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戊酮可可鹼

Pentoxifylline

1-(5-oxohexyl)-3,7-dimethylxanthine

血液流變學改善劑 / 免疫調節劑POIV狗貓馬

別名: Trental · BL-191 · oxpentifylline · pentoxifyllinum · Oxypentifylline

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

Inflammatory/autoimmune dermatologic conditions (extralabel)

8–10 mg/kgPO
  • q8-12h

NA

必須同時考慮的臨床上下文 (4)
  • NOTE: The commercially available pentoxifylline product is a 400 mg extended-release tablet. Cutting or crushing the tablets may negate the extended-release characteristics and alter pharmacokinetics but splitting tablets may be necessary to administer or accurately dose. Avoid crushing tablets for small animal use.
  • ■ Give this medicine with food.
  • ■ Extended-release tablets can be split if necessary to give the appropriate dose. Crushing the tablets may increase the risk for side effects and should be avoided when possible.
  • The commercially available tablets should be stored in well-closed containers, protected from light at 20°C to 25°C (68°F -77°F).
formulary方案年份 2023審核 dose-audit-plumb-v13

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概覽

戊酮可可鹼是一種合成的​甲基黃嘌呤衍生物​（結構上與茶鹼和咖啡因相關），具有獨特的血液流變學改善及免疫調節特性。

  • ​犬​：主要用於治療伴隨微血管受損的免疫介導性皮膚疾病，如​家族性犬皮肌炎​、耳廓邊緣皮脂漏/壞死及皮膚血管炎（如阿拉巴馬腐爛病）。也可作為異位性皮膚炎的輔助療法，並正被研究用於擴張性心肌病（DCM）。
  • ​馬​：作為皮膚血管炎、內毒素血症、舟狀骨病及胎盤炎的輔助治療。
  • ​貓​：偶爾與潑尼松龍（prednisolone）併用，以減輕與貓傳染性腹膜炎（FIP）相關的血管炎。

​臨床提示​：由於其對組織重塑和發炎的影響需要時間，皮膚疾病的臨床療效可能需要 4 到 8 週才能顯現。

作用機制

The exact mechanisms are multifaceted, combining rheological improvement with anti-inflammatory effects:

  • Phosphodiesterase (PDE) Inhibition: Inhibits erythrocyte PDE → increases intracellular cAMP → increases erythrocyte flexibility and deformability, allowing red blood cells to navigate compromised microvasculature.
  • Blood Viscosity Reduction: Reduces plasma fibrinogen and increases fibrinolytic activity.
  • Immunomodulation: PDE inhibition in leukocytes decreases the production of inflammatory cytokines, notably ​TNF-α​, reducing the negative effects of endotoxemia.
  • Enzyme Inhibition: In horses, it acts as a potent inhibitor of ​matrix metalloproteinase-9 (MMP-9)​ and a modest inhibitor of MMP-2, which may aid in preventing tissue degradation.

安全性與警告

禁忌症

  • Intolerance or hypersensitivity to pentoxifylline or other xanthines (e.g., theophylline, caffeine, theobromine)
  • Cerebral hemorrhage
  • Hypersensitivity to methylxanthines (e.g., theophylline, caffeine)
  • Cerebral or retinal hemorrhage
  • Severe hepatic or renal impairment (use with caution)

不良反應

  • Vomiting
  • Inappetence
  • Loose stools
  • Excitement
  • Nervousness
  • Dizziness (humans)
  • Headache (humans)
  • Erythema multiforme (rare in dogs)
  • Transient leukocytosis (horses IV)
  • Muscle fasciculations (horses IV)
  • Sweating on shoulders/flanks (horses IV)
  • Mild increases in heart rate (horses IV)
  • Anorexia
  • Diarrhea
  • Restlessness
  • Tachycardia
  • Tremors

注意事項

Caution in patients with severe hepatic or renal impairment, or those at risk for hemorrhage.

  • Pregnancy: FDA Category C. May be teratogenic at high dosages.
  • Nursing: Excreted in maternal milk. Use cautiously in nursing patients due to potential tumorigenicity seen in rats.

藥物相互作用

Antihypertensive drugs

May increase hypotensive effect when used concurrently

NSAIDs

Controversial in horses; may negate beneficial effects for endotoxemia, though some studies show superior efficacy when used with flunixin

Platelet-aggregation inhibitors (e.g., aspirin, clopidogrel)

Increased risk for bleeding

TheophyllineMajor

Serum levels of theophylline may be increased when used concurrently

WarfarinModerate

Increased risk of bleeding; use together with enhanced monitoring and caution

CiprofloxacinModerate

May increase pentoxifylline levels

AntihypertensivesMinor

Potential for additive hypotensive effects

監測

  • Clinical efficacy (resolution of dermatologic or vascular signs)
  • Adverse effects (GI upset, CNS signs)
  • Clinical response (resolution of skin lesions/improved blood flow)
  • Gastrointestinal tolerance
  • Signs of bleeding

藥物動力學

半衰期

貓Unknown狗6-7 hours (parent compound), 36 hours (active metabolite 1), 8 hours (active metabolite 5)

吸收

Horses: Rapidly absorbed after PO administration of crushed sustained-release tablets, with wide interpatient variation (bioavailability ~68%). Dogs: Bioavailability is approximately 50% with peak levels occurring 1-3 hours after dosing. Humans: Rapid and almost complete absorption, but undergoes a significant first-pass effect.

分佈

Distributive characteristics are not fully described, but it is known that the drug enters maternal milk.

代謝

Metabolized both in the liver and erythrocytes; all identified metabolites appear to be active.

排除

Excreted primarily via urine (inferred from human data).

過量

Signs of overdose in humans include flushing, seizures, hypotension, unconsciousness, agitation, fever, somnolence, GI distress, and ECG changes. One patient who ingested 80 mg/kg recovered completely. Overdoses should be treated using standard methods of appropriate gut emptying (emesis/lavage) and supportive therapies.

可用產品

劑型

  • Tablets (sustained-release / controlled-release)
  • Injection (IV)
  • 400 mg tablet (often modified-release)

人用標示

  • Pentoxifylline Controlled/Extended Release Tablets: 400 mg; Trental® (Hoechst Marion Roussel); generic
  • Trental 400 mg modified-release tablets

各地核准狀態

European Union✓ 已核准處方藥EMA

Human POM used off-label under the cascade.

United Kingdom✓ 已核准處方藥VMD

Human POM used off-label under the cascade.

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

儲存與穩定性

Commercially available tablets should be stored in well-closed containers, protected from light at 15-30°C.

飼主須知

  • ​給藥方式​：請​與食物一起​餵食此藥物，以大幅降低腸胃不適（嘔吐或食慾不振）的機率。
  • ​需要耐心​：對於皮膚和血管疾病，可能需要​數週（長達 6-8 週）​才能看到明顯的改善。除非獸醫師指示，否則請勿提早停藥。
  • ​副作用​：請留意是否有嘔吐、腹瀉或異常的神經質/興奮。如果出現這些情況，請聯繫您的獸醫師。
  • ​預期心理​：飼主應了解獸醫學界對此藥物的使用經驗有限，其風險與效益的評估尚未完全明確。

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