A rather well-known and popular modern remedy is Xenical tablets based on orlistat, the instructions for use of which are worth considering in more detail. In pharmacies, the drug is dispensed strictly according to the doctor’s prescription. Those who underwent treatment with this agent mainly assure its effectiveness and strong effect: under the influence of active substances and in combination with additional therapeutic measures, patients were able to quickly get rid of extra pounds. However, not everything is so positive: there are also negative reviews about Xenical, partly due to individual reactions of the body, partly to non-compliance with the manufacturer's recommendations.
What's on sale?
In the instructions for use for the Xenical preparation, the manufacturer indicates that the product is available in the form of hard capsules made using gelatin. The hue is turquoise, on each copy there is an inscription “Xenical 120”. Inside the capsule is a white or close to white pellet orlistat. One tablet contains 120 mg of active substance.
As additional components are used:
- talc;
- cellulose;
- primogel;
- povidone;
- sodium lauryl sulfate;
- gelatin;
- titanium dioxide;
- dye (carmine).
It is especially important for people suffering from intolerance to any substances or allergic reactions to familiarize themselves with the instructions for the Xenical preparation in the part that describes the composition.
One cardboard package contains several blisters (from one to four), each blister contains 21 capsules.
Pharmacology
The main substance "Xenical" is a specific component that inhibits the activity of lipases in the digestive tract. The action of orlistat is reversible, rather long. The activity of the components is manifested in the gastric lumens, intestinal tract. Orlistat forms bonds with lipases:
As the manufacturer explains the effectiveness of Xenical tablets in the manufacturer’s instructions, under the influence of orlistat, GIT enzymes cannot interact with mono-, triglycerides, fatty acids. Unsplit triglycerides are not able to penetrate the walls of the gastric tract, which means that the body receives fewer calories, therefore, body weight gradually decreases. An important advantage mentioned in the instructions for the Xenical drug is the inability of the active compound to be absorbed, exerting a systemic effect. The drug affects locally, strictly within the gastrointestinal tract, does not enter the circulatory system.
Studies of feces of patients show that a pronounced effect is observed after 1-2 days from the start of therapy. The indicators return to their previous values 2-3 days after the termination of the use of the product.
Does it work?
In the instructions for the tablets "Xenical" mentioned the results of clinical trials designed to identify the effectiveness of the drug. To determine the exact results, two groups of patients were simultaneously tested - those who took Xenical and underwent treatment only with diet. In the first group, persistent weight loss was observed in the first two weeks from the start of administration, and lasted from six months to a year, while diet therapy did not show significant results. Reception of "Xenical" allowed to lose weight even to those patients whose response to the diet was negative.
The instructions for use of “Xenical” indicate that prolonged (two years or more) use of the composition allowed us to reduce the risks associated with weight gain and normalize metabolism. A comparison with the placebo group showed a significant reduction in body fat. The active component, as tests have shown, has a pronounced preventive effect, preventing the return of extra pounds. In half of the patients, after completing the course, body weight increased again, but not more than by a quarter from the lost kilograms. The other half, even after the completion of the program, did not experience repeated increases, and some showed a tendency to further lose weight.
Overweight and Diabetes
The most interesting results are obtained when patients with the second type of diabetes mellitus take Xenical tablets. In the instructions for use by the manufacturer, the results of clinical trials of the effectiveness of the drug for this group of people are mentioned. The duration of observations varied from six months to a year, and two groups were simultaneously monitored:
- receiving orlistat;
- corrective body weight only diet.
In the first group, the results were much more pronounced. The effects of weight loss in the instructions of "Xenical" are explained by a decrease in the number of fatty structures in the body of patients.
The manufacturer pays particular attention to the following fact: prior to the use of Xenical, many patients took hypoglycemic drugs that did not show a sufficient effect. The use of orlistat has increased glycemic control. The effect is proved by statistics, the improvement was evaluated as clinical. Both in the reviews about the drug, and in the instructions of "Xenical" it is indicated that the use of this composition can reduce the volume of hypoglycemic drugs, insulin. Patients decreased insulin resistance.
