兩性黴素B
Amphotericin B
別名: Abelcet · AmBisome · Amphotec · Fungizone · Amphocil · Amphotericin B deoxycholate · Amphotericin B lipid complex · Liposomal amphotericin B · Anfotericina B · Amphotericinum B
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
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各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible systemic fungal infections (Rapid-Infusion Technique) | 0.25 mg/kg IV over 5 minutes, then 0.5 mg/kg 3 times a week until 9-12 mg/kg accumulated dosage is given | IV | 3 times a week | Until 9-12 mg/kg accumulated | 🌎 NA |
| Susceptible systemic fungal infections (Slow IV Infusion Technique) | 0.25 mg/kg IV over 4-6 hours, then 0.5 mg/kg 3 times a week until 9-12 mg/kg accumulated dosage is given | IV | 3 times a week | Until 9-12 mg/kg accumulated | 🌎 NA |
| Systemic fungal infections (Dehydrated/compromised) | 0.5 mg/kg diluted in D5W given by slow IV over 15 minutes (normal renal) or 3-6 hours (compromised renal) | IV | Every other day | Until cumulative dose of 8-10 mg/kg (or higher depending on disease) | 🌎 NA |
| Systemic mycoses (Lipid-based: AmBisome, Amphocil, Abelcet) | Test dose of 0.5 mg/kg; then 1-2.5 mg/kg IV q48h (or Monday, Wednesday, Friday) for 4 weeks or until the total cumulative dose is reached | IV | q48h | 4 weeks or until cumulative dose reached | 🌎 NA |
| Systemic mycoses (ABLC; Abelcet) | 2-3 mg/kg IV three days per week for a total of 9-12 treatments (cumulative dose of 24-27 mg) | IV | 3 days per week | 9-12 treatments | 🌎 NA |
| Blastomycosis | 0.5 mg/kg 3 times weekly until a total dose of 6 mg/kg is given | IV | 3 times weekly | Until 6 mg/kg cumulative | 🌎 NA |
| Blastomycosis | 0.15-0.5 mg/kg IV 3 times a week | IV | 3 times a week | Until total dose reaches 4-6 mg/kg, then start maintenance | 🌎 NA |
| Blastomycosis (severe cases, using Abelcet) | 1-2 mg/kg IV three times a week (or every other day) to a cumulative dose of 12-24 mg/kg | IV | 3 times a week | Until 12-24 mg/kg cumulative | 🌎 NA |
| Cryptococcosis | 0.5-0.8 mg/kg SC 2-3 times per week | SC | 2-3 times per week | — | 🌎 NA |
| Histoplasmosis | 0.15-0.5 mg/kg IV 3 times a week | IV | 3 times a week | Until total dose reaches 2-4 mg/kg, then start maintenance | 🌎 NA |
| Histoplasmosis | 0.5 mg/kg IV given over 6-8 hours. If dose is tolerated, increase to 1 mg/kg given on alternate days until total dose of 7.5-8.5 mg/kg cumulative dose is achieved | IV | Alternate days | Until 7.5-8.5 mg/kg cumulative | 🌎 NA |
| Leishmaniasis (Liposomal form) | 3-3.3 mg/kg IV 3 times weekly for 3-5 treatments | IV | 3 times weekly | 3-5 treatments | 🌎 NA |
| Leishmaniasis (AmBisome) | Give initial test dose of 0.5 mg/kg, then 3-3.3 mg/kg IV every 72-96 hours until a cumulative dose of 15 mg/kg is reached | IV | q72-96h | Until 15 mg/kg cumulative | 🌎 NA |
| Gastrointestinal pythiosis (ABLC; Abelcet) | 1-2 mg/kg IV three times weekly for 4 weeks (cumulative dose 12-24 mg) | IV | 3 times weekly | 4 weeks | 🌎 NA |
| Systemic fungal infections and leishmaniosis | Dose not specified in monograph; requires specific protocols | IV | As directed | Until clinical resolution | 🌍 EU |
- Susceptible systemic fungal infections (Rapid-Infusion Technique): Dilute in 30 mL of 5% dextrose. Flush with 10 mL D5W before and after.
- Susceptible systemic fungal infections (Slow IV Infusion Technique): Dilute in 250-500 mL of D5W.
- Systemic fungal infections (Dehydrated/compromised): Must rehydrate before administration. Discontinue if BUN exceeds 50 mg/dL.
- Systemic mycoses (Lipid-based: AmBisome, Amphocil, Abelcet): 1 mg/kg for susceptible yeast/dimorphic fungi (cumulative 12 mg/kg); 2-2.5 mg/kg for resistant filamentous fungi (cumulative 24-30 mg/kg).
