ジアゼパム

動物種別の用量

投与経路

禁忌

• 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)

有害事象

• 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)
• Sedation
• Muscle weakness
• Ataxia
• 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)

薬物相互作用

• Amitriptyline · May increase diazepam levels
• Antacids · May decrease oral diazepam absorption
• Azole Antifungals (itraconazole, ketoconazole) · May increase diazepam levels by inhibiting metabolism
• Cimetidine · May decrease metabolism of benzodiazepines · moderate
• CNS Depressants (barbiturates, narcotics, anesthetics) · Additive CNS depression effects may occur
• Dexamethasone · May decrease diazepam levels
• Digoxin · Diazepam may increase digoxin levels · moderate
• Erythromycin · May decrease the metabolism of benzodiazepines
• Mineral Oil · May decrease oral diazepam absorption
• Omeprazole · May inhibit the metabolism of diazepam and increase levels · moderate
• Phenobarbital · May decrease diazepam concentrations · moderate
• Phenytoin · May decrease diazepam concentrations
• Quinidine · May increase diazepam levels
• Rifampin · May induce hepatic microsomal enzymes and decrease the pharmacologic effects of benzodiazepines

モニタリング

• 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

過量投与

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.