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Info on fat lose drugs

workinhard

Registered User
Dec 18, 2003
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by Decadent -- .musclechemestry

Available Drugs for weight loss....some pro's and con's for
each:

Orlistat (Xenical )120 mg with each meal Peripheral: Blocks absorption of about 30% of consumed fat Gastrointestinal symptoms (oily spotting, flatus with discharge, fecal urgency, oily stools, incontinence)

Sibutramine (Meridia) 5-15 mg/d Central: Inhibits synaptic reuptake of norepinephrine and serotonin Dry mouth, constipation, headache, insomnia, increased blood pressure, tachycardia

Phentermine( Adipex, Fastin, Ionamin and others) 15-37.5 mg as a single or split dose Central: Stimulates release of norepinephrine CNS stimulation, tachycardia, dry mouth, insomnia, palpitations

Diethylpropion (Tenuate) 25 mg 3x/d or 75 mg/d Central: Stimulates release of norepinephrine CNS stimulation, tachycardia, dry mouth, insomnia, palpitations

Phenyl-propanolamine (PPA)* Various OTC preparations 75 mg/d Central: Stimulates release of norepinephrine CNS stimulation, tachycardia, dry mouth, insomnia, palpitations

Ephedrine+/-caffeine "Elsinore"pill Varies: usually 75-150 mg ephedrine and 100-150 mg caffeine Central: Stimulates adrenergic receptors CNS stimulation, tachycardia, dry mouth, insomnia, palpitations

Bupropion (Wellbutrin) 100-300 mg/d Central: Inhibits reuptake of dopamine norepinephrine and serotonin. CNS stimulation, dry mouth, headache, GI effects

*Because PPA is associated with a small risk of hemorrhagic stroke, in November, 2000, the FDA announced that it had asked manufacturers to discontinue marketing nasal decongestants and weight control products containing PPA. FDA also plans to remove PPA from all drug products.


Drugs used to treat obesity fall into 2 classes: (1) CNS-acting appetite suppressants and (2) lipase inhibitors that act on the stomach and the gastrointestinal system.
CNS-acting appetite suppressants. There are 2 types of CNS-acting appetite suppressants. Noradrenergic drugs act primarily to enhance the CNS concentrations of norepinephrine but also marginally increase the CNS levels of dopamine. Higher levels of norepinephrine lead to diminished appetite and hunger. Other CNS-acting drugs produce increased concentrations of serotonin along with norepinephrine and dopamine. Higher concentrations of serotonin result in an increased sense of satiety.


Phentermine. A noradrenergic anoretic, phentermine is the most commonly prescribed drug for the treatment of obesity. It has been on the market for more than 30 years. Its long-term availability, along with its lower price (generic forms are available) both contribute to its popularity. There are negligible differences between the resin (15 and 30 mg) and hydrochloride (18.75 and 37.5 mg) forms of this drug. Although it was used as part of the phen-fen combination, no studies have shown that phentermine, alone or in combination with fenfluramine, caused the valvulopathy now attributed to the fenfluramine preparations (the "fen" part of phen-fen).[19-21]

Phenylpropanolamine (PPA). Also a noradrenergic anorectic, PPA -- was historically a frequent addition to over-the-counter (OTC) preparations as a nasal decongestant and for weight loss. However, the FDA recently withdrew approval for these uses because of reports of a small increase in hemorrhagic strokes.[22] PPA will no longer be available for weight control, or for any other indication, either OTC or by prescription.

Sibutramine. Sibutramine selectively inhibits the reuptake of noradrenaline, serotonin, and, to a smaller degree, dopamine. Studies have shown that after 1 year of treatment, patients taking sibutramine lose an average of 7% of basal body weight.[23-26] Weight loss is dose-dependent, and studies have shown weight losses of up to 9% of body weight at higher doses. Although sibutramine increases blood pressure and heart rate in some patients,[27] this effect is relatively small in most patients and easily identified. Mild blood pressure changes should not cause patients to abandon this medication if it is otherwise effective because the benefits weight loss usually more than compensates for its cardiac effects. Its use, however, obligates careful medical monitoring. Early return visits for blood pressure checks are mandatory. Patients with otherwise well-controlled hypertension can usually use sibutramine successfully.

Intestinal lipase inhibitors.
Orlistat. Orlistat is the only commonly used drug to treat obesity that is does not act on the CNS. The drug works by blocking the action of pancreatic lipase -- the enzyme responsible for fat absorption -- thereby causing fat and calorie loss in stools.[28] Studies lasting 1 to 2 years show that patients taking orlistat experience a 4% to 5% greater weight loss than those taking a placebo.[29,30] Although weight loss with orlistat seems to peak at 6 months, it has been maintained for up to 2 years.

Because of the potential for associated uncomfortable gastrointestinal side effects, such as rectal incontinence and oily stools, orlistat also has the potential to result in beneficial aversive conditioning. Patients who use it must modify their food choices to avoid the side effects. Thus, the objectionable side effects associated with consuming excessive fat may reinforce more healthy eating habits. However, because orlistat can reduce the absorption of fat-soluble vitamins, multivitamin supplementation is recommended.
Patients will derive the most benefits from orlistat if they are instructed in how to use it effectively. With this drug, more than with any of the others, a knowledgeable patient will be more satisfied with both the side effects and results of taking orlistat. Passive patients will not do well; however, many patients using this drug value the opportunity to be an active participant in the management of their weight loss.

Other products. Bupropion, which is an FDA-approved antidepressant and agent for smoking cessation, has been shown in a number of small controlled studies to produce weight loss comparable to other obesity drugs.[31,32] It is believed to act centrally as a weak blocker of neuronal reuptake of norepinephrine, serotonin, and dopamine. It may be useful (albeit currently off-label) in the treatment of depressed patients who have gained weight with other psychotropic medications.

A number of other OTC products -- such as chitosan, hydroxycitrate; a variety of so-called fat blockers, gums and fibers; and chromium (usually as picolinate) -- are advertised as treatments for weight loss.
Be aware that they are packaged in uncertain dosages and are usually of uncertain potency and purity. More importantly, there are NO studies demonstrating any evidence of efficacy in the treatment of obesity.

Ephedrine is sold in various forms as an herbal product, most commonly as a variant of ephedra (or ma huang). Studies have demonstrated that patients using this thermogenic agent have experienced significantly more weight loss than those taking a placebo.[33-35] Uncontrolled botanical preparations vary substantially, however, in their potency, purity, and reliability. The most common side effects of the ephedrine/caffeine combination are increased heart rate and a sense of palpitations. Reports of associated complications (some of which have been catastrophic) may have been related to individual preparations with unusually high potency or to patient misuse partially attributable to the erroneous assumption that "natural" products must be safe.