青黴胺
Penicillamine
D-Penicillamine, beta,beta-Dimethylcysteine, D-3-Mercaptovaline
別名: Depen · Cuprimine · Pendramine · D-Penicillamine · beta,beta-Dimethylcysteine · D-3-Mercaptovaline · penicillaminum
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 |
|---|---|---|---|---|---|
| Copper-associated hepatopathy | 10-15 mg/kg PO q12h on an empty stomach. Do not give concurrently with any medication, including zinc or a vitamin-mineral supplement. | PO | q12h | — | 🌎 NA |
| Copper-associated hepatopathy | 15 mg/kg PO twice daily 30 minutes before meals. Give supplemental pyridoxine. Chelate at least 6 months, and then use a second liver biopsy to determine efficacy and chronic treatment plan. | PO | q12h | At least 6 months | 🌎 NA |
| Copper-associated hepatopathy | 10-15 mg/kg PO two times a day 30 minutes prior to food. Start low and increase. | PO | q12h | — | 🌎 NA |
| Copper-associated hepatopathy | 15 mg/kg PO twice daily on an empty stomach. | PO | q12h | — | 🌎 NA |
| Cystine urolithiasis | 15 mg/kg: PO twice daily. If nausea and vomiting occur, mix with food or give at mealtime. Some dogs may need to have the dosage slowly increased to full dose in order to tolerate the drug. | PO | q12h | — | 🌎 NA |
| Cystine urolithiasis | 15 mg/kg: PO twice daily with food | PO | q12h | — | 🌎 NA |
| Lead poisoning | 110 mg/kg/day, PO divided q6-8h for 1-2 weeks. If vomiting, depression, and anorexia occur, may reduce dose to 33-55 mg/kg/day divided q6-8h, which should be better tolerated. | PO | q6-8h | 1-2 weeks | 🌎 NA |
| Lead poisoning | 110 mg/kg/day divided q6-8h PO 30 minutes before feeding for 1-2 weeks. If vomiting a problem may premedicate with dimenhydrinate (2-4 mg/kg PO). Alternatively, may give 33-55 mg/kg/day divided as above. | PO | q6-8h | 1-2 weeks | 🌎 NA |
| Copper storage disease / Copper-associated hepatopathy | Dose not specified in monograph | PO | Not specified | Long-term (weeks to months) | 🌍 EU |
| Cystinuria | Dose not specified in monograph | PO | Not specified | Not specified | 🌍 EU |
| Lead toxicity | Dose not specified in monograph | PO | Not specified | Long-term | 🌍 EU |
- Copper-associated hepatopathy: If patient is zinc intolerant, use chronic penicillamine at a dose restriction of 50%. Do not use chelation and zinc together.
- Lead poisoning: After initial therapy regimen with CaEDTA and if continued therapy is desired at home.
- Lead poisoning: As an alternate or adjunct to CaEDTA. Dissolving medication in juice may facilitate administration.
- Copper storage disease / Copper-associated hepatopathy: Not helpful in an acute crisis. Pretreat with antiemetics 30-60 mins before if poorly tolerated.
- Cystinuria: Decreases cystine excretion by forming soluble complex.
- Lead toxicity: Used when injecting EDTA is too difficult or long-term chelation is required.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Lead poisoning | 125 mg q12h PO for 5 days. | PO | q12h | 5 days | 🌎 NA |
- Lead poisoning: After initial therapy with CaEDTA and if blood lead is greater than 0.2 ppm at 3-4 weeks post-treatment.
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Adjunctive treatment of lead poisoning | 55 mg/kg PO q12h for 1-2 weeks. | PO | q12h | 1-2 weeks | 🌎 NA |
- Adjunctive treatment of lead poisoning: Suggested to combine CaEDTA and penicillamine for several days until symptoms dissipate followed by a 3-6 week treatment with penicillamine.
牛
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Lead or mercury toxicity | 110 mg/kg PO for 1-3 weeks. | PO | Unknown | 1-3 weeks | 🌎 NA |
- Lead or mercury toxicity: To prevent continued metal absorption, must clear GI tract of toxic metal before therapy. FARAD recommends a minimum milk withdrawal time of 3 days after the last treatment and a 21-day preslaughter withdrawal.
羊
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Copper toxicity | 52 mg/kg daily for 6 days | PO | q24h | 6 days | 🌎 NA |
| Copper toxicity | 26-52 mg/kg PO once daily for 6 days. | PO | q24h | 6 days | 🌎 NA |
| Lead or mercury toxicity | 110 mg/kg PO for 1-3 weeks. | PO | Unknown | 1-3 weeks | 🌎 NA |
- Copper toxicity: FARAD recommends a minimum milk withdrawal time of 3 days after the last treatment and a 21-day preslaughter withdrawal.
- Lead or mercury toxicity: Must clear GI tract of toxic metal before therapy.
山羊
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Copper toxicity | 52 mg/kg daily for 6 days | PO | q24h | 6 days | 🌎 NA |
| Copper toxicity | 26-52 mg/kg PO once daily for 6 days. | PO | q24h | 6 days | 🌎 NA |
| Lead or mercury toxicity | 110 mg/kg PO for 1-3 weeks. | PO | Unknown | 1-3 weeks | 🌎 NA |
- Copper toxicity: FARAD recommends a minimum milk withdrawal time of 3 days after the last treatment and a 21-day preslaughter withdrawal.
- Lead or mercury toxicity: Must clear GI tract of toxic metal before therapy.
