Zonisamide

Zonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures, infantile spasm, mixed seizure types of Lennox–Gastaut syndrome, myoclonic, and generalized tonic clonic seizure.

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CAT No: 10-101-130

CAS No: 68291-97-4

Synonyms/Alias: AD-810; CI-912; PD-110843; 1,2-Benzisoxazole-3-methanesulfonamide; 3-(Sulfamoylmethyl)-1,2-benzisoxazole; Benzo[d]isoxazol-3-yl-methanesulfonamide

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M.F/FormulaC8H8N2O3S
M.W/Mr.212.23
Labeling TargetCarbonic anhydrase;
Voltage-dependent T-type calcium channel;
Sodium channel protein type 1 subunit alpha
ApplicationZonisamide has been used in the treatment in Epilepsy & Parkinson's disease & Tardive dyskinesia & Obesity & Migraines & Bipolar depression.
AppearanceSolid powder
Purity>98% (or refer to the Certificate of Analysis)
ActivityInhibitor
Biological ActivityZonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity.
Areas of InterestCardiovascular System & Diseases
Pituitary & Hypothalamic Hormones
FunctionsVasopressin receptor activity
TargetCarbonic Anhydrase
Source#Synthetic
Long-term Storage ConditionsSoluble in DMSO, not in water
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Short-term Storage ConditionsDry, dark and at 0 - 4 °C
Solubility-20 °C
OrganismHuman
InChIInChI=1S/C8H8N2O3S/c9-14(11,12)5-7-6-3-1-2-4-8(6)13-10-7/h1-4H,5H2,(H2,9,11,12)
InChI KeyUBQNRHZMVUUOMG-UHFFFAOYSA-N
BoilingPoint457.2±47.0 °C at 760 mmHg
ShelfLife>2 years if stored properly
References

Zonisamide is a modern antiepileptic drug (AED) that is distinguished from other AEDs by its unique structure and broad mechanistic profile. Preclinical studies have reported a range of potential mechanisms of action for zonisamide, such as blocking voltage-gated sodium channels, reduction of T-type calcium channel currents, and enhancement of gamma-aminobutyric acid (GABA)-mediated inhibition, which are indicative of its broad antiseizure effects. Zonisamide has a favorable linear pharmacokinetic profile, a long half-life, and a low incidence of protein-binding interactions with other AEDs.

Wilfong, A. A., & Willmore, L. J. (2006). Zonisamide–a review of experience and use in partial seizures. Neuropsychiatric disease and treatment, 2(3), 269.

The limitations of currently available therapies in addressing the non motor symptoms of Parkinson's disease (PD) have egged on the search for newer options. Zonisamide has been in use for epilepsy and it was serendipitously found to improve the symptoms of PD in a patient who had both epilepsy and PD. Thereafter, various trials were designed to assess the use of zonisamide in PD. The present article investigates the evidence for use of zonisamide in PD from the various clinical trials that were designed to address this issue. Furthermore, the article also summarizes the various mechanisms of its use in PD as described in various animal experiments.

Grover, N. D., Limaye, R. P., Gokhale, D. V., & Patil, T. R. (2013). Zonisamide: a review of the clinical and experimental evidence for its use in Parkinson's disease. Indian journal of pharmacology, 45(6), 547.

Epilepsy is one of the most common neurologic disorders, affecting about 50 million people around the world. It is recognized that around 50% of patients with newly diagnosed epilepsy become seizure-free with the first drug treatment, so the choice of first antiepileptic drug is crucial. This paper provides a comprehensive overview of zonisamide as monotherapy for partial seizures, with special attention to the possibility of a once-daily regimen. The available data suggest that zonisamide is an effective and well tolerated option as monotherapy.

Mula, M. (2013). Profile of once-daily zonisamide as monotherapy for treatment of partial seizures in adults. Drug design, development and therapy, 7, 397.

Melting Point275°C dec.
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