テルビナフィン
Terbinafine
Terbinafine Hydrochloride
別名: Lamisil · Terbinex · Alamil · Daskil · Daskyl · DesenexMax · Finex · Maditez · Micosil · Terekol · Osurnia · Terbinafine hydrochloride · Terbinafinum
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
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 |
|---|---|---|---|---|---|
| Dermatophytic infections | 10-20 mg/kg | PO | q24h | — | 🌎 NA |
| Dermatophytic infections (when other drugs are not tolerated) | 25 mg/kg | PO | q24h | — | 🌎 NA |
| Adjunctive treatment of nasal Aspergillus infections (if cribriform plate is penetrated) | 5-10 mg/kg | PO | q12h | 3-6 months | 🌎 NA |
| Pythiosis (where advanced disease precludes complete surgical excision) | 10 mg/kg | PO | q24h | — | 🌎 NA |
| Lagendiosis (where disease precludes complete surgical excision) | 5-10 mg/kg | PO | q24h | — | 🌎 NA |
| Antifungal (Systemic/Dermatophytosis) | 20-40 mg/kg | PO | q24h | Not specified | 🌍 EU |
| Localized Malassezia infections | Apply a thin layer | topical | Not specified | Not specified | 🌍 EU |
| Acute otitis externa (S. pseudintermedius, M. pachydermatis) | 1 tube per infected ear | topical | Repeat after 7 days | 2 doses total | 🌍 EU |
- Dermatophytic infections: Appears to be better tolerated than either ketoconazole or itraconazole.
- Adjunctive treatment of nasal Aspergillus infections (if cribriform plate is penetrated): Used with topical therapy.
- Pythiosis (where advanced disease precludes complete surgical excision): Given concurrently with itraconazole (10 mg/kg PO twice daily).
- Lagendiosis (where disease precludes complete surgical excision): Given concurrently with itraconazole (10 mg/kg PO q24h) and repeated aggressive surgical resection.
- Antifungal (Systemic/Dermatophytosis): Doses greater than 30 mg/kg may be required to reach therapeutic levels in the skin of dogs.
- Localized Malassezia infections: Use 1% cream.
- Acute otitis externa (S. pseudintermedius, M. pachydermatis): Ear gel should be instilled in a cleaned ear. Maximum clinical response may not be seen until 21 days after the second administration.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Dermatophytic infections (Pulse therapy) | 20 mg/kg | PO | q24h | 7 days on, then 21 days off | 🌎 NA |
| Dermatophytic infections | 10-20 mg/kg | PO | q24h | — | 🌎 NA |
| Dermatophytic infections (when other drugs are not tolerated) | 25 mg/kg | PO | q24h | — | 🌎 NA |
| Dermatophyte (M. canis) mycetomas | 26-31 mg/kg | PO | q24h | 12-14 weeks | 🌎 NA |
| Cryptococcal infections (azole-resistant) | 10 mg/kg | PO | q24h | Life-long | 🌎 NA |
| Antifungal (Systemic/Dermatophytosis) | 20-40 mg/kg | PO | q24h | Not specified | 🌍 EU |
| Localized Malassezia infections | Apply a thin layer | topical | Not specified | Not specified | 🌍 EU |
- Dermatophytic infections (Pulse therapy): Maintained terbinafine concentrations in hair above therapeutic levels. Higher doses (40 mg/kg) or continuous administration caused emesis and elevated hepatic enzymes.
- Dermatophytic infections: Appears to be better tolerated than either ketoconazole or itraconazole.
- Dermatophyte (M. canis) mycetomas: Achieved clinical and mycological cure in a case report of two cats.
- Cryptococcal infections (azole-resistant): Can rectify clinical signs, though cats with CNS cryptococcus usually require treatment for life.
- Localized Malassezia infections: Use 1% cream.
鳥
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Avian mycotic infections (Aspergillus) | 10-15 mg/kg | PO | q12-24h | — | 🌎 NA |
| Avian mycotic infections (Aspergillus) | 1 mg/mL aqueous solution | Nebulization | Not specified | — | 🌎 NA |
| Avian mycotic infections | 10-15 mg/kg | PO | q12-24h | — | 🌎 NA |
| Avian mycotic infections | 1 mg/mL | Nebulization | Not specified | — | 🌎 NA |
| Aspergillosis (suspected via leukocytosis and pulmonary nodules) | 10-15 mg/kg | PO | q12h | 4 weeks | 🌎 NA |
- Avian mycotic infections (Aspergillus): Appears to be well tolerated by a number of avian species.
- Avian mycotic infections: Suspend a 250 mg tablet in 25 mL water. Can be used in combination with itraconazole.
- Avian mycotic infections: Mix 500 mg terbinafine plus 1 mL Mucomyst plus 500 mL of distilled water.
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。
概要
テルビナフィンは、経口および外用製剤として利用可能な合成アリルアミン系抗真菌薬です。
主な臨床的特徴:
- 主な用途: 犬や猫の皮膚糸状菌感染症(小胞子菌、白癬菌など)に非常に有効です。また、特に鳥類における全身性真菌感染症(アスペルギルス症など)の治療にも使用されます。
- 良好な相互作用プロファイル: アゾール系抗真菌薬(ケトコナゾール、イトラコナゾールなど)とは異なり、テルビナフィンの主な作用機序はシトクロムP-450酵素系に依存しないため、薬物相互作用が著しく少なく、哺乳類のテストステロンやコルチゾール合成を抑制しません。
- 薬理学的特徴: テルビナフィンは高い脂溶性と親ケラチン性を持っています。皮膚、皮脂、毛包に広く分布し、治療中止後も数週間にわたってこれらの組織で治療濃度を維持します(これによりパルス療法が可能になります)。
- 忍容性: 獣医療において一般的に非常に忍容性が高く、最もよく報告される副作用は軽度の胃腸障害(嘔吐)です。
作用機序
Terbinafine exerts its antifungal activity by interfering with fungal sterol biosynthesis at an early stage.
