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Tizanidine Profile: Abuse, Effects and Treatment

Like many other prescription FDA-approved medications, tizanidine can be addictive. Tizanidine is not a narcotic. The drug is considered to be a muscle relaxer that helps to reduce pain, but in a different way than a narcotic. Rather than binding to pain receptors in the central nervous system, tizanidine blocks pain involving the skeletal muscle areas. Because tizanidine is not a narcotic, there is a societal perception that it is not as dangerous or addictive as narcotics. Consequently, tizanidine abuse has become more socially acceptable.

Identifying Tizanidine

Tizanidine comes in the form of small white tablets, commonly imprinted with E34. The most common brand name is Zanaflex and it is most often prescribed to treat muscle spasms. When abused, the medication is taken more often and for a longer duration than medically recommended. Tizanidine is a generic prescription drug but is known by other brand names, including:

  • Zanaflex
  • Sirdalud
  • Relentus
  • Tizanadine (intentional misspelling)
  • Xanaflex

What Does Tizanidine Do?

Tizanidine is an antispasmodic prescription drug prescribed to be taken orally at designated intervals of time. It is typically used to treat symptoms occurring as the result of multiple sclerosis, stroke, spinal and brain injury. The drug is a controlled, pain-relief medicine that must be prescribed by a doctor. A common question asked is, “Is Tizanidine a narcotic?” The answer is that it is not a narcotic because it is a muscle relaxer. Technically speaking, it is an alpha-2 adrenergic agonist used for treating:

  • Muscle cramping
  • Muscle spasms
  • Extreme tightening of muscles

Traumatic injuries and some diseases may require the use of tizanidine including:

  • Spine or central nervous system injuries
  • Spastic diplegia
  • Severe and persistent back pain
  • Multiple sclerosis

Tizanidine is an FDA-approved muscle relaxer medication used to treat muscle spasticity caused by:

  • Traumatic brain injury
  • Multiple sclerosis
  • Spinal cord injury

It can also be effectively used to manage pain associated with:

  • Lumbosacral neuralgia
  • Chronic neck issues
  • Musculoskeletal pain syndrome
  • Migraine headaches

Tizanidine is used in some cases as an anti-convulsant effective for the managing of migraine headaches and severe insomnia. Spasm and muscle tone are symptoms in those who have had a stroke, multiple sclerosis, brain or spinal injury. Tizanidine is effective for slowing down brain and nervous system action, allowing the muscle systems to relax. Muscle relaxers have a half-life of about 37 hours, and it takes 3-5 days for the drug to be completely eliminated from your body.

Addiction to Tizanidine

A case study conducted by NIH reported that addiction to tizanidine occurs when the average dose exceeds 20 to 36 mg. If you have been taking tizanidine regularly for a prolonged period of time, you will more than likely experience symptoms once you cease to take it.

Does Tizanidine Have Addictive Qualities?

Like many other similar drugs, tizanidine can be addictive. Sometimes addiction develops as the result of misuse; at other times, prolonged use may lead to addiction. Tizanidine affects the central nervous system, which leads to withdrawal symptoms when it is stopped immediately.

What Are the Dangers of Abusing Tizanidine

If you are taking tizanidine in high doses for a prolonged period (more than nine weeks), you may experience the following symptoms:

  • Hypertension
  • Tachycardia
  • Spasticity

Those who abuse this drug typically mix it with other drugs, which can cause more complicated risks and side effects. Severe drowsiness, increased euphoria, confusion and/or other symptoms are common.

Doctors employ a gradual reduction plan for patients taking this drug to try to avoid withdrawal symptoms. The withdrawal symptoms experienced may include:

  • Tachycardia
  • Hypertension
  • Tremor
  • Hypertonia
  • Severe anxiety

Tizanidine is a short-acting medication and its effects take 1-3 hours to activate.

Signs of Short-Term and Long-Term Abuse

Patients who abuse tizanidine may do so because they are experiencing pain and want to relieve their pain using the muscle relaxer. However, taking higher doses than what is prescribed often provides a euphoric feeling that can become addictive.

If you notice that a loved one is experiencing the following physical issues, they may be suffering from the potential side effects of tizanidine abuse or addiction:

  • drowsiness or weakness;
  • nervousness
  • blurred vision
  • flu-like symptoms
  • intense dry mouth
  • abnormal liver function
  • chronic runny nose or sore throat
  • urination problems
  • sporadic muscle movements

The drug may impair thinking or reactions. The risks of poor judgment and falling asleep at the whee are high for those who drive while taking tizanidine. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

A short-term addiction to tizanidine can be tricky to identify: It does not manifest itself in the more obvious ways that a short-term addiction to narcotics would. The most dangerous part of tizanidine addiction are the risks associated with withdrawal when a long-term user stops taking the drug.

