Drug name: Shuangyiping Tablet (Huperzine A)
Description of Shuangyiping Tablet: Shuangyiping (Huperzine A) is a cholinesterase inhibitor, which can selectively inhibit the true ChE, promote memory reproduction and enhance memory retention, and is suitable for benign memory disorders, and improve patients' directed memory, associative learning, image recall and meaningless graphic reproduction. It can also improve the memory disorder caused by dementia patients and brain organic diseases.
Description of Shuangyiping Tablets:
Generic name: Huperzineatables
English name: Huperzineatables
Chinese pinyin: ShishanjianjiaPian
The main component is Huperzine A, and its chemical name is: (5r, 9r, 11e)-5-.
its structural formula:
the related pictures of this topic are as follows:
molecular formula: C15H18N2O
molecular weight: 242.32
characteristics: this product is a white tablet
pharmacology and toxicology: this product is a cholinesterase inhibitor, which has selective inhibition on true ChE and easily passes through the blood-brain barrier. Has the functions of promoting memory reproduction and enhancing memory retention.
1 pharmacological action
1.1 anticholinesterase: Huperzine A is a powerful reversible acetylcholinesterase inhibitor, and its action characteristics are similar to those of neostigmine, but its action lasts longer than the latter. Animal experiments show that this product has selective inhibition on true cholinesterase, and the inhibition intensity is thousands of times that of false cholinesterase. The inhibition mode is a mixture of competitive and non-competitive inhibition. It is significantly different from simple competitive inhibitors. It is easy to enter the center through the blood-brain barrier, and has central and peripheral therapeutic effects, with long effective time, good absorption from gastrointestinal tract, large safety index and good stability. The inhibitory intensity of acetylcholine (Ach) is huperzine A >: Physostigmine > Xin si de Ming > Huperzine b > Galanthamine, with little adverse reaction, was originally used for myasthenia gravis, but now it is mainly used to treat benign memory impairment, and it has also improved the memory impairment caused by AD and brain organic diseases.
1.2 antioxidant free radicals: Zhou Yongqi and others injected D-galactose 5 (kg d) subcutaneously into rats for 6 weeks, and then gave huperzine A at a dose of .1-.2m (kg d) for 2 weeks, respectively, to detect the activity of superoxide dismutase (SOD) and the content of malondialdehyde (MDA) in serum and brain tissue. The results showed that huperzine A could significantly increase the activity of SOD in serum and brain tissue of rats, while reducing the content of MDA, thus accelerating the scavenging of oxygen free radicals.
pharmacokinetics because the dosage of this product is extremely small, there is no drug detection method for human pharmacokinetics research at present. Animal experiments show that the oral absorption of this product is rapid and complete, and the distribution is also rapid. The half-life (t1/2α) of the distribution phase is 9.8 minutes, the bioavailability is high, and the elimination phase half-life (t1/2β) is 247.5 minutes, which is mainly excreted in the form of prototype and metabolite through urine. Because the dosage of this product is very small, there is no drug detection method for human pharmacokinetics research at present. Animal experiments show that the oral bioavailability of huperzine A is 96.9%, and it is distributed rapidly and widely in the body, with the highest distribution in the kidney and liver. Followed by lung, spleen, adrenal gland, heart, fat and brain. In the brain, frontal parietal lobe, striatum, hippocampus and nucleus accumbens are more concentrated. Huperzine A is eliminated from the body at a moderate speed, mainly through urine in its original form and its metabolites with high water solubility. < P > Clinical effect
1 A multicenter randomized double-blind method was used to treat aging-related memory dysfunction (the effect of AAMIJ on Sheng Jianhua, etc.). 63 patients with AAMI were given Huperzine A capsules or Huperzine A tablets (trade name: Shuangyiping) for 8 weeks. After treatment, the scores of Wechsler Memory Scale (wMS) and Mini-Mental State Examination (MMSE) in both groups were significantly improved (P < .5), and there was no significant difference in the increase of WMS and MMSE scores (P> .5)。 The total effective rates of capsule group and tablet group were 65.8% and 62.3% respectively, and there was no significant difference between the two groups (P> .5), and there were fewer adverse reactions in both groups. Similar studies show that huperzine A capsules and tablets have the same curative effect on AAMI.
