Orlistat powder

AASraw is with synthesis and production ability from gram to mass order of Orlistat powder (96829-58-2), under CGMP regulation and trackable quality control system.

Orlistat powder is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. Orlistat is a drug designed to treat obesity. However, due to its relative simplicity an stability, orlistat was chosen over lipstatin for development as an anti-obesity drug.

Product Description

 

Orlistat powder video

 

 


 

I.Orlistat powder basic Characters:

Name: Orlistat powder
CAS: 96829-58-2
Molecular Formula: C29H53NO5
Molecular Weight: 495.7
Melt Point: 50 °C
Storage Temp: 2-8°C
Color: White powder

 


 

Product Name: Orlistat

IUPAC Name: [(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-4-methylpentanoate

 

Orlistat Introduction

More than half the world population has ever tried the weight management program, such as dieting, exercising, surgery, or medication. All of these weight loss remedies are effective only if you’re faithful to them and follow the instructions to the latter. However, opting for surgery or medication may turn out to be detrimental when you don’t take maximum precautions.

Chemical structure of Orlistat (3-D conformation)

Chemical structure of Orlistat (2-D conformation)

 

Chemical properties of the Orlistat

Property Name Property Value
Covalently-Bonded Unit Count 1
Isotope Atom Count 0
Undefined Bond Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Atom Stereocenter Count 4
Heavy Atom Count 35
Formal Charge 0
Compound Is Canonicalized True
XLogP3-AA 10
Exact Mass 495.392 g/mol
Monoisotopic Mass 495.392 g/mol
Topological Polar Surface Area 81.7 A^2
Complexity 579
Rotatable Bond Count 23
Hydrogen Bond Acceptor Count 5
Hydrogen Bond Donor Count 1
Molecular Weight 495.745 g/mol

 

A simple description of Orlistat powder

One of the weight loss medications that you’ll come across in your quest to find the most effective weight management drugs is Orlistat. In this Orlistat review, you’ll find crucial information, including what it is, how it works, and how it should be used, so you can decide if it’s the right pick for you.

 

What’s Orlistat?

Orlistat, which is sold as a prescription medication under the trade name Xenical, is a prescription weight loss drug that’s formulated to treat adverse weight issues such as obesity, as well as other weight-related conditions. It’s made available by GlaxoSmithKline as an over-the-counter drug called Alli in both the United States and the United Kingdom.

Orlistat’s generic formulations are available in several countries. Since 2000, it has been classified as an S3 over-the-counter medication in Australia. The approval of Orlistat as an over-the-counter drug was a controversial subject in the United States. It was repeatedly opposed on efficacy and safety grounds by a consumer advocacy group known as Public Citizen.

Orlistat’s acts as a lipase inhibitor, which generally means that it prevents the absorption of fats from food, thus reduce the amount of calories you take. Just like many other weight loss medications, Orlistat is meant for use in combination with other lifestyle modifications such as exercise and diet. Clinical studies show that people who stick by this combination stand a chance of losing two to three kilograms more than those that do not include the drug into their weight loss regiment.

One of the desirable aspects about Orlistat is that it not only helps you lose weight but it also reasonably reduces blood pressure. Additionally, this weight management drug is believed to prevent the onset of type 2 diabetes in people who are obese in the same way that lifestyle changes do.

While there are several Orlistat benefits to be happy about, there are also some Orlistat side effects to pay attention to. The most frequently reported side effect of this weight loss pill is steatorrhea. This is a gastrointestinal disease that is characterized by oily, loose stools. The symptoms, luckily, decrease with time.

 

Orlistat Mechanism of action

Orlistat is a powerful Intestinal Lipase Inhibitor. This drug is a reversible active-site inhibitor for gastrointestinal lipases. The drug forms a covalent bond with the active serine site in pancreatic and gastric lipases, thus inhibiting their action and preventing fat from the diet from being hydrolyzed and absorbed. (NCI04).

In simpler terms, Orlistat facilitates weight loss by slowing down pancreatic and gastric lipases, which are the essential enzymes in the intestines that break down triglycerides. When these lipases are blocked, the hydrolyzation of triglycerides from your diet into absorbable fatty acids is prevented.

The diet pills are taken orally and once taken; local lipase inhibition takes place within the GI tract. Only tiny amounts of the drug are absorbed into the body, with most of the drug being eliminated through feces.

Recent studies have found Orlistat to be potent in inhibiting an enzyme that is involved in the propagation of dangerous cancer cells. Nonetheless, potential side effects of the drug (such as inhibition of other untargeted cells or poor bioavailability) impede its use as a useful antitumor agent. In one study, researchers took on a chemical proteomics approach to find new cellular targets of the drug, including its off-targets.

