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    Home > Active Ingredient News > Digestive System Information > How to choose a gastrointestinal motility drug for functional dyspepsia?

    How to choose a gastrointestinal motility drug for functional dyspepsia?

    • Last Update: 2021-10-21
    • Source: Internet
    • Author: User
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    It is only for medical professionals to read.
    Drug treatments mainly include gastrointestinal motility drugs, acid inhibitors, Helicobacter pylori (Hp) eradication therapy, and the application of antidepressants
    .

    Functional dyspepsia (FD) is a common clinical functional gastrointestinal disease with a high incidence and an increasing trend year by year
    .

    The prevalence of FD is 23.
    5% among the health examiners (15-75 years old) in our country, and on average, more than 1 out of every 5 people have FD
    .

    The condition of FD is easy to recur, which seriously affects the quality of life of patients and significantly increases the economic burden of patients
    .

    FD refers to symptoms of chronic dyspepsia, mainly including upper abdominal pain or burning, upper abdominal distension or early fullness or fullness after meals, lack of appetite, belching, nausea or vomiting, but upper gastrointestinal endoscopy, hepatobiliary and pancreatic Imaging and biochemical examinations showed no obvious abnormalities, and peptic ulcers, gastrointestinal tumors, hepatobiliary malignancies, parasitic infections, chronic pancreatic diseases, hyperthyroidism and (or) hypothyroidism, chronic renal failure, electrolyte disturbances can be ruled out Organic, systemic, or metabolic diseases that may have symptoms similar to FD, such as adverse reactions to some drug treatments
    .

    Those with obvious abnormalities in the aforementioned examinations are called organic dyspepsia (OD)
    .

    FD can be divided into epigastric pain syndrome (EPS) or postprandial discomfort syndrome (PDS), and some patients may overlap the two
    .

    1.
    Prokinetic drug treatment of FD The drug treatment of FD includes the application of gastrointestinal motility drugs, acid inhibitors, Helicobacter pylori (Hp) eradication therapy, and the application of antidepressants
    .

    Gastrointestinal motility drugs are a class of drugs that stimulate smooth muscle contraction to enhance gastric emptying and small intestinal transport.
    They can significantly improve FD by accelerating gastric emptying, reducing visceral hypersensitivity, promoting antral motility, antiemetic and other mechanisms.
    patients with meal-related upper abdominal symptoms, such as abdominal postprandial fullness, early satiety
    .

    Promoting gastrointestinal motility drugs can be used as the first choice empirical treatment for FD, especially PDS
    .

    Meal-related dyspepsia (such as PDS) can be used as the first choice for gastrointestinal motility drugs or combined with acid suppressants; for non-meal-related dyspepsia/acid-related dyspepsia (such as EPS), acid suppressants can be used, and when necessary, gastro-stimulating drugs can be used together.
    Intestinal motility drugs
    .

    Experience treatment for 2 to 4 weeks
    .

    Those who are ineffective should undergo a one-step inspection to rule out organic diseases or adjust the treatment plan
    .

    The most commonly used gastrointestinal motility drugs in China are domperidone, mosapride, and itopride
    .

    Many studies on the efficacy of gastrointestinal motility drugs on FD have centered on cisapride, but the drug has been banned due to adverse effects of the cardiovascular system
    .

    Because its mechanism of action is similar to that of cisapride, mosapride has no adverse effects in the cardiovascular system, so it can be used instead of cisapride in clinical practice
    .

    Itopride is a new type of gastrointestinal motility drug.
    Domestic studies have shown that Itopride has a similar efficacy to mosapride, but its effect on improving postprandial fullness and discomfort symptoms is better than the latter
    .

    Foreign studies have shown that the safety and tolerability of itopride are similar to placebo, but it can significantly increase the level of prolactin in the body
    .

    Metoclopramide can cause adverse reactions in the central nervous system, especially irreversible tardive dyskinesia, which largely limits its clinical application
    .

