Tizanidine tablets: instructions for use, price, reviews and analogues

pharmachologic effect

Tizanidine is a centrally acting muscle relaxant. When the active substance of the drug enters the body, it helps to reduce the tone of skeletal muscles, reduces their resistance during passive movements, reduces the spasmodic reaction, and enhances voluntary contractions.

In general, the drug has a muscle-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.

Pharmacological properties of the drug Tizanidine

A centrally acting muscle relaxant, it has an antispastic effect in chronic spastic conditions of spinal and cerebral origin, eliminates acute painful muscle spasms and clonic convulsions. Tizanidine reduces muscle resistance to passive movements and also increases the strength of voluntary muscle contractions. Does not affect neuromuscular transmission. The mechanism of action of tizanidine is likely due to a decrease in the release of excitatory amino acids from interneurons, which leads to selective suppression of polysynaptic mechanisms of the spinal cord responsible for muscle hypertonicity. When taken orally, it is quickly and almost completely absorbed from the digestive tract. Simultaneous food intake does not affect the absorption of tizanidine. The maximum concentration in the blood plasma is reached after 1–2 hours. Plasma protein binding is insignificant - 30%. Metabolism occurs mainly in the liver. Metabolites do not have pronounced pharmacological activity. The parent substance and its metabolites are excreted mainly by the kidneys (approximately 70%). The half-life is 3–5 hours.

Pharmacodynamics and Pharmacokinetics

Absorption and distribution

After oral administration, Tizanidine is essentially completely absorbed. Absolute bioavailability is approximately 40% (CV = 24%), due to extensive first pass through the liver.

The active substance of the drug is distributed with an average steady-state volume of distribution of 2.4 l/kg (CV = 21%). Protein binding 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. Their half-life ranges from 20 to 40 hours.

Excreted mainly through the kidneys (60%) and the gastrointestinal tract (20%).

Indications for use of Tizanidine

Tizanidine is prescribed for the treatment of skeletal muscle spasticity, which accompanies the development of neurological diseases, such as:

degenerative diseases of the spinal cord;
stroke;
multiple sclerosis;
chronic myelopathy.

The drug is also indicated for painful spasms of skeletal muscles that develop as a result of damage to the spine.

Side effects

In studies of the effects of Tizanidine in patients, side effects such as drowsiness , dry mouth , hypotension , decreased blood pressure, bradycardia , dizziness , weakness or asthenia , muscle cramps, hallucinations , fatigue, liver dysfunction and hepatotoxicity were identified.

Less commonly, the following unwanted effects may occur during treatment with this drug:

Stevens-Johnson syndrome;
anaphylactic shock;
exfoliative dermatitis;
ventricular tachycardia;
hepatitis;
convulsions;
depression;
joint pain;
paresthesia;
rash;
tremor.

Special instructions for the use of Tizanidine

Caution should be exercised when prescribing tizanidine to patients with impaired renal and/or liver function. Patients who experience drowsiness when taking tizanidine should, at the beginning of treatment, avoid all activities that require increased concentration (driving, working with potentially dangerous mechanisms). Experience with tizanidine in children is limited. The safety of tizanidine during pregnancy has not been established. If it is necessary to prescribe tizanidine during breastfeeding, breastfeeding should be discontinued.

List of pharmacies where you can buy Tizanidine:

Moscow
Saint Petersburg

Instructions for use of Tizanidine (Method and dosage)

In accordance with the instructions for use of Tizanidine, the recommended starting dose is 2 mg.

Because the effect of the tablets peaks approximately 1 to 2 hours after dosing and dissipates between 3 and 6 hours after dosing, treatment may be given at 6 to 8 hour intervals. You can take no more than three tablets during the day.

The dosage may be gradually increased to 4 mg per dose if there is no benefit after four days of starting treatment. The total daily dose should not exceed 36 mg. Single doses greater than 16 mg have not been studied.

Dosing in patients with renal impairment

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

Dosing in patients with hepatic impairment

Also, this drug should be prescribed with caution to patients with any form of liver failure. In such patients, individual doses should be reduced during titration.

When treating patients with liver failure, aminotransferase levels should be regularly monitored. First monitoring is recommended one month after treatment.

