伊曲康唑
Itraconazole
別名: Sporanox · Intrafungol · Itrafungol · itraconazolum · oriconazole · R-51211
由 VetSheet 獸醫團隊審訂更新於 2026年5月15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 |
|---|---|---|---|---|---|
| Malassezia dermatitis | 5 mg/kg PO once daily | PO | q24h | 3 weeks | 🌎 NA |
| Pulse therapy for Malassezia dermatitis | 5 mg/kg for 2 consecutive days per week | PO | 2 consecutive days per week | 3 weeks | 🌎 NA |
| Dermatophytosis | 5 mg/kg PO once daily | PO | q24h | Prolonged course required | 🌎 NA |
| Dermatophytosis (Pulse therapy) | 5 mg/kg PO once daily on an every other week schedule | PO | q24h (pulse) | Three 'pulses' of one week on, one week off | 🌎 NA |
| Blastomycosis | 5 mg/kg PO once daily | PO | q24h | At least 30 days after all signs resolve (total 60-90 days) | 🌎 NA |
| Histoplasmosis | 10 mg/kg daily PO | PO | q24h | At least 30 days after all signs resolve (total at least 90 days) | 🌎 NA |
| Blastomycosis (Alternative) | 5 mg/kg PO once a day or divided twice a day | PO | q24h or q12h | 2-3 months or until active disease is not apparent | 🌎 NA |
| Coccidiomycosis | 5-10 mg/kg PO once daily | PO | q24h | 6-12 months | 🌎 NA |
| Sporotrichosis | 5-10 mg/kg once daily | PO | q24h | 30 days beyond complete resolution of detectable lesions | 🌎 NA |
| Pythiosis or lagendiosis (after lesion resection) | 10 mg/kg PO once daily | PO | q24h | At least 2 months after surgery | 🌎 NA |
| Zygomycosis | 5-10 mg/kg PO q24h | PO | q24h | 3-6 months for non-resectable lesions | 🌎 NA |
| Idiopathic lymphoplasmacytic (chronic) rhinitis (LPR) | 5 mg/kg PO q12h | PO | q12h | Minimum of 3-6 months | 🌎 NA |
| Nasal aspergillosis | 5 mg/kg PO q12h | PO | q12h | 3-6 months | 🌎 NA |
| Coccidioidomycosis | 5-10 mg/kg PO q24h or 5 mg/kg PO q12h | PO | q24h or q12h | — | 🌎 NA |
| General use (fungal infections) | 5 mg/kg | PO | q24h | 4-20 weeks of treatment may be needed, dependent upon culture results | 🌍 EU |
- Malassezia dermatitis: Fair evidence supports recommendation
- Dermatophytosis: Begin taking cultures after 4 weeks. Continue therapy for 2 weeks beyond clinical cure and when 2-3 negative cultures are obtained at weekly intervals.
- Dermatophytosis (Pulse therapy): Toxicity problems are rare with this protocol.
- Blastomycosis: Give with food.
- Histoplasmosis: Give with food. If intestinal histoplasmosis, treat with amphotericin B initially.
- Blastomycosis (Alternative): A loading dose of 10 mg/kg once a day (or divided twice a day) for the first three days may reduce the 'lag' phase.
- Pythiosis or lagendiosis (after lesion resection): Given with terbinafine at 5-10 mg/kg PO q24h.
- Zygomycosis: After aggressive surgical resection or for non-resectable lesions.
- Idiopathic lymphoplasmacytic (chronic) rhinitis (LPR): Has shown dramatic beneficial improvement in some dogs.
