Expiration date: 03/2026
Tablets coated with a film shell of white or almost white color, round, with an engraving "100" on one side and smooth on the other; on the cross section there is a core from white to light yellow.
1 tablet contains:
acotiamide (in the form of acotiamide hydrochloride hydrate) 100 mg
Excipients: microcrystalline cellulose (type 101), lactose monohydrate - 27 mg, sodium starch glycolate (type A), hyprolose, silicon dioxide colloidal, magnesium stearate; film shell Opadray white Y-1-7000 (hypromellose 2910, titanium dioxide, macrogol 400).
10 pcs. - contour cell packages (5) - cardboard packs.
10 pcs. - contour cell packages (9) - cardboard packs.
Clinical and pharmacological group: A drug that increases the tone and motility of the gastrointestinal tract. Acetylcholinesterase inhibitor
Pharmacotherapeutic group: Gastrointestinal motility stimulants
Pharmacological action
The active ingredient of the drug Dyspevict is acotiamide. By suppressing the activity of acetylcholinesterase, acotiamide enhances gastric motility and accelerates the process of gastric emptying.
Acotiamide demonstrated inhibition of acetylcholinesterase activity (in vitro) and enhancement of postprandial motility of the antrum of the stomach in dogs and rats. In addition, the drug reduces the severity of the clonidine-induced decrease in the motility of the antrum of the stomach in dogs and rats. Acotiamide has been shown to accelerate delayed gastric emptying induced by clonidine in rats.
Clinical efficacy and safety
The duration of application is 4 weeks
A randomized, double-blind, placebo-controlled phase III trial evaluated the efficacy of acotiamide in patients with functional dyspepsia. Patients took placebo (n=442) or acothiamide orally daily at a dose of 100 mg (n=450) 3 times / day before meals for 28 days. After the end of taking acotiamide, patients underwent a follow-up period lasting another 28 days. The primary endpoints of effectiveness were "the degree of improvement in the patient's overall impression at the last assessment time during treatment" and "the degree of elimination of three symptoms (feeling full in the stomach after eating, bloating and early satiation) at the time of the last assessment during treatment." If there was a statistically significant difference between the indicators of patients taking acotiamide at a daily dose of 300 mg and patients taking placebo at both primary endpoints, it was believed that the effectiveness of acotiamide exceeded the effectiveness of placebo.
Statistically significant differences were observed between the indicators of patients taking acotiamide at a daily dose of 300 mg and those of patients taking placebo at both main endpoints (p< 0.001 and p=0.004, respectively; Fisher's exact criterion, bilateral significance level of 5%).
The duration of application is 28 weeks
In a long-term use study, the "participant assessment improvement rate" was 48.9% (193 of 395 remaining participants) at week 4 and 48.9% (69 of 141 remaining participants) at week 24. Twenty-two of the total 405 patients continued to receive the drug without interruption for up to 24 weeks. In addition, 75.1% (304/405 cases) of patients stopped treatment because the effect was achieved, among them 50.7% (154/304 cases) retained symptom relief for 12 weeks, and the use of this drug was also discontinued.
Pharmacokinetics
Suction
Pharmacokinetic parameters after a single oral administration of 100 mg of acotiamide: Tmax is 2.42±0.97 h, Cmax in serum is 30.82±13.3 ng /ml, AUC0-∞ - 171.3±59.43 ng×h/ml, T1/2 - 13.31±6.91 h.
Pharmacokinetic parameters after repeated oral administration of 100 mg of acotiamide 1 tablet 3 times / day for 9 days: Css in blood plasma is achieved, as a rule, with the third dose taken on day 3. In addition, with repeated administration, its pharmacokinetics does not change.
The effect of food intake on the absorption of the drug
In a study of the effect of food intake on the pharmacokinetics of the drug, it was found that the maximum Cmax value of acotiamide is achieved when taking the drug before a meal, and the minimum value is achieved when taking the drug after a meal.
Distribution
It was shown that the degree of binding of acotiamide to human plasma proteins, measured in vitro by equilibrium dialysis and amounting to approximately 84.21-85.95%, is comparable to the degree of binding to human serum albumin, which was approximately 82.64-85.1%. Thus, the main binding protein of acotiamide is albumin.
Metabolism
After ingestion of a solution of radioactively labeled acotiamide (600 mg / 103 MCI) on an empty stomach by 6 healthy adult men, 60% of the radioactivity in blood plasma was accounted for by the unchanged drug.
