Pharmacodynamics and pharmacokinetics
Tizalud is a muscle relaxant with central action.
The effect of tizanidine on presynaptic α2-adrenergic receptors inhibits the release of excitatory amino acids from spinal interneurons , which leads to inhibition of polysynaptic impulse propagation in the spinal cord . Through this mechanism of action, the tone of muscle tissue . In parallel with the muscle relaxant effect , tizanidine exhibits a moderate analgesic effect.
Tizaluda tablets are effective for acute painful muscle spasms , as well as chronic spasms of cerebral and spinal etiology . Taking the drug reduces clonic convulsions and spasticity , as a result of which the resistance to passive movements decreases and the possibility of active actions increases.
Pharmacological properties of the drug Tizalud
Centrally acting muscle relaxant. The mechanism of action is associated with stimulation of presynaptic α2 receptors, which leads to suppression of the release of excitatory amino acids (glutamic acid, aspartic acid), which stimulate receptors for N-methyl-D-aspartate. As a result, polysynaptic transmission of excitation is suppressed at the level of interneurons of the spinal cord. It also has a moderate central analgesic effect due to inhibition of the function of interneurons of the dorsal horns of the spinal cord. Reduces resistance to passive movements, reduces spasms and clonic convulsions, increases the strength of voluntary contractions. Does not affect neuromuscular transmission. After use, tizanidine is quickly and almost completely absorbed from the gastrointestinal tract. Concomitant food intake does not affect the pharmacokinetics of tizanidine. In the dose range from 4 to 20 mg, the pharmacokinetics of the drug is linear. The drug is characterized by a low individual range of pharmacokinetic parameters. The maximum concentration in blood plasma is achieved 1–2 hours after administration. Due to the pronounced effect of the first passage through the liver, bioavailability is 34%, binding to plasma proteins is 30%. Tizanidine is quickly and in large quantities metabolized in the liver to form inactive metabolites. Penetrates through the blood-brain barrier and in small amounts into breast milk. The half-life of elimination from the systemic circulation is 2–4 hours. Excretion occurs mainly by the kidneys (60–70%) and intestines (20–25%), mainly in the form of metabolites, as well as unchanged (about 5%). In patients with renal failure (creatinine clearance ≤25 ml/min), the maximum concentration in blood plasma is 2 times higher than that in healthy volunteers, the half-life is extended to 14 hours. When taken orally, the effect of the drug appears after 30–45 minutes, the maximum effect occurs within 1–2 hours.
Indications for use
Muscle spasms in pathologies of the spine, accompanied by pain , including hemiplegia , spondylosis , osteochondrosis , syringomyelia , lumbar and cervical syndromes.
Postoperative period after surgery for osteoarthritis of the hip joint and intervertebral hernias .
Pain syndrome and spasticity provoked by neurological diseases , including chronic myelopathy , multiple sclerosis , cerebral palsy , degenerative changes in the spinal cord, stroke cerebral circulatory disorders , traumatic brain injuries, convulsions of central origin.
General characteristics of the drug
Tizalud belongs to adrenergic agonists - stimulants (agonists) of alpha 2 adrenergic receptors. This group of substances has the following properties:
- cause depolarization of synaptic fibers, which leads to relaxation of smooth muscles;
- help reduce the release of norepinephrine;
- inhibit the activity of vascular activity, which reduces heart rate and leads to dilation of blood vessels.
The main therapeutic value is the muscle relaxant effect of the drug. Its activity is aimed at suppressing polysynaptic reflexes of the spinal cord and relaxing the muscle frame.
Tizalud is a muscle relaxant, the action of which is aimed at reducing the tone of the flexor and extensor muscles
The mechanism of action of the drug is to block the transmission of impulses between neurons. The active substance inhibits the release of the mediator glutamic acid and acts directly on neurotransmitter receptors, causing a cell response. As a result of the blockade of spinal synaptic impulses, the contraction of skeletal muscles stops.
Contraindications
- hypersensitivity to tizanidine or other constituent ingredients of Tizalud tablets;
- severe liver pathologies;
- periods of breastfeeding and pregnancy ;
- age under 18 years;
- parallel therapy with the use of Ciprofloxacin , fluvoxamine and other strong inhibitors of the CYP1A2 isoenzyme .
