Cinnazine

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Cinnazine

Quick Facts

Property Description
Active ingredient Cinnarizine (INN)
Form Tablet (Oral)
Pharmacological Class Antihistamine; Calcium Channel Blocker
General Purpose Anti-Vertigo Agent
Origin Synthetic Compound

Cinnazine: Core Identity and Composition (Synthetic Origin)

Cinnazine is the trade name for a medicine containing the active ingredient Cinnarizine, an International Nonproprietary Name (INN). This substance is a synthetic chemical compound, meaning it is laboratory-derived, and is primarily formulated as an oral tablet for systemic administration. Cinnarizine is chemically defined by its piperazine structure.

What Pharmacological Class Does Cinnarizine Belong To?

Cinnarizine is classified within two distinct pharmacological classes: it acts as a First-generation Antihistamine and, more significantly, a non-specific Calcium Channel Blocker. Although its chemistry aligns with the antihistamine class, its primary physiological action stems from its ability to modulate calcium ion movement, distinguishing it as a potent vasoactive agent. It is classified as an antivertigo preparation.

The General Purpose of Cinnarizine (Anti-Vertigo Agent)

The general purpose of Cinnarizine is to serve as an Anti-Vertigo Agent and a Labyrinthine Suppressant. It functions by calming the over-activity, or vestibular excitability, of the balance system located in the inner ear. This mechanism is primarily achieved through its calcium channel blocking properties, which also improve localized blood flow. Cinnarizine is used for the symptomatic treatment of vestibular vertigo, demonstrating its core therapeutic utility in reducing sensations of disequilibrium.

What side effects are possible with Cinnazine?

Possible Side Effects and Safety Information

The safety profile of Cinnarizine is formally documented across several System Organ Classes, with effects classified by frequency based on regulatory standards (e.g., EMA/ICH frequency bands) derived from clinical trial data and post-marketing surveillance.

Common Adverse Reactions

Adverse reactions classified as Common (occurring in ge 1/100 to < 1/10 patients) primarily involve the Nervous System and Gastrointestinal systems. The most frequently reported reactions are Somnolence (drowsiness) and gastrointestinal issues such as Nausea and Dyspepsia. Somnolence is noted to be more noticeable at the start of treatment. Weight Increased is also commonly documented within the Investigations System Organ Class.


Officially Documented Uncommon and Serious Reactions

Other reactions may include Headache, Vomiting, Fatigue, and effects on the skin like Lichen planus or a Rash (classified as Uncommon or Not Known frequency).

Clinically significant, serious adverse reactions documented in regulatory materials include the risk of Extrapyramidal symptoms (such as Parkinsonism and Tremor), which is specifically associated with long-term use, particularly in older adults. Rare occurrences of Hypersensitivity reactions and Cholestatic Jaundice are also officially listed.


Safety Considerations for Specific Populations

Cinnarizine must be used with caution in patients with documented hepatic impairment or renal insufficiency. It should be avoided in patients with the genetic disorder porphyria. For patients with pre-existing Parkinson's disease, the medicine carries the risk of aggravating the condition. Furthermore, the concurrent use of alcohol or other Central Nervous System depressants may potentiate the sedative effects of Cinnarizine.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory documents describe the manifestations of Cinnarizine overdose, requiring immediate professional attention.

Documented Manifestations and Severe Outcomes

Overdosage may lead to acute effects on the central nervous system (CNS). Documented clinical manifestations include changes in consciousness, ranging from somnolence (drowsiness) to stupor and coma. Other signs include vomiting, hypotonia (low muscle tone), and extrapyramidal symptoms (movement disorders). These signs are primarily attributed to the drug’s documented anticholinergic activity. Overdose has been reported with ingested amounts between 90 mg and 2,250 mg. Severe outcomes, including fatalities, have been documented in regulatory sources following both single and polydrug overdoses. A specific risk noted in official labeling is the development of seizures (convulsions) in a small number of young children following overdosage.

Emergency Action and Treatment

Urgent medical attention is required for any suspected overdose. Regulatory guidance explicitly states that no specific antidote is known for Cinnarizine poisoning. Therefore, the mandated response is symptomatic and supportive care. Officially described procedures include the use of gastric lavage and the administration of activated charcoal to help manage the absorption of the drug. Contacting a poison control centre is advised to obtain the latest recommendations for management.

Therapeutic Uses of Cinnazine

Main Uses and Symptom Support

Cinnarizine is commonly used to help with conditions involving symptoms related to systemic imbalance and acute or disruptive episodes, particularly those affecting the inner ear and balance system. It is used in contexts involving heightened systemic burden, supporting the management of symptoms such as vertigo, dizziness, tinnitus, and those associated with motion sickness.

The medicine is commonly used across conditions presenting with acute episodes, which can include symptom patterns seen in conditions such as Ménière's disease. It helps address symptom clusters that may become intense or disruptive, often used during phases when symptoms become more noticeable.

