Sultiame



Sultiame
Systematic (IUPAC) name
4-(1,1-dioxothiazinan-2-yl)benzenesulfonamide
Identifiers
CAS number 61-56-3
ATC code N03AX03
PubChem 5356
Chemical data
S2 
Mol. mass 290.0395 g/mol
Pharmacokinetic data
Bioavailability 100% (oral)
Protein binding 29%
Metabolism Hepatic secretion
Half life 24 hours
Excretion Fecal (10%) and renal (90%)
Therapeutic considerations
Pregnancy cat.

D(AU) D(US)

Legal status

-only(US)

Routes Oral

Sultiame (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 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 metabolism have been occasionally reported after long-term use.

Interactions

Sultiame taken together with phenobarbitone blood levels. Alcohol must not be consumed during treatment.

Overdose

Vomiting, hypotension, headache, vertigo, ataxia, metabolic antidote. It is not known whether dialysis may help in case of overdose.

References

  1. ^ Hansen JM et al. Sulthiame (Ospolot) as inhibitor of diphenylhydantoin metabolism. Epilepsia 1968;9:17-22.
  2. ^ Green JR et al. Sulthiame: Evaluation as an anticonvulsant. Epilepsia 1974;15:329-49.
  3. ^ Doose H et al. Benign partial epilepsy - treatment with sulthiame. Dev Med Child Neurol 1988;30:683-4.
  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.
  6. ^ Koepp MJ et al. Sulthiame in adults with refractory epilepsy and learning disability: an open trial. Epilepsy Res 2002;50:277-82.
  7. ^ Pharmalab Pty Ltd. Product Information Ospolot (Sulthiame).


 
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