Cinnarizine is a class IV calcium channel blocker with a predominant effect on cerebral vessels, a piperazine derivative. Basically, the drug is used in the treatment of cerebral circulatory disorders.
According to modern data, the pharmacological properties of Cinnarizine are largely due to its ability to block membrane calcium. It inhibits the entry of calcium ions into cells.
Cinnarizine has a positive effect on cerebral, peripheral and coronary (cardiac) circulation, improves microcirculation. Increases the ability of red blood cells to deform (increase plasticity) and reduces the increased viscosity of the blood.
Increases the resistance of tissues to hypoxia (insufficient supply of oxygen to tissues or impaired absorption).
After oral administration, it is absorbed from the gastrointestinal tract, Cmax in plasma is reached after 1-4 hours. Plasma protein binding is 91%. undergoes metabolism. T1 / 2 is 3-6 hours. It is excreted through the intestines mainly unchanged, with urine - mainly in the form of metabolites.
Indications for use
What helps Cinnarizine? The drug is prescribed for the following conditions / diseases:
- The period of convalescence (recovery) after a traumatic brain injury;
- Ischemic stroke;
- Vestibular disorders, including Meniere's disease;
- Tinnitus, dizziness, nausea, labyrinthine nystagmus;
- Post-stroke state (including in the period after a hemorrhagic stroke);
- Encephalopathy;
- Prevention of kinetosis (sea, air sickness);
- Migraine attack prevention.
Instructions for use Cinnarizine and dosage
Take the drug inside after a meal:
- For disorders of cerebral circulation - usually 25 mg (I tablet) 3 times a day or 75 mg (1 capsule) 1 time per day;
- In case of peripheral circulation disorders - 50-75 mg (2-3 tablets) 3 times a day or 2-3 capsules (75 mg each) per day.
- For disorders of the vestibular apparatus: 1 tablet three times a day.
Cinnarizine is prescribed for a relatively long time (courses from several weeks to several months). The maximum dosage per day is 225 mg.
For children from 12 years old, the dosage is halved. Age less than 12 years is a contraindication to the use of the drug.
Contraindications
Cinnarizine is contraindicated in the following cases:
- Individual intolerance to the drug or its components;
- Pregnancy and lactation;
- Hypersensitivity to the drug or its components.
Overdose
Drowsiness, vomiting, coma, excessive drop in blood pressure, tremor.
In case of an overdose, gastric lavage is performed and activated charcoal is prescribed. Also, in case of an overdose of the drug, a sick person is monitored by a qualified doctor. An antidote has not been developed.
With any negative and negative manifestations, Cinnarizine should be discontinued.
Side effects
Possible side effects when using Cinnarizine:
- dyspepsia, dry mouth;
- rarely - cholestatic jaundice;
- headaches, drowsiness; in elderly patients with prolonged use, extrapyramidal symptoms, depression are possible;
- rarely - skin rash;
- weight gain, increased sweating;
- in isolated cases - lupus-like syndrome, lichen planus.
Due to the possible development of drowsiness as one of the side effects in the initial period of treatment, the appointment of persons whose work is associated with the speed of reaction, the speed of decision-making or the management of complex mechanisms, including various vehicles, should be accompanied by some caution.
Cinnarizine analogues, list of drugs
If necessary, replace the drug, you can use the analogues of Cinnarizine, they are, the list of drugs:
- stugeron,
- Cynarizine.
When choosing analogues, it is important to understand that the instructions for use of Cinnarizine, the price and reviews of drugs of similar action do not apply. It is important to consult a doctor and not to make an independent replacement of the drug.
Similar drugs:
- stugeron,
- Stutgeron,
- cinniprin,
- Dimitronal,
- Glamil,
- labyrinth,
- marizan,
- midronal,
- Mitronal.
Release form:
Tablets of 0.025 g (25 mg) in a pack of 50; capsules of 75 mg of cinnarizine (stugeron forte) in a pack of 20 and 60 pieces, also in the form of drops in 20 ml vials containing 75 mg of the active substance.
The price of Cinnarizine in pharmacies for 1 pack is from 29 rubles.
Store in a dry, dark place at a temperature of 15–25 °C.
Cinnarizine (Cinnarizinum) is a drug that improves cerebral circulation.
