納洛酮
Naloxone
Naloxone hydrochloride, N-allylnoroxymorphone
別名: Narcan · N-allylnoroxymorphone · naloxona · EN-15304 · naloxoni · Naloxonum · Naloxone hydrochloride
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
經審核的非計算證據經審核的非計算證據 (2)
只供證據參考，不會自動計算
Green tree monitors/reversal of butorphanol
TABLE 127.5. Agent: Naloxone. Dosage: 4 mg/kg IM95. Species/Comments: Green tree monitors/reversal of butorphanol.
只供證據參考，不會自動計算
Corn snakes, bearded dragons, red-eared sliders/µ-opioid agonist reversal
TABLE 127.5. Agent: Naloxone. Dosage: 0.04–2 mg/kg SC304,305,307,309. Species/Comments: Corn snakes, bearded dragons, red-eared sliders/µ-opioid agonist reversal.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
納洛酮 (Naloxone) 是一種純鴉片類拮抗劑，在獸醫學中主要用於逆轉鴉片類促效劑的作用（如呼吸抑制、鎮靜和煩躁不安）。它是鴉片類藥物過量時的救命解毒劑。
除了主要用途外，目前也在研究將其用於治療各種類型的休克（敗血性、低血容性、心因性），以及透過阻斷內源性腦內啡來抑制追尾等自殘行為。
臨床要點： 納洛酮本身沒有鎮痛作用。當用於逆轉鴉片類藥物引起的呼吸抑制時，它會同時逆轉鴉片類藥物的鎮痛效果，可能導致疼痛突然恢復並引發兒茶酚胺釋放。
作用機制
Naloxone acts as a competitive antagonist at opioid receptors. It binds primarily to the mu (μ) receptor, but also has affinity for kappa (κ) and sigma (σ) receptors.
By occupying these receptors without activating them, it displaces opioid agonists → rapid reversal of opioid-induced respiratory and CNS depression.
At very high doses, naloxone may exhibit additional pharmacologic activity, including GABA antagonism and the ability to increase dopamine levels.
安全性與警告
禁忌症
- Hypersensitivity to naloxone
- Indiscriminate use in animals that have undergone major surgery or trauma (due to severe pain from analgesia reversal)
不良反應
- Reversal of analgesia (return of pain)
- Acute withdrawal syndrome in opioid-dependent patients
- CNS excitement (especially if used in meperidine overdose)
- Seizures (at very high doses, likely secondary to GABA antagonism)
- Acute severe discomfort or pain (due to sudden loss of analgesia)
- Antanalgesic effects in opioid-naïve subjects
- Transient elevation of unconsciousness (at low doses)
注意事項
Important Warning: The duration of action of naloxone (45-90 minutes) is often shorter than the opioid it is reversing. Patients may slip back into respiratory depression and require re-dosing or continuous ventilatory support.
- Use with caution in animals with preexisting cardiac abnormalities.
- Use cautiously in opioid-dependent animals or those that have received exceedingly large doses of narcotics, as it may precipitate an acute withdrawal syndrome.
- Meperidine Toxicity: Naloxone is reportedly not effective for reversing meperidine-induced seizures and may elicit CNS excitement if normeperidine excitotoxicity is present. Avoid unless severe respiratory depression is present without ventilatory support.
- Buprenorphine: Naloxone is not a good reversal agent for buprenorphine due to buprenorphine's high receptor affinity; massive doses (100X usual) may be required.
藥物相互作用
Naloxone may antagonize the effects of these agents (respiratory depression, analgesia). It should not be relied upon to treat respiratory depression caused by buprenorphine.
Naloxone may reduce the hypotensive and bradycardic effects of clonidine; potentially useful for clonidine overdoses.
Naloxone may increase the CNS effects of yohimbine (anxiety, tremors, nausea, palpitations) and increase plasma cortisol levels.
Naloxone reverses the analgesic, sedative, and respiratory depressant effects of opioid agonists.
Buprenorphine binds tightly to opioid receptors; naloxone may not fully reverse its effects or may require much higher doses.
監測
- Respiratory rate and depth
- CNS function (level of sedation/arousal)
- Pain associated with opiate reversal
- Respiratory rate and effort
- Level of consciousness / sedation score
- Pain score (monitor for acute pain upon reversal)
- Heart rate and blood pressure
藥物動力學
半衰期
吸收
Minimally absorbed orally (rapidly destroyed in the GI tract). Very rapid onset of action when given IV (1-2 minutes). IM onset is generally within 5 minutes. Duration of action usually persists from 45-90 minutes, but may act for up to 3 hours.
分佈
Distributed rapidly throughout the body with high levels found in the brain, kidneys, spleen, skeletal muscle, lung, and heart. Readily crosses the placenta.
代謝
Metabolized in the liver, principally via glucuronidative conjugation.
排除
Metabolites are excreted into the urine.
過量
Naloxone is considered a very safe agent with a very wide margin of safety. However, massive overdoses have initiated seizures in a few patients, which is theorized to be secondary to GABA antagonism.
可用產品
劑型
- Injection: 0.4 mg/mL
- Neonatal Injection: 0.02 mg/mL
- Injectable: 0.02 mg/ml solution
- Injectable: 0.4 mg/ml solution
獸醫用
- Naloxone 0.02 mg/ml injectable solution
- Naloxone 0.4 mg/ml injectable solution
人用標示
- Naloxone HCl Injection: 0.4 mg/mL (400 micrograms/mL) in 1 mL amps, syringes and 1 mL, 2 mL, & 10 mL vials (Narcan)
- Naloxone HCl Neonatal Injection: 0.02 mg/mL in 2 mL vials
- Narcan 0.4 mg/ml injectable solution
- Narcan nasal spray
各地核准狀態
POM (Prescription Only Medicine)
POM-V
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儲存與穩定性
Store at room temperature (15-30°C) and protect from light. Sterile water for injection is the recommended diluent. When given as an IV infusion, either D5W or normal saline should be used. Do not mix with solutions containing sulfites, bisulfites, long-chain or high molecular weight anions, or any solutions at alkaline pH.
飼主須知
- 用途：納洛酮是一種急救藥物，用於逆轉鴉片類止痛藥的作用或治療鴉片類藥物過量。
- 預期反應：您的寵物可能會從鎮靜狀態中迅速醒來。因為它會抵消止痛藥的效果，寵物可能會突然感到疼痛。
- 密切觀察：納洛酮的藥效消退時間可能比鴉片類藥物快。請密切觀察寵物是否再次出現極度嗜睡、呼吸緩慢或無反應的現象。
- 給藥方式：通常由獸醫專業人員給藥，但在某些情況下（如新生幼犬/幼貓），可能會指示您將藥滴在舌下。
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠方最新藥品說明書。