異克舒普林
Isoxsuprine
Isoxsuprine Hydrochloride
別名: Vasodilan · Voxsuprine · Caa-40 · isoxsuprini hydrochloridum · phenoxyisopropylnorsuprifen · Dilum · Duvadilan · Fadaespasmol · Fenam · Inibina · Isodilan · Isotenk · Uterine · Vadosilan · Vasolan · Vasosuprina Ilfi · Xuprin
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Treatment of 'Raynaud-like' disease | 1 mg/kg/day PO | PO | daily | — | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Treatment of orthopedic conditions, such as navicular disease (For long break-over if therapeutic shoeing does not correct) | 1.2 mg/kg PO q8h for 3 weeks. The dose is decreased as soundness improves, to 1.2 mg/kg PO once daily for 6 weeks, then every other day until heel first landing occurs. | PO | q8h initially | 3 weeks initially, then tapered | 🌎 NA |
| Treatment of orthopedic conditions, such as navicular disease (To increase the circulation to the podotrochlea) | 0.6-1.2 mg/kg twice daily until sound, then decreased to once daily for 2 weeks then further decreased to every other day. | PO | twice daily initially | Until sound, then tapered | 🌎 NA |
| Treatment of orthopedic conditions | 0.6-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| As a tocolytic agent | 0.4-0.6 mg/kg IM or PO twice daily | IM or PO | twice daily | — | 🌎 NA |
- Treatment of orthopedic conditions, such as navicular disease (For long break-over if therapeutic shoeing does not correct): Phenylbutazone is added if lameness is greater than grade II on a scale of I-V, or until recheck occurs. The drug is classified as a 'blocking' agent by the AHSA.
- As a tocolytic agent: Efficacy is unproven and oral bioavailability appears highly variable.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
Isoxsuprine 是一種周邊血管擴張劑,在獸醫學中主要用於治療馬的舟狀骨病 (navicular disease),但由於其口服生物利用度差,近期的研究對其口服療效提出質疑。
- 馬科應用:歷史上用於改善馬蹄及舟狀骨滑車的血液循環。也有傳聞用作安胎劑。
- 犬科應用:傳聞可用於治療類雷諾氏症候群(週期性指端發紺、甲彎曲)。
- 鳥類應用:可能改善微循環。
臨床要點:由於顯著的首過代謝效應,馬匹口服給藥通常無法達到可測量的血漿濃度,導致許多現代獸醫對其在舟狀骨症候群的臨床實用性產生質疑,轉而傾向使用如 pentoxifylline 等其他血液流變學藥物。
作用機制
Isoxsuprine acts as a beta-adrenergic agonist (specifically beta-2 receptors), though its vasodilatory effects may also stem from direct smooth muscle relaxation independent of beta-receptors.
- Vasodilation: Stimulates beta-2 receptors → increases intracellular cAMP → decreases intracellular calcium → vascular smooth muscle relaxation (primarily in skeletal muscle).
- Uterine Relaxation: Relaxes uterine smooth muscle, acting as a tocolytic agent.
- Hemorrheologic Effects: At high doses, it can decrease blood viscosity and reduce platelet aggregation.
- Cardiac Effects: May exhibit positive inotropic and chronotropic effects on the heart via beta-1 receptor stimulation.
- Analgesia: Does not appear to possess significant analgesic properties in horses.
安全性與警告
禁忌症
- Immediately post-partum
- Presence of arterial bleeding
不良反應
- CNS stimulation (uneasiness, hyperexcitability, nose-rubbing)
- Sweating
- Hypotension
- Tachycardia
- Gastrointestinal disturbances
注意事項
Warning: Do not administer immediately post-partum or in the presence of active arterial bleeding due to its vasodilatory properties.
- Pregnancy: FDA Category C (animal studies show adverse fetal effects; use with caution).
- Lactation: Safety is unknown.
- Regulatory: Classified as an ARCI Class 4 drug and a 'blocking' agent by the AHSA.
監測
- Clinical efficacy (improvement in lameness or digital circulation)
- Adverse effects (tachycardia, GI disturbances, CNS stimulation)
藥物動力學
半衰期
吸收
In humans, almost completely absorbed from the GI tract. In horses, bioavailability is low after oral administration, probably due to a high first-pass effect.
代謝
Undergoes significant first-pass metabolism in horses.
過量
Serious toxicity is unlikely in horses after an inadvertent oral overdose due to poor bioavailability.
- Clinical Signs: CNS stimulation (uneasiness, hyperexcitability, nose-rubbing), sweating, hypotension, tachycardia, and GI disturbances.
- Treatment: Provide supportive care. Treat CNS hyperexcitability with diazepam, and hypotension with intravenous fluids.
可用產品
劑型
- Tablets
人用標示
- Isoxsuprine HCl Tablets: 10 mg & 20 mg (Vasodilan, Voxsuprine, generic)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored in tight containers at room temperature (15-30°C).
飼主須知
- 按時服藥:為了達到最佳療效,必須嚴格按照獸醫的指示按時給藥。
- 給藥技巧:在給藥前,可以將藥片壓碎,並加入玉米糖漿或櫻桃糖漿等製成泥狀或糊狀,以提高動物的接受度。
- 注意事項:如果您發現寵物出現焦躁不安、過度出汗、心跳過快或腸胃不適的跡象,請立即聯繫您的獸醫。
- 儲存方式:請將藥片保存在密封容器中,並置於室溫下。
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