Stugeron
Cinnarizine
Stugeron contains cinnarizine, an antihistamine and calcium channel blocker with a selective action on the balance organs of the inner ear. It is used to prevent motion sickness and to relieve vertigo of vestibular origin, including Meniere's disease. Its main limitations are drowsiness and, with prolonged use especially in older adults, drug-induced parkinsonism.
Ingredients & Drug Type
- Active ingredient
- Cinnarizine
- Therapeutic class
- Neurology
- Dosage form
- Tablet
- Strength
- 25mg
Overview
Cinnarizine is a piperazine derivative that combines H1 antihistamine activity with calcium channel blocking activity, and it also has weak dopamine D2 receptor blocking activity. It is grouped here among neurological medicines because it acts mainly on the vestibular system, the part of the inner ear and brain that senses movement and position. It is not marketed in the United States, so no US FDA label exists for it, and this monograph relies on established pharmacology and European and British product information.
The catalog product is Stugeron as a 25 mg oral tablet, with a catalog dosing pattern of one tablet three times daily. Other strengths of cinnarizine exist in other countries, so the tablet strength printed on the pack and the leaflet supplied with it should always be followed. The tablets are intended mainly for short-term use around travel and for symptomatic control of vertigo, and tablets of this kind may also contain lactose.
In treatment, cinnarizine is a symptomatic medicine and does not cure the underlying disorder. For motion sickness it works best as prevention taken before the journey, and it is much less effective once nausea and vomiting have started. For recurrent vertigo, the cause should be identified by a doctor, because dizziness without a clear trigger can arise from the ear, the nervous system, the heart or blood pressure. Whether the tablet can be supplied without a prescription depends on national regulation, and the catalog draft describes it as available without one, so the pharmacist should confirm the status that applies at the time of dispensing. The former US pregnancy category recorded in the catalog is C.
Mechanism of Action
Cinnarizine blocks voltage-gated calcium channels in the hair cells of the vestibular apparatus and in vascular smooth muscle. By limiting calcium entry into vestibular sensory cells, it reduces the excessive firing of the balance organ and the transmission of signals to the vomiting and balance centres in the brainstem. This is thought to account for its benefit in vertigo and in motion sickness, where conflicting sensory input from the eyes, ear and body overstimulates the system.
Cinnarizine also blocks histamine H1 receptors, which contributes to its antiemetic and sedative effects, and it has weak antimuscarinic activity. Its blockade of dopamine D2 receptors in the basal ganglia is weak but clinically relevant, because it explains the extrapyramidal movement symptoms that can appear with long-term use, particularly in older people. Its calcium channel blocking effect on blood vessels has been the basis for its older use in circulatory disorders.
Pharmacokinetics
- Absorption
- Cinnarizine is absorbed from the gut after oral administration, and peak plasma concentrations are reached about 1 to 4 hours after a dose. Absorption is better in an acidic stomach, which is one reason it may be taken after food.
- Onset and duration of action
- The effect against motion sickness is intended to be in place before travel begins, which is why the first dose is taken from half an hour to two hours beforehand. The action lasts for several hours, so doses are repeated every 6 to 8 hours when continued cover is needed.
- Distribution
- Cinnarizine is highly bound to plasma proteins and is lipophilic, so it distributes widely into tissues including the brain. This explains the central effects of drowsiness and, at higher exposure, movement disorders.
- Metabolism
- It is extensively metabolised in the liver, with the enzyme CYP2D6 playing an important part. Medicines that inhibit CYP2D6 can therefore increase exposure, and people who metabolise through this enzyme slowly may be more sensitive.
- Elimination half-life
- The elimination half-life varies considerably between individuals and is in the range of several hours. Prolonged dosing, impaired metabolism and older age may lengthen the time the drug remains in the body.
- Excretion
- Metabolites are eliminated mainly in the faeces, with a smaller share in the urine, and very little unchanged drug is excreted.
Indications
- Prevention of motion sickness
- Cinnarizine is taken before sea, road or air travel to reduce nausea, vomiting and dizziness. It is more useful when taken in advance than after symptoms have begun.
- Vestibular vertigo and Meniere's disease
- It is used for symptomatic relief of vertigo, nausea and vomiting caused by disorders of the balance system of the inner ear, including Meniere's disease. Treatment is usually given as regular doses over a limited period under medical supervision.
- Cerebral and peripheral circulatory disorders (older use)
- Some national labels list symptomatic treatment of cerebrovascular insufficiency and peripheral circulatory disturbances such as cold extremities. The evidence for these uses is limited, and they are now considered historical rather than first-line.
