Diazepam
7-chloro-1-methyl-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
También conocido como: Valium · Diastat · Diazepam Intensol · Diazedor · Diazemuls · Stesolid · Diazepam Rectubes · diazepamum · LA-III · NSC-77518 · Ro5-2807
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Evidencia posológica v13 auditada
Evidencia revisada no calculableEvidencia revisada no calculable (1)
Solo evidencia; no apta para cálculo automático
Persistent seizures during an insulinoma hypoglycemic crisis despite IV dextrose
Diazepam if seizures persist despite IV dextrose
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El diazepam es un derivado clásico de las benzodiacepinas de acción prolongada, ampliamente utilizado en medicina veterinaria por sus propiedades ansiolíticas, relajantes musculares, hipnóticas, estimulantes del apetito y anticonvulsivantes.
Perlas clínicas:
- Manejo de convulsiones: El diazepam es el fármaco de elección de primera línea para el tratamiento de emergencia del estado epiléptico y las convulsiones en racimo. Sin embargo, generalmente es ineficaz como anticonvulsivante de mantenimiento a largo plazo en perros debido a su corta duración de acción y al rápido desarrollo de tolerancia.
- Consideraciones en felinos: Aunque la tolerancia es menos problemática en gatos, la administración oral de diazepam es altamente controvertida debido al riesgo de necrosis hepática fulminante idiosincrásica, que puede ser mortal.
- Particularidad de la formulación: La formulación inyectable contiene propilenglicol, que puede causar hipotensión, bradicardia y cardiotoxicidad si se administra por vía intravenosa demasiado rápido. Además, se adsorbe fácilmente a los plásticos de PVC, lo que lo hace inadecuado para su almacenamiento en jeringas de plástico o para la administración prolongada a través de bolsas de fluidos IV estándar.
Mecanismo de acción
Diazepam exerts its effects by binding to specific allosteric sites on GABA-A receptors in the central nervous system (primarily in the limbic system, thalamus, and hypothalamus).
- Binding to the benzodiazepine site → enhances the affinity of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) for its receptor.
- This facilitation → increases the frequency of chloride channel opening → influx of chloride ions → neuronal hyperpolarization.
- The resulting hyperpolarization leads to profound CNS depression, producing anxiolytic, sedative, muscle relaxant, and anticonvulsant effects.
Seguridad y advertencias
Contraindicaciones
- Known hypersensitivity to benzodiazepines
- Cats exposed to chlorpyrifos (potentiates organophosphate toxicity)
- Significant liver disease (especially in cats)
- Intra-carotid artery injections (must be strictly avoided)
- CNS depression
- Respiratory depression
- Severe muscle weakness
- Hepatic impairment (may worsen hepatic encephalopathy)
- Long-term treatment of behavioural disorders (due to risks of disinhibition and interference with memory/learning)
Efectos adversos
- Sedation and ataxia (most common)
- Dogs: Paradoxical CNS excitement/agitation (especially at doses >0.8 mg/kg)
- Dogs: Increased appetite
- Cats: Idiosyncratic hepatic failure (with oral use)
- Cats: Behavior changes (irritability, depression, aberrant demeanor)
- Horses: Muscle fasciculations, weakness, ataxia, recumbency (at doses >0.2 mg/kg)
- Hypotension and phlebitis (with rapid IV injection)
- Muscle weakness
- Paradoxical excitation and aggression (especially with rapid IV injection or oral overdose in dogs)
- Pain and erratic absorption (IM injection)
- Fulminant hepatic necrosis (cats, repeated oral dosing)
- Thrombophlebitis (associated with propylene glycol injectable formulations)
Precauciones
Intravenous Administration: Inject IV slowly (over 1-3 minutes). Rapid injection, especially in small animals or neonates, may cause hypotension or cardiotoxicity secondary to the propylene glycol vehicle. Flush the IV catheter with fluids after administration to help prevent thrombophlebitis.
Feline Hepatotoxicity: Use in cats is controversial due to reports of serious, potentially fatal idiosyncratic hepatotoxicity associated with oral administration. Baseline and follow-up liver function tests are strongly recommended if used.
- Patient Selection: Use cautiously in patients with hepatic or renal disease, debilitated or geriatric patients, and those in coma, shock, or with significant respiratory depression.
- Behavioral Disinhibition: Use very cautiously in aggressive patients, as it may disinhibit anxiety that normally suppresses aggressive behavior.
- Working Animals: May impair the abilities of working animals.
- Toxicity Treatment: Do not use to treat paradoxical CNS stimulation caused by human sleep aids (zolpidem, eszopiclone); use phenothiazines or phenobarbital instead.
- Pregnancy: May be teratogenic (FDA Category D). Use during the first trimester only if benefits clearly outweigh risks.
