Peringatan Keamanan

LD50 information

Oral LD50 (rat): 414 mg/kg; Subcutaneous LD50 (rat): 282 mg/kg; Oral LD50 (mouse): 235 mg/kg MSDS

Use in pregnancy

Animal studies have determined that this drug causes fetal harm FDA label. Studies have not been performed in humans, and it is advisable to ensure that tizanidine use in pregnant women should be reserved for cases in which possible benefit clearly outweighs the possible risk to mother and unborn child F4471.

Use in breastfeeding

In studies of rat models, this tizanidine was found excreted in the breastmilk with a milk-to-blood ratio of 1.8:1 FDA label. In young nursing rats, abnormal results were obtained in tests indicative of central nervous system function. Various developmental changes that may have been attributable to the drug were observed. It is unknown whether tizanidine is excreted in human milk. It is a lipid-soluble drug, however, and likely to be excreted into breast milk F4471.

Carcinogenesis and mutagenesis

No signs of carcinogenicity were observed in two dietary studies performed in rodent models. Tizanidine was given to mice for 78 weeks at doses reaching a maximum 16 mg/kg (equivalent to twice the maximum recommended human dose). In addition, the drug was given to rats for 104 weeks at doses reaching 9 mg/kg (equivalent to 2.5 times the maximum recommended human dose). There was a lack of a statistically significant increase in the occurrence of tumors in either study group F4471.

Tizanidine was not found to be mutagenic or clastogenic in several laboratory essays, including the bacterial Ames test, the mammalian gene mutation test, in addition to the chromosomal aberration test in Chinese hamster cells and several other assays F4471.

Tizanidine

DB00697

small molecule approved investigational

Deskripsi

Tizanidine is a fast-acting drug used for the management of muscle spasm, which may result from the effects of multiple sclerosis, stroke, an acquired brain injury, or a spinal cord injury T574. It may also be caused by musculoskeletal injury A177583. Regardless of the cause, muscle spasticity can be an extremely painful and debilitating condition.

Initially approved by the FDA in 1996, tizanidine is an Alpha-2 adrenergic receptor agonist reducing spasticity by the presynaptic inhibition of excitatory neurotransmitters that cause firing of neurons promoting muscle spasm FDA label.

Struktur Molekul 2D

Berat 253.711
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 2.5 hours [FDA label].
Volume Distribusi Extensively distributed throughout the body. The average steady-state volume of distribution is 2.4 L/kg [FDA label].
Klirens (Clearance) **A note on renal impairment** Tizanidine clearance is found to be decreased by more than 50% in elderly patients with renal insufficiency (creatinine clearance < 25 mL/min) compared to healthy elderly subjects; this would be expected to lead to a longer duration of clinical effect. This drug should be used with caution in patients with renal impairment [FDA label].

Absorpsi

This drug undergoes significant first-pass metabolism. After the administration of an oral dose, tizanidine is mostly absorbed. The absolute oral bioavailability of tizanidine is measured to be about 40% FDA label. Effect of food on absorption Food has been shown to increase absorption for both the tablets and capsules. The increase in absorption with the tablet (about 30%) was noticeably higher than the capsule (~10%). When the capsule and tablet were administered with food, the amount absorbed from the capsule was about 80% of the amount absorbed from the tablet FDA label. It is therefore advisable to take this drug with food for increased absorption, especially in tablet form.

Metabolisme

About 95% of the ingested dose of tizanidine is metabolized. The main enzyme involved in the hepatic metabolism of tizanidine is CYP1A2 FDA label.

Rute Eliminasi

This drug is mainly eliminated by the kidney FDA label.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Maintain the same schedule with regard to meals, as concentrations increase in the fasted state and decrease in the fed state.

