What Is Domperidone?

Domperidone tablets, 1. Indigestion caused by delayed gastric emptying, gastroesophageal reflux, and esophagitis. -Bloating feeling in the upper abdomen, abdominal distension, epigastric pain;-belching, flatulence;-nausea, vomiting;-burning sensation in the mouth with or without reflux stomach contents. 2. Functional, organic, infectious, dietary, radiation therapy or chemotherapy-induced nausea and vomiting. Dopamine receptor agonists (such as levodopa, bromocriptine, etc.) are used to treat nausea and vomiting caused by Parkinson's disease, which is a specific indication for this product.

Drug Name: Domperidone tablets
Drug type: Work Injury Medical Insurance Class A Double Span

Hanyu Pinyin: Duo Pan Li Tong Pian
Use classification: Gastrointestinal stimulants

Domperidone tablets ingredients

Active ingredient: Domperidone Chemical name: 5_-chloro-1- [1- [3- (2,3-dihydro-2-oxo-1H-benzimidazole-1 -yl) propyl] piperidine-4- Group] -1,3-dihydro-2H -benzimidazol-2-one chemical structural formula:

Molecular weight: 425.91

Domperidone tablet properties

This product is a white tablet.

Domperidone Tablets Action Category

This product is an over-the-counter drug for gastrointestinal prokinetic drugs.

Domperidone tablets indications

1. Indigestion caused by delayed gastric emptying, gastroesophageal reflux, and esophagitis.
-Stomach bloating, abdominal distension, epigastric pain;
-Belching, flatulence;
-feel sick and vomit;
-A burning sensation in the mouth with or without reflux stomach contents.
2. Functional, organic, infectious, dietary, radiation therapy or chemotherapy-induced nausea and vomiting. Dopamine receptor agonists (such as levodopa, bromocriptine, etc.) are used to treat nausea and vomiting caused by Parkinson's disease, which is a specific indication for this product.

Domperidone Tablets Specifications

10mg

Domperidone tablets dosage

oral.
Adults: 1-3 times a day, 1 tablet each time. If necessary, the dose can be doubled or as directed by your doctor.
Children (over 12 years and over 35 kg): 3-4 times a day, 0.3 mg per kg of body weight each time.
This product should be taken 15-30 minutes before meals. If taken after meals, absorption will be delayed.
The highest daily dose of this product is 80 mg.

Adverse reactions of domperidone tablets

According to the standard practice of incidence: very common (> 1/10); common (> 1/100, <1/10); rare (> 1 / 1,000, <1/100); rare (> 1 / 10,000, < 1 / 1.000); very rare (<1 / 10,000), including individual cases, ranked by incidence of adverse reactions:
immune system:
Very rare: allergic reactions including anaphylactic shock, angioedema, allergic reactions endocrine:
endocrine:
Rare: elevated prolactin levels mental system:
Rare: Excitement, nervousness, nervous system:
Very rare: extrapyramidal side effects, convulsions, drowsiness, headache gastrointestinal tract:
Rare: gastrointestinal discomfort, including very rare transient intestinal cramps skin and subcutaneous tissue:
Very rare: rash, pruritus, urticaria reproductive system and breast:
Rare: Breast milk, feminization of male breasts, amenorrhea:
Very rare: abnormal liver function tests. Dopperidone may cause elevated prolactin levels because the pituitary is outside the blood-brain barrier. In rare cases, this hyperprolactinemia may cause neuro-endocrine side effects such as galactorrhea, feminization of male breasts, and amenorrhea.
Extrapyramidal symptoms are very rare in children, and even more rare in adults. These symptoms can fully recover on their own after stopping treatment.
Other CNS-related reactions such as convulsions, excitement, and lethargy are very rare and are reported primarily in infants and children.

Domperidone tablets contraindications

This product is banned in the following privacy:
· Persons who are allergic to domperidone or any component of this product.
· Increased gastric motility may be dangerous, such as gastrointestinal bleeding, mechanical obstruction, perforation.
Patients with pituitary tumors (prolactinoma) that secrete prolactin.
· Combined oral ketoconazole preparations, erythromycin, or other potent CYP3A4 enzyme inhibitors that may prolong the QTc interval, such as fluconazole, voriconazole, clarithromycin, amiodarone, and telithromycin.

