2-(디플루오로메틸)-DL-오르니틴

2-(디플루오로메틸)-DL-오르니틴 화학적 특성, 용도, 생산

• Antimicrobial activity

  Cultured bloodstream trypomastigotes of T. brucei are relatively insensitive, but high doses are effective against bloodstream and CNS infections of T. brucei brucei and T. brucei gambiense in rodents, provided a strong antibody response is also present. Eflornithine entry into the CNS can be enhanced with suramin. T. brucei rhodesiense infections do not respond. Synergy with some arsenicals has been demonstrated.
  Eflornithine is active against P. falciparum in experimental models and against Leishmania promastigotes and Giardia lamblia in culture.

• 원료

  Acquired resistance in T. brucei gambiense in West Africa has not been reported. East African T. brucei rhodesiense strains are innately less sensitive. Reported treatment failures are thought to be associated with severity of disease.

• Pharmaceutical Applications

  An analog of ornithine, formulated as the hydrochloride for intravenous infusion. It is freely soluble in water.

• Pharmacokinetics

  Oral absorption: 55%
  C_max 10 mg/kg oral: c. 7 mg/L after 4 h
  200 mg/kg intravenously: 15.9 mg/L (87.5 nmol/mL) (mean)
  Plasma half-life: 3.3 h
  Volume of distribution: 0.34 L/kg
  Plasma protein binding: Very low
  Renal clearance is 83%, with most eliminated unchanged. In a study in Zaire the mean serum concentration in children under 12 years old was half that of adults, probably due to more rapid renal clearance. CNS penetration is good in adult patients, with a CSF:plasma ratio of 0.91 at the end of administration for 14 days. However, the CSF:plasma ratio in children under 12 years old was 0.58. Relapses have been recorded in patients in whom CSF levels dropped below 9 mg/L (50 nmol/mL) at the end of treatment.

• Clinical Use

  2-(Difluoromethyl)-DL-ornithine has been used speculatively for treatment of Pn. jirovecii infections in AIDS patients. Co-administration with oral nifurtimox has been added to the World Health Organization (WHO) List of Essential Medicines for second-stage sleeping sickness caused by T. brucei gambiense.

• 부작용

  Osmotic diarrhea and bone marrow suppression are common, and up to 50% of sleeping sickness patients develop leukopenia. Reversible anemia and thrombocytopenia have been observed. Convulsions and seizures, different from those observed in melarsoprol-induced encephalopathy, have been reported in 4–18% of treated sleeping sickness patients but not in patients treated for Pn. jirovecii pneumonia. This difference might be due to the CNS inflammation associated with sleeping sickness.

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