Cinnarizine

Cinnarizine (Cinnarizine) is a medication used to treat a variety of conditions associated with circulatory disorders, especially within the ear and brain. This medication has antihistamine and local vasodilating properties.

Indications Cinnarizine

Cinnarizine is used to treat various conditions associated with circulatory disorders, especially within the ear and brain. Here are the main indications for the use of cinnarizine:

1. Vertigo and vestibular disorders: Cinnarizine is effective in the treatment of various forms of vertigo, including labyrinthine hyperplasia and other vestibular disorders.
2. Meniere's disease: This drug may help reduce the frequency and intensity of attacks of dizziness, nausea and vomiting in patients with Meniere's disease.
3. Tinnitus: Cinnarizine may be used to reduce the intensity of tinnitus (tinnitus), especially if it is associated with circulatory problems within the ear.
4. Migraine: The drug may be used to treat symptoms of migraine, including headache and nausea.
5. Prevention of motion sickness: Cinnarizine may be used to prevent motion sickness (motion sickness) during travel or other situations involving movement.

Release form

Cinnarizine is available in several forms, the most common of which are:

1. Tablets: This is the most common form of release of cinnarizine. Tablets usually contain 25 mg or 75 mg of the active ingredient. Tablets allow precise dosing of the medicine and are convenient to use.
2. Capsules: In some countries, cinnarizine may be available in capsule form, which also provides precise dosing and ease of administration. Capsules, like tablets, may contain varying amounts of active ingredient.

Pharmacodynamics

Cinnarizine is a nitroimidazole drug with a number of pharmacodynamic effects that make it useful in the treatment of various conditions:

1. Inhibition of vasoconstriction and improvement of microcirculation: Cinnarizine acts as a calcium channel inhibitor by blocking Ca2+ entry into cells, which leads to a decrease in vascular smooth muscle tone and improved blood flow, especially in the microvasculature. This effect makes it useful for the treatment of conditions associated with microcirculatory disorders and vasoconstriction.
2. Antivertigo and antimigraine action: Cinnarizine is effective in the treatment of vertigo and vertigo due to its ability to improve blood flow in the inner ear and due to its antagonistic action on H1-histamine receptors.
3. Anti-asthmatic effect: In one study, cinnarizine was shown to have an anti-asthmatic effect, making it suggested as a potential treatment for chronic asthma.
4. Effects on neurotransmitters: Cinnarizine may affect neurotransmitter systems, including the dopaminergic system, which is of clinical importance in the treatment of some neurological and psychiatric disorders. However, this same property may contribute to the development of side effects such as parkinsonism.
5. Antioxidant Action: Studies have shown that cinnarizine has antioxidant properties, which may contribute to its protective effects against cells and tissues.

Pharmacokinetics

The pharmacokinetics of cinnarizine, as with most drugs, can vary depending on individual patient characteristics and the form of the drug. Here are the general features of cinnarizine pharmacokinetics:

1. Absorption: Cinnarizine is usually well absorbed from the gastrointestinal tract after oral administration. Maximum plasma concentrations are usually reached 1-3 hours after administration.
2. Distribution: Cinnarizine has high affinity to plasma proteins (approximately 90%). It is distributed throughout body tissues, including the central nervous system and the ear.
3. Metabolism: Cinnarizine is metabolized in the liver with formation of various metabolites. The main metabolites are decinnarizine and paramethoxyphenylethylpiperazine. The metabolites also have pharmacological activity.
4. Excretion: Cinnarizine and its metabolites are mainly excreted with urine as conjugates.
5. Half-excretion: The half-excretion of cinnarizine from the body is about 3-6 hours.

Dosing and administration

The method of administration and doses of cinnarizine may vary depending on the specific indications for use, the age of the patient, and his general state of health. It is important to follow the doctor's instructions and recommendations specified in the drug's instructions for use. The following are general recommendations for cinnarizine dosing, which may be adapted by your doctor.

Dosage for adults:

• For the treatment of dizziness, including Meniere's and vestibular disorders: It is generally recommended to take 25-75 mg (1-3 25 mg tablets) three times daily.
• For the prevention and treatment of motion sickness (motion sickness): It is recommended to start by taking 30 minutes before the expected start of travel with a dose of 25-50 mg, if necessary the dose can be repeated every 6 hours during travel.
• To improve peripheral circulation (e.g. In obliterative atherosclerosis): The dose may vary from 50 to 150 mg per day, divided into several doses.

Dosage for children:

The use of cinnarizine in children should be carried out with extreme caution and under the strict supervision of a doctor. The dosage for children will depend on their weight and age, as well as on the specific indications for use.

Method of Application:

Cinnarizine should be taken after meals to improve its absorption. The tablets should be swallowed whole, drinking enough water.

Important Notes:

• Always consult your doctor before starting cinnarizine, especially if you have a chronic condition or are taking other medications.
• Carefully follow your doctor's instructions for dosage and duration of treatment.
• Do not stop taking the drug suddenly without consulting your doctor, especially if you are taking it on a regular basis.
• If you miss a dose, take it as soon as possible, but if it is almost time for the next dose, skip the forgotten dose and continue as scheduled. Do not double a dose to make up for a missed dose.

