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**μμΈνλ‘λ§μ§(Acepromazine)**μ μμνμμ κ³ μ μ μ΄κ³ λ리 μ¬μ©λλ νλ Έν°μμ§κ³ μ κ²½μ΄μμ λ‘, μ£Όλ‘ μ λ’°ν μ μλ μ§μ λ° μ κ²½μμ ν¨κ³Όλ₯Ό μν΄ μ¬μ©λ©λλ€. **μ£Όμ μμ ν¬μΈνΈ:** * **μ§ν΅ ν¨κ³Ό μμ:** μμΈνλ‘λ§μ§μ **μ§ν΅ ν¨κ³Όκ° μ ν μμ΅λλ€**. ν΅μ¦μ΄ λλ°λλ μμ μ λ°λμ μ μ ν μ§ν΅μ (μ: λ§μ½μ± μ§ν΅μ )μ λ³μ©ν΄μΌ ν©λλ€(μ κ²½μ΄μμ§ν΅). * **μ¬νκ΄κ³ μν₯:** μν-1 μλλ λ λ¦° μμ©μ²΄ μ°¨λ¨ μμ©μΌλ‘ μΈν κ°λ ₯ν νκ΄ νμ₯μ λ‘, νν **μ νμ**μ μ λ°ν©λλ€. μ νλμ¦, μΌν¬ λλ νμνμ μΌλ‘ λΆμμ ν νμμκ²λ μ¬μ©μ νΌν΄μΌ ν©λλ€. * **νμ’ λ―Όκ°μ±:** μ΄λν견 λ° μκ°νμ΄λ(μ: κ·Έλ μ΄νμ΄λ)λ λ§€μ° λ―Όκ°ν©λλ€. **MDR1(ABCB1) μ μ μ λμ°λ³μ΄**κ° μλ κ°(μ: μ½λ¦¬, μ€μ€νΈλ μΌλ¦¬μ μ °νΌλ)λ μ©λμ ν¬κ² μ€μ¬μΌ ν©λλ€(25-50%). * **λ§μ λν μ£Όμμ¬ν:** μλ§μμ μ§μμ μΈ μκ²½ λμΆμ΄λ μ§μλ°κΈ°μ¦μ μ λ°ν μ μμΌλ©°, μ΄λ μ경견μΈκ·Όμ μꡬμ μΈ λ§λΉλ‘ μ΄μ΄μ§ μ μμ΅λλ€. κ³Όκ±°μλ μ¬ν λΆμμ΄λ μμ 곡ν¬μ¦μ μμ£Ό μ¬μ©λμμΌλ, νλ μμ νλνμλ€μ κ·Όλ³Έμ μΈ λλ €μμ΄λ 곡ν¬λ₯Ό μ€μ΄μ§ λͺ»ν μ± λλ¬Όλ§ μ§μ μμΌ μ€νλ € μμ λ―Όκ°μ±μ μ¦κ°μν¬ μ μμΌλ―λ‘ μ΄λ¬ν μνμ λν λ¨λ μλ²μΌλ‘ μ¬μ©νλ κ²μ κΆμ₯νμ§ μμ΅λλ€.
μμ© κΈ°μ : 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) β depresses the reticular activating system β produces **sedation and tranquilization**. * **Alpha-1 Adrenergic Antagonism:** Blocks peripheral alpha-1 receptors β causes peripheral vasodilation β 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.
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- Sedation Β· 0.05-0.1 mg/kg IM Β· IM
- Sedation Β· 0.05-0.1 mg/kg IM Β· IM
- Labeled dose Β· 0.55-2.2 mg/kg PO or 0.55-1.1 mg/kg IV, IM or SC Β· PO, IV, IM, SC Β· Considered by many clinicians to be 10 times greater than necessary.
- Restraint/sedation Β· 0.025-0.2 mg/kg IV; maximum of 3 mg or 0.1-0.25 mg/kg IM Β· IV, IM
- Preanesthetic Β· 0.1-0.2 mg/kg IV or IM; maximum of 3 mg; 0.05-1 mg/kg IV, IM or SC Β· IV, IM, SC
- To reduce anxiety in the painful patient (not a substitute for analgesia) Β· 0.05 mg/kg IM, IV or SC; do not exceed 1 mg total dose Β· IM, IV, SC
- Premedication Β· 0.03-0.05 mg/kg IM or 1-3 mg/kg PO Β· IM, PO Β· Give at least one hour prior to surgery (PO not as reliable).
- As a premedicant with morphine Β· acepromazine 0.05 mg/kg IM; morphine 0.5 mg/kg IM Β· IM
- Sedation and premedication (Non-Boxers) Β· 0.01-0.02 mg/kg Β· IV Β· single dose Β· up to 6 hours Β· Administer slowly. Generally given as part of a combination with opioids.
- Sedation and premedication (Non-Boxers) Β· 0.01-0.05 mg/kg Β· IM/SC Β· single dose Β· up to 6 hours Β· Onset of sedation is 20-30 minutes after IM administration.
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κΈκΈ°
- 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
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- 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)
μ½λ¬Ό μνΈμμ©
- Acetaminophen Β· Possible increased risk for hypothermia
- Antacids Β· May cause reduced GI absorption of oral phenothiazines
- Antidiarrheal mixtures (Kaolin/pectin, bismuth) Β· May cause reduced GI absorption of oral phenothiazines
- CNS Depressant Agents (barbiturates, narcotics, anesthetics) Β· May cause additive CNS depression if used with acepromazine
- Dopamine Β· Acepromazine may impair the vasopressive action of dopamine
- Emetics Β· Acepromazine may reduce the effectiveness of emetics
- Epinephrine, Ephedrine Β· Concomitant use can lead to unopposed beta-activity causing vasodilation and increased cardiac rate (epinephrine reversal)
- Metoclopramide Β· May increase risks for extrapyramidal adverse effects
- Opiates Β· May enhance hypotensive effects; dosages of acepromazine are generally reduced when used with an opiate
- Organophosphate Agents Β· Effects may be potentiated; do not give within one month of worming with these agents
- Phenytoin Β· Metabolism may be decreased if given concurrently
- Procaine Β· Activity may be enhanced by phenothiazines
λͺ¨λν°λ§
- 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)
κ³Όμ©λ
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.
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