The active ingredient of the same name, Cinnarizine, is a white or off-white crystalline powder. Practically insoluble in water, slightly soluble in ethyl alcohol, sparingly soluble in ether, and very soluble in chloroform.
This diphenylperazine derivative has the chemical formula C 26 H 28 N 2 and the name 1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine.
Mechanism of action
The drug belongs to the group of calcium channel blockers. It is on the blocking of these channels that its mechanism of action is based.
Calcium ions along with many other components provide muscle contraction. Each muscle is a collection of muscle fibers (myofibrils). The contraction of the entire muscle is the contraction of each myofibril.
As you know, all muscles are divided into striated (skeletal) and smooth. There is also a heart muscle, myocardium, with special properties. All muscles, both smooth and skeletal, contract due to the interaction of two main contractile proteins - actin and myosin.
These proteins, located in the cytoplasm of the muscle cell, look like thin threads (filaments). In the process of muscle contraction, a complex of contractile proteins, actomyosin, is formed.
In this case, the filaments go behind each other, the muscle fiber thickens and shortens. The formation of actomyosin occurs with the participation of calcium ions.
Normally, the concentration of calcium outside the muscle cell is 25 times greater than inside it. It cannot be otherwise, otherwise all the muscles would be in a state of constant contraction, and the normal maintenance of all vital functions would be impossible.
And so the muscle contracts - calcium enters the cell, relaxes - they groom out of it. Calcium transport from the cell is an active, energy-dependent process carried out with the help of the enzyme calcium-dependent ATP-ase. The energy expended for this process is formed during the splitting of ATP molecules. The entry of calcium into the cell during muscle contraction is also an active process.
The capture of calcium and its intracellular transport is carried out by specific carrier proteins located on the surface of the cell membrane. These proteins are calcium channels. Calcium channels are heterogeneous, and differ among themselves in localization, properties and functions.
In smooth muscle cells of blood vessels, myocardium, its conducting system, bronchi, organs of the genitourinary system, there are slow long-lived channels or L-channels.
The drugs of this group have an affinity for calcium channels, and upon contact with these channels block them. At the same time, the entry of calcium into the cell is hampered, and the muscle does not contract, but, on the contrary, relaxes.
Calcium channel blockers are heterogeneous both in their structure and in their application points. There are drugs that block channels in the blood vessels, in the myocardium, in its conduction system. Cinnarizine primarily acts on the blood vessels in the brain.
Under the action of this drug, the vascular lumen expands, and cerebral (cerebral) circulation improves. This is of great clinical importance in TBI (traumatic brain injury), as well as in various non-communicable diseases with CNS damage, incl. and in cerebral stroke.
Cinnarizine does not cause a steal phenomenon when vasodilation occurs in healthy unaffected areas. At the same time, the blood supply to the pathological zones worsens even more. However, the use of Cinnarizine is recommended only in the recovery period of these severe conditions.
The problem is that Cinnarizine can cause extrapyramidal disorders, manifested by movement disorders and impaired muscle tone. These concomitant disorders (parkinsonism, tics, chorea, athetosis, muscle atony) hinder the use of Cinnarizine in clinical practice.
Cinnarizine is also indicated for dyscirculatory encephalopathy. This condition, caused by impaired blood circulation in the cerebral vessels in hypertension, cerebral atherosclerosis, is characterized by negative changes in the psyche and neurological status of the patient.
Under the action of the drug, memory and thinking improve, general well-being normalizes, headache and dizziness decrease or disappear. But recently, due to the aforementioned extrapyramidal disorders, the use of Cinnarizine in these conditions is also limited.
Due to the ability to eliminate headaches, the drug is effective in migraine. Under the action of Cinnarizine, blood viscosity decreases - red blood cells become more elastic, easily change their shape, and oxygen delivery to tissues is facilitated.
An additional vasodilating effect of Cinnarizine is due to the fact that it enhances the effect of carbon dioxide on the vascular wall.
Under the action of carbon dioxide, the lumen of the vessels also expands. The drug eliminates the effect on the vessels of the sympathetic nervous system and some biologically active substances (dopamine, vasopressin, angiotensin), which spasm blood vessels.
