洛哌丁胺

Loperamide

Loperamide hydrochloride

別名: Imodium A-D · Neo-Diaral · K-Pek II · Diah-Limit · Diarolaeze · Entrocalm · Norimode · PJ 185 · R 18553 · Loperamida · Loperamidum

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

0.08 mg/kgPO· three times daily

體重— 🐕

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
Antidiarrheal	0.08 mg/kg	PO	three times daily	—	🌎 NA
Antidiarrheal	0.1-0.2 mg/kg	PO	q8-12h	—	🌎 NA
Antidiarrheal	0.1 mg/kg	PO	three times a day	Maximum 5 days	🌎 NA
Adjunctive treatment for diarrhea associated with chemotherapy	0.08 mg/kg	PO	three times daily	—	🌎 NA
Antidiarrheal	0.08 mg/kg	PO	3-4 times a day	—	🌎 NA
Antidiarrheal	0.1-0.2 mg/kg	PO	q6-12h	—	🌎 NA
Management of non-specific acute and chronic diarrhoea, and irritable bowel syndrome	0.04-0.2 mg/kg	PO	q8-12h	As needed	🌍 EU

Antidiarrheal: Collies and related breeds (MDR1 mutation) may be overly sensitive
Antidiarrheal: Potentially contraindicated when diarrhea is suspected to be caused by enteric infections
Management of non-specific acute and chronic diarrhoea, and irritable bowel syndrome: Do not use in dogs likely to be ivermectin-sensitive (e.g., collies) due to MDR1 mutation risk.

貓

適應症	劑量	途徑	頻次	療程	地區
Diarrhea	0.04-0.06 mg/kg	PO	twice daily	—	🌎 NA
Diarrhea	0.08-0.16 mg/kg	PO	q12h	—	🌎 NA
Management of non-specific acute and chronic diarrhoea, and irritable bowel syndrome	0.04-0.2 mg/kg	PO	q8-12h	As needed	🌍 EU

Diarrhea: Using the suspension. Use is controversial; may react with excitatory behavior.
Diarrhea: Use is controversial.
Management of non-specific acute and chronic diarrhoea, and irritable bowel syndrome: Use with care; excitability may be seen.

小型哺乳類

適應症	劑量	途徑	頻次	療程	地區
Antidiarrheal (Rabbits)	0.1 mg/kg in 1 mL of water	PO	q8h for 3 days, then once daily for 2 days	5 days total	🌎 NA
Antidiarrheal (Mice, Rats, Gerbils, Hamsters, Guinea pigs, Chinchillas)	0.1 mg/kg in 1 mL of water	PO	q8h for 3 days, then once daily for 2 days	5 days total	🌎 NA

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。

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概覽

洛哌丁胺是一種合成的、具周邊作用的哌啶衍生物鴉片類促效劑，在獸醫學中主要用作止瀉藥和胃腸道（GI）動力調節劑。

與許多其他鴉片類藥物不同，洛哌丁胺是血腦屏障處 P-醣蛋白 (P-gp) 藥物排出幫浦的受質。在正常動物中，這能防止藥物在中樞神經系統 (CNS) 中積聚，從而將典型的鴉片類神經副作用降至最低。

臨床要點： 洛哌丁胺對於緩解非感染性腹瀉（例如由 toceranib 等藥物引起的化療相關腹瀉）非常有效。然而，由於 ABCB1-1Δ (MDR1) 基因突變，在牧羊犬品種（如牧羊犬、澳洲牧羊犬）中使用時必須極度謹慎，甚至完全避免。在這些犬隻中，有缺陷的 P-gp 幫浦會讓洛哌丁胺穿過血腦屏障，即使在標準劑量下也會導致嚴重且可能致命的神經毒性。

作用機轉

Loperamide exerts its antidiarrheal effects through multiple mechanisms within the gastrointestinal tract:

μ-opioid receptor agonism: Binds to mu-receptors in the myenteric plexus of the intestinal wall → inhibits the release of acetylcholine and prostaglandins → reduces peristalsis and increases intestinal transit time, allowing for greater fluid absorption.
δ-opioid receptor agonism: Binds to delta-receptors → decreases intestinal secretion induced by cholera toxin and prostaglandins.
Calcium channel modulation: Inhibits diarrheas caused by factors utilizing calcium as a second messenger (non-cAMP/cGMP mediated).
Mucosal absorption: Directly enhances the mucosal absorption of water and electrolytes.

安全性與警告

禁忌症

Dogs tested positive for the ABCB1-1Δ (MDR1) mutation
Untested dogs of herding breeds susceptible to the MDR1 mutation
Diarrhea caused by toxic ingestion (until the toxin is eliminated)
Known hypersensitivity to narcotic analgesics
Infectious enteritis (relative contraindication, as decreased motility can delay pathogen clearance)
Intestinal obstruction
Dogs likely to be ivermectin-sensitive (MDR1/ABCB1 mutation, e.g., Collies, Australian Shepherds)
Infectious enteritis (where decreased motility may delay pathogen clearance)
Toxigenic diarrhea

不良反應

Constipation
Bloat
Paralytic ileus
Toxic megacolon
Pancreatitis
CNS depression (especially in MDR1-mutant dogs)
Excitatory behavior (cats)
Excitability (especially in cats)
Profound sedation and ataxia (in MDR1 mutant dogs)

注意事項

Use with caution in patients with hypothyroidism, severe renal insufficiency, adrenocortical insufficiency (Addison's disease), and in geriatric or severely debilitated patients.

Use with extreme caution in patients with head injuries or increased intracranial pressure, as well as acute abdominal conditions (e.g., colic), as opiates may obscure the diagnosis or clinical course.

Use with extreme caution in patients suffering from respiratory disease or acute respiratory dysfunction (e.g., pulmonary edema secondary to smoke inhalation).

Use with extreme caution in patients with hepatic disease exhibiting CNS clinical signs of hepatic encephalopathy, as hepatic coma may result.

Small Patient Dosing: Many clinicians recommend avoiding tablet/capsule forms in dogs weighing less than 10 kg due to potency; dosage titration using liquid forms is recommended for safe use.