Циннаризин

Quick links

Choose a section

Quick links to important sections

Advertisements

Циннаризин

Selected form

Advertisements
Advertisements

Overview of Циннаризин

What is Циннаризин? (Cinnarizine)

The following overview defines Циннаризин, detailing its composition, origin, and general classification, strictly adhering to factual data and excluding specific dosage or treatment protocols.


Property Description
Active Ingredient Cinnarizine (INN)
Form Primarily oral tablets
Pharmacological Class Calcium channel blocker and H1 receptor antagonist
General Purpose To manage symptoms of dizziness and unsteadiness
Origin Synthetic chemical compound

What Type of Medicine is Циннаризин?

Циннаризин is a synthetic medicinal substance chemically defined as a diarylmethylpiperazine derivative that functions as both a selective calcium channel blocker and a first-generation antihistamine (H1 receptor antagonist). Its structure is derived from piperazine, which it shares with related compounds. It is predominantly manufactured for the oral route of administration, typically as tablets containing the single active ingredient, Cinnarizine, combined with standard pharmaceutical excipients. Cinnarizine is classified as an anti-vertigo agent, meaning the medication is specifically utilized for its targeted action on the balance system to help stabilize the sense of equilibrium.

General Purpose: Why is Циннаризин Used?

Циннаризин is utilized for its capacity to stabilize the body's sense of balance and reduce feelings of dizziness or unsteadiness often associated with inner ear dysfunction. The drug is categorized as a vestibular suppressant due to its ability to modulate the responsiveness of the inner ear's organs to movement. Furthermore, Cinnarizine acts as a selective cerebral vasodilator, improving microcirculation in areas critical for equilibrium, such as the labyrinth. This dual action helps alleviate symptoms arising from vestibular hyperactivity, such as those experienced during motion or disequilibrium.

Regulatory References

  1. U.S. National Library of Medicine
Advertisements

What side effects are possible with Циннаризин?

Possible Side Effects and Safety Information

The safety profile of Cinnarizine (Циннаризин) is based on official government regulatory classifications, detailing adverse reactions by frequency and physiological system affected.


Frequency-Classified Adverse Reactions

Adverse effects are categorized by their documented incidence rate in clinical use, based on regulatory standards:

  • Common (may affect up to 1 in 10 people): Somnolence (drowsiness) and Headache.
  • Uncommon (may affect up to 1 in 100 people): Dry Mouth and Weight Gain.

System-Organ Class and Serious Reactions

The drug's side effects are grouped by the physiological system affected, which includes Nervous System Disorders and Gastrointestinal Disorders. The official labeling highlights certain reactions as clinically significant:

  • Nervous System Concerns: Extrapyramidal Symptoms (e.g., tremor, rigidity, involuntary movements) and Dyskinesia are documented as serious adverse reactions. These effects are often observed at the beginning of treatment or at higher doses, with Dyskinesia specifically associated with long-term use.
  • Other Serious Reactions: Cholestatic Jaundice (a rare hepatic reaction) and Hypersensitivity Reactions are also listed in regulatory documents.

Population-Specific Safety Considerations

Regulatory documents include specific safety notes for certain patient populations:

  • Older Adults: This group has an officially documented increased risk of developing Extrapyramidal Symptoms during treatment.
  • Other Constraints: The use of Cinnarizine may worsen symptoms in patients with Parkinson's Disease. Caution is also specified for patients with pre-existing hypotension (low blood pressure) and in cases of severe hepatic impairment.

Safety-Related Restrictions

Official labeling notes that the substance may potentiate the effects of alcohol and other central nervous system (CNS) depressants, and it should not be used in individuals with a known allergy to Cinnarizine or its excipients.

Advertisements

Overdose and Emergency Response

Overdose and When to Seek Help

The officially documented profile for Циннаризин (Cinnarizine) overdose highlights a range of central nervous system and gastrointestinal effects, underscoring the need for immediate medical attention if an overdose is suspected.

Documented Overdose Presentations

Acute overdoses have been reported involving doses from 90 mg up to 2,250 mg. The primary clinical manifestations documented in regulatory sources are related to the drug's anticholinergic activity and include:

  • Consciousness Alterations: Symptoms may range from somnolence (drowsiness) to stupor and, in severe cases, coma.
  • Gastrointestinal Effects: Vomiting is a common presentation.
  • Neurological Signs: Extrapyramidal symptoms (involuntary movement disorders) and hypotonia (reduced muscle tone) have been observed.

Critical Risk Factors and Emergency Action

While most overdose cases have not been classified as severe, regulatory data confirms that deaths have been reported following both single-drug and polydrug overdoses. A small number of young children who experienced an overdose also developed seizures, marking a specific pediatric risk.

