米索前列醇
Misoprostol
Synthetic prostaglandin E1 analog
別名: Cytotec · Arthotec · Arthrotec · Artotec · Artrenac Pro · Condrotec · Corrigast · Cyprostol · Cytolog · Diclotec · Glefos · Menpros · Misodex · Misofenac · Napratec · Normulen · Oxaprost · Symbol · SC-29333 · Misoprostolum
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Prevention of aspirin-induced gastric injury (extra-label)
- q8-12h
NA
必須一併考量的臨床脈絡 (4)
- ■ Give this medicine with food if stomach upset occurs or to prevent stomach upset.
- ■ Common side effects include diarrhea, abdominal/stomach pain, vomiting, and flatulence (ie, gas). These effects may only last a few days, and giving the drug with food may help, but if any of these effects are severe, get worse, or continue to be a problem, contact your veterinarian.
- ■ This medicine is considered to be a hazardous drug because it may affect the reproductive ability of males or females actively trying to conceive, women who are pregnant or may become pregnant, as it can cause miscarriage, and women who are breastfeeding. It is recommended that you wear gloves when administering this medicine to your animal and wash your hands thoroughly afterwards. If you have questions about this medicine’s hazards, please speak with your veterinarian or pharmacist.
- Misoprostol tablets should be stored in well-closed containers at room temperature of 25°C (77°F) or less.
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
米索前列醇（Misoprostol）是一種合成的前列腺素E1（PGE1）類似物，在獸醫學中主要用於預防和治療因使用非類固醇抗發炎藥（NSAIDs）引起的胃潰瘍。
NSAIDs會抑制環氧化酶（COX），導致胃黏膜中具保護作用的前列腺素減少；米索前列醇能有效補充這些流失的前列腺素，從而恢復黏膜防禦機制。
除了胃腸道的應用外，米索前列醇還具有強烈的子宮收縮特性。它能增加子宮收縮力並促進子宮頸鬆弛，使其成為生殖系統適應症（如終止妊娠、治療子宮蓄膿/子宮炎以及交配後處置）的重要輔助療法。
臨床要點： 雖然它曾被研究用於異位性皮膚炎和環孢素引起的腎毒性，但由於療效有限且胃腸道副作用普遍，通常不作為這些疾病的首選藥物。
作用機轉
Misoprostol exerts its effects through multiple prostaglandin (EP) receptors across different organ systems:
- Gastric Acid Suppression: Binds directly to EP3 receptors on gastric parietal cells → inhibits adenylate cyclase → decreases intracellular cAMP → reduces the activity of the apical H+/K+ ATPase proton pump → decreased basal and stimulated gastric acid secretion.
- Gastric Cytoprotection: Binds to EP receptors on superficial foveolar epithelial cells → stimulates the secretion of protective mucin and bicarbonate. It also increases mucosal blood flow and accelerates epithelial cell turnover, enhancing the overall mucosal barrier and healing capacity.
- Reproductive Tract: Binds to EP receptors in the myometrium → increases intracellular calcium concentrations → increases the amplitude and frequency of uterine contractions. It also induces collagen breakdown in the cervix, leading to cervical softening and dilation.
安全性與警告
禁忌症
- Pregnancy (unless being used specifically as an abortifacient)
- Nursing mothers (can cause severe diarrhea in nursing offspring)
- Known sensitivity to prostaglandins or prostaglandin analogs
- Pregnant animals (unless being used specifically to induce abortion)
不良反應
- Diarrhea
- Abdominal pain
- Vomiting
- Flatulence
- Uterine contractions (in females)
- Vaginal bleeding (in females)
- Diarrhoea
- Nausea
- Abortion
注意事項
WARNING FOR PREGNANT WOMEN: Misoprostol is a potent abortifacient. Pregnant women or women who may become pregnant should handle this drug with extreme caution (e.g., wearing gloves or avoiding handling altogether).
- Use with caution in patients with cerebral or coronary vascular disease. While not explicitly reported with misoprostol, other prostaglandins have precipitated seizures in epileptic patients and caused hypotension.
- Adverse GI effects are common but often transient; they can be minimized by adjusting the dose or administering the drug with food.
藥物交互作用
May aggravate misoprostol-induced diarrhea. If an antacid is required, an aluminum-only antacid is preferred.
May exacerbate renal dysfunction
Human combination products (misoprostol + diclofenac) are highly toxic to small animals due to different NSAID pharmacokinetics
監測
- Clinical efficacy (resolution of ulcer signs, successful pregnancy termination, etc.)
- Adverse effects (GI distress, diarrhea, vomiting)
- Vaginal bleeding or discharge (if used in females)
- Resolution of clinical signs of gastric ulceration (e.g., vomiting, melena, anorexia)
- Monitoring for adverse GI effects (diarrhoea, abdominal pain)
藥物動力學
半衰期
吸收
Approximately 88% of an oral dose is rapidly absorbed from the GI tract. The presence of food and antacids will delay absorption. Undergoes significant first-pass metabolism.
分佈
Both misoprostol and its active acid metabolite are highly bound to plasma proteins (approximately 90%). It is unlikely that misoprostol enters maternal milk, but it is unknown if the active acid metabolite does.
代謝
Rapidly de-esterified in the liver to its primary active metabolite, misoprostol acid. Misoprostol acid is further biotransformed via oxidative mechanisms to pharmacologically inactive metabolites.
排除
Metabolites, free acid, and small amounts of unchanged drug are principally excreted into the urine.
過量
Information on acute toxicity is limited. Overdoses in laboratory animals have produced:
- Diarrhea and emesis
- GI lesions
- Tremors and seizures
- Focal cardiac, hepatic, or renal tubular necrosis
- Hypotension
Treatment: Overdoses should be treated seriously. Employ standard gut-emptying techniques (e.g., emesis induction, activated charcoal) when applicable and safe. Treat resultant toxicity symptomatically with supportive care (e.g., IV fluids for hypotension and GI fluid loss).
可用產品
劑型
- Compounded cream
- Vaginal suppository (compounded/off-label use of tablets)
- Oral: 200 μg tablet
人用標示
- Misoprostol Tablets: 100 micrograms & 200 micrograms (Cytotec, generic)
- Cytotec 200 μg tablets
各地核准狀態
POM (Prescription Only Medicine). Human product used under the cascade.
POM (Prescription Only Medicine). Human product used under the cascade.
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儲存與穩定性
Misoprostol tablets should be stored in well-closed containers at room temperature. After manufacture, misoprostol has an expiration date of 18 months.
飼主須知
孕婦的重大警告：此藥物可能引起子宮收縮和流產。孕婦或準備懷孕的女性絕對不應接觸此藥物。如果必須處理，必須採取嚴格的預防措施（例如戴上拋棄式手套）。
- 胃腸道不適：最常見的副作用是腹瀉、腹部絞痛和嘔吐。這些症狀通常是暫時的，會隨著寵物身體適應藥物而在幾天內緩解。
- 給藥方式：將此藥物與食物一起餵食有助於減少胃部不適和腹瀉。
- 何時聯繫獸醫師：如果腹瀉變得嚴重、持續超過幾天，或者您的寵物變得昏昏欲睡，請聯繫您的獸醫師。他們可能需要調整劑量或建議使用特定的制酸劑（請避免使用含鎂的制酸劑，因為它們會加重腹瀉）。
- 雌性寵物：如果給予未結紮的雌性犬隻，由於藥物對子宮的作用，您可能會注意到陰道出血或分泌物。
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