Clorazepato
Clorazepate
Clorazepate dipotassium
También conocido como: Tranxene-SD · Gen-Xene · Tranxene T-tab · Abbott-35616 · AH-3232 · 4306-CB · clorazepic acid · dipotassium clorazepate · dikalii clorazepas
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 medication in the treatment of seizures (in combination with phenobarbital) | 1-2 mg/kg PO q12h, but may need to divide q12h dose and give q8h to minimize adverse effects and maintain therapeutic levels | PO | q8-12h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures (in combination with phenobarbital) | 0.5-1 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures | 2-4 mg/kg PO twice daily, some dogs may require three times daily | PO | q8-12h | — | 🌎 NA |
| Third-line agent for seizures | 1-2 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Management of cluster seizures | 0.5-2 mg/kg two to three times daily | PO | q8-12h | 48-96 hours | 🌎 NA |
| Adjunctive therapy for fears and phobias | 11.25-22.5 mg per dog PO once to twice daily | PO | q12-24h | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 22.5 mg for large dogs, 11.25 mg for medium dogs and 5.6 mg for small dogs PO | PO | prn | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 0.55-2.2 mg/kg PO as needed up to q8h | PO | up to q8h | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 0.2-1 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
- Adjunctive medication in the treatment of seizures (in combination with phenobarbital): No advantage gained with using sustained release products. May affect phenobarb levels; monitor 2 and 4 weeks later.
- Management of cluster seizures: Give immediately after first seizure and stop after 48-96 hours. Used only during seizure activity, not as maintenance.
- Adjunctive therapy for fears and phobias: Recommends the sustained-delivery product (Tranxene-SD).
- Adjunctive therapy for fears and phobias: Using sustained delivery product. Adjust dosage according to dog's response.
- Adjunctive therapy for fears and phobias: Titrate to clinical sedation; dose may vary for individual dogs.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| Anxiolytic or for compulsive behaviors | 0.2-0.5 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Alternative drug to phenobarbital for seizures | 3.75-7.5 mg (total dose per cat) PO once to twice daily | PO | q12-24h | — | 🌎 NA |
- Alternative drug to phenobarbital for seizures: Similar precautions are necessary as described for diazepam use in cats (risk of hepatic necrosis).
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El clorazepato es una benzodiacepina utilizada principalmente en medicina veterinaria como anticonvulsivo adyuvante y para el manejo de trastornos del comportamiento relacionados con la ansiedad o fobias.
- Perla clínica: El clorazepato es un profármaco. Requiere el ambiente ácido del estómago para ser descarboxilado rápidamente a su metabolito activo, nordiazepam (desmetildiazepam), antes de su absorción.
- En perros, se combina frecuentemente con fenobarbital para convulsiones refractarias. Aunque puede desarrollarse tolerancia a sus efectos anticonvulsivos, se reporta que ocurre con menor rapidez que con el clonazepam.
- En gatos, se utiliza como ansiolítico y ocasionalmente como alternativa al fenobarbital para el manejo de convulsiones, aunque se requiere precaución debido al riesgo de hepatotoxicidad idiosincrásica asociada con las benzodiacepinas orales en felinos.
Mecanismo de acción
Benzodiazepines exert their effects by enhancing the inhibitory activity of gamma-aminobutyric acid (GABA) in the central nervous system.
- Mechanism: They bind to specific allosteric sites on the GABA-A receptor complex → increases the frequency of chloride channel opening → cellular hyperpolarization → decreased neuronal excitability.
- This depression of subcortical CNS levels (primarily limbic, thalamic, and hypothalamic) produces the characteristic anxiolytic, sedative, skeletal muscle relaxant, and anticonvulsant effects.
- Other postulated mechanisms include antagonism of serotonin and diminished release or turnover of acetylcholine in the CNS.
