氨茶鹼 / 茶鹼
Aminophylline / Theophylline
1,3-dimethyl-7H-purine-2,6-dione (Theophylline); Theophylline ethylenediamine (Aminophylline)
別名: Theochron · Theo-Cap · Theo-24 · Uniphyl · Bronkodyl · Elixophyllin · Theo-Dur · Slo-Bid · aminofilina · aminophyllinum · euphyllinum · metaphyllin · theophylline and ethylenediamine · theophylline ethylenediamine compound · theophyllinum ethylenediaminum · anhydrous theophylline · teofillina
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 |
|---|---|---|---|---|---|
| Bronchodilation (Extended-Release) | 10 mg/kg PO every 12 hours initially, if no adverse effects are observed and the desired clinical effect is not achieved, give 15 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Tracheal collapse (mild clinical signs, <50% collapse) | 11 mg/kg PO, IM or IV three times daily. | PO/IM/IV | q8h | — | 🌎 NA |
| Severe, acute pulmonary edema and bronchoconstriction | Aminophylline 4-8 mg/kg IV or IM, or 6-10 mg/kg PO every 8 hours. | IV/IM/PO | q8h | — | 🌎 NA |
| Cough | Aminophylline: 10 mg/kg PO, IV three times daily | PO/IV | q8h | — | 🌎 NA |
| Collapsing trachea (bronchodilator) | 11 mg/kg PO or IV q6-12h | PO/IV | q6-12h | — | 🌎 NA |
- Bronchodilation (Extended-Release): Using Theochron Extended-Release Tablets or Theo-Cap Extended-Release Capsules
- Tracheal collapse (mild clinical signs, <50% collapse): Aminophylline
- Severe, acute pulmonary edema and bronchoconstriction: Long-term use is not recommended.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Bronchodilation (Extended-Release) | 20 mg/kg PO once daily in the PM; using Slo-Bid: 25 mg/kg PO once daily in the PM | PO | q24h | — | 🌎 NA |
| Bronchodilation | 6.6. mg/kg PO twice daily; using sustained release tablets (Theo-Dur): 25-50 mg (total dose) per cat PO in the evening | PO | q12h or q24h | — | 🌎 NA |
| Tracheal collapse (mild clinical signs, <50% collapse) | aminophylline: 5 mg/kg PO, two times daily. | PO | q12h | — | 🌎 NA |
| Bronchoconstriction associated with fulminant CHF | Aminophylline 4-8 mg/kg SC, IM, IV q8-12h. | SC/IM/IV | q8-12h | — | 🌎 NA |
| Cough | Aminophylline: 5 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
- Bronchodilation (Extended-Release): Products Theo-Dur and Slo-Bid are no longer available in the USA. Cautious use of dog dose/products is a reasonable alternative.
- Bronchodilation: Using aminophylline tablets or sustained release tablets
雪貂
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Bronchodilation | 4.25 mg/kg PO 2-3 times a day | PO | q8-12h | — | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Pulmonary edema | Aminophylline 2-7 mg/kg IV q6-12h; Theophylline 5-15 mg/kg PO q12h | IV/PO | q6-12h | — | 🌎 NA |
| Pulmonary edema | 11 mg/kg PO or IV q8-12h. | PO/IV | q8-12h | — | 🌎 NA |
| Heaves (RAO) | Aminophylline: 5-10 mg/kg PO or IV twice daily. | PO/IV | q12h | — | 🌎 NA |
| Heaves (RAO) | Aminophylline: 4-6 mg/kg PO three times a day. | PO | q8h | — | 🌎 NA |
- Pulmonary edema: IV aminophylline should be diluted in at least 100 mL of D5W or normal saline and administered slowly (not >25 mg/min).
- Pulmonary edema: To 'load' may either double the initial dose or give both oral and IV dose at the same time. IV infusion in ~1L fluids over 20-60 mins.
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
氨茶鹼與茶鹼屬於甲基黃嘌呤類衍生物，在獸醫學中主要用作強效的支氣管擴張劑。它們常被用於治療下呼吸道疾病（如貓氣喘、馬復發性呼吸道阻塞及犬支氣管炎）、氣管塌陷，以及作為心因性肺水腫的輔助治療。
臨床要點： 氨茶鹼本質上是茶鹼的水溶性鹽類（透過加入乙二胺製成）。100毫克的含水氨茶鹼約含有79毫克的無水茶鹼。 在兩種劑型之間轉換時，必須仔細計算劑量。
雖然這些藥物非常有效，但其治療指數狹窄。毒性與劑量相關，不過犬貓對血清濃度的耐受度通常高於人類。由於不同病患在代謝上存在顯著差異，強烈建議進行治療藥物監測（TDM），特別是對於患有肝臟或心臟疾病的動物。
作用機轉
The primary mechanism of action involves the competitive inhibition of phosphodiesterase (PDE) enzymes.
- PDE Inhibition → Decreased breakdown of cyclic AMP (cAMP) → Elevated intracellular cAMP levels.
- Increased cAMP → Enhanced release of endogenous epinephrine → Relaxation of bronchial and pulmonary vascular smooth muscle.
- Elevated cAMP also inhibits the release of inflammatory mediators like histamine and slow-reacting substance of anaphylaxis (SRS-A) from mast cells.
- Intracellular Calcium Translocation: Methylxanthines alter intracellular ionized calcium dynamics, contributing to increased diaphragmatic contractility (reducing respiratory fatigue) and weak positive inotropic/chronotropic effects on the heart.
