Ksenikal

Ксеникал Drug photo

The description is actual on 16.11.2015

  • Latin name: Xenical
  • ATH code: A08AB01
  • Active ingredient: Orlistat (Orlistat)
  • Producer: F. Hoffmann-La Roche Ltd, Switzerland

Structure

Ksenikal (capsules) are a part of one tablet: 120 mg of an orlistat (in the form of pellets 240 mg) and talc as an excipient.

Contain in one pellet: 120 mg of an orlistat, MKTs, primogel (Na carboxymethylstarch), K-30 povidone, Na lauryl sulfate.

At production of a cover of capsules indigo carmine, gelatin, titanium dioxide are used.

Release form

Capsules.

Capsules are firm, gelatinous, turquoise color. On the body the text of "XENICAL 120", is applied on a lid a text of "ROCHE".

Capsules are packaged in blisters on 21 pieces, unitary enterprise. No. 21, No. 42, No. 84.

Pharmacological action

Inhibiting gastrointestinal tract lipases.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Drug in unusual way, powerfully and reversibly influences gastrointestinal tract lipases (the enzymes helping to fraction, dissolve and digest fats). It is characterized by long action.

Effect of drug is carried out in a gleam of a stomach and a small bowel. Therapeutic effects are caused by ability of an orlistat to form a covalent bond with an active serinovy site of lipases of PZhZh and a stomach.

After an inactivation enzyme is not capable to split the food fats arriving in the form of triglycerides on monoglycerides and not esterified (free) fatty acids.

The split triglycerides in an organism are soaked up owing to what receipt of calories decreases and body weight decreases.

Thus, drug works, without being soaked up in a system blood stream.

By results of the analyses defining concentration of fat in Calais it is possible to see that effects of an orlistat begin to be shown 1-2 days later after reception of capsules.

After Ksenikal's cancellation concentration of fat returns to Calais to the level which took place prior to therapy, in 2-3 days.

Pharmacokinetics

System influence of substance is minimum as at the persons having normal body weight and at the persons having obesity. After a single dose of three capsules of 120 mg substance in not changed look in plasma is not defined that demonstrates that its plasma concentration does not exceed 5 ng/ml.

After reception of therapeutic doses of Ksenikal it was possible to find not changed substance in a blood plasma extremely seldom, at the same time its contents was insignificant a little.

Because of bad absorption of an orlistat it is impossible to determine its volume of distribution. In vitro of more than 99% of substance is in connected with plasma proteins states (communication mainly with albumine and lipoproteins). In the minimum concentration it can get into erythrocytes.

Experiments on animals showed what orlistat biotransformirutsya mainly in an intestinal wall. Researches in group of patients with obesity allowed to establish that about 42% of the exposed system absorption of fraction of substance are the share of 2 metabolites M1 and M3.

Molecules of metabolites have the open b-oriented lactone ring and very poorly suppress a lipase (in 1 and 2.5 thousand the orlistata, respectively is weaker). Low plasma concentration and the low inhibiting activity of M1 and M3 allow to consider products of a metabolism of an orlistat as pharmacological inactive.

And at having normal weight and at the persons having obesity drug is removed mainly by elimination of not soaked up drug with intestines contents (about 97% of the accepted dose). From them 83% in the form of an orlistat in not changed look.

Kidneys bring no more than 2% of all structurally connected with orlistaty substances.

Drug eliminirutsya completely from an organism (with excrements and urine) within 3-5 days. A ratio of ways of excretion of the people having obesity and the people having normal weight, identical.

And orlistat, and products of its metabolism can be removed with bile.

Indications to use

Drug is intended for prolonged use at patients with an excess weight, at patients with obesity, and also at the persons having the risk factors associated with obesity.

Ksenikal appoint in combination with a hypocaloric diet, sick non-insulin-dependent diabetes with obesity or excess weight with moderately limited low-calorie diet or sakharosnizhayushchy means.

Contraindications

The following contraindications to Ksenikal's use are listed in the instruction:

  • cholestatic syndrome;
  • sprue;
  • intolerance of any of components of capsules.

Side effects

It was established that the most frequent (incidence ³1/10) side effects of use of drug are reactions from a gastrointestinal tract. The pharmacological action of an orlistat interfering absorption of the fats coming to an organism with food is their reason.

These side effects were shown in a look:

  • imperative (urgent) desires on defecation;
  • release of gases (flatulention) with evacuation of a quantity of contents of intestines;
  • liquid chair;
  • oily allocations from an anus;
  • meteorism;
  • steatorrhea;
  • defecation increase;
  • discomfort and/or abdominal pains.

