| Parkinson's disease is common as a progressive neurodegenerative disease in the elderly The typical clinicaI manifestations are static tremor, rigidity, bradykinesia, gait abnormalities and postural instability. The pathological changes are very clear, the presence of proteinaceous inclusions known as Lewy bodies in the residual neurons intracytoplasmic, gliosis, the selective loss of dopaminergic neurons in the nigrostriatal system. But the exact pathogenesis is still not clear, oxidative stress, mitochondrial dysfunction, ubiquitin-proteasome system dysfunction, inflammatory reaction, excitat-ory amino acid toxicity, apoptosis etc.are involved in the pathogenesis of PD. In recent years, as the decryption of familial disease genes, we have made new progress on the understanding of the pathogenesis of PD, the familial PD and sporadic PD were linked together. The important status of mitochondrial dysfunction,oxidative stress, ubiquitin-proteasome system dysfunction in pathogenesis of PD were gradually displayed. People are trying to find a common pathogenic molecular pathway. PD gradually progresses, often cause significantly disabled in the advanced of disease. It brought great suffering to the patients, impose a heavy burden upon the social and families. There is no radical approach at present. In 1950s~1960s, People began to use L-dopa to compensate for the nigrostriatal system, and made a great success. So far, L-Dopa agents compound L-dopa (L-Dopa/ dopa decarboxylase (DDC) inhibitor), are still the most basic and effective drugs in treatment of PD, and called the gold standard treatment of PD. However, campaign complications is an insurmountable obstacle in the treatment of PD, as reserchers understanding on the pathogenesis of complications movement gradually deepening, at present, the congruous views are related to the long-term striatal neurons by stimulating the volatility, as the short half-life of L-dopa, the concentration fluctuates significantly in the blood and brain, in addition, as the disease progressing, Neurons degenerate constantly, it's capacity of buffering disappeared, cause the pulse-like stimulation to dopamine receptor, made the receptor too high or too low activation, the proposed of treatment strategy continuous dopaminergic stimulation updated treatment ideas of PD. Entacapone is a selective, reversible, peripheral inhibitor of the enzyme catechol-O-methyltransferase (COMT), came into chinese market in 2005, which breakdown levodopa to 3-O-methyldopa (3-OMD). By reducing the catabolism of levodopa, entacapone increases the plasma half-life and bioavailability of levodopa, resulting in a smoother, more continuous delivery of levodopa to the brain. Maybe the best choice to realize CDS,which brought about dawn for drug treatment of PD.objective:To study the efficacy and safety of entacapone as an adjunct to levodopa treatment in parkinsonian patients.Methods: Adopt the method of self-control study, the efficacy and safety of 6 weeks of entacapone treatment in 22 parkinsonian patients was assessed by using the Unified Parkinson's Disease Rating Scale third part (UPDRS-III) and the improved Webster score to evaluate the drug efficacy. The formula is Efficacy=score before treatment- score after treatment/score before treatment×100%, the score reduce more than 61% as effectual, 31～60% as effective, less than 30% as noneffective, use Spss12.0 statistical software to process data, regard p<0.05 as significant.Results: 1.Compared with L-Dopa Individual treatment, after received entacapone for six weeks, wo found that the UPDRSⅢand Webster scores were significantly reduced, UPDRS-ⅢScore before treatment was 51.32±5.58,score after treatment was 29.50±7.28, there was significant difference(P<0.05), in 22 patients, 17 cases confirmed effective, 3 cases noneffective, 2 cases was effectual. The average efficacy was 39.16±6.05%. the Webster score reduced notble than UPDRS-Ⅲbetween before treatment and after treatment, before treatment score was 18.13±6.02, after treatment score was 8.77±1.97, there was significant difference(P<0.05). The average efficacy was 45±6.15%. 2. In L-Dopa monotherapy, the average dose of compound L-dopa was 632.95±210.92mg, after received entacapone for 6 weeks, 7 cases reduced the dose of compound L-dopa, the total dose was 612.5mg, the average dose was 605.11±188.41mg, the average dose reduced 27.84±9.76mg.Before received entacapone, 5cases experienced dyskinesias, 1case experienced end-of-dose wearing-off, after received entacapone, the symptoms all disappeared. 3. after received entacapone, 6 cases appeared dyskinesias, 1of the 6 persons got nausea, vomiting, anorexia, orthostatic hypotension, the symptoms also disappeared after reduce the compound L-dopa dose. 2 cases of abdominal pain, one case of diarrhea, insomnia two cases, 2 cases of dry mouth, the symptoms were not obvious, and disappeared in the following treament.Conclusion: 1. Compared with L-Dopa monotherapy, the UPDRSⅢand Webster scores significantly reduced after received entacapone. 2. It made a reduction in the levodopa dosage required to control symptoms. 3. Entacapone was effective to fluctuations and dyskinesias. 4. There was no adverse event and serious laboratory result. 5. A continuous dopaminergic stimulation may not only offer clinical benefits in terms of improved symptom control, but also offer protective benefits in terms of delaying the onset of motor complications, it's conducive to the long-term levodopa therapy . Entacapone is an effective and safe levodopa extender and enhancer, whice improve the symptomatic efficacy of compound levodopa in PD. |
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