Of all the available strategies to induce long-term weight loss and combat obesity, dieting may be the least effective. Even worse, regular dieting has been shown to be a strong predictor of future weight gain and increased risk of chronic disease.1
In the most rigorous and comprehensive analysis of dieting outcomes to date, a groundbreaking UCLA study revealed that a majority of dieters not only regain lost weight after dieting—they put on even more weight.1 The researchers also found evidence to suggest that repeatedly losing and gaining weight (so-called “yo-yo” dieting) is linked to increased risk of cardiovascular disease, stroke, diabetes, and altered immune function.2
Fortunately, there are safe, effective interventions to help reduce fat uptake while gradually lowering your overall calorie burden.
One of these is a drug that blocks the absorption of ingested fats by inhibiting lipase, the enzyme that breaks down dietary fat in the intestine. The lipase inhibitor orlistat (brand name Xenical® and alli®) has been clinically proven to block fat absorption in the digestive tract.3-5 Life Extension® has advocated a 60- to 90-day course of orlistat to limit one’s exposure to fat calories while gradually making the necessary dietary changes and other modifications to facilitate optimal weight loss. Green tea extracts also help block lipase activity, though not as potently as orlistat.
Another strategy that may be used with orlistant/green tea or by itself is to consume a special fiber called propolmannan before heavy meals. Propolmannan binds bile acids in the small intestine that would otherwise help facilitate dietary fat absorption into the bloodstream. When taken before meals, propolmannan forms a viscous sponge that can help further reduce the impact of excess calories.
When taking drugs or nutrients that impede fat absorption, it is important to ensure that you continue to absorb vital fat-soluble nutrients such as vitamin D, vitamin K, vitamin E and the omega-3s. Since fat normally shuttles these nutrients into the bloodstream, you should make sure to take these nutrients at the time of day that ensures maximum absorption.
Here we detail how orlistat works to diminish your exposure to killer fat calories. You will also learn how it decreases your body’s absorption of the fat-soluble vitamins D, E, and K. We will then show how to maintain optimal intake of these key nutrients while obtaining the benefit of lipase inhibitors.
How Orlistat Works
To absorb fats, your body needs to break them down in the intestinal tract. It does so partially by the action of an enzyme produced in the pancreas that converts triglycerides in ingested dietary fats to monoglycerides and free fatty acids. The name of this enzyme that breaks down fat is lipase.
Once acted on by lipase, ingested fat molecules are transported via the bloodstream to the membranes of adipose or muscle cells, bringing calories and health risks with them. As a lipase inhibitor, orlistat reduces fat absorption by as much as 30%.5
This has two important effects. Of course, the unabsorbed fat eventually passes out of the body. Just as importantly, if you don’t cut back on the amount of fat you eat, the lack of absorption will produce some very unpleasant side effects, such as bloating, diarrhea, and even fecal soiling. The result, to quote the manufacturer, is that orlistat “helps your head learn healthy habits that stick… to teach your body a new, healthier way of eating.”6 In other words, you become conditioned to eat less fat so you’ll stay comfortable. The ultimate objective is to provide an incentive to ingest fewer fat calories.
Orlistat is effective. A two-year European study found a mean decrease in body weight of 10.2% in the orlistat group compared to 6.1% in the placebo group at 1 year.5 And 9.3% of the orlistat group lost more than 20% of their initial weight, versus 2.1% of the placebo group. But there’s a downside.
