卡比馬唑
Carbimazole
Thioimidazole-derivative antithyroid drug
別名: Vidalta · Neo-Carbimazole · Carbazole · Basolest · Camazol · Carbistad · Neo Tomizol · NeoMercazole · Neo-Thyreostat · Thyrostat · Tyrazol · Neo-morphazole · Neo-Mercazole · carbimazolum
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。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Hyperthyroidism | 15 mg/animal (starting dose) or 10 mg/animal if total thyroxine <100 nmol/l. Adjust dose in 5 mg increments. | PO | q24h | Long-term | 🌍 EU |
- Hyperthyroidism: Do not break tablets. Note: There are no data on the use of the sustained-release formulation in dogs.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Hyperthyroidism | 2.5-5 mg (total dose) per cat | PO | twice daily | — | 🌎 NA |
| Hyperthyroidism | 10-15 mg total dose daily per cat in divided doses | PO | divided doses | for 1-3 weeks | 🌎 NA |
| Hyperthyroidism | Initially, give 5 mg (total dose) | PO | q8h | for 2-3 weeks | 🌎 NA |
| Hyperthyroidism (Sustained-release tablets) | 15 mg | PO | once daily | — | 🌎 NA |
| Hyperthyroidism | 15 mg/animal (starting dose) or 10 mg/animal if total thyroxine <100 nmol/l. Adjust dose in 5 mg increments. | PO | q24h | Long-term | 🌍 EU |
- Hyperthyroidism: Will produce a euthyroid state for most patients. Then adjust dosage for the patient to the lowest effective dose. Most cats will need dosing at least once daily.
- Hyperthyroidism: Then adjust. May need to increase dose in approximately 10% of cats. Most cats require 5 mg PO q12h to maintain euthyroidism.
- Hyperthyroidism (Sustained-release tablets): Give at the same time each day. Do not break or crush tabs. Adjust dose upwards or downwards within a range of 10 mg-25 mg per day in 5 mg increments depending on clinical signs and TT4. If cat requires doses less than 10 mg per day, use alternative treatment.
- Hyperthyroidism: Do not break tablets.
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。
概覽
卡比馬唑 (Carbimazole) 是一種硫咪唑衍生物的抗甲狀腺藥物，在獸醫學中主要用於控制貓甲狀腺機能亢進。
- 它是一種前驅藥 (prodrug)，在體內會迅速轉化為甲巰咪唑 (methimazole)。
- 因為它沒有甲巰咪唑的苦味，貓咪的接受度通常較高，能減少腸胃道副作用的發生率。
- 雖然在美國或加拿大未上市，但在歐洲及其他地區被廣泛使用。
- 臨床重點：由於分子量的差異，卡比馬唑需要大約兩倍於甲巰咪唑的毫克劑量，才能達到相等的血清濃度。
作用機制
Carbimazole is a prodrug that is almost entirely converted to methimazole in the body.
- Methimazole actively inhibits the enzyme thyroid peroxidase (TPO).
- Inhibition of TPO → blocks the oxidation of iodide to iodine → prevents iodine incorporation into tyrosyl residues of thyroglobulin.
- It also inhibits the coupling of iodinated tyrosyl residues (monoiodotyrosine and diiodotyrosine) → prevents formation of thyroxine (T4) and triiodothyronine (T3).
- Note: It does not affect the release or activity of pre-formed thyroid hormones already in circulation, which accounts for the 1-3 week lag time before clinical improvement is seen.
安全性與警告
禁忌症
- Hypersensitivity to carbimazole or methimazole
- Not recommended in cats intolerant to methimazole
- History of or concurrent hematologic abnormalities
- Liver disease
- Autoimmune disease
不良反應
- Vomiting
- Anorexia
- Depression
- Eosinophilia (usually transient)
- Leukopenia (usually transient)
- Lymphocytosis (usually transient)
- Self-induced excoriations (rare but serious)
- Bleeding (rare but serious)
- Hepatopathy (rare but serious)
- Thrombocytopenia (rare but serious)
- Agranulocytosis (rare but serious)
- Positive direct antiglobulin test (rare but serious)
- Acquired myasthenia gravis (rare but serious)
- Positive ANA (with chronic use)
注意事項
Hypersensitivity: Contraindicated in patients hypersensitive to carbimazole or methimazole. Cross-Reactivity: Because carbimazole is a prodrug converted into methimazole, cats who have had prior serious reactions to methimazole should receive carbimazole with great caution. Pregnancy/Nursing: High levels of methimazole cross the placenta and may induce hypothyroidism in kittens. Levels higher than those found in plasma are found in breast milk. Kittens should be placed on a milk replacer after receiving colostrum from mothers on methimazole. FDA categorizes methimazole as category D for use during pregnancy.
藥物相互作用
Potential for increased risk for hepatotoxicity; increased monitoring (LFT's) necessary
Carbimazole may decrease digoxin efficacy
Potential for decreased anticoagulant efficacy if carbimazole added
Carbimazole interferes with the uptake and efficacy of radioiodine therapy. It must be discontinued prior to treatment.
Concurrent use is not recommended as it may interfere with the dietary management of hyperthyroidism.
監測
- CBC, platelet counts (baseline and every 2-3 weeks during first 3 months)
- Serum T4 (baseline and every 2-3 weeks during first 3 months)
- Liver function tests (if indicated by clinical signs)
- ANA (if indicated by clinical signs)
- T4 at 3-6 month intervals (after stabilized)
- Other diagnostic tests as dictated by adverse effects
藥物動力學
半衰期
吸收
Rapidly absorbed from the GI tract.
分佈
In cats, the volume of distribution of methimazole is variable (0.12-0.84 L/kg). Methimazole apparently concentrates in thyroid tissue and biologic effects persist beyond measurable blood levels. Crosses the placenta and enters breast milk.
代謝
Rapidly and nearly totally converted to methimazole in vivo.
排除
Plasma elimination half-life of methimazole ranges from 2.3-10.2 hours in cats and 8-9 hours in dogs.
過量
Acute toxicity that may be seen with overdosage includes vomiting, anorexia, depression, and more serious effects such as agranulocytosis, hepatopathy, and thrombocytopenias.
Treatment: Consists of following standard protocols in handling an oral ingestion (empty stomach if not contraindicated, administer charcoal, etc.) and treating symptomatically and supportively.
可用產品
劑型
- Oral Tablets
- Oral Sustained-Release Tablets
獸醫用
- Carbimazole Oral Sustained-Release Tablets: 10 mg & 15 mg (Vidalta, Intervet-UK)
人用標示
- Carbimazole Oral Tablets: 5 mg & 20 mg (NeoCarbimazole, Carbazole, Neo Mercazole)
各地核准狀態
Approved for feline hyperthyroidism.
POM-V (Prescription Only Medicine - Veterinarian)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Unless otherwise labeled, carbimazole tablets should be stored at room temperature in well-closed containers.
飼主須知
- 用途：此藥物透過減少甲狀腺素的產生來控制貓咪的甲狀腺機能亢進。這是一種長期的控制方式，而非根治。
- 需要耐心：通常需要 1 到 3 週的時間才能看到貓咪症狀有明顯改善。
- 給藥方式：請嚴格按照處方給藥。請勿壓碎或剝半長效型錠劑（如 Vidalta）。
- 需注意的副作用：如果您的貓咪出現嘔吐、食慾不振、精神沉鬱或嚴重的臉部搔抓/發癢，請立即聯繫您的獸醫師。
- 安全須知：孕婦或哺乳期婦女在接觸此藥物時應格外小心（建議戴手套），因為藥物可能會穿過胎盤並進入母乳。
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