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頭孢噻肟

Cefotaxime

Cefotaxime sodium

抗生素 - 第三代頭孢菌素IVIMSCRegional perfusionNebulization爬蟲類

別名: Claforan · cefotaximum natricum · CTX · HR-756 · RU-24756

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

WHO 極重要抗生素請謹慎使用,避免不必要的處方
22 mg/kg IV, IM or SC q8h for 7 days or less or 50 mg/kg IV or IM q12h for 7 days or lessIV, IM, SC· q8h or q12h· 7 days or less
🐕

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。

各物種劑量

🌎 NA — North America🌍 EU — Europe

適應症劑量途徑頻次療程地區
Soft tissue infections22 mg/kg IV, IM or SC q8h for 7 days or less or 50 mg/kg IV or IM q12h for 7 days or lessIV, IM, SCq8h or q12h7 days or less🌎 NA
Orthopedic infections20-40 mg/kg IV, IM or SC q6-8h for 7 days or lessIV, IM, SCq6-8h7 days or less🌎 NA
Severe bacteremia20-80 mg/kg IV q6h or 10-50 mg/kg IV q4-6h for as long as necessaryIVq4-6hAs long as necessary🌎 NA
Susceptible infections25-50 mg/kg IV, IM or SC q8hIV, IM, SCq8h🌎 NA
Sepsis20-80 mg/kg IV, IM q8hIV, IMq8h🌎 NA
CNS infections (spinal cord)25 mg-50 mg/kg IV, IM q8hIV, IMq8h🌎 NA
Acute sepsis or serious susceptible infections40-50 mg/kgIV/IM/SCq8hUntil clinical resolution🌍 EU
Susceptible infections10-20 mg/kgIV/IM/SCq12hUntil clinical resolution🌍 EU
  • Acute sepsis or serious susceptible infections: Standard recommended dose.
  • Susceptible infections: Lower dose suggested by some authors to have good clinical efficacy.

適應症劑量途徑頻次療程地區
Severe bacteremia20-80 mg/kg IV or IM q6h as long as necessaryIV, IMq6hAs long as necessary🌎 NA
Susceptible infections25-50 mg/kg IV, IM or SC q8hIV, IM, SCq8h🌎 NA
Sepsis20-80 mg/kg IV, IM q8hIV, IMq8h🌎 NA
CNS infections (spinal cord)25 mg-50 mg/kg IV, IM q8hIV, IMq8h🌎 NA
To prevent bacterial colonization of pancreas in severe pancreatitis, anorexia, or SIRS50 mg/kg IM q8hIMq8h🌎 NA
Acute sepsis or serious susceptible infections40-50 mg/kgIV/IM/SCq8hUntil clinical resolution🌍 EU
  • Acute sepsis or serious susceptible infections: Standard recommended dose.

適應症劑量途徑頻次療程地區
Susceptible infections (most birds)50-100 mg/kg IM three times a dayIMTID🌎 NA
Bacterial infections, bacterial hepatitis75-100 mg/kg IM or IV q4-8hIM, IVq4-8h🌎 NA
Susceptible infections in ratites (young birds)25 mg/kg IM 3 times dailyIMTID🌎 NA
Susceptible infections75 mg/kg IM q8hIMq8h🌎 NA
  • Susceptible infections (most birds): May be used with aminoglycosides, but nephrotoxicity may occur. Reconstituted vial good for 13 weeks if frozen.

爬蟲類

適應症劑量途徑頻次療程地區
Susceptible infections20-40 mg/kg IM once daily for 7-14 daysIMq24h7-14 days🌎 NA
Susceptible infections in chelonians20-40 mg/kg IM q24hIMq24h🌎 NA
Nebulized antibiotic therapy100 mg twice dailyNebulizationBID🌎 NA

適應症劑量途徑頻次療程地區
Susceptible infections in foals40 mg/kg IV q6hIVq6h🌎 NA
Meningitis in foals40 mg/kg IV 3-4 times a dayIV3-4 times a day🌎 NA
Systemic therapy in foals20-30 mg/kg IV or IM q6-8hIV, IMq6-8h🌎 NA
Regional perfusion for adjunctive treatment of septic arthritis in foals1 gram cefotaxime in 20 mL of saline. Tourniquet above and below joint. Inject antibiotic solution and leave tourniquet in place for 20 minutes.Regional perfusionOnce20 minutes🌎 NA

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概覽

頭孢噻肟是一種​第三代注射用頭孢菌素​抗生素,對革蘭氏陽性菌和革蘭氏陰性菌均具有廣泛的抗菌活性。

主要臨床特徵包括:

  • ​擴展的革蘭氏陰性菌覆蓋範圍​:對腸桿菌科(如克雷伯氏菌、大腸桿菌、沙門氏菌、變形桿菌)高度有效。
  • ​抗厭氧菌活性​:對許多厭氧菌有效,包括脆弱擬桿菌和梭狀芽孢桿菌屬。
  • ​中樞神經系統穿透力​:與第一代和多數第二代頭孢菌素不同,當腦膜發炎時,頭孢噻肟能在​腦脊髓液 (CSF)​ 中達到治療濃度,使其成為治療細菌性腦膜炎和脊髓感染的重要選擇。
  • ​給藥方式​:因口服吸收不佳,必須經腸胃外途徑(靜脈、肌肉、皮下)給藥。靜脈注射應緩慢進行(超過3-5分鐘)以減少不良反應。

​臨床要點​:雖然它對許多革蘭氏陰性需氧菌具有優異的活性,但對綠膿桿菌的療效不一,臨床效果通常不如預期。進行紙片擴散法藥敏試驗時,應使用30微克的頭孢噻肟紙片。

作用機制

Cefotaxime is a time-dependent, bactericidal antibiotic.

