Duspatalin

Duspatalin (mebeverine) is a drug used to relieve symptoms of irritable bowel syndrome (IBS) and other gastrointestinal disorders associated with smooth muscle hypertonicity.

Mebeverine works by blocking calcium channels in the smooth muscles of the intestine, causing them to relax. This helps reduce spasms, reduce pain, and improve intestinal permeability.

Duspatalin is usually taken orally in tablet or capsule form. It is usually taken before meals or as needed as directed by a doctor.

Indications Duspatalina

1. Abdominal pain and discomfort associated with irritable bowel syndrome (IBS).
2. Intestinal spasms and colic-like pain.
3. Incomplete bowel movement and other symptoms associated with bowel dysfunction.

Release form

Duspatalin is usually available as tablets or capsules for oral administration.

Pharmacodynamics

1. Mechanism of action:

   • Selective antispasmodic action: Mebeverine selectively relaxes the smooth muscles of the intestine without significantly affecting normal intestinal peristalsis. This allows for the reduction of spasms and associated pain without disrupting normal motor function.
   • Sodium channel blocking: Mebeverine blocks sodium channels in the cell membranes of smooth muscle cells, which results in membrane stabilization and prevents uncontrolled sodium entry into the cells. This prevents depolarization and subsequent contraction of smooth muscle.
   • Antispasmodic action: The drug reduces increased tone and hypermotor activity of intestinal smooth muscles, which helps relieve symptoms such as pain, spasms and abdominal discomfort.

2. Effects on the gastrointestinal tract:

   • Reduction of pain and discomfort: By relaxing the smooth muscles of the intestine, mebeverine helps reduce pain and discomfort associated with functional bowel disorders.
   • No effect on normal motility: Unlike some other antispasmodics, mebeverine does not suppress normal intestinal motility, which avoids side effects such as constipation or slow intestinal transit.

3. Clinical effects:

   • Improved patient condition: Mebeverine is effective in the treatment of irritable bowel syndrome (IBS) and other functional gastrointestinal disorders. Patients report reduced pain, reduced spasms, and improved overall well-being.

4. Advantages:

   • Minimal systemic effects: Due to its selective action on intestinal muscles, mebeverine has minimal systemic side effects, making it safe for long-term use.
   • No anticholinergic effects: Mebeverine does not have anticholinergic properties, so it does not cause side effects such as dry mouth, blurred vision or urinary retention, which are typical for some other antispasmodics.

Pharmacokinetics

1. Suction:

   • Following oral administration, mebeverine is rapidly and completely absorbed from the gastrointestinal tract. Modified release formulations such as capsules provide prolonged release of the active substance, which helps maintain stable plasma levels.

2. Distribution:

   • Mebeverine is well distributed in tissues, especially in the smooth muscles of the intestine, where it exerts its effect.
   • Plasma protein binding is approximately 75%, indicating moderate protein binding.

3. Metabolism:

   • Mebeverine undergoes extensive metabolism in the liver via hydrolysis of esters, forming veratric acid and mebeverine alcohol.
   • The main metabolites do not have pharmacological activity, which minimizes the risk of systemic side effects.

4. Withdrawal:

   • Mebeverine metabolites are excreted primarily by the kidneys. Approximately 60% of the metabolites are excreted in the urine as carboxylic acids and their glucuronides.
   • Some of the metabolites may be excreted in the bile.

5. Half-life:

   • The half-life of mebeverine and its metabolites is approximately 5-6 hours, allowing the drug to be taken twice daily when using modified-release capsules.

Special instructions:

• Elderly patients and patients with impaired renal or hepatic function:
  • No dosage adjustment is necessary for elderly patients or patients with renal or hepatic impairment, making mebeverine suitable for use in these patient groups.
• Food interactions:
  • Food intake does not significantly affect the absorption of mebeverine, but it is recommended to take the drug 20 minutes before meals to achieve the best therapeutic effect.

Dosing and administration

Recommended doses and methods of administration depend on the form of release.

Extended release capsules (200 mg):

• Suggested Dose: One capsule (200 mg) twice daily.
• Directions for use: Take the capsules whole, without chewing, with a sufficient amount of water (at least half a glass). It is recommended to take the capsules 20 minutes before meals (morning and evening).

Tablets (135 mg):

• Recommended dose: One tablet (135 mg) three times daily.
• Directions for use: Tablets should be taken whole with sufficient amount of water. It is recommended to take tablets 20 minutes before meals.

General recommendations:

1. Duration of treatment:

   • The duration of the course of treatment is determined by the doctor individually, depending on the patient’s condition and his response to treatment.
   • Treatment may be continued until a sustained improvement in the condition is achieved, after which a gradual reduction in the dose is recommended.

2. Missed dose:

   • If you miss a capsule or tablet, take it as soon as possible. If it is almost time for your next dose, do not double the dose, just continue taking the medicine as usual.

3. Discontinuation of treatment:

   • The drug can be stopped gradually to avoid possible relapse of symptoms. It is recommended to consult a doctor about gradual reduction of the dose.

