Usage
Cinnarizine + Domperidone is prescribed for the management of vertigo, dizziness, nausea, and vomiting associated with various conditions, including Meniere’s disease, labyrinthitis, motion sickness, and migraine. It is also used to alleviate symptoms of nausea and fullness related to dyspepsia and gastritis.
Pharmacological Classification: This combination drug falls into two categories:
- Cinnarizine: Antihistamine, Calcium channel blocker
- Domperidone: Antiemetic, Dopamine antagonist, Prokinetic agent
Mechanism of Action: Cinnarizine reduces the excitability of the vestibular system in the inner ear by blocking calcium channels and also acts as an antihistamine. Domperidone is a dopamine antagonist that acts on the chemoreceptor trigger zone in the brain and the upper digestive tract, thus reducing nausea and vomiting. It also increases the movements and contractions of stomach muscles and acts as a prokinetic agent, facilitating gastric emptying and controlling acid reflux.
Alternate Names
No internationally recognized alternate names exist for the combination product itself. The individual components, however, may be known by other names (primarily related to specific salt forms).
Brand Names: Cinnarizine + Domperidone is marketed under various brand names, some examples include: Atmozin-D, Cindom, and others. (Note: Brand availability may vary by region).
How It Works
Pharmacodynamics: Cinnarizine acts by blocking calcium channels in the inner ear and peripheral blood vessels, stabilizing vestibular function and improving microcirculation. As an antihistamine, it reduces the effects of histamine, a chemical messenger involved in allergic reactions and motion sickness symptoms. Domperidone blocks the action of dopamine, a neurotransmitter that stimulates the vomiting center in the brain. This action prevents nausea and vomiting. Its prokinetic effect enhances gastric motility and emptying, relieving fullness and discomfort.
Pharmacokinetics:
- Absorption: Both drugs are absorbed orally. Domperidone absorption can be slightly delayed if taken after meals.
- Metabolism: Cinnarizine is metabolized in the liver by CYP enzymes. Domperidone is also primarily metabolized in the liver, specifically by CYP3A4.
- Elimination: Both drugs are primarily excreted through urine and feces.
Mode of Action: Cinnarizine affects vestibular function by reducing calcium influx into cells, leading to decreased sensitivity of the balance organs. It also antagonizes H1 histamine receptors. Domperidone exerts its antiemetic effect by antagonizing dopamine D2 receptors in the chemoreceptor trigger zone and the gastrointestinal tract. It enhances gastrointestinal motility by blocking dopamine receptors in the gut.
Elimination Pathways: Cinnarizine is extensively metabolized in the liver and excreted mainly in urine and feces. Domperidone is metabolized in the liver, involving CYP3A4 enzymes and excreted primarily in urine and to a lesser extent in feces.
Dosage
Standard Dosage
Adults: The typical adult dose is one tablet containing 20mg of cinnarizine and 15mg of domperidone, taken two to three times a day. The maximum dose is typically three tablets per day.
Children: Use with caution in children. Domperidone is not recommended in children weighing less than 35kg. Doses for eligible children must be carefully calculated based on body weight (0.25mg/kg up to three times per day) and administered with a device that allows for accurate measurement. Tablets are unsuitable for use in these cases; liquid formulations are necessary.
Special Cases:
- Elderly Patients: Dose adjustment might be required. Start with a lower dose and monitor for side effects.
- Patients with Renal Impairment: Caution and potential dose reduction are necessary.
- Patients with Hepatic Dysfunction: Contraindicated in moderate to severe hepatic impairment. Caution is required in mild hepatic impairment.
- Patients with Comorbid Conditions: Careful evaluation of cardiovascular status is necessary, especially in patients with pre-existing cardiac conditions.
Clinical Use Cases
The primary use cases for Cinnarizine + Domperidone are focused on the management of vertigo, nausea, and vomiting, and not typically employed in clinical settings like intubation, surgical procedures, mechanical ventilation, or ICU. In emergency situations requiring management of nausea and vomiting, other agents may be more appropriate.
Dosage Adjustments
Dose adjustments are essential in patients with renal or hepatic impairment, as well as in elderly patients. It is crucial to consider drug interactions when determining the appropriate dosage.
Side Effects
Common Side Effects:
Drowsiness, dry mouth, headache, gastrointestinal discomfort (nausea, vomiting, abdominal pain), fatigue, weight gain, and indigestion are common side effects.
Rare but Serious Side Effects:
Extrapyramidal symptoms (especially with high doses of domperidone), cardiac arrhythmias (QT prolongation), and allergic reactions are rare but serious side effects.
