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zhyf2005

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[交流] 【求助】盐酸依氟鸟氨酸的英国药典标准？

急求助盐酸依氟鸟氨酸的英国药典或欧洲药典或美国药典标准？
化学品英文名称： Eflornithine hydrochloride
CAS No.：68278-23-9
分子式： C6H12F2N2O2.HCl
非常感谢！

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windli

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zhyf2005(金币+16,VIP+0):非常感谢！ 6-19 13:12

Eflornithine Hydrochloride
Drug Nomenclature
Date of monograph revision: 22-Aug-1996; 16-Jul-1998; 07-Jun-1999; 23-Aug-2000; 09-Aug-2001; 20-Sep-2002; 07-Jan-2005; 20-Jul-2006
Synonyms: α-Difluoromethylornithine Hydrochloride; DFMO; Eflornitina, hidrocloruro de; MDL-71782; MDL-71782A; RMI-71782
BAN: Eflornithine Hydrochloride [BANM]
USAN: Eflornithine Hydrochloride
INN: Eflornithine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de eflornitina [rINNM (es)]
INN: Éflornithine, Chlorhydrate d' [rINNM (fr)]
INN: Eflornithini Hydrochloridum [rINNM (la)]
INN: Ефлорнитина Гидрохлорид [rINNM (ru)]
Chemical name: 2-(Difluoromethyl)-dl-ornithine monohydrochloride monohydrate
Molecular formula: C6H12F2N2O2,HCl,H2O =236.6
CAS: 67037-37-0 (eflornithine); 96020-91-6 (eflornithine hydrochloride)
ATC code: D11AX16; P01CX03

Chemical Structure of Eflornithine

Adverse Effects and Precautions
Myelosuppression may lead to anaemia, leucopenia, and thrombocytopenia. Some patients have experienced hearing loss and alopecia. Gastrointestinal disturbances, especially diarrhoea, may occur. Seizures have occurred in about 8% of patients given eflornithine but they may have been related to the disease rather than treatment.

Dosage should be reduced in patients with renal impairment.

Skin irritation, such as erythema or a stinging or burning sensation, has been reported following topical application of eflornithine.

Effects on the ears.
A study in 58 patients1 receiving eflornithine alone or with interferon alfa for the treatment of metastatic melanoma found that hearing loss was related to the cumulative dose of eflornithine and was worse in patients with pre-existing hearing deficit.

1. Croghan MK, et al. Dose-related α-difluoromethylornithine ototoxicity. Am J Clin Oncol 1991; 14: 331–5. PubMed
Effects on the heart.
Fatal cardiac arrest occurred in an AIDS patient with pneumocystis pneumonia during the intravenous infusion of eflornithine 100 mg/kg over 1 hour.1 Sudden death after infusion of eflornithine had occurred in several other critically ill patients with AIDS.

1. Barbarash RA, et al Alpha-difluoromethylornithine infusion and cardiac arrest. Ann Intern Med 1986; 105: 141–2. PubMed
Pharmacokinetics
Eflornithine hydrochloride is absorbed from the gastrointestinal tract. After intravenous doses about 80% is excreted unchanged in the urine in 24 hours. The terminal elimination half-life is about 3 hours. It is distributed to the CSF.

Less than 1% of a dose is absorbed following topical application.

References.

1. Haegele KD, et al Kinetics of α-difluoromethylornithine: an irreversible inhibitor of ornithine decarboxylase. Clin Pharmacol Ther 1981; 30: 210–17. PubMed
2. Milord F, et al. Eflornithine concentrations in serum and cerebrospinal fluid of 63 patients treated for Trypanosoma brucei gambiense sleeping sickness. Trans R Soc Trop Med Hyg 1993; 87: 473–7. PubMed
3. Malhotra B, et al. Percutaneous absorption and pharmacokinetics of eflornithine HCl 13.9% cream in women with unwanted facial hair. J Clin Pharmacol 2001; 41: 972–8. PubMed
Uses and Administration
Eflornithine is an antiprotozoal that acts as an irreversible inhibitor of ornithine decarboxylase, the rate-limiting enzyme in polyamine biosynthesis; trypanosomes are more susceptible to the effects of eflornithine than are humans, probably because of their slower turnover of this enzyme.