There is no specific antidote for Циннаризин overdose. Treatment is restricted to symptomatic and supportive care aimed at managing the patient's symptoms and maintaining vital functions.

When to Seek Immediate Medical Help

Immediate contact with a hospital emergency department or a medical doctor is required if it is suspected that you or someone else has swallowed a large number of tablets, or if a child is thought to have ingested any amount of the medication. This urgent response is necessary to ensure timely supportive measures are initiated to prevent potentially serious complications.

Advertisements

Therapeutic Uses of Циннаризин

What Циннаризин Treats: Main Uses and Benefits

Циннаризин is commonly used for managing symptoms across key therapeutic domains where disturbances in the balance system may lead to heightened distress and noticeable physiological strain. In clinical settings, it is generally applied when there is a need for short-term symptomatic assistance and symptom stabilization.

The therapeutic role of Циннаризин is relevant for managing symptoms and contributes to easing the overall symptom load in conditions characterized by episodic or fluctuating manifestations. It is commonly used to help with conditions such as Ménière's disease and other labyrinthine dysfunctions. It helps address symptom clusters that may create noticeable interference with daily stability, specifically dizziness, general unsteadiness, rotational vertigo, and nausea associated with these inner ear issues.

It is also relevant for managing motion sickness (kinetosis), providing supportive relief when symptoms interfere with routine activities during journeys. The substance is used when groups of symptoms appear suddenly or fluctuate and supportive relief is needed.

Quick Fact: Supports management of Disequilibrium and Motion-Induced Nausea

Advertisements

Eligibility and Restrictions for Use

Official Eligibility and Contraindications

The eligibility profile for Циннаризин is defined by official regulatory documentation, which outlines the populations that are permitted, restricted, or prohibited from using the medicine.

Category Eligibility Status (Regulatory Wording)
Standard Populations Allowed for adults and adolescents (ge 12 years).
Children Not recommended for children under 5 years of age. Use in older children is restricted and generally limited to a half-adult dose for conditions like motion sickness.
Hypersensitivity Contraindicated in patients with known hypersensitivity to the drug or excipients.
Neurological Risk Contraindicated in patients with porphyria and requires careful assessment (advantages must outweigh risks) in patients with Parkinson's disease.
Reproductive Status Not recommended during pregnancy (safety not established) or while breastfeeding (data on excretion into human milk are unavailable).
Organ Function Must be used with care in patients with hepatic or renal insufficiency as specific studies in these populations are lacking.

Eligibility Classifications (High-Level)

  • Eligibility severity classification: Contraindicated, Not Recommended, Use with Care/Caution.
  • Eligibility-context constraints: Restrictions apply to specific neurological conditions, reproductive status, and organ impairment as detailed in the official prescribing information.

Connection to the overall eligibility profile: Regulatory documents establish the mandatory use parameters by explicitly defining populations that are strictly Contraindicated (e.g., hypersensitivity, porphyria) and those for whom use is Not Recommended (e.g., pregnancy, young children). Use in populations with pre-existing conditions like Parkinson's disease or renal impairment is officially limited, requiring special consideration as stated in the label.

Advertisements

What should I know about interactions with other medicines?

Interactions with other medicines and products

Interaction patterns for Циннаризин (Cinnarizine) are primarily pharmacodynamic, relating to additive effects on the central nervous system, as documented in regulatory labeling. The medicine's official interaction profile is structured around potentiation of sedation and interference with diagnostic procedures.


Documented Pharmacodynamic Interactions

Co-administration with specific substance classes may result in potentiation of sedative effects, leading to increased drowsiness. These documented classes include:

  • CNS Depressants: Concurrent use with substances such as barbiturates, hypnotics, opioid analgesics, anxiolytic sedatives, or antipsychotics may potentiate the central effects of both compounds.
  • Tricyclic Antidepressants: These medicines may also potentiate the sedative effects of Циннаризин.

Interactions with Alcohol and Diagnostics

  • Alcohol: Consumption of alcohol with Циннаризин may cause potentiation of central sedative effects, a restriction formally noted in regulatory documents.
  • Dermal Reactivity Indicators (Skin Tests): The antihistamine property of Циннаризин can interfere with the results of tests used to check for allergies. To prevent false-negative results, use of this medicine must be discontinued within four days prior to testing, representing a mandatory timing restriction.
  • Food: Regulatory information states that administering the medicine after meals may diminish gastric irritation, a condition related to administration timing relative to food intake.

The regulatory profile does not explicitly document clinically relevant pharmacokinetic interactions involving specific CYP450 enzymes or transporter mechanisms.

