亮丙瑞林 (Leuprolide)
Leuprolide
Leuprolide acetate
別名: Lupron Depot · Eligard · Carcinil · Daronda · Enanton · Lucrin · Prostap · Viadur · Leuproprelin · Leuprorelinum · Abbott-43818 · TAP-144
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
經審核的 v13 劑量證據
結構化劑量計算證據Prevention of further egg laying after egg binding
須由已驗證獸醫確認
- repeat in two weeks · one repeat in two weeks
必須一併考量的臨床脈絡 (1)
- Egg binding is common in canaries and finches
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
亮丙瑞林 (Leuprolide) 是一種促性腺激素釋放激素 (GnRH) 的合成九肽類似物。在獸醫學中，主要用於內科治療雪貂的腎上腺相關內分泌病，以及抑制圈養鳥類的不當產卵或繁殖障礙。
主要臨床重點：
- 雪貂腎上腺疾病：與狗不同，雪貂的腎上腺疾病是由過量的性荷爾蒙（雄性激素/雌性激素）驅動，而非皮質醇。亮丙瑞林能有效抑制導致這些臨床症狀（如脫毛、外陰腫脹、搔癢）的荷爾蒙軸。
- 劑型：最常以長效儲庫型注射劑（微球體）給藥，可提供 1、3 或 4 個月的持續釋放。
- 成本：此藥物極為昂貴，不過調劑藥局通常會將人類用藥瓶分裝成較小、較經濟的等份供特寵使用。
- 安全性：具有高度致畸胎性，懷孕期間絕對禁用。
作用機轉
Leuprolide acts as a luteinizing hormone-releasing hormone (LHRH/GnRH) agonist.
- Initial Phase (Flare): Upon initial administration, it stimulates the pituitary gland, causing a transient surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
- Downregulation Phase: Continuous exposure via depot formulation causes profound downregulation and desensitization of GnRH receptors in the anterior pituitary.
- Suppression: This negative feedback → halts the release of LH and FSH → drastically decreases serum levels of gonadal steroids (estrogen and androgens), thereby resolving hormonally driven clinical signs.
安全性與警告
禁忌症
- Pregnancy (FDA Category X - major fetal abnormalities may result)
- Nursing/lactating animals (use with extreme caution, excretion in milk is unknown)
不良反應
- Pain or irritation at the injection site
- Dyspnea (reported in ferrets)
- Lethargy (reported in ferrets)
- Tachyphylaxis (higher dosages required over time to obtain the same effect in ferrets)
- Transient worsening of clinical signs (flare effect) shortly after initial administration
注意事項
Pregnancy Warning: Leuprolide is highly teratogenic. Pregnant women should handle this medication with extreme caution, and it must never be administered to pregnant animals.
- Tachyphylaxis: Ferrets may develop a tolerance to the drug over time, necessitating dose escalations.
- Laboratory Interference: Diagnostic tests measuring pituitary gonadotrophic and gonadal functions may be misleading during therapy and for several months after discontinuation.
- Handling: Depot formulations contain microspheres. Freezing reconstituted depot suspensions is controversial; the manufacturer warns against freezing as it may destroy the microspheres, though some compounding pharmacies do freeze individual aliquots.
監測
- Ferrets: Resolution of clinical signs (decreased vulvar swelling, reduced pruritus, cessation of undesirable sexual behaviors/aggression, and increased hair regrowth)
- Birds: Decreased egg-laying behavior and physical reproductive activity
- Injection site for signs of pain, irritation, or necrosis
藥物動力學
吸收
Depot forms provide slow, sustained release of the drug from the injection site.
分佈
No specific veterinary data available.
代謝
No specific veterinary data available. In humans, it is degraded by peptidases.
排除
No specific veterinary data available.
過量
Because of its high expense and the method of dosing (usually administered by the veterinarian in-clinic), an acute overdose is highly unlikely. Studies in laboratory animals at massive dosages of up to 5 grams/kg IM produced no untoward effects, suggesting a wide margin of safety for acute exposure.
可用產品
劑型
- Injection solution (5 mg/mL)
- Depot injection (microspheres for suspension)
- Powder for injection (lyophilized)
人用標示
- Leuprolide Acetate Injection: 5 mg/mL in 2.8 mL multi-dose vials (Lupron)
- Leuprolide Acetate Injection (Eligard): 22.5 mg, 30 mg, & 45 mg in single-use kits
- Leuprolide Powder for Injection (Eligard): 7.5 mg in single-use kits
- Leuprolide Acetate Microspheres for Injection (Lupron Depot): 3.75 mg, 7.5 mg, 11.25 mg, 15 mg, 22.5 mg, & 30 mg in single dose kits
各地核准狀態
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儲存與穩定性
The standard injection should be stored below room temperature (<78°F); do not freeze and protect from light. The depot form may be stored at room temperature. After reconstituting, the suspension is stable for 24 hours, but immediate use is recommended as it contains no preservatives. Freezing the depot form is controversial; the manufacturer advises against it as it may destroy the microspheres.
飼主須知
什麼是亮丙瑞林 (Leuprolide)？ 亮丙瑞林是一種荷爾蒙調節藥物，主要用於特殊寵物。在雪貂中，它透過阻止性荷爾蒙的過度分泌來治療腎上腺疾病。在鳥類中，它被用來阻止慢性、不健康的產卵行為。
寵物主人重要須知：
- 費用與承諾：這種藥物非常昂貴。雪貂腎上腺疾病的治療通常是終身的，需要嚴格遵守注射時間表（例如每 1、3 或 4 個月一次）。
- 「潮紅 (Flare)」效應：首次給藥時，藥物會短暫刺激荷爾蒙釋放，然後才將其關閉。您可能會注意到寵物的症狀（如搔癢或性行為）在開始好轉前幾天會稍微惡化。這是正常現象。
- 安全性：在特殊寵物身上的長期安全性仍在研究中，但通常耐受性良好。有些雪貂可能會在注射部位感到疼痛或出現輕微的嗜睡。
- 懷孕警告：此藥物會導致嚴重的出生缺陷。絕對不能用於懷孕的動物，孕婦也應避免接觸此藥物。
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