Use Cinnarizine during pregnancy

The use of cinnarizine during pregnancy is not recommended, especially in the first trimester, due to the lack of sufficient data on its safety for the developing fetus. Cinnarizine is a calcium antagonist and may affect blood flow in the placenta and other aspects of pregnancy physiology. Cinnarizine should also be avoided during lactation, as it is not known whether it penetrates into breast milk.

If it becomes necessary during pregnancy to treat conditions for which cinnarizine is commonly used (e.g., dizziness or migraine), you should discuss possible alternatives with your doctor and evaluate the risks and benefits of any therapy to the mother and fetus.

Contraindications

1. Allergy to cinnarizine or any other component of the drug: Patients with known hypersensitivity to cinnarizine should avoid its use.
2. Parkinsonism: Cinnarizine may worsen the symptoms of Parkinson's disease or parkinsonism, so it is not recommended for use in patients with this condition.
3. Severe hepatic insufficiency: Because cinnarizine is metabolized in the liver, its use may be limited in patients with severe hepatic impairment.
4. Pregnancy and lactation: The use of cinnarizine during pregnancy andlactation should be avoided, as there is insufficient data on the safety of its use during these periods. The physician should carefully weigh the potential risks and benefits of the drug for each individual patient.
5. Pediatric age: The use of cinnarizine in children may be limited due to the lack of studies confirming its safety and efficacy in this age group. A doctor should be consulted for more detailed information.

Side effects Cinnarizine

Cinnarizine is usually well tolerated, but like any other medication, it can have side effects. Some of the possible side effects of cinnarizine may include:

1. Drowsiness: One of the most common side effects of cinnarizine is drowsiness or fatigue. Patients may notice impaired concentration and reaction time, especially at the beginning of the drug.
2. Dry mouth: Some people may experience a dry mouth sensation when taking cinnarizine.
3. Headache: Some patients may experience headaches or dizziness.
4. Vomiting or stomach discomfort: Rarely, cinnarizine may cause dyspeptic symptoms such as nausea or stomach discomfort.
5. Increased appetite and weight gain: Some people may experience increased appetite and weight gain after taking cinnarizine.
6. Rare allergic reactions: In rare cases, cinnarizine may cause allergic reactions such as skin rash, itching, or swelling of the face.
7. Extrapyramidal symptoms: Extrapyramidal symptoms such as tremors, muscle rigidity, or inability to control movements may develop.

Overdose

An overdose of cinnarizine can lead to an increase in its side effects. Symptoms of overdose may include:

1. Severe drowsiness and fatigue.
2. Increased dizziness and headache.
3. Movement coordination disorders and decreased reaction time.
4. Dry mouth.
5. Increased heart rate and blood pressure.
6. Tremor or muscle weakness.
7. Vomiting and nausea.

In case of suspected cinnarizine overdose it is necessary to seek immediate medical attention or call an ambulance. The patient may require symptomatic treatment and maintenance of vital functions of the body. The doctor may take measures to remove part of the drug from the gastrointestinal tract and conduct symptomatic therapy to eliminate the manifestations of overdose.

Interactions with other drugs

Cinnarizine may interact with a number of other medicines, which may increase or decrease their effects and increase the likelihood of side effects. Before starting cinnarizine, it is important to tell your doctor about all medications you are taking, including over-the-counter medications, vitamin supplements, and herbal preparations. Here are some interactions of cinnarizine with other medicines:

Enhanced sedative effect

• Sedatives and sedatives: The use of cinnarizine concomitantly with sedatives, such as benzodiazepines, may increase their sedative effect.
• Alcohol: Alcohol consumption during treatment with cinnarizine may increase the sedative effect and reduce the ability to concentrate and react quickly.

Interaction with antihypertensive drugs

• Antihypertensive drugs: Cinnarizine may increase the hypotensive effect of blood pressure-lowering drugs, which will require adjustment of their dosage.

Interaction with other calcium channel blockers

• Calcium channel blockers: Since cinnarizine also acts as a calcium channel blocker, its concomitant use with other drugs of this class (e.g., verapamil, nifedipine) may lead to increased effects and side effects such as hypotension or bradycardia.

Other interactions

• Anti-Parkinsonian medications: Cinnarizine may weaken the effects of medications used to treat Parkinson's disease because of its potential effects on neurotransmitters.

Storage conditions

Cinnarizine should be stored according to the manufacturer's instructions and your doctor's recommendations. The following is usually recommended:

1. Storage temperature: Cinnarizine should be stored at a temperature of 15°C to 30°C. It is not allowed to freeze the drug.
2. Protection from light: The drug should be stored in a place protected from light to prevent decomposition of the active substance by light.
3. Protection from moisture: Cinnarizine should be stored in a dry place to avoid moisture in the drug package or container.
4. Keep out of reach ofchildren: The drug should be stored out of the reach of children or in a package that cannot be opened by children.
5. Storage conditions according to the type of packaging: If special storage conditions (e.g. Storage in a refrigerator or protection from moisture) are indicated on the drug package, the instructions should be followed.