Frequency of emergence of the specified symptoms increases at increase of content of fat in a diet. Patients have to be informed on a possibility of development of similar reactions and are trained as it is correct to accept drug to minimize or eliminate them.

At treatment by Ksenikal very important as it is possible to keep better to the appointed diet and with special care to control contents in a fat diet.

Use of a diet with the low content of fats reduces risk of emergence of disturbances from a gastrointestinal tract and thus helps to control and regulate consumption of greasy food.

In most cases the listed above side effects were poorly expressed and had tranzitorny character. There were they generally in the first three months of treatment, and practically at all patients no more than one episode of similar reactions were noted.

Slightly less often (with a frequency of ³1/100, <1/10) were fixed:

  • discomfort and/or rectum pain;
  • abdominal distention;
  • "soft" chair;
  • incontience calla;
  • damage of gums and/or teeth.

Other side effects:

  • very frequent flu, upper respiratory tract infections, headaches;
  • frequent lower respiratory tract infections, uneasiness, a dysmenorrhea, infections of urinary tract, weakness.

At patients with non-insulin-dependent diabetes the frequency and nature of undesirable reactions were comparable to those at patients with an excess weight and obesity, but without withakharny diabetes. The only new side effects they had hypoglycemic states and abdominal distention.

Hypoglycemic states arose more, than at 2% of patients of patients with diabetes. Their incidence in comparison with placebo ³1% (the reason, most likely, improvement of compensation of carbohydrate metabolism is).

Four years' clinical trials showed that the profile of safety of Ksenikal does not differ from that, received in one - and two years' researches. The general frequency of development of undesirable effects from a gastrointestinal tract throughout the four-year period of use of drug annually decreased.

Post-marketing supervision

Today there are descriptions of cases of development of reactions of hypersensitivity which main clinical manifestations were the small tortoiseshell, a bronchospasm, an itch, an enanthesis, a Quincke's disease, an anaphylaxis.

Increase of activity of ShchF and transaminases and violent rash were in rare instances fixed. Separate (possibly serious) cases of hepatitis against treatment are also described by drug (neither pathophysiological mechanisms of development, nor relationship of cause and effect using Ksenikal were installed).

Use of drug in a combination with anticoagulants led to decrease in a prothrombin and change of haemo static parameters.

Other side effects fixed during post-marketing supervision:

  • oxalic nephropathy;
  • diverticulitis;
  • cholelithiasis;
  • pancreatitis;
  • rectal bleeding.

At administration of drug with antiepileptic means cases of development of spasms were noted.

Tablets Ksenikal, application instruction

Prolonged treatment of patients with an excess weight / obesity (including the patients having the contributing obesity factors) is carried out using 120 mg on each of the main meals. The capsule is accepted in time or within an hour (but not later!) after food.

To patients with non-insulin-dependent diabetes drug is appointed in a standard dosage 1 capsule at each meal. If in the eaten food there is no fat or the patient misses meal, Ksenikal it is possible not to accept.

How to accept drug to grow thin?

As addition to therapy of the patient has to adhere to the balanced, low-calorie diet in which kalorazh in the form of fats does not exceed 30%. A daily dose of proteins, fats and carbohydrates it is necessary to distribute on three the main reception. In a diet vegetables and fruit have to prevail.

In the application instruction of Ksenikal it is specified that increase in the recommended dose (360 mg/days) does not lead to strengthening of its therapeutic effect.

Overdose

It is authentically known that neither the single dose of 0,8 g of Ksenikal, nor a multiple dose of drug on 0,4 g of 3 rubles/day for 15 days cause essential by-effects.

Besides, there is an experience of treatment of obesity using a dose of 720 mg/days for half a year. Therapy was not followed by reliable increase in frequency of development of undesirable reactions.

In case of overdose by Ksenikal undesirable symptoms either are absent at all, or do not differ from those which are noted at reception of a therapeutic dose.

At the expressed overdose of the patient has to be under supervision within 24 hours.

The researches which were carried out on animals and people showed that any system effects associated with pharmacological properties of an orlistat have to be quickly reversible.

Interaction

Researches of medicinal interaction showed what orlistat does not enter interaction with Atorvastatit, alcohol, Digoxin, Amitriptyline, guanyl guanidines, Fluoxetine, Phenytoinum, fibrata, Lozartan, peroral contraceptives, Warfarin, Pravastatin, Phentermine, Nifedipine (the prolonged action or GITS), Sibutramin.