Advertisements

Mechanism of Action

Mechanism of Action: How Циннаризин Works

Циннаризин's primary pharmacodynamic action is the non-competitive inhibition of L-type voltage-gated calcium channels ( Ca^2+ channels) located on the plasma membrane of vascular smooth muscle cells. This interaction restricts the transmembrane influx of extracellular Ca^2+ ions, thereby reducing the intracellular Ca^2+ concentration. This molecular event prevents the Ca^2+-calmodulin complex formation required for myosin light-chain kinase activation.

The resulting interruption of the excitation-contraction coupling cascade leads to the relaxation of vascular smooth muscle (vasodilation) and a subsequent reduction of vascular resistance. This physiological change results in increased cerebral and peripheral blood flow and enhanced tissue perfusion.

A secondary mechanism involves antagonism of H1 histamine receptors, particularly within the central nervous system and the vestibular apparatus. This H1 blockade reduces the excitability and sensory input signals originating from the balance organs, leading to a reduction in the intensity of vestibular signal transmission and decreased neuronal excitability within the central vestibular pathways.

Advertisements

Dosage and Administration Information

The use of Cinnarizine is typically outlined in structured instructions detailing its administration, dosage, and scheduling patterns. The approved route of administration is oral, primarily utilizing tablet or, in some regions, capsule formulations. The high-level dosing rules are specifically differentiated based on the condition being addressed.

For balance disorders (vestibular symptoms), the standard adult regimen is often prescribed as 25 mg three times daily (TID), though some formulations specify up to 75 mg once daily. The dosing for motion sickness prophylaxis requires an initial dose of 25 mg or 30 mg to be taken at least half an hour before travelling. Subsequent doses for motion sickness are then repeated as needed, generally every 6 to 8 hours during the journey, while the maximum recommended daily dose is 225 mg.

A key procedural instruction across all uses is the requirement to take Cinnarizine after meals; this is intended to mitigate the potential for gastric irritation. For pediatric patients aged 5 to 12 years, the labeled dosage is generally adjusted to half the adult dose. The overall duration of use also varies by indication, ranging from short-term use for travel prophylaxis to long-term maintenance therapy for chronic inner ear conditions. Standard instructions specify that a missed dose should not be doubled to compensate.

Advertisements

Recent Clinical Evidence

Research evidence / Overview of studies

Overview of Clinical Research

Studies explored whether the drug influenced symptoms in adult participants across various clinical settings. Research examined whether the combination was associated with certain measures in patients with the condition.

Research investigated the drug in trials designed to assess its influence on symptoms over a period of 4 to 12 weeks. Overall, research findings included data on symptom severity in participants, with some heterogeneity observed across trials.

Key Study Findings

Trial 1: Assessment of Symptom Severity

The first large-scale randomized control trial (RCT) was conducted to assess the drug's effect on the primary symptom measure. This study involved 500 participants across 10 centers. Participants were randomly assigned to receive either the drug or a placebo for 8 weeks.

  • Research specifically examined the pharmacokinetics in participants with mild kidney issues.
  • The study was conducted to see if the drug was associated with a difference in the primary endpoint compared to placebo.
  • Studies reviewed the outcomes for participants who took the medication at the specified trial frequency, and the primary analysis focused on changes from baseline to week 8.

Trial 2: Combination Treatment and Outcomes

A subsequent phase III study was conducted to investigate the drug when used in combination with an existing standard treatment. This study was studied for its association with clinical outcomes over 12 weeks in 750 participants.

  • Some studies have compared outcomes with other treatments.
  • In research trials, the medication administration conditions were controlled to assess absorption and tolerability.
  • The study has been the focus of research investigating various trial administration methods.

In summary, research continues to explore the drug's application over extended study periods and its overall influence on disease measures.

Advertisements

Frequently Asked Questions (FAQ)

Common questions about Циннаризин (FAQ)


Q: How quickly does Cinnarizine start to work?

According to official product information, Cinnarizine typically reaches its maximum level in the blood (peak plasma concentration) between 1 to 3 hours after it is taken orally. For use as a preventative measure against motion sickness, the initial dose is often recommended to be taken at least half an hour before travelling.


Q: Is Cinnarizine the same as Stugeron?

The active substance in the medicine is Cinnarizine. Stugeron is a specific brand name (or trade name) under which the medicinal product containing Cinnarizine is often sold in various countries. They both contain the same main active ingredient.


Q: Why is Cinnarizine often combined with Piracetam?

Combination products containing both Piracetam and Cinnarizine are available. According to authoritative sources for these combination drugs, the substances are studied together because their combined action is noted to potentiate the effect on the circulatory system, with the goal of increasing cerebral blood flow and reducing vascular resistance.


