Orlistat – Product Information
|Molar Mass||495,735 g/mol-1|
|IUPAC Name||(2S)-2-[(1R)-1-hydroxy-2-[(2S)-5-oxooxolan-2-yl]ethyl]octanoic acid|
What is Orlistat?
It is the only OTC weight-loss medication currently on the market that has received FDA and EMA approval [R][R]. It has been demonstrated to be a reliable, selective inhibitor of the pancreatic and stomach lipases, which are responsible for breaking down dietary fat. Currently, type 2 diabetes and cardiovascular disease caused by obesity are also being treated clinically with Orlistat [R] [R].
Studies have also suggested that it may have additional clinical uses, such as the management of chylous ascites. Even though it has a very selective impact, some adverse effects have nonetheless been noted.
Purerawz sells Orlistat for research purposes only.
How Does Orlistat Work?
Tetrahydrolipstatin, also known as Orlistat, is marketed as a prescription medication under the brand names Xenical or Alli. This natural substance was obtained from Streptomyces toxytricini and is a saturated derivative of lipstatin. [R]
Tetrahydrolipstatin has an inhibitory impact on pancreatic and gastric lipases, just like lipstatin, an irreversible inhibitor of pancreatic lipase [R][R]. By hydrolyzing triacylglycerols (TGs) into free fatty acids and monoacylglycerols, which are ultimately absorbed by the body, these two enzymes play crucial roles in the absorption of fat [R]. Orlistat, however, has negligible to no activity against phospholipases, trypsin, chymotrypsin, and amylase.
Only the gastrointestinal tract is affected [R]. To stop TGs from being hydrolyzed into free fatty acids that can be absorbed by cells and the undigested TGs from being expelled in stool, it can bind covalently to the active serine site in the lipase enzyme of the digestive tract. [R].
As a result, orlistat’s inhibition of lipases will prevent the absorption of dietary lipids, resulting in a decrease in calorie intake.
Extensive research has been done on the potential of Orlistat as a weight loss aid. Below follows some of the relevant findings and other potential applications:
Orlistat’s Potential Effect on Weight Loss
Long-term studies have potentially verified the claims that Orlistat will cause significant weight loss. The value of 24-hour fecal fat excretion was used as a representative pharmacodynamic parameter to assess the impact of Orlistat. The use of a treatment dose of orlistat (120 mg, major meals) can impede a portion of fat absorption; corresponding to 30% of the consumption of fat, which is equivalent to roughly 200 additional calories when practicing a well-balanced, modestly low-calorie low-fat diet. [R] [R]
A double-blind study with 657 orlistat (120 mg ) -treated patients and 223 placebo-treated subjects who both followed a controlled-energy diet for a year, revealed that orlistat-treated subjects lost more weight than placebo-treated subjects (approximately 8.76 kg/year vs. about 5.81 kg/year). [R]
Another comparable one-year trial showed that the orlistat (120 mg) treated group (consisting of 1,561 people, 268 men, and 1,293 women) lost more weight than the placebo group (consisting of 1,119 people, 174 men, and 954 women) by roughly 9.2% (8.92 kg) and 5.8% (5.63 kg). [R]
A meta-analysis of over 10,000 individuals participating in clinical trials revealed a mean weight loss of 2.9 kg throughout 12 months of treatment. [R]
Another similar investigation revealed that treatment at the full dose of 120mg three times per day for 12–18 months, resulted in a weight reduction of 2.6-2.9%, after adjusting for the effect of the placebo. [R][R][R]
Since 2007, certain marketplaces have offered orlistat treatment at a modest dose of 60 mg three times per day without a prescription. A weight loss of 1.2 kg in comparison to placebo was seen in a 4-month study using low-dose orlistat[R].
Its ability to prevent weight gain has also been demonstrated in longer-term studies. Patients who received orlistat medication (120mg) gained less weight than with the placebo over the second year (about 3.2 kg vs. 5.63 kg), without following a controlled-energy diet. [R]
Additionally, results from a 4-year experiment with nearly 3,000 obese participants showed that the mean weight loss from lifestyle changes with orlistat medication was considerably higher after 4 years than with placebo (3.0 kg) [R].
