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Sunday, July 27, 2025

Cinnarizine


Cinnarizine is a first-generation antihistamine with additional calcium channel blocking properties. It is primarily used to manage motion sickness, nausea and vomiting, labyrinthine disorders, and peripheral vestibular vertigo such as that seen in Ménière’s disease. While not approved in some countries like the United States, it remains widely used in Europe, Asia, and the Middle East, either alone or in combination with dimenhydrinate for enhanced vestibular control.

This professional reference outlines the pharmacological profile of cinnarizine, including its classification, mechanism of action, indications, dosages, contraindications, side effects, precautions, and drug interactions.

Pharmacological Classification

  • Therapeutic Class: Antivertigo agent, antiemetic

  • Pharmacological Class: First-generation H1-antihistamine

  • ATC Code: N07CA02

  • Other properties: Calcium channel antagonist, vestibular suppressant

Brand Names

  • Stugeron® (Janssen)

  • Stugeron Forte®

  • Cinzan®, Cinnabloc®, Arlevert® (with dimenhydrinate)

  • Cinnageron, Cinnadiz, Cinnarizine Actavis (various generics)

Mechanism of Action

Cinnarizine acts through two main pharmacological pathways:

1. Histamine H1 Receptor Antagonism

  • Blocks H1 receptors in the vestibular nuclei and vomiting center in the brainstem

  • Reduces nausea, vomiting, and dizziness associated with motion sickness and inner ear disorders

2. Calcium Channel Blocking Activity

  • Inhibits L-type voltage-gated calcium channels in smooth muscle and neurons

  • Leads to vasodilation, improved cerebral and peripheral blood flow, and reduction of labyrinthine excitability

  • Reduces abnormal vestibular stimulation in conditions like Ménière’s disease

These dual actions make cinnarizine effective in controlling both peripheral and central vestibular symptoms.

Indications and Clinical Uses

Approved Indications

  • Motion sickness prevention and treatment

  • Vertigo of central or peripheral origin

  • Ménière’s disease (and other vestibular disorders)

  • Labyrinthitis, vestibular neuritis

  • Nausea and vomiting from various causes

  • Peripheral circulation disorders (off-label)

  • Cerebral vascular insufficiency (off-label in some regions)

Off-label/Adjunctive Uses

  • Migraine-related vertigo

  • Travel-induced nausea

  • Visual vertigo (motion sensitivity)

Dosage and Administration

Adults

Motion Sickness

  • Tablet: 15–30 mg taken 2 hours before travel, then every 8 hours as needed

  • Maximum: Usually 90 mg/day

Vertigo / Labyrinthine Disorders

  • 25–30 mg three times daily

  • Onset of relief may take several days to weeks

Ménière’s Disease

  • 30 mg three times daily, long-term use may be required

  • Periodic assessment is advised

Children (over 5 years)

  • Half the adult dose, i.e., 15 mg three times daily

  • For motion sickness: 15 mg 2 hours before travel, then every 8 hours if needed

Note: Cinnarizine is not recommended in children under 5 years unless directed by a specialist.

Pharmacokinetics

  • Absorption: Oral, peak plasma levels at 2–4 hours

  • Bioavailability: ~80%

  • Protein Binding: High (~91%)

  • Metabolism: Hepatic (via CYP enzymes, including CYP2D6)

  • Half-life: 3–6 hours

  • Excretion: Mainly fecal (via bile); minor renal excretion

Contraindications

  • Hypersensitivity to cinnarizine or other antihistamines

  • Parkinson’s disease or extrapyramidal disorders

  • Porphyria

  • Hepatic insufficiency (relative)

  • Children <5 years (due to risk of CNS effects and extrapyramidal symptoms)

Precautions and Warnings

  • Sedation: Causes drowsiness and reduced alertness; caution with driving or machinery

  • Parkinsonism risk: Can worsen symptoms; avoid long-term use in susceptible individuals

  • Elderly patients: More prone to sedation, falls, and anticholinergic side effects

  • Liver dysfunction: Monitor if prolonged use is necessary

  • Alcohol use: Potentiates CNS depression

  • QT prolongation: Theoretical risk; use with caution in patients on QT-prolonging drugs

  • Pregnancy and lactation: Use only if clearly necessary; insufficient data available

Adverse Effects

Common

  • Drowsiness, sedation

  • Dry mouth, blurred vision

  • Gastric upset, nausea, epigastric discomfort

  • Weight gain (long-term use)

Less Common

  • Headache, dizziness

  • Extrapyramidal symptoms (especially with prolonged use):

    • Tremor, bradykinesia

    • Parkinsonism-like symptoms

    • Dyskinesia

  • Hypotension (rare)

  • Hepatic enzyme elevations

Rare

  • Allergic reactions: rash, urticaria

  • Agranulocytosis (extremely rare)

  • Jaundice, hepatitis-like symptoms

Drug Interactions

CNS Depressants

  • Alcohol, benzodiazepines, opioids, barbiturates

  • Potentiates sedative and depressant effects

Anticholinergic Drugs

  • Additive effects with atropine, tricyclic antidepressants, antipsychotics

  • May cause increased dry mouth, blurred vision, urinary retention

Parkinson’s Medications

  • Antagonizes the effects of levodopa, dopamine agonists

  • May worsen Parkinsonian symptoms

QT-Prolonging Agents (use with caution)

  • Macrolide antibiotics, quinolones, antipsychotics, antiarrhythmics

CYP2D6 Substrates/Inhibitors

  • Potential interactions with SSRIs, beta-blockers, antidepressants

Pregnancy and Lactation

Pregnancy

  • Category C (not formally assigned in most jurisdictions)

  • Animal studies are limited

  • Use only if potential benefits justify potential risks

Lactation

  • Unknown if excreted in human milk

  • Avoid use unless advised by a physician

Patient Counseling Advice

  • Take cinnarizine after food to reduce gastric upset

  • For motion sickness, take dose 2 hours before travel

  • May cause drowsiness: avoid driving, operating machinery

  • Avoid alcohol and other CNS depressants

  • Report any symptoms of tremor, rigidity, or slowness of movement

  • For long-term therapy, monitor for neurological and hepatic side effects

Clinical Notes

  • Cinnarizine is often used in combination with dimenhydrinate (e.g., Arlevert) for improved control of vertigo and nausea

  • Its use is more prevalent in Europe, the Middle East, and Asia, and it is not approved in the U.S.

  • Compared to meclizine or betahistine, cinnarizine may be more sedating

  • Long-term use in elderly patients should be reviewed regularly to minimize extrapyramidal risk




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