Butorfanol
Butorphanol
Butorphanol tartrate
También conocido como: Stadol · Torbutrol · Torbugesic · Dolorex · Equanol · Alvegesic · Butomidor · Torphasol · levo-BC-2627 · butorphanol tartrate
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Evidencia de dosis v13 auditada
Evidencia revisada no calculableEvidencia revisada no calculable (5)
Solo evidencia; no apta para cálculo automático
Chelonians/minimal sedation
TABLE 127.5. Agent: Butorphanol. Dosage: 0.2 mg/kg IM118,275. Species/Comments: Chelonians/minimal sedation.
Solo evidencia; no apta para cálculo automático
Most species/sedation; preanesthetic
TABLE 127.5. Agent: Butorphanol. Dosage: 0.4–1 mg/kg SC, IM295. Species/Comments: Most species/sedation; preanesthetic.
Solo evidencia; no apta para cálculo automático
Most species/preanesthetic
TABLE 127.5. Agent: Butorphanol. Dosage: 0.5–2 mg/kg IM, or 0.2–0.5 mg/kg IV, IO23. Species/Comments: Most species/preanesthetic.
Solo evidencia; no apta para cálculo automático
Butorphanol combinations follow; see ketamine for combinations; inadequate for analgesia
TABLE 127.5. Agent: Butorphanol. Dosage: —. Species/Comments: Butorphanol combinations follow; see ketamine for combinations; inadequate for analgesia.
Solo evidencia; no apta para cálculo automático
Lizards/administer 30 min before isoflurane for smoother, shorter induction
TABLE 127.5. Agent: Butorphanol. Dosage: 1–1.5 mg/kg SC, IM295. Species/Comments: Lizards/administer 30 min before isoflurane for smoother, shorter induction.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El butorfanol es un agonista parcial opioide sintético ampliamente utilizado en medicina veterinaria en múltiples especies.
- Analgesia: Proporciona analgesia visceral de leve a moderada. Debido a su "efecto techo", dosis más altas no aumentan el alivio del dolor, lo que lo hace inadecuado para dolores intensos (p. ej., procedimientos ortopédicos mayores).
- Antitusígeno: Altamente eficaz para suprimir la tos crónica no productiva (p. ej., traqueobronquitis infecciosa, colapso traqueal) en perros.
- Agente de reversión: Útil de forma única para revertir la profunda depresión respiratoria y del SNC de los agonistas mu puros (como fentanilo, metadona o morfina) manteniendo al mismo tiempo un grado de analgesia mediada por kappa.
- Sedación: Se combina frecuentemente con agonistas alfa-2 (como dexmedetomidina o xilazina) y benzodiazepinas para una sedación sinérgica y contención química.
Perla clínica: Aunque el butorfanol es un excelente antitusígeno y sedante leve en animales pequeños, su duración de acción muy corta (a menudo <1 hora para la analgesia en perros) limita su utilidad como analgésico primario. Por el contrario, es un analgésico visceral altamente eficaz y comúnmente utilizado en caballos (p. ej., para cólicos).
Mecanismo de acción
Butorphanol exerts its effects by interacting with specific opioid receptors in the central nervous system:
- Kappa (κ) and Sigma (σ) Agonist: Activation of κ-receptors in the limbic system and spinal cord provides visceral analgesia and sedation.
- Mu (μ) Antagonist: Competitively binds to and blocks μ-receptors. This antagonism is responsible for its ability to reverse pure μ-agonist drugs and is the reason for its analgesic "ceiling effect."
- Antitussive Mechanism: Directly suppresses the medullary cough center, elevating the threshold to stimuli (like CO2) without depressing respiratory center sensitivity as profoundly as pure agonists.
- Cellular Pathway: Binds to κ-receptors → inhibits adenylate cyclase → decreases intracellular cAMP → closes voltage-gated calcium channels and opens potassium channels → hyperpolarization and reduced neuronal excitability.
Seguridad y advertencias
Contraindicaciones
- Known hypersensitivity to butorphanol
- Lower respiratory tract conditions with copious mucous production (suppressing cough prevents clearance)
- Caution in patients with head trauma, increased CSF pressure, or severe CNS dysfunction (e.g., coma)
- Caution in severe liver disease, renal insufficiency, hypothyroidism, or Addison's disease
- Caution in dogs with heartworm disease (safety not established)
Efectos adversos
- Sedation and ataxia
- Anorexia or diarrhea (rare in small animals)
- Respiratory depression (mild compared to pure agonists)
- CNS excitement, head tossing, and increased ambulation (especially in horses at high doses or rapid IV administration)
- Decreased gastrointestinal motility and potential ileus (horses)
- Nystagmus, salivation, seizures, and hyperthermia (at massive overdoses in horses)
Precauciones
MDR1 (ABCB1) Mutation Warning: Dogs with the MDR1 mutation (e.g., Collies, Australian Shepherds) may develop pronounced and prolonged sedation. Reduce the dose by 25% in heterozygous dogs and by 30-50% in homozygous mutant dogs.
