Huperzine A In Dementia
Pharmacol Biochem Behav. 2003 Jun;75(3):675-86.
The psychopharmacology of huperzine A: an alkaloid with cognitive enhancing and neuroprotective properties of interest in the treatment of Alzheimer's disease.
Zangara A. Cognitive Drug Research, CDR House, 24 Portman Road, Reading RG30 1EA, UK.
Huperzine A (HupA), extracted from a club moss (Huperzia serrata), is a sesquiterpene alkaloid and a powerful and reversible inhibitor of acetylcholinesterase (AChE). It has been used in China for centuries for the treatment of swelling, fever and blood disorders. It has demonstrated both memory enhancement in animal and clinical trials and neuroprotective effects. Recently it has undergone double-blind, placebo-controlled clinical trials in patients with Alzheimer's disease (AD), with significant improvements both to cognitive function and the quality of life. Most of the clinical trials are from China, but HupA and derivatives are attracting considerable interest in the West, where AD is a major and growing concern. Furthermore, both animal and human safety evaluations have demonstrated that HupA is devoid of unexpected toxicity. Other interesting aspects of HupA pharmacological profile relate to its neuroprotective properties: it has been shown in animal studies that HupA can be used as a protective agent against organophosphate (OP) intoxication and that it reduces glutamate-induced cell death.
Zhonghua Yi Xue Za Zhi. 2002 Jul 25;82(14):941-4.
Clinical efficacy and safety of huperzine Alpha in treatment of mild to moderate Alzheimer disease, a placebo-controlled, double-blind, randomized trial
Zhang Z, Wang X, Chen Q, Shu L, Wang J, Shan G. Department of Neurology and Clinical Epidemiology Unit, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100730, China.
OBJECTIVE: To evaluate the clinical efficacy and safety of huperzine Alpha in treatment of patients with mild to moderate Alzheimer disease (AD). METHODS: Two hundred and two patients with the diagnosis of possible or probable AD from 15 centers the nationwide were randomly divided into two groups: huperzine Alpha group (n = 100, given huperzine Alpha 400 micro g/day for 12 weeks) and placebo group (n = 102 ). Different scales were used to evaluate the cognitive function, activity of daily life (ADL), non-cognitive disorders, and overall clinical efficacy. Safety evaluation was conducted every 6 weeks. RESULTS: In comparison with the baseline data, there was an improvement of 4.6 points in cognition assessed by ADAS-Cog (P = 0.000); an improvement of 2.7 points by MMSE (P = 0.000), an improvement of 1.5 points in behavior and mood by ADAS-non-Cog (P = 0.008) with 59.2% of the patients being on the mend clinically; and an improvement of 2.4 points by ADL (P = 0.001) with the capacity of ADL improved by at least 10% among 32.75% of the patients. 70% of the patients in huperzine Alpha group scored 1 approximately 3 points, and 27.8% of them scored 1 approximately 2 points by CIBIC-plus. The proportions of patients with an improvement of >/= 4 points by ADAS-Cog were 56.1% and 12.5% in the huperzine Alpha group and placebo group respectively (P = 0.000). The proportions of patients with an improvement of >/= 4 points by MMSE were 37.8% and 10.1% in the huperzine Alpha group and placebo group respectively (P = 0.000). The proportions of patients with an improvement of 1 approximately 3 points in global rating by CIBIC-plus were 59.2% and 40.6% in the huperzine Alpha group and placebo group respectively (P = 0.01). The proportions of patients with an improvement of >/= 10% points by ADL were 32.7% and 17.2% in the huperzine Alpha group and placebo group respectively (P = 0.01). The proportions of patients with an improvement of > 0 points by ADS-non-C0g were 70.0% and 36.3% in the huperzine Alpha group and placebo group respectively (P = 0.000). Mild and transient adverse events (edema of bilateral ankles and insomnia) were observed in 3% of huperzine Alpha treated patients. CONCLUSION: A safe and effective medicine, huperzine Alpha remarkably improves the cognition, behavior, ADL,and mood of AD patients.
Zhongguo Yao Li Xue Bao. 1999 Jun;20(6):486-90.
Huperzine-A in capsules and tablets for treating patients with Alzheimer disease.
