同: Gabitril

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/03/13 00:16:19」(JST)

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Tiagabine (brand name Gabitril) is an anticonvulsive medication. The medication is also used in the treatment of panic disorder, as are a few other anticonvulsants.^{[citation needed]} It is produced by Cephalon

Medical uses

Tiagabine is approved by U.S. Food and Drug Administration (FDA) as an adjunctive treatment for partial seizures in ages 12 and up. It may also be prescribed off-label by physicians to treat anxiety disorders and neuropathic pain (including fibromyalgia). For anxiety and neuropathic pain, tiagabine is used primarily to augment other treatments. Tiagabine may be used alongside SSRIs, SNRIs, or benzodiazepines for anxiety, or antidepressants, gabapentin, anticonvulsants or opiates for neuropathic pain.^[1]

Side effects

Tiagabine's most common side effects include confusion, difficulty speaking clearly/stuttering, mild sedation, and in doses over 8 mg, a tingling sensation (paresthesia) in the body's extremities, particularly the hands and fingers. Tiagabine may induce seizures in those without epilepsy, especially if they are taking another drug which lowers the seizure threshold.^[1]

Tiagabine overdose can produce neurologic symptoms such as lethargy, seizures (multiple), status epilepticus, seizure (single), coma, confusion, agitation, tremors, dizziness, dystonias/abnormal posturing, and hallucinations. Other symptoms of tiagabine overdose include respiratory depression, tachycardia, hypertension, and hypotension. Overdose may be fatal especially if the victim presents with severe respiratory depression and/or fails to respond to verbal and physical stimuli. Emergency medical services should be sought immediately for any overdose.^{[citation needed]}

Pharmacology

Tiagabine increases the level of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system by blocking the GABA transporter and hence is classified as a GABA reuptake inhibitor.^[2]

History

The drug was discovered at Novo Nordisk in Denmark in 1988 by a team of medicinal chemists and pharmacologists under the general direction of Claus Bræstrup.^[3] The drug was co-developed with Abbott Laboratories, in a 40/60 cost sharing deal, with Abbott paying a premium for licensing the IP from the Danish company.^{[citation needed]}

Abbott did initially embrace the drug enthusiastically after its US launch in 1998, and provided further clinical studies with the goal of gaining FDA approval for monotherapy in epilepsy. However, the senior management at Abbott drew back after realizing that the original deal with Novo would limit the company's financial gain from a monotherapy approval. After a period of co-promotion, Cephalon licensed tiagabine from Abbott/Novo and now is the exclusive producer.^{[citation needed]}

References

^ ^a ^b Stahl, S. Stahl's Essential Psychopharmacology: Prescriber's Guide. Cambridge University Press: New York, NY. 2009. pp. 523-526
^ Pollack MH, Roy-Byrne PP, Van Ameringen M, Snyder H, Brown C, Ondrasik J, Rickels K (November 2005). "The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study". The Journal of Clinical Psychiatry 66 (11): 1401–8. doi:10.4088/JCP.v66n1109. PMID 16420077.
^ Andersen KE, Braestrup C, Grønwald FC, Jørgensen AS, Nielsen EB, Sonnewald U, Sørensen PO, Suzdak PD, Knutsen LJ (1993). "The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate". J. Med. Chem. 36 (12): 1716–25. doi:10.1021/jm00064a005. PMID 8510100.

External links

Gabitril (manufacturer's website)
Pharmacology

UpToDate Contents

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1. 抗てんかん剤：作用機序、薬理学、および有害事象 antiepileptic drugs mechanism of action pharmacology and adverse effects
2. Pharmacotherapy for posttraumatic stress disorder in adults
3. 成人におけるてんかんの初期治療 initial treatment of epilepsy in adults
4. パニック障害の薬物療法 pharmacotherapy for panic disorder
5. 成人におけるコカイン関連疾患の治療 treatment of cocaine use disorder in adults

English Journal

Do antiepileptic drugs increase the risk of infectious diseases? A meta-analysis of placebo-controlled studies.

