丹曲林鈉
Dantrolene Sodium
Dantrolene Sodium (Hydantoin derivative)
別名: Dantrium · Danlene · Dantamacrin · Dantralen · F-440 · F-368 · Dantrolene sodium
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。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Treatment of functional urethral obstruction due to increased external urethral tone | 1-5 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Treatment of functional urethral obstruction due to increased external urethral tone | 1 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
| Canine stress syndrome (CSS)/Malignant Hyperthermia (MH) - acute attack | 0.2-3 mg/kg IV | IV | Once/PRN | — | 🌎 NA |
| MH-like syndrome associated with hops (Humulus lupulus) ingestion | 2-3 mg/kg IV or 3.5 mg/kg PO as soon as possible after ingestion. | IV/PO | Once | — | 🌎 NA |
| Adjunctive treatment of rhabdomyolysis | 1.5 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
| Adjunctive treatment of Black Widow Spider bite | 1 mg/kg IV ; followed by 1 mg/kg PO q4h | IV, then PO | q4h | — | 🌎 NA |
- Adjunctive treatment of rhabdomyolysis: From a case report; very intensive drug and supportive therapy used in this case.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Treatment of functional urethral obstruction due to increased external urethral tone | 0.5-2 mg/kg PO q12h OR 0.5-1 mg/kg IV | PO/IV | q12h | — | 🌎 NA |
| Treatment of functional urethral obstruction due to increased external urethral tone | 0.5-2 mg/kg PO three times daily | PO | TID | — | 🌎 NA |
| Treatment of functional urethral obstruction due to increased external urethral tone | 2-10 mg (total dose) PO three times daily | PO | TID | — | 🌎 NA |
| Treatment of functional urethral obstruction due to increased external urethral tone | 0.5-1 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
- Treatment of functional urethral obstruction due to increased external urethral tone: IV product very expensive.
- Treatment of functional urethral obstruction due to increased external urethral tone: Given with either prazosin (0.5 mg/cat once to twice daily) or phenoxybenzamine (2.5-7.5 mg/cat once to twice daily).
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Treatment of acute rhabdomyolysis | 15-25 mg/kg slow IV four times daily | IV | QID | — | 🌎 NA |
| Treatment of acute rhabdomyolysis | 2-4 mg/kg PO via nasogastric tube once daily | PO | SID | — | 🌎 NA |
| Prevention of recurrent exertional rhabdomyolysis in Thoroughbreds | 4 mg/kg PO in horses fasted (12-hour fast in study) prior to administration. | PO | Once | — | 🌎 NA |
| Prevention of rhabdomyolysis | 2 mg/kg PO once daily for 3-5 days and then every 3rd day for a month | PO | SID then q3d | 1 month | 🌎 NA |
| Prevention of rhabdomyolysis | 300 mg (total dose) PO once daily | PO | SID | — | 🌎 NA |
| Prevention of rhabdomyolysis | 500 mg (total dose) PO for 3-5 days and then 300 mg PO every third day. | PO | SID then q3d | — | 🌎 NA |
| Prevention of rhabdomyolysis | 800 mg (total dose); within 30 minutes prior to administration contents of capsules mixed with 9 mL tap water to make a suspension and given PO one hour before exercise. | PO | Once before exercise | — | 🌎 NA |
| Prevention of post-anesthetic myositis (PAM) | 6 mg/kg enterally (given via NG tube in study) 60 minutes prior to general anesthesia. | Enteral | Once | — | 🌎 NA |
| Prevention of post-anesthetic myositis (PAM) | 10 mg/kg PO (intragastric) 1.5 hours before surgery. | PO | Once | — | 🌎 NA |
| Prevention of post-anesthetic myositis (PAM) | 1.9 mg/kg loading | IV | Once | — | 🌎 NA |
| Prevention of post-anesthetic myositis (PAM) | 4 mg/kg | IV | Once | — | 🌎 NA |
- Prevention of rhabdomyolysis: Drug is diluted in normal saline and given via stomach tube. Monitor hepatic function.
- Prevention of rhabdomyolysis: May be preferable because the drug is hepatotoxic.
- Prevention of post-anesthetic myositis (PAM): Does not appear to prolong recovery time.
- Prevention of post-anesthetic myositis (PAM): Should give peak levels at the time surgery begins and maintain postulated therapeutic levels for an additional 2 hours. Additional doses of 2.5 mg/kg PO (intragastric) q60 minutes can be given.
- Prevention of post-anesthetic myositis (PAM): Will give therapeutic levels but will only persist for about 20 minutes.
- Prevention of post-anesthetic myositis (PAM): Will maintain therapeutic levels for about 2 hours, but peak levels will be quite high.
