地西泮 (Diazepam)
Diazepam
7-chloro-1-methyl-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
別名: Valium · Diastat · Diazepam Intensol · Diazedor · Diazemuls · Stesolid · Diazepam Rectubes · diazepamum · LA-III · NSC-77518 · Ro5-2807
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
經審核的 v13 劑量證據
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Persistent seizures during an insulinoma hypoglycemic crisis despite IV dextrose
Diazepam if seizures persist despite IV dextrose
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概覽
地西泮 (Diazepam) 是一種經典的長效苯二氮平類 (Benzodiazepine) 衍生物，在獸醫學中廣泛用於其抗焦慮、肌肉鬆弛、安眠、促進食慾及抗痙攣的特性。
臨床要點：
- 癲癇管理： 地西泮是緊急治療癲癇重積狀態 (status epilepticus) 和叢集性癲癇的首選藥物。然而，由於其作用時間短且容易快速產生耐受性，通常不適合作為犬隻的長期維持性抗癲癇藥物。
- 貓咪注意事項： 雖然貓咪較不易產生耐受性，但口服地西泮在貓咪身上極具爭議，因為有引發特異體質性、潛在致命的猛爆性肝壞死的風險。
- 劑型特性： 注射劑型含有丙二醇 (propylene glycol)，若靜脈注射過快可能導致低血壓、心跳過緩及心臟毒性。此外，它容易吸附在 PVC 塑膠上，因此不適合儲存在塑膠針筒中或透過標準靜脈輸液袋長時間給藥。
作用機制
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.
安全性與警告
禁忌症
- 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)
不良反應
- 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)
注意事項
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.
藥物相互作用
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)
監測
- 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
藥物動力學
半衰期
吸收
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%.
分佈
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).
代謝
Metabolized in the liver to several pharmacologically active metabolites, including desmethyldiazepam (nordiazepam), temazepam, and oxazepam.
排除
Metabolites are conjugated with glucuronide and eliminated primarily in the urine.
過量
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.
可用產品
劑型
- 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
獸醫用
- None (No veterinary-labeled products available)
- Diazedor
- Diazemuls
- Diazepam Rectubes
人用標示
- 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
各地核准狀態
POM-V, POM
POM-V, POM
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儲存與穩定性
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.
飼主須知
- 儲存方式： 請放置於兒童及其他寵物無法觸及之處。保存在緊密閉合的容器中。此為管制藥品。
- 給藥方式： 請嚴格依照獸醫師的指示給藥。若在家中透過直腸給藥以控制癲癇，請仔細遵循獸醫師指導的安全給藥方式。
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貓咪的重大警告： 若您的貓咪在服用此藥物期間出現食慾不振、嘔吐，或眼白、牙齦變黃（黃疸）的現象，請立即停藥並立刻聯絡您的獸醫師，因為這可能是嚴重肝臟損傷的徵兆。
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