Cinnarizine has antihistamine properties. True, these properties are weakly expressed in him. The antihistamine effect at the level of the central nervous system is manifested by a decrease in the excitability of the vestibular apparatus.
Therefore, the drug can be used for various vestibular disorders, accompanied by disorientation in space, dizziness, nausea, vomiting, nystagmus, tinnitus. For this reason, Cinnarizine is used for transport sickness that occurs against the background of pitching.
Under the action of Cinnarizine, peripheral blood circulation is enhanced, which leads to an improvement in metabolic processes in tissues and an increase in their resistance to hypoxia. Therefore, it is prescribed for various types of disorders of trophism and blood microcirculation in tissues, including thrombophlebitis, Raynaud's syndrome, atherosclerosis obliterans and diabetic lesions of small tissue vessels.
However, the level of blood pressure ( blood pressure) Cinnarizine has practically no effect, and therefore cannot be used as an antihypertensive agent.
A bit of history
Cinnarizine was first obtained in 1955 by employees of the Belgian pharmaceutical company Janssen Pharmaceutica (Janssen Pharmaceuticals), and in 1962 its commercial production was launched.
The drug was produced both in Russia and abroad, including in some of the then socialist countries (Bulgaria, Hungary). Initially, it was positioned as a vasodilator and antihistamine.
Later, it began to be used for organic and functional disorders of the central nervous system, for violations of the peripheral circulation. However, later the indications were revised, mainly due to side effects from the CNS. However, the drug is still used today, mainly for migraine and vestibular disorders.
Synthesis technology
Before obtaining Cinnarizine, chemical reactions are first carried out to form the precursor substance, Cinnamyl chloride.
Then, in the course of subsequent reactions carried out in a special temperature regime in the presence of organic and inorganic catalysts, the final product, Cinnarizine, is obtained.
In addition to Cinnarizine, excipients are used in the production of tablets: microcrystalline cellulose, wheat starch, polyvinylpyrrolidone, aerosil 200, lactose monohydrate and magnesium stearate.
Release form
Tablets 25 mg
Cinnarizine is produced by many Russian pharmaceutical companies. In Bulgaria, it is produced by Milve and Sopharma.
The original Cinnarizine under the patent name Stugeron is produced by the world famous Hungarian company Gedeon Richter. The mass of all tablets, regardless of the manufacturer, is the same - 25 mg. However, the price of Stugeron is much higher than generic generic drugs.
Indications
- Conditions after strokes and TBI;
- Cerebral disorders of vascular origin, including dyscirculatory encephalopathy;
- Vestibular disorders, accompanied by headache, dizziness, tinnitus, nausea, vomiting;
- Migraine;
- Senile dementia (dementia);
- Road sickness prevention;
- Diabetic angiopathy, Raynaud's disease, thrombophlebitis, intermittent claudication, and other types of peripheral circulatory disorders.
Dosages
For vestibular disorders, take 1 tablet 3 times a day, for disorders of cerebral circulation - 1-2 tablets 3 times a day, for disorders of peripheral circulation - 2-3 tablets 3 times a day. Tablets are taken after meals, not chewed, washed down with water.
For the prevention of road sickness, adults take 1 tablet half an hour before the trip. If necessary, the reception is repeated after 6 hours. Children take Cinnarizine at half the adult dose.
Pharmacodynamics
Absorbed in the stomach and intestines. Plasma protein binding - 91%. The maximum concentration of Cinnarizine in the blood plasma is formed after 1-3 hours after ingestion. In the liver, Cinnarizine is completely metabolized by glucuronidation. In the form of metabolites, it is excreted through the kidneys and through the intestines in a ratio of 1:2. The half-life is 4 hours.
Side effects
- CNS: headache, general weakness, drowsiness, depression, in elderly patients - extrapyramidal disorders in the form of trembling of the limbs and impaired muscle tone;
- gastrointestinal tract: dry mouth, abdominal pain, dyspeptic disorders, bile stasis, jaundice;
- Leather: rash, sweating, lupus syndrome, extremely rarely - lichen planus.