豬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Prevention or treatment of malignant hyperthermia | 3.5 mg/kg IV | IV | Once/PRN | — | 🌎 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
丹曲林鈉是一種獨特的直接作用型骨骼肌鬆弛劑。與中樞作用的肌肉鬆弛劑（如美索巴莫或地西泮）不同，它直接作用於周邊肌肉纖維。
在獸醫學中，其主要適應症包括：
- 惡性高熱 (MH)： 針對豬隻和犬隻惡性高熱及豬緊迫症候群的救命藥物。
- 馬匹肌肉病變： 廣泛用於馬匹以預防和治療勞力性橫紋肌溶解症（「綁住」症候群）及麻醉後肌炎 (PAM)。
- 小動物泌尿科： 常用於降低犬貓尿道外括約肌張力，以治療功能性尿道阻塞。
- 毒素咬傷： 建議作為黑寡婦蜘蛛咬傷的輔助治療，因該毒素會引起大量乙醯膽鹼釋放及嚴重的肌肉痙攣。
臨床要點： 由於注射劑型極為昂貴且重配後保存期限短，通常僅保留用於嚴重、急性的危機（如惡性高熱），而口服劑型則用於慢性管理或預防。
作用機轉
Dantrolene acts intracellularly to uncouple the excitation-contraction process in skeletal muscle.
- It binds specifically to the ryanodine receptor (RyR1) located on the sarcoplasmic reticulum (SR).
- This binding blocks the release of calcium (Ca²⁺) from the SR into the myoplasm.
- Decreased intracellular calcium → prevents the interaction of actin and myosin → produces skeletal muscle relaxation.
Because it specifically targets the RyR1 isoform (found primarily in skeletal muscle) rather than RyR2 (cardiac muscle), it has minimal direct effects on cardiac or smooth muscle at standard therapeutic doses. The exact mechanism for its mild CNS effects (drowsiness, dizziness) remains poorly understood.
安全性與警告
禁忌症
- Preexisting liver disease (use with extreme caution)
- Severe cardiac dysfunction (use with caution)
- Pulmonary disease (use with caution)
不良反應
- Weakness
- Sedation
- Dizziness
- Headache
- Nausea
- Vomiting
- Constipation
- Increased urinary frequency
- Hypotension
- Hepatotoxicity (especially with chronic use)
注意事項
Hepatotoxicity Warning: Dantrolene can cause hepatotoxicity. It should be used with extreme caution in patients with preexisting liver disease. Monitor liver enzymes closely during chronic therapy.
- Use with caution in patients with severe cardiac dysfunction or pulmonary disease.
- Pregnancy: FDA Category C (human); Papich Class C (veterinary). Use cautiously as a last resort when benefits clearly outweigh risks.
- Nursing: Distributed into milk; safe use cannot be assured during nursing.
藥物交互作用
Increased sedation may be seen if tranquilizing agents are used concomitantly.
Rare reports of cardiovascular collapse in humans; concomitant use during malignant hyperthermia crises is not recommended.
Increased risks of hepatotoxicity have been seen in women >35 years of age; veterinary significance is unknown.
Dantrolene may be displaced from plasma proteins by warfarin, resulting in increased effects or adverse reactions.
監測
- Baseline and periodic liver function tests (ALT, AST, Alk Phos, etc.) if projecting to be used chronically or using high dosages
- Body temperature (especially for malignant hyperthermia)
- Urine volume, frequency, continence
藥物動力學
半衰期
吸收
Bioavailability after oral administration is ~35% in humans and ~39% in horses (intragastric). Fairly slowly absorbed; peak levels occur ~5 hours post-oral dose in humans and 1.5 hours in horses. In horses, oral absorption is affected by food and must be given to a fasted horse to achieve therapeutic levels.
分佈
Substantially bound to plasma proteins (principally albumin). Many drugs may displace it.
代謝
Metabolized in the liver.
排除
Metabolites are excreted in the urine. Only about 1% of the parent drug is excreted unchanged in the urine and bile.
過量
There is no specific antidotal therapy for dantrolene overdoses.
- Decontamination: Remove the drug from the gut if possible (e.g., emesis induction, activated charcoal) if exposure was recent and oral.
- Supportive Care: Treat supportively, monitoring respiratory, cardiovascular, and hepatic function.
可用產品
劑型
- Oral Capsules
- Powder for Injection Solution
人用標示
- Dantrolene Sodium Oral Capsules: 25 mg, 50 mg, & 100 mg (Dantrium; generic)
- Dantrolene Sodium Powder for Injection Solution: 20 mg/vial (approx. 0.32 mg/mL dantrolene after reconstitution; with mannitol 3 g/vial) in 70 mL vials (Dantrium Intravenous)
各地核准狀態
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Capsules should be stored in well-closed containers at room temperature. Powder for injection should be stored at temperatures less than 30°C and protected from prolonged exposure to light. After reconstitution, the powder for injection should be used within 6 hours when stored at room temperature and should be protected from direct light. It is NOT compatible with either normal saline or D5W injection.
飼主須知
- 預期副作用： 丹曲林可能會引起輕微的腸胃不適（嘔吐、食慾不振）、排尿頻率增加以及鎮靜（嗜睡或虛弱）。
- 肝臟警告： 在極少數情況下，丹曲林會引起肝臟毒性。如果您的寵物出現持續嘔吐、食慾不振、不明原因的嚴重嗜睡，或眼白/牙齦發黃（黃疸），請立即聯繫您的獸醫。
- 給藥方式： 此藥物的靜脈注射應僅由熟悉其用法及監測要求的獸醫專業人員進行。
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。