氟康唑
Fluconazole
Fluconazole (UK-49858)
別名: Diflucan · UK-49858 · Fluconazolum
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 |
|---|---|---|---|---|---|
| Cryptococcosis, candidiasis, systemic mycoses, nasal aspergillosis | 2.5-5 mg/kg PO or IV q12-24h | PO/IV | q12-24h | 56-84 days | 🌎 NA |
| Fungal meningitis | 5-8 mg/kg PO or IV q12h OR 8-12 mg/kg PO or IV once daily (q24h) | PO/IV | q12h or q24h | 56-84 days | 🌎 NA |
| Urinary candidiasis | 5-10 mg/kg PO q24h | PO | q24h | 21-42 days | 🌎 NA |
| Urinary Candida glabrata infection | 12 mg/kg PO once daily | PO | q24h | 21-42 days | 🌎 NA |
| Cryptococcosis | 5 mg/kg PO once or twice daily | PO | q12h or q24h | At least 2 months beyond resolution of clinical signs | 🌎 NA |
| Blastomycosis | 5 mg/kg PO q12h | PO | q12h | 60 days | 🌎 NA |
| Cryptococcosis | 5-15 mg/kg PO q12-24h | PO | q12-24h | 6-10 months | 🌎 NA |
| Treatment of Malassezia (may be safer than itraconazole or ketoconazole in dogs with hepatic disease) | 5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Systemic treatment of Malassezia dermatitis | 5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Recurrent Malassezia dermatitis | 5 mg/kg PO 3 times per week | PO | 3 times per week | — | 🌎 NA |
| Systemic treatment of Malassezia dermatitis | 2-5 mg/kg PO once daily (q24h) | PO | q24h | — | 🌎 NA |
| Nasal aspergillosis (alternative to itraconazole or terbinafine) | 2.5-5 mg/kg PO q12h | PO | q12h | 3-6 months | 🌎 NA |
- Cryptococcosis, candidiasis, systemic mycoses, nasal aspergillosis: Often treat neurologic ocular cryptococcosis for at least 12 weeks or 2 weeks after CSF exam shows resolution
- Nasal aspergillosis (alternative to itraconazole or terbinafine): Cure rates up to 60%
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Nasal or dermal cryptococcosis | 5-10 mg/kg PO q12-24h, or 10 mg/kg PO q24h | PO | q12-24h | — | 🌎 NA |
| CNS, intraocular, or multisystemic cryptococcosis | 50-100 mg/cat PO or IV q12h | PO/IV | q12h | — | 🌎 NA |
| CNS, intraocular or multisystemic mycoses | 50 mg/cat PO once daily (q24h) | PO | q24h | — | 🌎 NA |
| Cryptococcosis | 50 mg (total dose) PO twice daily | PO | q12h | 1 month beyond resolution of clinical signs | 🌎 NA |
| Cryptococcosis | 50 mg (total dose) PO twice daily | PO | q12h | At least 2 months beyond resolution of clinical signs | 🌎 NA |
- Nasal or dermal cryptococcosis: For most infections, 50 mg/cat PO once daily achieves adequate therapeutic levels
- CNS, intraocular, or multisystemic cryptococcosis: Often treat neurologic ocular cryptococcosis for at least 12 weeks or 2 weeks after CSF exam shows resolution
小型哺乳類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General (Rabbits) | 25-43 mg/kg slow IV q12h | IV | q12h | — | 🌎 NA |
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Candidiasis (cockatoos, parrots) | 20 mg/kg PO q24-48h or 10 mg/kg PO q24h | PO | q24-48h | — | 🌎 NA |
| Candidiasis (cockatiels) | 10 mg/kg fluconazole PO suspension and 100 mg/mL fluconazole treated drinking water | PO | — | — | 🌎 NA |
| Alternate treatment of aspergillosis | 5-10 mg/kg PO once daily | PO | q24h | up to 6 weeks | 🌎 NA |
- Candidiasis (cockatoos, parrots): Likely effective for C. albicans. C. galabrata and C. papasilosis may have higher MICs.
- Candidiasis (cockatiels): Maintained plasma levels above the MIC for most strains of Candida albicans
- Alternate treatment of aspergillosis: With or after amphotericin B
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| C. immitis infection or Candida bacteremia | Loading dose of 14 mg/kg followed by 5 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| Fungal keratitis | 1 mg/kg PO q24h | PO | q24h | — | 🌎 NA |
- Fungal keratitis: Anecdotal reports of successful treatment
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
氟康唑（Fluconazole）是一種全身性的三唑類抗黴菌藥物。與早期的第一代唑類藥物（如酮康唑）不同，它具有高度親水性，能夠極佳地穿透進入中樞神經系統 (CSF)、眼睛和泌尿道。
臨床要點： 它的吸收不需要酸性胃部環境，因此即使在接受制酸劑治療的病患中，其口服生物利用度也非常穩定。此外，與酮康唑相比，它對哺乳動物細胞色素 P450 酵素的親和力低得多，這意味著它對哺乳動物類固醇激素合成的影響極小，且通常副作用較少。
作用機轉
Fluconazole acts by inhibiting the fungal cytochrome P450-dependent enzyme lanosterol 14-α-demethylase.
