Orlistat powder (96829-58-2) video

Orlistat powder (96829-58-2) Base Information

Orlistat Powder: An Anti-Obesity Medication

The obesity pandemic is upon us with approximately 39 percent of the world’s adult population suffering from obesity. Moreover, about one in five teenagers and children also suffer from obesity. This increases their risk of obesity-associated health problems.

After understanding the mechanism of obesity, and how hormones in the body may be able to help combat this problem, Orlistat was discovered and manufactured to be sold with a prescription under the trade names Xenical by Roche, and without prescription as Alli by GlaxoSmithKline.

What is Orlistat?

Orlistat is an anti-obesity drug that is widely sold to help treat not only obesity but also manage and treat obesity-associated health problems. It falls in the category of lipase inhibitors in the body and is considered to be a saturated derivative of a potent inhibitor of lipase enzymes synthesized and secreted by the pancreas, namely, lipstatin. This enzyme is isolated from the bacteria, Streptomyces toxytricini and is then further treated to saturate it and form Orlistat powder.

Orlistat is preferred over Lipstatin as an anti-obesity drug because of the enhanced pharmacokinetics and pharmacodynamics of the former over the latter. Furthermore, Orlistat is far more stable and simpler to produce and package, than Lipstatin. Orlistat has a half-life of 1 hour to 2 hours and is metabolized in the gastrointestinal or GI tract. After its metabolism, the powder is excreted in the feces.

Orlistat powder is a white powder that does not dissolve in water and has nearly negligible bioavailability. Its use is recommended in adults only and as its main function is weight loss through reduced caloric intake, it is highly recommended to take the medication with a doctor-recommended caloric restriction diet.

What are the Uses of Orlistat?

Orlistat’s use is recommended medically for the purpose of treating and managing obesity. It is also prescribed to help patients treat weight-related problems and to reduce the incidence of health problems that arise as a result of obesity. It is also recommended for use in patients with significant prior weight loss to reduce the risk of regaining the weight.

The indication for the use of Orlistat powder is usually a BMI value over the levels of 30 in an obese patient, or over the levels of 27 if other obesity-related comorbidities are present. As it is not known if the drug is safe to use in children under the age of 12 years, its use in those populations is not recommended, even with severe obesity.

Mechanism of Action of Orlistat Powder

Orlistat powder mainly functions through inhibiting lipid absorption in the intestines, to allow the caloric restriction to be more effective. Orlistat works in the stomach and small intestines, to inhibit the absorption of triglycerides by inhibiting the action of both gastric and pancreatic lipases. As the triglycerides are hence not broken down and hydrolyzed and because they cannot be utilized by the body in their original form, they are directly excreted. This reduced the triglyceride content along with the content of their metabolites, free fatty acids, in the body, making caloric restriction more effective.

Moreover, orlistat powder only shows its effects on triglycerides taken from the diet in the intestines, as it is not absorbed systemically. This is also the reason for the relatively negligible bioavailability of the compound because it only is effective in the gastrointestinal tract.

Recent studies have found other mechanisms of action of Orlistat powder, mainly an inhibitory effect of the compound on the thioesterase compound of the fatty acid synthase. However, this effect is not as effective in managing obesity because this enzyme is only effective in cancer cells, helping them proliferate at a higher speed. This mechanism of orlistat powder points towards the compound’s anti-tumor properties; however, further research is required before it can be added to the treatment regimens for different cancers.

Orlistat also produces benefits in a dose-dependent manner, with the net effect of fat excreted in the feces being 30 percent. At thirty percent, the net effect plateaus despite an increase in the dose of the chemical compound. Moreover, once consumed, it has a binding capacity of 99 percent meaning that it binds to lipoproteins and albumin in the blood with minimal partitioning into erythrocytes.

Benefits of Orlistat Powder

The main benefit of Orlistat Powder is weight loss, which has been backed by several scientific studies and researches. However, the benefits are surrounded by controversy despite the scientific evidence and the Food and Drug Association or FDA’s approval of Orlistat as a treatment option for obesity.

A randomized clinical trial was performed with the purpose of comparing the effects of orlistat and low-fat diet with the effects of the ketogenic diet, a popular weight loss diet in overweight and obese patients. This study aimed to prove that the benefits of this popular diet are the same as orlistat therapy, to further support its use in medical settings. It was found that both groups had similar results in weight loss, with minimal effects on glucose levels and blood pressure of the patients. The levels of total cholesterol, triglycerides, high-density lipoproteins, and low-density lipoproteins improved significantly in both groups. These findings hence prove the efficiency of orlistat as the ketogenic diet is widely used and believed to cause significant weight loss.

Apart from the anti-obesity properties of the orlistat powder, it also has anti-tumor effects that were initially not believed due to a lack of scientific evidence backing the claim. However, a study performed on animal models showed that this compound may be effective in treating and managing different cancers. The study was performed on mice with activated AKT and c-Met proto-oncogenes to study the antitumor effects in detail. The results of the study showed that these mice did not develop hepatic cancer, despite having activated proto-oncogenes as a result of Orlistat administration. Orlistat is believed to have increased the PTEN expression and inhibited the expression of AKT/SREBP1/FASN signaling pathways. This suppression further leads to inhibition of lipogenesis and proliferation of the two activated proto-oncogenes in the animal models, hence, not only having anti-tumor effects but also having anti-steatotic effects on the liver.

