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OBJECTIVE: To investigate the chiral separation of the manidipine enantiomers by the proposed synthetic route, and the blood pressure effect of the hydrochlorides. METHODS: Based on the solubility differences of the salts which are the reaction products of the manidipine enantiomers and the different chiral resolution agents[(+)-Di-p-toluoyl-D-tartaric acid/(-)-Di-p-toluoyl-L-tartaric acid] in the specific solvents, the S and R manidipine enantiomers were obtained respectively, which is called the chemical salting out crystal method. The changes of systolic pressure, diastolic pressure, and mean arterial pressure of spontaneously hypertensive rats(SHR) before and after manidipine hydrochloride medications administration were monitored through implantable physiological signal remote sensing pressure monitoring system (data science international, DSI). RESULTS: The chiral separation process is simple, maneuverability is strong and the ee values and purity of the S and R enantiomorphism isomers are both higher in the synthetic route; in the SHR model, the antihypertensive effect was equivalent between manidipine hydrochloride group and S-manidipine hydrochloride group; R-manidipine hydrochloride did not have the antihypertensive effect. CONCLUSION: The chiral resolution of manidipine enantiomers has certain scientific value, which can improve the efficacy and safety of drug, and which is of great significance to develop manidipine single enantiomeric new drugs.
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Objective To study the influence analysis of patients with anxiety and depression in elderly patients with hypertension antihypertensive effect of psychological intervention combined with Flupentixol and Melitracen Tablets.Methods 60 elderly patients with hypertension accompanied by anxiety and depression in our hospital from January 2014 to December 2016 were selected as the subjects.They were randomly divided into the control group and the experimental group, with 30 patients in each group.The control group was treated with conventional antihypertensive treatment, the experimental group were given psychological intervention combined with treatment of Flupentixol and Melitracen Tablets.The clinical indexes of the experimental group and the control group were compared and analyzed.Results After the corresponding treatment, the effective rate of antihypertensive treatment in the experimental group was 28 cases, and the effective rate of depressurization was 93.3%.The effective rate of antihypertensive treatment in the control group was 21, and the effective rate of antihypertensive treatment was 70%.After treatment, the HAMD score and HAMA score of the experimental group were significantly lower than those before the treatment, and the score of the experimental group was significantly lower than that of the control group, with statistical difference(P<0.05).Conclusion The treatment of elderly hypertensive patients with anxiety and depression in patients with better antihypertensive effect of psychological intervention combined with Flupentixol and Melitracen Tablets, can improve the depression and anxiety of patients in a large extent, high safety, is further applied in clinical significance.
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OBJECTIVE:To optimize the extraction technology of Compound qima capsules. METHODS:With the blood pres-sure lowering of rats as index,pharmacological efficacy test was used to screen the preparation technology(A was whole herb de-coction;B was Gastrodia elata fine powder mixed with other decocted medical materials). The extraction technology was opti-mized by single factor and orthogonal test using the contents of astragaloside and isoflavone grape glycosides and the quality of sol-id as indexes,with added water,decoction time,decoction times as factors;and the verification test was carried out. RESULTS:Pharmacological efficacy test showed that antihypertensive effect of sample by technology B was superior. The optimal extraction condition of other medical materials of technology B was as follows as 12-fold water per time,decocting for 1.5 h,for 3 times. In verification test,average extraction rates of astragaloside and isoflavone grape glycosides were 64.02% and 51.97%,and average value of the quality of solid was 5.69 g(RSD≤1.92%,n=3). CONCLUSIONS:The optimized extraction technology is stable and feasible.
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Objective To study the antihypertensive effects and treatment compliance of extended release nifedipine tablets and nifedipine controlled release tablets .Methods 120 cases of patients with hypertension from April 2012 to April 2013,with informed consent of patients and in accordance with the medical ethics standard ,were divided into the group I and group II of 60 cases in each group according to the random number table method , the group I was given extended release nifedipine tablets for treatment while the group II was given nifedipine controlled release tablets for therapy ,antihypertensive effect ,treatment compliance and adverse reaction of two groups were com-pared.Results The total efficiency of group II was 93.3%,which was higher than 80.0%of the group I,there was statistically significant differences between the two groups (χ2 =12.019,P=0.019);The adverse reaction rate of group II was 8.3%,which was significantly lower than 18.3%of the group I,there was statistically significant differ-ences between the two groups (χ2 =11.271,P=0.021);The treatment compliance of group II was 96.7%,which of the group I was 95.0%,there was no significant differences between the two groups (χ2 =5.419,P =0.067). Conclusion Nifedipine controlled release tablets has a better antihypertensive effect ,with less adverse reaction when compared with nifedipine controlled release tablets .