Use of the drug Tizanidine

To eliminate painful muscle spasms, 2-4 mg is prescribed 3 times a day. In severe cases, an additional 2–4 mg is prescribed at night. In case of spastic muscle condition caused by neurological diseases, the dose should be set individually, taking into account the patient's response to tizanidine. The initial dose should not exceed 6 mg/day, the frequency of administration is 3 times a day. The dose is gradually increased by 2–4 mg at intervals of 3–4 days to 1 week. The optimal therapeutic effect is usually achieved at a dose of 12–24 mg/day, divided into 3–4 doses at equal intervals. The dose should not exceed 36 mg/day.

Overdose

During a study of the effects of this drug on the body, specialists identified cases of intentional 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 . Overdose also manifests itself in cardiac muscle dysfunction, including bradycardia and hypotension.

Tizanidine-SZ

When using the drug Tizanidine-SZ with inhibitors of the CYP1A2 isoenzyme, an increase in the concentration of tizanidine in the blood plasma is possible. In turn, an increase in the concentration of tizanidine in the blood plasma can lead to symptoms of drug overdose, including prolongation of the QT(c) interval.

The simultaneous use of Tizanidine-SZ with inducers of the CYP1A2 isoenzyme may lead to a decrease in the concentration of tizanidine in the blood plasma, which may lead to a decrease in the therapeutic effect of the drug.

Contraindicated combinations with tizanidine

The simultaneous use of tizanidine with fluvoxamine or ciprofloxacin, inhibitors of the CYP1A2 isoenzyme, is contraindicated. When tizanidine was used with fluvoxamine or ciprofloxacin, a 33-fold and 10-fold increase in tizanidine AUC was observed, respectively. The result of simultaneous use may be significant and prolonged hypotension accompanied by drowsiness, dizziness, and a decrease in the speed of psychomotor reactions (in some cases, up to circulatory collapse and loss of consciousness).

Not recommended combinations with tizanidine

It is not recommended to use tizanidine simultaneously with other inhibitors of the CYP1A2 isoenzyme - antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, some fluoroquinolones (enoxacin, pefloxacin, norfloxacin), rofecoxib, oral contraceptives, ticlopidine.

Combinations with tizanidine requiring caution

Caution must be exercised when using Tizanidine-SZ simultaneously with drugs that prolong the QT interval (for example, cisapride, amitriptyline, azithromycin).

Antihypertensive drugs

The simultaneous use of Tizanidine-SZ with antihypertensive drugs, including diuretics, can sometimes cause a pronounced decrease in blood pressure (in some cases, up to circulatory collapse and loss of consciousness) and bradycardia.

When the drug Tizanidine-SZ was abruptly discontinued after simultaneous use with antihypertensive drugs, the development of tachycardia and an increase in blood pressure was observed, which in some cases can lead to acute cerebrovascular accident.

Rifampicin

Simultaneous administration of tizanidine and rifampicin leads to a 50% decrease in the concentration of tizanidine in the blood plasma. As a result, the therapeutic effect of the drug may be reduced, which may be clinically significant for some patients. Long-term simultaneous use of rifampicin and tizanidine should be avoided; if this is not possible, careful selection of the dose of tizanidine (increase) is recommended.

Smoking tobacco

The systemic bioavailability of tizanidine in smoking patients (more than 10 cigarettes per day) is reduced by approximately 30%. Long-term drug therapy in patients in this category may require higher doses of tizanidine than the average therapeutic dose.

Alcohol

During drug therapy, you should avoid drinking alcohol, as it may increase the likelihood of adverse events (for example, decreased blood pressure and lethargy). Tizanidine may enhance the depressant effect of alcohol on the central nervous system.

Other medicines

Sedatives, hypnotics (benzodiazepine, baclofen) and other drugs such as antihistamines may also increase the sedative effect of tizanidine. Avoid taking the drug with other alpha2-adrenergic agonists (eg, clonidine) due to the potential for increased hypotensive effects.

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 decrease in blood pressure, drowsiness and impaired psychomotor functions.

Interaction with CYP1A2 inhibitors

Due to potential drug interactions, concomitant use of tizanidine with other CYP1A2 inhibitors such as zileuton and fluoroquinolone should be avoided.

Taking the drug together with strong CYP1A2 inhibitors ( Amiodarone , Mexiletine , Propafenone , Verapamil , Cimetidine , Famotidine , oral contraceptives, Acyclovir and Ticlopidine ) is strictly contraindicated.

