伏立康唑
Voriconazole
UK-109496 (Synthetic derivative of fluconazole)
別名: Vfend · UK-109496 · voriconazol · voraconazolum
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。
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 | 4 mg/kg PO q12h. | PO | q12h | — | 🌎 NA |
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Orbital aspergillosis | 10 mg/kg PO once daily. | PO | q24h | — | 🌎 NA |
- Orbital aspergillosis: Use with extreme caution; significant systemic and neurologic adverse reactions are common.
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General / Pharmacokinetic study | 18 mg/kg PO q8h for 11 days | PO | q8h | 11 days | 🌎 NA |
| Avian aspergillosis | 12.5 mg/kg PO twice daily for 60-90 days or by nebulization as a 1 mg/mL solution for 60 minutes once daily. | PO / Nebulization | q12h / q24h | 60-90 days | 🌎 NA |
- General / Pharmacokinetic study: Studied in Hispaniolan Amazon parrots; further studies needed for long-term safety.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Aspergillosis | 3 mg/kg PO q24h | PO | q24h | — | 🌎 NA |
- Aspergillosis: Higher doses (4-5 mg/kg) are probably necessary to treat infections with Fusarium spp.
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
伏立康唑 (Voriconazole) 是一種廣效的第二代三唑類抗黴菌藥物，為氟康唑 (fluconazole) 的衍生物，專為治療嚴重且具抗藥性的黴菌感染而開發。
- 廣效性：對多種黴菌具有高度療效，特別是麴菌 (Aspergillus)、芽生菌 (Blastomyces) 和 隱球菌 (Cryptococcus)，以及念珠菌、組織漿菌和鐮刀菌等。
- 獸醫臨床應用：目前在獸醫病患中的臨床經驗有限，且藥費極為昂貴，限制了其普及性。然而，由於寵物鳥體型較小，使用此藥治療鳥類麴菌病的關注度正在增加。
- 組織穿透力：在多種動物體內具有極佳的口服生物可用率，並能輕易穿透進入中樞神經系統 (CNS)、淚液和滑液中，對於全身性及深層感染極具價值。
- 貓的敏感性：貓似乎對此藥的不良反應（神經系統及全身性）極度敏感，因此僅應在無其他選擇的情況下作為最後手段使用。
- 藥物交互作用：與其他唑類藥物一樣，它是細胞色素 P450 酵素的強效抑制劑，會導致許多顯著的藥物交互作用。
作用機轉
Voriconazole exerts its fungistatic (and sometimes fungicidal against Aspergillus) effects by inhibiting fungal cell membrane synthesis.
- Primary Mechanism: It inhibits the cytochrome P-450-dependent enzyme 14-alpha-sterol demethylase (lanosterol 14-alpha-demethylase) → blocks the conversion of lanosterol to ergosterol → depletes ergosterol in the fungal cell wall → alters cell membrane fluidity and permeability, leading to fungal cell death.
- Secondary Mechanism: Unlike fluconazole, voriconazole also inhibits 24-methylene dehydrolanosterol demethylation in molds such as Aspergillus, which confers its enhanced activity against these specific fungi.
安全性與警告
禁忌症
- Hypersensitivity to voriconazole or other azole antifungals
- Concurrent use with barbiturates, carbamazepine, cisapride, pimozide, quinidine, rifampin, or rifabutin
- Caution in patients with hepatic dysfunction
- Caution in patients with proarrhythmic conditions
- Caution with the IV formulation in patients with decreased renal function (due to accumulation of the SBECD vehicle)
不良反應
- Dogs: Liver enlargement, significant increase in cytochrome P450 hepatic enzymes
- Cats: Azotemia, inappetence, lethargy, weight loss, cutaneous drug reactions, ataxia, hind limb paresis/paraplegia, visual signs (mydriasis, decreased PLR), arrhythmias, hypokalemia
- Humans: Visual disturbances (blurring, spots, wavy lines), rashes, GI effects (nausea, vomiting, diarrhea), hepatotoxicity, hypertension/hypotension, tachycardia, peripheral edema, hypokalemia, hypomagnesemia
- Rare (Humans): Eye hemorrhage, anemia, leukopenia, thrombocytopenia, pancytopenia, QT prolongation, nephrotoxicity
注意事項
Feline Warning: Cats are highly susceptible to severe neurologic and systemic adverse effects. Use only as a last resort.
- Hepatic Effects: Can cause liver enlargement and enzyme induction (in dogs). Use with caution in patients with pre-existing hepatic dysfunction.
- Renal Impairment: The IV formulation contains sulfobutyl ether beta-cyclodextrin sodium (SBECD), which can accumulate in patients with reduced renal function.