Pharmacological group: Calcium channel blockers
Pharmacological action: Selective blocker of slow calcium channels, reduces the entry of ions into cells and reduces their content in the plasma membrane depot, reduces the tone of smooth muscles of arterioles, enhances the vasodilating effect of carbon dioxide. Directly affecting the smooth muscles of blood vessels, reduces their response to biogenic substances (adrenaline, norepinephrine, dopamine, angiotensin, vasopressin). It has a vasodilating effect (especially in relation to cerebral vessels), without significantly affecting blood pressure. Shows moderate antihistamine activity, reduces the excitability of the vestibular apparatus, lowers the tone of the sympathetic nervous system. It is effective both in initial and chronic cerebrovascular insufficiency (including in patients in the residual stage of ischemic stroke). In patients with impaired peripheral circulation, it improves the blood supply to organs and tissues (including myocardium). Increases the elasticity of erythrocyte membranes, their ability to deform, reduces blood viscosity. Increases muscle resistance to hypoxia.
Effects on receptors: Antagonist of calcium channel ions of T-type calcium channels; Antihistamine H1 receptors; Antiserotonergic receptors 5 - HT2; Antidopaminergic D2 receptors.
Systematic (IUPAC) name: (E)-1-(diphenylmethyl)-4-(3-phenylprop-2-enyl)piperazine
Trade names: Stugeron, Stunarone
Half-life: 3-4 hours
Formula: C 26 H 28 N 2
Mol. mass: 368.514 g/mol
Cinnarizine (trade names Stugeron, Stunarone, R5) is a piperazine derivative that is characterized as an antihistamine and calcium channel blocker. It is also known that the drug increases cerebral blood flow, and therefore is used to treat cerebral apoplexy, post-traumatic cerebral symptoms, and cerebral atherosclerosis. However, the drug is most often prescribed for nausea and vomiting caused by motion sickness or other causes such as chemotherapy, dizziness, or Meniere's disease. Cinnarizine was first synthesized by Janssen Pharmaceutica in 1955. The generic name of the drug comes from the Latin name of the herb genus - "cinna" (cinna), while "riza" means "roots", since the substance was originally extracted from the roots of cinna. Cinnarizine is not available in the United States or Canada. It is manufactured and sold in Bangladesh under the brand name Suzaraon by Rephco Pharmaceuticals Limited.
Pharmacokinetics
Cinnarizine is most often taken by mouth, in tablet form, with the frequency and number of doses depending on the reason for taking the drug. Once in the body, the substance is absorbed fairly quickly and reaches peak plasma concentrations 1-3 hours after administration. Cmax, the maximum level of the drug in the study area (usually in blood plasma), is 275+/- 36 ng / ml, and tmax (the amount of time that the drug is present in the blood at the maximum amount), was 3.0 +/- 0 ,5:00. AUC∞, (area under the curve extrapolated to infinity), which can be used to assess bioavailability, is 4437+/-948 (ng h/mL). The half-life of the drug is from 3.4-60 hours, depending on the age of the patient. The mean terminal half-life in young volunteers when administered with 75 mg cinnarizine is 23.6 +/- 3.2 hours. A study in which cinnarizine was administered to healthy volunteers at a dose of 75 mg twice daily for twelve days showed that cinnarizine can accumulate in the body, with a steady-state accumulation factor of 2.79 +/- 0.23. However, AUCT for this time period (T = 12 days) did not differ significantly from AUC∞, which was measured after a single dose of the drug. Being a very weak base as well as a lipophilic compound with low water solubility, Cinnarizine can cross the blood-brain barrier by simple diffusion. It is because of this that Cinnarizine is able to affect the flow of blood in the brain. When administered orally, cinnarizine has a generally low and variable bioavailability due to a high degree of degradation. However, it was found that when administered intravenously as a lipid emulsion, better pharmacokinetics and tissue distribution were observed. The lipid emulsion has increased AUC and reduced clearance compared to the solution form. The plasma pharmacokinetics of intravenous cinnarizine follow a three-phase pattern, beginning with a rapid distribution phase, followed by a slower distribution phase, and ending with very slow elimination. The Vss (steady-state volume of distribution) of the lipid emulsion is 2 times lower (6.871 +/- 1.432 L/kg) than that of the Cinnarizine solution (14.018 +/- 5.598 L/kg). In addition, it was found that Cinnarizine in much smaller quantities enters the lungs and brain in the form of a lipid emulsion. This reduces the likelihood of toxic side effects in the central nervous system.