Precautions for domperidone tablets

-This product contains lactose and may not be suitable for patients with lactose intolerance, galactosemia or glucose / galactose malabsorption.
-When antacids or drugs that inhibit gastric acid secretion are combined with this product, the first two types of drugs cannot be taken before meals, and should be taken after meals, that is, it should not be taken at the same time as this product.
-Because domperidone is mainly metabolized in the liver, patients with impaired liver function are afraid to use it.
-The elimination half-life of domperidone in patients with severe renal insufficiency (serum creatinine> 6 mg / 100 ml, or> 0.6 mmol / L) increased from 7.4 hours to 20.8 hours, but its blood concentration was lower than that of healthy volunteers. Because there are very few prototype drugs excreted by the kidneys, patients with renal insufficiency may not need to adjust the dose once, but when repeated administration is required, the frequency of medication should be reduced to 1-2 per day according to the severity of renal impairment. At the same time, the dose should be reduced at the same time. Periodic inspection of such patients should be performed regularly.
-Keep it out of reach of children.

Domperidone tablets for pregnant and lactating women

Pregnant women: This product has limited experience in pregnant women. Its potential harm to the human body is unknown. But in a study in rats, domperidone showed reproductive toxicity at higher doses that are toxic to the mother (40 times the human recommended dose). Therefore, for pregnant women, this product should only be used with caution after weighing the pros and cons.
Lactation: The concentration of domperidone in the milk of a lactating woman is 10-50% of its corresponding plasma concentration, but not more than 10ng / ml in the milk. The total amount of domperidone in breast milk is less than 7ug / day when breastfeeding women take the most recommended dose of this product, it is unknown whether it will harm the newborn. Therefore, breastfeeding women are advised not to breastfeed while taking this product.

Domperidone tablets for children

Rare neurological side effects in infants. Because the metabolism and the function of the thin barrier are not fully developed in the first few months after birth, the incidence of neurological side effects is higher in infants than in children. Therefore, it is recommended that the dosage should be accurately formulated for newborns, infants and young children and strictly followed. Overdose may cause neurological side effects, but other reasons should also be considered.

Domperidone tablets for the elderly

Elderly patients take the same medications as adults.

Domperidone tablets drug interactions

Combination with anticholinergic drugs will include the anti-digestive effect of this product.
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 as this product.
Domperidone is mainly metabolized by the CYP3A4 enzyme. Data from in vitro and human studies have shown that combination with drugs that significantly inhibit the CYP3A4 enzyme results in increased blood levels of domperidone,
Examples of potent inhibitors of CYP3A4 enzyme are as follows:
· Azole antifungals, such as fluconazole *, itraconazole, ketoconazole *, and voriconazole *
· Macrolide antibiotics, such as erythromycin and clarithromycin *
· HIV protease inhibitors, such as: ampennavir, atazanavir, fosanavir, indinavir, nafinavir, ritonavir, saquinavir, calcium inhibitors, such as: Diltiazem and verapamil amiodarone *
· Aprepitant · Nefazodone · Telomycin *
(* QTc interval will also be extended, see [taboo] for details)
Ketoconazole and erythromycin significantly inhibited the first dose of domperidone mediated by CYP3A4 in pharmacokinetic / pharmacodynamic trials with ketoconazole or erythromycin oral preparations in healthy volunteers Over effects.
In the domperidone-ketoconazole interaction test, it was observed that the combination of domperidone (10 mg / times, 4 times / day) and ketoconazole (200 mg / times, 2 times / day) increased the average QTc interval by 9.8 ms. The variation range of individual QTc interval is 1.2-17.5 milliseconds. In the domperidone-erythromycin interaction test, it was observed that the combination of domperidone (10 mg / time, 4 times / day) and erythromycin (500 mg / time, 3 times / day) increased the average QTc interval by 9.9 milliseconds. The individual QTc interval ranges from 1.6 to 14.3 milliseconds. In the above interaction test, the steady state C _max and AUC of domperidone increased by about three times.
The relationship between the increase of domperidone plasma concentration and the effect of QTc interval is unknown.
During the observation period of the interaction test with ketoconazole and erythromycin, the use of domperidone alone (10 mg / time, 4 times / day) increased the average QTc interval by 1.6 ms and 2.5 ms. Ketoconazole (200 mg / time, 2 times / day) or erythromycin (500 mg / time, 3 times / day) alone increased the QTc interval by an average of 3.8 ms and 4.9 ms.
In another repeated-dose study on healthy volunteers, there was no QTc interval when the domperidone monotherapy was stable at a dose of 40 mg / time, 4 times / day (160 mg daily, twice the highest daily dose) Significantly extended record. Domperidone blood paddle concentrations in this study are at least similar to those found in previous interaction studies.
Because domperidone has a gastrokinetic effect, it theoretically affects the absorption of oral drugs (especially slow-release or enteric-coated preparations) used in combination. However, for patients who have taken diazepam or acetaminophen with blood drug concentrations at a stable level, the combination of domperidone does not affect their blood drug concentrations.
Domperidone is used in combination with:
Neurosuppressants: Domperidone does not enhance the effects of neurosuppressants.
Dopaminergic agonists: Domperidone reduces peripheral side effects of dopaminergic agonists (such as bromocriptine. Levodopa), such as gastrointestinal symptoms, nausea, and vomiting, but does not include anti-central effects.