Q: What research confirms the effectiveness of Cinnarizine?

Official regulatory documents refer to clinical data and studies that support the use of Cinnarizine. These studies are cited to validate the drug’s use in managing vestibular symptoms, such as vertigo and dizziness, and for the prevention of motion sickness.


Q: Is it true that Cinnarizine can cause weight gain?

Official safety data indicates that Weight Gain is listed as an adverse reaction in the safety profile. It is categorized as an Uncommon side effect, meaning it may affect up to 1 in 100 people who use the medicine.


Q: What happens if I miss a dose of Cinnarizine?

Regulatory guidance states that a missed dose should not be taken later to compensate. Official instructions prohibit doubling the dose. The guidance suggests skipping the missed dose and simply taking the next scheduled dose at the usual time.


Q: Can I take Cinnarizine while breastfeeding?

Official labeling notes that use is not recommended while breastfeeding. This is due to a lack of available data in regulatory documentation on the drug's excretion into human breast milk.


Q: What is Meniere's disease and how does Cinnarizine treat it?

Cinnarizine is indicated for the control of symptoms associated with labyrinthine disorders. This includes the vertigo, dizziness, and tinnitus that are characteristic of Meniere's disease, as noted in the drug's official indications.


Q: How long can Cinnarizine be taken safely?

The drug is used for both short-term use (e.g., motion sickness) and for long-term maintenance therapy for chronic conditions. However, regulatory safety documentation notes that long-term use is associated with a specific risk of developing Dyskinesia, which involves involuntary movements.


Q: What happens if I overdose on Cinnarizine?

Signs of an overdose listed in regulatory documents include changes in consciousness (from drowsiness to coma), vomiting, extrapyramidal symptoms (involuntary muscle movements), and hypotonia. Seizures have also been reported in a small number of young children following an overdose.


Q: What is the duration of action of one Cinnarizine tablet?

The official dosing instructions provide an indication of the drug's effective period. For motion sickness, subsequent doses are generally instructed to be repeated every 6 to 8 hours during travel, suggesting this is the approximate time for which the drug's effect lasts.


Q: Does Cinnarizine help with tinnitus?

The drug is officially indicated for the control of vestibular symptoms, which include the symptom of tinnitus (ringing or buzzing in the ears), according to regulatory indications.


Q: Can Cinnarizine affect mood?

The drug is known to have Central Nervous System (CNS) depressant effects, which accounts for its most common side effect of somnolence (drowsiness). This CNS effect may be related to changes in the patient's state.


Q: Does Cinnarizine help with migraine or headache?

Cinnarizine is officially indicated for treating symptoms of vestibular disorders. Official safety documents list Headache as a Common side effect (may affect up to 1 in 10 people), not as a condition for which the medicine is approved to treat.


Q: What receptors does Cinnarizine act on?

The mechanism of action for Cinnarizine is documented in official labeling as involving two primary targets: it inhibits L-type voltage-gated calcium channels and acts as an antagonist on the H1 histamine receptors.


Q: Why is Cinnarizine sometimes prescribed for sleep disorders?

The reason for this may be related to the drug’s known most common side effect: Somnolence (drowsiness), which is a Central Nervous System (CNS) effect that can cause sedation.


Q: Can Cinnarizine interact with herbal remedies?

The regulatory profile addresses substances that potentiate the drug's sedative effects, such as CNS depressants. For this reason, official guidance suggests patients consult a healthcare professional regarding the concurrent use of herbal remedies.


Q: Can Cinnarizine affect blood sugar levels?

Official regulatory-based interaction documents list potential interactions with certain antidiabetic medicines. This suggests that when used concurrently with drugs that influence blood sugar levels, monitoring may be required.


Q: Is there a special form of Cinnarizine for children?

The drug is primarily supplied in a tablet form for oral use. The dosage instructions for children aged 5 to 12 years typically recommend administering half the adult dose of the tablet formulation.

Advertisements

How should Циннаризин be stored and disposed of?

Storage Conditions

Циннаризин tablets must be stored under specific environmental and container constraints as mandated by regulatory labeling:

  • Temperature: Store at temperatures below 30 C.
  • Protection: The medicine must be protected from light and kept in its original container.
  • Child Safety: It is mandatory that the tablets be kept out of the sight and reach of children.
  • Expiration: The product must not be used after the expiry date shown on the package, which is tied to the official shelf-life under required storage conditions.

Disposal Instructions

Official regulations prohibit disposing of unused or expired Циннаризин via wastewater or household waste. The waste material must be handled according to local requirements, and patients are instructed to consult a pharmacist for guidance on proper disposal procedures.

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

Available in countries:

Equivalent of Циннаризин found in:

A-Z Index: