sultiame

スルチアム

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/09/23 22:05:44」(JST)

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Sultiame

Systematic (IUPAC) name
4-(1,1-dioxothiazinan-2-yl)benzenesulfonamide
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	D (AU) D (US)
Legal status	POM (UK) ℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	100% (oral)
Protein binding	29%
Metabolism	Hepatic secretion
Half-life	24 hours
Excretion	Fecal (10%) and renal (90%)
Identifiers
CAS number	61-56-3 N
ATC code	N03AX03
PubChem	CID 5356
DrugBank	DB08329
ChemSpider	5163 Y
UNII	I00Q766CZ2 Y
KEGG	D01787 Y
ChEMBL	CHEMBL328560 Y
Chemical data
Formula	C10H14N2O4S2
Mol. mass	290.0395 g/mol
SMILES O=S2(=O)N(c1ccc(cc1)S(=O)(=O)N)CCCC2
InChI InChI=1S/C10H14N2O4S2/c11-18(15,16)10-5-3-9(4-6-10)12-7-1-2-8-17(12,13)14/h3-6H,1-2,7-8H2,(H2,11,15,16) Y Key:HMHVCUVYZFYAJI-UHFFFAOYSA-N Y
N (what is this?)  (verify)

Sultiame (rINN, also known as sulthiame) is a sulfonamide and inhibitor of the enzyme carbonic anhydrase. It is used as an anticonvulsant.

History

Sultiame was first synthesised in the laboratories of Bayer AG in the mid 1950s and eventually launched as Ospolot in Europe and other markets the early 1960s. It never became a registered drug in the USA. The brand was transferred to Desitin GmbH in 1993 and is sold in several European countries, in Israel, Japan, and Australia.

Sultiame became established as a second-line drug for treatment of partial epilepsy in the 1960s and 1970s and was often used in combination with the established anticonvulsant phenytoin. Temporal lobe seizures appeared particularly responsive to sultiame. Doubts subsequently arose as to whether sultiame has intrinsic anticonvulsant properties. After discovering sultiame's ability to raise the blood levels of phenytoin, it was assumed that sultiame would only act in combination with phenytoin. This finding, together with the equivocal results of a study in the US, resulted in a quick decline of sultiame's use. It was only in 1988, that the German child neurologist Hermann Doose discovered its specific effects in benign focal epilepsies of childhood. Today, sulthiame is the drug of choice for benign focal epilepsies of childhood (such as benign rolandic epilepsy) in the German-speaking countries and Israel. There is renewed interest in sultiame's other potential uses, e.g., in West syndrome and other refractory epilepsies

Indications

Historically, sultiame has been used to treat partial seizures. In Australia, it is currently registered for behavioural disorders associated with epilepsy; hyperkinetic behaviour; temporal lobe epilepsy; myoclonic seizures; grand mal attacks; and Jacksonian seizures. In contrast to other sulfonamide drugs, sultiame is devoid of antibacterial activity.

Adverse effects

The more common adverse effects are ataxia, paraesthesia of face and limbs, hyperpnoea, dyspnoea, and anorexia. Less common adverse effects include giddiness, rash, Stevens–Johnson syndrome, nausea, weight loss, leukopenia, headache, psychic changes, depression, drooling, increased pain, frequency of fits, insomnia, status epilepticus. Disturbances in calcium and vitamin D metabolism have been occasionally reported after long-term use.

Interactions

Sultiame taken together with primidone may lead to severe side-effects, including psychotic reactions. The addition of sulthiame to phenytoin therapy has shown to be followed by a rise in the serum levels of phenytoin. Sultiame may also lead to a rise of phenobarbitone blood levels. Alcohol must not be consumed during treatment.

Overdose

Vomiting, hypotension, headache, vertigo, ataxia, metabolic acidosis with hyperpnoea and catatonic state may occur. There is no specific antidote. It is not known whether dialysis may help in case of overdose.

References

English Journal

• Management of Landau-Kleffner syndrome.

• Mikati MA, Shamseddine AN.SourceDepartment of Pediatrics, and Adult and Pediatric Epilepsy Program, Faculty of Medicine, American University of Beirut, Beirut, Lebanon. mamikati@aub.edu.lb
• Paediatric drugs.Paediatr Drugs.2005;7(6):377-89.
• Landau-Kleffner syndrome (LKS) is an acquired epileptic aphasia disorder in which children, usually 3-8 years of age who have developed age-appropriate speech, experience language regression with verbal auditory agnosia, abnormal epileptiform activity, behavioral disturbances, and sometimes overt se
• PMID 16356025

• Detection of anticonvulsants and their metabolites in urine within a "general unknown" analysis procedure using computerized gas chromatography-mass spectrometry.

• Maurer HH.SourceInstitut fur Pharmakologie und Toxikologie, Universitat des Saarlandes, Homburg, Saar, Federal Republic of Germany.
• Archives of toxicology.Arch Toxicol.1990;64(7):554-61.
• Detection of the anticonvulsants carbamazepine, clonazepam, diazepam, ethosuximide, mephenytoin, mesuximide, methylphenobarbital, phenobarbital, phenytoin, primidone, propylhexedrine, sultiame, trimethadion and their metabolites in urine is described. The method presented is integrated in a general
• PMID 1981464

Japanese Journal

• A case with multiple abnormalities born to epileptic mother taking anticonvulsant drugs. Anticonvulsant embryopathy.:anticonvulsant embryopathy

• 今井 裕,横倉 幸弘,永島 知明,豊橋 真成,鈴木 克昌,岡部 清幸,細谷 玲子,坂元 晴彦,朝倉 昭人
• 日本口腔外科学会雑誌 37(2), 413-418, 1991
• … We would like to supply arguments for its diagnosis and also to make examination of the operative time for cleft palate associated with this case.<BR>The case is a 7-month-old male infat without siblings, whose parents' blood relative and lineages deny teratogenic diseases, His moher, who was diagnosed as epilepsy at age 9, has so far been taking anticonvulsant drugs (phenobar, sodium valporate, primidon, sultiame) without interruption during the pregnancy. …
• NAID 130001356350

Related Links

• Sultiame - Wikipedia, the free encyclopedia

Sultiame was first synthesised in the laboratories of Bayer AG in the mid 1950s and eventually launched as Ospolot in Europe and other markets the early 1960s . It never became a registered drug in the USA. The brand was transferred to ...

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