Cinnarizine: English spelling of the antivertigo agent Cinnarizin
Cinnarizine is the English spelling of the substance Cinnarizin. It appears in English language literature, in many international brand names and in combination products. In Germany the spelling Cinnarizin is used. Pharmacologically it is the same drug, a hybrid substance with calcium channel blocking and H1 antihistaminic properties.
Cinnarizine has been used for over 60 years in vertigo of various origin, motion sickness and migraine prophylaxis. In some countries a combination with dimenhydrinate (Arlevert in Germany) is also available, particularly proven in vestibular vertigo.
Mechanism of action
Cinnarizine has several sites of action:
- Inhibition of voltage gated calcium influx in smooth muscle cells, particularly in the vasa nervorum of the inner ear
- Block of H1 histamine receptors with antihistaminic and antiemetic effect
- Modulation of vestibular function at brainstem level
- Weak inhibition of dopaminergic and serotonergic receptors
The combination of these effects makes cinnarizine effective in vestibular vertigo, motion sickness and migraine. Calcium channel block is weak compared with verapamil or nifedipine and cardiovascular relevance is small.
Cinnarizine is metabolised hepatically; the half life is about 4 to 5 hours, requiring multiple daily doses.
Indications
- Vestibular vertigo: in Ménière disease, vestibular migraine, vertebrobasilar insufficiency, peripheral vertigo of unclear origin
- Motion sickness (kinetosis): prevention and treatment
- Migraine prophylaxis: off label or in vestibular migraine
- Tinnitus: adjunctive in some patients with inner ear problems
- Peripheral arterial disease (PAD): historic indication, less used today
Dosing and administration
Vertigo: 25 mg three times daily, possibly stepped up to 75 mg per day. In acute symptoms a higher initial dose may be appropriate.
Motion sickness: 25 mg 30 minutes before travel, repeat every 6 to 8 hours during the journey if needed. Maximum 75 mg per day.
Children from 5 years: half the adult dose after individual evaluation.
Take with sufficient fluid, preferably after meals, to minimise gastrointestinal complaints.
Adverse effects
Common: sedation, fatigue, dizziness, headache, dry mouth, gastrointestinal complaints, weight gain.
Uncommon: rash, pruritus, sweating, tremor, depressive mood.
Rare and very rare: extrapyramidal symptoms (parkinsonism), particularly in older patients with longer therapy; lupus erythematosus like reaction, cholestasis, lichen planus.
Important points:
- Sedation impairs driving, particularly at the start
- Watch elderly patients on longer therapy for extrapyramidal symptoms
- Anticholinergic effects can be problematic in narrow angle glaucoma or prostatic hyperplasia
- Contraindicated in Parkinson disease because of symptom aggravation
Interactions
- Alcohol and CNS depressants: additive sedation, caution or avoid
- Tricyclic antidepressants, antipsychotics: additive anticholinergic and sedative effect
- Antihypertensives: possible additive blood pressure lowering
- L Dopa: antagonistic action, worsening of Parkinson symptoms
Special considerations
Pregnancy: limited data, use only with clear indication.
Breastfeeding: not adequately studied, so cautious.
Elderly: increased sensitivity, fall risk through sedation, risk of extrapyramidal symptoms with longer therapy. PRISCUS list classes cinnarizine as potentially unsuitable.
Contraindications: Parkinson disease, acute narrow angle glaucoma attacks, phaeochromocytoma, severe heart failure with cardiac decompensation.
Driving: impaired particularly at the start of therapy.
Patient communication: in chronic vertigo diagnostics should clarify the cause before symptomatic chronic therapy. In vestibular migraine modern options (triptans, antiemetics, migraine prophylactics) are often more suitable.
Related substances
- Cinnarizin, German spelling of the same substance
- Dimenhydrinate, classical antiemetic in motion sickness
- Betahistine, histamine analogue in Ménière disease
- Triprolidine, classical H1 antihistamine
- Sumatriptan, migraine therapeutic
Frequently asked questions
Cinnarizine or Cinnarizin?
English cinnarizine, German Cinnarizin. Identical substance with calcium channel blocking and H1 antihistaminic properties.
How does cinnarizine differ from dimenhydrinate?
Both are H1 antihistamines with antiemetic effect. Cinnarizine also has weak calcium channel block and acts directly on inner ear circulation. In vestibular vertigo a fixed combination of both (Arlevert) is often used, with study advantages over single agents.
Does cinnarizine help in migraine?
In vestibular migraine cinnarizine can be a useful option, particularly as prophylaxis. Data for pure migraine prophylaxis are limited; modern options such as topiramate, beta blockers, CGRP antibodies or onabotulinumtoxinA have more evidence.
Why not in Parkinson disease?
Cinnarizine has weak dopaminergic inhibition. In patients with Parkinson disease the substance can worsen symptoms or trigger drug induced parkinsonism. Use is therefore contraindicated.
Sources
- BfArM German Federal Institute for Drugs and Medical Devices
- EMA European Medicines Agency
- AWMF guidelines vertigo and migraine
- Gelbe Liste cinnarizine monograph
Legal notice and disclaimer
The information on this page is provided for general information only and does not constitute medical advice, diagnosis or treatment recommendation. It does not replace advice from a qualified physician or pharmacist. Medicines should only be used on prescription or after dispensing by a pharmacist. All information is based on the product information available at the time of writing and on recognised scientific sources; the manufacturer's current product information always prevails. Sanoliste assumes no liability for completeness, timeliness or accuracy of the information presented. In a medical emergency call the European emergency number 112.