Furthermore, it is important to notice that the anti-obesity effects of Orlistat powder are not limited to weight loss but also to other disorders and comorbidities that arise as a result of obesity. Infertility is one of the most severe side effects of obesity that is believed to be managed via weight loss. Taking orlistat powder is not only hypothesized to improve the weight loss journey of the patients but also helps manage and treat infertility.

According to a recent study performed on male animal models, it was found that orlistat therapy may be beneficial in reversing infertility through its action on the decline of intratesticular lactate transport. The study also focused on the impairment of testicular glucose transport and erectile dysfunction, as a result of obesity in mice on a high-fat diet. By the 12th week of the study, the effects of the therapy were analyzed through the evaluation of mating and glucose parameters. It was found that the levels of testicular mRNA levels of glucose transporters (Glut1 and Glut3), monocarboxylate transporters (Mct2 and Mct4), and lactate dehydrogenase type C (Ldhc) increased significantly in these mice.

Moreover, the levels of intratesticular lactate and glucose levels and activity of LDH showed a marked decrease, hence proving the efficiency of orlistat in improving erectile dysfunction disorders and reversing infertility in animal models. In the same study, it was found that orlistat also has a negative effect on the oxidative stress levels in the penis, which may be increased as a result of a high-fat diet and result in erection and fertility disorders.

Another study was performed on male animal models to study the effect of obesity on spermatogenesis and how orlistat may be effective in improving the sperm levels in the male models. According to the results of this study, obesity increases the levels of leptin and sperm nDNA fragmentation in the body, while decreasing the levels of adiponectin, follicle-stimulating hormone, luteinizing hormone, testosterone, and sperm count along with their morphology and viability. However, researchers found that orlistat opposed the effects of obesity and severely decreased fragmentation of DNA in the sperm along with a marked decrease in leptin levels. It also increased the levels of the hormones and enzymes that were negatively affected by obesity. This resulted in increased spermatogenesis as a result of an increase in spermatogenesis-stimulating reproductive hormones.

Dosage of Orlistat Powder

Orlistat Powder has been approved by the FDA for use in the obese and overweight population, at a dose of 120mg, three times a day, to be taken prior to meals. It is important to note that although orlistat powder has a dose-dependent mechanism of action, doses higher than 120mg do not produce more potent results. 120mg of the compound, when taken every day, results in the prevention of 30 percent of the fat consumed.

Side Effects of Orlistat Powder

Orlistat Powder is a therapeutic agent, and as such has several side effects and complications associated with it. However, these side effects are mostly gastrointestinal in origin, given that that is where the compound works and begins in the early phases of therapy. These side effects often resolve themselves as time passes, but there are some severe side effects that require immediate medical intervention.

Moreover, one of the most common adverse effects of Orlistat powder is vitamin deficiency as it prevents the absorption of fat-soluble vitamins and minerals, along with the fats in the stomach and intestine. To ensure that these side effects do not occur, the compound is usually used with vitamin and mineral supplements, the bioavailability and effectiveness of which is subject to change as a result of orlistat use.

Other adverse effects of orlistat on the liver, such as cholelithiasis, cholestatic hepatitis, and subacute liver failure have been reported although the compound has been shown to produce benefits in the management of the non-alcoholic fatty liver disease.

The most common side effects of Orlistat Powder include:

oily or fatty stools,
oily spotting in your undergarments,
orange or brown colored oil in your stool,
gas or oily discharge,
loose stools,
urgent need to go to the bathroom,
inability to control bowel movements,
increased number of bowel movements,
stomach pain,
Nausea,
Rectal pain

More severe side effects of orlistat powder that require immediate medical intervention include:

severe stomach pain,
severe pain in your lower back,
blood in your urine,
painful or difficult urination,
little or no urination,
swelling in your feet or ankles,
feeling tired,
shortness of breath,
nausea,
upper stomach pain,
itching,
loss of appetite,
dark-colored urine,
clay-colored stools, and
yellowing of the skin or eyes (jaundice)

Apart from the side effects, Orlistat use is contraindicated in certain medical conditions, and it’s in those conditions could produce nearly fatal complications. These conditions include:

Chronic Malabsorption Syndrome
Pregnancy
Bulimia
Anorexia
Pancreatic Disease
Obstructed bile duct and cholestasis
Impaired liver function
Reduced gallbladder function

Our orlistat powder manufacturers follow the safety guidelines and production protocols to manufacture highly potent and safe orlistat powder that is then labeled with quality control trackers. This allows the manufacturers to recall a product or know the batch of a specific package if a problem arises after the delivery of transport of the products. Moreover, after the production process is completed, orlistat powder is subjected to further testing as the last quality control check to ensure the best products are being shipped out. After passing the test, the products are then either shipped for delivery or put into storage.

Where to Buy Orlistat Bulk Powder

Wisepowder offers orlistat powder in 40g package, and offers wholesale different quantity according to your need. Wisepowder’s Orlistat Powder has been lab-tested and verified for both product purity and identity.