哌替啶
Meperidine
Meperidine hydrochloride
別名: Demerol · Alodan · Centralgine · Dolantina · Dolantine · Dolestine · Dolosal · Pethidine HCl · Isonipecaine · Meperidine hydrochloride · Pethidini hydrochloridum · Pethidinum
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
結構化劑量計算證據Analgesic (extra-label)
須由已驗證獸醫確認
- q2-3h
NA
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
哌替啶(又稱 pethidine)是一種合成的鴉片類促效劑,主要用於鎮痛。
臨床要點:
- 雖然過去很受歡迎,但由於其作用時間極短(在犬貓體內小於 1-2 小時),且極易引起組織胺釋放和低血壓(特別是靜脈注射時),其在現代獸醫學中的使用已大幅減少。
- 與大多數其他鴉片類藥物不同,哌替啶具有抗膽鹼(迷走神經抑制)和負性肌力作用,這可能導致心跳過速,而非純 mu 促效劑常見的心跳過緩。
- 其效力約為嗎啡的 1/3 至 1/8,但在等效鎮痛劑量下會產生同等程度的呼吸抑制。
- 本品為第二級管制藥品(C-II)。
作用機轉
Meperidine acts primarily as an agonist at the mu (μ) opioid receptors in the central nervous system (CNS) and peripheral tissues.
- Receptor Binding: Binds to G-protein coupled mu receptors → inhibits adenylate cyclase → decreases intracellular cAMP.
- Ion Channel Modulation: Promotes opening of potassium channels (causing hyperpolarization) and inhibits voltage-gated calcium channels (decreasing neurotransmitter release).
- Analgesia: Inhibits ascending nociceptive pathways and alters the perception of pain.
- Unique Mechanisms: Exhibits anticholinergic (vagolytic) effects and can cause direct mast cell degranulation leading to histamine release.
安全性與警告
禁忌症
- Hypersensitivity to narcotic analgesics
- Patients receiving monamine oxidase inhibitors (MAOIs)
- Diarrhea caused by a toxic ingestion (until toxin is eliminated)
- Envenomations from Centruroides scorpion species, Gila monsters, or Mexican beaded lizards
- Intravenous (IV) administration
- Animals at risk from histamine release (e.g., skin allergies, asthma, mast cell tumours)
不良反應
- Respiratory depression
- Histamine release
- Bronchoconstriction (dogs)
- CNS depression
- Nausea and vomiting
- Decreased intestinal peristalsis
- Mydriasis (dogs)
- Salivation (especially cats)
- Physical dependence (chronic use)
- Tachycardia with PVCs (horses)
- Profuse sweating (horses)
- Hyperpnea (horses)
- Severe hypotension (if given IV rapidly)
- Hypotension (especially if given IV)
- Local urticaria (after IM injection)
- Dry mouth
- Pain on IM injection (due to volume)
- Neonatal sedation (if given to bitches prior to parturition)
注意事項
Important Administration Note: Many clinicians state meperidine should NOT be administered intravenously. If given IV, it must be given very slowly to avoid severe hypotension and histamine release. It may also be irritating when given SC.
- Extreme Caution: Patients with respiratory disease or acute respiratory dysfunction (e.g., pulmonary edema secondary to smoke inhalation).
- Caution: Hypothyroidism, severe renal insufficiency, adrenocortical insufficiency (Addison's disease), geriatric or severely debilitated patients.
- Caution: Head injuries or increased intracranial pressure, and acute abdominal conditions (e.g., colic) as it may obscure diagnosis.
- Equine Note: May potentiate intestinal obstruction secondary to reduced intestinal motility.
藥物交互作用
May cause increased CNS or respiratory depression when used with meperidine.
Opiates may decrease efficacy in CHF patients.
Meperidine may enhance INH adverse effects.
Contraindicated. Can cause severe opiate overdose signs; avoid meperidine for at least 14 days after receiving MAOIs.
Meperidine may enhance neuromuscular blockade.
Meperidine may exacerbate the effects of tricyclic antidepressants.
Opiates may potentiate anticoagulant activity.
Increased CNS or respiratory depression
Serious interaction resulting in coma, convulsions, and hyperpyrexia
監測
- Respiratory rate and depth
- CNS level of depression or excitation
- Blood pressure (especially with IV use)
- Analgesic activity
- Pain score
- Heart rate
- Signs of histamine release (urticaria, bronchoconstriction)
藥物動力學
半衰期
吸收
Generally well absorbed orally, but a marked first-pass effect limits oral effectiveness. Peak analgesic effects occur between 30-60 minutes after IM or SC injection, with IM having a slightly faster onset.
分佈
Widely distributed. Enters human breast milk at concentrations slightly higher than serum.
代謝
Metabolized primarily in the liver (mostly hydrolysis with some conjugation).
排除
Approximately 5% is excreted unchanged in the urine.
過量
Overdosage may produce profound respiratory and/or CNS depression. Other effects can include cardiovascular collapse, hypothermia, and skeletal muscle hypotonia.
- Species Differences: Some species (especially cats) may demonstrate CNS excitability (hyperreflexia, tremors) and seizures at doses >20 mg/kg.
- Treatment: Naloxone is the agent of choice for respiratory depression. In massive overdoses, naloxone doses may need to be repeated, as its effects can diminish before subtoxic levels of meperidine are attained. Mechanical respiratory support should be considered. Pentobarbital has been suggested for CNS excitement/seizures in cats, but extreme caution is required as barbiturates and narcotics have additive respiratory depressant effects.
可用產品
劑型
- Injection
- Tablets
- Syrup/Oral Solution
- Injectable: 10-50 mg/ml solutions (50 mg/ml is most commonly used in veterinary practice)
獸醫用
- Pethidine 50 mg/ml injection
人用標示
- Meperidine HCl Injection: 25 mg/mL, 50 mg/mL, 75 mg/mL, 100 mg/mL
- Meperidine HCl Tablets: 50 mg, 100 mg
- Meperidine HCl Syrup/Oral Solution: 50 mg/5 mL
- Demerol
- Meperidine injection
各地核准狀態
POM (Prescription Only Medicine)
POM-V CD SCHEDULE 2
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Stable at room temperature. Avoid freezing the injectable solution and protect from light during storage. Does not exhibit significant adsorption to PVC IV bags or tubing.
飼主須知
重要提示: 哌替啶是一種強效的處方止痛藥(鴉片類藥物),通常僅在醫院環境中由獸醫直接監督下使用。
- 短效性: 這種藥物在寵物體內的藥效消退非常快(通常不到一小時),因此通常在手術過程中作為注射劑給予,而不是讓寵物帶回家服用。
- 副作用: 可能會引起嗜睡、噁心或流口水。如果口服給藥,藥水或藥片可能會刺激口腔,特別是在貓咪身上。
- 安全性: 絕對不要在沒有獸醫嚴格指導的情況下給您的寵物服用人類止痛藥或剩餘的哌替啶,因為過量會導致危及生命的呼吸問題。
VetSheet 藥物參考供合格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商最新仿單。
