氧嗎啡酮
Oxymorphone
Oxymorphone HCl
別名: Numorphan · Opana · 7,8-Dihydro-14hydroxymorphinone hydrochloride · oximorphone 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
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。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| For sedation for minor procedures | Up to 0.2 mg/kg IM or IV ; initially a maximum of 5 mg total dose | IM/IV | Once | — | 🌎 NA |
| For sedation for minor procedures | 0.05-0.1 mg/kg IV or 0.1-0.2 mg/kg IM, SC | IV/IM/SC | Once | — | 🌎 NA |
| For analgesia (acute pain) | 0.1-0.2 mg/kg IM, IV, or SC | IM/IV/SC | q1-3h | — | 🌎 NA |
| For analgesia (acute pain) in animals with cardiovascular disease | 0.05-0.1 mg/kg IV, IM or SC | IV/IM/SC | q2-4h | — | 🌎 NA |
| Epidural administration | 0.05 mg/kg | Epidural | Once | — | 🌎 NA |
| For acute pain | 0.1-0.2 mg/kg IM or SC | IM/SC | q3-4h | — | 🌎 NA |
| For analgesia | 0.05-0.4 mg/kg IV, IM, or SC | IV/IM/SC | q2-4h | — | 🌎 NA |
| For premedication to anesthesia in healthy dogs | 0.05-0.1 mg/kg IM, IV ; 0.2 mg/kg for extra heavy sedation | IM/IV | Once | — | 🌎 NA |
- For sedation for minor procedures: Combine with acepromazine 0.05-0.1 mg/kg IM or IV
- Epidural administration: Recommend to dilute with sterile saline to a volume not to exceed 0.3 mL/kg to a maximum of 6 mL. Use of preservative-free opioids is best.
- For premedication to anesthesia in healthy dogs: Maximum initial dose: 5 mg.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| As a preanesthetic/analgesic | 0.05-0.1 mg/kg IM | IM | Once | — | 🌎 NA |
| As an analgesic (acute pain) | 0.05-0.1 mg/kg IM, SC or IV | IM/SC/IV | q1-3h | — | 🌎 NA |
| As an analgesic (acute pain) for animals with cardiovascular disease | 0.05-0.1 mg/kg IV, IM or SC | IV/IM/SC | q2-4h | — | 🌎 NA |
| As an analgesic (acute pain) | 0.025-0.1 mg/kg IV (IM or SC) | IV/IM/SC | q2-6h | — | 🌎 NA |
| As an analgesic (acute pain) | 0.02-0.1 mg/kg IV, IM, or SC | IV/IM/SC | q3-4h | — | 🌎 NA |
- As a preanesthetic/analgesic: may cause dysphoria or excitement, add sedative.
- As an analgesic (acute pain): concomitant tranquilization recommended
小型哺乳類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Analgesia | 0.2 mg/kg IM | IM | q2-4h | — | 🌎 NA |
| Anesthetic/analgesic for minor surgical procedures | 0.15 mg/kg IM | IM | Once | — | 🌎 NA |
| Analgesia | 0.2-0.5 mg/kg SC, IM | SC/IM | q6-12h | — | 🌎 NA |
| Analgesia | 0.05-0.2 mg/kg SQ (or IM for rabbits only) | SQ/IM | q8-12 hrs | — | 🌎 NA |
- Analgesia: Rabbits
- Anesthetic/analgesic for minor surgical procedures: for a hamster-sized animal
- Analgesia: Hamsters, Gerbils, Mice, Rats, Guinea pigs
- Analgesia: Rabbits, Rats, Mice, Gerbils, Guinea Pigs, Hamsters, Chinchillas
雪貂
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Analgesia | 0.05-0.2 mg/kg IV or IM | IV/IM | 2-4 times daily | — | 🌎 NA |
| Analgesia | 0.05-0.2 mg/kg SQ or IM | SQ/IM | q8-12 hrs | — | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| As an analgesic | 0.01-0.02 mg/kg IV | IV | Once | — | 🌎 NA |
| As an analgesic | 0.01-0.022 mg/kg IV ; up to 15 mg total | IV | Once | — | 🌎 NA |
| As an analgesic | 0.02-0.03 mg/kg IM | IM | Once | — | 🌎 NA |
| As an analgesic | 0.015-0.03 mg/kg IV | IV | Once | — | 🌎 NA |
| Anesthetic induction in severely compromised horses | 0.01-0.022 mg/kg IV | IV | Once | — | 🌎 NA |
- As an analgesic: divide dose into 3-4 increments and give several minutes apart
- Anesthetic induction in severely compromised horses: after approx. 45 minutes, may be necessary to 'top off' with another 1/3 of the original dose
豬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| To increase analgesia when used with ketamine/xylazine | 0.075 mg/kg IV | IV | Once | — | 🌎 NA |
- To increase analgesia when used with ketamine/xylazine: duration of anesthesia and recumbency: 20-30 minutes
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
氧嗎啡酮是一種強效的半合成鴉片類促效劑,在獸醫學中主要用作鎮靜/保定劑、鎮痛劑和麻醉前給藥。
- 效力: 按重量計算,其效力約為嗎啡的10倍。
- 心血管作用: 對心血管系統的影響通常無臨床顯著性,使其成為心血管疾病患者相對安全的選擇。
- 組織胺釋放: 與嗎啡或配西汀不同,靜脈注射氧嗎啡酮似乎不會引起顯著的組織胺釋放。
- 臨床要點: 由於具有高度濫用潛力,它屬於第二級(C-II)管制藥品。雖然對中度至重度疼痛非常有效,但在獸醫臨床上,取得難易度及費用有時會成為限制因素。
作用機制
Oxymorphone acts primarily as a full agonist at mu (μ) opioid receptors, with some possible activity at delta (δ) receptors.
