Antihypertensive Agents ; administration & dosage ; therapeutic use ; Humans ; Hypertension ; drug therapy ; genetics ; Molecular Biology

Adult ; Antihypertensive Agents ; administration & dosage ; therapeutic use ; Cardiomyopathy, Dilated ; diagnosis ; drug therapy ; Echocardiography ; Humans ; Male ; Valsartan ; administration & dosage ; therapeutic use

Classic formulae have a wide prospect in the treatment of hypertension with such advantages as symposium relief, improvement of body constitution and uncontrollable blood pressure factors. The paper systematically reviews the application of classic formula in pre-hypertension, different stages of hypertension, special type of hypertension, secondary hypertension, and uncontrollable blood pressure factors. It is believed that classic formulae are effective under the premise of their in-depth understanding of objective indications, modern pathogenesis and evolvement regularity.
Antihypertensive Agents ; administration & dosage ; Blood Pressure ; drug effects ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Hypertension ; drug therapy ; physiopathology

OBJECTIVETo evaluate the effects of amlodipine-based antihypertensive combination regimen on blood pressure control and impact on cardiovascular events.

METHODSFrom Oct. 2007 to Oct. 2008, a total of 13 542 hypertensive patients from 180 centers in China were included in this multi-centre randomized, controlled, blind-endpoint assessment clinical trial. Inclusion criteria were: essential hypertension, 50 - 79 years of age with at least one cardiovascular risk factor and signed consent forms. Patients were randomly assigned to receive low-dose amlodipine + diuretics (group A) or low-dose amlodipine + telmisartan (group T). The primary endpoints are composite of non-fatal stroke/myocardial infarction and cardiovascular death. All patients will be followed-up for 4 years.

RESULTSThe characteristics of patients between the two groups were similar: mean age (61.5 +/- 7.7) Yrs with 19% history of cerebrovascular diseases, 12% coronary diseases, 18% diabetes, 42% dyslipidemia, mean initial blood pressure 157/93 mm Hg. After 8-week treatment, mean blood pressure in group A and B were reduced to (133.0 +/- 11.0)/(81.0 +/- 7.6) mm Hg, (132.9 +/- 11.6)/(80.6 +/- 7.9) mm Hg respectively. Blood pressure control rates reached 72.1% and 72.6% in group A and T, respectively.

CONCLUSIONAmlodipine-based antihypertensive combination regimens achieved satisfactory blood pressure control rate in patients with essential hypertension in this patient cohort.

Aged ; Amlodipine ; administration & dosage ; Antihypertensive Agents ; administration & dosage ; Benzimidazoles ; administration & dosage ; Benzoates ; administration & dosage ; Blood Pressure ; Drug Therapy, Combination ; Female ; Humans ; Hypertension ; drug therapy ; physiopathology ; Male ; Middle Aged

AIMTo determine clonidine in rabbit plasma by LC-MS.

METHODSThe LC-MS system consisted of Waters Alliance 2790 HPLC and Micromass ZQ-4000 MS. The HPLC was performed by using XTerra C18 (150 mm x 2.1 mm ID, 5 microm). The mobile phase, consisting of acetonitrile/ammonium hydrogen carbonate solution, was maintained to a flow-rate of 0.2 mL x min(-1) and the linear gradient elution was adopted. Mass spectrum was obtained by using electrospray ionization interface and the m/z of SIM was 230.

RESULTSThe average recovery was high and the method was reproducible. The calibration curve showed good linearity in the range of 1 - 80 microg x L(-1), the lowest limit of detection was 0.05 microg x L(-1). The Cmax, AUC0-t, and Tmax value of the pharmacokinetics parameter were (27 +/- 9) microg x L(-1), (5,352 +/- 1,121) microg x L(-1), (79 +/- 17) h.

CONCLUSIONThe results demonstrated that the method had high sensitivity, good selectivity, accuracy and precision. It is used to determine the clonidine concentration in plasma. The transdermal patch can deliver clonidine to the surface of rabbit skin stably for periods of up to 1 week after a single application.

Administration, Cutaneous ; Animals ; Antihypertensive Agents ; administration & dosage ; blood ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; methods ; Clonidine ; administration & dosage ; blood ; pharmacokinetics ; Rabbits ; Spectrometry, Mass, Electrospray Ionization ; methods

Administration, Cutaneous ; Adolescent ; Antihypertensive Agents ; administration & dosage ; therapeutic use ; Child ; Clonidine ; administration & dosage ; therapeutic use ; Double-Blind Method ; Female ; Humans ; Male ; Tic Disorders ; drug therapy

OBJECTIVETo investigate the effect of oral bosentan in the treatment of congenital heart disease-associated pulmonary arterial hypertension.

METHODS24 patients with congenital heart disease-associated pulmonary arterial hypertension, including 4 receiving heart surgery and 20 with surgical contraindications, were enrolled in this study. All the patients were given oral bosentan and followed up regularly for analyzing the outcomes and side effects.

RESULTSOne patient was lost to follow up and one patient died. Systolic pulmonary artery pressure showed no significant changes at 2 (93.6 ± 17.2 mmHg) and 4 months (85.7 ± 25.5 mmHg) of bosentan treatment compared to that before the medication (97.8 ± 14.9 mmHg) (P=0.096), but decreased significantly after a 6-month therapy (80.9 ± 25.0 mmHg, P=0.029). The 6-minute walking distance increased significantly after a 2, 4, and 6-month therapy [(488 ± 98.8, 496.3 ± 89.0, and 491.3 ± 114.2 m, respectively; P=0.004, 0.003, and 0.004 vs the distance before medication (317.0 ± 134.1)]. The New York heart functional classification was improved significantly after a 2, 4, and 6-month therapy [(2.0 ± 0.5, 1.8 ± 0.4, and 1.7 ± 0.5, respectively; P<0.001 vs pre-medication score (2.9 ± 0.5)). Hepatic and renal function remained normal, and ALT and AST showed no significant variations during the medication (P>0.05).