Interaksi Obat

1586 Data
Citalopram The serum concentration of Tizanidine can be increased when it is combined with Citalopram.
Anagrelide The serum concentration of Tizanidine can be increased when it is combined with Anagrelide.
Conjugated estrogens The serum concentration of Tizanidine can be increased when it is combined with Conjugated estrogens.
Cimetidine The serum concentration of Tizanidine can be increased when it is combined with Cimetidine.
Trovafloxacin The serum concentration of Tizanidine can be increased when it is combined with Trovafloxacin.
Tocainide The serum concentration of Tizanidine can be increased when it is combined with Tocainide.
Genistein The serum concentration of Tizanidine can be increased when it is combined with Genistein.
Viloxazine The serum concentration of Tizanidine can be increased when it is combined with Viloxazine.
Rucaparib The serum concentration of Tizanidine can be increased when it is combined with Rucaparib.
Pipemidic acid The serum concentration of Tizanidine can be increased when it is combined with Pipemidic acid.
Famotidine The serum concentration of Tizanidine can be increased when it is combined with Famotidine.
Estradiol The serum concentration of Tizanidine can be increased when it is combined with Estradiol.
Estradiol acetate The serum concentration of Tizanidine can be increased when it is combined with Estradiol acetate.
Estradiol benzoate The serum concentration of Tizanidine can be increased when it is combined with Estradiol benzoate.
Estradiol valerate The serum concentration of Tizanidine can be increased when it is combined with Estradiol valerate.
Nevirapine The serum concentration of Tizanidine can be increased when it is combined with Nevirapine.
Estradiol dienanthate The serum concentration of Tizanidine can be increased when it is combined with Estradiol dienanthate.
Ethambutol The serum concentration of Tizanidine can be increased when it is combined with Ethambutol.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Tizanidine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Tizanidine is combined with Levodopa.
Risperidone Tizanidine may increase the hypotensive activities of Risperidone.
Ceritinib Tizanidine may increase the bradycardic activities of Ceritinib.
Ivabradine Tizanidine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Tizanidine.
Deferasirox The serum concentration of Tizanidine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Tizanidine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Tizanidine can be decreased when it is combined with Teriflunomide.
Ramipril The risk or severity of hypotension can be increased when Tizanidine is combined with Ramipril.
Fosinopril The risk or severity of hypotension can be increased when Tizanidine is combined with Fosinopril.
Trandolapril The risk or severity of hypotension can be increased when Tizanidine is combined with Trandolapril.
Benazepril The risk or severity of hypotension can be increased when Tizanidine is combined with Benazepril.
Enalapril The risk or severity of hypotension can be increased when Tizanidine is combined with Enalapril.
Moexipril The risk or severity of hypotension can be increased when Tizanidine is combined with Moexipril.
Perindopril The risk or severity of hypotension can be increased when Tizanidine is combined with Perindopril.
Quinapril The risk or severity of hypotension can be increased when Tizanidine is combined with Quinapril.
Omapatrilat The risk or severity of hypotension can be increased when Tizanidine is combined with Omapatrilat.
Rescinnamine The risk or severity of hypotension can be increased when Tizanidine is combined with Rescinnamine.
Captopril The risk or severity of hypotension can be increased when Tizanidine is combined with Captopril.
Cilazapril The risk or severity of hypotension can be increased when Tizanidine is combined with Cilazapril.
Spirapril The risk or severity of hypotension can be increased when Tizanidine is combined with Spirapril.
Temocapril The risk or severity of hypotension can be increased when Tizanidine is combined with Temocapril.
Enalaprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Enalaprilat.
Imidapril The risk or severity of hypotension can be increased when Tizanidine is combined with Imidapril.
Zofenopril The risk or severity of hypotension can be increased when Tizanidine is combined with Zofenopril.
Delapril The risk or severity of hypotension can be increased when Tizanidine is combined with Delapril.
Benazeprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Benazeprilat.
Fosinoprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Fosinoprilat.
Ramiprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Ramiprilat.
Trandolaprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Trandolaprilat.
Moexiprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Moexiprilat.
Perindoprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Perindoprilat.
Quinaprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Quinaprilat.
Cilazaprilat The risk or severity of hypotension can be increased when Tizanidine is combined with Cilazaprilat.
Buprenorphine Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Hydrocodone Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Tizanidine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Tizanidine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Mirtazapine Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Orphenadrine Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Pramipexole Tizanidine may increase the sedative activities of Pramipexole.
Ropinirole Tizanidine may increase the sedative activities of Ropinirole.
Rotigotine Tizanidine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Tizanidine.
Sodium oxybate Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.
Thalidomide Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Tizanidine can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Tizanidine can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Tizanidine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Tizanidine may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Tizanidine.
Benzylpenicilloyl polylysine Tizanidine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Spironolactone The therapeutic efficacy of Tizanidine can be decreased when used in combination with Spironolactone.
Lisinopril Tizanidine may increase the hypotensive activities of Lisinopril.
Caffeine The serum concentration of Tizanidine can be increased when it is combined with Caffeine.
Moxifloxacin The serum concentration of Tizanidine can be increased when it is combined with Moxifloxacin.
Lidocaine The serum concentration of Tizanidine can be increased when it is combined with Lidocaine.
Imipramine The serum concentration of Tizanidine can be increased when it is combined with Imipramine.
Alosetron The serum concentration of Tizanidine can be increased when it is combined with Alosetron.
Ketoconazole The serum concentration of Tizanidine can be increased when it is combined with Ketoconazole.
Gatifloxacin The serum concentration of Tizanidine can be increased when it is combined with Gatifloxacin.
Simeprevir The serum concentration of Tizanidine can be increased when it is combined with Simeprevir.
Vemurafenib The serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.
Dosulepin The risk or severity of hypertension can be increased when Dosulepin is combined with Tizanidine.
Lobeglitazone The serum concentration of Tizanidine can be increased when it is combined with Lobeglitazone.
Pazufloxacin The serum concentration of Tizanidine can be increased when it is combined with Pazufloxacin.
Osilodrostat The serum concentration of Tizanidine can be increased when it is combined with Osilodrostat.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Tizanidine.
Nicorandil Nicorandil may increase the hypotensive activities of Tizanidine.