- Pathway: Binds to G-protein coupled mu-opioid receptors in the CNS (limbic system, spinal cord, thalamus, midbrain) and peripheral tissues (GI tract, urinary tract) → inhibits adenylate cyclase → decreases intracellular cAMP → promotes opening of potassium channels and inhibits voltage-gated calcium channels → hyperpolarizes nociceptive neurons and inhibits the release of pain neurotransmitters (e.g., Substance P).
- Effects: This results in profound analgesia, sedation, respiratory depression, and altered GI motility.
安全性與警告
禁忌症
- Hypersensitivity to narcotic analgesics
- Patients receiving monoamine oxidase inhibitors (MAOIs)
- Diarrhea caused by a toxic ingestion (until toxin is eliminated)
- Scorpion stings (Centruroides sculpturatus and C. gertschi)
不良反應
- Respiratory depression
- Bradycardia
- Decreased GI motility (constipation)
- Panting (commonly seen in dogs)
- Ataxia, hyperesthesia, and behavioral changes (cats at high dosages)
- CNS excitement (horses)
注意事項
Extreme Caution: Use with extreme caution in patients with head injuries, increased intracranial pressure, acute abdominal conditions (e.g., colic, as it may obscure diagnosis), respiratory disease, or acute respiratory dysfunction.
- Caution: Use cautiously in patients with hypothyroidism, severe renal insufficiency, adrenocortical insufficiency, preexisting bradyarrhythmias, and in geriatric or severely debilitated patients.
- Species Specifics: In cats, high dosages can produce bizarre behavioral changes; concomitant use of a tranquilizer is recommended. In horses, opiates can mask behavioral and cardiovascular signs of mild colic.
藥物相互作用
Potentially could antagonize opiate effects
Additive CNS effects possible
Opiates may decrease efficacy in CHF patients
Extreme caution; may cause signs of opiate overdose
Oxymorphone may enhance effects
May antagonize analgesic effects and increase risk for hypotension
Oxymorphone may exacerbate the effects of tricyclic antidepressants
Opiates may potentiate anticoagulant activity
監測
- Respiratory rate/depth
- CNS level of depression/excitation
- Blood pressure (especially with IV use)
- Analgesic activity
- Cardiac rate
藥物動力學
半衰期
吸收
Absorbed when given by IV, IM, SC, and rectal routes. Oral bioavailability is reduced due to a high first-pass effect. Analgesic efficacy usually occurs within 3-5 minutes after IV administration, and about 15 minutes after IM administration.
分佈
Concentrates in the kidney, liver, and lungs; lower levels are found in the CNS. Crosses the placenta and is distributed into maternal milk.
代謝
Metabolized in the liver primarily by glucuronidation. Cats are deficient in this metabolic pathway, leading to prolonged half-lives.
排除
The kidneys excrete the glucuronidated metabolite.
過量
Massive overdoses may produce profound respiratory and/or CNS depression in most species. Other effects may include cardiovascular collapse, hypothermia, and skeletal muscle hypotonia.
- Antidote: Naloxone is the agent of choice in treating respiratory depression.
- Management: In massive overdoses, naloxone doses may need to be repeated. Animals should be closely observed as naloxone's effects sometimes diminish before sub-toxic levels of oxymorphone are attained. Mechanical respiratory support should be considered in cases of severe respiratory depression.
可用產品
劑型
- Injection
- Extended-Release Oral Tablets
- Suppositories
人用標示
- Oxymorphone HCl Oral Tablets: 5 mg & 10 mg; Opana®
- Oxymorphone HCl Extended-Release Oral Tablets: 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg, 30 mg & 40 mg; Opana® ER
- Oxymorphone HCl for Injection: 1 mg/mL in 1 mL amps; Opana®
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
The injection should be stored protected from light and at room temperature (15-30°C); avoid freezing. Commercially available suppositories should be stored at temperatures between 2-15°C.
飼主須知
- 注射給藥時,應在住院環境或專業人員直接監督下使用。
- 安全警告: 這是一種強效鴉片類藥物及管制藥品。如果配發供居家使用,請務必將其放置在兒童和其他寵物絕對接觸不到的地方。
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。