CONCLUSIONOral bosentan can effectively relieve the symptoms, decrease pulmonary artery hypertension, and improve exercise tolerance and cardiac function classification in patients with pulmonary artery hypertension associated with congenital heart disease with good safety and mild side effects.

Administration, Oral ; Antihypertensive Agents ; therapeutic use ; Heart Defects, Congenital ; complications ; Humans ; Hypertension, Pulmonary ; drug therapy ; etiology ; Sulfonamides ; therapeutic use

European Medicines Agency withdrew valsartan from European market in July 2018 because it was contaminated with carcinogen, N-nitrosodimethylamine (NDMA) and N-nitrosodiethylamine (NDEA). Medicines and Healthcare Products Regulatory Agency also found the same contamination and withdrew it from England market. US Food and Drug Administration followed the action after confirming its contamination. Ministry of Food and Drug Safety (MFDS) conducted testing all the valsartans at Korean market and withdrew some of them from market after confirming the contamination with NDMA. MFDS provided the pharmaceutical companies and laboratory institutions with the manual for testing both NDMA and NDEA and educated relevant personnels. MFDS also evaluated the health impact of the contaminated valsartan on the hypertensive patients who took the valsartan, which was shown to be very low risk of additional cancer incidence. MFDS pronounced strengthening of the safety management for the raw materials of the medicines. For guaranteeing the safety of medicines, more comprehensive drug safety management system from developing new drugs to consuming the medicines should be established. For achieving such a goal, active participation of all the stakeholders of the medicines including governmental agencies including MFDS and Ministry of Health and Welfare, the National Assembly, healthcare professionals, pharmaceutical companies, mass media, and general population including patients should be needed.
Antihypertensive Agents ; Delivery of Health Care ; Diethylnitrosamine ; Dimethylnitrosamine ; England ; Humans ; Incidence ; Mass Media ; Safety Management ; United States Food and Drug Administration ; Valsartan

OBJECTIVETo investigate the chronic efficacy of low-dose hydrochlorothiazide (HCTZ) in patients with mild-to-moderate hypertension.

METHODSAfter a 2-weeks placebo run-in period, 232 patients with mild or moderate hypertension were recruited and received HCTZ (12.5 mg once daily) therapy for one year. Patient compliance and blood pressure were monitored and serum BUN, Cr, glucose, electrolytes, and lipids were measured before, 6 weeks and 1 year after treatment.

RESULTS(1) Reduction of SBP, DBP and MAP were more significantly at 1 year [(10.45 +/- 17.28) mm Hg, (8.45 +/- 11.06) mm Hg, (9.12 +/- 10.88) mm Hg] than that at 6 weeks post therapy [(6.01 +/- 16.05) mm Hg, (2.90 +/- 10.33) mm Hg, (3.94 +/- 10.68) mm Hg, all P < 0.05]. Blood pressure were reduced to normal in 35.1% patients at 1 year and in 20.3% patients at 6 weeks (P < 0.05). (2) No patient developed diabetes mellitus or hypokalemia during therapy while the serum uric acid at 1 year post therapy was significantly higher than that at before therapy (P < 0.05).

CONCLUSIONThe study indicates that low dose HCTZ is an effective and safe antihypertensive agent for patients with mild-to-moderate hypertension and uric acid changes during therapy need to be monitored.

Adult ; Aged ; Antihypertensive Agents ; administration & dosage ; Blood Pressure ; Female ; Humans ; Hydrochlorothiazide ; administration & dosage ; Hypertension ; drug therapy ; physiopathology ; Male ; Middle Aged ; Treatment Outcome

AIMTo investigate the preparation of pulsatile release tablets, the release of the drug in vitro and the pharmacokinetics in vivo.

METHODSDiltiazem hydrochloride (DIL) was used as model drug. The pulsatile release tablets were prepared by film-coated method using ethylcellulose and Eudragit L. The effect of formulation on pulsatile release of diltiazem hydrochloride was investigated under release rate test. The mechanism of pulsatile release of drug was proved by the test of water-uptake. The pharmacokinetic and bioavailability study in eight human subjects was performed by HPLC method.

RESULTSThe release of diltiazem hydrochloride effected by the formulation of the core tablets and the composition and thickness of the coating film. In vitro, the delayed-release time T10 was 4.4 h, the maximum release time Trm was 8.0 h and the pulsed-release time Trm-10 was 3.6 h. In vivo, the delayed-release time Tlag was 4.9 h, the peak time was 8.0 h and the pulsed-release time was 3.1 h. The relative bioavailability was 105%.

CONCLUSIONThe release of drug from pulsatile release tablets of diltiazem hydrochloride was shown to be in pulsed way both in vitro and in vivo.

Adult ; Antihypertensive Agents ; administration & dosage ; pharmacokinetics ; Biological Availability ; Chemistry, Pharmaceutical ; Delayed-Action Preparations ; Diltiazem ; administration & dosage ; pharmacokinetics ; Drug Delivery Systems ; Fluorocarbons ; chemistry ; Humans ; Male ; Polymethacrylic Acids ; chemistry