Eflornithine is used in African trypanosomiasis due to Trypanosoma brucei gambiense. It is effective in the early and, more importantly, in the late stage of the disease (when there is CNS involvement).

In the treatment of African trypanosomiasis, eflornithine hydrochloride is given by intravenous infusion. The dose is 100 mg/kg every 6 hours for at least 14 days. Each dose should be administered over a period of at least 45 minutes. Dosage should be reduced in patients with renal impairment. It has also been given orally, in some instances after intravenous therapy, but diarrhoea can be troublesome with this route.

Eflornithine hydrochloride is also applied topically twice daily for the reduction of unwanted facial hair in women. It is available as a cream containing 15% eflornithine hydrochloride monohydrate; in the UK this content is expressed as 11.5% eflornithine and in the USA as 13.9% anhydrous eflornithine hydrochloride.

Cryptosporidiosis.
Eflornithine has been tried in the treatment of cryptosporidiosis () in AIDS patients.1

1. Rolston KVI, et al. Intestinal cryptosporidiosis treated with eflornithine: a prospective study among patients with AIDS. J Acquir Immune Defic Syndr 1989; 2: 426–30. PubMed
Hirsutism.
Topical eflornithine hydrochloride applied twice daily as a 13.9% cream is effective in reducing the growth of unwanted facial hair in females (see Hirsutism, ), although it must be used indefinitely to prevent regrowth.1 Its action is thought to be due to the irreversible inhibition of ornithine decarboxylase in hair follicles.

1. Barman Balfour JA, McClellan K. Topical eflornithine. Am J Clin Dermatol 2001; 2: 197–201. PubMed
Malignant neoplasms.
Eflornithine has antimetabolic activity and is being studied as a potential chemopreventive agent in patients at high risk of a variety of malignant diseases, including cancer of the bladder, breast, cervix, colon, oesophagus, prostate, and skin.1

1. Meyskens FL, Gerner EW. Development of difluoromethylornithine (DFMO) as a chemoprevention agent. Clin Cancer Res 1999; 5: 945–51. PubMed
African trypanosomiasis.
Eflornithine is effective in the treatment of Trypanosoma brucei gambiense infections (), and is particularly valuable in providing an alternative to melarsoprol in meningoencephalitic disease. Eflornithine 100 mg/kg intravenously every 6 hours for 7 days, rather than the standard 14 days, produced long-term responses in 42 of 47 patients who had relapsed after other treatment regimens.1 Similar positive results in relapsing cases were obtained with a short 7-day course in a multicentre randomised controlled study,2 although this short course was inferior to the 14-day course for new cases, in whom it could not be recommended. A patient who had relapsed after treatment with melarsoprol and eflornithine given singly was cured when the drugs were given together.3 Eflornithine is not effective when given alone in T. b. rhodesiense infections, and early reports of its use with suramin were not encouraging.4

1. Khonde N, et al. A seven days course of eflornithine for relapsing Trypanosoma brucei gambiense sleeping sickness. Trans R Soc Trop Med Hyg 1997; 91: 212–13. PubMed
2. Pepin J, et al. Short-course eflornithine in Gambian trypanosomiasis: a multicentre randomized controlled trial. Bull WHO 2000; 78: 1284–95. PubMed
3. Simarro PP, Asumu PN. Gambian trypanosomiasis and synergism between melarsoprol and eflornithine: first case report. Trans R Soc Trop Med Hyg 1996; 90: 315. PubMed
4. Clerinx J, et al. Treatment of late stage rhodesiense trypanosomiasis using suramin and eflornithine: report of six cases. Trans R Soc Trop Med Hyg 1998; 92: 449–50. PubMed
Preparations
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

France: Vaniqa; Ireland: Vaniqa; Spain: Vaniqa; United Kingdom: Vaniqa; United States: Ornidyl; Vaniqa;