2' s effect on memory and cognitive function of AD patients Chen Meijuan and others studied the comparison of huperzine A capsules and tablets in the treatment of AD. 92 AD patients were randomly divided into two groups, with 55 cases in capsule group. 37 cases in tablet group. Huperzine A capsules or tablets were taken orally at .15nag twice a day. * * * Take it for 8 weeks. Results The total effective rates of capsule group and tablet group in treating mild and moderate AD were 69% and 57% respectively. There was no significant difference between the two groups (P> .5)。 Similar studies show that huperzine A capsules and tablets have the same curative effect on AD. Kuang Mingzi and other studies believe that after 8 months of treatment, there is a significant difference in MMSE scores between the treatment group and the placebo control group, suggesting that huperzine A is effective in treating mild and moderate AD. A multicenter, double-blind, placebo and parallel control evaluation was conducted in 22 AD patients in 15 mental health centers in China. After 12 weeks of treatment, the MMSE score improved by an average of 2.7 points compared with the baseline. The cognitive subscale (ADAS-Cog) score of AD assessment scale improved by 4.6 points on average, with significant difference (P <: .5)。 The total adverse reaction rate of huperzine A was 3%, and all the adverse reactions were mild and transient. It shows that huperzine A can significantly improve the cognitive function, behavioral and psychological disorders, Et activity and general function of AD patients. Has good safety. Jiang Yabin et al. treated 33 AD patients with cognitive dysfunction with huperzine A orally, and observed the improvement of patients' cognitive function at the 12th, 24th and 48th weeks after treatment. The results showed that the effective rates were 5.2%, 63.6% and 66.7% respectively. Patients' behavioral disorders have also improved to varying degrees. Compared with the fourth week after the start of treatment, the dosage of psychotropic drugs also decreased significantly (P < .5)。 Only 5 patients (15.2%) had adverse drug reactions. It shows that huperzine A has a good effect on stabilizing the condition of AD patients and improving their cognitive function and behavioral disorders. The effect of
3 on memory and cognitive function of VD patients in recent years, clinical studies have found that huperzine A can also achieve satisfactory results in the treatment of VD. Bian Xin and others randomly divided 57 VD patients who met the diagnostic criteria of DAM—IVR and AIRENVD into two groups. All of them were given the same routine treatment. In addition, the patients in the treatment group (29 cases) were given Huperzine A orally, 1 times, 3 times a day for 12 weeks. The curative effect was evaluated according to MMSE, Clinical Dementia Scale (cDR) and Et Daily Living Scale (ADL). Results The memory, cognition and neurological function of mild and moderate patients in the treatment group were significantly improved. Compared with the control group, there was significant difference (P <; .5), but the curative effect of severe patients is poor. It shows that huperzine A can effectively improve the cognitive function, dementia degree and self-care ability of daily life of VD patients.
In another study, 7 patients with VD were treated with a randomized controlled method, combining meclofenoxate hydrochloride capsules and huperzine A tablets. Results Huperzine A can obviously improve the symptoms of dementia in patients with mild and moderate VD (that is, neurological deficit after stroke), and obviously improve urinary incontinence caused by stroke with few adverse reactions. It is suggested that this scheme is a better one for VD.
4 Effects on memory and cognitive function of patients with craniocerebral trauma Zhang Jianhong et al. randomly divided 6 patients with mild and moderate craniocerebral trauma into routine treatment group and huperzine A treatment group. memory quotient (MQ) and MMSE were used to evaluate memory and cognitive function before treatment and 1 and 3 months after treatment, respectively, and upper limb sensory evoked potential (SEP) was detected. Results The memory and cognitive function of huperzine A patients were improved obviously. After one or three months of treatment, the memory function of the treatment group was improved significantly compared with that of the routine group (P <: .5), the N2 latency and N13.N2 peak latency of SEP were significantly shortened. It shows that huperzine A can improve the memory function of patients with mild and moderate craniocerebral trauma and improve their brain nerve conduction function.
5 The effect of huperzine A on students' memory function can improve students' memory function. Some scholars used a double-blind method to divide 68 junior high school students into two groups according to the requirements of mental health, memory quotient proximity and the same sex in the same class, and evaluated the curative effect with the average scores of Chinese, mathematics and English and memory quotient as observation indicators. After four weeks of oral administration of Huperzine A capsule (.1mg/ time, twice a day), the results of double-blind and paired evaluation showed that the memory quotient of Huperzine A students was significantly higher than that of the comfort group (P < .5), and the scores of students in Huperzine A group have been significantly improved.
the effect of 6 on memory function of convalescent schizophrenics Ma Jiandong believes that huperzine A can improve the memory function of convalescent schizophrenics. He randomly divided 6 patients into huperzine A group (2-4 g/d) and placebo group. After 12 weeks, the scores of memory quotient, total score and subscales in Hu-PA group were significantly higher than those before treatment and placebo group (P < .5), suggesting that huperzine A has a good effect on memory impairment in schizophrenic patients. No obvious adverse reactions were found in this experiment. Many related studies have similar conclusions. In addition, some studies have found that huperzine A can improve the therapeutic effect of clozapine on 65 patients with negative symptoms of schizophrenia who meet CCMD-2-R standards when it is combined with clozapine < P > Clinical application study
1 Treatment of myasthenia gravis: Xia Qiang et al. orally administered halperine tablets to 32 patients with myasthenia gravis for 3 days, The clinical complete remission is significantly higher than that of the control group (P
2). Treatment of Alzheimer's disease: Epidemiological data show that the incidence of dementia in people over 65 years old is 4% ~ 6%, and that in people over 8 years old is 2%. With the in-depth study of etiology and pathology of senile dementia, great progress has been made in drug treatment of senile dementia. The decrease of brain metabolic function in Alzheimer's patients leads to the lack of neurotransmitters in the brain, and the most common abnormality of neurotransmitters is the low cholinergic system. Cholinergic system is necessary to maintain people's short-term memory and attention. The decline of cholinergic system function is also related to some neuropsychiatric symptoms and behaviors of patients. It has been proved that using cholinesterase inhibitors is an effective method to improve the function of cholinergic system. Huperzine A is a reversible cholinesterase inhibitor with high selectivity to true cholinesterase. The content of acetylcholine in the synaptic space of the nerve in the distribution area is obviously increased, thus enhancing the excitation conduction of neurons, strengthening the excitation of learning and memory brain areas, improving cognitive function, enhancing memory retention and promoting memory reproduction.
