替卡西林 / 克拉維酸
Ticarcillin / Clavulanate
Ticarcillin disodium and clavulanate potassium
別名: Timentin · Claventin · BRL-2288 · ticarcillinum natricum · BRL-14151K · kalii clavulanas · Ticarcillin/Clavulanic acid · Ticarcillin potassium clavulanate
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 |
|---|---|---|---|---|---|
| Sepsis | 40-50 mg/kg | IV | q6-8h | — | 🌎 NA |
| Susceptible infections | 15-50 mg/kg | IV, IM or SC | q6-8h | — | 🌎 NA |
| Pseudomonas sepsis/bacteremia | 20-50 mg/kg | IV | q6-8h | — | 🌎 NA |
| Adjunctive treatment of Pseudomonas otitis | 0.5 mL in each ear | topical | twice daily | — | 🌎 NA |
| Serious systemic infections | 15-25 mg/kg followed by CRI at 7.5-15 mg/kg/h | IV | CRI | As directed | 🌍 EU |
| Pseudomonas otitis (adjunct) | 0.25-0.5 ml of a 100 mg/ml injectable ticarcillin solution | topical | q8h | As directed | 🌍 EU |
- Sepsis: Dosed on the basis of ticarcillin content
- Susceptible infections: Dosed on the basis of ticarcillin content
- Pseudomonas sepsis/bacteremia: Dosed on the basis of ticarcillin content
- Adjunctive treatment of Pseudomonas otitis: Using the ticarcillin/clavulanic acid product (Timentin). Dilute according to manufacturer's directions, draw into 2 mL aliquots and freeze. Thaw and use each aliquot.
- Serious systemic infections: Initial bolus followed by continuous rate infusion
- Pseudomonas otitis (adjunct): Instil into the affected ear
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Sepsis | 40-50 mg/kg | IV | q6-8h | — | 🌎 NA |
| Pseudomonas sepsis/bacteremia | 40 mg/kg | IV | q6h | — | 🌎 NA |
| Resistant Pseudomonas infections | 50 mg/kg | IV or IM | 4 times daily | — | 🌎 NA |
| Susceptible infections | 15-50 mg/kg | IV, IM or SC | q6-8h | — | 🌎 NA |
| Serious systemic infections | 15-25 mg/kg followed by CRI at 7.5-15 mg/kg/h | IV | CRI | As directed | 🌍 EU |
| Pseudomonas otitis (adjunct) | 0.25-0.5 ml of a 100 mg/ml injectable ticarcillin solution | topical | q8h | As directed | 🌍 EU |
- Sepsis: Dosed on the basis of ticarcillin content
- Pseudomonas sepsis/bacteremia: Dosed on the basis of ticarcillin content
- Resistant Pseudomonas infections: May need more frequent dosing or constant rate infusion for resistant infections
- Susceptible infections: Dosed on the basis of ticarcillin content
- Serious systemic infections: Initial bolus followed by continuous rate infusion
- Pseudomonas otitis (adjunct): Instil into the affected ear
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible infections | 50 mg/kg | IV | q6h | — | 🌎 NA |
| Neonatal septicemia (Foals) | 40-60 mg/kg | IV or IM | q8h | — | 🌎 NA |
| Susceptible infections (Foals) | 50 mg/kg | IV or IM | q6-8h | — | 🌎 NA |
| Intrauterine infusion | 3-6 grams with a minimum of 200 mL of saline | Intrauterine | every 4-6 h | — | 🌎 NA |
- Susceptible infections: Dosed on the basis of ticarcillin content
- Neonatal septicemia (Foals): Dosed on the basis of ticarcillin content
- Susceptible infections (Foals): Dosed on the basis of ticarcillin content
- Intrauterine infusion: Mares need to be treated frequently in order to maintain drug concentrations above MIC.
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
替卡西林/克拉維酸 (Timentin®) 是一種強效的注射用廣效青黴素（抗綠膿桿菌青黴素），並結合了β-內醯胺酶抑制劑。
- 擴展抗菌譜： 添加克拉維酸可保護替卡西林免受酵素降解，將其療效擴展至產生β-內醯胺酶的大腸桿菌、巴斯德桿菌、葡萄球菌、克雷伯氏菌和變形桿菌。
- 臨床要點： 在獸醫學中，它對綠膿桿菌的療效特別受到重視，通常保留用於嚴重的院內感染、敗血症或菌血症。
- 替代用途： 雖然主要作為全身性醫院用藥，但常被調配成耳藥，用於輔助治療犬隻頑固的綠膿桿菌耳炎。
作用機轉
Ticarcillin is a bactericidal beta-lactam antibiotic:
- Binds to specific Penicillin-Binding Proteins (PBPs) (such as transpeptidases and carboxypeptidases) located inside the bacterial cytoplasmic membrane.
- Inhibits bacterial cell wall mucopeptide synthesis → creates an osmotically unstable spheroplast → leads to cell lysis and death.
Clavulanate Potassium is a "suicide inhibitor":
- Competitively and irreversibly binds to beta-lactamase enzymes (including types II, III, IV, V, and staphylococcal penicillinases).
- Prevents these enzymes from hydrolyzing the beta-lactam ring of ticarcillin, thereby restoring and expanding its antimicrobial spectrum.
