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Tizanidine

Tizanidine is a fast-acting antispasmodic drug that is U.S. Food and Drug Administration–approved for the treatment of muscle spasms caused by multiple sclerosis (MS), stroke, brain injury, spinal cord injury, or musculoskeletal injury. It is also prescribed as an anticonvulsant.

6 Minute Read | Published Oct 04 2023 | Updated Mar 07 2024 Expert Verified
Emma Collins
Written by
Dameisha Gibson
Reviewed by
Emma Collins
Written by
Dameisha Gibson
Reviewed by

Common Brand Names: Zanaflex, Sirdalud, Relentus

As a centrally-acting noradrenergic alpha-2 receptor agonist, tizanidine slows down the release of amino acids that enable high-speed synaptic transmissions in the brain. In short, it allows the brain to relax.

A study has also shown that tizanidine has comparable efficacy with baclofen or diazepam and that tizanidine is more tolerable than the other two.

In the United States, Tizanidine is a prescription-only drug.

Tizanidine is primarily prescribed to manage spasticity, or the tightness of muscles due to prolonged and excessive contractions. It is a fast-acting drug, with effects peaking at about 1 to 2 hours after dosing and lasting anywhere between 3 and 6 hours.

Another common application of tizanidine is for the management of chronic neck and lumbosacral (lower back) pain. It may also be used as part of a detoxification regimen, specifically to assist patients with headaches stemming from analgesic withdrawal.

Off-label, tizanidine is used for managing neck pain, back pain, and migraine headaches. In addition, the drug can also be used for managing refractory insomnia in spastic quadriplegic patients and regional musculoskeletal pain syndromes. Patients with ALS or amyotrophic lateral sclerosis may also benefit from the effects of tizanidine.

Due to insufficient studies or proven adverse effects, tizanidine is not typically given to

  • Pregnant women
  • Nursing mothers
  • Children
  • Elderly
  • Persons with impaired renal (kidney) function
  • Persons with impaired hepatic (liver) function

While it’s not a scheduled substance under the federal drug scheduling system, tizanidine has a potential for abuse and dependence. This is particularly true for patients who have been receiving the drug for a prolonged period. Indeed, there have been reported cases of patients experiencing withdrawal symptoms after discontinuing the treatment.Tizanidine is also prone to misuse because the contents of its capsule formulation can be sprinkled on soft foods.

It’s important to note, however, that tizanidine’s abuse potential has not been completely explored in clinical studies. There is also the possibility that tizanidine abuse is underreported.

Still, there are records of patients abusing tizanidine. Many of them use the drug together with opioids, benzodiazepines, hypnotics, or a combination of painkillers.

A study also revealed that the abuse of muscle relaxants like tizanidine is very possibly induced iatrogenically. This means that it’s unintentionally caused by medical treatments or procedures that require the use of the drug.

Tizanidine Drug Interactions

Tizanidine interacts with a variety of substances, which may result in a range of unpleasant side effects. In particular, using the substances listed below concomitantly with tizanidine may increase the severity and risk of adverse events:

  • Alcohol. Taking alcohol with tizanidine can increase the amount of tizanidine in the blood. This can result in increased central nervous system (CNS) depressant effects, as well as an increase in the overall adverse reactions of the drug.
  • Other CNS Depressants. CNS depressants like benzodiazepines and opioids can produce excessive sedation when taken with tizanidine.
  • Ciprofloxacin and fluvoxamine. Patients who are taking either ciprofloxacin or fluvoxamine should not use tizanidine and vice versa. Doing so can result in decreased blood pressure and increased drowsiness. It can also impair psychomotor functions.
  • Oral contraceptives. For women taking oral contraceptives, the use of tizanidine is not advised. If it’s absolutely necessary, the patient should be monitored for adverse reactions like low blood pressure or excessive drowsiness.

Adverse Effects of Tizanidine

While tizanidine is generally a well-tolerated medication, several adverse effects may arise from both short-term and long-term use, especially when it is used as a substance of abuse. Some adverse effects associated with tizanidine use are:

  • Dry mouth
  • Drowsiness
  • Dizziness
  • Blurred vision
  • Hypotension or low blood pressure
  • Decreased heart rate
  • Urinary frequency
  • Constipation
  • Rhinitis
  • Hallucinations

Meanwhile, serious adverse effects of tizanidine include:

  • Bradycardia (slow heart rate)
  • Exfoliative dermatitis (extreme shedding of skin)
  • Long QT interval (the time from the start of the Q wave to the end of the T wave in an ECG)
  • Liver impairment
  • Hypotension (low blood pressure)
  • Syncope (fainting or loss of consciousness)
  • Steven-Johnson Syndrome (a rare skin condition that causes painful rashes and blisters)
  • Life-threatening allergic reactions

Should any of the above happen to you or someone else you know who is using or abusing tizanidine, get in touch with emergency services ASAP. If you’re able to, go to the nearest hospital to receive medical attention.