    2.
    Classical prescription analysis ■Prescription 1 domperidone tablet 10mg, 3 times a day, orally half an hour before meals
    .

    Indications: Patients with abdominal fullness and early satiety symptoms above FD
    .

    Medication analysis: Domperidone is a peripheral dopamine receptor blocker that directly acts on the gastrointestinal wall, can increase the tension of the lower esophageal sphincter, prevent gastro-esophageal reflux, enhance gastric motility, accelerate gastric emptying, and improve postprandial fullness and early Symptoms such as fullness; reduce the sensitivity of the stomach to distension and pain, improve symptoms such as bloating, abdominal pain, and belching; improve symptoms such as nausea and vomiting; prevent bile reflux
    .

    During the use of domperidone, individual patients, especially elderly men, may experience breast tenderness or galactorrhea after long-term use
    .

    Under normal circumstances, the drug rarely penetrates the blood-brain barrier, so extrapyramidal side effects are rare, but they can be seen in infants and patients with dementia with imperfect blood-brain barrier
    .

    In patients with severe renal insufficiency, the elimination half-life of the drug is prolonged, and the dose must be reduced as appropriate
    .

    There are reports of sudden cardiac death and severe arrhythmia caused by the drug abroad
    .

    Reducing the recommended dose and shortening the course of treatment are key measures to minimize the risk of domperidone
    .

    The usual dose is 10 mg, 3 times a day
    .

    Under normal circumstances, the course of treatment should not exceed 1 week
    .

    Prolactinoma, pheochromocytoma, breast cancer, gastrointestinal bleeding, mechanical obstruction, and perforation are prohibited
    .

    It is forbidden for patients with moderate to severe liver dysfunction
    .

    It is forbidden to use it in combination with ketoconazole oral preparations, erythromycin or other CYP3A4 enzyme potent inhibitors (such as fluconazole, voriconazole, clindamycin, amiodarone, telithromycin) that may prolong the QTc interval
    .

    Combined use with anticholinergic drugs will antagonize the effect of this product in the treatment of dyspepsia
    .

    Antacids and drugs that inhibit gastric acid secretion will reduce the oral bioavailability of this product, and should not be taken at the same time with this product
    .

    ■ Prescription 2 mosapride citrate tablets 5mg, 3 times a day, orally before meals
    .

    Indications: Patients with abdominal fullness and early satiety symptoms above FD, poor effect of domperidone or contraindications
    .

    Medication analysis: Mosapride can excite cholinergic interneurons in the gastrointestinal tract and serotonin 4 receptors in the myenteric plexus, promote the release of acetylcholine, and enhance gastrointestinal motility
    .

    This drug has no affinity with dopamine D2 receptor, adrenaline α1 receptor, serotonin 1 receptor and serotonin 2 receptor on the synaptic membrane of brain nerve cells, so it will not cause extrapyramidal syndrome and cardiovascular Adverse reactions
    .

    Although its chemical structure is similar to cisapride, there is no report of torsade de pointes ventricular tachycardia caused by mosapride alone.
    However, for safety reasons, one should remain vigilant and avoid and prolong QT.
    Interval drugs (such as flecainide, amiodarone, procaine, quinidine, sotalol, tricyclic antidepressants, etc.
    ) are used in combination
    .

    In addition, usually after taking this drug for 2 weeks, if the symptoms do not improve, the drug should be discontinued; combined with anticholinergic drugs (such as atropine, scopolamine, etc.
    ) may weaken the effect of this drug; combined with drugs that can cause hypokalemia should be cautious to avoid heart rhythm Abnormal
    .

    ■ Prescription 3 Itopride Hydrochloride Tablets 50mg, 3 times a day, orally before meals
    .

    Indications: Patients with symptoms of abdominal fullness and early fullness above FD, and contraindications to the application of mosapride citrate
    .

    Medication analysis: Itopride is a dopamine D2 receptor antagonist and an acetylcholinesterase inhibitor.
    It can increase the concentration of acetylcholine in the gastrointestinal tract, increase the amplitude and frequency of duodenal fast waves, accelerate gastric emptying, and reduce the duodenum and stomach Reflux, thereby promoting gastrointestinal motility
    .