Diabetes prevention
It is known that the risk of developing diabetes is more inherent in people suffering from extra pounds, expressed as obese. The Xenical instructions refer to the results of a four-year research program designed to identify the effects on the likelihood of developing diabetes in people with extra pounds. The results show that the second type of disease develops much less frequently, the difference with the placebo group was 37%.
A sufficiently significant reduction in risks was noted in the group of people with impaired glucose tolerance. Clinical trials show a 45% reduction in hazard. At the same time, patients got rid of extra pounds, a reduced mass was maintained throughout the observation period of patients. Compared to the placebo group, those taking Xenical, as the tests showed, were at lower risk of metabolic disturbance.
Xenical in adolescence
The instructions to "Xenical" mentioned the possibility of using the drug to get rid of excess weight in the puberty. Clinical trials were conducted for one year, adolescents with severe weight problems were selected for them. The analysis was conducted with the participation of a placebo group. As a result, the body mass index among users of orlistat decreased, and in the opposite group increased.
Among the patients who used Xenical according to the instructions, the majority of the fat masses in the body became smaller, and their body size decreased. When taking Xenical, the patients returned to normal pressure, which was not observed in the placebo group.
Is it safe?
As the manufacturer assures, the drug on orlistat does not provoke specific risks - this is indicated in the instructions attached to the Xenical tablets. Reviews of losing weight using a medication under the supervision of a doctor also confirm that the remedy does not provoke health problems. Tests have shown that the drug does not affect the reproductive organs, does not initiate cancer and does not violate the gene structure, cannot be the cause of mutations. Animal studies have shown no teratogenic effect, on the basis of which it is possible to speak with a high degree of confidence about the absence of such in humans.
Kinetics
The instruction “Xenical” contains data obtained during the study of a mixed group of volunteers, some of which had normal weight indicators, while others were diagnosed with obesity. Observations showed that when 360 mg was taken orally in plasma, the active component in an unchanged form is not detected, therefore, its concentration in the circulatory system is 5 ng / ml or less.
After the use of oral therapeutic doses in extremely rare cases, the presence of an un metabolized orlistat in the bloodstream was found, the concentration level was estimated at less than 10 ng / ml. It was not possible to identify the cumulative effect, on the basis of which the manufacturer with confidence declares the minimum absorption.
It is impossible to determine how orlistat is distributed in the body, which is explained by a low level of absorption (this is mentioned in the instructions for use of "Xenical" for weight loss). Special studies have revealed that up to 99% of a substance comes into contact with plasma proteins, mainly interacting with albumin, lipoproteins. A small amount of the active component was observed in red blood cells.
Metabolism and elimination
Animal experiments have shown that orlistat transformation occurs in the intestinal walls. When studying a group of obese people, it was revealed that about 42% of the minimum absorbed volume of orlistat are two products of chemical reactions: M1, M3. Both molecules are characterized by an open beta-lactone ring, a low level of lipase inhibition. This makes it possible to classify metabolic products as inactive compounds if Xenical is used in dosages recommended by the manufacturer.
As it was possible to identify in the study of patients with excess weight, as well as individuals with normal body weight, excretion of orlistat occurs with feces - up to 97% of the total substance used in food. About 83% leave the body unchanged.
The total withdrawal of orlistat and its metabolic products through the kidneys is estimated at less than 2%. The duration of orlistat excretion in full is from three days to five. Orlistat and its metabolic products may be excreted with bile. A study of different groups of patients showed that the withdrawal routes of the compounds are independent of the patient’s body weight.
Special occasion
Comparative studies of a group of adult patients and minors were conducted. It was not possible to identify clinically significant differences in the concentration of orlistat and the main products of its metabolism in blood plasma in different age groups. Fat with feces with the use of "Xenical" is excreted in an amount of 27%, in the placebo group the indicator was estimated at 7%.
When to use?