Geriatric/Debilitated Patients: Use with caution and consider dose reductions.
Hepatic/Renal Impairment: The manufacturer advises against use in dogs with a history of liver disease. Use cautiously in renal insufficiency.
Pregnancy/Nursing: Category C (human). Safe for use if used cautiously in dogs/cats, but manufacturer does not recommend use in pregnant bitches, foals, weanlings, or breeding horses.
Interacciones farmacológicas
May cause increased CNS or respiratory depression; dosage may need to be decreased.
Could potentially decrease the metabolism of butorphanol, prolonging its effects.
Butorphanol may antagonize analgesic effects, but will also reverse sedative and respiratory depressant effects.
May cause increased conjunctival changes when used concurrently.
Could potentially decrease the metabolism of butorphanol.
Reduces the doses of other drugs required for induction and maintenance of anaesthesia
Addition of butorphanol will reduce analgesia produced from the full mu agonist; combination is not recommended for analgesia
Synergistic sedation
Synergistic sedation and analgesia
Butorphanol's mu-antagonist properties may block or partially reverse the analgesic effects of full mu-agonists. Higher doses of full mu-agonists may be required.
Monitorización
- Analgesic and/or antitussive efficacy
- Respiratory rate and depth
- Appetite and bowel function
- CNS effects (sedation vs. excitement)
Farmacocinética
Vida media
Absorción
Completely absorbed in the gut when administered orally, but due to a high first-pass effect, only about 16% (1/6th) reaches systemic circulation. Completely absorbed following IM administration.
Distribución
Well distributed. Highest levels found in liver, kidneys, and intestine. Approximately 80% bound to plasma proteins. Crosses the placenta (neonatal levels roughly equivalent to maternal) and distributes into maternal milk.
Metabolismo
Metabolized in the liver, primarily by hydroxylation, as well as N-dealkylation and conjugation. Metabolites do not exhibit analgesic activity.
Eliminación
Metabolites and parent compound are mainly excreted into the urine (only 5% unchanged). 11-14% is excreted into the bile and eliminated in feces.
Sobredosis
Acute life-threatening overdoses are unlikely (LD50 in dogs is 50 mg/kg). However, because veterinary injection comes in two highly different strengths (0.5 mg/mL and 10 mg/mL), inadvertent overdoses can occur in small animals.
Clinical Signs: CNS effects (profound sedation or excitement), cardiovascular changes, and respiratory depression.
Treatment:
- Administer intravenous naloxone immediately to reverse opioid effects.
- Provide supportive measures: IV fluids, oxygen therapy, vasopressors, and mechanical ventilation if required.
- If seizures occur and persist, use diazepam for control.
Productos disponibles
Formulaciones
- Veterinary Injection: 0.5 mg/mL, 2 mg/mL, 10 mg/mL
- Veterinary Tablets: 1 mg, 5 mg, 10 mg
- Human Injection: 1 mg/mL, 2 mg/mL
- Human Nasal Spray: 10 mg/mL
Veterinario
- Butorphanol Tartrate Injection: 0.5 mg/mL (Torbutrol)
- Butorphanol Tartrate Injection: 2 mg/mL (Torbugesic-SA)
- Butorphanol Tartrate Injection: 10 mg/mL (Torbugesic, Dolorex, Butorject, Torphaject, Equanol)
- Butorphanol Tartrate Tablets: 1 mg, 5 mg, and 10 mg (Torbutrol)
Etiquetado para humanos
- Butorphanol Tartrate Injection: 1 mg/mL, 2 mg/mL (Stadol)
- Butorphanol Nasal Spray: 10 mg/mL
Estado regulador
Subject to specific member state controlled drug regulations.
Classified as POM-V (Prescription Only Medicine - Veterinarian).
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
The injectable product should be stored out of bright light and at room temperature; avoid freezing.
Información para el cliente
¿Qué es este medicamento? El butorfanol es un medicamento utilizado para aliviar la tos, proporcionar un alivio leve del dolor o actuar como sedante antes de procedimientos veterinarios.
¿Qué debo esperar?
- Es probable que su mascota se sienta somnolienta o ligeramente descoordinada (tambaleante). Esto es normal, pero debe mantenerla en un entorno seguro y tranquilo (p. ej., evitar escaleras) hasta que pasen los efectos.
- Si se receta para la tos, debería notar una disminución significativa en los episodios de tos.
Advertencias importantes:
- No administre más de lo recetado. Administrar demasiado no aumentará el alivio del dolor, pero puede aumentar los efectos secundarios.
- Si la tos de su mascota cambia de una tos "seca y perruna" a una tos "húmeda y productiva", comuníquese con su veterinario. Suprimir una tos húmeda puede atrapar moco en los pulmones.
- Informe a su veterinario sobre cualquier cambio significativo en el comportamiento, pérdida de apetito o estreñimiento/diarrea severos.
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.