カベルゴリン
Cabergoline
1-[(6-allylergolin-8β-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
別名: Dostinex · Galastop · Cabasar · Actualene · Sostilar · Kelactin · FCE-21336 · cabergolina · Cabergolinum
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
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Estrus induction | 5 micrograms/kg PO once daily induces fertile proestrus in 4-25 days. | PO | q24h | 4-25 days | 🌎 NA |
| Estrus induction | 5 micrograms/kg PO once daily until an induced proestrus is pronounced for 2 days or until onset of estrus | PO | q24h | Until proestrus is pronounced for 2 days or onset of estrus | 🌎 NA |
| Estrus induction | 0.6 micrograms/kg PO once daily. Make a 10 micrograms per mL solution by dissolving commercial tablets in warm distilled water (One 0.5 mg tablet (500 micrograms) per 50 mL of distilled water.) Give the appropriate dose for the patient within 15 minutes of preparation and discard the remaining solution. Continue until day 2 after the onset of the first signs of proestrus, or until day 42 without signs of proestrus. | PO | q24h | Until day 2 after onset of proestrus, or up to 42 days | 🌎 NA |
| Pseudocyesis (pseudopregnancy) | 5 micrograms/kg once a day PO for 5-10 days. | PO | q24h | 5-10 days | 🌎 NA |
| Pseudocyesis | 5 micrograms/kg once a day or every other day SC | SC | q24h or q48h | Not specified | 🌎 NA |
| Pseudocyesis | 5 micrograms/kg PO once daily for 4-5 days; occasional failures can be handled by repeating treatment and extending duration to 8-10 days. | PO | q24h | 4-5 days (up to 8-10 days) | 🌎 NA |
| Adjunctive treatment of mastitis after puppies weaned | 5 micrograms/kg PO daily. | PO | q24h | Not specified | 🌎 NA |
| Pre-treat mammary tumors prior to surgery (during diestrous period) | 5 micrograms/kg PO 5-7 days before surgery. | PO | q24h | 5-7 days | 🌎 NA |
| Pregnancy termination | Administer after day 40: 5 micrograms/kg PO for 5 days | PO | q24h | 5 days | 🌎 NA |
| Pregnancy termination | Between days 35-45: Cabergoline 5 micrograms/kg PO once daily for 7 days in food and cloprostenol at 1 microgram/kg SC (after a tenfold dilution with physiologic saline) on days 1 and 3 given at least 8 hours after food. If pregnancy not terminated by day 8, cabergoline continued (at same dose) until day 12. | PO | q24h | 7-12 days | 🌎 NA |
| Pituitary-dependent hyperadrenocorticism (Cushing's Disease) | 0.1 mg/kg PO every 3 days. | PO | q72h | Not specified | 🌎 NA |
| Pseudopregnancy / Suppression of lactation | 5 μg/kg | PO | sid | 4-6 days | 🌍 EU |
| Estrus induction | 5 μg/kg | PO | sid | Until proestrus begins (up to 40 days) | 🌍 EU |
- Estrus induction: 81% (22 of 27) of dogs treated at this low dose showed proestrus between days 4 and 48.
- Pseudocyesis: Likely needs to be compounded.
- Pseudocyesis: Additional protocols for treatment failures include combining cabergoline with metergoline (500 micrograms/kg PO twice daily), or cabergoline with bromocriptine (10-30 micrograms/kg PO twice daily).
- Pregnancy termination: Approximately 50% effective.
- Pituitary-dependent hyperadrenocorticism (Cushing's Disease): Effective in 70% of dogs treated. Dogs with tumor sizes greater than 5 mm did not respond.
- Pseudopregnancy / Suppression of lactation: Administer directly into the mouth or mixed with food.
- Estrus induction: Off-label use.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Pregnancy termination | At 30 days post-coitus, cabergoline at 5 micrograms/kg PO q24h and cloprostenol 5 micrograms/kg SC q48h in 7-13 days was used to induce abortion. | PO | q24h | 7-13 days | 🌎 NA |
| Reduce prolactin production in queens | 5 micrograms/kg PO once daily | PO | q24h | Not specified | 🌎 NA |
| Pre-treat mammary tumors prior to surgery (during diestrous period) | 5 micrograms/kg PO 5-7 days before surgery. | PO | q24h | 5-7 days | 🌎 NA |
| Suppression of lactation / Pseudopregnancy | 5 μg/kg | PO | sid | 4-6 days | 🌍 EU |
- Suppression of lactation / Pseudopregnancy: Off-label in some regions, but widely used.
鳥
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Persistent egg laying in psittacines (in combination with removal of males, altered light cycle) | Initially 10-20 micrograms/kg PO daily; higher dosages were also used. | PO | q24h | Not specified | 🌎 NA |
- Persistent egg laying in psittacines (in combination with removal of males, altered light cycle): Further work needed to determine the exact dose rate.
