目前治疗帕金森病 (PD) 的药物分为以下几类:
- Anticholinergics: Trihexyphenidyl (Artane)
- Antihistamines: Diphenhydramine (Benadryl), Amantadine
- Levodopa-based Drugs: Madopar (Levodopa/Benserazide), Sinemet (Carbidopa/Levodopa), Xilaimei
- Dopamine Agonists: Pramipexole (Mirapex), Ropinirole (Requip), Cabergoline (Cripar), Bromocriptine
- MAO-B Inhibitors: Selegiline (Eldepryl), Rasagiline (Azilect)
- COMT Inhibitors: Entacapone (Comtan)
1. Levodopa and Combination Therapies
- Levodopa: Introduced in 1967, levodopa revolutionized PD treatment by replenishing dopamine in the brain. Alone, it struggles to cross the blood-brain barrier, so it’s often combined with peripheral decarboxylase inhibitors (e.g., benserazide or carbidopa).
- Madopar (Levodopa/Benserazide): A leading global PD drug, Madopar dominates the Chinese market with a 5.49% share in neurological drug sales (2002 data).
- Sinemet (Carbidopa/Levodopa): Developed by Bristol Myers Squibb, Sinemet generated $108 million globally in 2003 but holds a smaller share in China.
2. Dopamine Agonists
Used as initial therapy or alongside levodopa to reduce long-term side effects:
- Bromocriptine (Parlodel): A first-generation agonist with $13.4 million in U.S. sales (2000). In China, Novartis and Gedeon Richter’s versions dominate.
- Pergolide (Celance/协良行): Withdrawn in some markets due to cardiac risks but still used in China via Eli Lilly’s imports.
- Ropinirole (Requip): Launched in 1996 by GSK, its global revenue reached $162 million by 2003.
- Pramipexole (Mirapex/森福罗): Developed by Boehringer Ingelheim, revenue grew to €232 million by 2003.
3. MAO-B and COMT Inhibitors
- Selegiline (司吉宁): Slows dopamine breakdown, extending levodopa’s effects.
- Entacapone (柯丹): Blocks COMT enzymes to prolong levodopa efficacy.
Market Insights
- Levodopa combinations like Madopar and Sinemet dominate global sales, with Madopar alone achieving $179 million (2003).
- In China, domestic manufacturers (e.g., Guangzhou Qiaoguang Pharma) compete with imports, driving affordability.
- Dopamine agonists (e.g., bromocriptine) remain critical, with bromocriptine sales hitting ¥52.56 million (2003) in China.
Key Takeaways:
- Levodopa remains foundational, but combination therapies enhance efficacy.
- Dopamine agonists balance symptom control and side-effect risks.
- Emerging generics in China improve access but challenge multinational brands.
Let me know if you need further refinements! 😊
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