All you should know about Fat killer--Orlistat

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1. What is orlistat?


Orlistat is a prescription medication indicated for treatment of obesity in combination with a supervised reduced calorie and low-fat diet. It is sold as a prescription drug under orlistat brand name Xenical and also as an over-the-counter anti-obesity drug under the trade name Alli.

Orlistat is a long-lasting oral gastrointestinal lipase inhibitor that primarily works to prevent the absorption of fats. Orlistat is the saturate form of lipstatin, which is an effective natural pancreatic lipase inhibitor. Orlistat is simple and stable hence chosen over its parent form lipstatin.

Orlistat works to offer modest weight loss over time as well as reduces visceral fats. It is however used along other weight loss techniques such a low-fat diet and exercise. Its benefits like with any other weight loss plan is not instant but a long-term plan, which is recommended by medical practitioners.

Since it works by blocking the absorption of dietary fats rendering them to be excreted unchanged in human feces, there is high incidence of gastrointestinal events that occur with its use. These side effects could turn into serious and adverse effects more so with increased dosage. To overcome or reduce the side effects orlistat should be taken along a low-fat diet as well as multivitamin supplements.




2. How Does Orlistat Work & What Does it Actually Do?


Orlistat is known as selective inhibitor pancreatic and gastric lipases. These enzymes (gastric and pancreatic lipases) are responsible for the breakdown of triglycerides (a fat/lipid in the body) in the intestines.

Orlistat mainly exhibits its effects in the lumen of the stomach as well as in the small intestine. Orlistat is known to bind to the active serine residue site of the gastric and pancreatic lipases to form a covalent bond. These enzymes are therefore deactivated and becomes unavailable to hydrolyze dietary fat in form of triglycerides into fatty acids and monogylcerides that can be easily absorbed by the body.

When their activity is inhibited, the triglycerides obtained from human diet are not transformed into fatty acids that the body can absorb. Therefore, the triglycerides are excreted unchanged in human feces. Since unchanged triglycerides are not absorbed in the body, this results into a caloric deficit which plays a role in weight control.

Recently, orlistat has also been found to be an inhibitor of thioesterase domain of fatty acid synthase (FAS). The enzyme, thioesterase, is linked to proliferation of cancerous cells but not in the growth of normal cells.


3. Does orlistat work if you don't eat fat?


Well, orlistat works to reduce the amount of fat absorbed in the body system. There is therefore no need to take orlistat when you are taking a meal without fat. In case you are on orlistat medication and you take a meal without fat, you are advised to skip a dose to avoid the associated side effects.

However, if you eat a meal that is very high in fats, you might experience the orlistat adverse effects such as fatty stool, intestinal gas and oily spotting.


4. Orlistat proven to reduce visceral fat?


Yes, indeed orlistat has been clinically proven to reduce visceral fat. Alli (orlistat 60 mg) is approved by Food and Drug Administration (FDA) as an over-the-counter drug to treat obesity.

Clinical studies have proved that orlistat not only contributes to weight loss but also significantly reduces visceral fats. It has been found to reduce the waist circumference.

Visceral fat also called active fat is a dangerous type of fat stored within the abdominal cavity hence surrounds most vital internal organs such as liver, intestines and pancreas. Higher amounts of visceral fat are linked to many health problems such as type 2 diabetes, heart disorders, certain cancers, hypertension, and Alzheimer s disease.

During weight loss, visceral fat is among the first fats to be lost. This greatly improves your health by reducing the risks of most health problems such as diabetes, hypertension, and heart disorders.

In a study involving 26 participants, orlistat 60 mg (Alli) was administered three times a day in combination with a reduced calorie, low-fat diet for 3 months. The results indicated that, orlistat was able to significantly reduce the waist circumference which is a measure of visceral fat. They reported 5.6 % reduction in body weight and 10.6% reduction in visceral fat.

In another study, 123 persons with obesity were given orlistat three times daily for 24 weeks. They were also advised to observe a low fat diet. After the sixth month, the participants reported a mean body weight reduction of 5.96% and a mean reduction in visceral fat of 15.66%.