- Systemic mycoses (ABLC; Abelcet): Dilute to 1 mg/mL in D5W and infuse over 1-2 hours.
- Blastomycosis: Given with ketoconazole.
- Blastomycosis: Given with ketoconazole.
- Cryptococcosis: Diluted in 0.45% NaCl with 2.5% dextrose. Concentrations >20 mg/L result in local irritation/sterile abscess.
- Histoplasmosis: Given with ketoconazole.
- Histoplasmosis: Alternative to ketoconazole treatment.
- Gastrointestinal pythiosis (ABLC; Abelcet): Follow-up medical therapy after surgical resection.
- Systemic fungal infections and leishmaniosis: Lipid formulations preferred if pre-existing renal insufficiency exists.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible systemic fungal infections (Rapid-Infusion Technique) | 0.25 mg/kg IV over 5 minutes 3 times a week until 9-12 mg/kg accumulated dosage is given | IV | 3 times a week | Until 9-12 mg/kg accumulated | 🌎 NA |
| Cryptococcosis | 0.25 mg/kg in 30 mL D5W IV over 15 minutes q48h | IV | q48h | 3-4 weeks after clinical signs resolve | 🌎 NA |
| Cryptococcosis | 0.15-0.4 mg/kg IV 3 times a week | IV | 3 times a week | Until total dose reaches 4-6 mg/kg, then start maintenance | 🌎 NA |
| Cryptococcosis | 0.5-0.8 mg/kg SC 2-3 times per week | SC | 2-3 times per week | — | 🌎 NA |
| Cryptococcosis (ABLC; Abelcet) | 1 mg/kg IV three days per week for a total of 12 treatments (cumulative dose of 12 mg) | IV | 3 days per week | 12 treatments | 🌎 NA |
| Histoplasmosis | 0.25 mg/kg in 30 mL D5W IV over 15 minutes q48h | IV | q48h | 4-8 weeks | 🌎 NA |
| Histoplasmosis | 0.15-0.5 mg/kg IV 3 times a week | IV | 3 times a week | Until total dose reaches 2-4 mg/kg, then start maintenance | 🌎 NA |
| Blastomycosis | 0.25 mg/kg in 30 mL D5W IV over 15 minutes q48h | IV | q48h | Until cumulative dose of 4 mg/kg is given | 🌎 NA |
| Blastomycosis | 0.15-0.5 mg/kg IV 3 times a week | IV | 3 times a week | Until total dose reaches 4-6 mg/kg, then start maintenance | 🌎 NA |
| Systemic fungal infections (e.g., cryptococcosis) | Dose not specified in monograph; requires specific protocols | IV | As directed | Until clinical resolution | 🌍 EU |
| Cryptococcosis (when IV access is problematic) | Dose not specified in monograph; requires specific protocols | SC | As directed | Until clinical resolution | 🌍 EU |
- Susceptible systemic fungal infections (Rapid-Infusion Technique): Dilute in 30 mL of 5% dextrose. Flush with 10 mL D5W before and after.
- Cryptococcosis: Given with flucytosine. Stop if BUN >50 mg/dL.
- Cryptococcosis: Given with flucytosine.
- Cryptococcosis: Diluted in 0.45% NaCl with 2.5% dextrose (400 mL for cats).
- Cryptococcosis (ABLC; Abelcet): Dilute to 1 mg/mL in D5W and infuse over 1-2 hours.
- Histoplasmosis: Given with ketoconazole. Stop if BUN >50 mg/dL.
- Histoplasmosis: Given with ketoconazole.
- Blastomycosis: Given with ketoconazole. Stop if BUN >50 mg/dL.
- Blastomycosis: Given with ketoconazole.
- Systemic fungal infections (e.g., cryptococcosis): SC alternative has been used for cryptococcosis if regular venous catheterization is problematic.
- Cryptococcosis (when IV access is problematic): SC route used as an alternative to IV.
