조니사미드

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H361：태아 또는 생식능력에 손상을 일으킬 것으로 의심됨

• 예방조치문구

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

조니사미드 MSDS

• 1-(1,2-Benzoxazol-3-yl)methanesulphonamide

조니사미드 화학적 특성, 용도, 생산

• 개요

  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.

• 화학적 성질

  Off-White Powder

• 용도

  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.

• 정의

  ChEBI: A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.

• 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.

• 일반 설명

  Zonisamide, a sulfonamide-type anticonvulsant was recentlyapproved for adjunctive therapy in the treatment ofpartial seizures in adults with epilepsy.Zonisamide isprimarily metabolized by reductive ring cleavage of the 1,2-benzisoxazole ring to 2-sulfamoyl-acetyl-phenol. This biotransformation is mainly carried out by theintestinal bacteria rather than the mammalian cytosolicaldehyde oxidase suggested earlier.Again, because ofthe presence of a sulfonamide moiety in zonisamide molecule,precaution should be given to patients who have ahistory of hypersensitivity reactions toward sulfonamidedrugs and concomitant use of zonisamide with other carbonicanhydrase inhibitors should also be avoided.

• Mechanism of action

  Zonisamide is a sulfonamide derivative that is indicated as an adjunct for partial seizures in patients older than 16 years whose seizures are not controlled by first-line drugs. In Japan, it is used for myoclonic seizures as well. Apparently, it has more than one mechanism of action—all as yet unidentified. It is known to produce blockade of both sodium and T-type calcium channels. Because it also affects dopaminergic transmission, bipolar or schizoaffective disorder patients may improve.

• Pharmacokinetics

  The absorption for orally administered zonisamide is slow but nearly complete. Its pharmacokinetics are nonlinear, with a half life of 50 to 70 hours when administered alone or 27 to 46 hours when administered concurrently with enzyme-inducing AEDs. Protein binding is moderate (<50%). An oral dose of zonisamide is completely absorbed, with peak plasma concentration occurring in 2 to 6 hours. Although the presence of food will delay the attainment of its peak plasma concentration, oral bioavailability does not appear to be altered. More than one-third of each oral dose is excreted in the urine in an unchanged form. The routes of metabolism for zonisamide include acetylation to form its N-acetyl metabolite, reduction by CYP3A4/CYP2D6, and the formation of an open-ring metabolite, 2-sulfamoylacetyl phenol. These metabolites subsequently are eliminated unconjugated or glucuronidated in the urine, with an elimination half-life of 63 hours. Its coadministration with enzyme-inducing AEDs, such as phenytoin, CBZ, or phenobarbital, and with valproate will alter its pharmacokinetics by reducing its half-life and serum concentration. The half-life for zonisamide is decreased to 27 hours in the presence of phenytoin, to 38 hours in the presence of either CBZ or phenobarbital, and to 46 hours with valproate. Other drugs that inhibit or induce CYP3A4 could affect the metabolism of zonisamide.
  Zonisamide should be used with caution in patients with hepatic or renal disease. It also has shown to be teratogenic in animal studies.

• 부작용

  Zonisamide is contraindicated in patients with a history of allergy to sulfonamides. The most frequent side effects include somnolence, anorexia, dizziness, agitation, confusion, headache, cognitive impairment, and memory loss. In addition, an incidence of drug-induced psychosis has been noted. Reports from both the United States and Europe have indicated that development of renal stones may occur with use of this drug. A family history of nephrolithiasis may be a contraindication, and urinary monitoring for hypercalciuria may be warranted in bedridden patients or those receiving multiple AEDs. Although the incidence of severe rashes attributable to zonisamide is low, sulfonamides are associated with Stevens-Johnson syndrome. Thus, it is recommended to discontinue the drug immediately should a rash occur.

• Safety Profile

  Moderately toxic by ingestion,intraperitoneal, subcutaneous, and intravenous routes. Anexperimental teratogen. Other experimental reproductiveeffects. When heated to decomposition it emits very toxicfumes of SOx and NOx. An anticonvulsant.

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