What Is Tizanidine?

Tizanidine, also known as spasm, mitthiadiazole, is a white solid chemical. The chemical name is 5-chloro-4- (4,5-dihydro-1H-imidazol-2-yl) -2,1,3-benzothiadiazole-4-amine, and the molecular formula is C ₉ H ₈ ClN ₅ S , Molecular weight is 253.71100, melting point is 221 ~ 223 ° C. Tizanib is a skeletal muscle relaxant. It is mainly used for painful muscle spasm in clinical practice.

Chinese name: Tizanidine
Foreign name: tizanidine

CAS number: 51322-75-9
Molecular formula: C9H8ClN5S

Introduction to Tizanidine Compounds

Tizanidine Basic Information

Chinese name:

Chinese alias: 5-chloro-4- (4,5-dihydro-1H-imidazol-2-yl) -2,1,3-benzothiadiazole-4-amine

English name: tizanidine

English alias: Tizanidinum [INN-Latin]; 5-chloro-N- (4,5-dihydro-1H-imidazol-2-yl) -2,1,3-benzothiadiazol-4-amine; Ternelin; Tizanidina [INN- Spanish]; Sirdalud

CAS number: 51322-75-9

Molecular formula: C ₉ H ₈ ClN ₅ S

Chemical structure:

Molecular weight: 253.71100

Exact mass: 253.01900

PSA: 90.44000

LogP: 1.55320 ^[1]

Tizanidine physical and chemical properties

Appearance and properties: white solid

Density: 1.82 g / cm ³

Melting point: 221-223ºC

Boiling point: 391.2ºC at 760 mmHg

Flash point: 190.4ºC

Stability: This material is stable if stored as directed.

Storage conditions: This product should be stored at room temperature. It should be kept in a tightly closed container. ^[1]

Tizanidine drug name

Chinese name:

English name: Tizanidine

Alias

Spasm Pain; Mitizodiazole; Sondele; Titonidine; Sirdalud; Ternelin; Tizanidin; Tizanidine Hydrochloride; Tizanidi-num; Zanaflex ^[2]

Tizanidine Classification

Anesthetics and Adjuvants> Skeletal Muscle Relaxants ^[2]

Tizanidine dosage form

2mg / tablet; 4mg / tablet; 6mg / tablet.

Tizanidine pharmacological effects

Tizanidine is a central muscle relaxant. It is an imidazole derivative that selectively inhibits multiple synaptic mechanisms related to excessive muscle tension and reduces the release of excitatory amino acids by intermediate neurons. Tizanidine does not affect the transmission of nerves and muscles, and is well tolerated. It can reduce the resistance to passive movements, reduce spasms and clonics, and increase the intensity of voluntary exercise. It is effective for acute painful muscle spasms and chronic tonicity originating from the spinal cord and brain. Tizanidine can also increase the anti-inflammatory effects of non-steroidal anti-inflammatory drugs (NSAIDs) and prevent NSAID-induced gastric mucosal damage. In animal experiments, tizanidine can reduce gastric acid secretion and reverse gastric mucosal glycoprotein reduction caused by aspirin. Tizanidine works similarly to baclofen. People who are ineffective or intolerant to baclofen can use tizanidine. Tizanidine and diazepam have similar effects in the treatment of spasticity in patients with hemiplegia and paraspinal muscle spasms, but in the treatment of paraspinal muscle spasms, tizanidine works faster.

Tizanidine pharmacokinetics

The bioavailability of the oral tablet is 40%, and the peak time (T _max ) is 1 to 2 hours. For the convulsive state, the effect can be taken orally for two weeks, and the maximum effect can be achieved at 8 weeks. Food can increase the peak concentration (C _max ) by 1/3 and decrease T _max by 40 min, but it does not affect absorption. The total protein binding rate was 30%. When tizanidine was administered at 4-20 mg, the half-life (t _1/2 ) was 2.1-4.2 h, and the distribution volume was 2.4 L / kg. It is metabolized mainly in the liver and metabolites are not active. The original drug and metabolites are mainly excreted by the kidney, and a small part is excreted by feces. Tizanidine is fat-soluble and may be secreted with milk. The clearance t _1/2 of the original drug is 2.5 h, and the clearance t _1/2 of the metabolite is 20 to 40 h ^[2] .

Tizanidine indication

1. For painful muscle spasms, such as cervical and lumbar syndrome (such as torticollis, lower back pain), lumbar disc herniation or hip osteoarthritis related to spinal stasis and dysfunction, postoperative pain.

2. For neurotic tonic states, such as increased muscle tone due to multiple sclerosis, chronic myelopathy, degenerative spinal cord disease, cerebrovascular disease and cerebral palsy.

3. Tizanidine may also have effects on chronic tension headaches that cannot be controlled by traditional therapies (such as antidepressants) ^[2] .

Tizanidine contraindications

Allergies to tizanidine are contraindicated ^[2] .

Tips for tizanidine

1. Tizanidine adverse reactions are dose-related. With increasing doses, the symptoms of adverse reactions are more frequent and obvious.

2. During the treatment delay period, liver and kidney function tests, serum electrolyte tests, and whole blood count classification should be performed. It is recommended to regularly monitor the aminotransferase level, which can be monitored during the first month, the third month, and the sixth month of treatment, and beyond.

3. Avoid taking activities that require high concentration such as driving, climbing, and operating precision instruments while taking tizanidine.

4. Use with caution in patients with liver disease (especially liver damage).

5. Patients with hypotension or taking antihypertensive drugs at the same time should be used with caution.

6. Patients with impaired renal function (creatinine clearance of 25-50ml / min) should be used with caution.

7. Used with caution in elderly patients.

8. The safety of children, pregnant women and lactating women has not been determined, and should be used with caution ^[2] .

Tizanidine adverse reactions

1. Common hypotension is dose-related (dosage is greater than 2mg), mostly mild. Bradycardia, palpitations, and premature ventricular contractions are rare and transient. Orthostatic hypotension, dizziness, dizziness, and syncope have also been reported.

2. Central nervous system: common sedation and drowsiness. Insomnia, fatigue or sleepiness are also common. It causes fewer headaches, nervousness, dizziness, anxiety, syncope, and tremor, and reports of depression, weakness, paresthesia, hallucinations, and delusions.

3. Endocrine / metabolism: high fever.

4. Digestive system: dry mouth, nausea, vomiting, indigestion, diarrhea or constipation are common. There have been reports of liver damage and even liver failure leading to death.

5. Skin: Occasionally rash, sweating, skin ulcers and itching during medication.

6. Skeletal muscles: often with back pain and muscle weakness.

7. Others: Tizanidine rarely causes dependence ^[2] .

Tizanidine dosage

1. 2 to 4 mg each time, 3 times a day. For severe pain, 2 to 4 mg can be added at night.

2. The dose of neurotic tonicity should be individualized. The dose on the first day should not exceed 6mg. Increase every 2 to 4 mg every 0.5 to 1 week. Generally the best effective dose is 12 to 24 mg daily, divided into 3 to 4 times. The maximum recommended daily dose is 36 mg ^[2] .

Tizanidine Drug Interactions

1. Tizanidine can delay the T _{max of} acetaminophen.

2. Contraceptives can reduce the clearance of tizanidine, thereby increasing the adverse reactions of tizanidine.

3. Tizanidine combined with phenytoin and fosphenytoin can increase the risk of phenytoin poisoning (ataxia, hyperreflexia, nystagmus, tremor, etc.).

4. Ethanol can increase the C _max (about 15%) and area under the curve (about 20%) of tizanidine. The combination of the two may increase the inhibitory effect on the central nervous system ^[2] .