Tetrahydrolipstatin
Tetrahydrolipstatin Uses, Dosage, Side Effects, Food Interaction and all others data.
Tetrahydrolipstatin is a reversible inhibitor of gastrointestinal lipase. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipase. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control.
Tetrahydrolipstatin helps with weight reduction and maintenance by inhibiting the absorption of dietary fats via the inhibition of lipase enzymes.
| Trade Name | Tetrahydrolipstatin |
| Availability | Rx and/or OTC |
| Generic | Orlistat |
| Orlistat Other Names | Orlipastat, Orlipastatum, Orlistat, Tetrahydrolipstatin |
| Related Drugs | phentermine, semaglutide, Wegovy, Saxenda, liraglutide, Alli |
| Type | |
| Formula | C29H53NO5 |
| Weight | Average: 495.7348 Monoisotopic: 495.392373811 |
| Protein binding | Orlistat is >99% bound to plasma proteins (mainly lipoproteins and albumin). |
| Groups | Approved, Investigational |
| Therapeutic Class | Appetite suppressant drugs/Anti-obesity drugs |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tetrahydrolipstatin is used for obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet. Tetrahydrolipstatin is also used for the reduction of the risk of weight regain after prior weight loss. Tetrahydrolipstatin 120 mg is used for obese patients with an initial body mass index (BMI) ≥30 kg/m2 or ≥27 kg/m2 in the presence of other risk factors (eg, hypertension, diabetes, dyslipidemia) and Tetrahydrolipstatin 60 mg is used for overweight & obese patients with an initial body mass index (BMI) ≥25 kg/m2.
Tetrahydrolipstatin is also used to associated treatment for these conditions: Weight Gain, Weight Reduction
How Tetrahydrolipstatin works
Tetrahydrolipstatin is a potent and selective inhibitor of various lipase enzymes responsible for the metabolism of fat. It acts in the gastrointestinal (GI) tract via covalent binding to the serine residues located on the active site of both gastric and pancreatic lipase. When orlistat is taken with food containing fat, it partially inhibits the hydrolysis of triglycerides. This decreases absorption of monoaclglycerides and free fatty acids, contributing to weight maintenance and weight loss.
Dosage
Tetrahydrolipstatin dosage
The recommended dose of Tetrahydrolipstatin is one 60 mg or 120 mg capsule three times a day with each main meal containing fat (during or up to 1 hour after the meal). The patient should be on a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat. The daily intake of fat, carbohydrate, and protein should be distributed over three main meals. If a meal is occasionally missed or contains no fat, the dose of Tetrahydrolipstatin can be omitted.
Because Tetrahydrolipstatin has been shown to reduce the absorption of some fat-soluble vitamins and beta-carotene, patients should be counseled to take a multivitamin containing fat-soluble vitamin to ensure adequate nutrition. The vitamin supplement should be taken at least 2 hours before or after the administration of Tetrahydrolipstatin, such as at bedtime.
Side Effects
Commonly-observed adverse events associated with the use of Tetrahydrolipstatin include oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation, fecal incontinence.
Toxicity
The oral LD50 of orlistat is >5000 mg/kg in rats. Single orlistat doses of 800 mg and multiple doses of up to 400 mg three times a day for 15 days have been administered to healthy weight and obese subjects without clinically significant adverse findings. In addition, doses of 240 mg three times a day have been given to obese patients for 6 months without a significant adverse effects. Post-marketing reports of overdoses cases indicate no adverse events or adverse events that are similar to those reported with the recommended dose. If a significant overdose with orlistat occurs, the patient should be observed for at least 24 hours. Based on the results of clinical studies, systemic effects caused by orlistat are likely to be rapidly reversible.
Precaution
Patients should be advised to adhere to dietary guidelines. gastrointestinal events may increase when orlistat is taken with a diet high in fat (>30% of calories from fat). The daily intake of fat should be distributed over three main meals. If a meal is missed, the dose of orlistat may be omitted.
Interaction
May reduce the absorption of iodine salts and/or levothyroxine, fat-soluble vit (A, D, E, K) and beta carotene. May decrease plasma levels of ciclosporin and amiodarone. May decrease the efficacy of antiepileptic drugs (e.g. valproate, lamotrigine), antiretrovirals, antidepressants, antipsychotics (including lithium). Additive effect on glycaemic control with antidiabetics. May cause hormonal contraceptive failure. May enhance the anticoagulant effect of warfarin.
Food Interaction
- Take with food. Take with meals or up to 1 hour after a meal. Doses may be skipped for missed meals or fat-free meals.