- Additional Effects: Induces mild diuresis, stimulates the central nervous system (CNS) and respiratory centers, and increases gastric acid secretion.
安全性與警告
禁忌症
- Hypersensitivity to any xanthines (including theobromine or caffeine)
- Hypersensitivity to ethylenediamine (specific to aminophylline)
不良反應
- Nausea and vomiting
- Diarrhea
- Insomnia / Restlessness
- Polyphagia (increased appetite)
- Polydipsia and polyuria (increased thirst and urination)
- Tachycardia (rapid heart rate)
- Nervousness, excitability, and tremors (especially in horses)
- Diaphoresis (sweating in horses)
- Ataxia
- Seizures (in severe toxicity)
- Cardiac dysrhythmias (in severe toxicity)
注意事項
Use with extreme caution in patients with severe cardiac disease, seizure disorders, gastric ulcers, hyperthyroidism, renal or hepatic disease, severe hypoxia, or severe hypertension.
- Arrhythmias: May cause or worsen preexisting cardiac arrhythmias; enhanced monitoring is required.
- Clearance Issues: Neonatal, geriatric, and congestive heart failure (CHF) patients may have decreased clearance and prolonged half-lives, making them more susceptible to toxicity.
- Dosing Weight: Because of low lipid solubility and low volume of distribution, obese patients should be dosed based on lean body weight.
- IM Injection: Aminophylline causes intense local pain when administered IM and is rarely recommended via this route.
藥物交互作用
May decrease theophylline levels via hepatic enzyme induction.
Can significantly increase theophylline levels. Consider reducing theophylline dose by 30% and monitor for toxicity.
Can increase theophylline levels.
Can increase theophylline levels by inhibiting hepatic metabolism.
Concurrent use can cause an increased incidence of seizures.
Concurrent use may cause an increased incidence of cardiac dysrhythmias.
Toxic synergism; can lead to severe cardiac arrhythmias.
Can increase theophylline levels and antagonize bronchodilatory effects.
Can increase theophylline levels.
監測
- Therapeutic efficacy (improvement in breathing/cough)
- Clinical signs of toxicity (GI upset, CNS stimulation, tachycardia)
- Serum trough levels at steady state (Target: >8-10 mcg/mL in small animals; do not exceed 15 mcg/mL in horses. Human therapeutic range is 10-20 mcg/mL)
藥物動力學
半衰期
吸收
Nearly 100% bioavailable after oral administration of non-sustained release products. Sustained-release products have variable bioavailability ranging from 30-76%.
分佈
Distributes throughout extracellular fluids and body tissues. Crosses the placenta and distributes into milk (70% of serum levels). Low plasma protein binding (7-14% in dogs). Volume of distribution: dogs 0.82 L/kg, cats 0.46 L/kg, horses 0.85-1.02 L/kg.
代謝
Metabolized primarily in the liver to 3-methylxanthine, which possesses weak bronchodilatory activity.
排除
Renal clearance contributes only about 10% to overall plasma clearance.
過量
Clinical signs of toxicity are usually associated with serum levels greater than 20 mcg/mL in humans, though dogs appear to tolerate higher levels.
Life-threatening signs:
- Tachycardia and severe cardiac arrhythmias
- CNS effects including seizures and hyperthermia
Treatment is supportive:
- Decontamination: Empty the gut, administer activated charcoal and a cathartic if oral ingestion was recent.
- Seizures: Maintain an adequate airway and treat with IV diazepam.
- Monitoring: Continuous ECG monitoring for arrhythmias. Monitor and correct fluid/electrolyte imbalances.
- Symptomatic Care: Hyperthermia may be treated with phenothiazines; severe tachycardia may be treated with propranolol if life-threatening.
可用產品
劑型
- Tablets (immediate and extended-release)
- Capsules (extended-release)
- Injection (solution)
- Oral elixir/solution
- Compounded oral suspension
人用標示
- Aminophylline Tablets: 100 mg & 200 mg
- Aminophylline Injection: 250 mg/10 mL (25 mg/mL)
- Theophylline Extended-Release Capsules and Tablets: 100 mg, 125 mg, 200 mg, 300 mg, 400 mg, 450 mg, & 600 mg
- Theophylline Tablets and Capsules: 100 mg, 200 mg, & 300 mg
- Theophylline Elixir: 80 mg/15 mL
- Theophylline & Dextrose Injection: Various concentrations (0.4 mg/mL to 4 mg/mL)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store oral products in tight, light-resistant containers at room temperature. Aminophylline injection should be stored below 30°C, protected from freezing and light. Do not inject solutions that contain a precipitate or visible crystals. Compounded oral suspensions should be protected from light and kept at room temperature (refrigeration causes precipitation).
飼主須知
此藥物用於幫助擴張寵物的呼吸道，使其呼吸更順暢。
- 給藥方式： 請嚴格按照獸醫師的指示給藥，切勿漏服。如果使用的是長效型（緩釋）錠劑或膠囊，除非獸醫師特別指示，否則請勿將其壓碎或讓寵物咀嚼。
- 副作用： 剛開始服藥時可能會出現輕微的腸胃不適、飲水量與排尿量增加，或輕微的焦躁不安，但這些症狀通常會自行緩解。
- 何時應聯繫獸醫師： 如果您發現寵物出現嚴重嘔吐、極度焦躁、肌肉顫抖、呼吸急促或癲癇發作，請立即聯繫獸醫師，因為這些可能是藥物過量的徵兆。
- 飲食注意事項： 避免讓寵物接觸巧克力或咖啡因，因為這些物質含有類似的化合物，會增加中毒的風險。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。