Long-Term Effects:
The potential long-term effects of this combination are not fully established. However, prolonged use of domperidone has been associated with an increased risk of cardiac events.
Adverse Drug Reactions (ADR):
Significant ADRs include cardiac arrhythmias, extrapyramidal reactions, and hypersensitivity reactions. These require immediate medical attention.
Contraindications
Contraindications include hypersensitivity to either component, gastrointestinal bleeding or obstruction, prolactinoma, pheochromocytoma, moderate to severe hepatic impairment, and concomitant use of drugs that prolong the QT interval or strongly inhibit CYP3A4.
Drug Interactions
Cinnarizine + Domperidone can interact with various medications including:
- CNS Depressants: Alcohol, benzodiazepines, opioids (increased sedation)
- Anticholinergic Agents: Atropine, scopolamine (additive anticholinergic effects)
- Dopamine Agonists: Levodopa, bromocriptine (reduced efficacy of domperidone)
- CYP3A4 Inhibitors: Ketoconazole, erythromycin (increased domperidone levels)
- QT Prolonging Drugs: Amiodarone, haloperidol (increased risk of arrhythmias)
Interactions with food and lifestyle factors, such as alcohol and grapefruit juice (CYP3A4 inhibitor), should be considered.
Pregnancy and Breastfeeding
Cinnarizine + Domperidone should be used with caution during pregnancy and breastfeeding, and only if clearly necessary under strict medical supervision. Fetal risks and drug excretion in breast milk are potential concerns. Consult a doctor for potential safer alternatives.
Drug Profile Summary
- Mechanism of Action: Cinnarizine: Calcium channel blocker, antihistamine. Domperidone: Dopamine antagonist, prokinetic agent.
- Side Effects: Drowsiness, dry mouth, headache, gastrointestinal discomfort, extrapyramidal symptoms (rare).
- Contraindications: Hypersensitivity, GI bleeding, prolactinoma, severe hepatic impairment, QT prolonging drugs.
- Drug Interactions: CNS depressants, anticholinergics, dopamine agonists, CYP3A4 inhibitors, QT prolonging drugs.
- Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
- Dosage: Adults: 20mg/15mg tablet, 1 tablet 2-3 times a day. Children: weight-based calculation; liquid formulations only.
- Monitoring Parameters: Cardiac function (ECG), extrapyramidal symptoms.
Popular Combinations
Cinnarizine and domperidone are commonly combined for their synergistic effect in managing vertigo, nausea, and vomiting.
Precautions
Pre-screening for allergies, metabolic disorders, and organ dysfunction is advised. Pregnant/breastfeeding women, children, and elderly individuals require extra caution. Alcohol and driving restrictions should be communicated to patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cinnarizine + Domperidone?
A: Adults: One tablet (20mg cinnarizine + 15mg domperidone) 2-3 times a day, maximum three tablets/day. Children: 0.25mg/kg up to three times daily; consider liquid formulations.
Q2: What are the common side effects?
A: Drowsiness, dry mouth, headache, gastrointestinal issues (nausea, vomiting, abdominal pain) are common.
Q3: What are the serious side effects?
A: Cardiac arrhythmias (QT prolongation), extrapyramidal symptoms (rare), allergic reactions. Seek medical attention immediately if these occur.
Q4: Can I drive while taking this medication?
A: It’s advised not to drive or operate heavy machinery due to potential drowsiness.
Q5: Can pregnant or breastfeeding women take this medicine?
A: Use with caution during pregnancy/breastfeeding, only if the potential benefits outweigh the risks. Consult a doctor for guidance.
Q6: How should I take this medicine?
A: Orally, with or without food. If taken after meals, absorption of domperidone may be slightly delayed.
Q7: What should I do if I miss a dose?
A: Take the missed dose as soon as remembered, unless it’s nearly time for the next dose. Do not double the dose.
Q8: Can this medicine interact with other medications?
A: Yes, potential interactions exist with CNS depressants, anticholinergics, dopamine agonists, CYP3A4 inhibitors, and QT prolonging drugs. Inform your doctor about all other medications you are taking.
Q9: Can I consume alcohol while taking this medicine?
A: No. Avoid alcohol as it can increase dizziness and drowsiness.
Q10: How does Cinnarizine + Domperidone work for vertigo?
A: Cinnarizine stabilizes vestibular function by blocking calcium channels in the inner ear, reducing dizziness. Domperidone alleviates associated nausea and vomiting.
