard to find even over the internet, so many dieters have resolved to 5-HTP a natural byproduct of the amino acid tryptophan, and readily available to any health food store. 5-HTP also increases serotonin as does the herb” St John’s Wort” . As an alternative to fenfluramine, dieters often combine 1000 mgs of St John’s Wort with 500 mg of 5-HTP before going to bed. In addition, they use a mix of caffeine, ma huang and coleus in the morning to stimulate the metabolism and increase the calorie expenditure.

Although the phen-fen mix were on the market for years, it was not until 1992 after a study at the University of Rochester showed a combination of the two appetite suppressing drugs were more effective than the traditional regime of lower calories and exercise. The Rochester study showed across the board that a diet and exercise plan combined with Phen-Fen yielded better results than diet and exercise alone. In the mean time, millions ran to the doctors for the dynamic due and in short time, reports of heart valve damage began to surface.  The drugs enhance the problems already present in the heart so may not prescribed to patients with heart problems.

Redux

 Redux also known as dexfenfluramine, they are originally found in France and former French colonies in North Africa. People in the US are still using it mainly because physicians are no longer having access to phentamine and fenfluramine. However, when approved by the FDA in the late 1990’s it lost 30% of it’s stock value in a single day.

Redux is very similar to fenfluramine but it is thought to work better with less side effects. Therefore with fewer side effects it can be used for longer period of time. Generally, physicians fell comfortable prescribing Redux for up to a full year where previously most seemed to feel comfortable to wean patients from Phen-Fen after a few months.

In a yearlong study with Redux, 6.4 % of subjects using the drug lost 5 % or more of their body weight and more than 20 % of the subjects lost at least 15 % of their body weight.

However, a study published in the New England Journal of Medicine (Aug, 29, 1996) reported a rare life threatening side effect of redux which is called primary pulmonary hypertension. The primary pulmonary hypertension creates a resistance which puts a stress on the heart. Researches in Europe found those using Redux have a 6 fold increase chance of experiencing primary pulmonary hypertension and those using the drug for very long periods of time will be subjecting themselves to a 23 fold increase in risk.

Neither redux or Phen-Fen are designed for people who have a few pounds to lose or are mildly over weight. First time dieters and those who have less than 30 pounds to lose can radically change body composition with the right training and eating program. These pills are not a magic bullet and an “end all” to weight management.



08
Dec 11

Mega Hoodia: The Wonders on Weight Loss

Mega Hoodia: The Wonders on Weight Loss

 

Mega Hoodia is a dietary supplement containing a dehydrated extract of Hoodia Gordonii, a spiny plant common in South Africa, Botswana and Nambia. The plant consists of a mixture of novel steroid glycosides that are said to suppress the appetite and therefore, decreasing food intake and body weight. The specific mechanism of action of these steroid glycosides on weight management is still unknown but it is associated with the bitter taste of the product that also stimulates the bitter receptors in the small intestines, and thus reducing the appetite. 1

 

The Origins

The plant Hoodia gondii had been known widely in South Africa, primarily from The Sans or the “Bushmen”, as an appetite suppressant and had been used by natives who travel and hunt in the wild for a long time. A small piece of the peeled stem was enough to exhibit its appetite suppressive effects. It is also currently being studied as a cure for tuberculosis and its flowers are said to have anti-cancer properties. It belongs to a family of species with known treatment for hypertension, abdominal cramps, diabetes, and intension. It is also currently being studied as a cure for tuberculosis and its flowers are said to have anti-cancer properties. It belongs to a family of species with known treatment for hypertension, abdominal cramps, diabetes, and intension.2

 

Scientific Background

In a scientific study, H.g. 12, a major steroid glycoside found in Mega Hoodia, can stimulate release of cholecystokinin (CCK), one of the neurotransmitters that have a major effect on appetite suppression. It specifically acts on human bitter receptors TAS2R7 and TAS2R14 found in the small intestine. When these receptors are activated, the action will travel through the vagus nerve found mostly in the gastrointestinal tract, cross the blood-brain barrier, and excite the nerve cells in the brain, specifically in the nucleus tractus solitarius, altering the sense of taste and further delaying gastric emptying or the feeling of “fullness” in the stomach.1 Due to poor bioavailability of these steroid glycosides, synthesis of the plant components are currently being done to promote more research studies on the safety and efficacy of the supplement.3

The subject on how these glycosides will survive in the gastrointestinal tract is also being studied and confirmed. One study suggests that its transport in the small intestines is assisted by P-gp and MRP transporters.  It was also found to be stable inside the human body and on drug-metabolizing enzymes and specifically weakly inhibits CYP3A4.4

A recent 15-day clinical study using the extract noted no serious adverse events but there were some episodes of nausea, vomiting and alteration in skin sensation.5 Several animal studies had been done and had shown promising results. Noted results include a decrease in fat pad weight in chickens by 18%.6

For Future Studies

            Mega Hoodia still needs further clinical trials and studies to support its effect on weight management.  The perception of fat in the body as a neuroendocrine organ and its close relationship with the gastrointestinal tract guarantees the promising result of this herbal supplement.7

 

References

1 Le Nevé B, Foltz M, Daniel H, Gouka R. The steroid glycoside H.g.-12 from Hoodia gordonii activates the human bitter receptor TAS2R14 and induces CCK release from HuTu-80 cells. Am J Physiol Gastrointest Liver Physiol. 2010 Dec;299(6):G1368-75. Epub 2010 Oct 7.

2 Vermaak I, Hamman JH, Viljoen AM.  Hoodia gordonii: an up-to-date review of a commercially important anti-obesity plant. Planta Med. 2011 Jul;77(11):1149-60. Epub 2011 Jan 21. Review.

3 Geoffroy P, Ressault B, Marchioni E, Miesch M. Synthesis of Hoodigogenin A, aglycone of natural appetite suppressant glycosteroids extracted from Hoodia gordonii. Steroids. 2011 Jun;76(7):702-8. Epub 2011 Apr 5.

4 Madgula VL, Avula B, Pawar RS, Shukla YJ, Khan IA, Walker LA, Khan SI. In vitro metabolic stability and intestinal transport of P57AS3 (P57) from Hoodia gordonii and its interaction with drug metabolizing enzymes. Planta Med. 2008 Aug;74(10):1269-75. Epub 2008 Jul 8.

5 Blom WA, Abrahamse SL, Bradford R, Duchateau GS, Theis W, Orsi A, Ward CL, Mela DJ. Effects of 15-d repeated consumption of Hoodia gordonii purified extract on safety, ad libitum energy intake, and body weight in healthy, overweight women: a randomized controlled trial. Am J Clin Nutr. 2011 Nov;94(5):1171-81. Epub 2011 Oct 12.

6 Mohlapo TD, Ng’ambi JW, Norris D, Malatje MM. Effect of Hoodia gordonii meal supplementation at finisher stage on productivity and carcass characteristics of Ross 308 broiler chickens. Trop Anim Health Prod. 2009 Oct;41(7):1591-6. Epub 2009 Apr 26.

7 Pereira CA, Pereira LLS, Correa AD. Hoodia gordonii in the treatment of obesity: A review. J of Med Plants Res. 2010 Nov; 4(22): 2305-2312.