- Nasal aspergillosis: May cure up to 60-70% of dogs, although some studies show marginal efficacy.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Histoplasmosis | 10 mg/kg daily PO | PO | q24h | At least 2-4 months | 🌎 NA |
| Cryptococcosis | 50-100 mg per cat per day PO | PO | q24h | Many months (mean 8.5 months) | 🌎 NA |
| Blastomycosis | 10 mg/kg PO once a day or divided twice a day | PO | q24h or q12h | 2-3 months or until active disease is not apparent | 🌎 NA |
| Coccidiomycosis | 5-10 mg/kg PO once daily | PO | q24h | 6-12 months | 🌎 NA |
| Sporotrichosis | 5-10 mg/kg once daily | PO | q24h | 30 days beyond complete resolution of detectable lesions | 🌎 NA |
| Cryptococcosis (mild to moderate, no CNS involvement) | Cats <= 3.5 kg: 50 mg PO once daily or 100 mg PO every other day; Medium/large cats: 100 mg PO once daily | PO | q24h or q48h | 3-12 months | 🌎 NA |
| Coccidioidomycosis | 25-50 mg (total dose) per cat q12-24h | PO | q12-24h | — | 🌎 NA |
| Generalized dermatophytosis (Microsporum canis) | 5 mg/kg PO once daily preferably between meals for 7 days on, 7 days off; repeat 3 times | PO | q24h (pulse) | 5 weeks (treated weeks 1, 3, 5) | 🌎 NA |
| Generalized dermatophytosis (Alternative) | 5 mg/kg PO twice daily or 10 mg/kg | PO | q12h or q24h | Generally 3-5 weeks | 🌎 NA |
| Dermatophyte granuloma | 10 mg/kg PO once daily | PO | q24h | Weeks to months | 🌎 NA |
| Dermatophytosis (Pulse therapy) | 5 mg/kg PO once daily on an every other week schedule | PO | q24h (pulse) | Three 'pulses' of one week on, one week off | 🌎 NA |
| General use (fungal infections) | 5 mg/kg | PO | q24h | 4-20 weeks of treatment may be needed, dependent upon culture results | 🌍 EU |
| Dermatophytosis (Microsporum canis) | 5 mg/kg | PO | q24h | Pulse dosing: 7 days on, 7 days off repeated x3 | 🌍 EU |
- Histoplasmosis: Given with food. Can also be divided twice daily.
- Cryptococcosis: If response inadequate, may add flucytosine.
- Blastomycosis: Cats usually require longer treatment than dogs.
- Cryptococcosis (mild to moderate, no CNS involvement): Give with food. Monitor ALT. Continue until completely normal, then check antigen titer.
- Generalized dermatophytosis (Alternative): Give with food. Give until culture is negative 2 times at two week intervals.
- Dermatophyte granuloma: At least one month beyond clinical resolution and until brush culture is negative x 2.
- Dermatophytosis (Microsporum canis): Authorized in the form of an oral solution. Used successfully to treat ringworm in Persian cats without the need for clipping.
小型哺乳類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Blastomycosis (Mice) | 50-150 mg/kg q24h | PO | q24h | — | 🌎 NA |
| Vaginal candidiasis (Rats) | 2.5-10 mg/kg q24h | PO | q24h | — | 🌎 NA |
| Systemic candidiasis (Guinea pigs) | 5 mg/kg q24h | PO | q24h | — | 🌎 NA |
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Fungal infections in Ratites | 6-10 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Fungal diseases | 5-10 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Aspergillosis (Amazon parrots) | 5-10 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Aspergillosis (African grey Parrots) | 2.5-5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
- Fungal infections in Ratites: If neuro signs develop reduce dose or discontinue.
- Fungal diseases: Use with caution in African grey parrots.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Guttural pouch mycosis, mycotic rhinitis or osteomyelitis | 5 mg/kg PO q24h | PO | q24h | — | 🌎 NA |
- Guttural pouch mycosis, mycotic rhinitis or osteomyelitis: Using the oral solution should be sufficient for treatment.
