Trazodona
Trazodone
Trazodone hydrochloride
También conocido como: Desyrel · Oleptro · Molipaxin · AF-1161 · trazodona · sleepeasy · Trazodone hydrochloride · Trazodonum
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 |
|---|---|---|---|---|---|
| Adjunctive treatment of anxiety-related disorders (Daily medication only) | 1.9 mg/kg/day-16.2 mg/kg/day (mean = 7.3 mg/kg/day) | PO | daily | — | 🌎 NA |
| Adjunctive treatment of anxiety-related disorders (As needed only) | 2.2 mg/kg/day- 14 mg/kg/day (mean 7.7 mg/kg/day) | PO | PRN | — | 🌎 NA |
| Adjunctive treatment of anxiety-related disorders (Daily medication and as needed) | 1.7 mg/kg/day-19.5 mg/kg/day (mean 7.25 mg/kg/day) | PO | daily and PRN | — | 🌎 NA |
| Adjunctive treatment of anxiety-related disorders | 1 mg/kg PO q12h for 7 days, then up to 3 mg/kg PO q12h. | PO | q12h | 7 days initially | 🌎 NA |
| Adjunctive treatment of anxiety-related disorders | 1-4.8 mg/kg PO twice daily; (titrate to effect in 1 mg increments every 7 days). | PO | q12h | — | 🌎 NA |
| Adjunctive treatment of anxiety-related disorders (Situational) | typical starting dose between 2-5 mg/kg and adjusting upwards as necessary to get control (maximum dose 14 mg/kg/day). | PO | PRN | — | 🌎 NA |
- Adjunctive treatment of anxiety-related disorders (Daily medication only): Begin at half target dose for 3 days to build tolerance.
- Adjunctive treatment of anxiety-related disorders (Situational): Given about an hour prior to the onset of anxiety.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
La trazodona es un Antagonista/Inhibidor de la Recaptación de Serotonina 2A (SARI) ampliamente utilizado en medicina veterinaria como ansiolítico y sedante leve.
- Utilidad Clínica: Altamente eficaz para la ansiedad situacional (p. ej., tormentas, fuegos artificiales, visitas al veterinario, viajes) y para facilitar el confinamiento postoperatorio o el reposo en jaula en perros.
- Terapia Adyuvante: A menudo se combina con ISRS (como fluoxetina) o gabapentina para trastornos del comportamiento refractarios.
- Perfil de Seguridad: Generalmente bien tolerado con un amplio margen de seguridad. Posee menos efectos anticolinérgicos y un menor riesgo de convulsiones en comparación con los antidepresivos tricíclicos (ATC).
- Usos en Humanos: Utilizado para tratar la depresión, el comportamiento agresivo, la abstinencia de alcohol/cocaína, la prevención de migrañas y el insomnio.
Mecanismo de acción
Trazodone exerts its anxiolytic and sedative effects through multiple neurochemical pathways:
- Serotonin Reuptake Inhibition: Blocks the serotonin transporter (SERT) → increases extracellular serotonin (5-HT) in the synaptic cleft.
- 5-HT2A Receptor Antagonism: Blocks 5-HT2A receptors → prevents overstimulation by serotonin, contributing to its anxiolytic and antidepressant efficacy. Downregulation of these receptors can augment the efficacy of concurrent SSRIs.
- Active Metabolite: Hepatic metabolism produces m-chlorophenylpiperazine (mCPP), which acts as a direct, non-selective serotonin receptor agonist.
- Alpha-1 Adrenergic Antagonism: Blocks peripheral alpha-1 receptors → can cause mild vasodilation and hypotension.
- Histamine (H1) Antagonism: Weak blockade of H1 receptors contributes to its sedative properties.
Seguridad y advertencias
Contraindicaciones
- Hypersensitivity to trazodone
- Concurrent use of MAO inhibitors (e.g., amitraz, selegiline)
- Glaucoma
- History of seizures
- Urinary retention
- Severe liver disease
Efectos adversos
- Sedation
- Lethargy
- Ataxia
- Cardiac conduction disturbances
- Increased anxiety (paradoxical)
- Aggression (paradoxical)
- Vomiting/gagging
- Increased excitement
- Increased appetite
- Colitis
- Serotonin syndrome (rare, usually with concurrent serotonergic drugs)
- Excitability
- Dry mouth
- Third eyelid protrusion (in cats)
Precauciones
Cardiac & Organ Impairment: Use with caution in patients with severe cardiac disease or hepatic or renal impairment. Pregnancy: FDA Category C. Animal studies show adverse effects at very high doses (15-50X). Weigh potential risks versus benefits in pregnant or nursing animals. Serotonin Syndrome: Risk increases significantly when combined with other serotonergic drugs (e.g., SSRIs, MAOIs, TCAs).
