酮康唑
Ketoconazole
Ketoconazolum
別名: Nizoral · Fungiconazole · ketoconazolum · R-41400
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 |
|---|---|---|---|---|---|
| Coccidioidomycosis (systemic form) | 5-10 mg/kg PO twice daily | PO | q12h | Minimum of 3-6 months | 🌎 NA |
| Coccidioidomycosis (CNS form) | 15-20 mg/kg PO twice daily | PO | q12h | Minimum of 3-6 months | 🌎 NA |
| Coccidioidomycosis (bony lesions or relapses) | 5 mg/kg PO every other day | PO | q48h | Lifelong | 🌎 NA |
| Coccidioidomycosis | 10-30 mg/kg PO divided twice a day | PO | q12h | 6-12 months | 🌎 NA |
| Blastomycosis | 10 mg/kg PO twice daily (15-20 mg/kg PO twice daily if CNS involvement) | PO | q12h | At least 3 months | 🌎 NA |
| Blastomycosis | 20 mg/kg/day PO once daily or divided twice daily; 40 mg/kg divided twice daily for ocular or CNS involvement | PO | q24h or q12h | At least 2-3 months or until remission | 🌎 NA |
| Histoplasmosis | 10 mg/kg PO once a day or twice a day | PO | q24h or q12h | At least 3 months | 🌎 NA |
| Histoplasmosis | 10-20 mg/day PO once daily or divided twice daily | PO | q24h or q12h | At least 2-3 months or until remission | 🌎 NA |
| Aspergillosis | 20 mg/kg PO | PO | Not specified | At least 6 weeks | 🌎 NA |
| Nasal aspergillosis | 10 mg/kg PO once daily (q24h) or 5 mg/kg PO q12h | PO | q24h or q12h | Many weeks; continue 1 month beyond last detection | 🌎 NA |
| Cryptococcosis | 10 mg/kg PO once daily or divided twice daily | PO | q24h or q12h | Maintenance | 🌎 NA |
| Fungal myocarditis | 10 mg/kg PO three times daily | PO | q8h | — | 🌎 NA |
| Candidiasis | 10 mg/kg PO once daily (q24h) or 5 mg/kg PO q12h | PO | q24h or q12h | Many weeks; continue 1 month beyond last detection | 🌎 NA |
| Sporotrichosis | 15 mg/kg PO q12h | PO | q12h | Many weeks; continue 1 month beyond last detection | 🌎 NA |
| Malassezia dermatitis (severe) | 5 mg/kg PO once daily to 10 mg/kg twice daily | PO | q24h to q12h | Until clinical signs abate and no organisms seen | 🌎 NA |
| Malassezia dermatitis | 5-10 mg/kg PO twice a day | PO | q12h | 30 days | 🌎 NA |
| Malassezia dermatitis | 5-10 mg/kg PO daily for 10 days, then every other day for an additional 10 days | PO | q24h then q48h | 20 days | 🌎 NA |
| Malassezia dermatitis | 5 mg/kg twice daily for 21-30 days, may increase to 10 mg/kg PO twice daily if poor response | PO | q12h | 21-30 days | 🌎 NA |
| Malassezia dermatitis | 2.5-10 mg/kg PO once daily (q24h) for 7-14 days; once a good response is seen taper to every other day (q48h) | PO | q24h then q48h | Until complete remission | 🌎 NA |
| Hyperadrenocorticism | 5-10 mg/kg PO twice daily initially; may increase to 15 mg/kg PO twice daily | PO | q12h | Long-term | 🌎 NA |
| Hyperadrenocorticism | 5 mg/kg q12h for 5-7 days, increase to 10 mg/kg q12h for 10-14 days; many require 15-20 mg/kg q12h | PO | q12h | Long-term | 🌎 NA |
| Hyperadrenocorticism (palliative) | 15 mg/kg PO q12h | PO | q12h | Long-term | 🌎 NA |
| Reduce cyclosporine dosage | 5-10 mg/kg PO per day | PO | q24h | Concurrent with cyclosporine | 🌎 NA |
| Perianal fistula (with cyclosporine) | 7.5 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
| Atopic dermatitis (with cyclosporine) | 5 mg/kg/day | PO | q24h | — | 🌎 NA |
| IMHA (with cyclosporine) | 10 mg/kg/day | PO | q24h | — | 🌎 NA |
- Blastomycosis: Used with amphotericin B
- Blastomycosis: Used with amphotericin B
- Histoplasmosis: Treat at least 30 days after complete resolution. Maintenance 5 mg/kg PO every other day indefinitely if relapse.