5. Does orlistat cause liver damage?


Orlistat has not been identified as the direct cause of severe liver damage in both pre-clinical and clinical trials. However, some rare cases of severe orlistat liver injury have been reported by people who used orlistat.

Orlistat can limit the function of a vital enzyme called carboxylesterase-2. The enzyme, carboxyleserase-2 plays an important role in detoxifying the liver, kidneys and the whole gastrointestinal tract. When these enzyme is inhibited it may result to serious toxicity of the vital organs.

The Food and Drug Administration has therefore labelled severe liver injury as safety concern in regards to orlistat. This is based on about 13 cases of post-market orlistat liver damage after the use of orlistat.

In the studies conducted, orlistat has not been found to be the direct cause of severe liver damage. However, the potential risk of orlistat liver injury associated should not be ignored. It is good to always consult your medical practitioner for best advice before taking orlistat or any other drug.


6. Orlistat benefits


The main orlistat benefit is weight loss. In fact, orlistat weight loss is the primary and the known benefit it is produced and marketed for. It is used to treat obesity and aid in weight loss.

The orlistat benefits are:


Treating obesity


Obesity and overweight refers to an abnormal or excessive fat accumulating in the body. This excessive accumulation possess a great health risk. The measure of obesity is the body mass index usually calculated as your weight in kilograms divided by the square your height in meters.

Obesity is associated with health problems such as heart disorder, diabetes, certain cancers and high blood pressure. Luckily, even the modest weight loss can prevent the health issues associated with obesity.

Naturally, many overweight and obese persons lose weight through checking on diet, lifestyle accompanied by exercise. Drugs or weight loss medications are prescribed to accompany a healthy lifestyle as an additional option.

Weight loss, however, cannot be achieved overnight but usually a long-term plan. A weight loss plan will usually consist of a proper diet, exercise, and where necessary medication. A weight loss plan is usually considered successful when you lose 5 percent or more of your pre-treatment weight within one year. This mean that you need to lose about half a kilogram within the first week of treatment. This modest weight loss ensures that you maintain the weight or even lose more weight with continued weight loss plan.

Orlistat used with a reduced calorie and low-fat diet as well as exercise provides a potent weight loss plan. Orlistat, a gastrointestinal lipase inhibitor, can decrease the amount of dietary fat you absorb by 25 %. Orlistat works by inhibiting the gastric and pancreatic lipases. These are enzymes that breakdown dietary fat(triglycerides) into absorbable form, fatty acids or monocerides.  

When the activity of these enzymes is inhibited, the body is not able to absorb calories but rather the fats are excreted undigested in feces. This is an important aspect in weight control.

Several clinical studies have been conducted and prove that orlistat weight loss benefits are indeed potent.

In a study involving 3,305 participants who were overweight, orlistat was administered at 120 mg three times daily for 4 years. The participants were also advised to stick to a low calorie diet with not more than 30 % of calories. They were advised to exercise by taking walks each day.

This study found that, the average weight lost in the first year was about 10.6 kg. Even though the participants gained weight over the last three years of the trial, at the end, the average weight lost was about 5.8 kg.

In another one-year study orlistat administered was found to result in 5% or more weight loss.

Other orlistat benefits include;


Orlistat Reduce the risk of type 2 diabetes


Type 2 diabetes or diabetes mellitus is a serious condition that influence sugar (glucose) metabolism in the body. It occurs when our bodies are not sensitive to insulin. Insulin is the hormone responsible for regulating the flow of sugars(glucose) in the body. It could also occur if the pancreas does not produce sufficient amounts of insulin to maintain the proper glucose levels in the body.

Although the exact causes of insulin insensitivity are not well known, overweight is one of the contributing factors to the development of type 2 diabetes. Type 2 diabetes symptoms may be easy to ignore as they develop very slowly, however, if untreated may lead to more complications. Advanced type 2 diabetes can result to more problems such hypertension, cardiovascular diseases and heart attack. These signs and symptoms include frequent urination, increased thirst, unintentional weight loss, fatigue, poor vision, frequent infections, slow-healing wounds and darkening in some areas of the skin such as neck and armpits.