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
カベルゴリンは、主に強力なプロラクチン低下作用を目的として獣医療で使用される合成麦角誘導体です。
- 主な適応症： 犬および猫の偽妊娠の治療、発情誘起/同期化、妊娠中絶、および乳腺炎の管理。
- 臨床的利点： ブロモクリプチンなどの古いドパミン作動薬と比較して、カベルゴリンは忍容性がはるかに高く、受容体特異性が高く、作用時間が長く、嘔吐の発生率が著しく低いです。
- 適応外使用： 犬の下垂体依存性副腎皮質機能亢進症（クッシング症候群）やオウムの持続的産卵の治療において、一定の有効性が示されています。
- コストの考慮： 特に大型犬では非常に高価になる可能性がありますが、現在ではジェネリック錠剤が利用可能です。正確な獣医用量を得るために、通常は薬剤師による調剤が必要です。
作用機序
Cabergoline is a highly specific, long-acting dopamine D2 receptor agonist.
- Mechanism: It binds with high affinity to D2 receptors on lactotroph cells in the anterior pituitary gland.
- Pathway: D2 receptor activation → inhibition of adenylyl cyclase → decreased intracellular cAMP → direct suppression of prolactin synthesis and secretion.
- Reproductive Impact: Because prolactin is luteotropic in dogs and cats (it maintains the corpus luteum during the second half of pregnancy), suppressing prolactin leads to a drop in progesterone. This mechanism is responsible for its ability to terminate pregnancy, resolve pseudopregnancy, and induce estrus.
安全性・警告
禁忌
- Pregnancy (unless abortion is desired)
- Hypersensitivity to ergot derivatives
- Uncontrolled hypertension (in humans)
- Nursing mothers
有害事象
- Vomiting (infrequent, alleviated by food)
- Coat color changes (in dogs treated >14 days)
- Postural hypotension (reported in humans)
- Dizziness (reported in humans)
- Headache (reported in humans)
- Nausea (reported in humans)
注意事項
Warning: Will cause spontaneous abortion in pregnant animals. Do not use unless pregnancy termination is the specific goal.
- Hepatic Impairment: Patients with significantly impaired liver function should receive the drug with caution, and possibly at a lower dosage.
- Estrus Induction: When using to induce estrus, it is recommended to wait at least 4 months after the prior cycle to allow the uterus to recover.
- Nursing: Because cabergoline suppresses prolactin, it should not be used in nursing mothers.
医薬品相互作用
Concomitant use may cause additive hypotension due to cabergoline's hypotensive effects.
Use with cabergoline may reduce the efficacy of both drugs and should be avoided.
Use of cabergoline with dopamine (D2) antagonists may reduce the efficacy of both drugs and should be avoided.
Antagonizes the therapeutic effect of cabergoline
May antagonize cabergoline effects due to dopamine receptor blockade
Additive hypotensive effects
監視
- Clinical efficacy (resolution of pseudopregnancy, estrus induction, etc.)
- Adverse effects (vomiting, behavioral changes)
薬物動態
半減期
吸収
Absorbed after oral dosing but absolute bioavailability is not known. Food does not appear to significantly alter absorption.
分布
Moderately bound to plasma proteins (≈50%).
代謝
Extensively metabolized in the liver via hydrolysis.
消失
Metabolites and about 4% of unchanged drug are excreted into the urine. Renal dysfunction does not appear to significantly alter elimination characteristics.
過剰投与
Overdose information is not available for dogs or cats, and remains very limited for humans.
- Potential Signs: It is postulated that cabergoline overdoses could cause severe hypotension, nasal congestion, syncope, or hallucinations.
- Treatment: Treatment is basically supportive and primarily focuses on supporting cardiovascular function and blood pressure.
製品
製剤
- Oral tablets
- Oral liquid
- Injection
動物用医薬品
- Galastop® 50 micrograms/mL oral liquid (miglyol base) (Europe)
- Galastop® Injectable (available in some countries)
ヒト用医薬品
- Cabergoline Oral Tablets: 0.5 mg (500 micrograms) (generic, Rx)
- Dostinex®
規制ステータス
Approved for treatment of false pregnancy in bitches.
POM-V classification.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Commercially available tablets should be stored at controlled room temperature (20°-25°C; 68°-77°F). The veterinary oral liquid product Galastop® should be stored below 25°C and protected from light. Do not refrigerate. Once opened, it should be used within 28 days. Cabergoline is unstable in aqueous suspensions; if compounded into a liquid not for immediate use, it should be in a lipid-based product. Fresh aqueous solutions for immediate use are stable.
飼主向け情報
- 目的： 獣医師は、偽妊娠の治療、発情の誘起、またはその他の生殖関連疾患の管理のためにカベルゴリンを処方しました。
- 投与方法： 胃の不調を防ぐため、この薬は食事と一緒に与えてください。
- 副作用： 一般的に忍容性は良好ですが、軽度の嘔吐が起こる場合があります。嘔吐がひどい場合や続く場合は、獣医師に連絡してください。
- 警告： 獣医師が妊娠中絶の目的で特別に処方した場合を除き、妊娠中のペットには絶対に与えないでください。流産を引き起こします。授乳中のペットにも与えないでください。
- 注意： 犬がこの薬を14日以上服用している場合、被毛の色が一時的に変化することがあります。
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