- Histoplasmosis: Used with amphotericin B
- Aspergillosis: May require long-term/maintenance therapy
- Nasal aspergillosis: Itraconazole somewhat more effective
- Cryptococcosis: Used with amphotericin B
- Malassezia dermatitis: Often used with therapeutic shampoos
- Hyperadrenocorticism: Monitor with ACTH stimulation test
- Perianal fistula (with cyclosporine): Given with cyclosporine 0.5-0.75 mg PO twice daily
- Atopic dermatitis (with cyclosporine): Given with cyclosporine 2.5 mg/kg/day
- IMHA (with cyclosporine): Allows reduction of cyclosporine dose
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Coccidioidomycosis | 10-30 mg/kg PO divided twice a day | PO | q12h | 6-12 months | 🌎 NA |
| Coccidioidomycosis | 50 mg per cat PO once daily; or 25-75 mg per cat q12-48h | PO | q24h or q12-48h | 9-12 months on average | 🌎 NA |
| Blastomycosis | 10 mg/kg q12h PO | PO | q12h | At least 60 days | 🌎 NA |
| Cryptococcosis | 10 mg/kg twice daily | PO | q12h | — | 🌎 NA |
| Aspergillosis | 10 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Dermatophytosis | 10 mg/kg PO once daily with an acidic meal | PO | q24h | Prolonged; 2 weeks beyond clinical cure and negative cultures | 🌎 NA |
| Sporotrichosis | 5-10 mg/kg PO q12-24h | PO | q12-24h | 2-4 months on average | 🌎 NA |
- Coccidioidomycosis: Use in cats is controversial
- Blastomycosis: Used with amphotericin B
- Cryptococcosis: Can produce anorexia and debility at this dosage
- Dermatophytosis: Reserved for when griseofulvin ineffective or not tolerated
小型哺乳類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections (Rabbits) | 10-40 mg/kg per day PO | PO | q24h | 14 days | 🌎 NA |
| Systemic mycoses/candidiasis (Hamsters, Gerbils, Mice, Rats, Guinea pigs, Chinchillas) | 10-40 mg/kg per day PO | PO | q24h | 14 days | 🌎 NA |
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Severe refractory candidiasis in Psittacines | 5-10 mg/kg as a gavage twice daily | PO (gavage) | q12h | 14 days | 🌎 NA |
| Susceptible fungal infections (most species) | 200 mg/L | PO (water) | Continuous | 7-14 days | 🌎 NA |
| Susceptible fungal infections (most species) | 10-20 mg/kg | PO (feed) | Daily | 7-14 days | 🌎 NA |
| Susceptible fungal infections (Moluccan Cockatoos) | 20-30 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
| Susceptible fungal infections (Ratites) | 5-10 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
- Severe refractory candidiasis in Psittacines: Dissolve in 0.2 mL 1 N HCl and add 0.8 mL water
- Susceptible fungal infections (most species): Dissolve in acid prior to adding to water
- Susceptible fungal infections (most species): Add to favorite food or mash
爬蟲類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections (most species) | 15-30 mg/kg PO once daily | PO | q24h | 2-4 weeks | 🌎 NA |