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
青黴胺是一種強效的螯合劑，在獸醫學中主要用於治療銅儲積性肝病（如貝林登㹴、拉布拉多犬和大麥町犬）。它也可用於鉛或汞中毒的長期口服治療，以及胱氨酸尿石症的溶解與預防。由於其具有抗纖維化特性，可能對慢性肝炎有益，但所需劑量通常難以耐受。
作用機轉
Penicillamine exerts its effects through multiple distinct mechanisms depending on the target condition:
- Heavy Metal Chelation: Contains sulfhydryl groups that bind to heavy metals (copper, lead, iron, mercury) → forms stable, water-soluble complexes → facilitates rapid excretion via the kidneys.
- Cystine Urolithiasis: Combines chemically with cystine via a disulfide interchange reaction → forms a stable, highly soluble penicillamine-cysteine mixed disulfide complex → readily excreted in urine, preventing stone formation.
- Antirheumatic Activity: Mechanism is not fully elucidated, but it improves lymphocyte function and decreases IgM rheumatoid factor and immune complexes in serum and synovial fluid.
- Antifibrotic Activity: Inhibits lysyl oxidase and collagen crosslinking → renders newly synthesized collagen more susceptible to enzymatic degradation.
安全性與警告
禁忌症
- Patients with a history of penicillamine-related blood dyscrasias
- Presence of lead in the gastrointestinal tract (can enhance absorption)
- Pregnancy (unless benefits outweigh teratogenic risks)
- Moderate to marked renal impairment
不良反應
- Nausea
- Vomiting
- Depression
- Anorexia
- Dietary mineral deficiencies (zinc, iron, copper, calcium) with long-term use
- Fever (rare)
- Lymphadenopathy (rare)
- Skin hypersensitivity reactions (rare)
- Immune-complex glomerulonephropathy (rare)
- Teratogenicity
- Pyrexia
- Nephrotic syndrome
- Leucopenia (human data)
- Thrombocytopenia (human data)
- Lymphadenopathy (human data)
- Skin hypersensitivity reactions (human data)
- Lupus-like reactions (human data)
注意事項
Penicillamine is contraindicated in patients with a history of penicillamine-related blood dyscrasias. Warning: Penicillamine potentially can cause enhanced absorption of lead from the gastrointestinal tract. If lead is still present in the gut (e.g., visible on radiographs), it should NOT be administered until the GI tract is cleared. Use with caution in pregnant animals due to known teratogenic potential (FDA Category D).
藥物交互作用
Concomitant administration may increase the risks for severe dermatologic adverse effects.
May decrease the effectiveness of penicillamine if given orally together due to chelation in the gut.
The amount of penicillamine absorbed from the GI tract may be reduced by concurrent administration.
May increase the risk of hematologic and/or renal adverse reactions.
May increase the risk of hematologic and/or renal adverse reactions.
May increase the risk of hematologic and/or renal adverse reactions.
Decreased gastrointestinal absorption of penicillamine
Decreased gastrointestinal absorption of penicillamine
Decreased gastrointestinal absorption of penicillamine
Decreased gastrointestinal absorption of penicillamine
Increased renal and haematological adverse effects
Increased risk of renal damage
Increased risk of renal damage
監測
- Clinical efficacy (e.g., resolution of neurologic signs in lead poisoning)
- Liver enzymes (ALT) and liver copper levels via biopsy (for hepatopathy)
- Urinalysis and stone dissolution (for cystine urolithiasis)
- Complete blood count (CBC) and urinalysis to monitor for rare blood dyscrasias or glomerulonephropathy
- Full blood count (weekly initially)
- Urinalysis (weekly initially)
- Renal function
- Dietary mineral levels (zinc, iron, copper, calcium) during long-term use
藥物動力學
吸收
In humans, well absorbed after oral administration. Peak serum levels occur about one hour after dosing. Food decreases bioavailability.
分佈
Crosses the placenta. Otherwise, little information is known about its distribution.
代謝
Penicillamine that is not complexed with either a metal or cystine is thought to be metabolized by the liver.
排除
Excreted in the urine and feces.
過量
No specific acute toxic dose has been established for penicillamine. Toxic effects generally occur in patients taking the drug chronically. Any relationship of toxicity to dose is unclear; patients on small doses may develop toxicity. Management of overdose would be largely supportive and symptomatic.
可用產品
劑型
- Titratable Oral Tablets: 250 mg
- Oral Capsules: 125 mg, 250 mg
- 125 mg oral tablet
- 250 mg oral tablet
獸醫用
- None
人用標示
- Penicillamine Titratable Oral Tablets: 250 mg (scored); Depen (Wallace)
- Penicillamine Oral Capsules: 125 mg & 250 mg; Cuprimine (Aton Pharma)
- Pendramine 125 mg tablets
- Pendramine 250 mg tablets
- Penicillamine 125 mg tablets
- Penicillamine 250 mg tablets
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
Penicillamine should be stored at room temperature (15-30°C). The capsules should be stored in tight containers; tablets in well-closed containers.
飼主須知
此藥物主要用於幫助您的寵物排出體內過多的金屬（如銅或鉛），或溶解特定類型的膀胱結石。
- 給藥方式：最好在空腹時給藥（餵食前至少30分鐘），以確保藥物被充分吸收。
- 副作用管理：如果您的寵物出現嘔吐或食慾不振，請聯繫獸醫。他們可能會建議：將每日劑量分成更小、更頻繁的劑量；暫時減少劑量；或與少量食物（如起司或麵包）一起餵食以減少腸胃不適。
- 請勿將此藥物與維生素/礦物質補充劑（特別是含鋅或鐵的產品）或制酸劑同時餵食，因為它們會與藥物結合並使其失效。
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。