小型哺乳類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible systemic fungal infections (Rabbits) | 1 mg/kg/day IV | IV | q24h | — | 🌎 NA |
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Aspergillosis (raptors and psittacines) | 1.5 mg/kg IV three times daily for 3 days | IV | q8h | 3 days | 🌎 NA |
| Aspergillosis (raptors and psittacines) | 1 mg/kg diluted in sterile water once to 3 times daily for 3 days | Intratracheal | q8-24h | 3 days | 🌎 NA |
| Aspergillosis | 1.5 mg/kg IV q12h for 3-5 days; topically in the trachea at 1 mg/kg q12h; 0.3-1 mg/mL nebulized for 15 minutes 2-4 times daily | IV/Intratracheal/Nebulization | Variable | 3-5 days (IV) | 🌎 NA |
| Macrorhabdiasis (Microrhabdus ornithogaster) | 100-150 mg/kg PO q12h for 30 days | PO | q12h | 30 days | 🌎 NA |
- Aspergillosis (raptors and psittacines): With or followed by flucytosine.
- Aspergillosis (raptors and psittacines): In conjunction with flucytosine.
- Macrorhabdiasis (Microrhabdus ornithogaster): Treatment failures common with shorter durations.
爬蟲類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible fungal respiratory infections | 1 mg/kg diluted in saline and given intra-tracheally once daily for 14-28 treatments | Intratracheal | q24h | 14-28 treatments | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Fungal pneumonia | Day 1: 0.3 mg/kg IV; Day 2: 0.4 mg/kg IV; Day 3: 0.6 mg/kg IV; days 4-7: no treatment; then every other day until a total cumulative dose of 6.75 mg/kg has been administered | IV | Variable | Until 6.75 mg/kg cumulative | 🌎 NA |
| Phycomycoses and pulmonary mycoses | Day 1: 0.3 mg/kg IV; Day 2: 0.45 mg/kg IV; Day 3: 0.6 mg/kg IV; then every other day for 3 days per week (MWF or TTHSa) | IV | Variable | 10-80 days | 🌎 NA |
| Intrauterine infusion | 200-250 mg | Intrauterine | q24h or q48h | 3-7 days | 🌎 NA |
- Phycomycoses and pulmonary mycoses: Administer in 1L D5W at 1 L/hr. Adjust if toxicity occurs.
- Intrauterine infusion: Little science available for recommending doses/diluents.
羊
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible systemic fungal infections (Llama) | 1 mg test dose, then initially at 0.3 mg/kg IV over 4 hours... Subsequent doses were increased by 10 mg and given every 48 hours until reaching 1 mg/kg q48h IV for 6 weeks | IV | q48h | 6 weeks | 🌎 NA |
- Susceptible systemic fungal infections (Llama): Single case report in a Llama (Coccidioidomycosis).
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。
概覽
兩性黴素B (Amphotericin B) 是一種強效的全身性多烯類大環內酯抗黴菌藥物，專門用於治療進行性、有致命危險的黴菌感染（如芽生菌病、組織漿菌病、隱球菌病、球黴菌病）。
由於其口服生物利用度極差，必須經由腸胃外途徑（通常為靜脈注射 IV）給藥。傳統劑型 去氧膽酸兩性黴素B (amphotericin B deoxycholate) 以引起顯著的腎毒性而聞名，這限制了它的使用並需要密集的監測。
較新的脂質體配方（例如微脂體兩性黴素B、兩性黴素B脂質複合體）將藥物包裹在脂質載體中。這些配方的腎毒性顯著較低，允許使用更高的累積劑量，且能更好地穿透組織（如肺、肝和脾），但價格相當昂貴。
臨床要點： 雖然對許多雙相型真菌高度有效，但犬貓的麴菌症 (aspergillosis) 對兩性黴素B的治療反應通常不佳。
作用機制
Amphotericin B is fungistatic or fungicidal depending on the concentration.
It works by binding to sterols—primarily ergosterol—in the fungal cell membrane. This binding creates transmembrane pores → alters membrane permeability → allows intracellular potassium (K+), magnesium, and other vital cellular constituents to leak out → leading to fungal cell death.
Toxicity Mechanism: Mammalian cell membranes contain cholesterol. While amphotericin B has a higher affinity for ergosterol, it still binds to mammalian cholesterol to some degree. This cross-reactivity, particularly in renal epithelial cells, is the primary mechanism behind its dose-limiting nephrotoxicity. It also induces renal vasoconstriction, leading to a decreased glomerular filtration rate (GFR).
安全性與警告
禁忌症
- Patients with known hypersensitivity to amphotericin B (unless the infection is life-threatening and no alternatives exist)
不良反應
- Nephrotoxicity (very common, dose-dependent)
- Anorexia and vomiting
- Hypokalemia and hypomagnesemia
- Distal renal tubular acidosis
- Phlebitis at injection site
- Cardiac arrhythmias
- Non-regenerative anemia
- Fever (can be mitigated with NSAIDs or low-dose steroids)
- Tachycardia, tachypnea, lethargy, restlessness (horses)
- Calcinosis cutis (dogs)
注意事項
Black Box Warning Equivalent: Amphotericin B is highly nephrotoxic. Renal function must be aggressively monitored during therapy.
