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QuickView for Zonisamide (compound)


PubChem
Name: zonisamide
PubChem Compound ID: 5734
Molecular formula: C8H8N2O3S
Molecular weight: 212.227 g/mol
Synonyms:
Excegram; Excegran; 3-(Sulfamoylmethyl)-1,2-benzisoxazole; HSDB 7293; Exceglan; Zonisamidum [Latin]; 68291-97-4; Excegran (TN); Zonisamide (JAN/USAN); Zonisamide.
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DrugBank
Identification
Name: zonisamide
Name (isomeric): DB00909
Drug Type: small molecule
Synonyms:
Zonisamidum [Latin]; Zonisamida [Spanish]
Brand: Zonegran, Exceglan, Excegran, Excegram
Category: Antioxidants, Anticonvulsants
CAS number: 68291-97-4
Pharmacology
Indication: For use as adjunctive treatment of partial seizures in adults with epilepsy.
Pharmacology:
Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium and calcium channels, which leads to the suppression of neuronal hypersynchronization (i.e. convul...
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Mechanism of Action: Zonisamide binds to sodium channels and voltage sensitive calcium channels, which suppresses neuronal depolarization and hypersynchronization. Zonisamide also inhibits carbonic anhydrase to a weaker extent, but such an effect is not thought to contribute substantially to the drug's anticonvulsant activity.
Absorption: Variable, yet relatively rapid rate of absorption with a time to peak concentration of 2.8-3.9 hours. Food has no effect on the bioavailability of zonisamide.
Protein binding: 40% (at concentrations of 1.0-7.0 µg/mL)
Biotransformation: Primarily hepatic through cytochrome P450 isoenzyme 3A4 (CYP3A4). Undergoes acetylation and reduction, forming N-acetyl zonisamide, and the open-ring metabolite 2–sulfamoylacetyl phenol, respectively.
Route of elimination: Zonisamide is excreted primarily in urine as parent drug and as the glucuronide of a metabolite.
Half Life: 63 hours
Clearance: 0.30 - 0.35 mL/min/kg [patients not receiving enzyme-inducing antiepilepsy drugs (AEDs)] 0.35 - 0.5 mL/min/kg [Concomitant administration of phenytoin and carbamazepine]
Toxicity: Symptoms of overdose include diminished breathing, loss of consciousness, low blood pressure, and slow heartbeat.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if voriconazole is initiated, discontinued or dose changed.
NefazodoneNefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if nefazodone is initiated, discontinued or dose changed.
MefloquineMefloquine may decrease the serum concentration and therapeutic effect of zonisamide. Concomitant therapy is contraindicated in patients with history of convulsions.
DelavirdineDelavirdine, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if delavirdine is initiated, discontinued or dose changed.
RitonavirRitonavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if ritonavir is initiated, discontinued or dose changed.
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