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
伊曲康唑（Itraconazole）是一種合成的、高度親脂性的口服三唑類抗黴菌藥物，在獸醫學中廣泛用於治療全身性黴菌感染（如麴菌症、隱球菌症、芽生菌症和組織漿菌症），以及表淺的皮癬菌症和馬拉色菌感染。
臨床要點與藥理特性：
- 卓越的療效： 與較早期的咪唑類（如酮康唑）相比，它通常被認為更有效，且內分泌副作用較少，因為它不會明顯抑制哺乳動物的激素合成。
- 組織分佈： 由於其高度親脂性和親角質性，它會大量集中在皮膚、皮脂和膿液中，使其對皮膚黴菌感染極為有效。
- 劑型差異： 伊曲康唑的吸收高度依賴於劑型。市售膠囊需要酸性胃環境和食物才能達到最佳吸收。市售口服液含有環糊精以提高溶解度，空腹吸收效果最佳。
- 調劑警告： 強烈不建議使用散裝粉末進行藥物調劑（Compounding），因為這通常會導致血液濃度低於治療標準或無法測出，在全身性黴菌感染中可能是致命的。
作用機制
Itraconazole is a fungistatic triazole.
Mechanism of Action:
- Enzyme Inhibition: Itraconazole selectively inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase.
- Pathway Disruption: This inhibition blocks the conversion of lanosterol to ergosterol (the primary sterol in fungal cell membranes) → leads to the accumulation of toxic 14α-methylsterols.
- Membrane Permeability: The lack of ergosterol alters the cellular membrane structure → increases membrane permeability → allows leakage of cellular contents and impairs the uptake of purine and pyrimidine precursors.
- Immunomodulation: Itraconazole also exhibits mild immune-suppressing activity, likely via the suppression of T-lymphocyte proliferation.
安全性與警告
禁忌症
- Hypersensitivity to itraconazole or other azole antifungals
- Hepatic impairment (relative contraindication)
- Achlorhydria or hypochlorhydria (relative contraindication)
- Reduced cardiac function (relative, due to potential negative inotropic effects)
- Pregnancy
- Liver disease (avoid use if present)
不良反應
- Anorexia (most common in dogs)
- Hepatotoxicity (increased ALT, jaundice)
- Ulcerative skin lesions/vasculitis (dogs at high doses)
- Limb edema (dogs at high doses)
- Erythema multiforme (rare)
- Toxic epidermal necrolysis (rare)
- Vomiting
- Weight loss
- Depression (especially in cats and African grey parrots)
- Diarrhoea
- Salivation
- Depression and apathy
- Abdominal pain
- Hepatic toxicosis
- Ulcerative dermatitis
- Limb oedema
- Serious cutaneous drug eruptions (occasional)
- Dose-related suppression of adrenal function
注意事項
Use with caution in patients with hepatic impairment, achlorhydria, or reduced cardiac function (due to potential negative inotropic effects). African grey parrots are extremely sensitive to itraconazole and can develop severe anorexia and depression; reduced dosages or alternative antifungals are recommended. Do not use compounded capsules from bulk powders, as they may not yield an absorbable dosage form, leading to treatment failure in life-threatening infections. Safety during pregnancy is not established (teratogenic and embryotoxic in lab animals at high doses).
藥物相互作用
May be antagonistic against Aspergillus or Candida; clinical importance unclear.
May reduce oral absorption of itraconazole; administer itraconazole at least 1 hour before or 2 hours after antacids.
Itraconazole may increase benzodiazepine levels.
Plasma concentrations may be elevated.
Itraconazole may increase levels.
Itraconazole may increase levels.
Increased cisapride levels and possibility for toxicity; concurrent use contraindicated in humans.
May decrease metabolism and increase clomipramine levels.
May inhibit the metabolism of corticosteroids; potential for increased adverse effects.
May inhibit metabolism of cyclophosphamide and its metabolites; potential for increased toxicity.
Increased cyclosporine levels.
May increase digoxin levels; concurrent use considered contraindicated in humans.
May increase fentanyl or alfentanil levels.
Increased gastric pH may reduce itraconazole absorption.
May increase risk for neurotoxicity.
May increase itraconazole concentrations.
May decrease itraconazole levels.
Increased gastric pH may reduce itraconazole absorption.