Carefully:
- age over 65 years;
- renal failure;
- bradycardia;
- arterial hypotension;
- use of oral contraceptives .
Contraindications and special conditions
The use of Tizalud has several limitations. The drug is contraindicated in the following cases:
- intolerance to the components of the drug;
- simultaneous use with ciprofloxacin-containing drugs, Fluvoxamine and other inhibitors of CYP1A2 isoenzymes;
- severe form of liver and kidney pathologies.
The presence of arterial hypotension may be a contraindication for taking the medicine. Tizalud has the ability to lower blood pressure and reduce heart rate, which is also a limitation if the patient has bradycardia.
It is not recommended to prescribe treatment with tizanidine during pregnancy and breastfeeding. Therapy is carried out with caution in childhood, since there is insufficient clinical data on safety for the child’s body. In old age, more careful dose selection and monitoring of creatinine clearance are required.
Side effects
Treatment with Tizalud may be accompanied by some changes in the nervous, cardiovascular and digestive systems. These include the following side effects:
- drowsiness and sleep disturbances;
- dizziness;
- decreased heart rate;
- low blood pressure;
- muscle weakness;
- increased liver transaminases (ALT and AST);
- dyspeptic disorders.
During long-term treatment, it is recommended to monitor liver function at least once a month.
Tizalud causes a slowing of psychomotor reactions
The interaction of the active substance with antihypertensive drugs contributes to the development of bradycardia and a severe drop in blood pressure.
When taken simultaneously with sedatives, the effect of the latter is enhanced. Tablets containing tizanidine should not be mixed with alcohol to avoid inhibiting the reaction.
Side effects
CNS:
- dizziness;
- drowsiness;
- hallucinations;
- sleep disorders;
- insomnia.
The cardiovascular system:
- decreased blood pressure;
- bradycardia.
Digestive system:
- dry mouth;
- dyspepsia;
- nausea;
- hepatitis;
- increased activity of “liver” transaminases;
- liver failure.
Musculoskeletal system:
- muscle weakness.
Other:
- hypercreatininemia;
- increased fatigue.
Abrupt withdrawal of Tizalud after combined use with antihypertensive drugs and long-term therapy and/or use of large doses can lead to increased blood pressure , tachycardia , and in some cases to acute cerebrovascular accident .
Tizalud tablets, instructions for use
The drug tablets are taken orally (orally) with water, regardless of meals.
Instructions for the use of Tizalud for neurological pathologies that cause spastic painful muscle contractions recommend starting treatment with a daily dose of 6 mg, taken in three doses. Every next 3-7 days, depending on the nature of the pain and spasm , increase the dose by 2-4 mg. The maximum therapeutic effect is observed when taking a daily dose of 12-24 mg. The dose of 36 mg is the maximum permissible daily dose.
To relieve painful spasms of skeletal muscles, Tizalud 2-4 mg is prescribed 3 times a day. In particularly severe situations, an additional dose of 2-4 mg at night is recommended.
The duration of Tizalud administration depends on the dynamics of pain and muscle-tonic manifestations. Acute muscle pain usually requires therapy for 7-21 days. Chronic pain syndrome , depending on its origin and severity, may require longer-term treatment, which is determined individually and sometimes lasts up to 1 year.
Overdose
In case of gross violation of the dosage regimen and taking increased doses of Tizalud, the following were observed: nausea , turning into vomiting , development of hypotension , drowsiness , dizziness, miosis , respiratory problems , anxiety, coma .
They recommend immediate gastric lavage , bowel cleansing with an enema, taking activated charcoal , forced diuresis and further symptomatic therapy.
Interaction
Ciprofloxacin , Fluvoxamine and other strong inhibitors of the CYP1A2 isoenzyme , including Amiodarone , Propafenone , Mexiletine , Cimetidine , Enoxacin , Norfloxacin , Pefloxacin , Rofecoxib , Ticlopidine and oral contraceptives is not allowed .
Antihypertensive drugs increase the risk of bradycardia and low blood pressure .
