硫酸慶大黴素
Gentamicin Sulfate
Gentamicin sulfate
別名: Gentocin · Garamycin · Amtech Gentamax 100 · Gentafuse · Gentaved · Gentozen · Legacy · Garasol · Garacin · Gen-Gard · Clinagel Vet · Easotic · Otomax · Tiacil · Genticin · gentamicin sulphate · gentamicini sulfas · NSC-82261 · Sch-9724 · Gentamicine · Gentamycin
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
經審核的 v13 劑量證據
結構化劑量計算證據Susceptible infections (extra-label)
須由已驗證獸醫確認
- q24h
NA
必須同時考慮的臨床上下文 (3)
- NOTE: Most infectious disease clinicians agree that aminoglycosides should be dosed once a day in most patients (mammals) with uncompromised renal function. This dosing regimen yields higher peak levels with resultant greater bacterial kill, and as aminoglycosides exhibit a postantibiotic effect, surviving susceptible bacteria generally do not replicate as rapidly even when antibiotic concentrations are below MIC. Periods where levels are low may decrease the adaptive resistance (bacteria take up less drug in the presence of continuous exposure) that can occur. Once-daily dosing may also decrease the toxicity of aminoglycosides, as lower urinary concentrations may mean less uptake into renal tubular cells.
- ■ Therapeutic drug monitoring (TDM) when possible in patients with uncompromised renal function; highly recommended for patients with risk factors for nephrotoxicity. Peak and trough levels are determined through samples collected 30 minutes after administration (peak) and immediately before administration of the next dose (trough). Generally, peak levels (≈30 to 60 minutes post IV dose) should be greater than 32 μg/mL and trough levels less than 1 – 2 μg/mL. 34 A clinical laboratory may be able to assist in sample-time determination and dosage amount and frequency adjustment.
- Gentamicin sulfate for injection and the oral solution should be stored at room temperature (15°C-30°C [59°F-86°F]); freezing or temperatures above 40°C (104°F) should be avoided. The soluble powder should be stored from 2°C to 30°C (46°F-86°F). Do not store or offer medicated drinking water in rusty containers or the drug may be destroyed.
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
慶大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。
主要藥理特徵包括：
- 抗菌譜：對革蘭氏陰性需氧菌（如大腸桿菌、克雷伯氏菌、變形桿菌、假單胞菌、沙門氏菌）及部分葡萄球菌具有優異的抗菌活性。對厭氧菌、真菌和病毒無效。
- 濃度依賴型殺菌活性：其療效取決於達到相對於病原體最低抑菌濃度（MIC）的高血清峰值濃度。
- 抗生素後效應（PAE）：即使藥物濃度降至MIC以下，細菌生長仍會受到抑制，這支持了現代的每日一次給藥方案。
- 毒性特徵：由於具有顯著的腎毒性和耳毒性風險，全身性使用通常僅限於其他毒性較低的替代藥物無效的嚴重感染。
臨床要點：毒性風險因素包括原發性腎臟疾病、年齡（新生兒和老年動物）、發燒、敗血症和脫水。貓對前庭（耳毒性）的影響特別敏感。
作用機制
Gentamicin is a concentration-dependent bactericidal antibiotic.
- Mechanism: It actively transports across the bacterial cell membrane via an oxygen-dependent mechanism → irreversibly binds to the 30S ribosomal subunit → causes misreading of mRNA → inhibits bacterial protein synthesis, leading to cell death.
- Environmental Factors: Antimicrobial activity is significantly enhanced in an alkaline environment and inhibited in acidic, purulent, or necrotic environments.
- Resistance: Because the transport mechanism requires oxygen, anaerobic bacteria are inherently resistant to all aminoglycosides.
安全性與警告
禁忌症
- Known hypersensitivity to aminoglycosides
- Use with extreme caution in preexisting renal disease
- Use with caution in working dogs (e.g., seeing-eye, herding, hearing-impaired assistance dogs) due to irreversible ototoxicity
- Use with caution in patients with neuromuscular disorders (e.g., myasthenia gravis)
- Do not use in animals with botulism
- Use with caution in rabbits (adversely affects GI flora)
- Use with caution in neonates, geriatrics, and dehydrated patients
- Perforated tympanum (for aural preparations)
- Concurrent use of other nephrotoxic drugs
- Systemic use exceeding 7 days
- Pregnancy
不良反應
- Nephrotoxicity (tubular necrosis)
- Ototoxicity (auditory and vestibular; cats are highly sensitive to vestibular effects)
- Facial edema
- Pain or inflammation at the injection site
- Peripheral neuropathy
- Hypersensitivity reactions
- Rarely: GI signs, hematologic, and hepatic effects
- Nephrotoxicity (acute tubular necrosis)
- Neuromuscular blockade (rare)
- Delayed epithelial healing of corneal ulcers (ophthalmic use)
- Local irritation
注意事項
Aminoglycosides are eliminated primarily through renal mechanisms; use cautiously with serum monitoring and dosage adjustments in neonatal or geriatric animals. Sighthound dogs have significantly smaller volumes of distribution and may require reduced dosages. IM injections in horses can cause muscle irritation; IV is preferred. Monitor for antibiotic-associated diarrhea/colitis in horses (may promote Beta-2 toxin production by C. perfringens).
