普氯哌嗪
普氯哌嗪(Prochlorperazine)是一種強效的**吩噻嗪類止吐藥**,在獸醫學中主要用於控制犬貓嚴重的噁心和嘔吐。 歷史上,它曾廣泛用於獸醫專用的複方產品(如含有抗膽鹼藥物的 Darbazine®),但目前多以仿單標示外使用(off-label use)人類藥物劑型。 **臨床要點:** 由於其廣泛的受體拮抗作用,普氯哌嗪對中樞性嘔吐非常有效。然而,由於它可能引起顯著的鎮靜作用和α-腎上腺素受體阻斷(導致低血壓),通常保留用於較新的標靶止吐藥(如 maropitant 或 ondansetron)無效或無法取得的病例。它還具有輕度的鎮靜和微弱的抗膽鹼特性。
作用機制: Prochlorperazine exerts its antiemetic effects primarily by acting on the brain's emetic center and the **Chemoreceptor Trigger Zone (CRTZ)**. Its broad-spectrum efficacy is due to the antagonism of multiple receptor types: * **Dopaminergic (D2) Antagonism** → Blocks dopamine signaling in the CRTZ, providing the primary antiemetic effect. * **Histaminergic (H1) & Cholinergic (M1) Antagonism** → Contributes to anti-motion sickness efficacy and mild antispasmodic effects in the GI tract. * **Alpha-1 Adrenergic Antagonism** → Causes peripheral vasodilation, which is responsible for the primary adverse effect of hypotension. It also has strong extrapyramidal effects due to central dopamine blockade in the basal ganglia.
各物種劑量
- As an antiemetic · 0.5 mg/kg · SC or IM · three times a day · Ensure adequate hydration
- As an antiemetic · 0.5 mg/kg · IM or SC · q8h
- As an antiemetic · 0.1-0.5 mg/kg · IM or SC · q6-8h
- All uses (motion sickness, emesis) · 0.1-0.5 mg/kg · IV/IM/SC · q6-8h
- All uses (motion sickness, emesis) · 0.5-1 mg/kg · PO · q8-12h
- As an antiemetic · 0.5 mg/kg · IM or SC · q8h · Ensure adequate hydration
- As an antiemetic · 0.1 mg/kg · IM · q6-8h · Use with extreme caution in dehydrated or hypotensive animals
- As an antiemetic · 0.1-0.5 mg/kg · IM or SC · q6-8h
- All uses (motion sickness, emesis) · 0.1-0.5 mg/kg · IV/IM/SC · q6-8h
- All uses (motion sickness, emesis) · 0.5-1 mg/kg · PO · q8-12h
劑量為合格獸醫專業人員的臨床參考。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
禁忌症
- Hypovolemia or dehydration
- Shock
- Tetanus
- Strychnine intoxication
- Hepatic dysfunction (use with caution)
- Cardiac disease (use with caution)
不良反應
- Sedation
- Hypotension
- Muscle fasciculations and tremors (extrapyramidal signs)
- Prolactin release
- Depression
- Extrapyramidal reactions (rigidity, tremors, weakness, restlessness)
藥物相互作用
- Antacids · May cause reduced GI absorption of oral phenothiazines · moderate
- Antidiarrheal mixtures (e.g., Kaolin/pectin, bismuth subsalicylate) · May cause reduced GI absorption of oral phenothiazines
- CNS Depressant Agents (barbiturates, narcotics, anesthetics) · May cause additive CNS depression if used with phenothiazines
- Dopamine · Phenothiazines may decrease pressor effects
- Epinephrine · Phenothiazines block alpha-adrenergic receptors; concomitant epinephrine can lead to unopposed beta-activity causing vasodilation and increased cardiac rate (epinephrine reversal)
- Metoclopramide · Phenothiazines may potentiate the extrapyramidal effects of metoclopramide
- Opiates · May enhance the hypotensive effects of the phenothiazines; dosages of prochlorperazine may need to be reduced
- Organophosphate Agents · Phenothiazines should not be given within one month of worming with these agents as their effects may be potentiated
- Paraquat · Toxicity of the herbicide paraquat may be increased by prochlorperazine
- Phenytoin · Metabolism may be decreased if given concurrently with phenothiazines
- Physostigmine · Toxicity may be enhanced by prochlorperazine
- Procaine · Activity may be enhanced by phenothiazines
監測
- Cardiac rate, rhythm, and blood pressure (if indicated and possible to measure)
- Anti-emetic/anti-spasmodic efficacy
- Hydration and electrolyte status
- Body temperature (especially if ambient temperature is very hot or cold)
- Heart rate and rhythm
- Blood pressure
- CNS status (sedation level, extrapyramidal signs)
- Liver function (with prolonged use)
過量
Overdose generally presents as an exaggeration of adverse effects, particularly profound sedation, hypotension, and **extrapyramidal clinical signs** (such as torticollis, severe tremors, muscle rigidity, and excessive salivation). > **Treatment:** Acute extrapyramidal signs have been successfully treated with injectable **diphenhydramine** in humans. Hypotension should be treated with intravenous fluids; avoid epinephrine due to the risk of "epinephrine reversal" causing further vasodilation.
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