Increased risk for quinidine toxicity.
May decrease itraconazole levels; itraconazole may increase rifampin levels.
May increase levels; hypoglycemia possible.
May inhibit vinca alkaloid metabolism and increase levels.
May cause increased prothrombin times in patients receiving warfarin or other coumarin anticoagulants.
Extends the activity of methylprednisolone
Inhibits metabolism, potentially leading to toxicity
Inhibits metabolism
Inhibits metabolism
Increases bioavailability and blood levels of ciclosporin (well-documented in cats)
Inhibits metabolism and increases plasma concentrations
Reduces the absorption of itraconazole
Reduces the absorption of itraconazole
Reduces the absorption of itraconazole
Increases plasma concentrations of benzodiazepines
Increases plasma concentrations of vincristine
Datasheet advises against concurrent administration in cats
Datasheet advises against concurrent administration in cats
監測
- Clinical Efficacy
- Liver function tests (monthly ALT recommended with long-term therapy)
- Appetite (anorexia is often the first sign of toxicity)
- Physical assessment for ulcerative skin lesions in dogs
- Liver enzymes (ALT, AST, ALP, Bilirubin) prior to and during prolonged treatment
- Clinical signs of hepatotoxicity (anorexia, vomiting, jaundice)
- Resolution of clinical signs and negative fungal cultures
藥物動力學
吸收
Highly dependent on gastric pH and presence of food. Empty stomach bioavailability may be <50%; with food, it approaches 100%. The oral solution is better absorbed on an empty stomach and possesses adequate bioavailability. Compounded capsules from bulk powders may not be absorbed.
分佈
Very high protein binding. Widely distributed to lipid-rich tissues (highly lipophilic). Skin, sebum, female reproductive tract, and pus have concentrations greater than serum. Minimal concentrations in CSF, urine, aqueous humor, and saliva.
代謝
Metabolized by the liver to many different metabolites, including the active metabolite hydroxyitraconazole.
排除
Elimination may be a saturable process. Because of its long half-life, steady-state plasma levels are not reached for at least 6 days without a loading dose.
過量
There is very limited information on acute toxicity.
- Decontamination: Giving oral antacids may help reduce absorption. If a large overdose occurs, consider gut emptying and provide supportive therapy.
- Clearance: Itraconazole is not removed by dialysis.
- Chronic Toxicity: In studies, dogs receiving 40 mg/kg PO daily for 3 months demonstrated no overt toxicity.
可用產品
劑型
- Capsules
- 100 mg capsule
- 10 mg/ml oral solution
獸醫用
- Intrafungol® (Janssen) oral liquid 10 mg/mL (Available in UK/select countries)
- Itrafungol 10 mg/ml oral solution
人用標示
- Sporanox® Capsules 100 mg (and generics)
- Sporanox® Oral Solution 10 mg/mL
- Sporanox 100 mg capsule
各地核准狀態
POM-V
POM-V, POM
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Capsules should be stored between 15-25°C and protected from light and moisture. Oral solution should be stored at temperatures less than 26°C, and protected from freezing.
飼主須知
重要給藥指示：
- 膠囊： 必須與食物一起餵食以確保適當吸收。對於貓和小型犬，可以打開膠囊，將顆粒與少量美味的食物（如奶油、起司、罐頭食品）混合。
- 口服液： 哺乳動物最好在空腹時給予。
注意事項：
- 食慾不振通常是藥物影響肝臟的第一個徵兆。如果您的寵物停止進食、開始嘔吐，或您注意到眼睛/牙齦變黃（黃疸），請立即聯繫您的獸醫。
- 在狗身上，請注意是否有不明原因的皮膚潰瘍或腿部腫脹。
安全警告：
- 請勿使用散裝粉末調劑的藥物。它們的吸收極差，可能導致治療失敗，這對於嚴重的黴菌感染是非常危險的。
- 未經獸醫同意，請勿與任何其他藥物（尤其是制酸劑）一起給予。
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。