Maropitant
(2S,3S)-2-benzhydryl-N-(5-tert-butyl-2methoxybenzyl) quinuclidin-3-amine citrate
También conocido como: Cerenia · Prevomax · Vetemex · CJ-11,972 · Maropitant citrate
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 |
|---|---|---|---|---|---|
| Prevention of acute vomiting | 1 mg/kg | SC | q24h | up to 5 consecutive days | 🌎 NA |
| Prevention of acute vomiting | 2 mg/kg | PO | q24h | up to 5 consecutive days | 🌎 NA |
| Treatment of acute vomiting | 1 mg/kg | SC | q24h | up to 5 consecutive days | 🌎 NA |
| Prevention of vomiting due to motion sickness | 8 mg/kg (minimum dose) | PO | q24h | up to 2 consecutive days | 🌎 NA |
| Treatment and prevention of vomiting (including chemotherapy) | Dose not specified in text | PO/SC/IV | Not specified (duration of activity is 24 hours) | Up to 5 days | 🌍 EU |
| Motion sickness | Dose not specified in text | PO/SC/IV | Not specified | Up to 2 days | 🌍 EU |
- Prevention of acute vomiting: Given at least one hour prior to anticipated emetogenic event
- Prevention of acute vomiting: Given at least two hours prior to anticipated emetogenic event
- Treatment of acute vomiting: If a longer duration of therapy is needed, a 48 hour washout period is recommended due to accumulation of the drug.
- Prevention of vomiting due to motion sickness: Given at least two hours prior to travel. If a longer duration of therapy is needed, a 72 hour washout period is recommended.
- Treatment and prevention of vomiting (including chemotherapy): Repeat treatment at a lower dose may be adequate in some individuals. If longer periods of treatment are required, a 72-hour interval is recommended between courses.
- Motion sickness: Not all preparations are specifically licensed for this purpose.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| As an antiemetic | 1 mg/kg | SC or PO | Unknown | — | 🌎 NA |
| As an antiemetic | 0.5-1 mg/kg | SC | once daily | up to 5 days | 🌎 NA |
| Treatment of vomiting | Dose not specified in text | SC/IV | Not specified | Not specified | 🌍 EU |
- As an antiemetic: Based on pharmacokinetic study
- Treatment of vomiting: Treatment by injection is recommended for frequent vomiting. Very high doses may cause haemolysis.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El citrato de maropitant (Cerenia®) es un antagonista del receptor de neuroquinina-1 (NK-1) altamente eficaz, aprobado por la FDA, utilizado principalmente como antiemético en medicina veterinaria.
- Antiemético de amplio espectro: Bloquea eficazmente el vómito mediado tanto periférica como centralmente, provocado por diversos estímulos (p. ej., quimioterapia, apomorfina, irritación gastrointestinal).
- Propiedades analgésicas: Más allá del control de la emesis, el maropitant proporciona analgesia visceral y se ha demostrado que reduce significativamente los requisitos de concentración alveolar mínima (CAM) para anestésicos inhalatorios como el sevoflurano.
- Uso en especies: Aprobado para perros (≥16 semanas para uso general, aunque se recomienda precaución en cachorros <11 semanas), y ampliamente utilizado fuera de etiqueta (extra-label) en gatos con excelente tolerabilidad.
- Nota clínica: Aunque no afecta los tiempos de vaciado gástrico, puede disminuir los patrones de presión de contracción del intestino delgado.
Mecanismo de acción
Maropitant exerts its effects by acting as a potent and selective antagonist at the neurokinin-1 (NK-1) receptors in the central nervous system (specifically the emetic center and chemoreceptor trigger zone).
- Substance P Inhibition: It competitively binds to NK-1 receptors, blocking the binding of Substance P, a key neuropeptide/neurotransmitter involved in the emetic pathway.
- Dual Action: Because Substance P is the final common pathway for vomiting, maropitant effectively suppresses emesis triggered by both central and peripheral stimuli.
- Pain Modulation: Substance P is also heavily involved in nociception; blocking its receptors in the visceral pathways provides significant visceral pain relief.