Interaction with contraceptives

Concomitant use of Tizanidine with oral contraceptives is not recommended. But, if the current health condition requires treatment with 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 unwanted reactions.

Tizanidine

When using the drug Tizanidine with inhibitors of the CYP1A2 isoenzyme, an increase in the concentration of tizanidine in the blood plasma is possible. In turn, an increase in the concentration of tizanidine in the blood plasma can lead to symptoms of drug overdose, including prolongation of the QT(c) interval.

Concomitant use of Tizanidine with inducers of the CYP1A2 isoenzyme may lead to a decrease in the concentration of tizanidine in the blood plasma, which may lead to a decrease in the therapeutic effect of the drug.

Contraindicated combinations with tizanidine

Concomitant use of tizanidine with fluvoxamine or ciprofloxacin, inhibitors of the CYP1A2 isoenzyme, is contraindicated.

When tizanidine was used with fluvoxamine or ciprofloxacin, a 33-fold and 10-fold increase in tizanidine AUC was observed, respectively. The result of simultaneous use may be significant and prolonged hypotension, accompanied by drowsiness, dizziness, and a decrease in the speed of psychomotor reactions (in some cases, up to circulatory collapse and loss of consciousness).

Combinations not recommended with tizanidine

Combinations with tizanidine

Requiring caution Caution
must be exercised when co-administering Tizanidine with drugs that prolong the QT interval (for example, cisapride, amitriptyline, azithromycin) .

Antihypertensive drugs

The simultaneous use of Tizanidine with antihypertensive drugs, including diuretics, can sometimes cause a pronounced decrease in blood pressure (in some cases, up to circulatory collapse and loss of consciousness) and bradycardia.

When tizanidine was abruptly discontinued after simultaneous use with antihypertensive drugs, the development of tachycardia and an increase in blood pressure was observed, which in some cases can lead to acute cerebrovascular accident.

Rifampicin

Simultaneous administration of tizanidine and rifampicin leads to a 50% decrease in the concentration of tizanidine in the blood plasma. As a result, the therapeutic effect of the drug may be reduced, which may be clinically significant for some patients. Long-term simultaneous use of rifampicin and tizanidine should be avoided; if impossible, careful selection of the dose of tizanidine (increase) is recommended.

Smoking tobacco

Alcohol

Alcohol intake should be avoided during drug therapy, as it may increase the likelihood of adverse events (for example, decreased LD and lethargy). Tizanidine may enhance the depressant effect of alcohol on the central nervous system.

Other medicines

Tizanidine analogs

Level 4 ATC code matches:
Tizanil

Tolperisone-OBL

Tizalud

Mydocalm

Baklosan

Sirdalud

Baclofen

There are analogues of Tizanidine on the pharmaceutical market, which include:

Sirdalud
Tizalud
Tizanil

Reviews of Tizanidine

Tizanidine is a drug that is tolerated differently by patients. Reviews about this drug allow us to conclude that taking it does not always have the expected effect.

Side effects occur in one out of three cases. For example, Elena from Barnaul writes:

“... Tizanidine was prescribed because I began to suffer from severe muscle pain and spasms. After taking the second pill, I felt severe dizziness, weakness and the urge to vomit. I thought it was just my body being so weak that it was reacting this way. I decided that continuing to take the pills would be fine. But no, everything continued and got worse - problems with the stomach, blood pressure, palpitations. After contacting a doctor, the tablets were replaced.”

It is worth noting that there are only a few such reviews on the Internet; reviews are mostly positive, which indicates the effectiveness of this drug.

Tizanidine price

The cost of Tizanidine is optimal in terms of price/quality ratio, which is why many specialists prescribe these tablets for the treatment of their patients.

The price of Tizanidine tablets varies from 120 to 200 rubles and depends on the quantitative content of the active substance in one tablet.

Online pharmacies in RussiaRussia

ZdravCity

Tizanidine tab.
2mg No. 30Ozon LLC/Ozone Pharm LLC 134 rub. order
Tizanidine-SZ tablets 2mg 30pcsNAO Northern Star
148 RUR order
Tizanidine tablets 4 mg 30 pcs. Berezovsky Pharm. z-d JSC
147 RUR order
Tizanidine tablets 2 mg 30 pcs. Berezovsky Pharm. z-d JSC
124 RUR order
Tizanidine tab. 4mg No. 30Ozon LLC/Ozone Pharm LLC
RUB 236 order