Duspatalin

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

The mechanism of action of mebeverine is to block calcium channels in the smooth muscles of the intestine, which leads to its relaxation. This helps reduce spasms, reduce pain and improve intestinal permeability.

Duspatalin is usually taken orally in the form of tablets or capsules. It is usually taken before meals or as needed as recommended by your doctor.

Indications Duspatalina

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

Release form

Duspatalin is usually available in the form of tablets or capsules for oral administration.

Pharmacodynamics

1. Mechanism of action:

   • Selective antispasmodic effect: Mebeverine selectively relaxes intestinal smooth muscle without significantly affecting normal intestinal motility. This allows you to reduce spasms and associated pain without interfering with normal motor functioning.
   • Sodium Channel Blocking: Mebeverine blocks sodium channels in the cell membranes of smooth muscle cells, resulting in membrane stabilization and preventing uncontrolled sodium entry into the cells. This prevents depolarization and subsequent contraction of smooth muscle.
   • Anti-spasmodic effect: The drug reduces the increased tone and hypermotor activity of intestinal smooth muscles, which helps relieve symptoms such as pain, cramps and abdominal discomfort.

2. Effects on the gastrointestinal tract:

   • Reducing pain and discomfort: By relaxing intestinal smooth muscle, 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 bowel movement.

3. Clinical effects:

   • Improvement of patient condition: Mebeverine is effective in the treatment of irritable bowel syndrome (IBS) and other functional gastrointestinal disorders. Patients note a decrease in pain intensity, a decrease in spasms and an improvement in overall well-being.

4. Advantages:

   • Minimal systemic effects: Due to the selectivity of action on the intestinal muscles, mebeverine has minimal systemic side effects, which makes 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 characteristic of some other antispasmodics.

Pharmacokinetics

1. Suction:

   • After oral administration, mebeverine is quickly and completely absorbed from the gastrointestinal tract. Modified-release formulations, such as capsules, provide sustained release of the active substance to 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 intensive metabolism in the liver through 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 mainly by the kidneys. Approximately 60% of metabolites are excreted in the urine in the form of carboxylic acids and their glucuronides.
   • Some of the metabolites may be excreted in bile.

5. Half-life:

   • The half-life of mebeverine and its metabolites is approximately 5-6 hours, which allows the drug to be taken 2 times a day 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 impaired renal or hepatic function, making mebeverine convenient 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):

• Recommended dose: One capsule (200 mg) twice a day.
• Directions for use: Capsules should be taken whole, without chewing, with a sufficient amount of water (at least half a glass). It is recommended to take capsules 20 minutes before meals (morning and evening).

Tablets (135 mg):

• Recommended dose: One tablet (135 mg) three times a day.
• Directions for use: Tablets should be taken whole with plenty of water. It is recommended to take the 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/her response to treatment.
   • Treatment can be continued until a stable improvement in the condition is achieved, after which a gradual reduction in the dose is recommended.

2. Missing a 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 drug as usual.

3. Discontinuing treatment:

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

Special instructions:

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

Approximate schedule of administration:

Extended-release capsules:

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

Tablets:

• In the morning: 1 tablet 20 minutes before breakfast.
• 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.

Efficacy 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. Effect on the kidneys and fetus: A study on 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 data highlight the need for careful use of the drug and consultation with a doctor before its use (Al-Essawi et al., 2022).
3. Metabolism and stability: Mebeverine is rapidly metabolized in the body, making it almost undetectable in blood 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 experienced allergic reactions to this drug, its use is strictly contraindicated.

2. Age up to 18 years:

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

Relative contraindications:

1. Pregnancy and lactation:

   • Pregnancy: The use of mebeverine during pregnancy is possible only in cases of extreme necessity and under the strict supervision of a physician. Data on the safety of the drug in pregnant women are limited.
   • Lactation: It is unknown whether mebeverine is excreted in breast milk, so 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 hepatic or renal impairment 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, so its use in such patients is not recommended.

Side effects Duspatalina

Possible side effects:

1. Allergic reactions:

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

2. Gastrointestinal tract:

   • Nausea
   • Diarrhea
   • Constipation
   • Stomach pain

3. On the part of the nervous system:

   • Headache
   • Dizziness (rare)

4. 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: Reaction to the drug may vary individually, and some patients may experience side effects not listed above. If unusual or severe symptoms occur, you should consult your doctor.

Overdose

1. From the central nervous system:

   • Excitement
   • Dizziness
   • Headache

2. Cardiovascular system:

   • Tachycardia (rapid heartbeat)

3. Gastrointestinal tract:

   • Nausea
   • Vomiting
   • 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 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 drugs may increase the antispasmodic effect on the intestines, which may require dosage adjustment and monitoring.

3. Antifungal drugs (for example, ketoconazole):

   • There are no known significant interactions between mebeverine and antifungals, but 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 opposing effects on intestinal motility.

Interactions with food and alcohol:

1. Food:

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

2. Alcohol:

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