Orlistat capsules combined with a low-calorie diet are suitable for obese and overweight people
Traits
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This product is a capsule, and the content is white to off-white pellets.
Indications
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Orlistat capsules combined with low-calorie diet are suitable for long-term treatment of obese and overweight patients, including those who have developed risk factors related to obesity. Orlistat capsules have long-term weight control (weight loss, weight maintenance and prevention of rebound) effects. Taking Orlistat capsules can reduce the risk factors associated with obesity and the incidence of other obesity-related diseases, including hypercholesterolemia, type 2 diabetes, impaired glucose tolerance, hyperinsulinemia, hypertension, and Reduce the fat content in the organs.
specification
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0.12g
Dosage
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adult:
The recommended dosage of orlistat capsules is one 0.12g capsule taken with or within one hour after a meal. If there is no meal or the food does not contain fat, you can omit a medication. The therapeutic effects of long-term use of Orlistat capsules (including weight control and improvement of risk factors) can be sustained. The patient’s diet should be nutritionally balanced, low-calorie energy, about 30% of the caloric energy comes from fat, and the food should be rich in fruits and vegetables. Fat, carbohydrate and protein intake should be distributed among three meals a day. There is no evidence that more than three times a day, 0.12g each time can enhance the efficacy.
There is no need to adjust the dose for the elderly.
Determination of fat content in feces shows that the efficacy of orlistat capsules can be manifested within 24 to 48 hours after administration. The fat content in the stool returned to the pre-treatment level 48 to 72 hours after stopping the treatment.
Patients with liver and (or) renal insufficiency do not need to adjust the dose. Or follow the doctor's advice.
Adverse reactions
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Clinical research experience
Orlistat capsules mainly cause gastrointestinal adverse reactions, which are related to the pharmacological effects of the drug to prevent the absorption of ingested fat. Common adverse reactions are: oily spots, increased gastrointestinal gas, stool urgency, fatty (oily) stools, seborrheic diarrhea, increased stool frequency and fecal incontinence.
As the fat content in the diet increases, the incidence of the above-mentioned adverse reactions increases accordingly. Patients should be informed about the possibility of gastrointestinal reactions and how to deal with them properly, such as improving the diet, especially the control of fat content. A low-fat diet can reduce the possibility of gastrointestinal adverse reactions, which helps patients to detect and adjust their fat intake.
These gastrointestinal adverse reactions are usually mild and transient. They appear in the early stage of treatment (the first 3 months), and most patients only experience a period of adverse reactions.
Acute gastrointestinal reactions that usually occur in patients taking Orlistat capsules are: abdominal pain/abdominal discomfort, flatulence, watery stool, soft stool, rectal pain/rectal discomfort, dental discomfort, gum discomfort .
Other rare adverse events observed are: upper respiratory tract infection, lower respiratory tract infection, influenza, headache, menstrual disorders, anxiety, fatigue, urinary tract infection.
Post-IPO experience
There are occasional reports of allergies to this product. The main clinical manifestations are pruritus, rash, urticaria, angioedema and allergic reactions.
Rarely, there have been reports of cases of herpes, elevated liver transaminase and alkaline phosphatase, and rare hepatitis.
After the market, when patients take orlistat in combination with anticoagulant, thrombin will decrease, INR (International Normalized Ratio) will increase, and the hemostatic parameters will change due to the imbalance of anticoagulant treatment.
Taboo
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Patients with chronic malabsorption syndrome or cholestasis and those who are allergic to orlistat or any ingredient in pharmaceutical preparations are contraindicated.
Precautions
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After up to two years of treatment with orlistat, most patients' vitamin A, E, K, and β-carotene levels are still within the normal range. In order to ensure sufficient nutrients, you can consider supplementing with multivitamins.
Patients should be educated to follow dietary guidelines (see [Usage and Dosage]). When orlistat capsules are combined with a high-fat diet (such as 2000 calories a day, more than 30% is supplied by more than 67 grams of fat), the possibility of gastrointestinal events (see [Adverse Reactions]) will increase . The daily fat intake should be distributed among the three main meals. When orlistat capsules are taken with a high-fat meal, the possibility of gastrointestinal reactions increases.
In patients with type 2 diabetes, orlistat capsules can cause weight loss and often accompanied by improved blood sugar control, which may or need to reduce the dose of oral hypoglycemic drugs (such as sulfonylurea drugs).
Orlistat capsules combined with cyclosporine can cause a decrease in the plasma concentration of the latter. Therefore, it is recommended that when orlistat capsules are used in combination with cyclosporine, the latter's serum concentration should be monitored more closely than usual. Patients should be monitored for blood coagulation parameters when combined with anticoagulants for oral administration. The results of the pharmacokinetic study of combined oral medication with amiodarone show that the systemic absorption of amiodarone and desethylamiodarone will be reduced by 25-30%. Due to the complex pharmacokinetics of amiodarone, the clinical effect of this result is unknown. There has not been a study on the efficacy of patients receiving amiodarone stabilization while taking orlistat, and it is expected that the efficacy of amiodarone may be reduced. (See [Drug Interactions])
Medication for pregnant and lactating women
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No embryo toxicity and embryo malformations related to orlistat were observed in animal reproductive toxicity studies. No embryo abnormalities have appeared in animal studies, and orlistat is not expected to cause teratogenicity in humans. In any case, in the absence of clinical data, it is not recommended to take Orlistat capsules during pregnancy. It has not been studied whether orlistat is excreted by human milk, so orlistat capsules should not be taken during breastfeeding.
