Sparex 200 mg 30 pcs. extended release capsules

Nosological classification (ICD-10)

• K30 Dyspepsia
• K31.3 Pylorospasm, not elsewhere classified
• K58 Irritable bowel syndrome
• K59.8.1* Intestinal dyskinesia
• K59.9 Functional bowel disorder, unspecified
• K80.5 Bile duct stones without cholangitis or cholecystitis
• K82.8.0* Dyskinesia of the gallbladder and biliary tract
• K92.9 Disease of the digestive system, unspecified
• R10.4 Other and unspecified abdominal pain
• R52 Pain not elsewhere classified

Spark

Pharmacological properties.

Pharmacodynamics.
Mechanism of action and pharmacodynamic effects.

Spark is a myotropic antispasmodic with a selective effect on the smooth muscles of the digestive tract. It relieves spasms without inhibiting normal intestinal motility. Because this action is not mediated by the autonomic nervous system, there are no typical anticholinergic side effects.

Clinical efficacy and safety.

Significant improvements in the predominant symptoms of irritable bowel syndrome (eg, abdominal pain, stool characteristics) have generally been observed in peer-reviewed and outcome-controlled clinical studies.

All mebeverine dosage forms were generally safe and well tolerated at the recommended dosage regimen.

Children.

Clinical studies of tablets and capsules were conducted only in adults. Clinical efficacy and safety data from clinical studies, as well as post-marketing experience with mebeverine pamoate suspension in patients over 3 years of age, have demonstrated that mebeverine is an effective, safe drug that is well tolerated.

Clinical studies of mebeverine suspension have shown that it is effective in reducing the symptoms of irritable bowel syndrome in children. Further open-label, baseline-controlled studies of the mebeverine suspension confirmed the effectiveness of the drug.

The dosage regimen for tablets and capsules is 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 mebeverine, no significant accumulation occurs.

Biotransformation.

Mebeverine hydrochloride is mainly metabolized by esterases, which in the first stage of metabolism cleave ester bonds to form veratric acid and mebeverine alcohol. In plasma, demethylcarboxylic acid (DMCA) is the main metabolite. The half-life of DMKK at steady state is 5.77 hours. With repeated use of capsules (200 mg 2 times a day), Cmax of DMKK was 804 ng/ml, and tmax was about 3 hours.

The relative bioavailability of extended-release capsules was found to be optimal with an average ratio of 97%.

Excretion.

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 in the form of the corresponding carboxylic acid (CA) or demethylcarboxylic acid (DMCA).

Children.

Pharmacokinetic studies have not been conducted in children.

Compound

Sparex 200 mg 30 pcs. extended release capsules

pharmachologic effect

Antispasmodic myotropic action, has a direct effect on the smooth muscles of the gastrointestinal tract (mainly the large intestine). Eliminates spasm without affecting normal intestinal motility. Inhibits phosphodiesterase. Stabilizes the level of cyclic adenosine monodiphosphoric acid. Does not have anticholinergic effects.

Composition and release form Sparex 200 mg 30 pcs. extended release capsules

Capsules - 1 capsule:

• Active substance: mebeverine hydrochloride 200 mg.
• Excipients: colloidal silicon dioxide (Aerosil) - 5 mg, hypromellose (hydroxypropyl methylcellulose) - 38 mg, povidone K90 - 5 mg, magnesium stearate - 2 mg.
• Composition of the hard gelatin capsule: body: titanium dioxide - 1.378 mg, gelatin - 44.522 mg, quinoline yellow dye - 0.308 mg, sunset yellow dye - 0.003 mg; cap: titanium dioxide - 0.893 mg, gelatin - 28.686 mg, quinoline yellow dye - 0.199 mg, sunset yellow dye - 0.002 mg;

10 pieces. — cellular contour packages (3) — cardboard packs.

15 pcs. — contour cell packaging (2) — cardboard packs.

Description of the dosage form

Extended-release hard gelatin capsules, size No. 1, yellow; the contents of the capsules are a mixture of granules and white or almost white powder; Lumps are allowed.

Directions for use and doses

Orally for adults and children over 12 years of age, 1 capsule (200 mg) 2 times a day 20 minutes before meals (morning and evening). Swallow whole with water.

Pharmacokinetics

When taken orally, it undergoes presystemic hydrolysis and is not detected in plasma. Metabolized in the liver to veratric acid and mebeverine alcohol. It is excreted mainly by the kidneys in the form of metabolites, and in small quantities by bile. Mebeverine capsules have sustained release properties. Even after repeated administration, no significant accumulation is observed.

Indications for use Sparex 200 mg 30 pcs. extended release capsules

In adults:

• spasm of the gastrointestinal tract (including those caused by organic disease);
• intestinal colic;
• biliary colic;
• irritable bowel syndrome.

For children over 12 years of age:

• functional gastrointestinal disorders accompanied by abdominal pain.

Contraindications

• Hypersensitivity;
• porphyria;
• pregnancy;
• children under 12 years of age (due to insufficient data on effectiveness and safety).

With caution: use during lactation.