Target Protein

Alpha-1 adrenergic receptors ADRA1A
Alpha-2 adrenergic receptors ADRA2A
Nischarin NISCH

Referensi & Sumber

Synthesis reference: Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny, "METHOD FOR THE PREPARATION OF TIZANIDINE HYDROCHLORIDE." U.S. Patent US20110263863, issued October 27, 2011.
Artikel (PubMed)
  • PMID: 18199279
    Henney HR 3rd, Runyan JD: A clinically relevant review of tizanidine hydrochloride dose relationships to pharmacokinetics, drug safety and effectiveness in healthy subjects and patients. Int J Clin Pract. 2008 Feb;62(2):314-24. doi: 10.1111/j.1742-1241.2007.01660.x.
  • PMID: 18671474
    Malanga G, Reiter RD, Garay E: Update on tizanidine for muscle spasticity and emerging indications. Expert Opin Pharmacother. 2008 Aug;9(12):2209-15. doi: 10.1517/14656566.9.12.2209 .
  • PMID: 9074844
    Wagstaff AJ, Bryson HM: Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders. Drugs. 1997 Mar;53(3):435-52. doi: 10.2165/00003495-199753030-00007.
  • PMID: 2600869
    Mathias CJ, Luckitt J, Desai P, Baker H, el Masri W, Frankel HL: Pharmacodynamics and pharmacokinetics of the oral antispastic agent tizanidine in patients with spinal cord injury. J Rehabil Res Dev. 1989 Fall;26(4):9-16.
  • PMID: 19629211
    Mense S: Muscle pain: mechanisms and clinical significance. Dtsch Arztebl Int. 2008 Mar;105(12):214-9. doi: 10.3238/artzebl.2008.0214. Epub 2008 Mar 21.
  • PMID: 7572012
    Taittonen M, Raty H, Kirvela O, Aantaa R, Kanto J: The metabolic effects of oral tizanidine in healthy volunteers. Acta Anaesthesiol Scand. 1995 Jul;39(5):628-32.
  • PMID: 25750484
    Chang E, Ghosh N, Yanni D, Lee S, Alexandru D, Mozaffar T: A Review of Spasticity Treatments: Pharmacological and Interventional Approaches. Crit Rev Phys Rehabil Med. 2013;25(1-2):11-22. doi: 10.1615/CritRevPhysRehabilMed.2013007945.
  • PMID: 29467587
    Suarez-Lledo A, Padulles A, Lozano T, Cobo-Sacristan S, Colls M, Jodar R: Management of Tizanidine Withdrawal Syndrome: A Case Report. Clin Med Insights Case Rep. 2018 Feb 13;11:1179547618758022. doi: 10.1177/1179547618758022. eCollection 2018.
Textbook
  • Shirin Ghanavatian; Armen Derian (2019). Tizanidine. StatPearls.

Contoh Produk & Brand

Produk: 343 • International brands: 18
Produk
  • Apo-tizanidine
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Apo-tizanidine
    Tablet • 4 mg • Oral • Canada • Generic • Approved
  • Comfort Pac with Tizanidine
    Kit; Tablet • 4 mg/1 • Oral • US • Generic • Approved
  • Mint-tizanidine
    Tablet • 4 mg • Oral • Canada • Generic • Approved
  • Mylan-tizanidine
    Tablet • 4 mg • Oral • Canada • Generic • Approved
  • Pal-tizanidine
    Tablet • 4 mg • Oral • Canada • Generic • Approved
  • Tizandine
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Tizanidine
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 343 produk.
International Brands
  • Cimbrar — Euroetika
  • Musant — Actavis
  • Myores — Meprofarm
  • Navizan — Caber
  • Relaxkov — Blaskov
  • Sirdalid — Novartis
  • Sirdalud — Novartis
  • Sirdalud MR — Novartis
  • Sizolan — Dr. Reddy's
  • Spaslax — Panion & BF

Sekuens Gen/Protein (FASTA)

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