    The drug has no affinity with serotonin 4 receptors, and there is no risk of cardiovascular adverse events caused by prolonged QT interval.
    It is metabolized by flavin monooxygenase (not CYP450 enzyme), and there are few interactions between drugs, so it has good safety.
    Sex
    .

    The results of a foreign randomized, double-blind, controlled study showed that itopride is better than mosapride in the efficacy and tolerability of FD
    .

    It is contraindicated for patients with gastrointestinal bleeding, mechanical obstruction or perforation
    .

    Since the safety of administration to pregnant women has not been confirmed, for pregnant women or women who are likely to become pregnant, they can only be administered when it is confirmed that the therapeutic benefit is higher than the risk
    .

    Breastfeeding should be avoided while taking this drug
    .

    The safety data for children taking this product has not been established and should be avoided
    .

    ■ Prescription 4 Trimebutine maleate tablets 0.
    1g, 3 times a day, orally
    .

    Indications: Patients with abdominal fullness and early satiety symptoms above FD, who have contraindications to the application of mosapride citrate or itopride hydrochloride
    .

    Medication analysis: Trimebutine maleate tablets are two-way regulators of gastrointestinal motility rhythm, which can regulate the excitement and inhibition of gastrointestinal smooth muscle in both directions
    .

    When the smooth muscle movement of the gastrointestinal tract is low, trimebutine maleate can act on the smooth muscle adrenergic receptors of the gastrointestinal tract to inhibit the release of adrenaline, thereby increasing the smooth muscle movement rhythm of the gastrointestinal tract; when the smooth muscle movement of the gastrointestinal tract is hyperactive At times, trimebutine maleate can act on the smooth muscle cholinergic receptors of the gastrointestinal tract, inhibit the release of acetylcholine, thereby reducing the rhythm of the smooth muscle movement of the gastrointestinal tract
    .

    Trimebutine maleate occasionally increased alanine aminotransferase and aspartate aminotransferase.
    When abnormalities were found, the drug was stopped and hepatoprotective treatment was given
    .

    Use with caution during pregnancy, breastfeeding women and children
    .

    Reference source: [1] Yu Jiao, Zheng Dan.
    Pathogenesis and treatment strategies of functional dyspepsia[J].
    Journal of Clinical Digestive Diseases, 2017, 29 (2): 122-125.
    [2] Chinese Medical Association Digestive Diseases Gastrointestinal kinetics group of the academic branch.
    Expert consensus on Chinese functional dyspepsia (2015, Shanghai) [J].
    Chinese Journal of Digestion, 2016, 36 (4): 217-229.
    [3] Hao Yue.
    Moshabi Observation on the efficacy of Li and domperidone in the treatment of functional dyspepsia[J].
    China Practical Medicine, 2021,16(10):138-141.
    [4]Zhou Tao.
    Weisu granule combined with mosapride on the stomach of patients with functional dyspepsia The effect of intestinal hormone levels[J].
    Medical Theory and Practice, 2021, 34(18): 3174-3176.
    [5] Zhang Wenguang, Qiu Hong, Song Fusheng.
    Xiangshapingwei granule combined with itopride in the treatment of functional digestion Clinical observation of dysfunction[J].
    Drug Evaluation Research, 2021, 44(3): 556-560.
    [6] Wen Guangde, Huang Chaofan.
    Clinical observation of trimebutine combined with compound digestive enzymes in the treatment of functional dyspepsia[J] .
    Modern Diagnosis and Treatment, 2018, 29(12): 1917-1919.
    [7] Sun Shouguang, Jiang Donglian.
    Observation on the efficacy of trimebutine maleate combined with venlafaxine in the treatment of functional dyspepsia and gastric receptivity And the influence of gastrointestinal hormone levels[J].
    World Chinese Journal of Digestion, 2018, 26(32): 1901-1906.
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