Instructions for Duspatalin Retard 200 mg hard capsules of prolonged action No. 30
Composition
active ingredient: mebeverine hydrochloride;
1 capsule contains mebeverine hydrochloride 200 mg;
excipients: magnesium stearate, methacrylate copolymer dispersion, talc, hypromellose, polyacrylate dispersion, glycerol triacetate;
hard gelatin capsule (size No. 1): titanium dioxide (E 171), gelatin.
Dosage form
Extended-release capsules, hard.
Main physicochemical properties: opaque white hard gelatin capsules, size No. 1, with corresponding marking 245, containing white to almost white granules.
Pharmacotherapeutic group
Drugs used in functional gastrointestinal disorders. Synthetic anticholinergics, esterified tertiary amines. Mebeverine. ATC code A0ZA A04.
Pharmacological properties
Pharmacodynamics.
Mechanism of action and pharmacodynamic effects.
Mebeverine is a myotropic antispasmodic with selective action on the smooth muscles of the digestive tract. It eliminates spasms without inhibiting normal intestinal motility. Since this action is not mediated by the autonomic nervous system, there are no typical anticholinergic side effects.
Clinical efficacy and safety.
The clinical efficacy and safety of different dosage forms of mebeverine have been studied in over 1500 patients. Significant relief of the predominant symptoms of irritable bowel syndrome (such as abdominal pain, bowel habits) has generally been observed in reference and baseline-controlled clinical trials.
All formulations of mebeverine were generally safe and well tolerated at the recommended dosage regimen.
Children.
Clinical studies with the tablets or capsules have been conducted only in adults. Clinical efficacy and safety data from clinical trials and post-marketing experience with mebeverine pamoate suspension in patients 3 years of age and older have demonstrated that mebeverine is an effective, safe, and well-tolerated drug.
Clinical trials of mebeverine suspension have shown that the drug is effective in reducing the symptoms of irritable bowel syndrome in children. Further open-label, baseline-controlled studies of mebeverine suspension have confirmed the drug's efficacy.
The dosage regimen of the drug in tablet or capsule form is determined based on the safety and tolerability of mebeverine.
Pharmacokinetics.
Absorption.
Mebeverine is rapidly and completely absorbed after oral administration in tablet form. Due to the prolonged release of the drug from the capsule, it can be taken twice a day.
Distribution.
With repeated use of Duspatalin® Retard 200, no significant cumulation occurs.
Biotransformation.
Mebeverine hydrochloride is mainly metabolized by esterases, which in the first stage of metabolism cleave the ester bonds with the formation of veratric acid and mebeverine alcohol. In plasma, demethylcarboxylic acid (DMCA) is the main metabolite. The half-life of DMCA at steady state is 5.77 hours. With multiple use of capsules (200 mg 2 times a day), Cmax for DMCA was 804 ng/ml, and tmax was about 3 hours. The relative bioavailability of the prolonged-release capsules was optimal with an average ratio of 97%.
Breeding.
Mebeverine is not excreted unchanged, it is completely metabolized, and the metabolites are excreted almost completely. Veratric acid is excreted in the urine. Mebeverine alcohol is also excreted by the kidneys partly as the corresponding carboxylic acid (CC) and partly as demethylcarboxylic acid (DMCC).
Children.
Pharmacokinetic studies in children have not been conducted.
Indication
Adults and children aged 10 and over:
symptomatic treatment of abdominal pain and cramps, intestinal disorders and discomfort in the intestinal area in irritable bowel syndrome;
treatment of gastrointestinal spasms of secondary genesis caused by organic diseases.
Contraindication
Hypersensitivity to the active substance or to any of the excipients of the drug listed in the "Composition" section.
Interaction with other medicinal products and other types of interactions
Interaction studies have not been conducted, except for the interaction with alcohol. In vitro and in vivo animal studies have demonstrated the absence of any interaction between Duspatalin® Retard 200 and ethanol.
Application features
None.
Use during pregnancy or breastfeeding
Pregnancy
There are only very limited data on the use of mebeverine in pregnant women. Animal reproductive toxicity studies are insufficient. Duspatalin® Retard 200 is not recommended for use during pregnancy.
Breast-feeding
It is not known whether mebeverine or its metabolites are excreted in human breast milk. The excretion of mebeverine in animal breast milk has not been studied. Duspatalin® Retard 200 should not be used during breastfeeding.
There are no clinical data on the effect on male or female fertility, however, data from available animal studies do not indicate a harmful effect of Duspatalin® Retard 200.
Ability to influence reaction speed when driving vehicles or other mechanisms
No studies on the effects on the ability to drive and use machines have been conducted. The pharmacodynamic and pharmacokinetic profile, as well as post-marketing experience, do not indicate any harmful effects of mebeverine on the ability to drive and use machines.
Method of administration and doses
For oral use.
The capsules should be taken with sufficient water (at least 100 ml). It is not recommended to chew them as the capsule coating is designed to provide a prolonged release mechanism.
Adults and children over 10 years of age should take 1 capsule 2 times a day (morning and evening).
The duration of use is not limited. If one or more doses are missed, the patient should take the next dose as prescribed. The missed dose(s) should not be taken in addition to the regular dose.
Special populations.
No dosage studies have been conducted in the elderly, patients with renal and/or hepatic impairment. Based on available post-marketing data, no specific risk has been identified in the elderly, patients with renal and/or hepatic impairment. No dose adjustment is considered necessary for these patient groups.
Children
Duspatalin® Retard 200 should not be used in children under 3 years of age due to the lack of clinical data for this age group. Duspatalin® Retard 200, 200 mg capsules, should not be used in children aged 3 to 10 years due to the high content of the active substance.
Overdose
Symptoms: Theoretically, central nervous system excitation is possible in case of overdose. In cases of overdose, symptoms were absent or mild and usually resolved quickly. The symptoms of overdose that were observed were of neurological or cardiovascular origin.
Treatment. Specific antidote is unknown. Symptomatic treatment is recommended. Gastric lavage is recommended only in case of intoxication with multiple drugs, which is diagnosed within 1 hour from the moment of taking the drugs. Measures to reduce absorption are not necessary.
Side effects
The following adverse reactions have been reported spontaneously during post-marketing use. The frequency cannot be estimated from the available data.
Allergic reactions were observed predominantly, but not exclusively, on the skin.
Skin and subcutaneous tissue disorders:
urticaria, angioedema, facial swelling, rash.
Immune system disorders:
hypersensitivity (anaphylactic reactions).
Expiration date
3 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C. Do not store at a temperature below 5 ° C. Keep out of the reach of children.
Packaging
10 capsules in a blister, 3 blisters in a cardboard box or 15 capsules in a blister, 1 or 2, or 4 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Mylan Laboratories SAS.
Address
Route de Belleville, Lieu dit Maillard, 01400, Chatillon-sur-Chalaronne, France.