3 Treatment of memory disorder and improvement of memory function: In order to observe the memory improvement effect of Shuangyiping on patients with different memory disorders, 9l patients with memory disorders were treated with Shuangyiping and Naofukang respectively, including 46 patients in the treatment group (Shuangyiping group) and 45 patients in the control group, with the dosage of Shuangyiping group .1mg, twice a day and two months respectively. Naofukang group was given .8mg twice a day for 2 months. The effective rates of the two groups were 6.8% and 35.3% respectively. FP <: .5), no obvious adverse reactions were observed. Conclusion: Shuangyiping has the same effect on memory disorder.
4 Treatment of vascular dementia: 4 patients with vascular dementia were randomly divided into huperzine A treatment group and control group, both of which were given the same basic medicine. The treatment group was given huperzine A (.2m) at the same time as the basic medicine for 6 months. Results The cognitive function, memory, computing power, language and application ability of the treatment group were significantly improved, which was significantly better than that of the control group (P & .5)。
5 Prevention and treatment of multi-infarct dementia: After Xiang Jun and others combined huperzine A with Changlongtong injection for one month, the whole blood viscosity, plasma viscosity, platelet count and adhesion test, blood lipid, bleeding time, coagulation time, acetylcholinesterase, memory IQ, intelligence score and other indicators of patients were significantly improved compared with those before treatment (P <: .5 or p <; .1), and the curative effect is remarkable.
6 treatment of children with mental retardation in iodine-deficient areas: 28 children with mental retardation in iodine-deficient areas were treated with huperzine A for 3 months. Compared with the placebo group, their short-term visual memory, square-setting, counting numbers, maze prescription, etc. (P(.5), memory, spatial thinking, structural reasoning, etc. were significantly improved, but their conceptual and abstract thinking abilities were not significantly improved (corpse >: .5)。 .
7 Treatment of chronic insomnia: 53 patients with chronic insomnia who failed to take various sedatives and hypnotics for a long time. After stopping using the original drugs for 3 days, they continued to enter treatment A for 2 weeks (clonazepam was taken at night), treatment B for 4 weeks (huperzine A and clonazepam were taken alternately day and night) and treatment C for 4 weeks (clonazepam was taken at night on the premise of giving priority to the curative effect). Results Taking huperzine A and clonazepam alternately day and night can prolong the sleep time of patients, improve the rhythm of sleep awakening cycle, improve the quality of sleep, and gradually reduce the dosage of clonazepam.
8. Adjuvant treatment of negative symptoms of schizophrenia: 32 schizophrenic patients were treated with clozapine and huperzine A for 3 months, and the curative effect on negative symptoms was significantly improved compared with that in the group of taking clozapine alone, with significant difference (P <: .1)。
indications: this product is suitable for benign memory disorder, and can improve patients' abilities of pointing memory, associative learning, image recall, meaningless figure recognition and portrait recall. It can also improve the memory disorder caused by dementia patients and brain organic diseases.
administration and dosage are taken orally. 1μ g ~ 2μ g (2 ~ 4 tablets) once, twice a day, with a maximum of 9 tablets a day, or as directed by the doctor.
Adverse reactions are generally not obvious. When the dosage is too large, it can cause dizziness, nausea, gastrointestinal discomfort, fatigue and other reactions, which can generally disappear by itself. When the reaction is obvious, it will be relieved or disappeared after the dosage is reduced or stopped. Huperzine A has good safety and few adverse reactions. Tinnitus, dizziness, muscle tremor, sweating, abdominal pain, etc. are common in a few patients. Some patients have miosis, vomiting, increased stool, blurred vision, heart rate change, salivation, drowsiness, etc. The incidence of these adverse reactions is lower than that of neostigmine except nausea, and they can all disappear by themselves. Atropine can be used to fight serious cases.
Patients with epilepsy, renal insufficiency, mechanical intestinal obstruction and angina pectoris are contraindicated.
Precautions
1. Patients with bradycardia and bronchial asthma should use it with caution.
2. This product is a reversible ChE inhibitor, and its dosage varies from individual to individual, so it should generally be