| Fungal shell diseases in turtles/tortoises | 25 mg/kg PO once a day | PO | q24h | 2-4 weeks | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible yeasts and Aspergillus spp | 5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Scopulariopsis pneumonia | 30 mg/kg q12h | NG tube | q12h | — | 🌎 NA |
- Susceptible yeasts and Aspergillus spp: Using commercial oral solution
- Scopulariopsis pneumonia: Administered via NG tube mixed with 0.2 Normal hydrochloric acid
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
酮康唑（Ketoconazole）是第一代咪唑類抗黴菌藥物。雖然由於安全性與療效的考量，它已在很大程度上被較新的三唑類藥物（如伊曲康唑和氟康唑）所取代，但對於治療某些全身性黴菌感染（如芽生菌病、組織胞漿菌病、球黴菌病及馬拉色菌性皮膚炎），它仍是一種具成本效益的選擇。
臨床要點： 除了抗黴菌特性外，酮康唑也是哺乳動物細胞色素 P450 酵素的強效抑制劑。獸醫學中常利用此獨特特性進行仿單標示外使用（Off-label use）：
- 節省藥物用量： 藉由抑制肝臟代謝，來降低昂貴藥物（如環孢素）的所需劑量與成本。
- 內分泌治療： 藉由可逆性抑制腎上腺類固醇生成，作為犬腎上腺皮質機能亢進（庫興氏症）的內科管理選項。
注意： 由於貓發生胃腸道與肝臟毒性的風險較高，酮康唑在貓的使用極具爭議；許多臨床獸醫師更傾向於在貓隻身上使用伊曲康唑。
作用機制
Antifungal Action: Ketoconazole inhibits lanosterol 14α-demethylase, a fungal cytochrome P450 enzyme → blocks the conversion of lanosterol to ergosterol → depletion of ergosterol in the fungal cell membrane → accumulation of toxic intermediate sterols → increased cellular membrane permeability and cell death. It is primarily fungistatic but can be fungicidal at high concentrations or prolonged exposures.
Endocrine/Metabolic Action: It reversibly inhibits mammalian cytochrome P450 enzymes (specifically CYP11A1 and CYP17) → blocks the synthesis of adrenal and gonadal steroids → decreases cortisol and testosterone production.
Immunomodulatory Action: Inhibits 5-lipooxygenase, providing mild anti-inflammatory effects, and suppresses T-lymphocyte proliferation.
安全性與警告
禁忌症
- Known hypersensitivity to ketoconazole
- Controversial/Contraindicated in cats (due to toxicity risks)
- Concurrent use with cisapride or ivermectin (in dogs)
- Hepatic insufficiency
- Pregnancy (due to possible teratogenic effects)
不良反應
- Anorexia (most common, especially in cats)
- Vomiting
- Diarrhea
- Hepatic toxicity (cholangiohepatitis, increased liver enzymes)
- Thrombocytopenia (rare)
- Reversible lightening of haircoat
- Transient suppression of gonadal and adrenal steroid synthesis
- Infertility in male dogs (reversible)
- Hepatotoxicity
- Alterations in hair-coat colour
- Thrombocytopenia (at high doses)
- Adrenal insufficiency (at high doses)
- Cataract development (in dogs)
- Teratogenic effects
注意事項
Use with caution in patients with hepatic disease or thrombocytopenia. Ketoconazole is a known teratogen and embryotoxin; weigh risks vs. benefits in pregnant animals. It may cause reversible infertility in male dogs by decreasing testosterone synthesis. Dogs undergoing high-dose antifungal therapy may need additional glucocorticoid support during periods of acute stress due to adrenal suppression.