Application of Sparex 200 mg 30 pcs. extended-release capsules during pregnancy and lactation

The use of the drug is contraindicated in children under 12 years of age (due to insufficient data on effectiveness and safety).

special instructions

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: central nervous system stimulation. A specific antidote is unknown. Gastric lavage and symptomatic therapy are recommended.

Side effects of Sparex 200 mg 30 pcs. extended release capsules

Dizziness, headache, diarrhea, constipation.

Allergic reactions: urticaria, angioedema, facial swelling and exanthema.

Sparex

Sparex caps prolong 200 mg x30 ATX code: A03AA04 (Mebeverine)

Active substance: mebeverine (mebeverine) Rec.INN registered by WHO

Dosage form

SPAREX® caps. prolong. actions 200 mg: 10, 30 or 60 pcs.

reg. No.: LSR-004416/09 dated 06/04/09 - Registration period. beat is not limited

Release form, composition and packaging

Extended-release hard gelatin capsules, size No. 1, yellow, the contents of the capsules are a mixture of granules and white or almost white powder, the presence of lumps is allowed.

1 caps. mebeverine hydrochloride 200 mg

Excipients: colloidal silicon dioxide (Aerosil) - 5 mg, hypromellose (hydroxypropyl methylcellulose) - 38 mg, povidone K90 - 5 mg, magnesium stearate - 2 mg.

Composition of the hard gelatin capsule: body: titanium dioxide - 1.378 mg, gelatin - 44.522 mg, quinoline yellow dye - 0.308 mg, sunset yellow dye - 0.003 mg, cap: titanium dioxide - 0.893 mg, gelatin - 28.686 mg, quinoline yellow dye - 0.199 mg, sunset yellow dye - 0.002 mg,

10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (6) — cardboard packs. 15 pcs. — contour cell packaging (2) — cardboard packs. 15 pcs. — contour cell packaging (4) — cardboard packs.

Clinical and pharmacological group: Myotropic antispasmodic

Pharmacotherapeutic group: Antispasmodic agent

Indications

In adults: - spasm of the gastrointestinal tract (including those caused by organic disease),

- intestinal colic,

- biliary colic,

- irritable bowel syndrome.

For children over 12 years of age:

- functional gastrointestinal disorders accompanied by abdominal pain.

Dosage regimen

Orally for adults and children over 12 years of age, 1 capsule (200 mg) 2 times a day 20 minutes before meals (morning and evening). Swallow whole with water.

Side effect

Dizziness, headache, diarrhea, constipation.

Allergic reactions: urticaria, angioedema, facial swelling and exanthema.

Contraindications for use

- hypersensitivity,

- porphyria,

- pregnancy,

- children under 12 years of age (due to insufficient data on effectiveness and safety).

With caution: use during lactation.

Use in children

The use of the drug is contraindicated in children under 12 years of age (due to insufficient data on effectiveness and safety).

special instructions

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: central nervous system stimulation. A specific antidote is unknown. Gastric lavage and symptomatic therapy are recommended.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored in a dry place, protected from light and out of reach of children, at a temperature not exceeding 25°C. Shelf life: 2 years.

Do not use after the expiration date.

Sparex 135 mg 30 pcs. film-coated tablets

pharmachologic effect

Antispasmodic.

Composition and release form Sparex 135 mg 30 pcs. film-coated tablets

Tablets - 1 tablet:

• Active ingredient: mebeverine hydrochloride 135.00 mg;
• excipients: potato starch 42.00 mg, lactose monohydrate 88.00 mg, magnesium stearate 5.50 mg, methylcellulose 16.00 mg, talc 6.50 mg, microcrystalline cellulose type 102 7.00 mg;
• composition of the film shell: Opadry 11 yellow (851732410) 21,000 mg, including: polyvinyl alcohol 8,400 mg, macrogol-4000 (polyethylene glycol-4000) 4,242 mg. talc 3.108 mg. titanium dioxide 4.935 mg, iron dye yellow oxide 0.315 mg.

Film-coated tablets, 135 mg.

10 or 15 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

3, 5, 6, 9 blister packs of 10 tablets each or 2, 4, 6 blister packs of 15 tablets each, together with instructions for use, are placed in a cardboard pack.

Description of the dosage form

The tablets are round, biconvex, yellow film-coated. On a cross section it is almost white.

Directions for use and doses

For oral administration.

The tablets must be swallowed without chewing, washed down with a sufficient amount of water (at least 100 ml).

One tablet 3 times a day, approximately 20 minutes before meals.

The duration of taking the drug is not limited.

If the patient forgets to take one or more doses, the drug should be continued with the next dose. Do not take one or more missed doses in addition to your regular dose.

Dosing regimen studies have not been conducted in elderly patients or patients with renal and/or hepatic impairment. Available data on post-marketing use of the drug have not identified specific risk factors for its use in elderly patients and patients with renal and/or hepatic insufficiency. No changes to the dosage regimen are required in elderly patients and patients with renal and/or hepatic impairment.

Pharmacodynamics

Antispasmodic myotropic action, has a direct effect on the smooth muscles of the gastrointestinal tract without affecting normal intestinal motility.