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We purified a novel angiotensin-I converting enzyme (ACE) inhibitor from fish sauce <i>Ishiru</i> prepared from squid, and identified it as the tripeptide Leu-Ala-Arg (LAR). IC<sub>50</sub> of this ACE inhibitor was 2.5 μM, demonstrating high potency among peptides previously purified from fish sauces. Moreover, LAR acted as an antihypertensive peptide, reducing systolic blood pressure in spontaneously hypertensive rats.<br>
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The present study was designed to investigate the antihypertensive effect of methanolic extract of the whole plant of Passiflora nepalensis Walp., Passifloraceae, (MPN) in renal hypertensive and normotensive rats. The blood pressure, pulse pressure, and heart rate fell dose-dependently in renal hypertensive and normotensive rats after intravenous administration of 75, 150, and 225 mg/kg MPN, suggesting that MPN possesses antihypertensive, hypotensive and negative chronotropic effects. The effect at doses of 150 and 225 mg/kg of MPN were more pronounced than that of 75 mg/kg body weight. Thus, the present study reveals that MPN exerts antihypertensive effect against renal hypertension.
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OBJECTIVE:To study the antihypertensive effect of the alcohol soluble composition of Wudiangui.METHODS:The active component in Wudiangui was extracted with 90% alcohol at 40 ℃;with isolated aortic smooth muscle strip of rabbits as experimental material to observe the effects of the alcohol soluble composition of Wudiangui on the dose-response curves of norepinephrine(NE) and Potassium Chloride(KCl) as well as ?-and ? receptors.RESULTS:The alcohol soluble composition of Wudiangui has potent vasodilating effect on rabbits' aortic smooth muscles ex vivo.CONCLUSION:The aortic smooth muscle strips that had been contracted by NE and KCL can be relaxed by the alcohol soluble composition of Wudiangui through blocking calcium channel,and this effect is independent of the blockage of ?-and ? receptors.
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BACKGROUND: Fosinopril is a new phosphorous containing angiotensin converting enzyme inhibitor. To assess the antihypertensive efficacy and safety of fosinopril, the clinical trial was done in patients with mild to moderate hypertension. METHODS: In 30 patients with mild to moderate essential hypertension, we administered fosinopril 10-20mg once daily for 10 weeks and checked their blood pressure every 2 weeks. RESULTS: The blood pressure decreased from 158+/-12.3/103.4+/-4.2mmHg to 139+/-7.5/88.4+/-5.9mmHg at the end of treatment(p<0.05). Heart rate did not change significantly during therapeutic period. Of 30 patients, the efficacy of fosinopril therapy disclosed 25 patients(83.7%) with normal diastolic pressure of more than 10mmHg decline of diastolic blood pressure. But two patients had no effects and three patients were not followed up. The adverse reactions due to fosinopril were reported in 3 patients(10%) with dry cough, 2 patients with palpitation(6.7%) and 1 patient with weakness(3.3%), but there were no patients who discontinued fosinopril due to adverse effect. CONCLUSION: Fosinopril has an excellent antihypertensive effect at low dosage as a first line antihypertensive agent or as a substituting agent for other antihypertensives in patients with mild to moderate essential hypertension.