- Use with extreme caution in patients with pre-existing renal disease.
- Cats are more sensitive to nephrotoxic effects; reduced dosages are often recommended.
- Ensure adequate hydration prior to administration. Sodium loading (e.g., normal saline administration before and after dosing) may help avert renal insufficiency by preventing tubuloglomerular feedback-induced vasoconstriction.
- Pregnancy: Weigh risks vs. benefits. FDA Category B (human); Papich Class A (veterinary).
藥物相互作用
May exacerbate the potassium-losing effects of amphotericin B.
Amphotericin B-induced hypokalemia may exacerbate digoxin toxicity.
In vitro synergy against Cryptococcus and Candida, but may also increase flucytosine toxicity.
Additive renal toxicity; avoid concurrent or sequential use if possible.
Increased risk of severe hypokalemia.
Reconstituting amphotericin B deoxycholate with these solutions may cause precipitation.
Amphotericin B-induced hypokalemia may enhance curariform effects.
Amphotericin may increase the toxic effects of fluorouracil.
Amphotericin may increase the toxic effects of doxorubicin.
Amphotericin may increase the toxic effects of methotrexate.
Concurrent use significantly increases the risk of severe nephrotoxicity.
監測
- BUN and serum creatinine (before each dose or every other day during dose escalation, then at least weekly)
- Serum electrolytes including sodium, potassium, and magnesium (weekly)
- Liver function tests (weekly)
- CBC and Packed Cell Volume (PCV) (weekly)
- Urinalysis (weekly)
- Total plasma protein (TPP) (at least weekly)
- Body weight
藥物動力學
半衰期
吸收
Poorly absorbed from the GI tract; must be given parenterally (IV) for systemic infections.
分佈
Penetrates well into most tissues but poorly into pancreas, muscle, bone, aqueous humor, and pleural/pericardial/synovial/peritoneal fluids unless inflamed. CSF levels are ~3% of serum levels. Highly protein bound (90-95%). Lipid forms have higher penetration into lungs, liver, and spleen.
代謝
Metabolic pathways are not fully known.
排除
Exhibits biphasic elimination. Approximately 2-5% of the drug is recovered in the urine in unchanged (biologically active) form. Can be detected in urine up to 7 weeks after therapy stops.
過量
Acute intravenous overdose reports are rare. Because of the severe toxicity of the drug, dosage calculations and solution preparation procedures must be double-checked.
If an accidental overdose occurs, renal toxicity is the primary concern. Toxicity may be minimized by aggressively administering intravenous fluids and mannitol to maintain GFR and promote diuresis.
可用產品
劑型
- Powder for injection (Deoxycholate)
- Suspension for injection (Lipid complex)
- Powder for injection (Liposomal/Cholesteryl sulfate complex)
- Topical formulations
人用標示
- Amphotericin B Desoxycholate Powder for Injection: 50 mg in vials
- Amphotericin B Lipid-Based Suspension for Injection: 100 mg/20 mL (Abelcet)
- Amphotericin B Lipid-Based Powder for Injection: 50 mg, 100 mg (Amphotec, AmBisome)
- Topical formulations (Fungizone)
各地核准狀態
Human authorized products used under the cascade.
Human authorized products used under the cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store un-reconstituted vials in the refrigerator (2-8°C), protected from light and moisture. Reconstitute with sterile water for injection (no preservatives). After reconstitution, stable for 24 hours at room temperature and 1 week refrigerated if protected from light. When diluted in D5W (pH >4.3) for IV use, protect from light during administration (though studies show potency remains largely unaffected for 8-24 hours of light exposure).
飼主須知
兩性黴素B 是一種強效的抗黴菌藥物，僅用於嚴重、危及生命的黴菌感染。
- 給藥方式： 必須透過注射（通常為靜脈注射）給藥，這通常需要您的寵物住院或頻繁前往診所。
- 腎臟風險： 此藥物對腎臟具有高度毒性。大多數寵物會經歷一定程度的腎臟壓力。我們將頻繁進行血液和尿液檢查，以密切監測腎臟功能。
- 副作用： 請密切觀察寵物是否有嘔吐、食慾不振、極度嗜睡或發燒等生病跡象。如果出現這些情況，請立即聯繫您的獸醫師。
- 費用與承諾： 治療費用可能很高，並且需要投入大量時間進行監測和給藥。
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