All that fat the body didn’t absorb? It carried with it essential vitamins that can only dissolve in fat—the fat-soluble vitamins A, D, E, and K. Clinical trials show that orlistat may induce malabsorption of fat-soluble vitamins to varying degrees, often resulting in the need to supplement patients to maintain normal blood levels.7-11 In fact, orlistat can reduce absorption of vitamin E by as much as 60%.11 This has led to expert recommendations that people taking orlistat should supplement with fat-soluble vitamins.8,12 That’s true even if they are already taking a daily multivitamin.13
Vitamin D was long associated only with calcium absorption and bone health, and indeed it is vital in those areas. In fact, existing recommended daily amounts of vitamin D were developed originally to help sustain adequate levels of calcium in blood and bone. In recent years, however, we’ve learned that vitamin D has essential effects throughout the body.14,15 In fact, vitamin D receptors are found in most body tissues, indicating the fundamental importance of this vitamin.16
For instance, vitamin D has profound neurocognitive effects. Insufficient vitamin D levels are associated with low mood and poorer cognitive performance in adults.17,18 Older adults in particular are at risk for cognitive impairment when they lack sufficient vitamin D.19 And low vitamin D levels are associated with frailty among older adults as well.20 On the other hand, there’s supportive evidence that adequate vitamin D levels may help prevent Alzheimer’s disease and other devastating forms of cognitive decline.21
A recent discovery is that vitamin D has profound impact on the immune system.22 Vitamin D insufficiency is associated with increased vulnerability to influenza, and many studies show that supplementing with vitamin D helps prevent the flu.23,24 Experts now strongly recommend testing and treating for vitamin D deficiency as part of a swine flu prevention strategy.25
Astonishingly, because of antiquated reference values for how much vitamin D we should take, a tremendous number of American adults are already vitamin D deficient or insufficient when blood levels are checked. Obese people—the very people who take orlistat—are even more likely to be deficient in vitamin D.26 Daily multivitamins don’t provide nearly enough vitamin D to sustain healthy levels. Experts recommend 2,000-7,000 IU vitamin D per day to maintain year-round adequate levels between 40-70 ng per mL.27
Vitamin E is the primary fat-soluble antioxidant in mammals, making it essential in preventing oxidative damage to lipid-rich cell membranes.28 As a result, vitamin E can prevent or mitigate oxidant-related diseases such as atherosclerosis, strokes, and many cancers.29,30 But vitamin E is now known to have many other health-giving properties as well, including intra- and inter-cellular signaling and regulation of gene expression.31-33 In fact, people with lifelong generous dietary vitamin E intakes enjoy substantial reductions in their risk of chronic disease.34 Tragically, more than 90% of Americans do not consume the recommended dietary amounts of 15 mg/day (22.5 IU/day).34 Decreased absorption resulting from orlistat use will only exacerbate the risk.35 And the effects are immediate and profound.
Lung, kidney, and colon tissue are all vulnerable to vitamin E depletion, predisposing to diseases in those organs.36-39 Low plasma concentrations of the gamma-tocopherol form of vitamin E are associated with increased rates of cardiovascular disease.40,41
Advancing age itself causes an increase in protein oxidation in memory-related brain regions—one of many reasons our memories begin to weaken with time.42 Vitamin E can prevent such changes in laboratory studies of older animals.42,43 In fact, people with high plasma levels of vitamin E were found in 2010 to have reduced incidence of Alzheimer’s disease.44
Finally, vitamin E, particularly in the form of gamma-tocopherol, is a powerful inducer of apoptosis (programmed cell death) in cancer cells.45 Gamma-tocopherol-rich supplements inhibit colon, prostate, mammary, and lung tumorigenesis in animal models, making them attractive as chemoprevention agents.46
Which Vitamin E Are You Taking?
“Vitamin E” is a catch-all term for a group of 8 related molecules called tocopherols and tocotrienols.47 Alpha-tocopherol is the form that has received most of the attention, but recent data suggest that gamma-tocopherol may have greater health benefits.40,48 Gamma-tocopherol has potent anti-inflammatory and antioxidant properties, and in fact is more effective at scavenging free radicals and nitrogen species than the more common alpha form.49,50 Supplementation with alpha-tocopherol decreases tissue concentrations of gamma-tocopherol. Fortunately, supplementation with gamma-tocopherol increases concentrations of both alpha- and gamma-tocopherols.40 Regardless of the form, impaired fat absorption resulting from orlistat use depletes the body of vitamin E, making supplementation vital.