The manufacturer recommends the use of the drug:
- as a means for the long-term treatment of overweight people in combination with a reduced calorie diet program;
- as an element of a comprehensive treatment for the second type of diabetes and extra pounds, including obesity.
The second option involves the combination of orlistat and hypoglycemic agents. The drug approach is enhanced by a diet with a minimum calorie content. As medicines that are acceptable for use in combination with Xenical, the following are mentioned:
- insulin;
- metformin;
- sulfonylurea products.
Terms of use
The manufacturer draws attention to the need to comply with the dosage recommended in the instructions for use. Reviews of those losing weight about the drug show that a violation of the recommendations of the manufacturer, the doctor can cause therapy inefficiency. You should not prescribe a dosage yourself.
Prolonged use of Xenical for overweight, obesity, supplemented by a low-calorie diet program, involves the use of the drug one capsule during the main meal. The course is suitable for people over the age of twelve. A single dosage is 120 mg of orlistat. The medication is used as food during a meal or shortly after, but no later than an hour from the moment the products enter the body.
For adults undergoing combination therapy with hypoglycemic drugs, a low-calorie diet and orlistat, the optimal dosage is similar: according to the instructions, the Xenical tablet. Reviews indicate the effectiveness of such a program in the second type of diabetes.
The manufacturer mentions the need to take the medication only during the main meal containing fats. If the meal is skipped, if low-fat products are used, you do not need to use Xenical.
Features of use
The manufacturer recommends combining the medication with a high-quality low-calorie nutrition program - this is especially noted in the Xenical instructions. Reviews indicate that doctors, prescribing the drug, also require the patient to follow a balanced diet, controlling the intake of calories with fatty structures: they should account for less than a third of the total energy volume. To achieve maximum results, the program is combined with three meals a day, evenly distributing carbohydrates, proteins, fatty structures for all three times.
Both in the reviews and in the instruction of “Xenical” it is mentioned that there is no amplification of the effect when the dose recommended by the manufacturer is exceeded. Therefore, it is wise to use the drug three times a day for 120 mg.
There is no information about the possibility of using Xenical in the following groups of patients:
- children under the age of twelve;
- elderly patients;
- persons suffering from impaired liver and kidney function.
No studies have been conducted that can confirm the effectiveness of the drug or identify the risks associated with its use for these categories.
Orlistat and gastrointestinal tract
In the reviews, instructions for use of "Xenical" for weight loss, the possibility of a negative response of the body is mentioned. Mostly, patients encountered gastrointestinal tract functioning problems associated with the pharmacological effect of the drug - fatty structures are not absorbed when passing through the intestines, so patients were disturbed by oily discharge. It is indicated that the following are possible:
- discharge with gases;
- imperative bowel movements;
- increased gas formation;
- diarrhea;
- discomfort, pain in the abdomen;
- increased frequency of bowel movements;
- steatorrhea.
In the reviews, instructions for use of "Xenical" it is mentioned that the manifestations are stronger and more often, the more fat comes with food. The manufacturer draws attention to the need to warn patients before the start of the course about the possibility of such manifestations. The doctor must explain how to behave, what kind of diet to follow during the course, how to regulate the amount of fat in the incoming food. The lower the percentage of fat in foods, the weaker the negative manifestations, which means that it is easier for the patient to tolerate treatment. In addition, a low-calorie low-fat diet increases the effectiveness of the program as a whole.
As follows from the reviews, the instructions for use of “Xenical”, along with medical recommendations, helps many to master the control of fat intake, which means to maintain normal weight at the end of therapy.
The listed adverse reactions in the majority of those taking orlistat are poorly expressed, which are more characteristic of the first three months of using the drug. As follows from the reviews, the overwhelming majority of patients did not encounter negative effects at all.
Side effects
The manufacturer indicates the possibility of occurrence when taking "Xenical" adverse events:
- fecal incontinence;
- discomfort, soreness in the intestines;
- diseases of the gums, teeth;
- headaches;
- menstrual irregularities;
- general weakness;
- anxiety;
- increased likelihood of viral, infectious diseases of the respiratory system;
- risk of urinary tract infection.