Orlistat is a potent weight loss drug hence plays a critical role in inhibiting the onset of type 2 diabetes. Some orlistat mode actions identified to play role in type 2 diabetes include enhancing insulin sensitivity, reducing postprandial plasma non-esterified fatty acids, slowing or preventing the digestion of dietary fats, reducing visceral fat, and inducing the secretion of glucagon-like peptide-1 in the lower small intestine.

In a study with obese persons, orlistat accompanied by a healthy lifestyle (low-fat diet and exercise) was found to greatly reduce the incidence of type 2 diabetes. It also resulted in a great weight loss.

Another study was conducted with obese or overweight persons suffering from type 2 diabetes. Orlistat 120 mg was administered three times every day for 6 or 12 months.

It was found that apart from the orlistat weight loss effect, orlistat was able to improve glycaemia control. The glycaemia parameters improved were a decrease in fasting plasma glucose (FPG) and haemoglobin A1c (HbA1c). The improved glycaemia control was independent of weight loss.


Orlistat  Can lower high blood pressure


High blood pressure also known as hypertension is a health condition that occurs when your blood pressure increases to very high levels and often to unhealthy levels. The blood pressure increase when he arteries becomes narrow.  

Prolonged exposure to high blood pressure can result to more chronic conditions that affect vital organs such as the heart, kidney any eyes. The most common symptoms of hypertension are headaches, noose bleeeding, vision changes, dizziness, chest pain, shortness of breath and even blood in the urine.

Orlistat which is a lipases inhibitor helps in preventing the absorption of dietary fat that usually could block the arteries. Orlistat can therefore slightly lower the blood pressure usually occurring due to overweight.

In a study involving 628 obese or overweight persons suffering from hypertension, orlistat was given at 120 mg three times a day for one year. These patients had either high uncontrolled diastolic pressure of isolated systolic pressure. In addition to orlistat prescription, the patients we advised to observe a low-fat diet for the period.

The study reported a significant weight loss as well as a decrease in both diastolic and isolated systolic hypertensions. They recorded a -9.4 mmHg reduction in systolic hypertension and a -7.7 mmHg reduction in the diastolic pressure.

This shows that orlistat can be used in the management of hypertension in obese or overweight individuals.

This slight reduction in high blood pressure is linked to the long-term use of orlistat accompanied with a low calorie diet and exercise.

In another study, the log-term use of orlistat was found to slightly reduce the blood pressure by mean reductions of 2.5 mmHg of systolic pressure and 1.9 mmHg of diastolic blood pressure.


Orlistat  Reduces total and LDL cholesterol


The low-density lipoprotein cholesterol (LDL cholesterol) is usually called the bad cholesterol since it accumulates in the walls of blood vessels thus increasing your risk of health problems such as heart disorder and stroke.

The total cholesterol consists of both low-density lipoprotein (LDL) and high-density lipoprotein (HDL) cholesterol. The high the level of total cholesterol the higher the risk of heart disorders.

Orlistat has been reported to reduce the LDL cholesterol in addition to its weight loss benefits.

In a study involving obese or overweight patients, orlistat was given at a dose of 120 mg three times daily for 24 weeks. The patients had a BMI (body mass index) of 27-40 kg/m2 and hypercholesterolemia (low-density-lipoprotein cholesterol, LDL-C, 4.1-6.7 mol/l).

Orlistat was found to significantly reduce weight as well as total and LDL cholesterol. It was further indicated that the LDL cholesterol lowering effect was independent of the weight loss benefits. In this study orlistat was well tolerated apart from the high incidence of gastrointestinal events.

In another study, 448 persons with very high levels of cholesterol were given orlistat at 120 mg thrice per day for about 6 months. The patients were also instructed to stick to a reduced calorie and low-fat diet. This resulted to a significant weight loss with an average weight loss of 7.4 kg. Similarly, there was a significant decrease in the total cholesterol and low-density lipoprotein cholesterol by 25-30 mg/dL.

They further stated that the orlistat cholesterol lowering effect was independent of the orlistat weigh loss effects.




7. Orlistat Interactions


Drug interactions refers to how different drugs relate or influence others. These drug interactions influence the way other drugs work and may increase the incidence of adverse side effects associated with use of a certain drug. Orlistat interactions with other drugs have been identified.

