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氟康唑

Fluconazole

Fluconazole (UK-49858)

抗黴菌藥 - 三唑類POIV狗貓小型哺乳類鳥馬

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

2.5-5 mg/kg PO or IV q12-24hPO/IV· q12-24h· 56-84 days
— 🐕

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
Cryptococcosis, candidiasis, systemic mycoses, nasal aspergillosis2.5-5 mg/kg PO or IV q12-24hPO/IVq12-24h56-84 days🌎 NA
Fungal meningitis5-8 mg/kg PO or IV q12h OR 8-12 mg/kg PO or IV once daily (q24h)PO/IVq12h or q24h56-84 days🌎 NA
Urinary candidiasis5-10 mg/kg PO q24hPOq24h21-42 days🌎 NA
Urinary Candida glabrata infection12 mg/kg PO once dailyPOq24h21-42 days🌎 NA
Cryptococcosis5 mg/kg PO once or twice dailyPOq12h or q24hAt least 2 months beyond resolution of clinical signs🌎 NA
Blastomycosis5 mg/kg PO q12hPOq12h60 days🌎 NA
Cryptococcosis5-15 mg/kg PO q12-24hPOq12-24h6-10 months🌎 NA
Treatment of Malassezia (may be safer than itraconazole or ketoconazole in dogs with hepatic disease)5 mg/kg PO once dailyPOq24h—🌎 NA
Systemic treatment of Malassezia dermatitis5 mg/kg PO once dailyPOq24h—🌎 NA
Recurrent Malassezia dermatitis5 mg/kg PO 3 times per weekPO3 times per week—🌎 NA
Systemic treatment of Malassezia dermatitis2-5 mg/kg PO once daily (q24h)POq24h—🌎 NA
Nasal aspergillosis (alternative to itraconazole or terbinafine)2.5-5 mg/kg PO q12hPOq12h3-6 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 cryptococcosis5-10 mg/kg PO q12-24h, or 10 mg/kg PO q24hPOq12-24h—🌎 NA
CNS, intraocular, or multisystemic cryptococcosis50-100 mg/cat PO or IV q12hPO/IVq12h—🌎 NA
CNS, intraocular or multisystemic mycoses50 mg/cat PO once daily (q24h)POq24h—🌎 NA
Cryptococcosis50 mg (total dose) PO twice dailyPOq12h1 month beyond resolution of clinical signs🌎 NA
Cryptococcosis50 mg (total dose) PO twice dailyPOq12hAt 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 q12hIVq12h—🌎 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 q24hPOq24-48h—🌎 NA
Candidiasis (cockatiels)10 mg/kg fluconazole PO suspension and 100 mg/mL fluconazole treated drinking waterPO——🌎 NA
Alternate treatment of aspergillosis5-10 mg/kg PO once dailyPOq24hup 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 bacteremiaLoading dose of 14 mg/kg followed by 5 mg/kg PO once dailyPOq24h—🌎 NA
Fungal keratitis1 mg/kg PO q24hPOq24h—🌎 NA
  • Fungal keratitis: Anecdotal reports of successful 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。

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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。

作用機制

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.

藥物相互作用

Amphotericin B

May be antagonistic against Aspergillus or Candida; clinical importance unclear

Buspirone

Plasma concentrations of buspirone may be elevated

Cisapride

May increase cisapride levels and the possibility for toxicity

Corticosteroids

May inhibit the metabolism of corticosteroids; potential for increased adverse effects

Cyclophosphamide

May inhibit the metabolism of cyclophosphamide and its metabolites; potential for increased toxicity

Cyclosporine

Increases cyclosporine levels; dosage of cyclosporine may need to be decreased by 29%-51%

Diuretics, Thiazides

Increased fluconazole concentrations

Fentanyl/Alfentanil

May increase fentanyl levels

Midazolam

Increased midazolam levels and effects

NSAIDs

May increase NSAID plasma levels; increased risk for adverse effects

Quinidine

Increased risk for cardiotoxicity

Rifampin

May decrease fluconazole efficacy; fluconazole may increase rifampin levels

Theophylline/Aminophylline

Increased theophylline concentrations

Tricyclic Antidepressants

May exacerbate the effects of tricyclic antidepressants (e.g., clomipramine, amitriptyline)

Sulfonylurea Antidiabetic Agents

May increase levels of agents like glipizide or glyburide; hypoglycemia possible

Vincristine/Vinblastine

May inhibit vinca alkaloid metabolism

Warfarin

May cause increased prothrombin times

TheophyllineModerate

Fluconazole inhibits cytochrome P450-dependent liver enzymes, which may increase plasma theophylline concentrations.

TerfenadineMajor

Co-administration has led to terfenadine toxicity in humans.

CiclosporinMajor

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

European Union✓ 已核准處方藥EMA
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine)

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs🐈 Cats

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。

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