Interacciones farmacológicas
May increase reductions in blood pressure and cause hypotension
Increase risk for GI bleeding; monitor
May increase trazodone blood levels
Use with trazodone may cause additive CNS depressant effects
Trazodone may increase digoxin levels
May increase trazodone blood levels
Increased risk for serotonin syndrome
Increased risk for GI bleeding; monitor
May increase trazodone blood levels; cause additive CNS effects
Increased risk for serotonin syndrome. Commonly used together, but monitor closely.
Contraindicated; high risk of serotonin syndrome
Metabolized by CYP450 2D6; potential for altered metabolism and toxicity
Metabolized by CYP450 2D6; potential for altered metabolism and toxicity
Increased risk of serotonin syndrome, though adjunctive therapy is sometimes used cautiously
Inhibits the breakdown of trazodone, leading to increased blood levels
Increases the breakdown of trazodone, leading to decreased blood levels
May inhibit the breakdown of trazodone (theoretical risk based on ketoconazole similarity)
Monitorización
- Clinical efficacy (behavioral calming)
- Adverse effects (sedation, GI upset, paradoxical excitement)
- Signs of serotonin syndrome (vomiting, diarrhea, seizures, hyperthermia, hyperesthesia, mydriasis)
- Renal function (in patients with pre-existing renal disease)
- Signs of serotonin syndrome (tremors, agitation, hyperthermia)
- Efficacy of anxiety reduction
Farmacocinética
Absorción
In humans, oral bioavailability of immediate-release tablets is about 65%. Presence of food increases absorption (AUC), decreases Cmax, and delays Tmax.
Distribución
Approximately 90-95% bound to plasma proteins. Volume of distribution ranges from 0.47-0.84 L/kg (in humans).
Metabolismo
Extensive hepatic metabolism. Oxidative cleavage via CYP3A4 forms the active metabolite m-chlorophenylpiperazine (mCCP), which is further metabolized to inactive compounds via CYP2D6.
Eliminación
Mostly (70-75%) excreted via renal mechanisms (only 0.13% unchanged in urine). About 21% is excreted in feces.
Sobredosis
No specific information is available regarding trazodone overdoses in veterinary patients. In humans, the incidence of serious toxicity from trazodone overdose alone is low compared with tricyclic antidepressant overdoses. In the event of a substantial overdose, contact an animal poison control center for guidance. Monitor for profound sedation, ataxia, hypotension, and signs of serotonin syndrome.
Productos disponibles
Formulaciones
- Oral tablets (immediate-release)
- Oral tablets (extended-release)
- 100 mg tablets
- 150 mg tablets
- 100 mg capsules
- 150 mg capsules
- 10 mg/ml oral liquid
Etiquetado para humanos
- Trazodone Oral Tablets: 50 mg, 100 mg, 150 mg, & 300 mg; generic; (Rx)
- Trazodone Extended-Release (24-hour) Oral Tablets: 150 mg & 300 mg; Oleptro® (Labopharm); (Rx)
- Desyrel
- Molipaxin
Estado regulador
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store between 20-25°C (68-77°F); excursions are permitted to 15-30°C (59-86°F). Keep in an airtight container and protect from light.
Información para el cliente
- Administración: Preferiblemente administrar con comida para minimizar las molestias gastrointestinales (como vómitos o arcadas).
- Momento: Para la ansiedad situacional (p. ej., visitas al veterinario, fuegos artificiales), administrar 1 a 2 horas antes del evento estresante previsto.
- Observación: Vigile a su mascota en busca de sedación excesiva, letargo o marcha descoordinada (ataxia).
- Efectos Paradójicos: En casos raros, las mascotas pueden mostrar mayor excitación, ansiedad o cambios en el apetito.
- Advertencia Importante: No combinar con otros medicamentos o suplementos (especialmente collares antiparasitarios que contengan amitraz) sin consultar a su veterinario, ya que esto puede provocar una afección rara pero grave llamada síndrome serotoninérgico.
- Comunicación: Informe cualquier efecto adverso imprevisto a su veterinario, ya que la trazodona aún está siendo estudiada para su uso extensivo en perros.
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.