Lanosterol → (blocked by fluconazole) → Ergosterol
This depletion of ergosterol disrupts the synthesis of the fungal cell membrane, increasing its permeability and causing leakage of essential cellular contents. It also impairs the uptake of purine and pyrimidine precursors. Fluconazole is primarily fungistatic.
安全性與警告
禁忌症
- Hypersensitivity to fluconazole or other azole antifungals
- Budgerigars (reportedly toxic)
- Pregnant animals
- Lactating animals
不良反應
- Inappetence
- Vomiting
- Diarrhea
- Hepatotoxicity (rare)
- Headache (humans)
- Increased liver enzymes (humans)
- Exfoliative skin disorders (humans)
- Thrombocytopenia (humans)
- Nausea
- Diarrhoea
注意事項
Use with caution in patients with hepatic impairment. Because fluconazole is eliminated primarily by the kidneys, doses or dosing intervals may need to be adjusted in patients with renal impairment. Safety during pregnancy has not been established (FDA Category C); use with caution in nursing dams as it is excreted in milk. Reportedly toxic to budgerigars.
藥物交互作用
May be antagonistic against Aspergillus or Candida; clinical importance unclear
Plasma concentrations of buspirone may be elevated
May increase cisapride levels and the possibility for toxicity
May inhibit the metabolism of corticosteroids; potential for increased adverse effects
May inhibit the metabolism of cyclophosphamide and its metabolites; potential for increased toxicity
Increases cyclosporine levels; dosage of cyclosporine may need to be decreased by 29%-51%
Increased fluconazole concentrations
May increase fentanyl levels
Increased midazolam levels and effects
May increase NSAID plasma levels; increased risk for adverse effects
Increased risk for cardiotoxicity
May decrease fluconazole efficacy; fluconazole may increase rifampin levels
Increased theophylline concentrations
May exacerbate the effects of tricyclic antidepressants (e.g., clomipramine, amitriptyline)
May increase levels of agents like glipizide or glyburide; hypoglycemia possible
May inhibit vinca alkaloid metabolism
May cause increased prothrombin times
Fluconazole inhibits cytochrome P450-dependent liver enzymes, which may increase plasma theophylline concentrations.
Co-administration has led to terfenadine toxicity in humans.
Fluconazole increases ciclosporin blood levels.
監測
- Clinical efficacy
- Liver function tests (occasional, with long-term therapy)
- Liver enzyme panel (ALT, AST, ALP, Bilirubin) prior to and during prolonged therapy
- Renal function (BUN, Creatinine)
- Resolution of clinical signs of fungal infection
- Therapeutic drug monitoring for concurrent medications like ciclosporin or theophylline
藥物動力學
吸收
Rapidly and nearly completely absorbed (90%) after oral administration. Gastric pH or the presence of food do not appreciably alter oral bioavailability.
分佈
Low protein binding and widely distributed throughout the body. Penetrates well into the CSF, eye, and peritoneal fluid.
代謝
Minimal hepatic metabolism compared to other azole antifungals.
排除
Eliminated primarily via the kidneys and achieves high concentrations in the urine.
過量
There is limited information on acute toxicity in domestic animals. In rodents, massive overdoses (1-2 g/kg) caused respiratory depression, salivation, lacrimation, urinary incontinence, and cyanosis, leading to death within several days.
Treatment: If a massive overdose occurs, consider gut emptying (emesis or gastric lavage) if recent, and provide supportive therapy as required. Fluconazole may be removed by hemodialysis or peritoneal dialysis.
可用產品
劑型
- Tablets
- Powder for oral suspension
- Injection
- 150 mg oral capsule
- 200 mg oral capsule
- 40 mg/ml oral suspension
- 2 mg/ml injectable solution
人用標示
- Fluconazole Oral Tablets: 50 mg, 100 mg, 150 mg, & 200 mg
- Fluconazole Powder for Oral Suspension: 10 mg/mL & 40 mg/mL (when reconstituted)
- Fluconazole Injection: 2 mg/mL in 100 mL or 200 mL bottles or Viaflex Plus
- Diflucan 50 mg, 150 mg, 200 mg capsules
- Diflucan 40 mg/ml oral suspension
- Diflucan 2 mg/ml injectable solution
各地核准狀態
POM (Prescription Only Medicine)
POM-V (Prescription Only Medicine - Veterinarian)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored at temperatures less than 30°C in tight containers. Injection should be stored at 5-30°C (5-25°C for Viaflex bags); avoid freezing. Do not add additives to the injection.
飼主須知
- 耐心是關鍵： 黴菌感染需要很長時間才能清除。治療通常持續數週至數個月。即使您的寵物看起來好轉，也不要提早停藥，因為感染可能會復發。
- 給藥方式： 氟康唑無論是與食物一起服用或空腹服用，都能被良好吸收。
- 注意副作用： 雖然通常非常安全，但請注意是否有食慾不振、嘔吐或腹瀉的情況。如果發生這些情況，請聯繫您的獸醫。
- 費用： 由於治療期長，費用可能會累積，不過學名藥的出現已使其變得較為負擔得起。
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。