- Pregnancy: Teratogenic in rats and embryotoxic in rabbits (FDA Category D). Weigh risks vs. benefits in pregnant animals.
- Cardiac: Use with caution in patients with proarrhythmic conditions.
藥物交互作用
May increase serum concentrations of these drugs and increase risk for hypoglycemia
Decreased voriconazole concentrations; concurrent use is contraindicated
May increase benzodiazepine concentrations
May increase serum concentrations; dosage adjustment may be required
Decreased voriconazole concentrations; concurrent use is contraindicated
Potential for serious cardiac arrhythmias; concurrent use is contraindicated
Potentially increased AUC for prednisolone
Increased concentrations; decrease cyclosporine dosage by 50% and tacrolimus dosage by 33% when starting voriconazole
May increase plasma concentrations of R-methadone; monitor for toxicity
Can decrease voriconazole concentrations and voriconazole can increase phenytoin concentrations
Potential for serious cardiac arrhythmias; concurrent use is contraindicated
May increase omeprazole (and potentially other PPIs) concentrations
Potential for serious cardiac arrhythmias; concurrent use is contraindicated
Decreased voriconazole concentrations; concurrent use is contraindicated
Possible increased Vinca alkaloid concentrations; monitor for toxicity
May potentiate warfarin's anticoagulant effects
監測
- Clinical efficacy (resolution of fungal infection)
- Liver function tests (baseline and periodic)
- Serum electrolytes (potassium, magnesium)
- Neurologic and visual signs (especially in cats)
藥物動力學
半衰期
吸收
Dogs: Rapidly and essentially completely absorbed PO; peak levels at ~3 hours. Horses: Well absorbed PO; peak levels at 1-3 hours. Alpacas: Low bioavailability (~24%) after single PO doses.
分佈
Dogs: Moderately bound to plasma proteins (51%), Vd ~1.3 L/kg. Horses: Low protein binding (31%), Vd 1.35-1.6 L/kg. Distributes well into CSF, tears, and synovial fluid.
代謝
Metabolized in the liver to various metabolites; the primary circulating metabolite is the N-oxide metabolite (weak antifungal activity). Dogs exhibit auto-induced metabolism after multiple doses.
排除
Dogs: Very complex, dose-dependent non-linear elimination and auto-induction. Horses: Elimination half-life is ~13 hours. Alpacas: Half-life is ~8 hours. Parrots: Short half-life (~1 hour).
過量
The minimum lethal dose in rats and mice is 300 mg/kg (4-7X maintenance dose).
- Clinical Signs: Increased salivation, mydriasis, ataxia, depression, dyspnea, and seizures. In human pediatric patients, accidental 5X overdoses caused brief photophobia.
- Treatment: No specific antidote is known. For very large oral overdoses, consider gut emptying (emesis/gastric lavage) followed by close observation and supportive treatment.
可用產品
劑型
- Tablets
- Powder for oral suspension
- Powder for injection (lyophilized)
獸醫用
- None
人用標示
- Voriconazole Tablets: 50 mg & 200 mg (Vfend®)
- Voriconazole Powder for Oral Suspension: 45 grams (40 mg/mL after reconstitution) (Vfend®)
- Voriconazole Powder for Injection, Lyophilized: 200 mg in single-use vials (Vfend I.V.®)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets: Store at 15-30°C. Unreconstituted powder for oral suspension: Store in refrigerator (2-8°C). Reconstituted suspension: Store at room temperature (15-30°C); do not refrigerate or freeze; stable for 14 days. Powder for injection: Store at room temperature (15-30°C). Reconstituted injection: Use immediately, or stable for up to 24 hours if refrigerated (2-8°C).
飼主須知
伏立康唑 (Voriconazole) 是一種進階的抗黴菌藥物，用於治療嚴重或具抗藥性的黴菌感染。
- 試驗性用藥：此藥物在獸醫學中相對較新，其使用通常被視為試驗性質，且費用相當昂貴。
- 給藥方式：請在餵食前至少一小時或餵食後一小時給藥，以確保藥物能被妥善吸收。
- 需注意的不良反應：由於此藥物在寵物身上的使用經驗有限，請密切觀察您的寵物。如果您發現以下情況，請立即聯繫您的獸醫師：
- 發癢或皮膚起疹子
- 眼白或牙齦變黃（黃疸）
- 食慾減退或體重減輕
- 行走困難、絆倒或無力（特別是後腿）
- 視力問題或瞳孔放大
- 貓咪特別注意：貓咪對此藥物特別敏感。請極度密切觀察牠們在行為、食慾或活動力上的任何變化。
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