“It provides support that helps ease the overall symptom burden, assisting patients in coping more steadily with difficult episodes.”

It assists with maintaining functional stability and contributes to improved day-to-day comfort during symptomatic periods.


Quick Fact: Symptom Support for Balance Issues


Eligibility and Restrictions for Use

Official Eligibility and Contraindications

Regulatory documents define specific population eligibility for Cinnazine (Cinnarizine). Use is generally established for adults and children aged 5 years and over for labeled conditions. However, several mandatory restrictions and cautionary requirements exist.

Absolute Contraindications

Cinnazine is contraindicated in patients with known hypersensitivity to cinnarizine or its components. It must also not be given to premature infants or neonates. Furthermore, its use should be avoided in patients diagnosed with Porphyria or those with specific hereditary intolerances (e.g., lactose or galactose intolerance) due to excipient content.

Restricted and Conditional Use

  • Parkinson's Disease: The medicine should only be given if the benefits outweigh the risk of aggravating the disease.
  • Age: Use is not recommended for children under 5 years old, and elderly patients require particular caution due to increased susceptibility to certain effects.
  • Organ Function: Use requires care in patients with hepatic insufficiency and renal insufficiency (liver and kidney problems).
  • Physiological States: The safety of Cinnarizine in human pregnancy has not been established, and its use is not recommended for nursing mothers due to a lack of data on excretion in breast milk.
  • Comorbidities: Caution is required for patients with conditions like primary angle closure glaucoma or urinary retention.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile for Cinnarizine is primarily defined by documented pharmacodynamic potentiation and official procedural constraints as outlined in regulatory sources.

Pharmacodynamic Interactions

Co-administration with other medicinal products may result in additive or enhanced effects, based on regulatory statements:

  • Central Nervous System (CNS) Depressants: Concurrent use with drugs such as tricyclic antidepressants, opioids, hypnotics, and sedatives may potentiate the sedative effects of Cinnarizine.
  • Antimuscarinic Drugs: The drug exhibits an additive antimuscarinic action when co-administered with other medicines that have anticholinergic properties.
  • Ototoxic Drugs: Cinnarizine may mask the warning signs of damage caused by ototoxic drugs, such as certain aminoglycoside antibiotics.

Restrictions and Procedural Constraints

Official regulatory guidance specifies certain substances and procedures to avoid due to interaction risks:

Substance or Procedure Official Restriction Outcome of Interaction
Alcohol Must be avoided Potentiation of sedative effects.
Dermal Reactivity Indicators (Allergy Tests) Avoid for 4 days prior to testing May prevent a positive reaction by masking results.

Certain official databases also note that Cinnarizine may affect the metabolism of specific co-administered drugs, such as Ouabain, leading to a potential rise in the serum concentration of the co-administered drug. Elderly patients are also noted to be more susceptible to the sedative effects of these interactions.

Mechanism of Action

Peripheral Labyrinthine Stabilization via Calcium Channel Blockade

The core mechanism of Cinnarizine involves non-competitive blockade of Voltage-Gated Calcium Channels ( VGCC), particularly the L- and T-types, primarily localized to the vestibular hair cells within the inner ear. Restricting the flow of Ca^2+ ions into these sensory cells limits the release of excitatory neurotransmitters, resulting in stabilization of peripheral vestibular cell activity. This mechanism directly reduces the rate of afferent signal transmission that often characterizes cellular excitability in the labyrinth.


Central Suppression of Vestibular and Autonomic Signaling

Cinnarizine acts as a competitive antagonist at multiple receptor sites in the brainstem, including Histamine H1, Dopamine D2, and Muscarinic Acetylcholine receptors ( AChR). By occupying these central receptors, the drug suppresses the key neurotransmitter systems responsible for receiving, processing, and relaying motion signals, initiating modulation of central vestibular activity. This central signal suppression facilitates a reduction in autonomic output associated with high sensory input.


Modulation of Vascular Tone and Localized Microcirculation

In addition to its neural effects, the VGCC blockade mechanism extends to the vascular smooth muscle cells in the walls of local blood vessels. By reducing the intracellular Ca^2+ needed for muscle contraction, Cinnarizine exerts a selective anti-vasoconstrictor effect. This action, coupled with increased erythrocyte deformability, modulates local vascular resistance and the cellular response to hypoxia, a consequence of the anti-vasoconstrictor mechanism.

Dosage and Administration Information

Cinnarizine is administered strictly via the oral route, primarily using the 15 mg or 25 mg tablet forms or a 75 mg capsule. The required dosage and frequency are defined by the clinical context. For ongoing administration related to vestibular disorders, the standard regimen is typically 25 mg taken three times daily, or a single 75 mg dose once a day. For motion sickness prophylaxis, an initial dose of 25 mg to 30 mg is taken prior to the journey, with a lower maintenance dose repeated every 6 to 8 hours as needed during travel, ensuring an 8-hour minimum interval between doses.