Pharmacodynamics
Cinnarizine is classified as a selective T-type calcium ion channel antagonist because its binding blocks the channels and keeps them inert. Cinnarizine has a Ki value (inhibitory constant) of 22 nm. It is also known that Cinnarizine can have antihistamine, antiserotonergic and andidopaminergic effects by binding to H1-histamine receptors and dopaminergic (D2) receptors. IC50 (half the maximum inhibitory concentration) of Cinnarizine for inhibition of soft muscle contraction is 60 mM. In addition, this drug has been shown to preferentially bind to target calcium channels when they are in the open position as opposed to the closed conformation. Cinnarizine was previously thought to help treat nausea and motion sickness by inhibiting calcium currents in tight, closed channels in type II vestibular hair cells in the inner ear. However, more recent evidence supports the idea that, at pharmacologically appropriate levels (0.3-0.5 µM), cinnarizine reduces vestibular vertigo not by blocking calcium channels, but rather by inhibiting potassium (K+) currents, which are activated by increased hydrostatic pressure on hair cells. Cinnarizine does block calcium currents in the vestibular hair cells, however, this is observed only at higher concentrations of the drug (3nbsp; microns). Inhibition of these currents reduces motion-induced dizziness and nausea by attenuating the overreactivity of the vestibular hair cells that send balance and movement information to the brain.
Cinnarizine (Stugeron) application
Cinnarizine is primarily used to treat nausea and vomiting associated with motion sickness, dizziness, Meniere's disease, or Cogan's syndrome. In fact, cinnarizine is only one of a select few drugs that have shown positive results in the chronic treatment of vertigo and tinnitus associated with Meniere's disease. However, because the drug causes drowsiness, it is generally of limited use among pilots and crew members who need to remain active for extended periods of time. In a clinical study (N=181), Cinnarizine was shown to reduce the risk of moderate dizziness by 65.8% and severe dizziness by 89.8%. Cinnarizine works by interfering with signal transmission between the vestibular apparatus of the inner ear and the vomiting center of the hypothalamus by limiting the activity of the vestibular hair cells that send signals for movement. The disparity in signal processing between motion receptors in the inner ear and the visual senses is reduced, resulting in less difficulty in moving or standing. Vomiting on movement may be due to a physiological compensatory mechanism in the brain to keep the person from moving so they can adjust to the signal, but the true evolutionary cause of this disease is currently unknown. Some sources claim that the body reacts by vomiting because it believes that it has been poisoned by a poison (such as alcohol), and what a person sees does not match what he feels. When prescribed to treat balance problems and dizziness, cinnarizine is usually taken two or three times a day, depending on the amount of each dose. When used to treat motion sickness, the tablet is taken at least two hours before travel and then every four hours while travelling. However, a recent 2012 study comparing the effects of Cinnarizine and transdermal Scopolamine for the treatment of motion sickness concludes that Scopolamine is a significantly more effective drug with significantly fewer side effects than Cinnarizine. This led to the conclusion that scopolamine transdermal is probably the best option for the treatment of motion sickness in fleet crew members and other sea travelers. In addition to being used to treat dizziness, cinnarizine may also be considered as a nootropic due to its vasorelaxant properties (due to blocking calcium channels), mainly in the brain. Cinnarizine is also used as a sedative. Cinnarizine inhibits flow in red blood cells by increasing the elasticity of the cell wall, thereby increasing their flexibility and making the blood less viscous. This contributes to a more efficient transfer of blood through the constricted vessels to carry oxygen to the damaged tissue. Cinnarizine is also effective in combination with other nootropics, primarily Piracetam, in this combination, each drug enhances the effect of the other, increasing the supply of oxygen to the brain. An animal study comparing the efficacy of Cinnarizine and Flunarizine (a derivative of Cinnarizine 2.5-15 times more potent) for the treatment of global transient cerebral ischemia found that Cinnarizine improved functional abnormalities in ischemia but did not help with neuronal damage. Flunarizine, on the other hand, provides greater neuronal protection but is less effective in treating subsequent behavioral changes. In addition, cinnarizine can be used by scuba divers without increasing the risk of central nervous system oxygen toxicity, which can lead to seizures and a high risk in closed oxygen diving. This also applies to divers, who may potentially be forced to undergo hypobaric decompression therapy, which uses high oxygen pressure, and may also be exposed to any risk of CNS oxygen poisoning caused by Cinnarizine. However, cinnarizine does not increase the risk of toxicity, and evidence also suggests that cinnarizine may contribute to the delay of O2 toxicity in the central nervous system. There is also evidence that cinnarizine can be used as an effective anti-asthma agent when taken regularly. It has also been shown that cinnarizine can be used as a second line treatment for idiopathic urticarial vasculitis.
