Chemical Property of 1,2-Benzoxazol-3-ylmethanesulfonimidic acid
Chemical Property:
- Appearance/Colour:off-white powder
- Melting Point:275°C dec
- Refractive Index:1.5690 (estimate)
- Boiling Point:457.2 °C at 760 mmHg
- PKA:10.2(at 25℃)
- Flash Point:230.3 °C
- PSA：94.57000
- Density:1.509 g/cm3
- LogP:2.39740
- Storage Temp.:Store at +4°C
- Solubility.:H2O: >5 mg/mL, soluble
- XLogP3:1.7
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:2
- Exact Mass:212.02556330
- Heavy Atom Count:14
- Complexity:314
- Purity/Quality:
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99% *data from raw suppliers
1,2-Benzisoxazole-3-methanesulfonate, Sodium Salt *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xn
- Hazard Codes:Xn,T,F
- Statements:
22-39/23/24/25-23/24/25-11
- Safety Statements:
7-16-36/37-45
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1=CC=C2C(=C1)C(=NO2)CS(=N)(=O)O
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Description
Zonisamide is a new generation of sulfonamide anticonvulsant that is primarily used as supplemental therapy in treatment of partial seizures in combination with other antiepileptic medications. Besides, it is approved to be applied as an adjunctive therapy in adults suffering from infantile spasm, mixed seizure types of Lennox–Gastaut syndrome, myoclonic, and generalized tonic clonic seizure. Recent studies have proved that zonisamide can acts as a migraine preventative medication and is effective in several cases of neuropathic pain. In an open-label trial, zonisamide shows positive effects on attenuating the symptoms of tardive dyskinesia.
Zonisamide is a second-generation antiepileptic drug (AED) known with the proprietary brand name of Zonegran? (Eisai) in the UK and USA. It is assumed that zonisamide functions on the sodium and calcium channels in the brain cells, in which it controls electric-currents that are responsible for seizure activity. The FDA approved zonisamide in March 2000. Zonisamide is a broad-spectrum antiepileptic effective in the treatment of refractory
seizures. In cultured spinal cord neurons, zonisamide blocks the sustained firing of action
potentials induced by depolarizing steps of current injected across the membrane.
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Indications
Epilepsy
Monotherapy of focal seizures with or without secondary generalization and adjunctive therapy of refractory focal seizures with or without secondary generalization.
Recommendations summarized from NICE (2012)
Seizure types: on referral to tertiary care (absence seizures, focal seizures, myoclonic seizures).
Epilepsy types: on referral to tertiary care (absence syndromes, juvenile myoclonic epilepsy, idiopathic generalized epilepsy, benign epilepsy with centrotemporal spikes, panayiotopoulos syndrome, late- onset childhood occipital epilepsy).
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Uses
anticonvulsant;carbonic anhydrase inhibitor, repetitive firing of voltage-gated sodium channels and reduction of T-type calcium channel currents blocker Sulfonamide antiseizure agent; blocks repetitive firing of voltagesensitive sodium channels and reduces voltage-sensitive T-type calcium currents. Heterocyclic methanesulfonide with anticonvulsant pro
perties. The compound is under investigation for potential therapeutic use as an antiepileptic drug. Anticonvulsant. muscarinic antagonist used as an antispasmodic For use as adjunctive treatment of partial seizures in adults with epilepsy.
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Therapeutic Function
Anticonvulsant; Antiepileptic
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Biological Functions
Zonisamide has only recently been approved for use in
the United States, although it has been available in
Japan for several years. It is effective in partial complex
and generalized tonic–clonic seizures and also appears
to be beneficial in certain myoclonic seizures. It has a
long half-life (about 60 hours) and requires about 2
weeks to achieve steady-state levels. It causes cerebellovestibular
side effects similar to those of most
other AEDs sharing its mechanism of action. In addition,
it appears to cause an increased incidence of kidney
stones.
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Drug interactions
Potentially hazardous interactions with other drugs
Antidepressants: anticonvulsant effect antagonised;
avoid with St John’s wort.
Antimalarials: anticonvulsant effect antagonised by
mefloquine.
Antipsychotics: anticonvulsant effect antagonised.
Orlistat: increased risk of convulsions.
