Tizanidine

What is Tizanidine

Tizanidine is an oral agent used to reduce muscle tone associated with spasticity related to cerebral or spinal cord injury, multiple sclerosis, or other spastic disorders.

The imidazoline chemical structure of tizanidine is related to that of clonidine and other central-acting alpha2-adrenergic agonists.

Tizanidine significantly reduces muscle tone and frequency of spasms in patients with spasticity due to spinal cord injury; but does not reduce muscle strength.

Both tizanidine and baclofen (see separate monograph) inhibit spinal interneuron firing, however, tizanidine’s effects are mediated by alpha2-receptors whereas baclofen acts directly on neuronal membrane polarization.

The efficacy of tizanidine in the treatment of spasticity is comparable to baclofen.

Tizanidine produces more drowsiness and sedation than baclofen, but tizanidine is not associated with the muscle weakness which may occur with baclofen therapy.

Tizanidine was approved by the FDA on December 3, 1996.

Brand Name

Zanaflex

Indications

  1. multiple sclerosis
  2. spasticity
  3. spinal cord injury

For the acute and intermittent management of increased muscle tone associated with spasticity (including spasticity related to multiple sclerosis or spinal cord injury)

Side Effects

  1. anaphylactoid reactions
  2. anemia
  3. angioedema
  4. arthralgia
  5. asthenia
  6. blurred vision
  7. bradycardia
  8. constipation
  9. cystitis
  10. depression
  11. dizziness
  12. drowsiness
  13. dyskinesia
  14. elevated hepatic enzymes
  15. excitability
  16. exfoliative dermatitis
  17. fatigue
  18. hallucinations
  19. hepatic failure
  20. hepatic necrosis
  21. hepatitis
  22. hypercholesterolemia
  23. hyperlipidemia
  24. hypotension
  25. increased urinary frequency
  26. infection
  27. influenza
  28. jaundice
  29. leukocytosis
  30. leukopenia
  31. paresthesias
  32. pharyngitis
  33. QT prolongation
  34. rash
  35. rhinitis
  36. Stevens-Johnson syndrome
  37. syncope
  38. thrombocytopenia
  39. tremor
  40. vomiting
  41. weakness
  42. withdrawal
  43. xerostomia

Monitoring Parameters

  • LFTs

Contraindications

  • abrupt discontinuation
  • breast-feeding
  • driving or operating machinery
  • geriatric
  • hepatic disease
  • hypotension
  • labor
  • obstetric delivery
  • pregnancy
  • psychosis
  • renal failure
  • renal impairment