Xu SS, Cai ZY, Qu ZW, Yang RM, Cai YL, Wang GQ, Su XQ, Zhong XS, Cheng RY, Xu WA, Li JX, Feng B. Zhejiang Mental Health Institute, Hangzhou, China.
AIM: To compare the efficacy and safety between huperzine-A (Hup) in capsules and tablets for treating patients with Alzheimer disease (AD). METHODS: Using multicenter, prospective, double-blind, double-mimic, parallel, positive controlled and randomized methods, 60 patients meeting with the NINCDS-ARDRA criteria of AD were divided into 2 equal groups. Patients in the capsule group received 4 capsules of Hup (each contains 50 micrograms) and 4 tablets of placebo (lactose and starch inside); while the tablet group received 4 tablets of Hup (each contains 50 micrograms) and 4 capsules of placebo, p.o., twice a day for 60 d. All the patients were evaluated with a lot of related ranting scales, and physiological and laboratory examination. RESULTS: There were significant differences (P < 0.01) on all the psychological evaluations between 'before' and 'after' the 60-d trial of 2 groups, but there was no significant difference between 2 groups by group t test (P > 0.05). The changes of oxygen free radicals in 2 groups showed marked improvement. No severe side effect besides moderate to mild nausea was found in both groups. CONCLUSION: There is equal efficacy and safety between Hup in capsule and tablet for treating patients with AD, and Hup can reduce the pathological changes of the oxygen free radicals in the plasma and erythrocytes of patients with AD.
Zhongguo Yao Li Xue Bao. 1995 Sep;16(5):391-5.
Efficacy of tablet huperzine-A on memory, cognition, and behavior in Alzheimer's disease.
Xu SS, Gao ZX, Weng Z, Du ZM, Xu WA, Yang JS, Zhang ML, Tong ZH, Fang YS, Chai XS, et al. Zhejiang Supervision and Detection Station of Drug Abuse, Zhejiang Medical University, Hangzhou, China.
AIM: To evaluate the efficacy and safety of tablet huperzine-A (Hup) in patients with Alzheimer's disease. METHODS: Using multicenter, prospective, double-blind, parallel, placebo controlled and randomized method, 50 patients were administered orally 0.2 mg (4 tablets) Hup and 53 patients were given po 4 tablets of placebo bid for 8 wk. All patients were evaluated with Wechsler memory scale, Hasegawa dementia scale, mini-mental state examination scale, activity of daily living scale, treatment emergency symptom scale, and measured with BP, HR, ECG, EEG, ALT, AKP, BUN, Cr, Hb, WBC, and urine routine. RESULTS: About 58% (29/50) of patients treated with Hup showed improvements in their memory (P < 0.01), cognitive (P < 0.01), and behavioral (P < 0.01 functions. The efficacy of Hup was better than placebo (36%, 19/53) (P < 0.05). No severe side effect was found. CONCLUSION: Hup is a promising drug for symptomatic treatment of Alzheimer's disease.
Zhongguo Yao Li Xue Bao. 1991 May;12(3):250-2.
Drug evaluation of huperzine A in the treatment of senile memory disorders
Zhang RW, Tang XC, Han YY, Sang GW, Zhang YD, Ma YX, Zhang CL, Yang RM.Zhejiang Academy of Medical Sciences, Hangzhou, China.
Huperzine A is an alkaloid which was first isolated from Huperzia serrata (Thumb) Trev by Zhejiang Academy of Medical Sciences and Shanghai Institute of Materia Medica, Chinese Academy of Sciences. It exhibits a significant anticholinesterase activity and has been used on myasthenia gravis patients. The therapeutic effects were studied by random, match and double-blind method on 56 patients of multi-infarct dementia or senile dementia and 104 patients of senile and presenile simple memory disorders. The curative effects were evaluated by Wechsler memory scale. The im dose for multi-infarct dementia was 0.05 mg bid for 4 wk, whereas that for senile and presenile simple memory disorders was 0.03 mg bid for 2 wk. Saline was used on control group. The result showed that the curative effect of huperzine A was significant. Only a few patients felt slight dizziness and this did not affect the therapeutic effects.
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