  • Mechanism: It binds to specific ​penicillin-binding proteins (PBPs)​ located inside the bacterial cell wall → inhibits the third and final stage of bacterial cell wall peptidoglycan synthesis → leads to cell lysis and death mediated by bacterial cell wall autolytic enzymes (autolysins).
  • Metabolism: It is partially metabolized in the liver to desacetylcefotaxime, an active metabolite that works synergistically with the parent compound to enhance antibacterial activity.

安全性與警告

禁忌症

  • Patients with a documented history of hypersensitivity to cephalosporins

不良反應

  • Pain at the IM injection site
  • Thrombophlebitis (after IV administration)
  • Hypersensitivity reactions (rashes, fever, eosinophilia, anaphylaxis)
  • Antibiotic-associated diarrhea (alteration of gut flora)
  • Sterile abscesses or local tissue reactions
  • Rarely: Nephrotoxicity, neurotoxicity (at high doses), neutropenia, agranulocytosis, thrombocytopenia, hepatitis

注意事項

Use with caution in patients with documented hypersensitivity to other beta-lactam antibiotics (e.g., penicillins, carbapenems) due to potential cross-reactivity (estimated 1-15% in humans). Dosage adjustments may be necessary in patients with renal failure. May cause false-positive direct Coombs' tests, falsely elevated 17-ketosteroid urine values, and false-positive urine glucose determinations when using cupric sulfate solution tests (e.g., Clinitest).

藥物相互作用

Aminoglycosides / Nephrotoxic drugs (e.g., amphotericin B)

Potential for additive nephrotoxicity. In vitro studies show synergistic antibacterial activity, but they must NOT be mixed in the same syringe or fluid bag.

Probenecid

Competitively blocks the renal tubular secretion of cefotaxime, significantly increasing its serum levels and prolonging its elimination half-life.

OxytetracyclineModerate

Bacteriostatic agents may antagonize the bactericidal activity of cephalosporins.

ErythromycinModerate

Bacteriostatic agents may antagonize the bactericidal activity of cephalosporins.

AminoglycosidesMinor

Synergistic antibacterial effect, but do not mix in the same syringe due to chemical incompatibility.

Amphotericin BMajor

Increased risk of nephrotoxicity.

FurosemideMajor

Loop diuretics may increase the risk of nephrotoxicity when used with cephalosporins.

監測

  • Clinical efficacy (resolution of infection signs)
  • Renal function parameters (BUN, creatinine, urinalysis) in compromised patients or those on concurrent nephrotoxic drugs

藥物動力學

半衰期

~1 hour45 minutes (IV), 50 minutes (IM), 103 minutes (SC)

吸收

Not appreciably absorbed after oral administration; must be given parenterally. Bioavailability is approximately 87-98% after IM injection and ~100% after SC injection.

分佈

Widely distributed in body tissues including bone, prostatic fluid, aqueous humor, bile, ascitic, and pleural fluids. Enters the CSF in therapeutic levels when meninges are inflamed. Crosses the placenta (activity in amniotic fluid equals or exceeds maternal serum) and distributes into milk in low concentrations. Protein binding is 13-40% in humans. Volume of distribution at steady state in dogs is 480 mL/kg.

代謝

Partially metabolized by the liver to desacetylcefotaxime, which exhibits some antibacterial activity. This is further degraded to inactive metabolites.

排除

Primarily excreted in the urine via tubular secretion. Total body clearance is 10.5 mL/min/kg in dogs and ~3 mL/min/kg in cats.

過量

Acute cephalosporin overdoses are unlikely to cause significant life-threatening problems. However, massive overdoses may exacerbate adverse effects, potentially leading to neurotoxicity (seizures, encephalopathy), nephrotoxicity, or severe gastrointestinal upset. Treatment should consist of standard supportive care and monitoring.

可用產品

劑型

  • Powder for injection
  • Premixed frozen injection solution

人用標示

  • Cefotaxime Sodium Powder for Injection: 500 mg, 1 g, 2 g, & 10 g in vials, bottles, infusion bottles & ADD-Vantage system vials
  • Cefotaxime Sodium for Injection: 1 g & 2 g in infusion bottles, & premixed, frozen 50 mL

各地核准狀態

European Union✗ 未核准處方藥EMA

Classified as a highest priority critically important antibiotic. Use is heavily restricted to cases where no other appropriate licensed veterinary medicine exists and culture/susceptibility testing justifies its use.

United Kingdom✗ 未核准處方藥VMD

Subject to strict antimicrobial stewardship guidelines.

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Sterile powder for injection should be stored at temperatures < 30°C and protected from light. Commercially available frozen injections should be stored at < -20°C. Powder or solutions may darken depending on storage conditions, which may indicate a loss in potency. Cefotaxime is unstable in solutions with a pH > 7.5 (e.g., sodium bicarbonate).

飼主須知

頭孢噻肟是一種強效的注射用抗生素,通常在獸醫院內用於治療嚴重的感染。

  • ​給藥方式​:因為它無法透過腸胃道吸收,必須以注射方式(靜脈、肌肉或皮下)給予。
  • ​副作用​:肌肉注射可能會引起疼痛。請觀察注射部位是否有腫脹、發紅或疼痛的跡象。
  • ​過敏反應​:如果您的寵物過去曾對青黴素或其他頭孢菌素類藥物有過敏反應,請立即告知您的獸醫師。
  • ​腸胃不適​:與許多抗生素一樣,它可能會改變腸道內的正常菌叢,偶爾會導致腹瀉。如果腹瀉變得嚴重或帶血,請聯繫您的獸醫師。

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