Orlistat in addition to lowering the user’s blood pressure, cholesterol and reduce our weight, we know that obesity is easy to cause diabetes, the use of Orlistat can reduce the incidence of diabetes to a large extent thirty-seven percent down.
It works by suppressing the gastrointestinal lipolytic enzymes in our body so that free fatty acids and monoacylglycerol, two compounds that are not hydrolyzed by triglycerides, are absorbed into the body and converted into body heat. Suppressing the intestinal enzymes reduces calorie intake and ensures that the body heat remains constant.
Orlistat Dosage
Adults: The recommended dosage is one 120mg capsule with a meal or within one hour of a meal. A single dose may be omitted if a meal has not been consumed or if the food does not contain fat. The therapeutic effects (including weight control and improvement of risk factors) of long-term administration of Xenical can be sustained.
The patient’s diet should be nutritionally balanced, minimally low in calories, with approximately 30% of calories coming from fat, and food should be rich in fruits and vegetables. Fat, carbohydrate and protein intake should be distributed over three meals per day. There is no evidence that exceeding 120 mg three times daily enhances efficacy. No dosage adjustment is required for the elderly.
Orlistat Side Effects
There have been rare cases of Orlistat use leading to elevated transaminase, elevated alkaline phosphatase, and severe hepatitis. There have also been cases of liver failure, some of which required liver transplant surgery or led to death. Orlistat has also had rare reports of allergic reactions, mostly including itchiness, rashes, hives, neurovascular edema, bronchospasm and allergic reactions, as well as very rare reports of herpes. Monitoring of sales also found reports of pancreatitis.
Warnings and Precautions It has led to rare cases of acute hepatocellular necrosis and acute liver failure, some of which required liver transplants or led to death. Thus, prescribing physicians must inform patients to immediately cease use of It and other suspicious drugs and seek inspection for liver functions if any symptoms or signs of liver function abnormalities occur (such as reduced appetite, itchiness, jaundice, dark urine, light feces, or pain in the upper right quadrant).
Biochem/physiol Actions
Orlistat weight loss, used in obesity research, is a pancreatic lipase inhibitor that acts locally in the gastrointestinal tract to inhibit lipase.
Clinical Use Adjunct in obesity
Drug interactions Potentially hazardous interactions with other drugs
Acarbose: avoid concomitant administration.
Amiodarone: possibly slightly reduces absorption.
Anticoagulants: monitor INR more frequently (due to reduction in vitamin K absorption).
Antiepileptics: possible increased risk of convulsions.
Antivirals: absorption of abacavir, atazanavir, darunavir, didanosine, efavirenz, elvitegravir, emtricitabine, enfuvirtide, etravirine, fosamprenavir, indinavir, lamivudine, lopinavir, maraviroc, nevirapine, raltegravir, rilpivirine, ritonavir, saquinavir, stavudine, tenofovir, tipranavir and zidovudine possibly reduced.
Ciclosporin: possibly reduces absorption of ciclosporin.
Tacrolimus: possibly reduces absorption of tacrolimus.
Thyroid hormones: possible increased risk of hypothyroidism with levothyroxine.
Vitamins: may reduce the absorption of fat soluble vitamins.
Orlistat powder Chemical Properties
Melting point <50 °C
alpha D20 -32.0° (c = 1 in chloroform)
Boiling point 615.9±30.0 °C(Predicted)
density 0.976±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: 19 mg/mL
form solid
pka 14.59±0.23(Predicted)
color white
Merck 14,6869
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
InChIKey AHLBNYSZXLDEJQ-FWEHEUNISA-N
SMILES C(O[C@H](C[C@H]1[C@H](CCCCCC)C(=O)O1)CCCCCCCCCCC)(=O)[C@H](CC(C)C)NC=O
CAS DataBase Reference 96829-58-2(CAS DataBase Reference)
More Introduction:https://en.wikipedia.org/wiki/Orlistat