To prevent addiction, it is important that patients take the drug exactly as prescribed and stay in close communication with their healthcare provider.

Often patients are instructed to take tizanidine up to three times in one day if needed. Allow 6-8 hours to pass between doses.

Tizanidine may be taken with or without food, but it is important to take it the same way each time. Taking tizanidine with food sometimes and taking it without food other times can reduce the effectiveness of the medicine.

Follow your doctor’s instructions carefully and contact your doctor immediately if you notice any changes.

Treatment for Tizanidine Addiction

As with other drugs, treatment for tizanidine addiction will depend on the severity of the addiction. Withdrawal should be supervised by a doctor to minimize potentially dangerous withdrawal symptoms. A step-down regiment by which the dosage is gradually reduced over time is the best course for addressing dependency and addiction.

Tizanidine side effects are commonly present after the medication is abruptly stopped, which is why doctors will regulate the process. Most Tizanidine warnings are related to withdrawal of the medicine. Related warnings include:

  • Hypotension
  • Liver injury
  • Increased drowsiness
  • Hallucination
  • Hypersensitivity reactions
  • Withdrawal adverse reactions
  • Nonclinical toxicology

Going off the drug on your own is dangerous and may lead to severe symptoms. The way in which other drugs interact with the drug can also increase the danger and complicate the treatment plan. Often, treatment for a tizanidine problem can be completed in an outpatient capacity. When an addiction is severe, inpatient treatment is the better choice.

 

Tizanidine: 7 things you should know

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Medically reviewed by Carmen Pope, BPharm. Last updated on April 4, 2023.

1. How it works

  • Tizanidine may be used to treat spasticity associated with a brain or spinal injury.
  • Tizanidine works by a central mechanism (this means it acts in the brain) but experts are not sure exactly how it works to reduce muscle tone and spasms, but suggest it may be due to tizanidine increasing presynaptic inhibition of the nerves that supply the muscles. Tizanidine works more on polysynaptic pathways rather than monosynaptic spinal reflexes. Tizanidine relaxes muscles by dampening down nerve impulses that are sent from spasming muscles along nerve fibers to the brain.
  • Tizanidine belongs to the class of medicines known as central alpha-2-adrenergic agonists. It may also be called a centrally-acting muscle relaxant.

2. Upsides

  • May be used to reduce muscle spasms that are associated with cerebral (brain) or spinal injury.
  • May be used alone or together with other treatments for muscle spasms, such as baclofen.
  • Effective at relaxing muscles (reduces muscle spasms).
  • No direct effects on skeletal muscle fibers.
  • May improve pain associated with muscle spasms.
  • May be used on an as-needed basis.
  • Despite being structurally related to clonidine, tizanidine has only 1/10th to 1/50th of clonidine’s antihypertensive effect which means it is less likely to lower blood pressure than clonidine.
  • Tizanidine is usually started as a dosage of 2mg to 4mg to minimize the risk of side effects; however, dosages less than 8mg have been shown to be ineffective in clinical trials. The dosage should be increased by 2-4mg daily for 2 to 4 weeks until the best effects are seen.
  • No dosage adjustments are needed for liver disease.
  • Generic tizanidine is available.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

  • Low blood pressure, drowsiness, dizziness, energy loss, and a dry mouth.
  • Has been associated with hallucinations and rarely psychosis in approximately 3% of people.
  • The dosage of tizanidine needs to be individualized according to a person’s requirements and response.
  • May not be suitable for people that rely on spasticity to sustain their posture and balance.
  • May cause a drop in blood pressure when going from a sitting or lying down position to standing. This may increase the risk of falls.
  • May affect a person’s ability to drive or operate machinery. Alcohol should be avoided.
  • May cause withdrawal symptoms such as high blood pressure and a fast heartbeat if stopped abruptly after regular extended dosing (decrease dose slowly under a doctor’s advice). Withdraw tizanidine slowly. Decrease by about 2mg to 4mg per day.
  • Seniors may be more susceptible to the side effects of tizanidine.
  • Tizanidine may cause allergic reactions in some people, such as anaphylaxis and urticaria.
  • May interact with several other drugs including those metabolized by hepatic enzymes CYP1A2 (such as fluvoxamine, ciprofloxacin, and some antiarrhythmics), and oral contraceptives. Alcohol increases the peak concentration of tizanidine and also the likelihood of side effects.
  • Liver enzymes (specifically aminotransferase) should be monitored when starting treatment, when clinically indicated, and for at least one month after the maximum dosage is achieved.
  • The different dosage forms of tizanidine (for example, the tablets vs capsules) and modification of the administration of tizanidine (for example swallowing the capsules whole vs opening them up and sprinkling them on applesauce) may cause clinically important differences in effect, such as more side effects or more rapid onset of activity.
  • Needs to be given every 6 to 8 hours. The maximum single dose is 16mg and the maximum total daily dose is 36mg in 24 hours.
  • The safety and effectiveness of tizanidine has not been established for people aged under 18 years.
  • Lower total daily dosages may be necessary with kidney disease. Increase individual dosages if higher dosages are needed rather than increasing dosage frequency.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

