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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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Excegram; Excegran; 3-(Sulfamoylmethyl)-1,2-benzisoxazole; HSDB 7293; Exceglan; Zonisamidum [Latin]; 68291-97-4; Excegran (TN); Zonisamide (JAN/USAN); Zonisamide; E-2090; D00538; AD-810; PD 110843; Zonegran; BRN 1077076; LS-33637; Tremode; Zonisamide [USAN:BAN:INN:JAN]; CI-912; Zonisamida [Spanish]; C07504; 1,2-Benzisoxazole-3-methanesulfonamide; ZINC00004321
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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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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. convulsions). Sonisamide has also been found to potentiate dopaminergic and serotonergic neurotransmission but does not appear to potentiate syanptic activity by GABA (gamma amino butyric acid).
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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: |
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Targets
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient
| UniProt ID: | P35498 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Gene: | SCN1A | ||||||||
| Actions: | inhibitor | ||||||||
| References: |
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Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient
| UniProt ID: | Q99250 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN2A | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient
| UniProt ID: | Q9NY46 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN3A | |||||||
| Actions: | inhibitor | |||||||
| References: |
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This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. This sodium channel may be present in both denervated and innervated skeletal muscle
| UniProt ID: | P35499 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN4A | |||||||
| Actions: | inhibitor | |||||||
| References: |
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This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is responsible for the initial upstroke of the action potential in the electrocardiogram
| UniProt ID: | Q14524 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN5A | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-sensitive Na(+) channel isoform. Plays a role in pain mechanisms, especially in the development of inflammatory pain
| UniProt ID: | Q15858 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN9A | |||||||
| Actions: | inhibitor | |||||||
| References: |
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This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant sodium channel isoform. Also involved, with the contribution of the receptor tyrosine kinase NTRK2, in rapid BDNF-evoked neuronal depolarization
| UniProt ID: | Q9UI33 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN11A | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-1 can modulate multiple alpha subunit isoforms from brain, skeletal muscle, and heart. Its association with neurofascin may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons
| UniProt ID: | Q07699 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN1B | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-2 causes an increase in the plasma membrane surface area and in its folding into microvilli. Interacts with TNR may play a crucial role in clustering and regulation of activity of sodium channels at nodes of Ranvier (By similarity)
| UniProt ID: | O60939 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN2B | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Modulates channel gating kinetics. Causes unique persistent sodium currents. Inactivates the sodium channel opening more slowly than the subunit beta-1. Its association with neurofascin may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons (By similarity)
| UniProt ID: | Q9NY72 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN3B | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Modulates channel gating kinetics. Causes negative shifts in the voltage dependence of activation of certain alpha sodium channels, but does not affect the voltage dependence of inactivation (By similarity)
| UniProt ID: | Q8IWT1 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | SCN4B | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by mibefradil. A particularity of this type of channels is an opening at quite negative potentials and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes
| UniProt ID: | O43497 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Gene: | CACNA1G | ||||||||||||
| Actions: | inhibitor | ||||||||||||
| References: |
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Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1H gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by nickel and mibefradil. A particularity of this type of channels is an opening at quite negative potentials, and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes
| UniProt ID: | O95180 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Gene: | CACNA1H | ||||||||||
| Actions: | inhibitor | ||||||||||
| References: |
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Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. Isoform alpha-1I gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by nickel and mibefradil. A particularity of this type of channels is an opening at quite negative potentials, and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes. Gates in voltage ranges similar to, but higher than alpha 1G or alpha 1H
| UniProt ID: | Q9P0X4 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Gene: | CACNA1I | ||||||||||
| Actions: | inhibitor | ||||||||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | P00915 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Gene: | CA1 | ||||||||
| Actions: | inhibitor | ||||||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | P00918 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Gene: | CA2 | |||||||||
| Actions: | inhibitor | |||||||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | P07451 | ||||||
|---|---|---|---|---|---|---|---|
| Gene: | CA3 | ||||||
| Actions: | inhibitor | ||||||
| References: |
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Reversible hydration of carbon dioxide. May stimulate the sodium/bicarbonate transporter activity of SLC4A4
| UniProt ID: | P22748 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA4 | |||||
| Actions: | inhibitor | |||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | P35218 | ||||||
|---|---|---|---|---|---|---|---|
| Gene: | CA5A | ||||||
| Actions: | inhibitor | ||||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | Q9Y2D0 | ||||||
|---|---|---|---|---|---|---|---|
| Gene: | CA5B | ||||||
| Actions: | inhibitor | ||||||
| References: |
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| UniProt ID: | P23280 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA6 | |||||
| Actions: | inhibitor | |||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | P43166 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA7 | |||||
| Actions: | inhibitor | |||||
| References: |
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Does not have a carbonic anhydrase catalytic activity
| UniProt ID: | P35219 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA8 | |||||
| Actions: | inhibitor | |||||
| References: |
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Reversible hydration of carbon dioxide. May be involved in the control of cell proliferation and transformation. Appears to be a novel specific biomarker for a cervical neoplasia
| UniProt ID: | Q16790 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA9 | |||||
| Actions: | inhibitor | |||||
| References: |
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Does not have a catalytic activity
| UniProt ID: | Q9NS85 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA10 | |||||
| Actions: | inhibitor | |||||
| References: |
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Does not have a catalytic activity
| UniProt ID: | O75493 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA11 | |||||
| Actions: | inhibitor | |||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | O43570 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA12 | |||||
| Actions: | inhibitor | |||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | Q8N1Q1 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA13 | |||||
| Actions: | inhibitor | |||||
| References: |
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Reversible hydration of carbon dioxide
| UniProt ID: | Q9ULX7 | |||||
|---|---|---|---|---|---|---|
| Gene: | CA14 | |||||
| Actions: | inhibitor | |||||
| References: |
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Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOB preferentially degrades benzylamine and phenylethylamine
| UniProt ID: | P27338 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | MAOB | |||||||
| Actions: | inhibitor | |||||||
| References: |
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Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine
| UniProt ID: | P21397 | ||
|---|---|---|---|
| Gene: | MAOA | ||
| Actions: | inhibitor | ||
| References: |
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Enzymes
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide
| UniProt ID: | P08684 | |||||
|---|---|---|---|---|---|---|
| Gene: | CYP3A4 | |||||
| Actions: | substrate | |||||
| References: |
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An aldehyde + H(2)O + O(2) = a carboxylic acid + H(2)O(2)
| UniProt ID: | Q06278 | ||
|---|---|---|---|
| Gene: | AOX1 | ||
| Actions: | substrate | ||
| References: |
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Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine
| UniProt ID: | P33261 | |
|---|---|---|
| Gene: | CYP2C19 | |
| Actions: | inhibitor | |
| References: |
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