All doses should preferably be taken after meals to mitigate potential gastric irritation. The maximum recommended daily dosage must not exceed 225 mg.

Key Dosing Patterns (Adults 12 years and older)

Condition Adult Regimen Children (5–12 years)
Vestibular/Balance 25 mg three times daily, or 75 mg once daily Half the adult dose
Motion Sickness 25 mg initial dose, repeated every 6-8 hours Half the adult dose

Use for chronic balance issues may require continuous administration for several months. The use of this medication in children under 5 years is generally not recommended.

Recent Clinical Evidence

Cinnazine: Recent Clinical Evidence


Evidence for Use in Vestibular Vertigo and Labyrinthine Disorders

Research on Cinnarizine was evaluated in conditions characterized by functional imbalance, such as vestibular vertigo and symptoms linked to labyrinthine disorders. Studies examined trials, including Randomized Controlled Trials (RCTs) and comprehensive Systematic Reviews, that included adults and older adults. Researchers monitored several outcomes related to systemic or functional imbalance, such as patient-reported scores for vertigo intensity and nausea. The findings describe patterns observed in the studies where Cinnarizine was administered during episodic or acute changes in vertigo symptoms. However, long-term outcomes are not fully established, as follow-up durations were typically short (between one and two months). Research also explored outcomes for generalized dizziness and tinnitus intensity as secondary measures, where the findings were mixed and the certainty remains low due to reliance on small study sizes.


Evidence for Use in Motion Sickness Prevention

Cinnarizine was evaluated in trials related to motion. Studies were often short-term RCTs involving healthy adult volunteers, primarily in controlled settings. The research examined outcomes describing episodic or acute changes such as the incidence and severity of nausea and vomiting, and subjective discomfort scores over brief periods. The research highlights changes measured during the study period after a single dose. Because motion sickness is an acute, temporary state, the follow-up durations were short, restricted to the span of the travel or simulation (typically a few hours). The results apply only to the populations studied, which were often healthy volunteers, not patient groups with pre-existing conditions.


What is Still Uncertain About Cinnarizine Research

The research base still contains several clear gaps. The consistency of findings varies across studies, particularly between those evaluating Cinnarizine alone versus those evaluating fixed-dose combinations, making the interpretation of research for the single agent more challenging. Data for certain specific groups, such as pregnant or breastfeeding individuals, is generally limited, meaning subgroup findings are uncertain.

Frequently Asked Questions (FAQ)

Common questions about Cinnazine (FAQ)

Q: How quickly should someone expect to feel the effects of Cinnazine?

According to official product information, the concentration of Cinnazine in the bloodstream typically reaches its highest level between 1 and 3.4 hours after the medicine is taken. This measurement indicates when the drug is most concentrated in the body following administration.

Q: Is Cinnazine a type of antihistamine, and if so, how is it different from others?

Official classifications define Cinnazine as a First-generation Antihistamine. However, the medicine's main therapeutic benefit for balance problems and motion sickness stems from its property as a selective Calcium Channel Blocker. This dual function, which helps control calcium movement in the inner ear, is what distinguishes its primary physiological action.

Q: What are the most commonly reported side effects of Cinnazine in patient forums?

Official safety surveillance data classifies the most commonly reported adverse reactions based on clinical trials and post-marketing reports. These common effects include drowsiness, nausea, indigestion (dyspepsia), and an increase in body weight. Regulatory bodies use this official data to inform patients, rather than relying on unofficial patient forum reports.

Q: Are there any known food or drink interactions with Cinnazine?

Official product information advises taking the medicine after meals to help minimize the possibility of stomach irritation. Official warnings state that alcohol should be avoided during the use of Cinnazine because it can significantly increase the sedative (drowsiness) effects of the drug. Specific interactions with general food groups or non-alcoholic drinks are typically not noted in regulatory documents.

Q: Does taking Cinnazine affect blood pressure readings?

Official product information describes the medicine as having vasodilatory effects, meaning it can cause blood vessels to widen. Because of this action, regulatory documents state that caution is necessary when the medicine is given to patients who have existing low blood pressure, known as hypotension.

Q: Can Cinnazine be taken with vitamin supplements or herbal remedies?

Regulatory guidance indicates that caution is necessary concerning herbal remedies or supplements, particularly those that may independently cause effects like sleepiness or dry mouth. Since Cinnazine can cause similar effects, the combined use could increase these adverse reactions (potentiation).

Q: Is it normal to feel a dry mouth while taking Cinnazine?

Yes, dry mouth is an officially documented adverse effect associated with Cinnazine. Regulatory safety data classifies this effect as uncommon or rare, meaning it does not occur frequently in patients using the medicine.