Tetrahydrolipstatin multivitamins interaction
[Minor] Tetrahydrolipstatin decreases the absorption of fat-soluble vitamins.
Studies have shown a 30% reduction in beta-carotene absorption and a 60% reduction in tocopherol acetate absorption when coadministered with orlistat.
Vitamin supplements should be taken at least two hours before or after orlistat administration.
Tetrahydrolipstatin Drug Interaction
Moderate: lamotrigine, levothyroxineMinor: cholecalciferolUnknown: amphetamine / dextroamphetamine, zolpidem, aspirin, lorazepam, celecoxib, duloxetine, omega-3 polyunsaturated fatty acids, fluticasone nasal, clonazepam, atorvastatin, pregabalin, acetaminophen, cyanocobalamin, ascorbic acid, alprazolam, sertraline, cetirizine
Tetrahydrolipstatin Disease Interaction
Major: malabsorptionModerate: diabetics, (fat soluble) vitamin deficiency, nephrolithiasis
Volume of Distribution
Volume of distribution cannot be obtained because the absorption of orlistat is minimal. Tetrahydrolipstatin is minimally distributed to erythrocytes and is primarily bound to proteins.
Elimination Route
The systemic absorption and exposure of orlistat is low, however, systemic absorption of the drug is not required for orlistat activity. After an oral dose with 360 mg of radiolabeled orlistat, plasma radioactivity achieved a peak at about 8 hours. Plasma concentrations of unchanged parent drug were close to the lower end of detection limits (15
Half Life
The half-life of orlistat of the small amount of absorbed orlistat ranges between 1-2 hours.
Elimination Route
After single oral dose of radiolabled orlistat in both normal weight and obese volunteers fecal excretion of the unabsorbed drug was found to be the major route of elimination with 11,20 Fecal elimination of orlistat is estimated between 95-97%. Complete excretion by both routes occurs within in 3 to 5 days.
Pregnancy & Breastfeeding use
Pregnancy Category X. Tetrahydrolipstatin is contraindicated during pregnancy, because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm.
It is not known whether Tetrahydrolipstatin is present in human milk or not. Caution should be exercised when Tetrahydrolipstatin is administered to a nursing woman.
Contraindication
Tetrahydrolipstatin is contraindicated in Pregnancy, Patients with chronic malabsorption syndrome, Patients with cholestasis, Patients with known hypersensitivity to Tetrahydrolipstatin or to any component of this product.
Special Warning
Pediatric use: Safety and effectiveness in pediatric patients below the age of 12 have not been established.
Acute Overdose
Single doses of 800 mg and multiple doses of up to 400 mg three times a day for 15 days have been studied in normal weight and obese subjects without significant adverse findings. If a significant overdose of orlistat occur, it is recommended that the patient be observed for 24 hours. Based on human and animal studies, any systemic effects attributable to the lipase inhibiting properties of orlistat should be rapidly reversible
Storage Condition
Store below 25°C; excursions permitted to 15° to 30°C. Keep the medicine out of reach of children.
Innovators Monograph
You find simplified version here Tetrahydrolipstatin
Tetrahydrolipstatin contains Orlistat see full prescribing information from innovator Tetrahydrolipstatin Monograph, Tetrahydrolipstatin MSDS, Tetrahydrolipstatin FDA label
FAQ
What is Tetrahydrolipstatin used for?
Tetrahydrolipstatin is used with an individualized low-calorie, low-fat diet and exercise program to help people lose weight. Prescription Tetrahydrolipstatin is used in overweight people who may also have high blood pressure, diabetes, high cholesterol, or heart disease.
How safe is Tetrahydrolipstatin?
The Food and Drug Administration published a safety review of orlistat in 2010 because of rare reports of serious liver injury in people using it. The FDA found no evidence to confirm that Tetrahydrolipstatin was the cause of the reported liver injuries.
How does Tetrahydrolipstatin work?
Tetrahydrolipstatin works by blocking the receptors in the brain that dopamine acts on. This prevents the excessive activity of dopamine and helps to control psychotic illness.
What are the common side effects of Tetrahydrolipstatin?
Common side effects of Tetrahydrolipstatin are include:
- Abdominal or stomach pain or discomfort
- back pain
- difficulty with moving
- gas with leaky bowel movements
- inability to hold bowel movement
- increases in bowel movements
- loss of bowel control
- oily bowel movements
- oily spotting of underclothes
Is Tetrahydrolipstatin safe during pregnancy?
