Tizanidine tabs 2mg #30

Tizanidine user manual

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Composition

Tizanidine contains the active substance tizanidine, as well as auxiliary components:
    anhydrous lactose;
    microcrystalline cellulose;
    colloidal silicon dioxide;
    stearic acid.

Form of issue

Tablets 2 and 4 mg, round in shape. White color.
On one side of the tablet is a separation strip, on the second marking T2 or T4.

pharmachologic effect

Tizanidine is a central muscle relaxant. Getting into the body the active substance of the drug helps to reduce the tone of skeletal muscles, reduces their resistance in passive movements, reduces spasmodic reaction, increases arbitrary contractions.
In general, the drug has a muscular-relaxing effect due to the inhibition of spinal polysynaptic reflexes. This action is due to the release of amino acids from the presynaptic terminals of spinal interneurons.

Pharmacodynamics and Pharmacokinetics

Absorption and distribution

After oral administration, tizanidine is essentially completely absorbed. Absolute bioavailability is approximately 40% (CV = 24%), because of extensive first passage through the liver.
The active substance of the preparation is distributed with an average stable distribution volume of 2.4 l / kg (CV = 21%). Binding to proteins is 30%.

Metabolism and excretion

The half-life of Tizanidine is approximately 2.5 hours (CV = 33%). Approximately 95% of the administered dose is metabolized. The main isoenzyme of cytochrome P450 is involved in the metabolism of CYP1A2 with the formation of active metabolites. The half-life is between 20 and 40 hours.
It is excreted mainly through the kidneys (60%) and the gastrointestinal tract (20%).

Indications for use Tizanidine

Tizanidine is prescribed to treat the spastic condition of skeletal muscles that accompanies the development of neurological diseases, such as:
    degenerative diseases of the spinal cord;
    stroke;
    multiple sclerosis;
    chronic myelopathy.
Also, the drug is indicated for painful spasms of skeletal muscles that develop due to damage to the spine.

Contraindications

The drug is contraindicated in patients taking potent CYP1A2 inhibitors, such as fluvoxamine or ciprofloxacin.

Side effects

During the study of the action of Tizanidine on patients, side effects such as drowsiness, dry mouth, hypotension, lowering of blood pressure, bradycardia, dizziness, weakness or asthenia, muscle spasms, hallucinations, fatigue, impaired liver function and hepatotoxicity were detected in patients.
Less frequently, treatment with this medication may result in the following undesirable effects:
    Stevens-Johnson syndrome;
    anaphylactic shock;
    exfoliative dermatitis;
    ventricular tachycardia;
    hepatitis;
    convulsions;
    depression;
    joint pain;
    paresthesia;
    rash;
    tremor.

Instructions for use Tizanidine

In accordance with the instructions for the use of Tizanidine, the recommended initial dose is 2 mg.
Since the effect of taking the tablets reaches a peak of about 1 to 2 hours after the dose is administered and is dispersed between 3 and 6 hours after administration, treatment can be conducted at an interval of 6 to 8 hours. Within a day you can take no more than three tablets.
Dosage can be gradually increased to 4 mg per dose, if after four days after the start of treatment, no positive effect will follow. The total daily dose should not exceed 36 mg. Single doses greater than 16 mg have not been studied.

Dosing in patients with renal insufficiency

Tizanidine tablets should be used with caution in patients with renal insufficiency (creatinine clearance

Dosing in patients with impaired liver function

Also, this drug should be given with caution to patients with any form of liver failure. In such patients, when titrating, individual doses should be reduced.
In the treatment of patients with hepatic insufficiency, it is necessary to regularly monitor the levels of aminotransferase. The first monitoring is recommended one month after treatment.

Overdose

During the study of the effect of this drug on the body, specialists detected cases of deliberate and accidental overdose of tizanidine. Clinical manifestations of overdose have different pharmacology.
In most cases there is a decrease in the sensorium, including lethargy, drowsiness, confusion and coma. Also, an overdose manifests itself in the dysfunction of the heart muscle, including bradycardia and hypotension.

Interaction with other drugs

Interaction with Fluvoxamine and Ciprofloxacin
The simultaneous use of fluvoxamine or ciprofloxacin and tizanidine is contraindicated. Changes in the pharmacokinetics of tizanidine when taken together with fluvoxamine or ciprofloxacin can lead to a significant reduction in blood pressure, drowsiness, and impaired psychomotor functions.

Interaction with inhibitors of CYP1A2

Because of potential drug interactions, simultaneous use of Tizanidine with other CYP1A2 inhibitors, such as Zileiton, Fluoroquinolone should be avoided.
Taking the drug together with strong inhibitors of CYP1A2 (Amiodarone, Mexiletin, Propafenone, Verapamil, Cimetidine, Famotidine, oral contraceptives, Acyclovir, and Ticlopidine) is strictly contraindicated.

Interaction with contraceptives

The simultaneous use of tizanidine with oral contraceptives is not recommended. But, if the current state of health requires treatment with the use of this drug, then the dosage should be minimal.
Incorrect dosing can lead to the development of side effects: arterial hypotension, bradycardia, excessive drowsiness.

Interaction with alcohol

Alcohol increases the concentration of the active substance of the drug in the blood, which can lead to the appearance of undesirable reactions.

Storage conditions

Store Tizanidine is recommended in a dark place at room temperature. Keep away from children.
Shelf life of the drug is 3 years.

Reviews of Tizanidine

Tizanidine is a drug that is transferred by patients in different ways. Reviews of this medication allow you to draw conclusions that far from always its reception has the expected effect.
Side effects are manifested in one of three cases. For example, Elena from Barnaul writes:
"... Tizanidine was prescribed, as they began to suffer severe muscle pains and spasms. After taking the second pill, I felt very dizzy, weak and urged to vomit. I thought that it's just that my body is so weak that it reacts so. Decided that the further taking of tablets will be normal. But no, everything went on and got even worse - problems with the stomach, pressure, strong palpitations. After going to the doctor, the pills were replaced. "
Oleg from Novosibirsk also wrote about the manifestation of an adverse reaction:
"... I started taking Tizanidine and after the first tablet I almost fell asleep right at work. I understood the mechanism of action - muscle spasm occurs during sleep. "
It is worth noting that such reviews on the Internet units, mostly reviews are positive, indicating that the effectiveness of this drug.