阿塞丙嗪
Acepromazine
Acepromazine maleate
別名: PromAce · Aceproject · Aceprotabs · Plegicil · Notensil · Atravet · Acecare · ACP · Acetylpromazine maleate
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 (1)
只供證據參考，不會自動計算
Tranquilization
a) Tranquilization: 0.25 – 0.75 mg/kg IM or SC 46 ; the lower to mid-range of the dosage is generally adequate.
必須同時考慮的臨床上下文 (4)
- 1. Acepromazine does not provide analgesia; addition of an analgesic agent is required when pain relief is needed.
- All dosages are extra-label.
- Store tablets and injection protected from light at 20°C to 25°C (68°F-77°F), with excursions permitted between 15°C and 30°C (59°F-86°F). Tablets should be stored in tight containers. There is no limit to the number of vial punctures throughout the full expiry period. 1
- 2. Administer IV doses slowly; allow at least 15 minutes for onset of action. 1
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
阿塞丙嗪 (Acepromazine) 是獸醫學中經典且廣泛使用的吩噻嗪類神經阻滯劑，主要用於其可靠的鎮靜與安神作用。
關鍵臨床要點：
- 無鎮痛作用： 阿塞丙嗪完全沒有止痛效果。對於疼痛性操作，必須結合適當的鎮痛藥（如鴉片類藥物）使用（神經安定鎮痛）。
- 心血管效應： 由於具有 α-1 腎上腺素受體阻斷作用，它是一種強效的血管擴張劑，常引起低血壓。應避免用於低血容、休克或血流動力學不穩定的病患。
- 品種敏感性： 巨型犬和視覺獵犬（如格雷伊獵犬）對此藥高度敏感。帶有 MDR1 (ABCB1) 基因突變的犬隻（如牧羊犬、澳洲牧羊犬）需要大幅降低劑量（25-50%）。
- 馬匹注意事項： 可能導致公馬陰莖長時間突出或陰莖異常勃起，進而造成陰莖牽引肌永久性麻痺。
雖然過去常用於旅行焦慮或噪音恐懼症，但現代獸醫行為學家通常不建議將其作為這些情況的單一療法，因為它可能僅讓動物鎮靜而無法減輕潛在的恐懼或恐慌，甚至可能增加對噪音的敏感度。
作用機制
Acepromazine exerts its effects through multiple receptor antagonisms:
- Dopamine (D2) Receptor Antagonism: Blocks postsynaptic D2 receptors in the CNS (specifically the basal ganglia and limbic system) → depresses the reticular activating system → produces sedation and tranquilization.
- Alpha-1 Adrenergic Antagonism: Blocks peripheral alpha-1 receptors → causes peripheral vasodilation → leads to hypotension and secondary hypothermia.
- Additional Blockade: Possesses varying degrees of anticholinergic (muscarinic), antihistaminic (H1), and antispasmodic effects.
- Antiemetic Effect: Blocks dopamine receptors in the Chemoreceptor Trigger Zone (CRTZ) of the medulla.
Clinical Pearl: Because of its alpha-blocking properties, administering epinephrine to an acepromazine-induced hypotensive patient can cause "epinephrine reversal" (unopposed beta-2 vasodilation), worsening the hypotension. Alpha-agonists like phenylephrine are preferred for treating severe acepromazine-induced hypotension.
安全性與警告
禁忌症
- Significant cardiac disease
- Hypovolemia, hypotension, or shock
- Tetanus or strychnine intoxication
- Intra-arterial injection in horses (can cause severe CNS excitement, seizures, death)
- Use with extreme caution in very young, geriatric, or debilitated animals
- Avoid in racing animals within 4 days of a race
不良反應
- Hypotension and cardiovascular collapse
- Bradycardia (vagally mediated) or reflex tachycardia
- Hypothermia or hyperthermia
- Penile protrusion/prolapse in large animals (especially stallions)
- Prolapse of the membrana nictitans (third eyelid)
- Decreased tear production (especially in cats)
- Paradoxical excitement, restlessness, or aggression
- Transient pain at IM injection sites
- Decreased hematocrit (due to splenic sequestration of RBCs)
注意事項
Dosage Adjustments: The manufacturer's labeled dose is often considered up to 10 times higher than clinically necessary. Use lower end of dose ranges.
Breed Sensitivities:
- MDR1 Mutation: Dogs with the MDR1 (ABCB1) mutation (Collies, Australian Shepherds, etc.) require a 25% dose reduction if heterozygous, and a 30-50% reduction if homozygous.
- Giant Breeds & Sight Hounds: Extremely sensitive; require lower doses.
- Terriers: May be somewhat resistant to effects.
