Lomustina
Lomustine
1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU)
También conocido como: CeeNu · Belustine · Cecenu · CiNU · Citosta · Lomeblastin · Lucostine · Prava · CCNU · Gleostine · lomustinum · NSC-79037 · RB1509 · WR-139017
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Esta dosis se basa en la superficie corporal (mg/m²). Convierta el peso en superficie corporal antes de administrarla.
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 |
|---|---|---|---|---|---|
| Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors, histiocytic sarcomas) | 50-90 mg/m2 | PO | every 2-6 weeks | — | 🌎 NA |
| All uses (brain tumours, mast cell tumours, lymphoma, histiocytic sarcoma) | 60-80 mg/m2 | PO | q3-4wk | As directed by oncologist | 🌍 EU |
- Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors, histiocytic sarcomas): Dosed in mg/m2, NOT mg/kg. Exact protocol depends on indication.
- All uses (brain tumours, mast cell tumours, lymphoma, histiocytic sarcoma): S-Adenosylmethionine and silybin may be used to prevent or treat hepatotoxicity.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors) | 60 mg/m2 | PO | every 6 weeks | — | 🌎 NA |
| Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors) | 10 mg | PO | every 3 weeks | — | 🌎 NA |
| All uses | 30-60 mg/m2 | PO | q4-6wk | As directed by oncologist | 🌍 EU |
- Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors): Administered as a single 10 mg total dose.
- All uses: Dose is suggested but not well established. Specialist advice should be sought, as dosing intervals may need to be increased due to delayed myelosuppression.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
La lomustina (conocida comúnmente como CCNU) es un agente antineoplásico alquilante de nitrosourea altamente lipofílico. Debido a su alta solubilidad en lípidos, atraviesa fácilmente la barrera hematoencefálica, lo que la hace excepcionalmente valiosa para el tratamiento de neoplasias del sistema nervioso central (SNC).
Indicaciones veterinarias clave:
- Mastocitomas (MCTs): Utilizada frecuentemente como terapia de primera línea o de rescate en perros y gatos.
- Histiocitosis maligna: Considerada un tratamiento de elección para formas localizadas o diseminadas en perros.
- Linfoma: A menudo utilizada como agente de rescate para linfoma multicéntrico recidivante, o como agente primario para linfoma epiteliotrópico (cutáneo).
- Neoplasias del SNC: Utilizada para tumores cerebrales primarios (p. ej., gliomas) o lesiones metastásicas en el SNC.
Perla clínica: La lomustina es conocida por causar hepatotoxicidad retardada, acumulativa y potencialmente irreversible en perros. Muchos oncólogos veterinarios recomiendan encarecidamente la administración concurrente de hepatoprotectores (como SAMe y silimarina).
Mecanismo de acción
Lomustine is a cell cycle-phase nonspecific antineoplastic drug, meaning it is toxic to cancer cells regardless of their current phase in the division cycle.
- Alkylating Activity: It undergoes spontaneous decomposition in vivo to form reactive intermediates. These intermediates transfer alkyl groups to DNA and RNA → causing cross-linking of DNA strands → preventing DNA replication and RNA transcription.
- Carbamoylation: The drug also causes carbamoylation of cellular proteins (specifically lysine residues) → inhibits DNA repair enzymes, preventing the cancer cell from fixing the alkylation damage, ultimately leading to apoptosis.
Seguridad y advertencias
Contraindicaciones
- Pre-existing severe bone marrow depression
- Active infections
- Pregnancy (Teratogenic - FDA Category D)
- Nursing/lactating animals
- Pre-existing bone marrow suppression
- Pre-existing liver disease
- Pregnancy and lactation
Efectos adversos
- Bone marrow depression (anemia, thrombocytopenia, leukopenia) - nadirs typically at 1-6 weeks
- Hepatotoxicity (delayed, cumulative, chronic, and irreversible in dogs)
- Stomatitis
- Alopecia
- Corneal de-epithelization
- Renal toxicity (rare)
- Pulmonary infiltrates or fibrosis (rare)
- Myelosuppression (dose-limiting; severe neutropenia and thrombocytopenia)
- Hepatotoxicity (cumulative, dose-related, potentially irreversible in dogs)
- Gastrointestinal toxicity (vomiting, diarrhea, anorexia)
Precauciones
Use only when potential benefits outweigh risks in patients with pre-existing anemia, bone marrow depression, pulmonary function impairment, current infection, impaired renal function, or sensitivity to lomustine. Extreme caution is required in patients who have received previous chemotherapy or radiotherapy due to compromised bone marrow reserves. Hepatotoxicity in dogs can be severe, delayed, and irreversible. Teratogenic in laboratory animals; suppresses gonadal function. Nursing puppies/kittens should receive milk replacer if the mother is treated.