Side effects of Cinnarizine (Stugeron)
Side effects when taking Cinnarizine range from mild to very serious. Possible side effects include drowsiness, sweating, dry mouth, headache, skin problems, lethargy, gastrointestinal disturbances, hypersensitivity reactions, and movement problems/muscle rigidity, and tremors. Because cinnarizine can cause drowsiness and blurred vision, users should ensure that their reactions are normal before driving, operating machinery, or any other type of work that could be hazardous if the person is not fully active or poorly sees. Cinnarizine is also known to cause both acute and chronic parkinsonism due to its affinity for D2 receptors, suggesting its actual benefit in improving nervous system health. Cinnarizine's antagonism at D2 dopamine receptors in the striatum results in symptoms of depression, tremors, muscle rigidity, tardive dyskinesia, and akathisia, characterized as drug-induced Parkinson's disease, the second leading cause of Parkinson's disease. Experience shows that one of the metabolites of Cinnarizine, C-2, plays an active role in the development of Parkinson's disease. It is also noted that an estimated 17 out of 100 new cases of Parkinson's disease are associated with the use of Cinnarizine or Flunarizine. People in a particular risk group are elderly patients, in particular women, and patients who have taken the drug for a longer period of time. There is also evidence that patients with a family history of Parkinson's disease, or a genetic predisposition to the disease, are more likely to develop a drug-induced form of the disease as a result of the use of Cinnarizine. In addition to D2 receptor antagonism, cinnarizine has also been shown to cause a decrease in presynaptic dopamine and serotonin, as well as changes in vesicular dopamine transport. Terland et al. showed that long-term use of cinnarizine leads to such high concentrations of the drug that they are able to interfere with the proton electrochemical gradient necessary for packing dopamine into vesicles. Cinnarizine, pKa = 7.4, acts as a protonophore, preventing MgATP-dependent production of the electrochemical gradient, which is critical in the transport and storage of dopamine in the vesicles, and thus may reduce the level of dopamine in the basal ganglion neurons and lead to the development of symptoms of Parkinson's disease. . In addition, several cases of overdose of Cinnarizine in children and adults have been reported, including a number of symptoms such as drowsiness, coma, vomiting, hypotension, stupor and convulsions. Cognitive complications are most likely due to the antihistamine effects of Cinnarizine, while movement effects are the result of andidopaminergic properties. In case of overdose, the patient should consult a doctor to prevent potential neurological complications.
"Cinnarizine", what does this vasodilator help with? The drug stimulates the blood circulation of the brain, reduces blood viscosity. The drug "Cinnarizine" instructions for use recommends taking with memory impairment, intellectual activity, atherosclerosis, migraine.
Composition and form of release
Produced in the form of white tablets. The medicine "Cinnarizine", from which it helps with circulatory disorders of the brain, contains the active element of the same name in a dosage of 25 mg. Magnesium stearate, starch, lactose monohydrate contribute to better absorption of the drug. 75 mg of the active ingredient includes a variety of "Cinnarizine Forte", which creates a more pronounced effect.
Pharmacological properties
The drug lowers the number of calcium ions in the cells, has a relaxing effect on the muscles of the arterioles, enhances the vasodilating ability of carbon dioxide. Tablets "Cinnarizine", which has an effect on vascular tone, reduces their response to adrenaline, dopamine, vasopressin.
The vasodilating properties of the drug do not cause a decrease in pressure. In addition, the drug increases the resistance of tissues to a lack of oxygen, thins the blood, and suppresses nystagmus. Observe and antihistamine effect after taking the pills. Absorption of the drug occurs in the digestive tract, the highest concentration appears 2 hours after application.