Administration: Give IV injections slowly. Allow at least 15 minutes for onset of action. Never inject intra-arterially in horses.
Behavioral: Use cautiously as a restraining agent in aggressive dogs; it may make the animal more prone to startle and react to noises.
Other: May cause regurgitation of ruminal contents in cattle during general anesthesia induction.
藥物相互作用
Possible increased risk for hypothermia
May cause reduced GI absorption of oral phenothiazines
May cause reduced GI absorption of oral phenothiazines
May cause additive CNS depression if used with acepromazine
Acepromazine may impair the vasopressive action of dopamine
Acepromazine may reduce the effectiveness of emetics
Concomitant use can lead to unopposed beta-activity causing vasodilation and increased cardiac rate (epinephrine reversal)
May increase risks for extrapyramidal adverse effects
May enhance hypotensive effects; dosages of acepromazine are generally reduced when used with an opiate
Effects may be potentiated; do not give within one month of worming with these agents
Metabolism may be decreased if given concurrently
Activity may be enhanced by phenothiazines
Increased blood levels of both drugs may result
May cause additive cardiac depression
Additive CNS depression; doses of other anaesthetic drugs should be reduced when ACP is used for premedication
Unopposed beta activity causing severe vasodilation and tachycardia (due to ACP's alpha-adrenergic blockade)
Reduced GI absorption of oral phenothiazines
監測
- Cardiac rate, rhythm, and blood pressure (especially in compromised patients)
- Degree of tranquilization and sedation
- Male horses: Monitor to ensure the penis retracts and is not injured
- Body temperature (especially if ambient temperature is very hot or cold)
藥物動力學
半衰期
吸收
Onset of action is fairly slow, requiring up to 15 minutes following IV administration, with peak effects seen in 30-60 minutes.
分佈
Fairly high volume of distribution (6.6 L/kg in horses), and is more than 99% protein bound.
代謝
Metabolized in the liver.
排除
Both conjugated and unconjugated metabolites are eliminated in the urine. Metabolites may be found in equine urine up to 96 hours after dosing.
過量
The LD50 in mice is 61 mg/kg IV and 257 mg/kg PO. Dogs have survived oral dosages up to 220 mg/kg, but overdoses can cause serious hypotension, CNS depression, pulmonary edema, and hyperemia.
Clinical Signs of Toxicity:
- Dogs: Ataxia, sedation, lethargy, depression, protrusion of the third eyelid, somnolence, bradycardia, and recumbency.
- Cats: Sedation, ataxia, lethargy, protrusion of the third eyelid, and depression.
Treatment:
- Because of relatively low toxicity, most overdoses are handled by monitoring and symptomatic treatment.
- Massive oral overdoses should be treated by emptying the gut if possible.
- Hypotension: Should not be treated initially with fluids. If fluids fail to maintain BP, use alpha-adrenergic pressor agents (e.g., phenylephrine). Note: Avoid epinephrine due to the risk of "epinephrine reversal" causing further vasodilation.
- Seizures: May be controlled with barbiturates or diazepam.
- CNS Depression: Doxapram has been suggested as an antagonist to the CNS depressant effects.
可用產品
劑型
- Injection: 10 mg/mL
- Tablets: 5 mg, 10 mg, 25 mg
獸醫用
- Acepromazine Maleate for Injection: 10 mg/mL in 50 mL vials (PromAce, generic)
- Acepromazine Maleate Tablets: 5 mg, 10 mg & 25 mg (PromAce, generic)
各地核准狀態
Classified as POM-V (Prescription Only Medicine - Veterinarian)
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儲存與穩定性
Store protected from light. Tablets should be stored in tight containers. Acepromazine injection should be kept from freezing. Stable and efficacious for at least 180 days after mixing with ketamine and xylazine if stored at room temperature in the dark.
飼主須知
- 尿液變色： 此藥物可能會使您寵物的尿液暫時變成粉紅色或紅棕色；這是正常的副作用，無需驚慌。
- 非止痛藥： 阿塞丙嗪能提供鎮靜效果，但不能止痛。如果您的寵物正在接受會引起疼痛的處置，將需要其他藥物。
- 保持環境安靜： 即使您的寵物看起來很睏，牠們仍可能被巨大的噪音或突然的動作嚇到，並可能做出不可預測的反應。在藥效消退期間，請讓牠們待在安靜、平靜的環境中。
- 第三眼瞼： 您可能會注意到寵物的「第三眼瞼」（眼內角的薄膜）覆蓋了部分眼睛。這是正常現象，會隨著藥效消退而恢復。
- 法規： FDA 批准用於非食用目的之犬、貓和馬匹。
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