Comparison of the results of the use of type II diabetes mellitus and other patients showed that there are no significant differences in the manifestation of side effects, with the exception of the possibility of hypoglycemia. The probability of this condition is estimated at more than 2%.
Tests were conducted to identify the safety profile based on the results of one-year, two-year and four-year observations. It was not possible to identify the difference, but statistics show that every year the risk of manifestation of negative effects on the digestive tract is reduced.
Post-marketing studies have shown that an allergy to the drug is possible, manifested:
- urticaria;
- skin rashes;
- itchy patches;
- angioedema;
- anaphylaxis;
- spasm of the bronchi.
With an extremely low probability, the following can be observed:
- bullous rash;
- activation of transaminases, phosphatases;
- hepatitis.
Regarding hepatitis, it was not possible to prove the connection between the development of the disease and the administration of Xenical. No mechanisms have been identified that could provoke such a side effect.
The combination of Xenical and anti-epilepsy drugs can cause a seizure condition. The use of anticoagulants and orlistat in a small percentage of cases led to a reduction in prothrombin, a change in blood parameters.
Contraindications "Xenical"
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Too much!
Observations were made of individuals who used 400 mg of orlistat three times a day or 800 mg once a day for 15 days. The results show that the frequency of side effects does not increase. The experience of the six-month use of 240 mg of orlistat three times a day against the background of obesity is also known, which was also not accompanied by an increase in the frequency of negative responses of the body.
In case of an overdose, the side effects either did not manifest themselves or did not differ from those characteristic of normal doses.
In case of severe overdose, the doctor should be informed about the incident: the manufacturer recommends monitoring the patient's condition in hospital conditions during the day. As the studies show, the systemic effect of orlistat should be reversible in a short time.
Mutual impact
Patients were monitored simultaneously with orlistat who consumed:
- warfarin;
- amitriptyline;
- fluoxetine;
- nifedipine;
- phentermine;
- sibutramine;
- oral contraceptives;
- fibrates;
- biguanides;
- digoxin;
- phenytoin.
Significant interactions could not be identified.
Attention should be paid to individuals using anticoagulants, including warfarin - such therapy requires INR monitoring in case of an atypical response of the body.
It is known that when consuming orlistat, the quality of absorption worsens:
- beta carotene;
- calciferol;
- tocopherol.
Multivitamin complexes are reasonable to eat two hours after orlistat or later. The manufacturer recommended the use of vitamins before bedtime.
The combination of "Xenical" and cyclosporins leads to a decrease in the concentration of the latter in blood plasma. To prevent the ineffectiveness of therapy, it is necessary to monitor blood quality indicators more often and adjust the dosage if necessary.
If orally prescribed drugs on amiodarone, the systemic exposure of this component against the background of orlistat can decrease by almost a third. A similar effect is possible with respect to desethylamiodarone. The clinical significance of this fact has not yet been established, since amiodarone has a very complex kinetics. Presumably, against the background of orlistat, a long course of amiodarone may be accompanied by a decrease in the therapeutic effect, but there were no studies to confirm or refute this fact.
The manufacturer recommends abstaining from the simultaneous use of acarbose and orlistat, since there is no data on a possible interaction.
The combination of orlistat with anti-epilepsy drugs can trigger seizures. No causal relationship has been identified at the moment, but it is recommended to monitor the condition of people using both types of medications.
Xenical: analogues
The instructions for the following drugs indicate that the active component is orlistat, which allows us to conclude that they are similar to Xenical:
- "Orsoten."
- "Allie."
- Listata.
- "Orliksen."
- Xenalten.
Before replacing a drug prescribed by a doctor with an analogue, you should consult your doctor about the possibility of such a replacement. On average, the prices for Xenical and their analogues are similar: packages with a minimum number of capsules (21 pieces) cost from 700-800 rubles, the maximum volume calculated for three months will cost the buyer 2-3 thousand rubles.