The medicine "Cinnarizine": what helps
Indications for use include:
- Minier's disease;
- migraine;
- conditions after a stroke;
- paresthesia;
- senile dementia;
- brain injury;
- dyscirculatory encephalopathy;
- thrombophlebitis.
Tablets "Cinnarizine" from what else do they help? The drug is prescribed for:
- violations of the vestibular apparatus;
- thromboangiitis obliterans;
- atherosclerosis;
- angiopathy;
- to prevent kinetosis;
- trophic anomalies;
- Raynaud's disease;
- motion sickness.
Contraindications
The medicine "Cinnarizine" instructions for use and doctors prohibit taking with:
- lactase deficiency;
- gluten enteropathy;
- hypersensitivity to the composition of Cinnarizine tablets, from which they can cause allergies;
- galactosemia;
- malabsorption syndrome;
- breastfeeding;
- children under 12 years of age.
The medicine "Cinnarizine" during pregnancy can be taken in special cases after medical recommendations. Caution during therapy is required for people suffering from parkinsonism.
The drug "Cinnarizine": instructions for use
In case of violation of the blood supply to the brain, it is required to drink 3-6 tablets per day. With pathologies of the peripheral circulation, the daily dosage reaches 150-225 mg or 6-9 capsules. With vestibular anomalies, 1-3 tablets per day are indicated.
Doctors recommend taking the medicine "Cinnarizine" for motion sickness and to prevent this condition. Patients respond positively to this therapy. When motion sickness, seasickness, half an hour before the departure of the ship, flight, trip, drink 25 mg (1 tab.). If necessary, re-admission is carried out after 6 hours. In case of poor tolerance of the drug, therapy begins with a half dose, gradually bringing it to the therapeutic one.
Side effects
The drug "Cinnarizine", instructions and reviews confirm this fact, can cause the following negative effects:
- drowsiness;
- discomfort in the abdomen;
- pressure drop;
- depression
- dry mouth;
- tremor of the limbs;
- skin rash;
- headache;
- fatigue;
- cholestatic jaundice;
- increased hypokinesia;
- excess body weight;
- dyspepsia;
- excessive sweating;
- increase in muscle tone;
- epigastric pain;
- parkinsonism;
- disorientation.
Side effects usually go away after the drug is discontinued.
special instructions
The drug "Cinnarizine" can show a positive result when taking doping samples from athletes. This effect is due to the antihistamine properties of the drug. With prolonged use, it is required to monitor the condition of the kidneys, liver, and blood. You should refrain from driving during treatment.
In case of insufficiency of blood circulation in the brain, a combination of drugs "Cinnarizine" and "Piracetam" is prescribed. The synergistic effect of these funds is described in Wikipedia.
Interaction 
The drug increases the effectiveness of sedative, antihypertensive, vasodilator drugs, nootropics. Simultaneous reception of means and alcohol strengthens toxicity. The drug reduces the effectiveness of therapy for arterial hypotension.
Analogues
Doctors prescribe the following analogues of "Cinnarizine" for the active ingredient:
- "Cinnaron".
- "Vertisin".
- "Stugeron".
- "Vertisin Forte".
- Cinnarizine Sopharma.
- "Cinedil".
- "Cinnasan".
Price
You can buy Cinnarizine tablets in Moscow at a price of 25-56 rubles. In Kiev, the cost of the drug reaches 6-28 hryvnia. In Minsk, it is sold for 0.02-1.36 bel. rubles. The price in Kazakhstan reaches 210 tenge (Cinnarizine Sopharma 0.025 No. 50 tablets (pcs.) SOPHARMA, S.A. (Bulgaria)).
Opinions of patients and doctors
Patients give reviews about the drug "Cinnarizine" as an inexpensive and effective remedy. The medicine helps well with headaches, increases intellectual performance, relieves the symptoms of dizziness and tinnitus.
Despite the contraindications to the use of tablets for children under 12 years of age, the medication is sometimes prescribed for infants. Parents respond positively.
Calcium channel blockers of the cinnarizine group.
Composition of Cinnarizine
The active substance is Cinnarizine.