Dosage and Administration
The doses below are the usual doses given in product information for the 25 mg tablet, and the prescriber or pharmacist sets the actual dose for each person. The leaflet of the specific pack should always be followed, because national labels differ.
| Group or condition | Usual dose |
|---|---|
| Adults — vertigo of vestibular origin | The catalog regimen is 25 mg (one tablet) three times daily, which equals 75 mg in 24 hours, and some national labels allow higher daily doses, so the maximum stated in the leaflet must not be exceeded. |
| Adults — prevention of motion sickness | One 25 mg tablet is taken from half an hour to two hours before the journey and may be repeated every 6 to 8 hours during the journey, without exceeding the daily maximum in the leaflet. |
| Children 5 to 12 years — motion sickness | Half the adult dose is usually used, which is half a 25 mg tablet, taken before travel and repeated at the same intervals if needed. |
| Children under 5 years | Use is generally not recommended unless a doctor decides otherwise, and the dose must then be set by the doctor. |
| Older adults | The lowest effective dose is used for the shortest time, and regular long-term use is avoided because of the risk of parkinsonian symptoms. |
| Kidney or liver impairment | No specific dose adjustment is established, so a lower dose or longer interval may be chosen on medical advice and the leaflet should be consulted. |
How to take it
- Tablets are swallowed whole with water and are best taken after food to reduce stomach upset.
- For motion sickness, the first dose should be taken before leaving and not after nausea has started, because treatment is far less effective once vomiting has begun.
- For vertigo, the doses should be spaced evenly through the day, and treatment should be reviewed by a doctor if there is no improvement after a few weeks.
If you miss a dose: If a dose is missed, it should be taken as soon as remembered unless the next dose is almost due, in which case the missed dose is skipped. A double dose must not be taken to make up for it.
Overdose: Overdose can cause marked drowsiness, vomiting, low muscle tone, tremor and stiffness, and in children it can cause seizures and loss of consciousness. It is a medical emergency, and urgent hospital care is needed, as there is no specific antidote and treatment is supportive.
Pregnancy, Breastfeeding and Special Groups
- Pregnancy
- Human data are limited and adequate studies are lacking, and the former US category was C. Cinnarizine should be avoided in pregnancy unless the doctor considers the benefit to outweigh the risk.
- Breastfeeding
- It is not known whether cinnarizine passes into breast milk in significant amounts. It is generally avoided during breastfeeding, and the infant should be watched for excessive sleepiness if a doctor decides it is needed.
- Children
- Cinnarizine is used for motion sickness in children from 5 years of age at half the adult dose. It is not generally recommended in younger children, and children may show movement-related side effects.
- Older adults
- Older adults are more prone to drowsiness, falls, depression and drug-induced parkinsonism, which can appear after weeks or months of regular use. Short courses at the lowest dose are preferred, and use should be stopped if tremor, slowness or stiffness appears.
- Kidney impairment
- There is no established dose adjustment, and the drug is eliminated mostly as metabolites. Caution and a reduced dose are sensible in severe impairment, and the leaflet should be followed.
- Liver impairment
- Because cinnarizine is metabolised in the liver, exposure may be higher in liver disease. It should be used with caution and the dose may need to be reduced, and rare liver reactions have also been reported.
Contraindications
- Cinnarizine must not be used in people with known hypersensitivity to cinnarizine or to any ingredient of the tablet.
- Because it can worsen the movement disorder, it should be avoided in established Parkinson's disease, although some labels phrase this as use only if the benefit clearly exceeds the risk.
- It should not be given to young children outside the age limits stated in the leaflet.
- It should not be used in people with acute porphyria, because it is considered unsafe in this condition.
Warnings and Precautions
- Drug-induced parkinsonism
- Prolonged use, especially in older people, can cause tremor, rigidity, slowness of movement and sometimes depression. These features usually reverse after stopping, but recovery can take weeks to months, so treatment should be stopped and a doctor consulted if they appear.
- Drowsiness and driving
- Cinnarizine can slow reactions and cause sleepiness, particularly at the start of treatment. Driving, operating machinery and climbing should be avoided until the individual response is known.
- Undiagnosed or persistent vertigo
- Dizziness that is frequent, occurs without travel, or is accompanied by hearing loss, weakness, speech problems, severe headache or fainting needs medical assessment. Cinnarizine may mask symptoms of a more serious disorder and should not be used as a long-term daily treatment without a diagnosis.
- Anticholinergic effects
- Cinnarizine has mild atropine-like activity, so caution is needed in angle-closure glaucoma, prostatic enlargement with urinary retention and intestinal obstruction. Symptoms such as eye pain or difficulty passing urine should be reported.
- Skin allergy tests
- As an antihistamine, cinnarizine can suppress the skin reaction and give false-negative results. It should be stopped about 4 days before skin testing, as advised by the testing doctor.
- Masking of ototoxicity
- Antihistamine-type medicines can hide early signs of damage to the inner ear from ototoxic antibiotics such as aminoglycosides. Patients taking such treatment should report any new hearing change or ringing in the ears.
