ペルゴリド
Pergolide
Pergolide mesylate
別名: Permax · Celance · Nopar · Parkotil · Parlide · Pharken · LY-127809 · pergolide mesilate · pergolidi mesilas
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
ペルゴリドは麦角由来のドパミン作動薬であり、獣医療においては主に馬の下垂体中葉機能不全（PPID、通称：馬クッシング症候群）の標準治療薬として使用されます。
- 臨床的重要性：多毛症（換毛遅延/長い被毛）、無気力、筋肉の萎縮、蹄葉炎など、馬のPPIDの臨床症状を管理するための最も効果的な内科的治療法です。
- 入手方法：ヒト用製剤は心臓弁膜症のリスクにより2007年に米国市場から撤退しているため、現在は動物用調剤薬局（compounding pharmacies）を通じてのみ入手可能です。
- 忍容性：馬における忍容性は一般的に非常に良好ですが、治療開始時に一過性の食欲不振が見られることがあります。
作用機序
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・警告
禁忌
- Hypersensitivity to pergolide or other ergot derivatives
有害事象
- 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.
医薬品相互作用
May decrease the effects of pergolide
May decrease the effects of pergolide
監視
- 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
薬物動態
半減期
吸収
Horses: Rapidly absorbed following oral administration, with Tmax within 1 hour. Humans: Orally absorbed (estimated 60% bioavailable).
分布
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.
消失
Humans: Principle route of elimination is via the kidneys.
過剰投与
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.
製品
製剤
- Compounded oral suspension
- Compounded capsules
- Compounded tablets
規制ステータス
規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
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.
飼主向け情報
重要：ペルゴリドは馬クッシング症候群（PPID）を管理するものであり、完治させるものではありません。通常、生涯にわたる投薬が必要です。
- 忍耐が必要です：被毛、活力、体重の明らかな改善が見られるまで、数週間から数ヶ月かかることがあります。
- 食欲の変化：治療の最初の1週間は食欲が低下する馬もいます。その場合は獣医師に相談してください。一時的な減量で解決することが多いです。
- 保管方法：調剤された液剤を使用する場合は、冷蔵庫で遮光保存してください。水中で急速に劣化するため、30日経過した場合や変色した場合は破棄してください。
- 総合的なケア：投薬に加えて、適切な栄養管理、定期的な装蹄、体重管理がこの病気の治療を成功させるために非常に重要です。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。