- Note: Type I beta-lactamases (often associated with E. coli, Enterobacter, and Pseudomonas) are generally not inhibited by clavulanic acid.
安全性與警告
禁忌症
- Documented hypersensitivity to penicillins or other beta-lactam antibiotics
- Known hypersensitivity to penicillins or other beta-lactam antibiotics
不良反應
- Hypersensitivity reactions (allergic reactions)
- Platelet dysfunction and bleeding (especially at high doses or with renal impairment)
- CNS effects including headache, giddiness, hallucinations, and seizures (at high doses)
- Pain at intramuscular (IM) injection sites
- Phlebitis or local vein irritation (IV administration)
- Antibiotic-associated diarrhea or colitis
- Nausea
- Diarrhoea
- Skin rashes
注意事項
Dosage adjustments should be made in patients with significantly impaired renal function. Patients receiving very high dosages or those with renal impairment are more prone to developing platelet function abnormalities (bleeding) or CNS toxicity. IV administration should be given slowly (over at least 30 minutes) using dilute concentrations to avoid vein irritation.
藥物交互作用
In vitro synergy against certain bacteria; however, penicillins can chemically inactivate aminoglycosides in vitro and in vivo (especially in renal failure or at massive doses). Do not mix in the same syringe or IV line.
Reduces renal tubular secretion of ticarcillin, maintaining higher systemic levels for a longer duration (does not affect clavulanate elimination).
Increased risk of bleeding due to potential ticarcillin-induced platelet dysfunction; use with caution.
Increased risk of bleeding due to potential ticarcillin-induced platelet dysfunction; use with caution.
Mutual inactivation if mixed in the same syringe. However, there is significant synergism in vivo against Pseudomonas when administered separately.
監測
- Clinical efficacy (resolution of clinical signs, WBC count, fever)
- Renal function (in patients with pre-existing impairment)
- Signs of bleeding or CNS abnormalities (if on high doses)
- Clinical signs of infection resolution
- Renal function (in prolonged use)
- Signs of hypersensitivity or adverse gastrointestinal effects
藥物動力學
半衰期
吸收
Ticarcillin is not appreciably absorbed after oral administration. When given IM to humans, peak levels occur in 30-60 minutes. Bioavailability in horses after IM administration is approximately 65%.
分佈
Distributes into pleural fluid, interstitial fluid, bile, sputum, and bone. CSF levels are low (6% of serum) with normal meninges, but increase (39%) with inflammation. Volume of distribution (Vd) is 0.34 L/kg in dogs and 0.22-0.25 L/kg in horses. Crosses the placenta and is found in small quantities in milk.
代謝
In humans, 10-15% of ticarcillin is hydrolyzed to inactive compounds. Clavulanic acid is extensively metabolized in dogs primarily to 1-amino-4-hydroxybutan-2-one.
排除
Ticarcillin is eliminated primarily by the kidneys via tubular secretion and glomerular filtration. Clavulanic acid is excreted unchanged in urine (34-52% in dogs), feces (25-27%), and respired air (16-33%).
過量
A single inadvertent overdose is unlikely to cause significant morbidity. However, very high dosages of parenteral penicillins (especially in patients with underlying renal disease) have induced CNS effects (hallucinations, headaches, seizures) and alterations in platelet function leading to bleeding.
可用產品
劑型
- Powder for injection
- Premixed frozen injection
- Injectable: 3 g ticarcillin and 200 mg clavulanic acid powder for reconstitution
人用標示
- Ticarcillin Disodium Powder for Injection and Clavulanate Potassium: 3 grams ticarcillin and 0.1 gram clavulanic acid in 3.1 gram vials, piggyback bottles, ADD-Vantage vials, 100 mL premixed frozen Galaxy plastic containers, and 31 gram pharmacy bulk packages (Timentin®)
- Ticarcillin Powder for Injection and Clavulanate Potassium: 3 grams ticarcillin and 0.1 gram clavulanic acid/100 mL (Timentin®)
- Timentin 3.2 g (3 g ticarcillin / 200 mg clavulanic acid) powder for injection
各地核准狀態
Human authorized product used under the prescribing cascade for serious infections.
Human authorized product used under the prescribing cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store unused vials at room temperature (below 24°C/75°F). Darkening of powder/solution indicates degradation of clavulanate. Reconstituted solutions (200 mg/mL) are stable for 6 hours at room temperature and 72 hours refrigerated. Diluted IV solutions (10-100 mg/mL) vary in stability; thawed solutions must be used within 8 hours and not refrozen.
飼主須知
注意： 此藥物主要作為注射劑在醫院內用於治療嚴重、危及生命的感染。
- 調配耳藥滴劑： 如果您的獸醫開立此藥作為治療頑固綠膿桿菌感染的調配耳藥，請將分裝的藥劑（注射器/小瓶）冷凍保存直到需要使用。請依照指示在每次使用前才解凍單次劑量。
- 副作用： 請注意過敏反應的跡象（面部腫脹、蕁麻疹、呼吸困難）或嚴重腹瀉，若發生這些情況請立即聯繫您的獸醫。
- 出血風險： 在極少數情況下，此藥物可能會影響血液凝固。若發現任何異常的瘀傷或出血，請告知獸醫。
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