Manufacturers
ICN Leksredstva (Russia), ICN Tomskhimfarm (Russia), Akrikhin KhFK (Russia), Analytical and Management Group (Russia), Antiviral (Russia), Aspharma (Russia), Balkanpharma-Dupnitsa AD (Bulgaria), Biomed ( Russia), Biomedia (Bulgaria), Biosintez JSC (Russia), Bryntsalov (Russia), Warsaw Pharmaceutical Plant Polfa (Poland), Veropharm Belgorod Branch (Russia), Gardis (Georgia), Dalkhimfarm (Russia), Irbit Chemical and Pharmaceutical Plant ( Russia), Medisorb ZAO (Russia), Moskhimfarmpreparaty im. ON THE. Semashko (Russia), Nizhpharm OJSC (Russia), Novosibirsk Plant of Medical Preparations (Russia), PFC Renewal (Russia), Ozon LLC (Russia), Organika OJSC (Russia), Rozpharm (Russia), Sintez AKO, Kurgan (Russia), Sopharma AO (Bulgaria), Tatkhimfarmpreparaty (Russia), Tyumen Chemical and Pharmaceutical Plant (Russia), Pharma AD (Bulgaria), Pharmasyntez JSC (Russia), Farmakhim (Bulgaria), Farmakhim Holding EAD, Troyapharm S.A. (Bulgaria), Farmakhim Holding EAD, Pharmacy AD (Bulgaria), Farmakhim-Pharmakon-93 (Bulgaria), Ferein (Russia), Schelkovo Vitamin Plant (Russia)
pharmachologic effect
Vasodilator, improves cerebral circulation, improves peripheral circulation.
It has a high affinity for calcium channels of cerebral vessels, improves cerebral circulation, reduces cerebrosthenic phenomena, headache, tinnitus.
Suppresses reactions to biogenic vasoconstrictor substances (adrenaline, norepinephrine, bradykinin).
Improves microcirculation, increasing the elasticity of erythrocyte membranes and lowering blood viscosity.
Increases cell resistance to hypoxia.
Reduces the excitability of the vestibular apparatus (including nystagmus and other autonomic disorders).
It has moderate antihistamine activity.
In patients with impaired peripheral circulation, it improves tissue blood supply and potentiates postischemic hyperemia.
Does not affect blood pressure and heart rate.
When taken orally, it is rapidly and completely absorbed.
Actively and completely metabolized.
Does not have teratogenicity.
Side effects of cinnarizine
From the nervous system and sensory organs:
- drowsiness;
- fatigue, weakness, dizziness, headache;
- in elderly patients, when taking large doses (150 mg / day), extrapyramidal disorders (tremor, muscle rigidity, hypokinesia) may develop, requiring discontinuation of the drug.
From the digestive tract:
- dry mouth,
- dyspepsia,
- cholestatic jaundice.
From the side of the skin:
- increased sweating,
- manifestations of lupus erythematosus or lichen planus.
Others:
- allergic skin reactions,
- weight gain.
Indications for use
Cerebrovascular insufficiency (dizziness, tinnitus, decreased ability to concentrate or memory, etc.), dyscirculatory encephalopathy, involutional psychosis or depression, post-stroke or traumatic brain injury, migraine, vestibular disorders (Ménière's syndrome, kinetosis, etc.). , manifested by imbalance, nausea, vomiting, nystagmus, etc.), peripheral circulatory disorders (Raynaud's disease, obliterating atherosclerosis, thromboangiitis, diabetic angiopathy, trophic and varicose ulcers, acrocyanosis, paresthesia, night cramps and cold extremities.
Contraindications Cinnarizine
Hypersensitivity, breastfeeding.
Method of application and dosage
Inside, after eating.
Violation of cerebral circulation and vestibular disorders - 25 mg 3 times a day; prevention of sea and air sickness - 25 mg 30 minutes before the trip, if necessary - again after 6-8 hours; violation of peripheral circulation - 50-75 mg 3 times a day, for a long time - from several weeks to several months.
Children are given half the adult dose.
Overdose
No data.
Interaction
The effect is enhanced (mutually) by tricyclic antidepressants, drugs that depress the central nervous system, and alcohol.
Enhances the effect of nootropics.
Increases the vasodilating activity of other agents.
special instructions
Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention.
Patients with Parkinson's disease may be prescribed only if the expected effect of therapy outweighs the risk of worsening of the underlying disease.
Within 4 days after ingestion, a false result is possible when conducting skin allergic tests.