Sedatives and ethanol may enhance the sedative effects of tizanidine .
Analogs of Tizalud
Level 4 ATC code matches:
Tizanil
Tizanidine
Tolperisone-OBL
Mydocalm
Baklosan
Sirdalud
Baclofen
Analogues of Tizalud that are similar in their action are represented by the following drugs: Lioresal , Baklosan , Mydocalm , Tolperisone , Tolperil and some others.
Analogues of the drug
Pharmacies offer a range of muscle relaxants, the main active ingredient of which is tizanidine. The table shows some analogues of Tizalud and their approximate cost.
| Name | Release form and quantity per package | Cost, rub |
| Sirdalud MR, 6 mg | modified release capsules, 30 pcs. | 498 |
| Tizanil, 4 mg | tablets, 20 pcs. | 216 |
| Tizanidine-Teva, 4 mg | tablets, 30 pcs. | 187 |
Among the line of similar medicines there are drugs with dosages of 2, 4 and 6 mg, in terms of the main active ingredient.
One of the drugs similar to Tizalud in pharmacological properties is Mydocalm. It is also a centrally acting muscle relaxant. The difference between Mydocalm is its effect on strychnine and the decrease in the increase in reflex excitability provoked by strychnine.
Reviews of Tizalude
On user forums there are both positive and negative reviews about Tizaluda. Typically, negative reviews most often concern the side effects of the drug that occur immediately after taking the first dose and are manifested by a decrease in blood pressure , weakness , dizziness , lethargy and drowsiness . Such effects are possible when taking the drug in large doses or if the patient has any contraindications. Therefore, even if you completely trust your doctor, it is better to start therapy by taking half or even a quarter of the recommended dose and, if the drug is well tolerated, switch to using the full dose.
Many patients are satisfied with the effectiveness of Tizalud, noting its rapid action and the absence of side effects. Of course, any medicine is individual for each individual patient, and if Tizalud did not cause any negative reactions in you, then most likely it will become a truly effective remedy.
Use during pregnancy or breastfeeding
Pregnancy. There is limited data on the use of Tizalud in pregnant women, so it should not be prescribed during pregnancy unless the potential benefit to the mother outweighs the possible risk to the fetus.
Lactation. It has been established that tizanidine passes into breast milk in small quantities. Therefore, women who are breastfeeding should not prescribe the drug.
Fertility. Available data indicate that tizanidine administered at a dose of 10 mg/kg per day in male rats and at a dose of 3 mg/kg per day in female rats did not cause impairment of fertility. Decreased fertility was observed in male rats that received tizanidine at a dose of 30 mg/kg per day and in female rats that received tizanidine at a dose of 10 mg/kg per day. Sedation, weight loss, and ataxia have also been observed with these doses.
Tizaluda price, where to buy
The average price of Tizalud in Russian pharmacies is: 130 rubles for 30 tablets of 2 mg and 175 rubles for 30 tablets of 4 mg.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Tizalud tablets 4 mg 30 pcs. JSC Veropharm
RUB 244 order
Pharmacy Dialogue
- Tizalud (tab. 4 mg No. 30) Veropharm
RUB 218 order
- Tizalud (tab. 2 mg No. 30) Veropharm
150 rub. order
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Pharmacy24
- Tizalud 4 mg No. 30 tablets PAT "Kiev Vitamin Plant", Kiev, Ukraine
126 UAH. order - Tizalud 2 mg No. 30 tablets PAT "Kiev Vitamin Plant", Kiev, Ukraine
96 UAH order
Composition and release form
The active ingredient of Tizalud is tizanidine, which belongs to the pharmacological group of centrally acting muscle relaxants. The main difference between the drug and other similar drugs is the possibility of oral use.
One tablet contains:
- tizanidine hydrochloride 2 mg (active ingredient);
- Lactopress 117 mg, magnesium stearate 2.5 mg, microcrystalline cellulose 14 mg, Primogel 4.2 mg (excipients).
Available in the form of biconvex tablets with a score, white or yellowish in color, and in the form of capsules. Manufactured by Veropharm, Teva, Novartis.
