培高利特
Pergolide
Pergolide mesylate
別名: Permax · Celance · Nopar · Parkotil · Parlide · Pharken · LY-127809 · pergolide mesilate · pergolidi mesilas
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
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Equine 'Cushing's-like' Disease [pituitary pars intermedia dysfunction (PPID)] | Initial dose of 1 mg (total dose) per day for horses and ponies with PPID. If the horse owner is willing to administer half the dose twice daily, this may be preferable on the basis of recent pharmacokinetic data. If anorexia or temporary dullness develop, treatment should be halted for 2 days or until appetite improves, and then restarted at 0.25 mg per day for 2 days, 0.5 mg per day for 2 days, and 0.75 mg per day for 2 days. | PO | q24h or divided q12h | — | 🌎 NA |
| Equine 'Cushing's-like' Disease [pituitary pars intermedia dysfunction (PPID)] | 1.7-5.5 micrograms/kg | PO | Varies | — | 🌎 NA |
| Equine 'Cushing's-like' Disease [pituitary pars intermedia dysfunction (PPID)] | 0.002 mg/kg. If no improvement is noted within 8-12 weeks, the daily dose can be increased by 0.002 mg/kg monthly up to a total dose of 0.006 mg/kg (3 mg/day for a 500 kg horse). If only a limited response is observed with 0.006 mg/kg dose, addition of cyproheptadine (0.5 mg/kg PO q12h) to pergolide therapy is recommended. | PO | q24h | — | 🌎 NA |
- Equine 'Cushing's-like' Disease [pituitary pars intermedia dysfunction (PPID)]: Dose varies considerably. The higher doses are used in the more advanced cases or those refractory to treatment at a lower dose.
- Equine 'Cushing's-like' Disease [pituitary pars intermedia dysfunction (PPID)]: Usually, only transient anorexia is recognized during the initial week of treatment and can be overcome in time or by cutting the dose in half for 2-4 days.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
培高利特（Pergolide）是一種麥角衍生物類多巴胺促效劑，在獸醫學中主要作為治療馬匹腦下垂體中葉功能障礙（PPID，俗稱馬庫興氏症）的黃金標準藥物。
- 臨床重要性：它是控制馬匹 PPID 臨床症狀（如多毛症/換毛延遲、嗜睡、肌肉萎縮和蹄葉炎）最有效的藥物療法。
- 取得方式：由於人類製劑因心瓣膜疾病風險已於 2007 年退出美國市場，目前獸醫臨床上專門透過獸醫調劑藥局（compounding pharmacies）取得。
- 耐受性：馬匹對此藥物的耐受性通常非常好，儘管在治療初期可能會出現短暫的食慾不振。
作用機轉
Pergolide acts as a potent, long-acting agonist at D1 and D2 dopamine receptors (estimated to be 10-1000 times more potent than bromocriptine).
- Mechanism in PPID: In healthy horses, the hypothalamus releases dopamine, which tonically inhibits the pituitary pars intermedia. In horses with PPID, there is a neurodegenerative loss of these dopaminergic neurons.
- Pathway: Pergolide replaces this lost dopamine tone → binds to D2 receptors on melanotropes in the pars intermedia → inhibits the hypersecretion of pro-opiomelanocortin (POMC) peptides (including ACTH, α-MSH, and CLIP).
- This reduction in POMC peptides normalizes endocrine function and alleviates the clinical signs associated with PPID.
安全性與警告
禁忌症
- Hypersensitivity to pergolide or other ergot derivatives
不良反應
- Anorexia/decreased appetite (up to 10% of horses during the first week)
- Colic (rare)
- Diarrhea (rare)
- Lethargy (dogs)
- Vomiting (dogs)
- Hypertension (dogs)
- Ptosis (dogs)
注意事項
Safety in pregnant horses has not been established. May interfere with lactation due to its ergot-derivative nature. Compounded aqueous suspensions are highly unstable; they must be stored in dark containers, refrigerated, and discarded after 30 days or if any color change occurs.
藥物交互作用
May decrease the effects of pergolide
May decrease the effects of pergolide
監測
- Dexamethasone suppression test (baseline and at 4-8 weeks post pergolide therapy initiation, repeat in 4-8 weeks if dosage is adjusted)
- Blood glucose (baseline, and if abnormal repeat as per dexamethasone suppression test)
- Clinical signs (hair coat, weight, PU/PD, etc.)
- Periodic CBC and clinical chemistry panel
藥物動力學
半衰期
吸收
Horses: Rapidly absorbed following oral administration, with Tmax within 1 hour. Humans: Orally absorbed (estimated 60% bioavailable).
分佈
Horses: Appears to be rapidly and widely distributed. Humans: 90% bound to plasma proteins.
代謝
Humans: At least 10 different metabolites have been identified, some of which are active.
排除
Humans: Principle route of elimination is via the kidneys.
過量
Limited information is available on pergolide overdoses.
- Potential effects: GI disturbances, CNS effects, seizures, and hypotension.
- Dogs: Accidental ingestion has resulted in vomiting, lethargy, hypertension, and ptosis.
- Treatment: Care is primarily supportive. Phenothiazines (dopamine antagonists) may be used to decrease CNS stimulation effects.
可用產品
劑型
- Compounded oral suspension
- Compounded capsules
- Compounded tablets
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
Store pergolide tablets in tight containers at room temperature (25°C; 77°F); excursions permitted to 15-30°C (59-86°F). Compounded pergolide formulations in aqueous vehicles should be stored in dark containers, protected from light, and refrigerated. Do not use more than 30 days after compounding. Formulations that have undergone a color change should be considered unstable and discarded.
飼主須知
重要提示：培高利特能控制馬庫興氏症（PPID）但無法根治。通常需要終身服藥。
- 需要耐心：可能需要數週到數月的時間，才能看到馬匹毛髮、活力和體重的明顯改善。
- 食慾變化：部分馬匹在治療第一週可能會食慾下降。若發生此情況請聯繫獸醫師，暫時降低劑量通常能解決問題。
- 藥物保存：若使用調劑的液體懸浮液，請冷藏並避光保存。若超過30天或藥水變色請丟棄，因為該藥物在水中容易快速降解。
- 全面照護：除了藥物治療，適當的營養、定期的蹄部護理和體重管理對於成功控制此疾病也至關重要。
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