- It selectively and reversibly inhibits the fungal enzyme squalene monooxygenase (also known as squalene 2,3-epoxidase).
- This blockade prevents the conversion of squalene to lanosterol → leading to a profound deficiency of ergosterol (a critical component of the fungal cell membrane).
- Simultaneously, the inhibition causes an intracellular accumulation of squalene, which is directly toxic to the fungal cell, leading to rapid cell death.
This dual mechanism makes terbinafine primarily fungicidal against dermatophytes, though it may only be fungistatic against certain yeasts like Candida spp.
安全性・警告
禁忌
- Known hypersensitivity to terbinafine
- Active or chronic liver disease
- Significantly impaired renal function
- Perforated eardrum (for ear gel administration)
- Generalized demodicosis (topical or systemic use)
- Pregnant animals
- Breeding animals
有害事象
- Vomiting
- Inappetence
- Diarrhea
- Lethargy (reported in cats)
- Hepatotoxicity / Liver failure (very rare, reported in humans)
- Neutropenia (very rare, reported in humans)
- Serious skin reactions like Toxic Epidermal Necrolysis or Stevens-Johnson syndrome (very rare, reported in humans)
- Diarrhoea
- Increased liver enzymes
- Pruritus (cats)
- Topical irritation (due to alcohol content in topical solutions)
- Transient deafness or impaired hearing (in elderly dogs after administration of ear gel)
注意事項
Hepatic and Renal Warning: Use with extreme caution, if at all, in patients with markedly impaired liver or renal function. Dosage adjustments should be considered if use is unavoidable.
- Pregnancy/Nursing: Definitive safety in pregnancy has not been established (FDA Category B in humans). The manufacturer recommends against use in pregnant or nursing individuals, as the drug concentrates in maternal milk at levels 7 times higher than plasma. Use with caution in nursing veterinary patients.
医薬品相互作用
Terbinafine may increase the elimination and decrease the efficacy of cyclosporine.
May increase terbinafine clearance, potentially requiring higher terbinafine doses.
Terbinafine shares the CYP2D6 metabolic pathway and could theoretically alter the metabolism of beta-blockers.
Terbinafine shares the CYP2D6 metabolic pathway and could theoretically alter the metabolism of MAOIs.
Terbinafine shares the CYP2D6 metabolic pathway and could theoretically alter the metabolism of SSRIs.
Terbinafine shares the CYP2D6 metabolic pathway and could theoretically alter the metabolism of TCAs.
May decrease the clearance of terbinafine, potentially increasing plasma concentrations (Clinical Pearl)
監視
- Clinical efficacy (resolution of fungal lesions)
- Baseline liver enzymes prior to therapy
- Periodic liver enzyme monitoring as needed, especially during long-term treatment
- CBC (baseline and periodic)
- Liver function tests (ALT, AST, Bilirubin)
- Renal function tests
- Clinical response (skin scrapings, fungal cultures)
薬物動態
半減期
吸収
In humans, oral absorption is >70%, but first-pass metabolism reduces bioavailability to about 40%. Food may slightly enhance absorption.
分布
Highly lipophilic and keratinophilic. Distributes extensively into the skin, sebum, and adipose tissue, where it can persist for very long periods. >99% bound to plasma proteins.
代謝
Metabolized in the liver.
消失
Eliminated primarily after hepatic metabolism.
過剰投与
There is limited information regarding acute toxicity in veterinary species. In humans, acute ingestions of up to 5 grams have been reported without serious adverse effects. Treatment of massive overdose should be supportive and symptomatic.
製品
製剤
- Oral granules
- Aqueous solution (for nebulization)
- 250 mg oral tablets
- 1% topical cream
- 1% topical gel
- 1% topical spray
- 10 mg ear gel (combination product containing terbinafine, florfenicol, and betamethasone)
動物用医薬品
- Osurnia ear gel (10 mg terbinafine, florfenicol, betamethasone)
ヒト用医薬品
- Terbinafine HCl Oral Tablets: 250 mg (Lamisil, Terbinex, generic)
- Terbinafine HCl Oral Granules (film-coated): 125 mg/packet & 187.5 mg/packet (Lamisil)
- Topical cream 1%
- Topical spray 1%
- Lamisil 250 mg tablets
- Lamisil 1% cream
- Lamisil 1% gel
- Lamisil 1% spray
規制ステータス
POM-V
POM-V, POM
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store tablets at room temperature in tight containers; protect from light.
飼主向け情報
飼い主様への重要な情報
- 投与方法: この薬は食事と一緒に与えることを強くお勧めします。これにより吸収が高まり、胃の不快感や嘔吐の可能性が大幅に減少します。
- 治療期間: 真菌感染症(白癬など)の治癒には時間がかかります。数週間から数ヶ月間、投薬を続ける必要がある場合があります。獣医師の指示がない限り、ペットの症状が良くなったように見えても、途中で投薬をやめないでください。
- 注意すべき症状: テルビナフィンは一般的に非常に安全です。ただし、持続的な嘔吐、食欲不振、重度の下痢、または極度の疲労が見られる場合は、獣医師にご相談ください。
- まれで重篤な症状: ごくまれに、この薬が肝臓に影響を与えることがあります。ペットの目、歯茎、または皮膚が黄色くなっている(黄疸)ことに気づいた場合は、すぐに獣医師に連絡してください。
- 費用: 治療の全コースにはかなりの費用がかかる場合がありますが、ジェネリック医薬品の普及により、以前より手頃な価格になっています。
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。