Signs of Tizanidine Overdose

Some of the most common signs of tizanidine overdose include:

  • Alterations of mental status
  • Confusion
  • Severe bradycardia
  • Severe hypotension
  • Extreme tiredness
  • Dizziness
  • Loss of consciousness
  • Slow or shallow breathing

Tizanidine: Dependence, Withdrawal, and Addiction

As mentioned, tizanidine’s potential for abuse and misuse needs to be further studied. On the other hand, there are records of patients who have developed a dependence on the drug and thus exhibited withdrawal symptoms after the cessation of tizanidine therapy. These can include the following:

  • Anxiety
  • Nausea
  • Vomiting
  • Generalized tremor
  • Dysthermia
  • Hypertension
  • Tachycardia
  • Delirium
  • Extrapyramidal symptoms (drug-induced movement disorders)
  • Autonomic dysfunction

Still, this doesn’t necessarily mean that tizanidine is addictive, only that the body can get quickly used to its presence. Once a person stops taking tizanidine, they end up developing withdrawal symptoms like tachycardia or a fast heart beat, rebound hypertension, and increased muscle tension. Addiction or substance use disorder, on the other hand, is a disorder that is characterized by continuing and compulsive drug use despite the negative consequences.

If withdrawal symptoms due to tizanidine become difficult to manage at home, your doctor may recommend that you undergo medical detoxification. This involves a series of interventions to address your drug dependence issue and to safely remove the presence of tizanidine or other drugs in your body.

Tizanidine Rehabilitation

If you feel that you or your loved one is having issues with tizanidine abuse or misuse , the best way to deal with it is to seek professional help. Through drug rehabilitation, recovery will be easier and definitely possible. There are two approaches to rehab, and one may be a better choice than the other depending on specific circumstances.

  • Inpatient treatment. Inpatient rehabilitation is a type of drug rehabilitation program that requires that you stay in the assigned treatment center for the entire duration of the treatment. You will be given different combinations of treatment modalities, including medications and behavioral therapies, especially if your tizanidine abuse problem involves other drugs or if you have co-occurring mental disorders. Counseling may be provided, along with coaching sessions that will teach you positive coping skills and other strategies to help you stay sober.
  • Outpatient treatment. For individuals with milder symptoms and are thus more likely (and willing) to be able to comply with the prescribed treatment, outpatient drug rehabilitation is ideal. In general, you can continue living and carrying out your daily routines in this setup. The only major difference is that you must attend therapy and counseling sessions at an assigned treatment center.

It may also be comforting to know that most insurance plans have a form of coverage for drug rehabilitation services. In case you don’t have insurance, there are still other ways to fund your treatment.

Get in touch with Better Addiction Care today (800) 429-7690. Our recovery support advisors are standing by to help you find the right treatment center for your needs. They can also verify your insurance coverage or assist you in looking for funding options.

A Brief History of Tizanidine

Tizanidine is a prescription medication. In 1996, it was approved for medical use by the US Food and Drug Administration (FDA).

In 2018, tizanidine was listed as the 86th most commonly prescribed medication in the US as it was prescribed more than 8 million times.

Resources

bullet U.S. National Library of Medicine, Medline Plus. (2015).
"Tizanidine."
Retrieved on July 06, 2021
bullet Ghanavatian, S. & Derian, A. (2021).
"Tizanidine. StatPearls."
Retrieved on July 06, 2021
bullet Kamen, L. et al. (2008).
"A Practical Overview of Tizanidine Use for Spasticity Secondary to Multiple Sclerosis, Stroke, and Spinal Cord Injury. Current Medical Research and Opinion."
Retrieved on July 06, 2021
bullet Acorda Therapeutics, Inc. (2013)
"Highlights of Prescribing Information: Zanaflex."
Retrieved on July 06, 2021
bullet Kitta, A. et al. (2020).
"Using Clonidine in the Treatment of Tizanidine Abuse and Withdrawal: a Case Report of a Patient with Somatoform Pain Disorder. Journal of Substance Use."
Retrieved on July 06, 2021
bullet Suarez-Lledo, A. et al. (2018).
"Management of Tizanidine Withdrawal Syndrome: A Case Report. Clinical Medicine Insights: Case Reports"
Retrieved on July 06, 2021
bullet University of Utah College of Pharmacy. (2016).
"Skeletal Muscle Relaxants Drug Class Review."
Retrieved on July 06, 2021
bullet AA Pharma Inc. (2015).
"Tizanidine Product Monograph."
Retrieved on July 06, 2021
bullet Elder, N.C. (1991).
"Abuse of Skeletal Muscle Relaxants. American Family Physician."
Retrieved on July 06, 2021
bullet Spiller, H.A. et al. (2004).
"Retrospective Review of Tizanidine (Zanaflex) Overdose. Journal of Toxicology. Clinical Toxicology."
Retrieved on July 06, 2021
bullet U.S. National Institute on Drug Abuse. (2017).
"Tolerance, Dependence, Addiction: What’s the Difference?"
Retrieved on July 06, 2021
bullet National Institute of Diabetes and Digestive and Kidney Diseases. (2012).
"Tizanidine. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury."
Retrieved on July 06, 2021
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