Interacciones farmacológicas
May increase the risk of severe infection due to additive immunosuppression.
Additive bone marrow depression; concurrent use should be avoided or strictly monitored.
Increased risk of vaccine-induced infection or decreased vaccine efficacy; use with extreme caution or avoid during therapy.
Increased risk of severe and potentially fatal bone marrow suppression.
Altered metabolism of lomustine, which requires hepatic microsomal enzyme hydroxylation. Use with caution.
Enhances the toxicity of lomustine (reported in humans).
Monitorización
- CBC with platelets one week after dosing and prior to next dose (If platelets < 200,000/mcl, stop therapy until thrombocytopenia is resolved)
- Liver function tests (ALT, AST, ALP, Bilirubin) initially before starting treatment and then every 3-4 months
- Complete Blood Count (CBC) including platelets, particularly 7-14 days post-administration (and up to 6 weeks in cats)
- Liver function tests (ALT, AST, ALP, Bilirubin) prior to every dose
- Clinical signs of gastrointestinal toxicity
Farmacocinética
Vida media
Absorción
Absorbed rapidly and extensively from the GI tract. Some absorption occurs after topical administration.
Distribución
Lomustine and its active metabolites are widely distributed in the body. Highly lipophilic. While parent lomustine is not detected in the CSF, its active metabolites cross the blood-brain barrier and are detected in substantial concentrations.
Metabolismo
Metabolized extensively in the liver to both active and inactive metabolites.
Eliminación
Eliminated primarily in the urine.
Sobredosis
Because of the severe potential toxicity of the drug (profound myelosuppression and hepatotoxicity), overdoses should be treated aggressively.
- Employ gut emptying protocols (emesis, activated charcoal) immediately if exposure was recent and the patient is asymptomatic.
- Provide aggressive supportive care and monitor CBC and liver enzymes closely.
- Consult an animal poison control center or a veterinary oncologist for specific guidance.
Productos disponibles
Formulaciones
- Capsules
- 40 mg oral capsule
Etiquetado para humanos
- Lomustine Capsules: 10 mg, 40 mg & 100 mg with mannitol; CeeNu® (Bristol Labs Oncology); (Rx)
- 10 mg capsule
- 40 mg capsule
- 100 mg capsule
Estado regulador
POM (Prescription Only Medicine). Handled under cascade.
POM-V. Handled under the prescribing cascade.
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store capsules in well-closed containers at room temperature. Expiration dates of two years are assigned after manufacture.
Información para el cliente
Directrices importantes de seguridad y manipulación:
- Precauciones citotóxicas: La lomustina es un fármaco de quimioterapia. Use guantes desechables al manipular las cápsulas. No abra, triture ni parta las cápsulas.
- Gestión de residuos: El fármaco y sus metabolitos tóxicos pueden detectarse en la orina y las heces de la mascota hasta 24 horas (algunos protocolos recomiendan precauciones durante 48-72 horas) después de una dosis. Use guantes al limpiar orina, heces o vómito, y lávese bien las manos después. Las mujeres embarazadas o personas inmunosuprimidas deben evitar manipular el fármaco o los residuos de la mascota.
Cuándo contactar al veterinario:
- La lomustina puede causar una supresión grave de la médula ósea y daño hepático.
- Contacte a su veterinario inmediatamente si su mascota desarrolla signos de infección, tiene fiebre, presenta hematomas o sangrado inusual, tiene coloración amarillenta en el blanco de los ojos o en las encías (ictericia), experimenta vómitos o diarrea persistentes, o simplemente se muestra letárgica y enferma.
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.