藥物相互作用
Synergistic effects against some bacteria; however, potential for in vitro inactivation of aminoglycosides (do not mix in the same syringe/bag) and in vivo inactivation in patients with renal failure.
Potential additive nephrotoxicity (well documented with older cephalosporins like cephalothin).
Concurrent use may increase the nephrotoxic or ototoxic potential of aminoglycosides.
Increased risk for nephrotoxicity.
Concomitant use could potentiate neuromuscular blockade.
Increased risk of nephrotoxicity and ototoxicity
Increased risk of nephrotoxicity and ototoxicity
In vitro chemical inactivation (do not mix in same syringe)
Enhanced neuromuscular blockade
監測
- Clinical efficacy (resolution of clinical signs, negative cultures)
- Renal toxicity: Baseline and ongoing urinalysis (casts in urine are often the initial sign of impending nephrotoxicity), serum BUN, and creatinine
- Gross monitoring for vestibular (balance) or auditory (hearing) toxicity
- Therapeutic Drug Monitoring (TDM): Serum levels drawn at 1, 2, and 4 hours post-dose. Peak should be >20 mcg/mL; 4-hour trough should be <10 mcg/mL
- Urinalysis (monitor for cellular casts as an early indicator of tubular damage)
- Serum creatinine and BUN
- Hydration status
- Therapeutic Drug Monitoring (TDM): Peak >20 μg/ml, Trough <1 μg/ml
- 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%. Peak levels occur 0.5 to 1 hour after IM administration.
分佈
Distributed primarily in extracellular fluid. Accumulates in inner ear and kidneys. Minimal protein binding (<20%). Does not readily cross the blood-brain barrier or penetrate ocular tissue. Vd is 0.15-0.3 L/kg in adult dogs/cats, and 0.26-0.58 L/kg in horses. Crosses the placenta.
代謝
Not significantly metabolized.
排除
Eliminated almost entirely by glomerular filtration. Patients with decreased renal function can have significantly prolonged half-lives.
過量
In the event of an inadvertent overdose, three treatments are recommended:
- Hemodialysis: Very effective in reducing serum levels, but rarely a viable option in veterinary medicine.
- Peritoneal dialysis: Reduces serum levels but is much less effective than hemodialysis.
- Complexation: Administration of ticarcillin (12-20 g/day in humans) is reportedly nearly as effective as hemodialysis in complexing and deactivating the drug.
可用產品
劑型
- Injection (100 mg/mL, 40 mg/mL, 10 mg/mL, 5 mg/mL, etc.)
- Oral solution (5 mg/mL)
- Soluble powder
- Ophthalmic preparations
- Otic preparations
- Topical preparations
- Injectable solution: 40 mg/ml, 100 mg/ml
- Ophthalmic gel: 0.3% w/w
- Ophthalmic drops: 0.5% w/v
- Aural drops/ointment: Combination products (e.g., with miconazole/hydrocortisone or clotrimazole/betamethasone)
獸醫用
- Gentamicin Sulfate Injection: 100 mg/mL (horses, poultry)
- Gentamicin Sulfate Injection: 5 mg/mL (piglets)
- Gentamicin Sulfate Oral Solution: 5 mg/mL (swine)
- Gentamicin Soluble Powder: 333.33 mg/g and 2 g/30 g (swine)
- Ophthalmic, otic, and topical preparations
- Clinagel Vet (Ophthalmic)
- Easotic (Aural combination)
- Genta (100 mg/ml Injectable)
- Otomax (Aural combination)
- Tiacil (Ophthalmic)
人用標示
- Gentamicin Sulfate Injection: 40 mg/mL, 10 mg/mL, 0.8 mg/mL, 0.9 mg/mL, 1 mg/mL, 1.2 mg/mL, 1.4 mg/mL, 1.6 mg/mL
- Topical, otic, and ophthalmic preparations
- Genticin (40 mg/ml Injectable)
各地核准狀態
POM-V / POM status
POM-V / POM status
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store injection and oral solutions at room temperature (15-30°C); avoid freezing or temperatures above 40°C. Store soluble powder from 2-30°C. Do not store or offer medicated drinking water in rusty containers, as the drug may be destroyed.
飼主須知
慶大黴素是一種保留用於嚴重感染的強效抗生素。
- 給藥方式：如果您被指示在家中進行皮下注射，請確保您已接受獸醫團隊的適當訓練。
- 毒性風險：此藥物具有顯著的腎臟損傷（腎毒性）和聽力/平衡問題（耳毒性）風險。
- 注意事項：如果您發現寵物飲水量異常增加、排尿頻率增加或減少、嘔吐、食慾不振、出現耳聾跡象，或表現出頭部傾斜、絆倒或失去平衡，請立即聯繫您的獸醫。
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