Children's medication
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For children under 18 years of age: The safety and efficacy of orlistat capsules for children have not been studied.
Elderly medication
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See 【Usage and Dosage】, or follow the doctor's advice.
medicine interactions
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In pharmacokinetic studies, no drug interactions between orlistat and alcohol, digoxin, metformin, nifedipine, oral contraceptives, phenytoin, statins, or warfarin were observed. However, when warfarin or other anticoagulants are used in combination with orlistat capsules, the patient's international normal blood clotting time ratio should be monitored.
It has been observed that the absorption of vitamin D, E and β-carotene is reduced when taken together with orlistat capsules. If a multivitamin supplement is needed, it should be taken at least 2 hours after taking Orlistat capsules, or before going to bed.
When was taken at the same time with orlistat capsules, a decrease in the plasma concentration of cyclosporin A has been observed. Therefore, when orlistat capsules and cyclosporine A are administered at the same time, the monitoring of the plasma concentration of cyclosporine A should be strengthened.
Overdose
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Studies in normal-weight and obese individuals have shown that oral orlistat capsules of 0.8 g as a single dose and 0.4 g three times a day for 15 days have no significant adverse events. In addition, obese people took orlistat 0.24g three times a day for 6 months, and no significant adverse events were observed.
After the market, there were no adverse events caused by overdose or the adverse events produced were similar to those produced by the recommended dose. If there is a significant overdose of this product, the patient should be observed for 24 hours. According to human and animal experiments, the systemic reaction caused by orlistat inhibition of lipase is rapid and reversible.
Pharmacology and Toxicology
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Orlistat is a long-acting and potent specific gastrointestinal lipase inhibitor. It forms a covalent bond with the active serine site of gastric lipase and pancreatic lipase in the stomach and small intestine to inactivate the enzyme. effect. Inactivated enzymes cannot hydrolyze fats in food (mainly triglycerides) into absorbable free fatty acids and monoacylglycerols. Undigested triglycerides cannot be absorbed by the body, thereby reducing calorie intake and controlling weight. The drug does not need to be absorbed systemically to be effective.
Pharmacokinetics
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absorb
Research on normal-weight and obese volunteers showed that the body's absorption of orlistat is minimal, and the complete plasma concentration of orlistat ([5 ng/ml) cannot be measured 8 hours after oral administration. The systemic absorption of usually therapeutic dose of orlistat is extremely limited and does not accumulate. Only occasionally intact orlistat can be detected in plasma at a very low concentration ([10 ng/ml or 0.02μm).
distribution
Since orlistat is hardly absorbed, it is difficult to measure the volume of distribution, and the systemic pharmacokinetics cannot be measured. In vitro, more than 99% of orlistat is bound to plasma proteins (lipoprotein and albumin are the main binding proteins). Orlistat rarely binds to red blood cells.
Metabolism
Animal experiments indicate that the metabolism of orlistat is mainly concentrated in the wall of the gastrointestinal tract. Studies conducted in obese patients have shown that there are two main metabolites in a very small part of the drug components that are absorbed systemically, M1 (4-ring lactone ring hydrolysate) and M3 (M1 attached to an N-formyl bright Amino acid cleavage products) accounted for 42% of the total plasma concentration.
M1 and M3 have an open β-lactone ring and have very weak inhibitory activity on lipase (compared with orlistat, 1000 times and 2500 times lower, respectively). At the therapeutic dose, the inhibitory activity and plasma concentration of M1 and M3 are very low (mean M1, 26 ng/ml and M3, 108 ng/ml), so these two metabolites have no pharmacological significance.
clear
Studies on people with normal weight and obesity show that unabsorbed drugs are mainly excreted through feces. Approximately 97% of the dose taken was excreted from the feces, of which 83% was original orlistat, and the cumulative renal excretion of all orlistat related substances was less than 2%. It takes 3 to 5 days for the drug to be completely discharged (feces and urine). For normal weight and obese subjects, the metabolism of orlistat is very similar. Orlistat, M1 and M3 can all be excreted via bile.
Store
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This product should be stored below 25°C, protected from moisture.
Medicines should be stored out of the reach of children.
package
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Aluminum plastic packaging
7 capsules/box, 21 capsules/box, 42 capsules/box, 84 capsules/box, 168 capsules/box, 252 capsules/box.
Valid period
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36 months. It should not be taken after the expiry date shown on the package. [1]
