ペニシラミン
Penicillamine
D-Penicillamine, beta,beta-Dimethylcysteine, D-3-Mercaptovaline
別名: Depen · Cuprimine · Pendramine · D-Penicillamine · beta,beta-Dimethylcysteine · D-3-Mercaptovaline · penicillaminum
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
ヤギ
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
ペニシラミンは強力なキレート剤であり、獣医学においては主にベドリントンテリアやラブラドールレトリバーなどの銅蓄積性肝疾患の管理に使用されます。また、鉛や水銀中毒の長期経口治療、およびシスチン尿石症の溶解・予防にも有効です。抗線維化作用を持つため慢性肝炎に有益な可能性がありますが、必要な用量は耐容性が低いことが多いです。
作用機序
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・警告
禁忌
- 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
有害事象
- 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).
医薬品相互作用
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
監視
- 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
薬物動態
吸収
In humans, well absorbed after oral administration. Peak serum levels occur about one hour after dosing. Food decreases bioavailability.
分布
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.
消失
Excreted in the urine and feces.
過剰投与
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.
製品
製剤
- Titratable Oral Tablets: 250 mg
- Oral Capsules: 125 mg, 250 mg
- 125 mg oral tablet
- 250 mg oral tablet
動物用医薬品
- None
ヒト用医薬品
- 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
規制ステータス
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Penicillamine should be stored at room temperature (15-30°C). The capsules should be stored in tight containers; tablets in well-closed containers.
飼主向け情報
この薬は、ペットの体内の過剰な金属（銅や鉛など）を排出したり、特定の種類の膀胱結石を溶解するために使用されます。
- 投与方法：薬が適切に吸収されるよう、できれば空腹時（食事の少なくとも30分前）に投与してください。
- 副作用の管理：ペットに嘔吐や食欲不振が見られる場合は、獣医師にご相談ください。1日の投与量を小分けにして回数を増やす、一時的に減量する、または胃の負担を和らげるために少量の食事（チーズやパンなど）と一緒に与えるなどの提案があるかもしれません。
- ビタミン・ミネラルサプリメント（特に亜鉛や鉄を含むもの）や制酸剤と同時に与えないでください。これらは薬と結合して効果を失わせる可能性があります。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。