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氟尼辛葡甲胺和非甾体类抗炎药(昔布类)在马房水中的分布。

Distribution of flunixin meglumine and firocoxib into aqueous humor of horses.

机构信息

William R. Pritchard Veterinary Medical Teaching Hospital, University of California, Davis, CA, USA.

出版信息

J Vet Intern Med. 2011 Sep-Oct;25(5):1127-33. doi: 10.1111/j.1939-1676.2011.0763.x. Epub 2011 Jul 22.

Abstract

BACKGROUND

Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used systemically for the treatment of inflammatory ocular disease in horses. However, little information exists regarding the ocular penetration of this class of drugs in the horse.

OBJECTIVE

To determine the distribution of orally administered flunixin meglumine and firocoxib into the aqueous humor of horses.

ANIMALS

Fifteen healthy adult horses with no evidence of ophthalmic disease.

METHODS

Horses were randomly assigned to a control group and 2 treatment groups of equal sizes (n = 5). Horses assigned to the treatment groups received an NSAID (flunixin meglumine, 1.1 mg/kg PO q24h or firocoxib, 0.1 mg/kg PO q24h for 7 days). Horses in the control group received no medications. Concentrations of flunixin meglumine and firocoxib in serum and aqueous humor and prostaglandin (PG) E(2) in aqueous humor were determined on days 1, 3, and 5 and aqueous : serum ratios were calculated.

RESULTS

Firocoxib penetrated the aqueous humor to a significantly greater extent than did flunixin meglumine at days 3 and 5. Aqueous : serum ratios were 3.59 ± 3.32 and 11.99 ± 4.62% for flunixin meglumine and firocoxib, respectively. Ocular PGE(2) concentrations showed no differences at any time point among study groups.

CONCLUSIONS AND CLINICAL IMPORTANCE

Both flunixin meglumine and firocoxib penetrated into the aqueous humor of horses. This study suggests that orally administered firocoxib penetrates the aqueous humor better than orally administered flunixin meglumine at label dosages in the absence of ocular inflammation. Firocoxib should be considered for the treatment of inflammatory ophthalmic lesions in horses at risk for the development of adverse effects associated with nonselective NSAID administration.

摘要

背景

非甾体类抗炎药(NSAIDs)常用于马的眼部炎症的全身治疗。然而,关于此类药物在马眼中的渗透情况,信息甚少。

目的

确定口服氟尼辛葡甲胺和非诺考昔在马的房水中的分布。

动物

15 匹无眼部疾病迹象的健康成年马。

方法

马被随机分配到对照组和 2 个相等大小的治疗组(n = 5)。接受 NSAID 治疗的马(氟尼辛葡甲胺,1.1 mg/kg PO q24h 或非诺考昔,0.1 mg/kg PO q24h 连续 7 天)。对照组马不接受任何药物。在第 1、3 和 5 天测定血清和房水中的氟尼辛葡甲胺和非诺考昔浓度以及房水中的前列腺素(PG)E2,并计算房水:血清比值。

结果

在第 3 和 5 天,非诺考昔在房水中的渗透程度明显大于氟尼辛葡甲胺。氟尼辛葡甲胺和非诺考昔的房水:血清比值分别为 3.59 ± 3.32 和 11.99 ± 4.62%。在任何时间点,研究组之间的眼内 PGE2 浓度均无差异。

结论和临床意义

氟尼辛葡甲胺和非诺考昔均渗透入马的房水。本研究表明,在无眼部炎症的情况下,与口服氟尼辛葡甲胺相比,按标签剂量口服非诺考昔更能渗透入房水。对于有发生与非选择性 NSAID 给药相关不良反应风险的眼部炎症性病变的马,应考虑使用非诺考昔进行治疗。

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