However at the accompanying therapy by anticoagulants in a peroral dosage form (in particular, Warfarin) it is necessary to control MNO indicators.

At a concomitant use with orlistaty absorption (according to Wikipedia, by 30%) fat-soluble vitamins decreases (β-carotene, α-tocopherol, vitamin K).

Patients to whom reception of polyvitamins was appointed should accept them at least 2 hours later after reception of capsules or before going to bed.

Orlistat promotes decrease in plasma concentration of Cyclosporine in this connection at administration of drugs in a combination it is recommended to a thicket to define concentration of the last in plasma.

Orlistat approximately on a third reduces system exposure of Amiodaronum and Dezetilamiodaron at a concomitant use of capsules with Amiodaronum in a peroral dosage form. However, as Amiodaronum has rather difficult farmakonetika, the clinical importance of such phenomenon was not succeeded to establish.

Reception of an orlistat against long therapy by Amiodaronum, most likely, will lead to decrease in efficiency of the last (researches were not conducted).

As pharmacokinetic researches of interaction of an orlistat in with Akarboza were not conducted, it is recommended to avoid use of these drugs in a combination.

At simultaneous use of drug with anticonvulsants cases of development of spasms took place.

Therapy relationship of cause and effect was not established with this phenomenon. Nevertheless, it is necessary to carry out careful monitoring of a condition of patients of rather possible changes of weight and/or frequency of a convulsive syndrome.

Terms of sale

According to the recipe.

Storage conditions

Capsules have to be stored at a temperature below 25 °C.

Period of validity

Three years.

Special instructions

Efficiency and safety of use of drug for patients with functional disorders of work of kidneys and/or a liver, and also at elderly people, were not investigated.

Means is effective in need of long control of body weight: Ksenikal promotes weight reduction and its maintenance at the new level, and also prevents a repeated set of weight.

Treatment leads to improvement of a profile of the contributing factors and pathologies accompanying obesity including non-insulin-dependent diabetes, a hypercholesterolemia, AG, a giperinsulinemiya, disturbance of tolerance to glucose, and promotes reduction of amount of visceral fat.

Using means for weight loss in combination with derivatives of a sulfonilmochevina, Metforminum and/or insulin at patients with non-insulin-dependent diabetes with IMT in the presence at them the excess weight or obesity, and also in combination with moderately limited low-calorie diet, it is possible to improve in addition compensation of carbohydrate metabolism and to reduce need for glucose-lowering drugs.

During four years' researches it was established that at most of patients of concentration of beta carotene, and also A, D, E, K vitamins remained remained within norm. To provide adequate intake of all necessary nutrients? treatment can be added with reception of polyvitamins.

It is confirmed that the additional risks concerning toxicity, reproductive toxicity, carcinogenicity, genotoxicity and a profile of safety of drug no. Researches on animals also did not reveal teratogenic action.

As teratogenic effect of drug at experimental animals is not revealed, it is possible to assume that it is improbable also at the person.

Ksenikal's analogs

Coincidence on the ATH code of the 4th level:

Structural analogs of drug are: Ksenalten, Orlistat Kanon, Allie, Orsoten, Orlimaks, Orsoten Slim.

The price of analogs of Ksenikal from 404 rub. The most inexpensive substitute of drug Orsoten Slim (capsules of 60 mg unitary enterprise. No. 42 is cost an average by 450 rub).

Body weight began to decrease within the first two weeks of treatment and continued to decrease for the next 6-12 months (including at patients with the negative response to treatment with a diet).

For 24 months statistically significant improvement of a profile of the metabolic risk factors accompanying obesity was observed. In comparison with placebo the amount of fat in an organism also considerably decreased.

Ksenikal effectively prevents a repeated set of weight: the weight increase which is not exceeding ¼ part from lost was noted approximately at 50% of patients, at the same time at a half of patients of a repeated increase of weight was not observed, and in certain cases weight continued to be lost.

Use of drug for weight loss at patients with non-insulin-dependent diabetes

Researches lasting from half a year about one year at patients with IMT more than 28 kg/sq.m showed that at the persons receiving therapy orlistaty big loss of weight in comparison with patients to whom only the medical diet was appointed is noted considerably.

Loss of weight happens mainly due to reduction of percent of fat in an organism.

It is necessary to emphasize that prior to research, despite reception of sakharosnizhayushchy means, at patients insufficient control of a hypoglycemia was quite often noted.

