Loperamida
Loperamide
Loperamide hydrochloride
También conocido como: Imodium A-D · Neo-Diaral · K-Pek II · Diah-Limit · Diarolaeze · Entrocalm · Norimode · PJ 185 · R 18553 · Loperamida · Loperamidum
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Dosis por especie
🌎 NA — North America🌍 EU — Europe
Perros
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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.
Pequeños mamíferos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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 |
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
La loperamida es un agonista opiáceo sintético derivado de la piperidina de acción periférica, utilizado principalmente como antidiarreico y modificador de la motilidad gastrointestinal en medicina veterinaria.
A diferencia de muchos otros opioides, la loperamida es un sustrato para la bomba de eflujo P-glicoproteína (P-gp) en la barrera hematoencefálica. En animales sanos, esto evita que el fármaco se acumule en el sistema nervioso central (SNC), minimizando así los efectos neurológicos típicos de los opioides.
Perla clínica: La loperamida es altamente efectiva para el alivio sintomático de la diarrea no infecciosa (como la diarrea inducida por quimioterapia con fármacos como el toceranib). Sin embargo, debe utilizarse con extrema precaución, o evitarse por completo, en razas de pastoreo (p. ej., Collies, Australian Shepherds) debido a la mutación ABCB1-1Δ (MDR1). En estos perros, la bomba P-gp defectuosa permite que la loperamida cruce la barrera hematoencefálica, provocando una neurotoxicidad profunda y potencialmente mortal incluso a dosis estándar.
Mecanismo de acción
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.
Seguridad y advertencias
Contraindicaciones
- 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
Efectos adversos
- 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)
Precauciones
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.
Interacciones farmacológicas
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Inhibits P-glycoprotein (P-gp), which may increase loperamide plasma concentrations and risk of CNS toxicity.
Additive reduction in GI motility, increasing risk of ileus
May increase CNS penetration of loperamide, leading to neurotoxicity
Additive sedation if loperamide crosses the blood-brain barrier
Monitorización
- 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
Farmacocinética
Vida media
Absorción
In dogs, reportedly has a faster onset of action than diphenoxylate.
Distribución
Unknown if the drug enters milk or crosses the placenta. Excluded from the CNS in normal animals by P-glycoprotein.
Metabolismo
Hepatic metabolism.
Eliminación
Primarily fecal elimination.
Sobredosis
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 (ABCB1-1Δ) 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.
Productos disponibles
Formulaciones
- Oral liquid
- Capsules
- Tablets
- 2 mg capsule
- 2 mg tablet
- 0.2 mg/ml syrup
Etiquetado para humanos
- Loperamide HCl Oral Liquid: 1 mg/5 mL (0.2 mg/mL) & 1 mg/7.5 mL
- Loperamide HCl Capsules and Tablets: 2 mg
- Diah-Limit
- Diarolaeze
- Entrocalm
- Imodium
- Norimode
Estado regulador
Available as POM, P, or GSL depending on pack size and specific formulation.
Classified as POM, P, or GSL depending on the product.
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Loperamide capsules or oral solution should be stored at room temperature in well-closed containers. It is recommended that the oral solution not be diluted with other solvents.
Información para el cliente
La loperamida es un medicamento utilizado para ayudar a controlar la diarrea en mascotas.
- Advertencia de raza: NO utilice este medicamento en razas de pastoreo (como Collies, Shelties, Australian Shepherds o razas mixtas con patas blancas) a menos que hayan sido específicamente analizados y descartada la mutación del gen MDR1. En estos perros, la loperamida puede causar reacciones neurológicas graves y potencialmente mortales.
- Gatos: Generalmente no se recomienda su uso en gatos a menos que sea estrictamente indicado por su veterinario, ya que puede causar un comportamiento de excitación inusual.
- Administración: Las formas líquidas suelen ser preferibles para perros pequeños para asegurar una dosificación precisa. No diluya el líquido oral con otros líquidos.
- Cuándo llamar al veterinario: Comuníquese con su veterinario de inmediato si la diarrea persiste por más de 48 horas, si su mascota parece inusualmente apática, deprimida o descoordinada, o si desarrolla fiebre alta o heces con sangre.
La referencia de medicamentos de VetSheet está destinada a profesionales veterinarios autorizados como ayuda para la toma de decisiones clínicas, no como sustituto del criterio profesional ni del prospecto actual del fabricante.