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Humans , Antihypertensive Agents , Blood Pressure , Cough , Fosinopril , Heart Rate , Hypertension , Peptidyl-Dipeptidase AABSTRACT
If hypertensive emergencies are left untreated, multiple damages on heart, brain and kindney can develop. So rapid control of blood pressure within safty with effective antihypertensive agents is mandatory. For the comparison of antihypertensive effects among hydralazine (IV or IM), clonidine (IV), and nifedipine (sublingual) in hypertensive emergency, which were frequently used in our hospital, we performed propective study with hypertensive emergency patients(243 cases) who visited emergency room from Oct. 1986 until Aug. 1987. The results are as follows ; 1) For 58 patients who recieved hydralazine (IV or IM), initial mean arterial blood pressure(MAP) was 167.2+/-21.5mmHg and 15 minutes later 138.9+/-24.4mmHg, 45 minutes later 141.7+/-21.1mmHg, 90 minutes later, 133.9+/-26.6mmHg and, respectively. For 55patients who recived clonidine(IV), initial MAP was 164+/-21.9mmHg and 15minytes later 137.4+/-18.9mmHg, 45 minutes later 127.5+/-34.9mmHg, respectively. For 130 patients who recived nifedipine(sublingual), initial MAP was 159.8+/-21.4mmHg and 15 minutes later 143.0+/-22.8mmHg, 45 minutes later 127.5+/-21.1mmHg, 90 minutes later 119.3+/-20.0mmHg, respectibely. 2) Pulse rate showed 12.9% increase afer administration of hydralazine, 15.8% decrease in clonidine, 5.6% increase in nifedipine, respectively. 3)Severe reduction of blood pressure(systolic BP<130mmHG) after administration of following antihypertensive agents was found. i.e., hydralazine 5.2%, clonidine 1.8%, nifedipine 1.5%, respectively. 4) In 4 cases(6.9%) out of the 58 cases using hydralazine, 3 cases(5.5%) out of the 55 cases using clonidine, 9 cases(6.9%) out of the 130 cases using nifedipine, acute paradoxic hyertensive effects were observed.
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Humans , Antihypertensive Agents , Blood Pressure , Brain , Clonidine , Emergencies , Emergency Service, Hospital , Heart , Heart Rate , Hydralazine , NifedipineABSTRACT
The antihypertensive effect of verapamil, a calcium channel blocker, was studied in 12 cases of essential hypertension (mean age 49, range 24-64). After 6 weeks administration (80-160mg t.i.d.), the following results were obtained : 1) Before medication, average systolic and diastolic blood pressure was 176.3/108.6mmHg. After completion of therapy, blood presure fell significantly down to 154.8/94.2mmHg (p<0.01). 2) Heart rate decreased slightly from average 74.3 per minute prior to medication to 69.3 per minute at the end of study (p<0.01). 3) Side effects, among which constipation was most common, were mild and did not compel any patient to diacontinue therapy. In conclusion, verapamil seems to be a safe and effective first-line drug for hypertension along with diuretics or beta blockers.
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Humans , Blood Pressure , Calcium Channels , Constipation , Diuretics , Heart Rate , Hypertension , VerapamilABSTRACT
The antihypertensive effect of Chinese celery decoction was studied using a renal-occlusive animal model. Sixteen male dogs were anaesthesized and operated. The left renal artery was then occluded. Three hours after the renovascular occlusion, eleven dogs were fed with distilled water in the same pattern. The intracarotid arterial pressure, electrocardiogram and urine output were continually recorded. Blood samples for plasma rennin activity (PRA) radio-immunoassay were collected before renovascular occlusion, just before feeding, and then two hours after feeding. In the experimental group, the systolic pressure (SP), diastolic pressure (DP), mean arterial pressure (MAP) and the PRA stepped up within three hours after renovascular occlusion. The celery feeding then brought the SP, DP, or MAP though the PRA came down slightly. In both groups, the urine volume decreased after renovascular occlusion then increased after feeding, but no statistically significant difference was found between the two groups. The study confirmed the antihypertensive effect of Chiness celery even in the renovascular hypertensive model. The celery decoction brought down the blood pressure without causing pronounced diuresis or any decrease in rennin activity.
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The blood pressure of conscious and anaesthetized animals feel significantly after iv IHC-64. IHC-64 acts rapidly but the time of acts was short. No acute tolerance was observed. After iv IHC-64 0. 5 and 1. 5 mg?kg-1 in anaesthetized dogs the blood pressure feel immediately, lasted for 12?5 min and 30 min . After iv IHC-64 0. 75,1. 5 and 3. 0 mg?kg-1in anaesthetized rabbits the blood pressure fell within 0. 5~ 1.0 min and the time of acts was re-spectively 10?5 min,12?7 min and 19?11 min . Antihypertensive effect of IHC-64 was more powerful than that of Clonidine and was similar to Sodium Notroprusside. The dosage of antihypertensive effect didn't affect the heart rate of conscious rabbits and anaesthetized dogs.