妥布黴素
Tobramycin
Tobramycin sulfate
別名: TOBI · Brulamycin · Gernebcin · Mytobrin · Tobrex · tobramycin sulphate · Tobramycinum
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 |
|---|---|---|---|---|---|
| General susceptible infections | 2 mg/kg | IV, IM, SC | q8h | — | 🌎 NA |
| Susceptible UTI | 1-2 mg/kg | SC | q8h | — | 🌎 NA |
| Sepsis | 2-4 mg/kg | IV | q8h | — | 🌎 NA |
| Soft tissue, systemic infections | 1-1.7 mg/kg IV q8h or 3-5.1 mg/kg IV q24h | IV | q8h or q24h | < 7 days | 🌎 NA |
| Systemic infections | 2 mg/kg SC q8-12h or 4-6 mg/kg SC q24h | SC | q8-12h or q24h | < 7 days | 🌎 NA |
| Persistent bacteremia | 3-5 mg/kg IV, IM, SC q8h or 9-15 mg/kg IV, IM or SC q24h | IV, IM, SC | q8h or q24h | <= 7 days | 🌎 NA |
| Gram-negative infections | 4-6 mg/kg | IV/IM/SC | q24h | Assess according to clinical response | 🌍 EU |
- General susceptible infections: Avoid use or reduce dosage in patients with renal failure; recommend therapeutic drug monitoring, particularly in young animals. Consider consolidating to once-daily dosing (e.g., 6 mg/kg q24h).
- Gram-negative infections: For severe infections (including sepsis), doses as high as 12 mg/kg/day have been advocated, but should be used with caution given potential adverse effects.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General susceptible infections | 2 mg/kg | IV, IM, SC | q8h | — | 🌎 NA |
| Susceptible UTI | 1-2 mg/kg | SC | q8h | — | 🌎 NA |
| Sepsis | 2-4 mg/kg | IV | q8h | — | 🌎 NA |
| Soft tissue, systemic infections | 2 mg/kg IV, IM or SC q12h or 4 mg/kg IV, IM, SC q24h | IV, IM, SC | q12h or q24h | <= 5 days | 🌎 NA |
| Persistent bacteremia | 2 mg/kg IV, IM, SC q8h or 6 mg/kg IV, IM or SC q24h | IV, IM, SC | q8h or q24h | <= 5 days | 🌎 NA |
| Gram-negative infections | 4-6 mg/kg | IV/IM/SC | q24h | Assess according to clinical response | 🌍 EU |
- General susceptible infections: Consider consolidating to once-daily dosing.
- Gram-negative infections: Cats may be more sensitive to toxicity. For severe infections (including sepsis), doses as high as 12 mg/kg/day have been advocated, but should be used with caution.
小型哺乳類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections (Llamas) | 4 mg/kg IV q24h; 0.75 mg/kg IV q8h | IV | q8h or q24h | — | 🌎 NA |
- Susceptible infections (Llamas): Dosing specifically for Llamas.
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections | 5 mg/kg | IM | q12h | — | 🌎 NA |
| Susceptible infections | 2.5-5 mg/kg/day | Parenteral | Daily | — | 🌎 NA |
爬蟲類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections | 2.5 mg/kg | IM | q24h | — | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections | 4 mg/kg | IV | q24h | — | 🌎 NA |
- Susceptible infections: Allows achievement of Cmax/MIC ratio higher than 10 for pathogen strains with a MIC of 1 microgram/mL.