At the normal prescription dose of 120 mg 3 times per day before meals, orlistat weight loss pill prevents around 30 percent of nutritional fat from being absorbed into the body. Taking more doses do not give more potent effects.

 

Use ofOrlistatpowder

Orlistat is used as a weight management drug. It’s an ideal choice for people who are overweight or obese. This weight loss pill is recommended for use by people with weight-related medical problems. It promises to help people not just lose weight, but it also helps to prevent them from gaining back the weight they have lost. By so doing, it helps to reduce the risk of high blood pressure, diabetes, heart disease, and other many health risks that are linked to obesity.

The amount of weight loss after taking Orlistat varies from one person to another. Researchers who run clinical trials spanning one year found out that between 35.5 percent and 54.8 percent of subjects managed to achieve a 5 percent greater decrease in body mass, even though not all of the lost mass was necessarily fat. About 16.4%-24.8 of the subjects managed to achieve at least a 10 percent decrease in body fat. When the subjects stopped taking Orlistat, a considerable number of them regained up to 35 percent of the weight they had managed to lose.

 

Dosage of Orlistat

Orlistat comes in the form of turquoise, hard-gelatin capsules that contain pellets of powder and weighs 120-mg. The recommended daily dosage is three capsules a day. You shouldn’t take all three pills at a go, but instead take each tablet with the main meal that contains fat, i.e., one for breakfast, one for lunch, and one for supper. You can take each pill with a meal or up to one hour after a meal. In case a meal is often missed, or if your meal does not contain fat, the Orlistat dose can be omitted.  Doses above the recommended daily dosage have not been found to provide any additional benefit.

Orlistat is most effective when combined with other weight loss strategies such as sticking to a nutritionally balanced, minimized-calorie diet and regular exercises. You are advised to take the weight loss pill with a meal that contains about 30 percent calories from fat. The effects of the drug are seen as soon as 24-48 hours after taking a dose.

Orlistat has been found to be effective in minimizing the absorption of certain fat-soluble vitamins and beta-carotene. As such, people who take the pill are advised to take it together with a multi-vitamin that contains fat-soluble vitamins to ensure sufficient nutrition.  It’s recommended that the vitamin supplement be taken at least two hours before or after taking Orlistat.

As for those patients receiving cyclosporine therapy, they are advised to administer cyclosporine at least 3 hours after taking Orlistat. For those receiving levothyroxine therapy, they are encouraged to administer levothyroxine therapy at least 4 hours after taking Orlistat. Those who take both Orlistat and levothyroxine should be observed carefully for changes in thyroid function.

 

OrlistatPrecautions

Previously, orlistat was strictly taken under the prescription of a doctor or pharmacist. However, in 2007, the U.S Food and Drug Administration approved it for over-the-counter market, hence, making it available for everyone.

 

Check out for any allergic reactions

Before taking this drug, it is advisable to talk to your doctor about any hypersensitivity reactions you may encounter. Orlistat contains inactive ingredients, which may not be favorable to you, leading to severe allergic reactions and side effects. Some of them include cellulose, microcrystalline, gelatin, silica, and sodium starch glycolate.

 

Consider your medical history

You need to share with your pharmacist or doctor concerning any medical conditions you might be having. This is because orlistat is contraindicated in specific abnormalities and problems, especially those associated with digestion.

If you suffer from any of the conditions below, it is advisable to seek further insights from a professional.

Malabsorption syndrome

This is an abnormality responsible for insufficient absorption of food nutrients along the GIT system. You should note that orlistat in itself works by inhibiting the digestion of fats. Therefore, this will end up being more tragic to anyone who takes the drug, yet they suffer from malabsorption syndrome.

Liver disorder or cholestasis

This is a condition in which there’s inhibition of bile flow to the liver. There are several reports which link orlistat to acute liver injury, though it occurs in rare cases or under high dosage.

Gallbladder disease

This includes cholecystectomy and associated syndromes.

Other health conditions you should state to your pharmacist include HIV infections, thyroid disease, kidney stones, seizures, or pancreatitis. In seizures or convulsions, orlistat may end up unbalancing the antiepileptic treatment by interfering with the absorption.

 

Eating disorders

Some of these disorders are bulimia and anorexia. Also, there’s no need to take orlistat if you are not overweight.

 

Other medications

It’s wise to inform your physician if you’re on any other medicines especially those that are likely to suppress the immune system. Drug-drug interactions will interfere with the pharmacokinetics, leading to an increased or decreased effect on either of them. For instance, orlistat will always interfere with the mechanism of drugs prescribed for an organ transplant.

If you are on cyclosporine, your doctor will probably tell you to avoid orlistat. However, you can still administer it only with strict instructions. To be on the safe side, you should take it at least two hours before this weight-management drug or two hours later.