Tizanidine relieves muscle spasms but may cause sleepiness, a drop in blood pressure, and sedation. The dosage should be individualized and because it only lasts for a short time in the body, can be taken on an as needed basis. Monitoring of liver enzymes is required.

5.

Tips

  • Capsules may be opened and the contents sprinkled on food.
  • Taking with food increases absorption by 20% but slows the time for effect. Can be taken with or without food, but should be dosed consistently (either with or without food).
  • Tizanidine is relatively short-acting; therefore it should be taken at times when relief of spasticity is the most important (such as before activities of daily living).
  • Take tizanidine exactly as directed. Do not increase the dosage without your doctor’s advice. Tizanidine tablets and capsules are not directly interchangeable; a dosage adjustment may be necessary (talk with your doctor).
  • Be careful when going from sitting or lying down position to standing as tizanidine may increase your risk of falls. Remove any fall hazards (such as loose rugs) from your home.
  • Seek immediate medical advice if you experience any worrying side effects including hallucinations, fainting, sleepiness, or allergic-type reactions.
  • Do not stop taking tizanidine suddenly without your doctor’s advice as high blood pressure and a fast heartbeat may result.
  • Effects are dose-related (the bigger the dose, the stronger the effect, but the more noticeable any side effects are).
  • Tizanidine can make you sleepy. The risk is greater if you also take other drugs, such as benzodiazepines, or sleeping pills. Do not drink any alcohol while taking tizanidine.
  • Do not take any other medication, including medicines brought over-the-counter, in addition to tizanidine, without checking with your doctor or pharmacist to make sure they are compatible.

6. Response and effectiveness

  • The effects of tizanidine peak within 1-2 hours and start to wear off within 3 to 6 hours. Because of this short duration of effect, tizanidine may be dosed on an “as needed” basis during times when muscle spasms are at their most severe.

7. Interactions

Medicines that interact with tizanidine may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with tizanidine. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with tizanidine include:

  • acyclovir
  • amiodarone
  • anti-anxiety medications
  • anticonvulsants
  • antidepressants, such as amitriptyline, imipramine, nortriptyline
  • antihistamines that cause sedation, such as diphenhydramine
  • azelastine
  • chlormethiazole
  • ciprofloxacin
  • dronedarone
  • duloxetine
  • fluvoxamine
  • HIV medications such as saquinavir
  • medications that lower blood pressure, such as ACE inhibitors (eg, enalapril), barbiturates, beta-blockers (such as atenolol), or calcium channel antagonists (such as diltiazem)
  • medicines that inhibit CYP1A2 enzymes such as cimetidine or rifampin
  • metoclopramide
  • opioid analgesics such as oxycodone and morphine
  • other muscle relaxants such as methocarbamol
  • pimozide
  • sleeping pills, such as zolpidem
  • some chemotherapy treatments
  • some medications used to treat mental illness, such as clozapine and thioridazine
  • smoked tobacco
  • treatments for erectile dysfunction, such as sildenafil or tadalafil
  • topiramate
  • zolpidem.

Alcohol may worsen the side effects of tizanidine such as drowsiness and dizziness.

Note that this list is not all-inclusive and includes only common medications that may interact with tizanidine. You should refer to the prescribing information for tizanidine for a complete list of interactions.

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Professional resources

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Related treatment guides

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References

  • Tizanidine. Revised 03/2023. NorthStar Rx LLC. https://www.drugs.com/pro/tizanidine.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use tizanidine only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Copyright 1996-2023 Drugs.com. Revision date: April 4, 2023.

