OXAMNIQUINE(200MG)DISCONTINUED

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H413：장기적 영향에 의해 수생생물에 유해의 우려가 있음

• 예방조치문구

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

  P301+P312：삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P330：입을 씻어내시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

OXAMNIQUINE(200MG)DISCONTINUED 화학적 특성, 용도, 생산

• 개요

  Oxamniquine was originally investigated in the 1960s and was found to have limited antiprotozoal activity, with activity against Schi stosoma mansoni but no activity against the other two schistosomal organisms. In addition, the drug is stage specific, with activity against cercariae and very young schistosomula and adult worms. For reasons that remain unknown, the drug is more effective against adult male worms than against female worms. The drug has structural similarity to hycanthone, which is no longer used because of severe toxicity and teratogenic effects.

• 용도

  Antischistosomal.

• 정의

  ChEBI: A member of the class of quinolines that is 1,2,3,4-tetrahydroquinoline which is substituted at positions 2, 6, and 7 by (isopropylamino)methyl, hydroxymethyl, and nitro groups, respectively.

• Indications

  Oxamniquine (Vansil) is a tetrahydroquinoline that stimulates parasite muscular activity at low concentrations but causes paralysis at higher concentrations. The drug may act by esterification and binding of DNA, leading to the death of the schistosome by interruption of its nucleic acid and protein synthesis. The fluke may esterify oxamniquine to produce a reactive metabolite that alkylates parasite DNA. Resistance results from absent or defective esterifying activity of the drug. Oxamniquine has a restricted range of efficacy, being active only against S. mansoni infections.
  Oxamniquine is given orally and is readily absorbed from the intestinal tract. Peak concentrations in plasma are obtained in about 3 hours. The drug is excreted in urine mostly as a 6-carboxyl derivative.
  Side effects include CNS toxicity with unsteadiness and occasionally seizures, especially in patients with a history of seizures. It is contraindicated in pregnancy.

• Antimicrobial activity

  Activity is restricted to Schistosoma mansoni. Some strains, particularly those in Egypt and Southern Africa, require higher doses for efficacy owing to innate tolerance.

• Pharmaceutical Applications

  A synthetic quinolinemethanol, available for oral administration.

• Mechanism of action

  Oxamniquine is activated via esterification to a biological ester that spontaneously dissociates to an electrophile, which alkylates the helminth DNA, leading to irreversible inhibition of nucleic acid metabolism. Resistant helminths do not esterify oxamniquine; therefore, activation does not occur. Other metabolic reactions consist of oxidative reactions, leading to inactivation. The metabolites are excreted primarily in the urine.

• Pharmacokinetics

  It is rapidly absorbed after oral administration, achieving a peak concentration of 0.3–2.5 mg/L 1–3 h after an oral dose of 15 mg/kg body weight. Peak levels following intramuscular treatment at 7.5 mg/kg generally do not exceed 0.15 mg/L. It is extensively metabolized to biologically inactive 6-carboxylic and 2-carboxylic acid derivatives, which are excreted in the urine, mostly within 12 h.

• Clinical Use

  Infection with S. mansoni

• 부작용

  Dizziness, sleepiness, nausea and headache occur frequently. Other side effects are probably due to the death and disintegration of the worms in the liver. Following treatment, urine may become red.

• Safety Profile

  Poison by ingestion, intraperitoneal and intramuscular routes. Human mutation data reported. An antischistosomal agent. When heated to decomposition it emits toxic fumes of NOx.

OXAMNIQUINE(200MG)DISCONTINUED 준비 용품 및 원자재

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