λ‘νλΌλ§μ΄λ
λ‘νλΌλ§μ΄λλ μμνμμ μ£Όλ‘ μ§μ¬μ λ° μμ₯κ΄(GI) μ΄λ μ‘°μ μ λ‘ μ¬μ©λλ ν©μ± λ§μ΄ μμ© νΌν리λ μ λ체 μνΈκ³ μμ©μ μ λλ€. λ€λ₯Έ λ§μ μ€νΌμ€μ΄λμ λ¬λ¦¬ λ‘νλΌλ§μ΄λλ νμ‘λμ₯λ²½μ μλ **P-λΉλ¨λ°±μ§(P-gp)** μ μΆ ννμ κΈ°μ§μ λλ€. μ μμ μΈ λλ¬Όμ κ²½μ°, μ΄λ μ½λ¬Όμ΄ μ€μΆμ κ²½κ³(CNS)μ μΆμ λλ κ²μ λ°©μ§νμ¬ μ νμ μΈ μ€νΌμ€μ΄λ μ κ²½κ³ λΆμμ©μ μ΅μνν©λλ€. > **μμ μμ :** λ‘νλΌλ§μ΄λλ λΉκ°μΌμ± μ€μ¬(μ: ν μΈλΌλκ³Ό κ°μ μ½λ¬Όλ‘ μΈν ννμλ² μ λ° μ€μ¬)μ μ¦μ μνμ λ§€μ° ν¨κ³Όμ μ λλ€. κ·Έλ¬λ **ABCB1-1Ξ(MDR1) λμ°λ³μ΄**λ‘ μΈν΄ λͺ©μ견 νμ’ (μ: μ½λ¦¬, μ€μ€νΈλ μΌλ¦¬μ μ °νΌλ)μ μ¬μ©ν λλ κ·Ήλλ‘ μ£Όμνκ±°λ μμ ν νΌν΄μΌ ν©λλ€. μ΄λ¬ν λ°λ €κ²¬μ κ²½μ° κ²°ν¨μ΄ μλ P-gp ννλ‘ μΈν΄ λ‘νλΌλ§μ΄λκ° νμ‘λμ₯λ²½μ ν΅κ³Όνκ² λμ΄ νμ€ μ©λμμλ μ¬κ°νκ³ μΉλͺ μ μΌ μ μλ μ κ²½ λ μ±μ μ λ°ν μ μμ΅λλ€.
μμ© κΈ°μ : Loperamide exerts its antidiarrheal effects through multiple mechanisms within the gastrointestinal tract: * **ΞΌ-opioid receptor agonism:** Binds to mu-receptors in the myenteric plexus of the intestinal wall β inhibits the release of acetylcholine and prostaglandins β reduces peristalsis and increases intestinal transit time, allowing for greater fluid absorption. * **Ξ΄-opioid receptor agonism:** Binds to delta-receptors β 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.
λλ¬Ό μ’ λ³ μ©λ
- Diarrhea Β· 0.04-0.06 mg/kg Β· PO Β· twice daily Β· Using the suspension. Use is controversial; may react with excitatory behavior.
- Diarrhea Β· 0.08-0.16 mg/kg Β· PO Β· q12h Β· Use is controversial.
- Management of non-specific acute and chronic diarrhoea, and irritable bowel syndrome Β· 0.04-0.2 mg/kg Β· PO Β· q8-12h Β· As needed Β· Use with care; excitability may be seen.
- Antidiarrheal (Rabbits) Β· 0.1 mg/kg in 1 mL of water Β· PO Β· q8h for 3 days, then once daily for 2 days Β· 5 days total
- Antidiarrheal (Mice, Rats, Gerbils, Hamsters, Guinea pigs, Chinchillas) Β· 0.1 mg/kg in 1 mL of water Β· PO Β· q8h for 3 days, then once daily for 2 days Β· 5 days total
- Antidiarrheal Β· 0.08 mg/kg Β· PO Β· three times daily Β· Collies and related breeds (MDR1 mutation) may be overly sensitive
- Antidiarrheal Β· 0.1-0.2 mg/kg Β· PO Β· q8-12h
- Antidiarrheal Β· 0.1 mg/kg Β· PO Β· three times a day Β· Maximum 5 days Β· Potentially contraindicated when diarrhea is suspected to be caused by enteric infections
- Adjunctive treatment for diarrhea associated with chemotherapy Β· 0.08 mg/kg Β· PO Β· three times daily
ν¬μ¬ κ²½λ‘
κΈκΈ°
- Dogs tested positive for the ABCB1-1Ξ (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
μ΄μλ°μ
- Constipation
- Bloat
- Sedation
- 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)
μ½λ¬Ό μνΈμμ©
- Amiodarone Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Carvedilol Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Erythromycin Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Ketoconazole Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Itraconazole Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Quinidine Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Tamoxifen Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Verapamil Β· Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
- Other antimotility drugs Β· Additive reduction in GI motility, increasing risk of ileus Β· moderate
- P-glycoprotein inhibitors (e.g., ketoconazole, cyclosporine, spinosad) Β· May increase CNS penetration of loperamide, leading to neurotoxicity Β· major
- CNS depressants Β· Additive sedation if loperamide crosses the blood-brain barrier Β· moderate
λͺ¨λν°λ§
- Clinical efficacy (resolution of diarrhea)
- Fluid and electrolyte status (especially in severe diarrhea)
- CNS effects (sedation, ataxia, depression), particularly if using high dosages or in susceptible breeds
- Fecal consistency and frequency
- Signs of constipation or paralytic ileus
- Neurological status (watch for sedation or ataxia, especially in at-risk breeds)
- Hydration status
κ³Όμ©λ
In dog toxicity studies, doses of 1.25-5 mg/kg/day produced **vomiting, depression, severe salivation, and weight loss**. > **CRITICAL WARNING:** Breeds with a defective MDR1 (ABCB1-1Ξ) gene are profoundly more sensitive to CNS depression with loperamide than other breeds and have shown clinical signs of toxicity at doses as low as **0.06 mg/kg**. Common clinical signs of overdose include diarrhea, vomiting, lethargy, anorexia, weakness, and hypersalivation. **Treatment:** * Follow standard GI decontamination protocols. * **Avoid apomorphine** for emesis, as it can have additive CNS or respiratory depressant effects. * **Naloxone** may be used to treat severe CNS/respiratory depression; higher than usual doses of naloxone may be required to reverse loperamide toxicity.
VetSheet μ½λ¬Ό λ νΌλ°μ€λ λ©΄ν μμ μ λ¬Έκ°λ₯Ό μν μμ μμ¬κ²°μ 보쑰 λꡬμ΄λ©°, μ λ¬Έμ νλ¨μ΄λ μ μ‘°μ¬μ μ΅μ λΌλ²¨μ λμ νμ§ μμ΅λλ€.