Interacciones farmacológicas
May increase diazepam levels
May decrease oral diazepam absorption
May increase diazepam levels by inhibiting metabolism
May decrease metabolism of benzodiazepines
Additive CNS depression effects may occur
May decrease diazepam levels
Diazepam may increase digoxin levels
May decrease the metabolism of benzodiazepines
May decrease oral diazepam absorption
May inhibit the metabolism of diazepam and increase levels
May decrease diazepam concentrations
May decrease diazepam concentrations
May increase diazepam levels
May induce hepatic microsomal enzymes and decrease the pharmacologic effects of benzodiazepines
Enhanced sedative effect
Enhanced sedative effect
Diazepam reduces the dose requirement of other anaesthetic agents
Can be used in combination for management of severe behavioural responses
Reverses the effects of diazepam (benzodiazepine antagonist)
Monitorización
- Horses should be observed carefully after receiving this drug.
- Cats receiving oral diazepam must have baseline liver function tests. Repeat and discontinue drug if emesis, lethargy, inappetence, or ataxia develop.
- When used for seizure control in cats, obtain serum levels 5 days after beginning therapy (therapeutic goal: 200-700 ng/mL or 2500-700 nmol/L).
- Hepatic function (especially in cats)
- Respiratory rate and effort
- Level of CNS depression / sedation
- Seizure activity
Farmacocinética
Vida media
Absorción
Rapidly absorbed following oral administration (peak plasma levels within 30 mins to 2 hours). Slowly and incompletely absorbed following IM administration. Rectal bioavailability in dogs is <10% for parent drug, but ~80% when factoring in active metabolites. Intranasal bioavailability in dogs is ~80%.
Distribución
Highly lipid soluble and widely distributed throughout the body. Readily crosses the blood-brain barrier. Highly bound to plasma proteins (87% in horses, 98-99% in humans).
Metabolismo
Metabolized in the liver to several pharmacologically active metabolites, including desmethyldiazepam (nordiazepam), temazepam, and oxazepam.
Eliminación
Metabolites are conjugated with glucuronide and eliminated primarily in the urine.
Sobredosis
When administered alone, diazepam overdoses are generally limited to significant CNS depression (confusion, coma, decreased reflexes, etc.). Hypotension, respiratory depression, and cardiac arrest have been reported in human patients, but are quite rare.
Treatment:
- Standard protocols for removing and/or binding the drug in the gut if taken orally (e.g., emesis, activated charcoal).
- Supportive systemic measures (fluids, respiratory support if needed).
- The use of analeptic agents (CNS stimulants like caffeine) is generally not recommended.
- Flumazenil (a specific benzodiazepine antagonist) may be considered for adjunctive treatment of severe overdoses.
Productos disponibles
Formulaciones
- Oral tablets
- Oral solution
- Injectable solution
- Rectal gel
- Injectable: 5 mg/ml emulsion (e.g., Diazemuls)
- Oral: 2 mg, 5 mg, 10 mg tablets
- Oral: 2 mg/5 ml solution
- Rectal: 2 mg/ml and 4 mg/ml solutions
- Rectal: 10 mg suppositories
Veterinario
- None (No veterinary-labeled products available)
- Diazedor
- Diazemuls
- Diazepam Rectubes
Etiquetado para humanos
- Diazepam Oral Tablets: 2 mg, 5 mg, & 10 mg (Valium, generic)
- Diazepam Oral Solution: 1 mg/mL and 5 mg/mL (Diazepam Intensol)
- Diazepam Injection: 5 mg/mL
- Diazepam Rectal Gel: 2.5 mg, 10 mg, & 20 mg (Diastat)
- Stesolid
Estado regulador
POM-V, POM
POM-V, POM
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store all products at room temperature (15°-30°C). Protect injection from freezing and light. Protect oral forms from light. Important: Diazepam adsorbs to plastic; do not store drawn up in plastic syringes or administer through PVC IV bags/tubing for prolonged periods.
Información para el cliente
- Almacenamiento: Manténgase fuera del alcance de los niños y otras mascotas. Almacenar en recipientes herméticamente cerrados. Este es una sustancia controlada.
- Administración: Administre exactamente según lo prescrito. Si utiliza la vía rectal para convulsiones en casa, siga cuidadosamente las instrucciones de su veterinario sobre cómo administrar la dosis de forma segura.
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ADVERTENCIA CRÍTICA PARA GATOS: Si su gato está tomando este medicamento y desarrolla falta de apetito, vómitos o muestra un color amarillento en el blanco de los ojos o en las encías (ictericia), suspenda el medicamento y contacte a su veterinario inmediatamente, ya que esto puede ser un signo de daño hepático grave.
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.