培高利特
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。
作用機制: 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.
各物種劑量
- 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
- Equine 'Cushing's-like' Disease [pituitary pars intermedia dysfunction (PPID)] · 1.7-5.5 micrograms/kg · PO · Varies · 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)] · 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 · 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。
給藥途徑
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)
藥物相互作用
- Dopamine antagonists (e.g., phenothiazines) · May decrease the effects of pergolide
- Metoclopramide · 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
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.
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。