Seguridad y advertencias
Contraindicaciones
- Hypersensitivity to benzodiazepines
- Significant liver disease/dysfunction
- Acute narrow angle glaucoma
- Fear-induced aggression (relative contraindication; may disinhibit bite inhibition)
Efectos adversos
- Sedation (most common)
- Ataxia
- Physical dependence (with chronic use)
- Acute hepatic necrosis (idiosyncratic in cats)
- Paradoxical excitation or disinhibition of aggression
Precauciones
Use with extreme caution in aggressive animals, particularly those with fear-induced aggression, as benzodiazepines can disinhibit anxiety-based bite inhibition and provoke attacks. Benzodiazepines may exacerbate myasthenia gravis. Safe use during pregnancy is not established (FDA Category D in humans; teratogenic effects noted in lab animals). The active metabolite, nordiazepam, is distributed into milk and may affect nursing neonates. Abrupt withdrawal after chronic use can precipitate severe rebound seizures.
Interacciones farmacológicas
May increase serum levels of benzodiazepines by inhibiting their metabolism.
May decrease the metabolism of benzodiazepines, leading to prolonged effects.
Additive CNS depression; may cause profound sedation or respiratory depression.
May decrease the metabolism of benzodiazepines.
Complex interaction: Clorazepate may initially increase phenobarbital serum levels. Over time, clorazepate levels may decrease, leading to decreased phenobarbital levels. Requires close monitoring.
May decrease clorazepate concentrations.
May induce hepatic microsomal enzymes and decrease the pharmacologic effects of benzodiazepines.
Monitorización
- Clinical efficacy (seizure frequency or behavioral improvement)
- Adverse effects (sedation, ataxia)
- Liver enzymes (especially critical in cats due to risk of acute hepatic necrosis)
- Phenobarbital serum levels (if used concurrently, monitor at 2 and 4 weeks after adding clorazepate)
Farmacocinética
Absorción
In dogs, peak serum levels generally occur within 1-2 hours.
Distribución
Volume of distribution is about 1.8 L/kg after multiple dosing in dogs. Nordiazepam is distributed into milk.
Metabolismo
Clorazepate is a prodrug that is rapidly decarboxylated in the acidic environment of the stomach to nordiazepam (active) and other metabolites.
Eliminación
Eliminated primarily via hepatic metabolism and subsequent renal excretion of metabolites.
Sobredosis
When used alone, clorazepate overdoses are generally limited to significant CNS depression (confusion, coma, decreased reflexes, profound sedation).
- Treatment: Consists of standard protocols for removing and/or binding the drug in the gut (e.g., emesis if asymptomatic and recent, activated charcoal) and supportive systemic measures.
- The use of analeptic agents (CNS stimulants such as caffeine, amphetamines) is generally not recommended.
- Flumazenil (a specific benzodiazepine reversal agent) may be considered for very serious, life-threatening overdoses.
Productos disponibles
Formulaciones
- Capsules
- Sustained-release tablets
Etiquetado para humanos
- Clorazepate Dipotassium Tablets: 3.75 mg, 7.5 mg, & 15 mg (Tranxene T-tab; generic)
Estado regulador
Sin datos reguladores para: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Clorazepate dipotassium is unstable in the presence of water. Keep the desiccant packets in the original container of the capsules and tablets. Consider adding a desiccant packet to the prescription vial when dispensing large quantities.
Información para el cliente
ADVERTENCIA CRÍTICA: No deje de administrar este medicamento abruptamente. La retirada repentina puede desencadenar convulsiones graves que ponen en peligro la vida. Consulte siempre a su veterinario para obtener un programa de reducción gradual si es necesario suspender la medicación.
- La constancia es clave: Un factor importante en el fracaso de la terapia anticonvulsiva es el olvido de dosis. Administre el medicamento a la misma hora todos los días.
- Gatos: Si su gato presenta falta de apetito, vómitos o coloración amarillenta en el blanco de los ojos o encías (ictericia), contacte a su veterinario inmediatamente, ya que esto podría indicar una reacción hepática grave.
- Efectos secundarios: Su mascota puede parecer somnolienta, descoordinada o torpe, especialmente al comenzar el tratamiento. Esto suele mejorar a medida que su cuerpo se ajusta.
- Almacenamiento: Mantenga el medicamento en su envase original con el sobre desecante (absorbente de humedad), ya que el fármaco se degrada rápidamente al exponerse a la humedad.
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.