チカルシリン / クラブラン酸
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
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 |
|---|---|---|---|---|---|
| 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
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
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
チカルシリン/クラブラン酸（Timentin®）は、強力な注射用広域ペニシリン（抗緑膿菌ペニシリン）にβ-ラクタマーゼ阻害薬を配合した薬剤です。
- 抗菌スペクトルの拡大： クラブラン酸の添加によりチカルシリンが酵素による分解から保護され、β-ラクタマーゼを産生する大腸菌、パスツレラ属、ブドウ球菌属、クレブシエラ、プロテウスに対する有効性が拡大します。
- 臨床的ポイント： 獣医学においては、緑膿菌に対する有効性が特に評価されており、重度の院内感染、敗血症、菌血症のためにしばしば温存されます。
- 代替用途： 主に全身用の院内薬剤ですが、犬の難治性緑膿菌性外耳炎の補助治療として、点耳薬として調剤されることがよくあります。
作用機序
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・警告
禁忌
- Documented hypersensitivity to penicillins or other beta-lactam antibiotics
- Known hypersensitivity to penicillins or other beta-lactam antibiotics
有害事象
- 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.
医薬品相互作用
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.
監視
- 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
薬物動態
半減期
吸収
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%.
分布
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.
消失
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%).
過剰投与
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.
製品
製剤
- Powder for injection
- Premixed frozen injection
- Injectable: 3 g ticarcillin and 200 mg clavulanic acid powder for reconstitution
ヒト用医薬品
- 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
規制ステータス
Human authorized product used under the prescribing cascade for serious infections.
Human authorized product used under the prescribing cascade.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
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.
飼主向け情報
注意： この薬は主に、重度で生命を脅かす感染症に対して病院内で注射薬として使用されます。
- 調剤点耳薬： 獣医師が難治性の緑膿菌感染症の治療のためにこの薬を点耳薬として処方した場合、小分けにされた薬（シリンジ/バイアル）は必要になるまで冷凍保存してください。指示に従い、使用の直前に1回分ずつ解凍してください。
- 副作用： アレルギー反応の兆候（顔の腫れ、じんましん、呼吸困難）や重度の下痢に注意し、これらが発生した場合は直ちに獣医師に連絡してください。
- 出血リスク： まれに、この薬は血液の凝固に影響を与えることがあります。異常な内出血や出血が見られた場合は報告してください。
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