Interactions

  • Acebutolol
  • Acetaminophen
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Dichloralphenazone; Isometheptene
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Guaifenesin; Phenylephrine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Pentazocine
  • Acetaminophen; Propoxyphene
  • Acetaminophen; Pseudoephedrine
  • Acetaminophen; Tramadol
  • Acrivastine; Pseudoephedrine
  • Acyclovir
  • Alfentanil
  • Aliskiren
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Aliskiren; Valsartan
  • Alprazolam
  • Ambrisentan
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amitriptyline; Chlordiazepoxide
  • Amobarbital
  • Anagrelide
  • Angiotensin II receptor antagonists
  • Angiotensin-converting enzyme inhibitors
  • Anxiolytics; Sedatives; and Hypnotics
  • Aripiprazole
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atenolol
  • Atenolol; Chlorthalidone
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azelastine
  • Azelastine; Fluticasone
  • Bacitracin
  • Baclofen
  • Barbiturates
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Belladonna; Opium
  • Bendroflumethiazide; Nadolol
  • Benzhydrocodone; Acetaminophen
  • Benzodiazepines
  • Beta-adrenergic blockers
  • Betaxolol
  • Bisoprolol
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Brimonidine; Timolol
  • Brompheniramine
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Buspirone
  • Butabarbital
  • Butorphanol
  • Canakinumab
  • Cannabidiol
  • Capmatinib
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Guaifenesin
  • Carbetapentane; Guaifenesin; Phenylephrine
  • Carbetapentane; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pseudoephedrine
  • Carbetapentane; Pyrilamine
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Carteolol
  • Carvedilol
  • Cenobamate
  • Central-acting adrenergic agents
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chlorcyclizine
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chlorpheniramine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Cimetidine
  • Ciprofloxacin
  • Clemastine
  • Clonazepam
  • Clorazepate
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • COMT inhibitors
  • Cyclizine
  • Cyproheptadine
  • Deutetrabenazine
  • Dexchlorpheniramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmedetomidine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Diazepam
  • Dienogest; Estradiol valerate
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Dimenhydrinate
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Dorzolamide; Timolol
  • Doxazosin
  • Doxylamine
  • Doxylamine; Pyridoxine
  • Dronabinol
  • Drospirenone
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Elagolix; Estradiol; Norethindrone acetate
  • Emapalumab
  • Entacapone
  • Eplerenone
  • Epoprostenol
  • Esketamine
  • Esmolol
  • Estazolam
  • Estradiol; Levonorgestrel
  • Estradiol; Norethindrone
  • Estradiol; Norgestimate
  • Ethanol
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Famotidine
  • Famotidine; Ibuprofen
  • Fentanyl
  • Fluphenazine
  • Flurazepam
  • Fluvoxamine
  • Fosphenytoin
  • Gabapentin
  • Givosiran
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Homatropine; Hydrocodone
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxyprogesterone
  • Hydroxyzine
  • Ibuprofen; Oxycodone
  • Iloprost
  • Indapamide
  • Labetalol
  • Lasmiditan
  • Leflunomide
  • Lemborexant
  • Leuprolide; Norethindrone
  • Levobetaxolol
  • Levobunolol
  • Levonorgestrel
  • Levorphanol
  • Lofexidine
  • Loop diuretics
  • Lorazepam
  • Loxapine
  • Lumateperone
  • Lurasidone
  • Mecamylamine
  • Meclizine
  • Mepenzolate
  • Meperidine
  • Meperidine; Promethazine
  • Mephobarbital
  • Mestranol; Norethindrone
  • Methadone
  • Methohexital
  • Methscopolamine
  • Metoprolol
  • Mexiletine
  • Midazolam
  • Molindone
  • Morphine
  • Morphine; Naltrexone
  • Nabilone
  • Nadolol
  • Nalbuphine
  • Nebivolol
  • Nebivolol; Valsartan
  • Norethindrone
  • Norgestrel
  • Obeticholic Acid
  • Oral Contraceptives
  • Osilodrostat
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Peginterferon Alfa-2b
  • Penbutolol
  • Pentazocine
  • Pentazocine; Naloxone
  • Pentobarbital
  • Phenobarbital
  • Phenoxybenzamine
  • Phentolamine
  • Phenytoin
  • Pindolol
  • Potassium-sparing diuretics
  • Prazosin
  • Pregabalin
  • Primidone
  • Propafenone
  • Propranolol
  • Quazepam
  • Ramelteon
  • Remifentanil
  • Reserpine
  • Rucaparib
  • Sarilumab
  • Secobarbital
  • Segesterone Acetate; Ethinyl Estradiol
  • Siltuximab
  • Simeprevir
  • Spironolactone
  • Sufentanil
  • Tacrine
  • Tapentadol
  • Temazepam
  • Terazosin
  • Teriflunomide
  • Thalidomide
  • Thiabendazole
  • Thiazide diuretics
  • Thiopental
  • Thiothixene
  • Ticlopidine
  • Timolol
  • Tocilizumab
  • Tolcapone
  • Tramadol
  • Trandolapril; Verapamil
  • Treprostinil
  • Triamterene
  • Triazolam
  • Triprolidine
  • Valerian, Valeriana officinalis
  • Vasodilators
  • Vemurafenib
  • Verapamil
  • Zileuton
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