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05/30/2023

Admission Campaign – 2023

On our website in the section Home / Applicants / Applicants (specialist / bachelor / master) there is a video that details the rules for admission to Ryazan State Medical University.

06/13/2023

ALL-RUSSIAN EDUCATIONAL AND LEGAL INTENSIVE FOR STUDENTS IN MEDICINE AND PHARMACY
Ryazan State Medical University is hosting the All-Russian Educational and Legal Intensive for students of medicine and pharmacy, dedicated to the issues of medical education and healthcare, which will be held on June 15-17, 2023 at the address: Ryazan, st. Shevchenko, 34, building 2.

05/25/2023

Intensive courses to prepare for entrance examinations
We invite you, dear applicants, to take intensive courses to prepare for the entrance exams, conducted by the university itself.

06/13/2023

Security in science and education
Vice-Rector for Educational Work and International Affairs Maria Viktorovna Gordova participated in the VIII All-Russian Scientific and Practical Forum “Safety in Science and Education”.

06/13/2023

Competition for a university grant
In the Ryazan State Medical University, the V Intra-university competition for the youth research grant dedicated to the memory of Professor Yu.I. Ukhov has been announced. Students of 1 and 2 courses can take part in the selection

09.06.2023

Awards of all merit
In the Olympiad in Surgical Dentistry and Maxillofacial Surgery, our students showed excellent results and deservedly won not only in the individual, but also in the team competition

06/09/2023

Rector spoke at the regional political council
The rector of the RyazGMU spoke at an enlarged meeting of the regional political council of the United Russia party. Kalinin Roman Evgenievich is the deputy secretary of the regional branch of the party and coordinates the Healthy Future project in the Ryazan region

09.06.2023

RyazGMU student works as a minister
Meet! The Minister of Health of the Ryazan Region is still in the Youth Government, but who knows what will happen in the future?

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Commonwealth of graduates of the Ryazan State Medical University
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Representative therapeutic forum in Ryazan State Medical University
Opening the First Congress of Therapists of the Central Federal District, the rector of the Ryazan State Medical University, MD. Professor Kalinin Roman Evgenievich noted that every event that the university holds within its walls is obligatory and educational too.

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14.02.2023

TELL YOU WHO IS ALREADY AVAILABLE ONLINE TUITION PAYMENT IN RYAZGMU

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Course “PSYCHOLOGICAL METHODS OF WORK WITH THE CONSEQUENCES OF PSYCHOTRAUFUL EVENTS”
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On February 16, a visit to the State Healthcare Institution “Novomoskovsk City Clinical Hospital” took place. On behalf of the Ministry of Health of the Tula region, tests were prepared to assess the knowledge of obstetrician-gynecologists. Head of the Department of Obstetrics and Gynecology of the Ryazan State Medical University Kovalenko M.S. and Dean of the FDPO RyazGMU Maksimtseva E.A. tested 21 specialists of the State Healthcare Institution “NGCH” and conducted a clinical tour of the departments of branch No. 2 of the State Health Institution “NGCH” together with the Deputy Chief Physician for Obstetrics and Gynecology Breus E.V. and department staff.

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Session 11. Antidepressants and antiepileptics

11

Purpose
classes:
form
ideas about the origin
antiepileptic and antidepressant
drug effect. Based on knowledge
their pharmacokinetics and pharmacodynamics,
as well as side effects and contraindications
be able to choose drugs for treatment
epilepsy and depression.

Questions and tasks for self-preparation of students for the lesson:

  1. Classification,
    localization and mechanism of action
    antiepileptic drugs.

  2. Facilities,
    used to treat large and
    focal epileptic seizures
    (phenobarbital, difenin, carbamazepine,
    acediprol, lamotrigine, topiramate,
    oxcarbazepine, levetiracetam, vigabatrin,
    felbamate). Pharmacodynamics and pharmacokinetics
    drugs. Comparative characteristics.
    Other pharmacological properties
    drugs (hypnotics, analgesics,
    muscle relaxant and others). Peculiarities
    applications.

  3. Preparations
    for the treatment of small epileptic
    seizures (ethosuximide, pufemid,
    felbamate, clonazepam, trimetine, acediprol,
    Cavinton). Pharmacodynamics and pharmacokinetics
    Comparative characteristics of funds.
    Indications for use.

  4. Preparations
    for the treatment of myoclonic seizures
    (ethosuximide, pufemide, clonazepam,
    sibazon).

  5. Preparations
    for the treatment of status epilepticus
    (benzodiazepines, phenobarbital, general
    anesthetics).