Special instructions:

• Patients with renal or hepatic impairment: No dosage adjustment is required.
• Elderly patients: No dosage adjustment is required.
• Pregnant and lactating women: Use of the drug should be agreed with a doctor.

Approximate schedule of admission:

Extended release capsules:

• In the morning: 1 capsule 20 minutes before breakfast.
• In the evening: 1 capsule 20 minutes before dinner.

Pills:

• In the morning: 1 tablet 20 minutes before breakfast.
• During the day: 1 tablet 20 minutes before lunch.
• In the evening: 1 tablet 20 minutes before dinner.

Use Duspatalina during pregnancy

The question of its safety when used during pregnancy is important to prevent possible risks to the mother and fetus.

Efficiency and safety

1. Treatment of functional gastrointestinal disorders: Studies show that Duspatalin is effective in the treatment of postcholecystectomy gastrointestinal spasms. It reduces the symptoms of abdominal pain and dyspepsia, normalizes the frequency and consistency of stool, which improves the quality of life of patients (Maev et al., 2018).
2. Effects on the kidneys and fetus: A study in white rats showed that mebeverine can cause histological changes in the kidneys of pregnant rats and their fetuses when used for a long time during pregnancy. These findings highlight the need for caution and consultation with a physician before use (Al-Essawi et al., 2022).
3. Metabolism and stability: Mebeverine is rapidly metabolized in the body, making it almost undetectable in plasma. The main metabolites of mebeverine include desmethylmebeveric acid (DMAC) and other derivatives that may influence the pharmacological effect of the drug (Moskaleva et al., 2019).

Contraindications

Absolute contraindications:

1. Hypersensitivity:

   • Hypersensitivity or allergy to mebeverine or any other component of the drug. If the patient has previously had allergic reactions to this drug, its use is strictly contraindicated.

2. Age under 18:

   • The drug is not recommended for use in children and adolescents under 18 years of age, as safety and efficacy data for this age group are limited.

Relative contraindications:

1. Pregnancy and lactation:

   • Pregnancy: Use of mebeverine during pregnancy is possible only in case of extreme necessity and under strict medical supervision. Data on the safety of the drug in pregnant women are limited.
   • Lactation: It is unknown whether mebeverine is excreted in human milk, therefore its use during breastfeeding is not recommended. If treatment is necessary, discontinuation of breastfeeding should be considered.

2. Severe liver or kidney dysfunction:

   • Patients with severe liver or kidney dysfunction should use mebeverine with caution and under medical supervision.

Special instructions:

• Patients with porphyria:
  • There are no data on the use of mebeverine in patients with porphyria, therefore its use in such patients is not recommended.

Side effects Duspatalina

Possible side effects:

1. Allergic reactions:

   • Skin rashes
   • Itching
   • Hives (urticaria)
   • Angioedema (Quincke's edema), which causes swelling of the face, lips, tongue, or throat that can cause difficulty breathing and requires immediate medical attention
   • Anaphylactic reactions (very rare)

2. From the gastrointestinal tract:

   • Nausea
   • Diarrhea
   • Constipation
   • Abdominal pain

3. From the nervous system:

   • Headache
   • Dizziness (rare)

4. From the cardiovascular system:

   • Palpitations (rapid heartbeat) (very rare)

Notes:

• Rarity of side effects: In general, mebeverine is well tolerated and serious side effects are rare.
• Individual reaction: The reaction to the drug may be individual and some patients may experience side effects not listed above. If unusual or severe symptoms occur, consult a doctor.

Overdose

1. From the central nervous system:

   • Excitation
   • Dizziness
   • Headache

2. From the cardiovascular system:

   • Tachycardia (rapid heartbeat)

3. From the gastrointestinal tract:

   • Nausea
   • Vomit
   • Diarrhea

4. Allergic reactions:

   • Rash
   • Itching
   • Hives

Interactions with other drugs

Drug interactions:

1. Medicines affecting the central nervous system:

   • Although mebeverine itself does not have significant central effects, its concomitant use with sedatives, antidepressants, or anticonvulsants may require monitoring of the patient for possible increased sedative effects or other central reactions.

2. Anticholinergics:

   • Mebeverine does not have anticholinergic properties, but theoretically its combination with other anticholinergic agents may enhance the spasmolytic effect on the intestine, which may require dosage adjustment and monitoring.

3. Antifungal medications (eg, ketoconazole):

   • There are no known significant interactions between mebeverine and antifungal agents, however ketoconazole may alter the metabolism of some drugs. Potential interactions should be considered and the patient monitored during combination therapy.

4. Drugs affecting the gastrointestinal tract:

   • Mebeverine may interact with other drugs that affect intestinal motility. This may include prokinetics (eg, metoclopramide), which may have opposite effects on intestinal motility.

Interactions with food and alcohol:

1. Food:

   • Food does not significantly affect the absorption and effectiveness of mebeverine. It is recommended to take Duspatalin 20 minutes before meals to achieve the optimal effect.

2. Alcohol:

   • Alcohol may increase the side effects of mebeverine, such as dizziness and sedation. It is recommended to avoid alcohol consumption during treatment with Duspatalin.