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Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.
Domperidone is a peripheral-specific antagonist of the dopamine receptor D2 (D2R), with antiemetic, gastrokinetic and galactagogue activities. Following administration, domperidone binds to D2R expressed by peripheral neurons; this inhibits dopamine binding and D2R-mediated signaling. Inhibition of peripheral D2R signaling prevents or relieves various gastrointestinal (GI) symptoms, such as nausea and vomiting, and may help relief reflux and symptoms of a variety of other upper GI disorders.
Domperidone is only found in individuals that have used or taken this drug. It is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting
Mechanism of Action of Domperidone
Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting
Indications of Domperidone
- Domperidone is used to help to move food faster through your food pipe (oesophagus), stomach and gut. This is so that it does not stay in the same place for too long.
- It is a dopamine agonist, and belongs to a group of medicines known as anti-emetics.
- In general this drug is used to relieve symptoms of feeling sick (nausea) and sickness (vomiting).
- Heartburn
- Epigastric Pain
- Gatroesophageal reflux disease
- Gastric outlet obstruction.
- Gastroparesis
- Nausea, and vomiting.
- Infantile reflex & pediatric reflux
- Parkinson’s disease
- Benefits of being on this drug can include relieving symptoms of nausea and vomiting.
- Management of dyspepsia
- Functional dyspepsia
- Parkinson’s disease is a chronic neurological condition where a decrease in dopamine in the brain leads to rigidity (stiffness of movement), tremor and other symptoms and signs. Poor gastrointestinal function, nausea and vomiting is a major problem for people with Parkinson’s disease because most medications used to treat Parkinson’s disease are given by mouth. These medications, such as levodopa, can cause nausea as a side effect. Furthermore, anti-nausea drugs, such as metoclopramide, which do cross the blood–brain barrier may worsen the extra-pyramidal symptoms of Parkinson’s disease.
Therapeutic Indications of Domperidone [FDA Level]
- For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.
- Domperidone is indicated for: dyspeptic symptom complex that is often associated with delayed gastric emptying, gastro-oesophageal reflux, and oesophagitis
- Epigastric sense of fullness, early satiety, feeling of abdominal distension, upper abdominal pain ,bloating, eructation, flatulence ,nausea and vomiting
- Heartburn with or without regurgitations of gastric contents in the mouth
- Nausea and vomiting of functional, organic, infectious or dietetic origin
- Nausea and vomiting induced by: radiotherapy or drug therapy dopamine agonists (such as L-dopa and bromocriptine) used in the treatment of Parkinson’s disease
Contra indications of Domperidone
- Triazole antifungal medications such as ketoconazole, itraconazole, fluconazole.
- Macrolide antibiotics such as erythromycin and clarithromycin.
- Grapefruit juice.
- QT-prolonging drugs like amiodarone.
- Prolactin secreting pituitary tumor (prolactinoma) or hyperprolactinemia.
- Mechanical bowel disorders such as bowel obstruction, gastrointestinal haemorrhage or bowel perforation
- Moderate hepatic impairment (liver disease).
- Severe renal impairment (kidney disease).
- Cardiac disease.
Dosage of Domperidone
Strengths: 10 mg ,
Nausea, and vomiting /gastrointestinal abnormality
- The usual dose for the treatment is 1 to 2 tablets taken 3 to 4 times a day before meals. Do not take more than 8 tablets (80mg) in 24 hours.
Infants and Children
- Children weighing less than 35kg (5 stone) should not take these tablets. The usual dose for the treatment is 0.25 0.5mg per kg bodyweight taken 3 to 4 times a day before meals. Your pharmacist may be able to help you if you are not sure.
Side Effects of Domperidone
Most common
- Headache, which disappeared when the dose was reduced
- Abdominal cramps
- Diarrhea
- muscle twitching
- weakness
- Any signs of infection, or a skin rash.
- Stomach pain, especially if it comes along with fever and diarrhea or constipation
- Yellowing of the skin or eyes
- Loss of appetite
- Constipation
- Chest pain or discomfort
- lightheadedness, dizziness, or fainting
- unusual tiredness or weakness
- decrease in the amount of urine
- fast, pounding, or irregular heartbeat or pulse
- increased watering of mouth
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Unexpected aggression, restlessness or irritability .
- Nightmares or hallucinations
Rare
- agitation
- anxiety
- behavioural changes, including aggressiveness, angry outbursts,
- confusion
- increased trouble sleeping
- muscle spasms
- shortness of breath
- difficult or labored breathing
- difficulty with swallowing
- dizziness, faintness, or lightheadedness
- frequent urination
- hallucinations
- bloating or swelling of the face, arms, hands, lower legs, or feet
- blurred vision
- hives or welts, itching, or skin rash
Drug Interactions of Domperidone
Domperidone may interact with following drugs, supplyments, & may change the efficacy of drugs
- antihistamines (e.g., cetirizine, diphenhydramine, hydroxyzine, loratadine)
- anti-psychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzepine, quetiapine,risperidone)
- “azole” antifungals (e.g., fluconazole ,itraconazole, ketoconazole, voriconazole)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- conivaptan
- cyclosporine
- dasatinib
- famotidine
- formoterol
- fusidic acid
- imatinib
- lapatinib
- macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
- metronidazole
- monoamine oxidase inhibitors (MAOIs; e.g. phenelzine, rasagiline, selegiline, )
- nilotinib
- quinolone antibiotics (e.g., ciprofloxacin, moxifloxacin, levofloxacin)
- selective serotonin reuptake inhibitors (SSRIS; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- serotonin antagonists ( e.g., granisetron, ondansetron)
- sotalol
- sunitinib
- tetracycline
- tricyclic antidepressants (e.g., amitriptyline, nortriptyline)
- trimethoprim
- vardenafil
Pregnancy & Lactation of Domperidone
FDA Pregnancy Category C
Pregnancy
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Breastfeeding
This medication passes into breast milk. If you are a breastfeeding mother and are taking domperidone, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.
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