The exact mechanism of action is unknown, but multiple mechanisms such as decreased ion channel permeability, blockade of norepinephrine reuptake, local anesthetic effects, and changes in water absorption may cause local effects of mebeverine on the gastrointestinal tract. Through these mechanisms, mebeverine exhibits an antispasmodic effect, normalizing intestinal motility and not causing constant relaxation of smooth muscle cells of the gastrointestinal tract (“hypotension”).

There are no systemic side effects, including anticholinergic ones.

Pharmacokinetics

Suction

Mebeverine is rapidly and completely absorbed after oral administration.

Distribution

When taking repeated doses of the drug, significant accumulation does not occur.

Metabolism

Mebeverine hydrochloride is mainly metabolized by esterases, which in the first stage split the ester into veratric acid and mebeverine alcohol. The main metabolite circulating in plasma is demethylated carboxylic acid.

The half-life at steady state of demethylated carboxylic acid is approximately 2.45 hours. When taking repeated doses, the maximum concentration of demethylated carboxylic acid in the blood (Cmax) is 1670 ng/ml, the time to reach the maximum concentration of demethylated carboxylic acid in the blood (Tmax) is 1 hour .

Removal

Mebeverine as such is not excreted from the body, but is completely metabolized; its metabolites are almost completely eliminated from the body. Veratric acid is eliminated at night. Mebeverine alcohol is also excreted by the kidneys, partly as a carboxylic acid and partly as a demethylated carboxylic acid.

Indications for use Sparex 135 mg 30 pcs. film-coated tablets

Symptomatic treatment of pain, spasms, dysfunction and intestinal discomfort associated with irritable bowel syndrome.

Symptoms may include: abdominal pain, cramping, feeling of bloating and flatulence, change in stool frequency (diarrhea, constipation or alternating diarrhea and constipation), change in stool consistency.

Contraindications

• Hypersensitivity to any component of the drug;
• Age up to 18 years;
• Congenital intolerance to galactose (lactose) or fructose, lactase deficiency, sucrase/isomaltase deficiency, glucose-galactose malabsorption syndrome;
• Pregnancy and breastfeeding period.

Application of Sparex 135 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding

Pregnancy

There are only very limited data on the use of mebeverine in pregnant women. Animal data are insufficient to assess reproductive toxicity. It is not recommended to use mebeverine during pregnancy.

Breastfeeding period

There is insufficient information on the excretion of mebeverine or its metabolites into breast milk. Studies of the excretion of mebeverine into milk in animals have not been conducted. Mebeverine should not be taken while breastfeeding.

Fertility

There are no clinical data on the effect of the drug on fertility in men or women, but known animal studies have not demonstrated any adverse effects of mebeverine.

special instructions

Before taking Sparex®, you should consult your doctor if:

• if symptoms of the disease occur for the first time;
• unintentional and unexplained weight loss;
• anemia;
• rectal bleeding or blood in the stool;
• fever;
• if anyone in your family has been diagnosed with colon cancer, celiac disease or inflammatory bowel disease;
• over 50 years of age and if symptoms of the disease appeared for the first time;
• recent use of antibiotics.

Contact your doctor if your condition worsens while taking the drug or if your symptoms do not improve after 2 weeks of use.

Impact on the ability to drive vehicles and operate machinery

Studies of the effect of the drug on the ability to drive a car and other mechanisms have not been conducted. The pharmacological properties of the drug, as well as the experience of its use, do not indicate any adverse effect of mebeverine on the ability to drive a car and other mechanisms.

Overdose

In case of overdose with Sparex®, you should immediately consult a doctor.

Symptoms: theoretically, in case of overdose, an increase in the excitability of the central nervous system is possible. In cases of mebeverine overdose, symptoms were either absent or mild and, as a rule, quickly reversible. The observed symptoms of overdose were neurological and cardiovascular in nature.

Treatment: specific antidote is unknown. Symptomatic treatment is recommended. Gastric lavage is necessary only if intoxication is detected within approximately one hour after taking several doses of the drug. Measures to reduce the level of absorption are not required.

Side effects of Sparex 135 mg 30 pcs. film-coated tablets

Reports of these side effects were spontaneous, and there is insufficient data to accurately estimate the incidence of cases.

Allergic reactions were observed mainly from the skin, but other manifestations of allergies were also noted.

Skin and subcutaneous tissue disorders

Urticaria (allergic rash), angioedema (serious allergic reaction which may include: difficulty breathing, swelling of the face, neck, lips, tongue, throat), facial swelling, exanthema (skin rash).

Immune system disorders

Hypersensitivity reactions (anaphylactic reactions are serious allergic reactions that may include: difficulty breathing, rapid pulse, sudden decrease in blood pressure (weakness and dizziness), sweating).

If you experience any side effects, including those not listed in these instructions, stop taking Sparex® and consult your doctor immediately!

Drug interactions

Only studies have been conducted on the interaction of this drug with alcohol. Animal studies have demonstrated the absence of any interaction between mebeverine and ethyl alcohol.