- Liver, kidney and epilepsy
- Caution is advised in people with liver or kidney disease and in those with epilepsy, as the dose may need adjustment and monitoring.
Side Effects
Common side effects
- Drowsiness is the most frequent effect, and it is reduced by taking the dose at night when possible and by avoiding driving.
- Headache and a feeling of heaviness or tiredness may occur, and they usually lessen as treatment continues.
- Dry mouth can occur, and sips of water or sugar-free gum can help.
- Mild stomach upset, nausea or heartburn may occur, and taking the tablet after food reduces it.
- Weight gain may develop with long-term use and should be discussed with the doctor if it is troublesome.
- Sweating and low blood pressure with dizziness may occur in some people.
Side effects that need urgent medical advice
- Tremor, stiffness, slowness of movement and abnormal movements of the face or limbs can indicate drug-induced parkinsonism, and the medicine should be stopped and a doctor consulted.
- Persistent low mood or depression has been reported, and it should be reported to a doctor.
- Allergic reactions with rash, swelling of the face or lips or difficulty breathing require urgent medical care.
- Yellowing of the skin or eyes, dark urine or severe upper abdominal pain may indicate liver injury, and the medicine should be stopped.
- Lichen-like or lupus-like skin eruptions have been reported rarely, and any new persistent skin eruption should be reviewed by a doctor.
Drug Interactions
| Medicine or class | Effect and what to do |
|---|---|
| Alcohol and sedatives | Alcohol, benzodiazepines, sleeping tablets and other central nervous system depressants increase drowsiness and impair coordination. They should be avoided or used with caution. |
| Levodopa and dopamine agonists | Cinnarizine may reduce the effect of medicines used in Parkinson's disease, and the combination should be avoided. |
| Antipsychotics and metoclopramide | Other dopamine-blocking medicines add to the risk of movement side effects, so they are used together only under medical supervision. |
| Tricyclic antidepressants and other anticholinergic medicines | Dry mouth, constipation, blurred vision and urinary difficulty may be increased when combined, and the combination is used with caution. |
| CYP2D6 inhibitors such as fluoxetine, paroxetine and quinidine | These medicines may raise cinnarizine levels and the risk of side effects, so a lower dose may be needed. |
| Other antihistamines | Taking another sedating antihistamine together may increase drowsiness and anticholinergic effects, and it is generally avoided. |
| Ototoxic medicines such as aminoglycosides | Cinnarizine may conceal early warning signs of inner-ear damage, so hearing should be monitored carefully. |
| Skin allergy tests | Cinnarizine reduces the skin response used in allergy testing, and it should be stopped several days beforehand. |
Food, Alcohol and Daily Life
- Alcohol should be avoided during treatment, as it increases drowsiness and may worsen dizziness.
- Driving and the use of machinery should be avoided until it is known how the medicine affects alertness.
- For travel, fresh air, looking at the horizon, sitting in a stable part of the vehicle such as the middle of a ship or over the wing of an aircraft, and avoiding heavy meals before the journey may help alongside the medicine.
Storage
The tablets should be stored at room temperature, below 25 degrees Celsius, in the original pack away from moisture and light.
They should be kept out of the sight and reach of children and should not be used after the expiry date.
Advice for Patients
- For travel, take the first dose before departure rather than waiting for nausea to start.
- Use it for occasional journeys or short courses, and do not turn it into a daily habit without a diagnosis.
- Report tremor, stiffness, slowed movement or low mood promptly, and stop the medicine if they develop.
- People over 60 should ask a doctor or pharmacist before using it regularly.
- Tell the doctor about all other medicines, especially sedatives, antidepressants and medicines for Parkinson's disease.
- Remember to stop the tablets about 4 days before any planned skin allergy test.
Frequently Asked Questions
When should Stugeron be taken for travel sickness?
The first dose is taken from half an hour to two hours before the journey so that it is active before the sensory conflict begins. Taking it after nausea has started is much less effective.
Can Stugeron be used every day?
It is intended for occasional use or for a limited course under medical advice. Daily use over months, particularly in older adults, raises the risk of tremor, stiffness and low mood.
Will Stugeron make me sleepy?
Drowsiness is common, particularly at first, so activities that need alertness should be avoided. Some people become less sleepy as treatment continues.
Is it safe in older people?
It can be used for short periods at the lowest effective dose, but regular long-term use is avoided because of the risk of drug-induced parkinsonism. A doctor or pharmacist should be asked before starting.
Can the movement symptoms disappear after stopping?
They usually improve after the medicine is stopped, but recovery may take weeks to months. A doctor should review persistent symptoms to exclude Parkinson's disease.
Does Stugeron treat ringing in the ears?
It is not an established treatment for tinnitus. Ringing in the ears needs medical assessment of its cause rather than self-treatment with this tablet.
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Trusted Medical Sources
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