藥物相互作用
May produce a disulfiram-like reaction (vomiting)
May reduce oral absorption of ketoconazole; administer at least 1 hour before or 2 hours after
Ketoconazole may reduce metabolism and increase adverse effects
Ketoconazole may increase levels
Plasma concentrations may be elevated
Ketoconazole may increase levels
Ketoconazole may increase levels
Ketoconazole may increase cisapride levels and possibility for toxicity; use together contraindicated
Ketoconazole may inhibit metabolism; potential for increased adverse effects
Ketoconazole may inhibit metabolism; potential for increased toxicity
Increased cyclosporine levels (often used therapeutically to reduce cyclosporine dose)
Ketoconazole may increase digoxin levels
Ketoconazole may increase fentanyl or alfentanil levels
Increased gastric pH may reduce ketoconazole absorption
Should be used cautiously together due to additive hepatotoxicity risk
May affect ketoconazole levels; concomitant use not recommended
Ketoconazole may increase risk for neurotoxicity; should never be used together in dogs
May increase ketoconazole concentrations
Not recommended together; adrenolytic effects of mitotane may be inhibited by ketoconazole
May decrease ketoconazole levels
Increased gastric pH may reduce ketoconazole absorption
Ketoconazole may increase quinidine levels
May decrease ketoconazole levels; ketoconazole may increase rifampin levels
May reduce absorption of ketoconazole
Ketoconazole may increase levels; hypoglycemia possible
Ketoconazole may decrease serum theophylline concentrations; monitor levels
Ketoconazole may inhibit vinca alkaloid metabolism and increase levels
Ketoconazole may cause increased prothrombin times
Ketoconazole increases blood levels of ciclosporin (used therapeutically to reduce ciclosporin dose requirements)
Used synergistically in systemic fungal disease, allowing for a reduced dose of amphotericin B
Increases gastric pH, which impairs the absorption of ketoconazole; stagger dosing
Increases gastric pH, which impairs the absorption of ketoconazole; stagger dosing
Increases gastric pH, which impairs the absorption of ketoconazole; stagger dosing
Ketoconazole extends the activity of methylprednisolone
Inhibits the metabolism of antihistamines (extrapolated from human data)
Inhibits the metabolism of oral hypoglycaemics (extrapolated from human data)
Inhibits the metabolism of antiepileptics (extrapolated from human data)
監測
- Liver enzymes with chronic therapy (at least every 1-2 months)
- CBC with platelets
- Clinical efficacy
- Adverse effects (GI signs, jaundice)
- Liver function tests (routine monitoring recommended)
- Platelet count (if high doses are used)
- Adrenal function/clinical signs of hypoadrenocorticism
藥物動力學
半衰期
吸收
Highly variable oral bioavailability in dogs (4-89%). Absorption is enhanced in an acidic environment and may be increased with food. Poor oral absorption of tablets in horses, but increases to 23% if given with hydrochloric acid, and 60% with oral solution.
分佈
Distributed into bile, cerumen, saliva, urine, synovial fluid, and CSF (CSF levels <10% of serum). High levels in liver, adrenals, and pituitary gland. 84-99% bound to plasma proteins. Crosses the placenta and is found in milk.
代謝
Extensively metabolized by the liver into several inactive metabolites.
排除
Metabolites are excreted primarily into the feces via the bile. About 13% is excreted into the urine (only 2-4% unchanged).
過量
No reports of acute toxicity associated with overdosage were located. The oral LD50 in dogs is >500 mg/kg. In the event of an acute overdose, employ supportive measures, including gastric lavage with sodium bicarbonate.
可用產品
劑型
- Oral tablets
- Oral suspension (compounded)
- Topical preparations
- 200 mg oral tablet
獸醫用
- None for systemic use
- Fungiconazole 200 mg tablet
人用標示
- Ketoconazole Tablets: 200 mg (scored)
各地核准狀態
POM-V classification
POM-V (Prescription Only Medicine - Veterinarian)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store tablets at room temperature in well-closed containers. Compounded oral suspensions (20 mg/mL) retain >95% potency for 60 days when stored at 5°C or 25°C and protected from light.
飼主須知
- 給藥方式： 請將此藥物與食物一起餵食，以增加吸收並減少胃部不適。如果您的寵物出現嘔吐或食慾不振，將每日劑量分次餵食可能會有所幫助。
- 副作用： 請留意寵物是否有食慾不振、嘔吐或腹瀉的情況。如果出現這些症狀，請聯繫您的獸醫師。在貓咪身上，這些副作用更為常見。
- 毛髮變化： 在治療期間，您可能會注意到寵物的毛色變淺，這是可逆的現象。
- 療程承諾： 黴菌感染通常需要連續數個月的治療。即使您的寵物看起來已經好轉，也不要提早停藥，因為感染很容易復發。
- 警告： 請告知獸醫師您的寵物正在服用的所有其他藥物，因為酮康唑會與許多藥物產生交互作用。
VetSheet 藥物參考供持牌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方最新藥品說明書。