Zaccara G1, Giovannelli F1,2, Giorgi FS3, Franco V4, Gasparini S5, Tacconi FM6.
British journal of clinical pharmacology.Br J Clin Pharmacol.2017 Sep;83(9):1873-1879. doi: 10.1111/bcp.13296. Epub 2017 May 7.
PMID 28370224

Neurophysiologically-informed markers of individual variability and pharmacological manipulation of human cortical gamma.

Shaw AD1, Moran RJ2, Muthukumaraswamy SD3, Brealy J1, Linden DE4, Friston KJ5, Singh KD6.
NeuroImage.Neuroimage.2017 Aug 11. pii: S1053-8119(17)30681-X. doi: 10.1016/j.neuroimage.2017.08.034. [Epub ahead of print]
PMID 28807873

Management of epilepsy in MERRF syndrome.

Finsterer J1, Zarrouk-Mahjoub S2.
Seizure.Seizure.2017 Aug;50:166-170. doi: 10.1016/j.seizure.2017.06.010. Epub 2017 Jun 24.
PMID 28686997

Japanese Journal

Impact of P-glycoprotein and breast cancer resistance protein on the brain distribution of antiepileptic drugs in knockout mouse models.

Nakanishi Haruka,Yonezawa Atsushi,Matsubara Kazuo,Yano Ikuko
European journal of pharmacology 710(1-3), 20-28, 2013-06-15
… In contrast, the plasma concentration profiles of phenytoin, lamotrigine, topiramate, tiagabine, and levetiracetam in the Mdr1a/1b(-/-)/Bcrp(-/-) mice were significantly lower than the corresponding ones in the wild-type mice. … The brain-to-plasma concentration ratio (Kpbrain) values of phenytoin, topiramate, and tiagabine in the Mdr1a/1b(-/-) mice were significantly higher than the corresponding ones in the wild-type mice. …
NAID 120005289852

Comparison of the Cognitive Effects of Tiagabine and Carbamazepine as Monotherapy in Newly Diagnosed Adult Patients with Partial Epilepsy : Pooled Analysis of Two Long-term, Randomized, Follow-up Studies

AIKIA Marja,JUTILA Leena,SALMENPERA Tuuli,MERVAALA Esa,KALVIAINEN Reetta
Epilepsia : journal of the International League against Epilepsy 47(7), 1121-1127, 2006-07-01
NAID 10019308152

Transient Athetosis Induced by Tiagabine

TOMBINI Mario,PACIFICI Loredana,PASSARELLI Francesco,ROSSINI Paolo M.
Epilepsia : journal of the International League against Epilepsy 47(4), 799-800, 2006-04-01
NAID 10019309389

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「チアガビン」

Tiagabine
Systematic (IUPAC) name
	(R)-1-[4,4-Bis(3-methylthiophen-2-yl)but-3-enyl] piperidine-3-carboxylic acid
Clinical data
Pronunciation	/taɪˈæɡəbiːn/
Trade names	Gabitril
AHFS/Drugs.com	monograph
MedlinePlus	a698014
Pregnancy; category	AU: B3; US: C (Risk not ruled out); ;
Routes of; administration	Oral
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	90%
Protein binding	96%
Metabolism	Hepatic (CYP450 system)
Biological half-life	7-9 hours
Excretion	Fecal and renal
Identifiers
CAS Number	115103-54-3
ATC code	N03AG06 (WHO)
PubChem	CID 60648
IUPHAR/BPS	4685
DrugBank	DB00906
ChemSpider	54661
UNII	Z80I64HMNP
KEGG	D08588
ChEBI	CHEBI:9586
ChEMBL	CHEMBL1027
Chemical data
Formula	C20H25NO2S2
Molar mass	375.55 g/mol
	SMILES O=C(O)[C@H]1CN(CCC1)CC/C=C(/c2sccc2C)c3sccc3C ;
	InChI InChI=1S/C20H25NO2S2/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23)/t16-/m1/s1 ; Key:PBJUNZJWGZTSKL-MRXNPFEDSA-N ;
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