Domperidone tablets overdose

Overdose is reported mainly in infants and children. Symptoms of overdose include excitement, altered consciousness, convulsions, disorientation, lethargy, and extrapyramidal reactions.
There is no specific remedy for this product. Once the drug is overdose, gastric lavage and administration of activated carbon may be helpful, and intensive clinical monitoring and supportive treatments are recommended. Anticholinergic or antiparkinsonian drugs may help control extrapyramidal responses.

Pharmacological effects of domperidone tablets

1. Pharmacological effect This product is a peripheral dopamine blocker, which directly acts on the gastrointestinal wall, can increase the lower esophagus sphincter tension, prevent gastric-esophageal reflux, enhance gastric motility, promote two emptying, coordinate the stomach and the twelve Duodenal exercise can inhibit nausea and vomiting, and can effectively prevent bile reflux without affecting gastric secretion.
This product does not easily penetrate the blood-brain barrier. Animal test results show that the concentration of domperidone in the brain is very low, and it also shows that domperidone has a very strong effect on the peripheral dopamine receptors. Extrapyramidal reactions are rare in users, especially adults, but domperidone promotes the release of prolactin from the pituitary. Its antiemetic effect is mainly due to its double blocking effect on the peripheral dopamine receptors and dopamine receptors in the chemoreceptor trigger region outside the blood-brain barrier.
2. Toxicology In a study in rats, domperidone showed reproductive toxicity at relatively high doses (40 times the recommended human dose) that are toxic to the mother. However, this phenomenon was not found in experiments on mice and rabbits.
In vitro and in vivo electrophysiological studies, domperidone may prolong the QTc interval at high concentrations.

Pharmacokinetics of domperidone tablets

This product is absorbed quickly after oral administration on an empty stomach, reaching peak blood concentration in 30-60 minutes. Reduced gastric acid can affect the absorption of domperidone. Domperidone has a blood protein binding rate of 91-93%. Healthy volunteers take this product orally in a single dose. The plasma half-life is 7-9 hours. The half-life of patients with severe renal insufficiency is prolonged. This product is almost exclusively metabolized in the liver. In vitro metabolism tests with diagnostic inhibitors show that CYP3A4 is the main form of cytochrome P-450 involved in N-dealkylation of domperidone, while CYP3A4, CYP1A2 and CYP2E1 are involved in aromatic hydroxylation of domperidone. The total excretion through urine is 31%, and the original drug accounts for 1%; the total fecal excretion is 66%, and the original drug accounts for 10%.

Storage of domperidone tablets

Protected from light and sealed.

Packaging of domperidone tablets

Packed in aluminum plastic blister board, 2X21 pieces / board / box.

Validity of domperidone tablets

60 months

Domperidone Tablets

National Drug Standard WS _1- (X-185) -97Z

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