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
妥布黴素是一種強效的非腸道給藥氨基醣苷類抗生素,主要用於治療嚴重的革蘭氏陰性需氧菌感染。
主要臨床特徵:
- 抗菌譜: 對需氧革蘭氏陰性桿菌(如綠膿桿菌、大腸桿菌、克雷伯氏菌、變形桿菌)及部分需氧革蘭氏陽性菌(如葡萄球菌)高度有效。對厭氧菌和真菌無效。
- 臨床應用: 由於其固有的毒性,全身性使用通常保留用於其他毒性較低的抗生素無效的嚴重、危及生命的感染,或用於治療已知的抗慶大黴素菌株。
- 毒性特徵: 與所有氨基醣苷類藥物一樣,具有顯著的腎毒性和耳毒性風險。部分實驗室證據表明其腎毒性可能略低於慶大黴素,但臨床上仍有爭議。
臨床要點: 氨基醣苷類藥物表現出濃度依賴性殺菌活性和顯著的抗生素後效應 (PAE)。這種藥代動力學/藥效學特徵強烈支持現代的高劑量、延長間隔(每日一次)給藥方案。這種方法最大化了用於殺菌的 $C_{max}$/MIC 比值,同時提供了一個無藥物間隔期,使腎小管細胞能夠清除藥物,從而將腎毒性降至最低。
作用機轉
Tobramycin is a bactericidal antibiotic that disrupts bacterial protein synthesis.
- Cellular Entry: The drug enters the bacterial cell via an oxygen-dependent active transport mechanism.
Note: Because this transport requires oxygen, aminoglycosides are completely ineffective against obligate anaerobic bacteria and have reduced efficacy in anaerobic environments (e.g., abscesses, necrotic tissue).
- Target Binding: Once inside, tobramycin irreversibly binds to the 30S ribosomal subunit.
- Mechanism: Binding → misreading of mRNA → incorporation of incorrect amino acids into the growing peptide chain → production of non-functional or toxic proteins → bacterial cell death.
- Environmental Factors: Antimicrobial activity is significantly enhanced in an alkaline environment and diminished in acidic, purulent conditions.
安全性與警告
禁忌症
- Known hypersensitivity to aminoglycosides
- Rabbits and hares (causes fatal disruption of GI flora)
- Pre-existing severe renal disease (unless benefits outweigh risks)
- Dehydration
- Corneal ulceration (specifically for ophthalmic preparations)
不良反應
- Nephrotoxicity (acute tubular necrosis)
- Ototoxicity (vestibular and auditory damage, potentially irreversible)
- Facial edema
- Pain or inflammation at the injection site
- Peripheral neuropathy
- Hypersensitivity reactions
- Rarely: GI signs, hematologic, and hepatic effects
- Neuromuscular blockade (rare)
注意事項
Extreme Caution Required:
- Renal Impairment: Use with extreme caution in patients with preexisting renal disease. Dosage intervals must be extended, and therapeutic drug monitoring is highly recommended.
- Risk Factors: Neonatal and geriatric patients, fever, sepsis, and dehydration significantly increase the risk of toxicity.
- Working Dogs: Use cautiously in working dogs (e.g., seeing-eye, herding, hearing-assistance dogs) due to the risk of irreversible ototoxicity (deafness or vestibular dysfunction).
- Neuromuscular Disorders: Avoid or use with extreme caution in patients with myasthenia gravis or other neuromuscular disorders due to the drug's neuromuscular blocking activity.
- Feline Sensitivity: Cats appear to be particularly sensitive to the vestibular toxic effects of aminoglycosides.
藥物交互作用
Synergistic antibacterial effects in vivo; however, can cause physical inactivation of aminoglycosides if mixed in the same syringe or IV line, or in vivo in patients with severe renal failure.
Potential for additive nephrotoxicity (historically documented with older generation cephalosporins like cephalothin).
Increased risk of nephrotoxicity and ototoxicity.
Increased risk of nephrotoxicity and ototoxicity.
Significantly increased risk of acute kidney injury.
Concomitant use can potentiate and prolong neuromuscular blockade, potentially leading to respiratory paralysis.
