Usage
This combination medication is primarily prescribed for the management of vertigo, a sensation of dizziness or spinning. It’s also used to alleviate symptoms associated with Ménière’s disease, such as nausea, vomiting, tinnitus (ringing in the ears), and balance problems. Additionally, it can be used to prevent and treat motion sickness.
Pharmacological Classification:
- Cinnarizine: Calcium channel blocker, antihistamine
- Dimenhydrinate: Antihistamine (H1 receptor antagonist), antiemetic
- Vitamin B6 (Pyridoxine): Vitamin, antiemetic
Mechanism of Action:
Cinnarizine works by preventing the constriction of blood vessels in the inner ear, improving microcirculation. Dimenhydrinate blocks the action of histamine, a chemical messenger responsible for motion sickness and vertigo symptoms. Vitamin B6 is thought to have anti-nausea properties and contribute to proper nerve function. The combination provides a multi-faceted approach to managing vertigo and related conditions.
Alternate Names
No internationally recognized non-proprietary name exists for this specific combination. Names are generally based on the constituent drugs.
Brand Names: Zipvert-B6, Cizinate, Dimezine (for Cinnarizine + Dimenhydrinate)
How It Works
Pharmacodynamics:
Cinnarizine improves blood flow in the inner ear, reducing vestibular stimulation. Dimenhydrinate acts centrally by blocking H1 receptors and muscarinic acetylcholine receptors, suppressing vestibular input and reducing nausea and vomiting. Vitamin B6 is involved in neurotransmitter synthesis and may contribute to reducing nausea.
Pharmacokinetics:
All three components are absorbed orally. Cinnarizine and dimenhydrinate are metabolized in the liver, primarily by CYP2D6. Cinnarizine is mainly excreted in feces, while dimenhydrinate is primarily excreted in urine. Vitamin B6 is water-soluble and excreted renally.
Mode of Action/Receptor Binding/Enzyme Inhibition:
Cinnarizine: Calcium channel blockade, H1 receptor antagonism, D2 receptor antagonism.
Dimenhydrinate: H1 receptor antagonism, muscarinic acetylcholine receptor antagonism.
Elimination Pathways:
Cinnarizine: Primarily fecal excretion.
Dimenhydrinate: Primarily renal excretion.
Vitamin B6: Renal excretion.
Dosage
Standard Dosage
Adults:
One tablet containing 20mg cinnarizine, 40mg dimenhydrinate, and 10mg vitamin B6, three times daily, taken after meals.
Children:
Not recommended for children under 5 years old. Dosage for older children should be determined by a physician based on weight and condition.
Special Cases:
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Elderly Patients: Start with a lower dose and adjust as needed. Monitor for drowsiness and confusion.
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Patients with Renal Impairment: Use with caution in mild to moderate impairment. Contraindicated in severe renal impairment (creatinine clearance ≤ 25 ml/min).
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Patients with Hepatic Dysfunction: Contraindicated in severe hepatic impairment. Use with caution in mild to moderate impairment.
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Patients with Comorbid Conditions: Caution in patients with glaucoma, prostatic hypertrophy, asthma, cardiovascular disease.
Clinical Use Cases
Dosage in specific clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations should be determined by the attending physician based on individual patient needs and condition. The standard dosage is typically used for vertigo and motion sickness management.
Dosage Adjustments
Dose adjustments should be made based on patient response and tolerance. Renal and hepatic impairment require careful consideration.
Side Effects
Common Side Effects:
Drowsiness, dry mouth, headache, stomach pain, nausea, indigestion, weight gain, sleepiness, dizziness, decreased blood pressure, weakness, impaired coordination, impaired concentration.
Rare but Serious Side Effects:
Allergic reactions, extrapyramidal symptoms, cholestatic jaundice, blood dyscrasias.
Long-Term Effects:
Potential for tolerance with prolonged use.
Adverse Drug Reactions (ADR):
Severe allergic reactions (anaphylaxis), agranulocytosis, hepatotoxicity.
Contraindications
Hypersensitivity to any component, angle-closure glaucoma, prostatic hypertrophy, urinary retention, pyloroduodenal obstruction, severe hepatic impairment, severe renal impairment, epilepsy, porphyria.
Drug Interactions
Alcohol, CNS depressants (barbiturates, benzodiazepines, opioids), anticholinergics (atropine), tricyclic antidepressants, antihypertensives, ephedrine, procarbazine, MAO inhibitors.
Pregnancy and Breastfeeding
Cinnarizine is category C; safety not established. Dimenhydrinate is generally considered safe in small doses, but larger doses may cause infant drowsiness. Vitamin B6 is considered safe. Consult a physician before use during pregnancy or breastfeeding.
Drug Profile Summary
- Mechanism of Action: See above.
- Side Effects: See above.
- Contraindications: See above.
- Drug Interactions: See above.
- Pregnancy & Breastfeeding: Consult a physician.
- Dosage: See above.
- Monitoring Parameters: Blood pressure, liver function tests, renal function tests.
Popular Combinations
This combination itself is a popular formulation for managing vertigo and related symptoms.
Precautions
See contraindications and drug interactions. Avoid alcohol. Use caution in driving or operating machinery. Monitor for drowsiness, especially in elderly patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cinnarizine + Dimenhydrinate + Vitamin B6?
A: The standard adult dose is one tablet (20mg cinnarizine, 40mg dimenhydrinate, 10mg vitamin B6) three times daily, taken after meals.
Q2: Can this combination be used in children?
A: It is not recommended for children under 5. Older children’s dosages must be determined by a physician.
Q3: What are the common side effects?
A: Drowsiness, dry mouth, headache, and gastrointestinal upset are common.
Q4: Is it safe to drive while taking this medication?
A: Use caution as drowsiness may impair driving ability.
Q5: What are the contraindications to using this medication?
A: Contraindications include hypersensitivity, glaucoma, prostatic hypertrophy, severe hepatic or renal impairment, and epilepsy.
Q6: Can this medication be used during pregnancy or breastfeeding?
A: Consult a physician before use during pregnancy or breastfeeding.
Q7: How long can I take this combination?
A: The duration of treatment should be determined by a physician but is generally not recommended for extended periods beyond 4 weeks without reassessment.
Q8: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it is close to the time for your next dose. Do not double the dose to catch up.
Q9: Does this medication interact with alcohol?
A: Avoid alcohol while taking this medication as it can increase drowsiness and other side effects.