塩酸チザニジン

関: tizanidine

WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/12/07 11:59:57」(JST)

wiki en

Tizanidine (trade names Zanaflex, Sirdalud) is a drug that is used as a muscle relaxant. It is a centrally acting α₂ adrenergic agonist. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, ALS, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label for migraine headaches, as a sleep aid, and as an anticonvulsant. It is also prescribed for some symptoms of fibromyalgia.^[1]

Tizanidine has been found to be as effective as other antispasmodic drugs and has superior tolerability to that of baclofen and diazepam.^[2] Tizanidine can be very strong even at the 2 mg dose and may cause hypotension, so caution is advised when it is used in patients who have a history of orthostatic hypotension, or when switching from gel cap to tablet form and vice versa.

Tizanidine can occasionally cause liver damage, generally the hepatocellular type. Clinical trials show that up to 5% of patients treated with tizanidine had elevated liver function test values, though symptoms disappeared upon withdrawal of the drug. Care should be used when first beginning treatment with tizanidine with regular liver tests for the first 6 months of treatment.

Availability[edit]

Tizanidine is supplied as 2 and 4 mg tablets for oral administration, and in gel cap form in doses of 2 mg, 4 mg, and 6 mg.

The tablets are composed of the active ingredient, tizanidine hydrochloride (2.288 mg equivalent to 2 mg tizanidine base and 4.576 mg equivalent to 4 mg tizanidine base), and the inactive ingredients, silicon dioxide colloidal, stearic acid, microcrystalline cellulose and anhydrous lactose.

Interactions[edit]

Concomitant use of tizanidine and moderate or potent CYP1A2 inhibitors is contraindicated. Concomitant use of tizanidine with fluvoxamine, a potent CYP1A2 inhibitor in man, resulted in a 33-fold increase in the tizanidine AUC (plasma drug concentration-time curve).^{[citation needed]} Tizanidine is a potent sedative.^{[citation needed]} It therefore has the potential to interact with other CNS depressants. Alcohol should be avoided, particularly as it can upset the stomach.

It has a Volume of Distribution of 2.6L (Manufacturers notes).

Side effects[edit]

Side effects include dizziness, drowsiness, weakness, nervousness, depression, vomiting, tingling sensation in the arms, legs, hands, and feet, dry mouth, constipation, diarrhea, stomach pain, heartburn, increased muscle spasms, back pain, rash and sweating.^[3]

References[edit]

^ Zanaflex for Fibromyalgia
^ Kamen, L.; Henney, HR.; Runyan, JD. (Feb 2008). "A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury.". Curr Med Res Opin 24 (2): 425–39. doi:10.1185/030079908X261113. PMID 18167175.
^ Tizanidine - PubMed Health

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 成人における緊張型頭痛：予防的治療 tension type headache in adults preventive treatment
2. 薬物乱用頭痛：治療および予後 medication overuse headache treatment and prognosis
3. クロニジンおよびイミダゾリンによる中毒 clonidine and related imidazoline poisoning
4. 成人における多発性硬化症の症状のマネージメント symptom management of multiple sclerosis in adults
5. 急性腰痛の治療 treatment of acute low back pain

English Journal

Pharmacological management of spasticity in multiple sclerosis: Systematic review and consensus paper.

Otero-Romero S1, Sastre-Garriga J2, Comi G3, Hartung HP4, Soelberg Sørensen P5, Thompson AJ6, Vermersch P7, Gold R8, Montalban X2.
Multiple sclerosis (Houndmills, Basingstoke, England).Mult Scler.2016 Oct;22(11):1386-1396. Epub 2016 May 19.
BACKGROUND AND OBJECTIVES: Treatment of spasticity poses a major challenge given the complex clinical presentation and variable efficacy and safety profiles of available drugs. We present a systematic review of the pharmacological treatment of spasticity in multiple sclerosis (MS) patients.METHODS:
PMID 27207462

Clinical efficacy and safety of eperisone for low back pain: A systematic literature review.

