苯乙哌啶與阿托品
Diphenoxylate and Atropine
Diphenoxylate hydrochloride and atropine sulfate
別名: Lomotil · Logen · Lonox · Lomanate · co-phenotrope · R 1132 · NIH 7562 · difenoxilato
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Antitussive agent (extra-label)
須由已驗證獸醫確認
- q8-12h
NA
必須一併考量的臨床脈絡 (2)
- ■ May be given with or without food. If your animal vomits or acts sick after receiving the drug on an empty stomach, try giving the next dose with food or a small treat. If vomiting continues, contact your veterinarian.
- Diphenoxylate/atropine tablets should be stored at room temperature of 20°C to 25°C (68°F-77°F). Diphenoxylate/atropine oral solution should be stored at room temperature of 20°C to 25°C (68°F-77°F); avoid freezing.
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
苯乙哌啶 (Diphenoxylate) 是一種合成的苯基哌啶衍生物鴉片類促效劑，結構上與配西汀 (meperidine) 相似。在獸醫學中主要用作止瀉藥和鎮咳藥（抑制咳嗽），最常用於犬隻。
主要藥理特徵包括：
- 調節腸道蠕動：減緩胃腸道排空時間，促進水分吸收，從而減少腹瀉。
- 防濫用機制：商業製劑中含有亞治療劑量的硫酸阿托品 (atropine sulfate)。在正常劑量下，阿托品不會產生臨床作用；但若過量服用，會產生令人不適的抗膽鹼副作用（如口乾、心跳過速），藉此防止藥物濫用。
- 管制藥物：由於其鴉片類特性，被歸類為第五級管制藥品。
臨床要點：由於可能引起矛盾的興奮行為，本藥在貓的使用極具爭議。對於體重低於 10 公斤的犬隻，強烈建議使用液體製劑，以便精確調整劑量，避免因高濃度錠劑導致意外過量。
作用機轉
Diphenoxylate exerts its effects primarily through interaction with opioid receptors in the gastrointestinal tract and central nervous system:
- GI Motility: Binds to μ-opioid receptors in the enteric nervous system (myenteric plexus) → decreases the release of acetylcholine and prostaglandins → inhibits excessive GI propulsion and increases segmental (non-propulsive) contractions → prolongs intestinal transit time.
- Secretion Reduction: Decreases intestinal secretion induced by cholera toxin, prostaglandin E2, and non-cAMP/cGMP mediated diarrheas. Enhances mucosal fluid and electrolyte absorption.
- Antitussive Effect: Acts directly on the medullary cough center in the brain → depresses the cough reflex.
- Atropine Component: Acts as a competitive antagonist at muscarinic acetylcholine receptors, though its dose in this combination is too low to exert significant systemic anticholinergic effects unless overdosed.
安全性與警告
禁忌症
- Known hypersensitivity to narcotic analgesics
- Patients receiving monoamine oxidase inhibitors (MAOIs)
- Diarrhea caused by toxic ingestion (until the toxin is eliminated from the GI tract)
- Intestinal obstruction
- Bacterial-induced acute diarrhea (may enhance bacterial proliferation)
不良反應
- Constipation
- Bloat
- Sedation
- Paralytic ileus (potential)
- Toxic megacolon (potential)
- Pancreatitis (potential)
- CNS depression or excitation
- Excitatory behavior (especially in cats)
注意事項
Use with caution in patients with respiratory disease, hepatic encephalopathy (hepatic coma may result), hypothyroidism, severe renal insufficiency, adrenocortical insufficiency (Addison's disease), head injuries or increased intracranial pressure, acute abdominal conditions (may obscure diagnosis), and in geriatric or severely debilitated patients.
- Small Dogs: Extreme care is required when dosing dogs under 10 kg; liquid formulations are recommended for accurate titration.
- Cats: Use is controversial and generally not recommended due to potential excitatory behavior.
- Horses/Infectious Diarrhea: Opiates may have a detrimental effect in acute diarrhea by enhancing bacterial proliferation, delaying microbe clearance, and prolonging the febrile state.
- Nursing/Pregnancy: Category C. Excreted in maternal milk; use caution in nursing patients.
藥物交互作用
May cause increased CNS or respiratory depression when used concurrently.
Contraindicated. Do not use opiate antidiarrheals for at least 14 days after receiving MAOIs due to risk of severe adverse reactions.
監測
- Clinical efficacy (resolution of diarrhea or cough)
- Fluid and electrolyte status (especially in severe diarrhea)
- CNS effects (sedation or excitation), particularly if using high dosages
- Bowel movements (monitor for constipation)
- Plasma amylase and lipase (may be artificially increased for up to 24 hours post-administration)
藥物動力學
吸收
In humans, rapidly absorbed after oral administration. Bioavailability of tablets is ~90% of the solution. Onset of action is 45-60 minutes, sustained for 3-4 hours.
分佈
Crosses the blood-brain barrier and is excreted in maternal milk.
代謝
Metabolized into diphenoxylic acid, which is an active metabolite.
排除
Primarily excreted via feces and urine.
過量
Acute overdosage can result in severe CNS, cardiovascular, gastrointestinal, or respiratory toxicity.
- Delayed Absorption: Because opiates significantly reduce GI motility, absorption of the drug from the GI tract may be delayed and prolonged, meaning toxicity can worsen over time.
- Opiate Toxicity: Signs include profound sedation, respiratory depression, and pinpoint pupils. Naloxone may be necessary to reverse the opiate effects.
- Atropine Toxicity: Massive overdoses may induce atropine toxicity (dry mouth, tachycardia, hyperthermia, dilated pupils, agitation).
可用產品
劑型
- Tablets
- Oral Liquid/Solution
人用標示
- Diphenoxylate HCl Tablets: 2.5 mg with 0.025 mg Atropine Sulfate (e.g., Lomotil, Logen, Lonox)
- Diphenoxylate HCl Liquid: 2.5 mg with 0.025 mg Atropine Sulfate per 5 mL (e.g., Lomotil, Lomanate)
各地核准狀態
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儲存與穩定性
Tablets should be stored at room temperature in well-closed, light-resistant containers. Oral solution should be stored at room temperature in tight, light-resistant containers; avoid freezing.
飼主須知
寵物主人重要須知
- 用途：本藥物用於治療犬隻的腹瀉，或抑制慢性的乾咳。
- 何時應聯繫獸醫：如果腹瀉持續超過 48 小時，或者您的寵物變得極度嗜睡/無精打采、發高燒或出現腹痛跡象，請立即聯繫您的獸醫。
- 注意便秘：因為這種藥物會減緩腸道蠕動，所以可能會引起便秘，特別是長期用於止咳時。如果您發現寵物排便困難，請告知獸醫；可能需要使用軟便劑。
- 劑量準確性：如果您飼養的是小型犬且使用液體製劑，請非常仔細地測量劑量。過量使用會導致嚴重的副作用，包括嚴重的嗜睡和呼吸問題。
- 儲存方式：請將本藥物嚴格存放在兒童和其他寵物接觸不到的地方。這是一種管制藥物。
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。