Increased risk of nephrotoxicity
Increased risk of ototoxicity and nephrotoxicity
In vitro chemical inactivation if mixed
Enhanced non-depolarizing neuromuscular blockade
監測
- Clinical efficacy (resolution of fever, improved clinical signs, negative follow-up cultures)
- Renal toxicity: Baseline and serial urinalysis (monitoring for tubular casts, which are often the first sign of impending toxicity), urine specific gravity, serum creatinine, and BUN
- Gross monitoring for vestibular toxicity (head tilt, nystagmus, ataxia) or auditory toxicity (deafness)
- Therapeutic drug monitoring (peak and trough serum levels) is highly recommended to ensure efficacy and prevent toxicity
- Urinalysis (daily, looking for cellular casts as an early warning)
- Serum creatinine and BUN (baseline and periodically)
- Hydration status and urine output
- Auditory and vestibular function
藥物動力學
半衰期
吸收
Not appreciably absorbed after oral or intrauterine administration. Absorbed from topical administration during surgical irrigations. Bioavailability from extravascular injection (IM or SC) is >90%. SC injection results in slightly delayed peak levels compared to IM.
分佈
Distributed primarily in the extracellular fluid. Found in ascitic, pleural, pericardial, peritoneal, synovial, and abscess fluids. High levels in sputum, bronchial secretions, and bile. Minimally protein bound (<20%). Does not readily cross the blood-brain barrier or penetrate ocular tissue. Crosses the placenta (fetal concentrations 15-50% of maternal serum). Accumulates in inner ear and kidneys. Volume of distribution (horses): 0.24-0.55 L/kg.
代謝
Aminoglycosides are not significantly metabolized.
排除
Eliminated almost entirely by glomerular filtration. Clearance (horses): 101-130 mL/kg/hr. Patients with decreased renal function can have significantly prolonged half-lives.
過量
In the event of an inadvertent overdose, rapid intervention is required to prevent permanent renal and otic damage:
- Hemodialysis: Highly effective in reducing serum levels of the drug, though rarely available in veterinary practice.
- Peritoneal Dialysis: Can reduce serum levels but is significantly less efficacious than hemodialysis.
- Drug Complexation: Intravenous administration of carbenicillin or ticarcillin (12-20 grams/day in humans) can complex with tobramycin in the blood, inactivating it. This is reportedly nearly as effective as hemodialysis.
可用產品
劑型
- Injection solution
- Powder for injection
- Inhalation solution
- Ophthalmic preparations
- Injectable: 40 mg/ml solution
獸醫用
- Tobramycin 40 mg/ml injectable solution
人用標示
- Tobramycin Sulfate Injection: 0.8 mg/mL and 1.2 mg/mL in single-dose containers
- Tobramycin Sulfate Solution for Injection: 10 mg/mL and 40 mg/mL
- Tobramycin Sulfate Powder for Injection: 1.2 grams (40 mg/mL after reconstitution)
- Tobramycin Solution for inhalation: 60 mg/mL (TOBI)
- Nebcin 40 mg/ml injectable solution
各地核准狀態
POM (Prescription Only Medicine)
POM-V
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at room temperature (15-30°C); avoid freezing and temperatures above 40°C. Do not use the product if discolored.
飼主須知
妥布黴素是一種保留用於嚴重感染的強效抗生素。由於其藥效強大,需要仔細監測以確保您寵物的安全。
- 給藥方式: 如果指示您在家中進行皮下注射,請確保您完全了解正確的注射技巧和給藥時間表。切勿給予超過處方劑量的藥物。
- 潛在風險: 此藥物具有引起腎臟損傷和聽力或平衡問題(耳毒性)的風險。
- 注意事項: 如果您發現以下任何情況,請立即聯繫您的獸醫:
- 排尿習慣改變(喝水變多、尿量增加或減少)
- 失去平衡、絆倒、頭部傾斜或眼球異常運動
- 明顯的聽力喪失或對聲音無反應
- 嗜睡、嘔吐或食慾不振
- 回診追蹤: 請務必按時進行血液和尿液檢查。這些檢查對於在發生永久性損傷之前及早發現腎臟壓力的早期跡象至關重要。
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