Spark

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT SPARK® (SPARK)

Composition:

Active substance: 1 capsule contains meparverine hydrochloride, pellets calculated as meparverine hydrochloride 200 mg;

Excipients in the pellet composition: spherical sugar, povidone, shellac, talc, methacrylic acid copolymer dispersion;

Capsule shell composition: gelatin, titanium dioxide (E 171).

Pharmaceutical form. Prolonged-release hard capsules.

Main physicochemical properties: hard gelatin capsules. The body of the capsule is transparent, the cap is white. The capsule contents are granules (pellets) of almost white color, spherical in shape.

Pharmacotherapeutic group. Drugs used in functional gastrointestinal disorders. Synthetic anticholinergic agents, esterified tertiary amines.

ATC code A03A A04.

Pharmacological Properties.

Pharmacodynamics.

Mechanism of action and pharmacodynamic effects.

Sparc® is a myotropic spasmolytic with selective action on smooth muscles of the gastrointestinal tract. It relieves spasms without suppressing normal intestinal motility. Since this action is not mediated via the autonomic nervous system, typical anticholinergic side effects do not occur.

Clinical efficacy and safety.

Significant relief of the main symptoms of irritable bowel syndrome (e.g., abdominal pain, characteristics of bowel movements) was generally observed in reference and placebo-controlled clinical trials.

All dosage forms of mebeverine have been generally safe and well tolerated at the recommended dosage regimen.

Children.

Clinical studies of tablets and capsules were conducted only in adults. Data on clinical efficacy and safety from clinical trials, as well as post-marketing experience with mebeverine pamotate suspension in patients aged 3 years and older, have demonstrated that mebeverine is an effective, safe medication that is well tolerated.

Clinical studies of mebeverine suspension have shown it to be effective in relieving symptoms of irritable bowel syndrome in children. Further open-label, baseline-controlled studies of mebeverine suspension have confirmed the efficacy 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 administered twice daily.

Distribution.

With repeated administration of mebeverine, no significant accumulation occurs.

Biotransformation.

Mebeverine hydrochloride is mainly metabolized by esterases, which in the first stage of metabolism cleave the ester bonds, forming 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 repeated administration of capsules (200 mg twice daily), the Cmax of DMCA was 804 ng/mL and tmax was approximately 3 hours. The relative bioavailability of the prolonged-release capsules was found to be optimal, with a mean ratio of 97%.

Elimination.

Mebeverine is not excreted unchanged; it is completely metabolized, and metabolites are excreted almost entirely. Veratric acid is excreted in urine. Mebeverine alcohol is also excreted by the kidneys, partially as the corresponding carboxylic acid (CA) and partially as demethylcarboxylic acid (DMCA).

Children.

Pharmacokinetic studies in children have not been conducted.

Clinical characteristics.

Indications.

Adults and children aged 10 years and older:

• symptomatic treatment of abdominal pain and spasms, gastrointestinal disorders and discomfort in the intestinal area in irritable bowel syndrome;
• treatment of secondary gastrointestinal spasms caused by organic diseases.

Contraindications.

Hypersensitivity to the active substance or to any of the excipients.

Interaction with other medicinal products and other forms of interaction.

Interaction studies have not been conducted, except for interaction with alcohol. In vitro and in vivo studies in animals have demonstrated the absence of any interaction between mebeverine hydrochloride and ethanol.

Special precautions for use.

If you have an intolerance to certain sugars, consult your doctor before taking this medicinal product.

Use during pregnancy or breastfeeding.

Pregnancy

There are only very limited data on the use of mebeverine in pregnant women. Reproductive toxicity studies in animals are insufficient. Mebeverine hydrochloride is not recommended for use during pregnancy.

Breastfeeding

It is unknown whether mebeverine or its metabolites are excreted in human breast milk. Excretion of mebeverine in the milk of animals has not been studied. Spark® should not be used during breastfeeding.

Fertility

There are no clinical data on the effect on male or female fertility; however, animal studies do not indicate harmful effects of mebeverine.

Ability to influence reaction speed when driving or operating machinery.

Studies on the influence of mebeverine on the ability to drive or operate machinery have not been conducted. However, the pharmacodynamic and pharmacokinetic profile, as well as post-marketing experience, do not indicate any harmful effect on the ability to drive or operate machinery.

Dosage and Administration.

For oral use.

Swallow the capsules with sufficient amount of water (not less than 100 ml). Chewing is not recommended due to the capsule coating designed to ensure prolonged release.

Adults and children aged 10 years and older should take 1 capsule twice daily (in the morning and evening).

Duration of use is not limited. If one or more doses are missed, the patient should take the next dose as prescribed. Missed dose(s) should not be taken additionally.

Special populations.

Dosage studies in elderly patients and patients with impaired renal and/or hepatic function have not been conducted. Based on available post-marketing data, no specific risk has been identified in elderly patients or patients with impaired renal and/or hepatic function. Dose adjustment in the above-mentioned patient groups is not considered necessary.

Children.

Sparq® should not be used in children under 3 years of age due to lack of clinical data in this age group. Sparq® 200 mg capsules should not be used in children aged 3 to 10 years due to the high content of active substance.

Overdose.

Symptoms. In cases of overdose, central nervous system stimulation may occur. In cases of mebeverine overdose, symptoms were absent or mild and rapidly disappeared. Observed symptoms of overdose were of neurological or cardiovascular origin.

Treatment. No specific antidote is known. Symptomatic treatment is recommended. Gastric lavage is recommended only in cases of intoxication with multiple drugs within 1 hour after drug intake. Measures to reduce absorption are not necessary.

Side effects

The adverse reactions listed below have been reported during post-marketing use. Due to the nature of the data, the frequency of these reactions cannot be accurately determined.

Allergic reactions were observed predominantly, but not exclusively, affecting the skin.

Skin and subcutaneous tissue disorders: urticaria, angioneurotic edema, facial swelling, rash.

Immune system disorders: hypersensitivity (anaphylactic reactions).

Shelf life. 2 years.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 10 capsules in a blister pack. 3 or 5 blisters per carton.

Prescription status. Prescription only.

Manufacturer: JSC "Farmak".

Manufacturer's name and address of the place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.