Q: Do I need a prescription to get Cinnazine in most places?

The availability of Cinnazine varies globally. In many regions, the medicine is available both on prescription and for direct purchase over-the-counter (OTC) in pharmacies. This usually depends on the strength of the tablet and whether it is being used to manage a short-term issue, like motion sickness, or a chronic condition.

Q: What does the research say about Cinnazine's use in Meniere's disease?

Regulatory documents and official product information indicate Cinnazine's use for controlling the symptoms associated with vestibular disorders. This includes symptoms related to conditions like Ménière’s disease, specifically addressing issues such as vertigo, tinnitus, nausea, and vomiting.

Q: Why are people with certain heart conditions advised to avoid Cinnazine?

Official safety documents state that caution is necessary for individuals with existing low blood pressure (hypotension). This is due to the medicine's vasodilatory mechanism, which causes blood vessels to relax and widen, potentially lowering blood pressure further.

Q: What should I do if I suspect an allergic reaction to Cinnazine?

Regulatory documents note that hypersensitivity (severe allergic reaction) is a rare but documented adverse reaction to Cinnazine. Official guidance states that, in the event of a suspected allergic reaction, emergency medical attention is required.

Q: Does Cinnazine cause weight gain, according to user reports?

Official regulatory safety data, collected from clinical trials and surveillance, lists "Weight Increased" as a Common adverse reaction. This documentation provides the factual basis for reporting this effect, regardless of user-reported experiences online.

Q: Does Cinnazine interact with blood thinners?

Regulatory information indicates that Cinnazine may interact with certain blood thinners, also known as anticoagulants, by influencing how the body processes those medicines (their metabolism). Regulatory information emphasizes that professional guidance is needed to manage co-administration and monitor the combined effects.

Q: How long can a person safely take Cinnazine for a chronic issue?

For chronic balance issues, administration may continue for several months, as mentioned in official guidelines for long-term use. However, official safety documents specify that the risk of certain serious side effects, such as movement disorders (Extrapyramidal symptoms), is specifically associated with long-term use, particularly in older individuals.

Q: What is the role of Cinnazine in treating circulation disorders?

In some regulatory jurisdictions, Cinnazine is indicated for controlling the symptoms of Peripheral Circulatory Disorders. This use is based on its anti-vasoconstrictor property, which helps to relax and widen blood vessels to modulate local blood flow.

Q: Does Cinnazine cause insomnia or affect sleep patterns?

The commonly documented effect Cinnazine has on the nervous system is Somnolence, which is a state of strong drowsiness or sleepiness. Regulatory documents state this is a common side effect, especially at the start of treatment. Insomnia (difficulty sleeping) is not listed as an official adverse reaction.

Q: Does Cinnazine interact with medications for diabetes?

Official interaction warnings note that Cinnazine may increase the risk of developing low blood sugar, a condition known as hypoglycemia, when combined with certain medications used for diabetes. This risk is specifically noted for a class of antidiabetic agents called sulfonylureas.

Q: Does Cinnazine interact with caffeine?

Official drug interaction information notes that combining Cinnazine with caffeine may decrease the rate at which the body processes the medicine (its metabolism). This interaction could potentially alter the concentration of Cinnazine in the body, affecting its function.

Q: Are there genetic factors that affect how people respond to Cinnazine?

Official drug characteristics indicate that Cinnazine is processed extensively by a specific liver enzyme known as CYP2D6. This enzyme is known to have genetic variations in the human population, which can lead to considerable differences in how quickly and effectively the body metabolizes the medicine from person to person.

Q: Do regulatory bodies classify Cinnazine as high-risk during therapeutic use?

Regulatory bodies do not use a single, defined 'high-risk' classification term for Cinnazine. Instead, they provide specific warnings that require caution for certain patient populations, such as older adults, individuals with pre-existing Parkinson's disease, and those with impaired liver or kidney function.

Q: Why is Cinnazine often sold over the counter?

In regions where Cinnazine is sold over-the-counter (OTC), this is typically based on its classification for treating acute, self-limiting conditions, such as the temporary symptoms of motion sickness. However, official regulations may require a prescription for its use in chronic or long-term vestibular conditions.

How should Cinnazine be stored and disposed of?

Storage Requirements

Cinnarizine tablets must be stored according to regulatory requirements to preserve product stability. The medicine must be kept at a maximum temperature not exceeding 25 C to 30 C and in a cool dry place. It is required that the product be protected from light and stored in its original package. For safety, the product must be kept out of the reach and sight of children.

Disposal Instructions

Disposal must adhere to specific non-household waste protocols. Unused or expired Cinnarizine must not be thrown away via wastewater or standard household waste. Disposal must be conducted in accordance with local regulations as advised by a pharmacist, which typically involves taking the medicine to a designated collection point.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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