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フルコナゾール

Fluconazole

Fluconazole (UK-49858)

抗真菌薬 - トリアゾール系POIV犬猫小型哺乳類鳥馬

別名: Diflucan · UK-49858 · Fluconazolum

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

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

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

動物種別用量

🌎 NA — North America🌍 EU — Europe

犬

適応用量経路頻度期間地域
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%

猫

適応用量経路頻度期間地域
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

適応用量経路頻度期間地域
General (Rabbits)25-43 mg/kg slow IV q12hIVq12h—🌎 NA

鳥

適応用量経路頻度期間地域
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

適応用量経路頻度期間地域
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

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

診察中ですか？VetSheet の AI が薬剤・用量・投与期間を構造化された診察記録に直接記入します。VetSheet の仕組みを見る

概要

フルコナゾールは全身性の​トリアゾール系抗真菌薬​です。ケトコナゾールなどの古い第一世代アゾール系とは異なり、親水性が高く、​中枢神経系（CSF）​、​眼​、​尿路​への移行性に優れています。

​臨床のポイント:​ 吸収に胃酸を必要としないため、制酸薬を服用している患者でも経口バイオアベイラビリティが非常に安定しています。さらに、ケトコナゾールに比べて哺乳類のシトクロムP450酵素への親和性がはるかに低いため、哺乳類のステロイドホルモン合成への影響が最小限であり、一般的に副作用が少ないです。

作用機序

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・警告

禁忌

  • Hypersensitivity to fluconazole or other azole antifungals
  • Budgerigars (reportedly toxic)
  • Pregnant animals
  • Lactating animals

有害事象

  • 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.

医薬品相互作用

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.

監視

  • 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

薬物動態

吸収

Rapidly and nearly completely absorbed (90%) after oral administration. Gastric pH or the presence of food do not appreciably alter oral bioavailability.

分布

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.

消失

Eliminated primarily via the kidneys and achieves high concentrations in the urine.

過剰投与

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.

製品

製剤

  • Tablets
  • Powder for oral suspension
  • Injection
  • 150 mg oral capsule
  • 200 mg oral capsule
  • 40 mg/ml oral suspension
  • 2 mg/ml injectable solution

ヒト用医薬品

  • 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

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine)

United Kingdom✓ 承認済み処方箋医薬品VMD
🐕 Dogs🐈 Cats

POM-V (Prescription Only Medicine - Veterinarian)

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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.

飼主向け情報

  • ​根気が必要です:​ 真菌感染症の治療には長い時間がかかります。治療は通常数週間から数ヶ月続きます。ペットの症状が良くなったように見えても、感染が再発する可能性があるため、早めに薬をやめないでください。
  • ​投与方法:​ フルコナゾールは食事と一緒でも、空腹時でも非常によく吸収されます。
  • ​副作用に注意:​ 一般的に非常に安全ですが、食欲不振、嘔吐、下痢に注意してください。これらの症状が見られた場合は獣医師に連絡してください。
  • ​費用:​ 治療が長期にわたるため費用がかさむことがありますが、ジェネリック医薬品の普及により手頃になってきています。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。