Bavage S1, Durg S2, Ali Kareem S3, Dhadde SB4.
Pharmacological reports : PR.Pharmacol Rep.2016 Oct;68(5):903-12. doi: 10.1016/j.pharep.2016.05.003. Epub 2016 Jun 29.
Eperisone, an analgesic and centrally acting muscle relaxant has been in use for the treatment of low back pain (LBP). The present systematic review evaluates the efficacy and safety of eperisone in patients with LBP. Cochrane Back and Neck (CBN) Group and Preferred Reporting Items for Systematic re
PMID 27371896

Poster 257 Tizanidine Reduces Night Sweats due to Dysautonomia in Syringomyelia: A Case Report.

Menard RA1, Moon D, Hurd P.
PM & R : the journal of injury, function, and rehabilitation.PM R.2016 Sep;8(9S):S243-S244. doi: 10.1016/j.pmrj.2016.07.430. Epub 2016 Sep 24.
PMID 27673012

Japanese Journal

筋緊張緩和剤と選択的セロトニン再取り込み阻害剤の併用による血圧低下に関する検討

坂野昌志,間瀬広樹,島田泉,山本初実,小林智晴,小山誠一,林誠,宮川慶子,伊藤由紀
医療薬学 31(6), 470-474, 2005-06-10
… The influence on blood pressure of the combined use of tizanidine hydrochloride and fluvoxamine maleate was investigated in the Mie Chuo Medical Center. …
NAID 110001258517

Decrease in Blood-Pressure due to Combined Use of Muscle Relaxants and Selective Serotonin Reuptake Inhibitors (SSRIs)

坂野昌志,間瀬広樹,島田泉,山本初実,小林智晴,小山誠一,林誠,宮川慶子,伊藤由紀
医療薬学 31(6), 470-474, 2005
… The influence on blood pressure of the combined use of tizanidine hydrochloride and fluvoxamine maleate was investigated in the Mie Chuo Medical Center. …
NAID 130004346702

耳鳴の薬物療法-テルネリン単独とヒデルギン併用

北奥恵之,松永喬,北村溥之,安里亮,金子賢一,太田和博,上田和孝,柏木令子,横田雅子,衛藤幸男,秋岡勝哉,山中泰輝,岡亮,畠史子,岡坂利章,岡本英之,鶴田至宏,金田宏和
耳鼻咽喉科臨床 88(5), 645-656, 1995-05-01
… Patients with tinnitus were treated with Ternelin® (tizanidine hydrochloride) alone or in combination with Hydergine® (dihydroergotoxine mesylate). …
NAID 10005603900

「チザニジン」

Tizanidine
Systematic (IUPAC) name
	5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)benzo[c][1,2,5]thiadiazol-4-amine
Clinical data
Trade names	Zanaflex
AHFS/Drugs.com	monograph
MedlinePlus	a601121
Pregnancy cat.	?
Legal status	℞-only (US)
Routes	Oral, Intranasal, Injection
Pharmacokinetic data
Protein binding	30%
Metabolism	CYP 1A2
Half-life	2.54 hours
Identifiers
CAS number	51322-75-9
ATC code	M03BX02
PubChem	CID 5487
DrugBank	DB00697
ChemSpider	5287
UNII	6AI06C00GW
KEGG	D08611
ChEMBL	CHEMBL1079
Synonyms	4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-8-thia-7,9-diazabicyclo[4.3.0]nona-2,4,6,9-tetraen-5-amine
Chemical data
Formula	C9H8ClN5S
Mol. mass	253.712 g/mol
	SMILES Clc1ccc3nsnc3c1NC/2=N/CCN\2;
	InChI InChI=1S/C9H8ClN5S/c10-5-1-2-6-8(15-16-14-6)7(5)13-9-11-3-4-12-9/h1-2H,3-4H2,(H2,11,12,13) ; Key:XFYDIVBRZNQMJC-UHFFFAOYSA-N ;
(what is this?) (verify);

　　[★]

英: tizanidine
化: 塩酸チザニジン tizanidine hydrochloride
商: エンチニン、ギボンズ、セブレチン、チザニジン、チザニン、チザネリン、チロルビット、テトリネン、テルザニン、テルネリン、メキタック、モトナリン、ザンピーク、テルリラーク

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[1] Zanaflex for Fibromyalgia

[Kamen-2008-2] Kamen, L.; Henney, HR.; Runyan, JD. (Feb 2008). "A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury.". Curr Med Res Opin 24 (2): 425–39. doi:10.1185/030079908X261113. PMID 18167175.

[3] Tizanidine - PubMed Health

匿名

検索

案内

案内

tizanidine hydrochloride