Tetrahydrolipstatin should not be used during pregnancy as it may harm your unborn baby. Weight loss offers no potential benefit to a pregnant woman and may result in fetal harm.
Is Tetrahydrolipstatin safe during breastfeeding?
It is unlikely that Tetrahydrolipstatin will be absorbed by the infant in amounts that would adversely affect the breastfed infant.
Can I drink alcohol with Tetrahydrolipstatin?
Tetrahydrolipstatin does not interact with alcohol, so it is safe to drink alcohol while taking Tetrahydrolipstatin.
Can I drive after taking Tetrahydrolipstatin ?
You may feel less alert, drowsy or sleepy and have blurred vision while taking this medicine. If this happens, do not drive or use any tools or machines.
When should be taken of Tetrahydrolipstatin?
You should take it with liquids during the meal or up to 1 hour after eating. If you occasionally miss a meal or eat a meal that contains no fat, you should skip the dose of Tetrahydrolipstatin.
Can I take Tetrahydrolipstatin on empty stomach?
Tetrahydrolipstatin only works when there are fats in what you eat, so if you miss a meal or if you eat a meal which is fat-free then do not take a dose of Tetrahydrolipstatin.
How long does Tetrahydrolipstatin take to work?
You can expect to see results in 1-3 months; aiming to lose 5% of your starting body weight in 3 months.
What is the half life of Tetrahydrolipstatin?
The half-life of the absorbed orlistat is in the range of 1 to 2 hours.
How long does Tetrahydrolipstatin take to work?
You should not take Tetrahydrolipstatin for more than six months over the counter.
What happen if I forget to take Tetrahydrolipstatin?
If you forget to take a dose at the right time, take it as soon as you remember, then go on as before. However, do not take a double dose to make up for a forgotten tablet.
What happen If I stop taking Tetrahydrolipstatin?
Keep taking Tetrahydrolipstatin until your doctor tells you to stop. Do not stop taking your medicine just because you feel better as your illness may get worse or come back. Unless your doctor tells you otherwise, Tetrahydrolipstatin should not be stopped suddenly as this may cause withdrawal effects such as muscle stiffness or unusual body movements.
Can I overdose on Tetrahydrolipstatin ?
Yes, you can overdose on Tetrahydrolipstatin. Although the symptoms of such an overdose are not known, they are probably the same as the side effects. This includes: nausea, vomiting, diarrhea, gas, abdominal distress, oily feces and incontinence of feces.
Does Tetrahydrolipstatin effect fertility?
In Tetrahydrolipstatin group, significant improvement was observed in lipid profile at the end of 3 months. Conception rates were 40% and 16.7% and 3.3% in Tetrahydrolipstatin, metformin group and control group respectively.
Can Tetrahydrolipstatin affects my heart ?
Treatment with Tetrahydrolipstatin in conjunction with diet promotes significantly greater weight loss and cardiovascular risk factor reduction than diet alone amongst obese patients at high risk of future coronary events.
Can Tetrahydrolipstatin affect my kidneys?
Tetrahydrolipstatin use has been limited by troublesome but benign gastrointestinal side effects, it has more recently been associated with acute kidney injury (AKI).
Can Tetrahydrolipstatin affects my liver?
The liver injury that occurs during Tetrahydrolipstatin therapy ranges in severity from minor serum aminotransferase elevations to acute symptomatic hepatitis to severe acute liver failure that can be fatal or require emergency liver transplantation. There is no known therapy for orlistat induced liver injury.
Is Tetrahydrolipstatin good for weight loss?
Tetrahydrolipstatin promotes weight loss by decreasing the amount of dietary fat absorbed in your intestines.
Is Tetrahydrolipstatin harmful?
More specifically, the use of Tetrahydrolipstatin has been associated with several mild-to-moderate gastrointestinal adverse effects, such as oily stools, diarrhoea, abdominal pain and faecal spotting.
Can Tetrahydrolipstatin affect periods?
Women may also notice irregularities in the menstrual cycle while taking Tetrahydrolipstatin. Side effects are most common in the first few weeks after beginning the drug.
Does Tetrahydrolipstatin cause depression?
Evidence suggested one in 10 people taking the Tetrahydrolipstatin, whose Tetrahydrolipstatin name is Acomplia, may develop mental side-effects including low mood and depression, anxiety, irritability, nervousness and sleep disorders.
Can Tetrahydrolipstatin cause weight gain?
Tetrahydrolipstatin can cause weight gain also with other side effects.