Seguridad y advertencias
Contraindicaciones
- Puppies less than 11 weeks old (due to risk of bone marrow hypoplasia)
- Suspected gastrointestinal obstruction
- Suspected gastrointestinal perforation
- Use for longer than 48 hours without a definitive diagnosis
Efectos adversos
- Pre-travel vomiting (especially at higher motion sickness doses)
- Hypersalivation
- Pain or swelling at the subcutaneous injection site
- Diarrhea
- Anorexia
- Localized injection site reactions (cats)
- Transient pain reaction during injection (very common, especially in cats)
- Haemolysis (at very high doses in cats)
Precauciones
Use with caution in dogs with hepatic dysfunction as maropitant is hepatically metabolized. Use with caution in puppies less than 11 weeks old due to a higher frequency and severity of bone marrow hypoplasia. The safe use of maropitant has not been evaluated in breeding, pregnant, or lactating dogs; use only following a benefit/risk assessment.
Interacciones farmacológicas
Use with caution; maropitant is highly protein-bound (99.5%) and could theoretically compete for binding sites, though clinical significance is undetermined.
Maropitant has an affinity for calcium-channels; concurrent use should be avoided.
Maropitant is highly bound to plasma proteins and may compete with other highly bound drugs, potentially altering free drug concentrations.
Monitorización
- Clinical efficacy (decreased episodes of vomiting)
- Adverse effects (e.g., injection site pain, hypersalivation)
- Resolution of vomiting
- Liver function (in patients with pre-existing hepatic disease)
- Signs of gastrointestinal obstruction or perforation
Farmacocinética
Vida media
Absorción
Rapidly absorbed after PO & SC administration. Bioavailability in dogs: 24% (2 mg/kg PO), 37% (8 mg/kg PO), and 91% (1 mg/kg SC). Feeding status does not affect bioavailability. In cats, bioavailability is ~50% (PO) and 100+% (SC).
Distribución
Plasma protein binding is very high (99.5%).
Metabolismo
Hepatic metabolism involves two cytochrome P450 enzymes: CYP2D15 (low capacity, high affinity) and CYP3A12 (high capacity, low affinity). The major pharmacologically active metabolite is CJ-18,518.
Eliminación
Eliminated primarily by the liver. Urinary recovery of maropitant and its major metabolite is minimal (<1%).
Sobredosis
Maropitant has a wide margin of safety.
- Dogs: Tolerance has been confirmed at doses up to 3 times the recommended oral dose (8 mg/kg) for 3 times longer than the maximum duration.
- High-Dose Toxicity (20 mg/kg/day in dogs): Can cause emesis, significant body weight loss (8-15%), ECG changes (slight increases in P-R interval, P wave duration, and QRS amplitude), slightly lower serum albumin, and increased adrenal weights.
- Rodent Studies: Doses up to 30-100 mg/kg PO caused decreased activity, irregular/labored respiration, ataxia, and tremors.
Productos disponibles
Formulaciones
- Oral tablets
- 10 mg/ml injectable solution
- 16 mg oral tablet
- 24 mg oral tablet
- 160 mg oral tablet
Veterinario
- Maropitant Citrate Injectable Solution: 10 mg/mL in 20 mL multidose vials (Cerenia®)
- Maropitant Citrate Oral Tablets: 16 mg, 24 mg, 60 mg, and 160 mg in blister packs (Cerenia®)
- Cerenia 10 mg/ml solution for injection
- Cerenia 16 mg, 24 mg, 60 mg, 160 mg tablets
- Prevomax 10 mg/ml solution for injection
- Vetemex 10 mg/ml solution for injection
Estado regulador
POM-V classification
POM-V classification
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Injectable solution: Store at controlled room temperature 20-25°C (68-77°F). Must be used within 28 days of first vial puncture. Tablets: Packaged in foil to protect from moisture uptake; keep in blister packs until use. Halved tablets show no loss of potency for 48 hours.
Información para el cliente
Nota importante sobre la administración: Los comprimidos no deben envolverse firmemente ni introducirse en alimentos/premios (como pill pockets o queso), ya que esto puede retrasar la disolución y absorción del comprimido.
- Ayuno: Evite el ayuno prolongado antes de la administración de los comprimidos.
- Mareo por movimiento: Para minimizar la aparición de vómitos previos al viaje causados por el propio medicamento, ofrezca a su mascota una comida pequeña o un premio una hora antes de administrar la dosis para el mareo.
- Sitio de inyección: Si su mascota recibió una inyección subcutánea, puede presentarse una leve inflamación o dolor en el sitio de la inyección. (Nota clínica: Los veterinarios suelen refrigerar la solución inyectable, lo cual reduce significativamente el escozor durante la inyección).
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.