With the participation of the isoenzymes CYP2C8, CYP1A1 or CYP3A4, acotiamide is metabolized to deisopropyl. In addition, based on an in vitro analysis of metabolism using the human microsomal enzyme uridine diphosphate glucuronyltransferase (UGT) expression system, it can be assumed that the drug is metabolized to form a conjugate of unchanged acotiamide with glucuronic acid with the participation of UGT1A8 or UGT1A9 isoenzymes.
Elimination
It was noted that 92.7% of the dose of acotiamide is excreted through the intestine and 5.3% is excreted by the kidneys.
Indications of the drug Dyspevict
in case of functional dyspepsia in adults aged 18 and over, to eliminate the following symptoms:
- feelings of overflow in the stomach after eating;
- bloating of the upper abdomen;
- feelings of early satiety.
Dosage regimen
Take orally, before meals, 1 tablet (100 mg) 3 times / day. Tablets should be swallowed whole, without chewing, with water.
If there is no improvement in symptoms 1 month after the start of acotiamide therapy, discontinuation of its use should be considered. If symptoms of dyspepsia persist, the possibility of an organic disease should be considered and, if necessary, in addition to gastroduodenoscopy, other examinations should be performed.
If there is a steady improvement in symptoms, discontinuation of treatment should also be considered. Acotiamide should not be used for a long period of time without medical supervision.
Elderly patients
Acotiamide should be used with caution in elderly patients who often have decreased kidney and/or liver function. If deviations from the norm are detected, appropriate measures should be taken, for example, the use of acotiamide should be suspended.
Children
The safety and efficacy of acotiamide in children aged 0 to 18 years have not been established at the moment. There is no data available.
Side effect
In clinical studies of acotiamide, the following adverse reactions were identified, the frequency of which was assessed based on the following criteria: very often (≥1/10); often (≥1/100, <1/10); infrequently (≥1/1000, <1/100); rarely (≥1/10000, <1/1000); very rarely (<1/10000); the frequency is unknown (it is impossible to estimate based on the available data).
Systemic organ class Frequency of adverse reactions
On the part of the gastrointestinal tract, Diarrhea, constipation are common
Infrequently Nausea, vomiting, abdominal pain
From the skin and subcutaneous tissues, Skin rash, urticaria are infrequent
Laboratory and
instrumental
These data Often Increase the concentration of prolactin, increase the concentration of TG, increase the activity of ALT, AST, GGT
Infrequently, an increase in the number of white blood cells, an increase in the concentration of bilirubin, an increase in the concentration of alkaline phosphatase
Contraindications to use
hypersensitivity to the active substance or to any of the excipients.
Use during pregnancy and lactation
Pregnancy
The use of acotiamide during pregnancy is contraindicated due to the lack of clinical data on the safety and effectiveness of its use in pregnant women.
Breastfeeding period
The use of acotiamide during breastfeeding is contraindicated. Preclinical studies have established that acotiamide penetrates into breast milk.
Fertility
There is no information about the effect of acotiamide on human fertility. In preclinical studies, the negative effect of the drug on fertility and general reproductive function has not been revealed.
Use in children
The safety and efficacy of acotiamide in children aged 0 to 18 years have not been established at the moment.
Use in elderly patients
Acotiamide should be used with caution in elderly patients who often have decreased kidney and/or liver function.
Special instructions
The effectiveness of acotiamide in epigastric pain and heartburn in functional dyspepsia has not been confirmed.
Before using acotiamide, it is necessary to exclude the presence of an organic lesion, including a malignant neoplasm such as stomach cancer.
Concomitant use of acotiamide with other cholinergic agents should be avoided.
The safety of acotiamide when used concomitantly with other prokinetic agents has not been established.
Influence on the ability to drive vehicles and mechanisms
Studies on the effect of acotiamide on the ability to drive vehicles and work with mechanisms have not been conducted. During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms: no cases of acotiamide overdose have been reported. The maximum daily dose of acotiamide in clinical trials was 900 mg. Against the background of taking acotiamide at this dose, no unexpected adverse reactions were noted, and all identified adverse reactions were similar in frequency and severity to those observed in patients from the placebo group. The effects of taking acotiamide in higher doses are unknown.
Treatment: withdrawal of the drug, gastric lavage and symptomatic therapy. There are no specific antidotes.
Drug interaction
Since nicotinamide has an inhibitory effect on acetylcholinesterase, when combined with drugs with anticholinergic effects (atropine, butylskopolamine), the effect of acotiamide decreases.
Since M-cholinomimetics, acetylcholinesterase inhibitors (acetylcholine, neostigmine) and acotiamide have a unidirectional effect, when used together, the effect of both acotiamide and concomitant drugs will be enhanced.
Storage conditions of the drug Dyspevict
The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C.
Shelf life of the drug Dyspevict
The shelf life is 3 years.