Apart from interactions with other drugs, orlistat has not been recommended for use by pregnant or breastfeeding women. It is also not for use by children under the age 12 years.

It is a highly advisable to keep a list of the drugs or medications and to always disclose to your health care provider for best advice on possible interactions. These orlistat drug interactions can be more detrimental to your health overriding the benefits it was taken. Therefore, do not ignore these interactions but rather take precautions.

Some of the known orlistat interactions are;


Orlistat interactions with blood thinners


Blood thinners are drugs that are used in treating certain heart disorders and conditions that put you at risk of dangerous blood clots. They usually help the blood to flow smoothly in the blood vessels. It also prevents clots from forming or becoming bigger.

These blood thinners include warfarin, heparin, apixaban, dabigatran and rivaroxaban among others.

Orlistat may reduce the absorption of vitamin K. Vitamin K is a group of compounds i.e. Vitamin k1 and vitamin K2. Vitamin K is plays a key role in helping the blood to clot and also to prevent excessive bleeding. When its absorption is limited, you will tend to bleed more and easily. This is why taking blood thinners together with orlistat increases your chances of over-bleeding and it can make you bleed more easily.

Some healthcare will advise you to adjust your dosage of the blood thinners to be able to use them together with orlistat. However, unless recommended never alter drugs dosages.


Orlistat interactions with HIV medications


These are also called antiretroviral drugs. The antiretroviral medications are administered to persons suffering from human immune-deficiency virus (HIV) patients to reduce the viral load hence increasing the rate of survival in the patients.

The drugs include lopinavir, ritonavir, atazanavir, efavirenz, tenofovir and emticitabine.

When these drugs are taken along with orlistat, it has been reported that the antiretroviral virology decreases thus the HIV viral load increases instead. You should therefore avoid using orlistat and antiretroviral drugs concomitantly.

In case there is need to take them together, the HIV viral load should be monitored closely and orlistat use should be discontinued if the viral load is found to increase.


Orlistat interactions with seizures medications


Seizures drugs also called antiepileptic drugs are used to reduce seizures/epilepsy symptoms. Fat is an important component in epileptic patients. This therefore leads to weight gain as an adverse effect of these drugs. The seizure drugs include lamotrigine.

Orlistat on the other hand reduces absorption of fat. When used together with antiepileptic drugs, orlistat have been reported to reduce the absorption of the drugs.

Some anecdotal reports that orlistat taken together with seizure drugs increases the occurrence of seizures.


Orlistat interactions with cyclosporine


Cyclosporine also called ciclosporin is a prescription immunosuppressant medication. It is used to prevent the body from rejecting organs after transplant.

When used together, orlistat significantly reduces the plasma levels of cyclosporine. This is because orlistat potentially interferes with the absorption of these drugs.

Some medical professionals recommend not using orlistat while using cyclosporine. However, some medics recommend taking cyclosporine about 3 hours after taking orlistat.


Orlistat interactions with amiodarone


This refers to anti-arrhythmic drug used to restore the normal heart beat as well as maintain a steady and regular rhythm.

Orlistat has been shown to impair the absorption of amiodarone in the blood. this inhibition leads to abnormal heart beat that is a great health risk.

Orlistat interactions with levothyroxine


Levothyroxine is a drug used in treatment of low thyroid activity and also treat certain types of goiters. Low thyroid activity is referred to as hypothyroidism and involves symptoms such as Fatigue, dry skin, impaired memory, weight gain, hoarseness, muscle weakness, high blood cholesterol level, heavier than normal or irregular menstrual periods, low heart beat rate, depression and goiters.

Co-administration of levothyroxine and orlistat has been reported to reduce the level of levothyroxine absorbed. Orlistat is reported to bind to levothyroxine hence, blocking its absorption in the intestines. These can result into severe hypothyroidism which can lead to health problems such as infertility, obesity, pain, and heart disorders.


Orlistat interactions with fat-soluble vitamins


Orlistat may inhibit the absorption of some fat-soluble vitamins and also certain nutrients. The fat soluble vitamins include vitamins A, D, E, K and beta-carotene.

