Sultiame

Revision as of 15:06, 10 April 2015 by Aparna Vuppala (talk | contribs)
(diff) ← Older revision | Latest revision (diff) | Newer revision → (diff)
Jump to navigation Jump to search
Sultiame
Clinical data
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
  • AU: D
  • US: D (Evidence of risk)
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability100% (oral)
Protein binding29%
MetabolismHepatic secretion
Elimination half-life24 hours
ExcretionFecal (10%) and renal (90%)
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC10H14N2O4S2
Molar mass290.0395 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

WikiDoc Resources for Sultiame

Articles

Most recent articles on Sultiame

Most cited articles on Sultiame

Review articles on Sultiame

Articles on Sultiame in N Eng J Med, Lancet, BMJ

Media

Powerpoint slides on Sultiame

Images of Sultiame

Photos of Sultiame

Podcasts & MP3s on Sultiame

Videos on Sultiame

Evidence Based Medicine

Cochrane Collaboration on Sultiame

Bandolier on Sultiame

TRIP on Sultiame

Clinical Trials

Ongoing Trials on Sultiame at Clinical Trials.gov

Trial results on Sultiame

Clinical Trials on Sultiame at Google

Guidelines / Policies / Govt

US National Guidelines Clearinghouse on Sultiame

NICE Guidance on Sultiame

NHS PRODIGY Guidance

FDA on Sultiame

CDC on Sultiame

Books

Books on Sultiame

News

Sultiame in the news

Be alerted to news on Sultiame

News trends on Sultiame

Commentary

Blogs on Sultiame

Definitions

Definitions of Sultiame

Patient Resources / Community

Patient resources on Sultiame

Discussion groups on Sultiame

Patient Handouts on Sultiame

Directions to Hospitals Treating Sultiame

Risk calculators and risk factors for Sultiame

Healthcare Provider Resources

Symptoms of Sultiame

Causes & Risk Factors for Sultiame

Diagnostic studies for Sultiame

Treatment of Sultiame

Continuing Medical Education (CME)

CME Programs on Sultiame

International

Sultiame en Espanol

Sultiame en Francais

Business

Sultiame in the Marketplace

Patents on Sultiame

Experimental / Informatics

List of terms related to Sultiame

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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,[1] 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,[2] 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.[3] 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.[4] There is renewed interest in sultiame's other potential uses, e.g., in West syndrome[5] and other refractory epilepsies[6]

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.[7] 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.

Synthesis

p-Aminobenzenesulfonamide can be alkylated by ω-chlorobutylsulfonyl chloride in base via presumed intermediate, which spontaneously cyclizes to give sulthiame.

References

  1. Hansen JM, Kristensen M, Skovsted L. Sulthiame (Ospolot) as inhibitor of diphenylhydantoin metabolism. Epilepsia 1968;9:17-22. PMID 4386877
  2. Green JR et al. Sulthiame: Evaluation as an anticonvulsant. Epilepsia 1974;15:329-49. PMID 4386877
  3. Doose H et al. Benign partial epilepsy - treatment with sulthiame. Dev Med Child Neurol 1988;30:683-4. PMID 2906619
  4. Wohlrab G. Epilepsiebehandlung im Kindes- und Jugendalter: Kontinuität und Wandel. Epileptologie 2003;20:25-30.
  5. Debus OM et al. Sulthiame in the primary therapy of West syndrome. Epilepsia 2004;45:103-8. PMID 14738417
  6. Koepp MJ et al. Sulthiame in adults with refractory epilepsy and learning disability: an open trial. Epilepsy Res 2002;50:277-82. PMID 12200218
  7. Pharmalab Pty Ltd. Product Information Ospolot (Sulthiame).

Template:Anticonvulsants