  6. Comparative
    characteristics of drugs used
    for the treatment of muscle spasticity and
    febrile seizures (tizanidine, dantrolene,
    mydocalm).

  7. Side effects
    effects of major antiepileptic
    funds.

8.
Classification
antidepressants:

I.
Indiscriminate
neuronal blockers
monoamine capture:

imipramine,
amitriptyline, azafen, maprotiline

II.
Electoral
neuronal blockers
serotonin uptake:

milnacipran,
sertraline, fluoxetine

III.
Inhibitors
monoamine oxidase
(MAO)

nialamide,
befol, inkazan, moclobemide, pyrazidol

IV.
Atypical antidepressants: trazodone,
mirtazapine, tianeptine, mianserin

9.
Mechanisms of development of antidepressant
actions of drugs of different groups. Other
pharmacological effects of antidepressants.
Comparative characteristics
antidepressants
according to the scheme:
mechanism
actions, pharmacological effects and
indications for use. Side effects
effects of antidepressants.

Independent work

Compose
tables

on pharmacological and clinical
efficacy and safety of drugs:
phenobarbital, difenin, acediprol,
ethosuximide, clonazepam, imipramine,
amitriptyline, moclobemide, trazodone.

Clinical and pharmacological efficacy of drugs

Group

Pharmacological
effects

Indications
for application

Preparations

Antiepileptics
products

1)
Suppresses
sensory areas of the cerebral cortex,
reduces movement and
cause drowsiness, sedation
and dream.

2) Reduces
excitability of epileptogenic neurons
focus and prevents the occurrence
and propagation of impulses, blocks
high frequency repeated discharges
neurons (due to the influence on the current
sodium ions).

3)B
combination with other drugs – antispasmodic,
vasodilating effect.

1) Insomnia,
excitation.

2) Epilepsy

3) Spasm
peripheral arteries

Phenobarbital

1) Possesses
anticonvulsant activity (no
pronounced sedative and hypnotic
effect).

2) Antiarrhythmic
effect (reduces maximum speed
depolarization, raises the threshold
excitability, slows down conduction
bundle of His and Purkinje fibers).

3) Suppresses
vestibular reflexes.

1) Generalized
and partial seizures. (Epilepsy).

2) Prevention
ventricular arrhythmias after surgery
on the heart, ventricular arrhythmias,
developing during anesthesia,
cardiac catheterization, coronary angiography.

3) Disease
Meniere.

Difenin

1) Reduces
excitability and convulsive readiness
motor areas of the brain.

2) Improves
mental state and mood
sick.

1) Epilepsy.

2) Conditional
epilepsy character changes, disorders
behaviors associated with epilepsy
baby tick.

Acediprol

1) Renders
pronounced anticonvulsant effect
(the effect of the drug is due to
inhibition of the motor centers of the cortex
cerebrum and increased convulsive
threshold. )

2) Analgesic
action.

1) Various
small seizures of the primary
and secondary generalized epilepsy.

2) When
trigeminal neuralgia.

Ethosuximide

1) Possesses
pronounced anticonvulsant
activity.

2) Renders
anxiolytic, tranquilizing,
sleeping pills and central muscle relaxant
actions.

1) Epilepsy.

2) All
forms of status epilepticus, focal
seizures, somnambulism, muscular
hypertonicity, insomnia (especially in
patients with organic lesions
brain), psychomotor
excitation.

Clonazepam

Antidepressants

1) Drug
reduces motor retardation,
improves mood, promotes
normalization of sleep, digestion and other
somatic functions, renders
some stimulating effect on
body tone.

2) Possesses
weak anticholinergic, myotropic
antispasmodic and antihistamine
activity.

1) Depression
and depressive states of various
etiologies accompanied by motor
and ideational retardation.

2) Functional
nocturnal enuresis in children.

Imipramine

1)
Antidepressant with pronounced sedative
effect. Has a central
anticholinergic, antihistamine,
antiserotonin action.

2) Renders
thymoleptic and analgesic
(central genesis) action.

.

1) Depressive
manic-depressive phase
psychosis, depression (including in childhood
age), mixed emotional
disorders and behavioral disorders.

2) Chronic
pain syndromes.

Amitriptyline

1) Possesses
antidepressant action, increases
mood and ability to concentrate
attention, eliminates fatigue, dysphoria,
nervous exhaustion, psychomotor
lethargy, improves sleep.

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