奧拉替尼
Oclacitinib
Oclacitinib maleate
別名: Apoquel · PF-03394197
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Feline atopic skin syndrome (FASS, formerly nonflea-, nonfood-induced hypersensitivity dermatitis [NFNFIHD]) (extra-label)
- q12-24h
NA
必須一併考量的臨床脈絡 (2)
- ■ Oclacitinib may be administered with or without food. If your animal vomits or acts sick after a dose, try administering the medicine with some food. If there is no improvement, discontinue the medication and contact your veterinarian.
- Store tablets at room temperature (20°C-25°C [68°F-77°F]). Excursions are allowed between 15°C-40°C (59°F-104°F).
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
奧拉替尼 (Oclacitinib) 是一種標靶免疫調節與止癢藥物，在獸醫學中主要用於控制犬隻因過敏性皮膚炎引起的搔癢，以及異位性皮膚炎的長期管理。
臨床警告： 奧拉替尼會調節免疫系統，可能增加感染（如毛囊蟲症、膿皮症）的風險，或使原有的腫瘤病情惡化。由於嚴重感染的風險較高，禁忌用於12個月齡以下的犬隻。
臨床提示： 奧拉替尼能快速緩解搔癢，其起效時間通常與皮質類固醇相當（4至24小時內），但不會產生糖皮質素常見的多渴/多尿及長期代謝副作用。
作用機轉
Oclacitinib is a targeted enzyme inhibitor that specifically inhibits Janus-kinases (JAK), with a pronounced selectivity for JAK1 and, to a lesser extent, JAK3.
By blocking these enzymes, oclacitinib prevents the signal transduction of a variety of cytokines dependent on JAK1/JAK3 pathways. Most notably, it inhibits Interleukin-31 (IL-31), a key pruritogenic (itch-inducing) cytokine in dogs.
Pathway: Cytokine binds to receptor → JAK1/JAK3 activation is blocked → STAT proteins are not phosphorylated → Pro-inflammatory and pruritogenic gene transcription is halted.
安全性與警告
禁忌症
- Dogs less than 12 months of age
- Dogs weighing less than 3 kg
- Dogs with severe systemic infections
- Breeding, pregnant, or lactating dogs
- Dogs with evidence of immune suppression (e.g., hyperadrenocorticism)
- Dogs with a history of progressive malignant neoplasia
不良反應
- Gastrointestinal upset (vomiting, diarrhea, anorexia)
- Lethargy
- Increased susceptibility to infections (e.g., pyoderma, otitis, demodicosis, pneumonia)
- Transient decreases in leukocytes and serum globulins
- Potential exacerbation of neoplastic conditions
- Histiocytomas or papillomas (benign skin masses)
注意事項
Use with caution in dogs with a history of recurrent infections or neoplasia. Routine monitoring for the development of infections (skin, ears, systemic) and abnormal growths is essential.
Note: Oclacitinib is not approved for use in cats, and its safety and efficacy profile in felines is not fully established, though it is sometimes used off-label by dermatologists.
藥物交互作用
Increased risk of immunosuppression and secondary infections.
Increased risk of profound immunosuppression.
Potential for decreased vaccine efficacy or vaccine-induced illness due to immunomodulation.
監測
- Baseline CBC, serum biochemistry, and urinalysis
- Periodic bloodwork (e.g., every 6-12 months) for dogs on long-term therapy
- Monitor for new or worsening skin, ear, or systemic infections
- Monitor for the development of cutaneous or systemic neoplastic lesions
藥物動力學
半衰期
吸收
Rapidly and well absorbed following oral administration. Peak plasma concentrations (Tmax) are reached in approximately 1 hour. Absolute bioavailability is high (approx. 89%).
分佈
Low plasma protein binding (approx. 66%). Volume of distribution is roughly 0.9 L/kg.
代謝
Metabolized extensively in the liver by multiple cytochrome P450 enzymes.
排除
Clearance is primarily via hepatic metabolism, with metabolites excreted in urine and feces.
過量
Overdoses up to 3-5 times the therapeutic dose are generally well tolerated but may increase the frequency and severity of expected side effects, particularly gastrointestinal distress (vomiting, diarrhea), lethargy, and localized alopecia or skin thickening. Chronic massive overdose increases the risk of severe immunosuppression and secondary infections. Treatment is supportive and symptomatic, as there is no specific antidote.
可用產品
劑型
- 3.6 mg oral tablet
- 5.4 mg oral tablet
- 16 mg oral tablet
獸醫用
- Apoquel 3.6 mg film-coated tablets
- Apoquel 5.4 mg film-coated tablets
- Apoquel 16 mg film-coated tablets
- Apoquel chewable tablets (various strengths)
各地核准狀態
Approved for dogs 12 months of age and older.
Classified as POM-V (Prescription Only Medicine - Veterinary).
Classified as POM-V.
暫無法規資料: 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at controlled room temperature between 20°C and 25°C (68°F - 77°F). Keep in the original packaging to protect from moisture and light. Half-tablets should be placed back in the blister pack and used within 3 days.
飼主須知
奧拉替尼 (Apoquel) 是一種速效藥物，用於停止狗狗的搔癢並減輕皮膚發炎。
- 給藥方式： 可隨餐或空腹餵食。如果發生嘔吐，請嘗試與少量食物一起給予。
- 注意事項： 觀察狗狗是否有嘔吐、腹瀉或精神不振的現象。因為此藥物會改變免疫系統的反應，請密切注意是否有新的感染跡象（如耳朵感染、皮膚紅疹或咳嗽），並及時告知獸醫師。
- 腫塊與突起： 定期檢查狗狗的皮膚是否有新的腫塊或疣，並在下次就診時請獸醫師檢查。
- 禁忌症： 請勿用於1歲以下的幼犬，或懷孕/哺乳中的母犬。
- 處理方式： 拿取藥錠後請洗手。
VetSheet 藥物參考供合格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商最新仿單。