Additionally, the FDA has approved it for the treatment of childhood and adolescent obesity in patients aged 12 to 16, while Orlistat’s efficacy in treating pediatric obesity is debatable. [R]
Orlistat and Diabetes
Obesity is a significant risk factor for type 2 diabetes. As a result, weight loss in people with type 2 diabetes is linked to improved glycemic control and lowered risk factors for cardiovascular disease.
According to a study conducted on 391 obese men and women with type 2 diabetes (aged > 18 and with a BMI of 28–40 kg/m2), the Orlistat group (120 mg) dropped 6.2–0.45% (mean SEM) of their starting weight after a year of medication, compared to 4.3–0.49% in the placebo group (P 0.001).
As evidenced by decreases in HbA1c (P 0.001), fasting plasma glucose (P 0.001), and dosage reductions of oral sulfonylurea medication (P 0.01), orlistat treatment plus diet was associated with a significant improvement in glycemic control, when compared to placebo plus diet, suggesting that it is an effective potential treatment in obese patients with type 2 diabetes, in respect to clinically meaningful weight loss and maintenance of weight loss. [R]
According to a lengthy trial, orlistat with lifestyle changes led to higher weight loss in a clinically relevant obese population over the course of four years, and a bigger decrease in the prevalence of type 2 diabetes when compared to lifestyle changes alone. [R]
Orlistat and Cardiovascular Disease
Along with potentially assisting with weight loss, it has also been shown to help lower blood pressure and lipid profiles, two risk factors for cardiovascular disease linked to obesity. Among the lipid parameters that significantly improved with orlistat therapy compared to placebo were apolipoprotein B (P 0.001), total cholesterol (P 0.001), LDL cholesterol (P 0.001), triglycerides (P 0.05), and the LDL-to-HDL cholesterol ratio (P 0.001). [R]
Orlistat and Binge Eating Disorder
Golay et al. discovered that patients receiving orlistat 120 mg for 24 weeks along with a mildly reduced-calorie diet lost considerably more weight than those receiving the placebo (-7.4% vs. -2.3%). At week 24, patients on it had significantly lower total Eating Disorder Inventory 2 scores than those taking a placebo. [R]
Orlistat and Cancer
Orlistat was discovered to be a promising anticancer compound because it can inhibit endothelial cell proliferation and angiogenesis, which slows tumor progression on a variety of cancer cells, including prostate, breast, ovary, and melanoma cancer cells, and it can block the FAS activity, which causes endoplasmic reticulum stress in tumor cells. [R]
Even though research indicates that Orlistat might be a potential anti-tumor drug, more related clinical research is needed.
Orlistat and Knee Osteoarthritis
In a study of 50 women with obesity (BMI > 30 kg/cm2) and knee osteoarthritis stage II-III Kellgren-Lawrence, aged 45 to 65, orlistat therapy (120 mg) was more effective in reducing weight by 9.05% (on average 9.5 kg), compared to patients who were only on a low-calorie diet, whose weight decreased by 2.54%. (average 2.66kg).
In a study of 50 women with obesity (BMI > 30 kg/cm2) and knee osteoarthritis stage II-III Kellgren-Lawrence, aged 45 to 65, orlistat therapy (orlistat 60 mg capsules in 120 mg) was more effective in reducing weight by 9.05% (on average 9.5 kg), compared to patients who were only on a low-calorie diet, where the weight decreased by 2.54%. (average 2.66kg). Additionally, WOMAC pain dropped by 48.7% for patients receiving this as medication, which was substantially less (P = 0.012) than the rate in the control group, which decreased by only 32.2%. These findings suggested that weight loss, particularly in obese people taking orlistat to lose weight, may result in a reduction in the clinical progression of knee osteoarthritis. [R]
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Orlistat is currently being researched as a potentially effective weight loss product and weight loss supplement pill for overweight adults or individuals. As a weight loss aid, it may have numerous other potential applications for research in the fields of diabetes, the digestive system, unabsorbed fat, cardiovascular health, and cancer. Although it is an FDA-approved over-the-counter weight loss aid, it still requires some research to evaluate its safety and efficacy. Always consult a health care professional before starting any weight loss program or consuming any weight loss pill. Purerawz sells Orlistat for research purposes only and it is not intended for human consumption.