It is highly advisable to take a multivitamin supplement containing the fat- soluble vitamins. The multivitamin supplement should be taken at least 2 hours before or after taking orlistat.


8. Orlistat Side effects


The most common orlistat side effects occur due to the undigested fats passing through your digestive system. They are mostly gastrointestinal effects since the primary route of orlistat is oral and the unchanged fats gets excreted in feces.

The orlistat side effects occur during the first few weeks of taking it and may go away. However, some symptoms may still persist.  The side effects may occur often if the dosage is not right.

These side effects may be overtaken by taking the appropriate prescription while following your doctor s advice on maintaining a reduced calorie, low-fat diet as well as exercise.

The recommended orlistat dosage is 120 mg taken three times daily. Orlistat should preferably be taken before meals as it usually prevents approximately 30% of dietary fat from being absorbed. Higher doses orlistat do not result to more potent effects but rather could lead to some adverse effects.

These orlistat side effects include;

Urgent or difficulty controlling bowel movements

Loose and more frequent bowel movements

Fatty or oily stools

Abdominal or rectum pain or even stomach discomfort

Passing gas more often with oily anal discharge.

The above orlistat side effects may worsen if you take more fat than you should be taking when on orlistat medication.

Some orlistat adverse effects though rare may occur. You are advised to seek medical help immediately when you notice these effects. These orlistat adverse effects may occur to an over dose of the drug. The adverse effects include;

Headaches

Anxiety

Interference in the menstrual cycle

Finding it difficult to breath

Difficulty swallowing

Severe stomach ache that wont go away

Severe dizziness

Swelling (mostly in the tongue, throat or face).

Since some very rare cases of severe liver injury have been linked to the use of orlistat, ensure you watch out for the symptoms of liver injury. You should stop immediately and seek medical help if you experience the following possible signs of liver injury;

Chronic fatigue

Loss of appetite

Hives or severe and persistent itching

Weakness

Vomiting or nausea

jaundice (yellowing of the eyes or skin)

Light-colored/pale stools

Dark urine

Bruising easily

Swelling in ankles or legs.

We have listed the many orlistat side effects and even adverse associated with it, however, always be keen to observe any effects that you may experience and talk to your healthcare provider. Be sure to follow instructions keenly on dosage and proper usage of orlistat to offset most of these effects.

Like with many drugs, the side effects may occur at the start of treatment and fade away with continued use however, some side effects may persist. Overdosing is another common contributor to incidence of most side effects, you therefore not take more of the orlistat than recommended.


9. Where to buy Orlistat?


Products containing orlistat occur in different orlistat brand names. This is because the orlistat manufacturers differ as well as the concentration.

The lower dose of orlistat occur in orlistat brand names such as Alli and Orlos. This can be easily bought online from the many orlistat manufacturers and orlistat suppliers. However, when you consider orlistat buy it from approved pharmacists. Wuhan Wingroup is one of the orlistat manufacturers and offer quality products. The Wuhan Wingroup company have been in the business for long and hence guarantees quality and well packaged orlistat.

Be very cautious with over-the-counter drugs. Read the labels carefully to understand the proper usage of the drugs. Check for the orlistat manufacturer or otherwise the orlistat suppliers, the date of manufacture as well as the date of expiry. Be sure to also check any side effects indicated and warning. For instance, orlistat liver injury is one of the warning or rather indications by the Food and Drug Administration (FDA) for users to take precaution when taking the medicines.  


References

1. "US orlistat label" (PDF). FDA. August 2015. Retrieved 18 April 2018. For label updates see FDA index page for NDA 020766

2. Barbier P, Schneider F (1987). "Syntheses of tetrahydrolipstatin and absolute configuration of tetrahydrolipstatin and lipstatin". Helvetica Chimica Acta. 70 (1): 196C202. doi:10.1002/hlca.19870700124.

3. Bodkin J, Humphries E, McLeod M (2003). "The total synthesis of (−)-tetrahydrolipstatin". Australian Journal of Chemistry. 56 (8): 795C803. doi:10.1071/CH03121.



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