Additionally, you ought to mention all the prescription and non-prescription drugs, diet supplements, vitamins, anticoagulants, or herbal products you might be taking.

 

Pregnant and breastfeeding women

This weight management medication is not for expectant mothers, anyone planning to conceive, or breastfeeding mums. The drug is unlikely to have any weight loss impact and will end up harming the fetus.

Although it is not yet clear whether orlistat passes to the mother’s breast, you’d rather avoid it and feel safe, than sorry.

 

Diabetics

Orlistat is what any person with diabetes would need to improve and control the blood sugar and improve glucose tolerance. Nonetheless, you will have to monitor the sugar levels regularly and make frequent visits to the doctor. Doing so helps you to know when to adjust the diabetes medication, the right diet, and the exercise program to take.

 

Orlistat Side Effects

Just like most treatments, orlistat has its side effects. The primary side effect is always observed in bowel habits. However, this may only be noticeable during the first few weeks of taking the weight loss drug.

To some people, the symptoms may subside while to others; it may continue throughout taking orlistat. At this point, it is wise to inform your doctor. The more compliant you are to a low-fat diet, the more likely it is for the side effects to reduce.

Here are some common side effects;

Steatorrhea

Though harmless, steatorrhea is the presence of oil and excess fats in the stool. Since orlistat inhibits lipases, there will be no absorptions of free fatty acids. As a result, the feces will appear oily and bulky.

To control this effect, one should avoid foods rich in calories and high-fat levels. According to FDA standards, the amount should be within 0.53 ounces and not exceed 30%.

Flatulence

In most cases, the gas passes out with some oil discharge. You will have to examine your clothing or underwear for traces of oily spotting.

  • Fecal incontinence

Loose, urgent, and frequent bowel movements

  • Discomfort and abdominal pain
  • Abnormal menstrual cycle
  • Low blood sugar levels

This is common among individuals who have diabetes type II.

  • Severe liver injury

Such cases are rare but would occur when you have some underlying liver problems, or you take a high dosage. In 2010, FDA included a safety warning on the orlistat labels, which indicate a risk of possible liver injuries.

However, this side effect is still a debate considering that another case study published on the British Medical Journal indicated otherwise.

Some of the warning signs of liver disease include vomiting, abdominal pain, yellowing skin, and dark urine.

 

Allergic reactions

It is very rare to experience any hypersensitivity or allergic reactions when taking orlistat weight loss pill. To some people, the inactive ingredients found in the drug may trigger nausea, itching, rash, body swelling, difficulty breathing, or dizziness.

Other less common side effects include anxiety, headache, bloating, rectal discomfort, tiredness, low appetite, and gallstones. If you experience acute symptoms, you should inform your doctor immediately or report to the FDA Reporting Program.

Final Verdict on Orlistat powder

Although orlistat has a few side effects, it is an excellent weight loss treatment that will deliver results within two weeks. The secret of benefiting from this drug is following the instructions, understanding the precautions, and checking on your diet.

As you take orlistat, it is important to follow the right nutrition program, consume less fat, low calories, and exercise regularly. A proper diet should include more fruits, vegetables, and grains. Additionally, you should supplement your diet with essential multivitamin products since orlistat blocks the absorption of fat-soluble vitamins.

When you’re in doubt, you can contact your pharmacist or doctor for further instructions. Alternatively, you can contact the U.S Food and Drug Administration for any inquiries or reporting life-threatening side effects, which have not been listed.

 

Bibliography

  1. Zhi J, Melia AT, Eggers H, Joly R, Patel IH (1995). “Review of limited systemic absorption of orlistat, a lipase inhibitor, in healthy human volunteers”. J Clin Pharmacol35(11): 1103–8
  2. Garcia SB, Barros LT, Turatti A, et al. The anti-obesity agent Orlistat is associated to increase in colonic preneoplastic markers in rats treated with a chemical carcinogen. Cancer Lett. 2006;240:221–4.
  3. FDA Approves alli (orlistat 60 mg capsules) Over-The-Counter” (PDF) (Press release). PRNewswire. 7 February 2007
  4. Mittendorfer B, Ostlund RE, Jr, Patterson BW, et al. Orlistat inhibits dietary cholesterol absorption. Obes Res. 2001;9:599–604
  5. Peng-Yu, Yang; Kai, Liu; Mun Hong, Ngai; J.Lear, Martin; R.Wenk, Markus; S.Qin, Yao (2010). “Activity-based proteome profiling of potential cellular targets of Orlistat−an FDA-approved drug with anti-tumor activities”. Journal of the American Chemical Society132(2): 656–66.

 


 

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