However against treatment drug observed clinically also statistically significant improvement of control of a hypoglycemia, reduction of an insulinrezistentnost, and also decrease in concentration of insulin and need of the patient for sakharosnizhayushchy means.

Besides, four years' clinical trials showed that Ksenikal's use allows significantly (approximately for 37% in comparison with placebo) to reduce risk of development of non-insulin-dependent diabetes. At the same time at patients with disturbance of tolerance to glucose extent of decrease in risk was even more considerable (45%).

Maintenance of weight and improvement of a profile of the contributing factors at the new level was noted throughout the entire period of researches.

Ksenikal's efficiency at pubertal obesity

In group of teenagers with obesity researches were conducted within a year. At all patients of IMT who were under supervision decreased it is more expressed, than at the patients accepting placebo.

At the patients taking medicine fat percent in an organism and diastolic pressure considerably decreased, and also the sizes of circles of a body (hips, a waist) in comparison with patients of control group who received placebo considerably decreased.

About Ksenikale for weight loss

About Ksenikale different from very good to sharply negative meet. For many side reactions and, in particular, diarrhea, dribble of contents of intestines at the time of a passage of flatus and need to use night laying were most unpleasant.

At the same time those who continued to grow thin with drug even despite side effects, note that they managed to lose weight significantly.

It should be noted what in most cases for reduction of expressiveness of side effects, was to reconsider the diet enough and whenever possible to exclude from it greasy food.

At pregnancy

Category B medicine.

In the course carried out on animals of researches of reproductive toxicity the embriotoksichesky and teratogenic effect was not revealed. However, the fact that drug did not cause disturbances of embryonic development in animals, does not mean that similar is not possible at the person.

Due to the lack of clinical data drug is not appointed to pregnant women.

Allocation of an orlistat with breast milk was not studied in this connection the feeding women are not recommended to accept Ksenikal.

About Ksenikale

Any tablets for weight loss cause disputable responses. If to see forums to which talk growing thin and grown thin it is possible to draw a conclusion that essential results can achieve only if in a complex to deal with the problem of excess weight.

Comments of doctors on Ksenikale generally good. According to specialists, an indispensable condition of success of treatment is observance by the patient of a low-fatty diet.

As a rule, within a month on drug it is possible to lose 1.5-2 kg (without special exercise stresses, only accepting Ksenikal). Responses growing thin with a photo demonstrate that weight loss process acceleration is promoted substantially by sports activities.

In that case, if to trust responses, in three months it is possible to get rid of 10-15 kg, and for half a year to dump up to 30 kg. Results, of course, depend on features of an organism and accuracy of observance of recommendations of the doctor.

It should be noted that drug has cheaper analog Orsoten (for weight loss it is accepted according to the same scheme, as Ksenikal). In Ukraine the average price of packaging of Ksenikal in which there are 21 tablets 285 UAH, in Russia Orsoten No. 21 it is possible to buy 900 rub from 560 rub.

Photos grown thin by means of Ksenikal:do_posle_ksenikala

207-355 Cost in Kharkiv, Kiev or Odessa approximately identical.

It is possible to buy Ksenikal in Moscow and in SPb from 1100 rubles (a tablet of 120 mg No. 21). Ksenikal No. 42 price 1800-2100 rub. Packaging No. 84 cost 3000-3900 rub (the cheapest way 84 pieces of drug sell in the Kremlin drugstore).

In Omsk, in Saratov, in Novosibirsk and in Barnaul the price varies from 600 to 3600 rub.

In Belarus tablets for weight loss of 120 mg No. 21 can be bought for 167.7-388.6 thousand rubles. Packaging No. 84 cost in Minsk from 394.8 to 426.1 thousand rubles.

In Kazakhstan the average price of drug 12,8 thousand.

In an Internet drugstore the price of drug is slightly lower, than in usual drugstores.

Zdravzona

  • Ksenikal of 120 mg No. 21 kapsulyroche
  • Ksenikal of 120 mg No. 42 kapsulyroche
  • Ksenikal of 120 mg No. 84 of a capsule

Drugstore of IFC

  • Ksenikal kaps 120 mg No. 84, Roche (prescription) Italy
  • Ksenikal kaps 120 mg No. 42, Roche (prescription) Italy
  • Ksenikal kaps 120 mg No. 21, Roche (prescription) Italy
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Apteka24

  • Ksenikalroche (Switzerland)

BIOSPHERE

  • Ksenikal of 120 mg No. 42 kaps.
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Section: For weight loss
PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Ksenikal surely consult with the attending physician.