Controlled-release Nifedipine Research Articles

Comparison of Clinical Effects of Sacubitril Valsartan Sodium Tablets and Nifedipine Controlled-Release Tablets in the Treatment of Chronic Renal Insufficiency Complicated with Hypertension

Objective: To compare the clinical effects of using sacubitril valsartan sodium tablets with nifedipine controlled-release tablets in patients with chronic renal insufficiency combined with hypertension. Methods: 110 patients with chronic renal insufficiency combined with hypertension treated in our hospital from April 2023 to February 2024 were taken as the study subjects. They were divided into the test group (n = 55) and the comparison group (n = 55) by randomized numerical table method. The test group was provided with sacubitril valsartan sodium tablets and the comparison group was treated with nifedipine controlled-release tablets. The urine excretion rate of albumin and blood urea nitrogen levels as well as adverse effects were compared before and after treatment in both groups. Results: In the test group, the urinary albumin excretion rate was 101.77 ± 7.42 μg/min and the blood urea nitrogen level was 15.81 ± 1.76 mmol/L, which was much lower than that of the comparison group; the total rate of adverse reactions in the test group was 1.82%, which was significantly lower than that of the comparison group, the difference between the data of the test group and the comparison group after treatment is statistically significant (P < 0.05). Conclusion: By providing treatment with sacubitril valsartan sodium tablets for patients with chronic renal insufficiency combined with hypertension, their urinary albumin excretion rate and blood urea nitrogen level are significantly improved, and the total occurrence rate of adverse reactions is low.

Comparative Bioequivalence and Food Effect of Two Formulations of 30-mg Nifedipine Controlled-Release Tablets in Healthy Chinese Adults.

Nifedipine is a potent antihypertensive medication classified as a dihydropyridine calcium channel blocker. The objective of this trial was to assess the bioequivalence of a 30-mg nifedipine controlled-release tablet and a reference drug in a cohort of healthy Chinese individuals. Two independent open-label, randomized, single-dose, crossover studies were conducted, 1 under fasting conditions (N = 44, with 1 participant dropping out midway) and the other under fed conditions (N = 44, with 4 participants dropping out midway). Plasma concentrations of nifedipine were determined using liquid chromatography-mass spectrometry, and pharmacokinetic (PK) parameters were calculated using noncompartmental analysis with Phoenix WinNonlin 8.0 software. In both fasting and fed studies, reasonable bioequivalence was observed for the PK parameters of both the test product and the reference drug. A good safety profile was demonstrated for both the test product and reference drug, with no serious adverse events reported, and both were similarly well tolerated. An important observation with food coadministration was that systemic exposure to nifedipine (based on area under the curve, AUC0-∞) was reduced by approximately 12%. The bioequivalence of the test product and reference drug under fasting/fed conditions in healthy subjects in China was demonstrated by the study results.

Effects of intravenous nicardipine followed by oral labetalol in combination with nifedipine controlled-release tablet on severe peripartum hypertension

Effects of intravenous nicardipine followed by oral labetalol in combination with nifedipine controlled-release tablet on severe peripartum hypertension

Tongue Edema Caused by Taking Nifedipine Controlled-Release Tablets.

Tongue Edema Caused by Taking Nifedipine Controlled-Release Tablets.

Therapeutic improvements of nifedipine controlled-release tablets combined with sacubitril valsartan on patients with diabetic nephropathy complicated with hypertension

This study aimed to evaluate the efficacy of nifedipine controlled-release tablets combined with sacubitril valsartan in diabetic nephropathy (DN) patients with hypertension. One hundred and twelve DN patients with hypertension were enrolled. They were randomly divided into the control group (treated with nifedipine controlled-release tablets combined with valsartan) and the observation group (treated with nifedipine controlled-release tablets combined with sacubitril valsartan). Renal function, endothelial function and inflammatory response were examined. After three-months treatment, the levels of clinical indexes (glycosylated hemoglobin, fasting blood glucose, systolic and diastolic blood pressure), renal function indicators (urinary albumin excretion rate, blood urea nitrogen, serum creatinine and cystatin C), endothelial function indicators (microalbumin, angiotensin II, thrombomodulin and cartilage oligomeric matrix protein) and inflammatory response factors (interleukin-6 and tumor necrosis factor-α) in the observation group were significantly lower than those in the control group. Nifedipine controlled-release tablets combined with sacubitril valsartan could effectively alleviate the progression of DN combined with hypertension.

PS-BPR01-1: SUCCESSFUL TREATMENT WITH ESAXERENONE IN A PREGNANT WOMAN WITH PRIMARY ALDOSTERONISM AND SUPERIMPOSED PREECLAMPSIA

Background: During pregnancy, there is no established treatment for idiopathic hyperaldosteronism (IHA), the most common form of primary aldosteronism (PA) due to bilateral adrenal hyperplasia. Here, we report the case of a pregnant patient with IHA who was successfully treated with esaxerenone, a non-steroidal mineralocorticoid receptor (MR) antagonist. Case: A 39-year-old woman was referred to our outpatient clinic for hypertension with high plasma aldosterone concentration (PAC). Her PAC was 204 pg/mL (radioimmunoassay) and plasma renin activity was 1.2 ng/mL/h at the time of referral. She was diagnosed with PA since the saline-loading test for PA was positive. She had no hypokalemia and computed tomography scans showed no adrenal tumors. Adrenal vein sampling indicated overproduction of aldosterone in both adrenal glands leading to the diagnosis of IHA. She was commenced on nifedipine controlled release (CR) 20 mg daily because she desired to be pregnant. After one year, she became pregnant. Her blood pressure was well controlled until 34 weeks of gestation when her home blood pressure became elevated up to 140/90 mmHg. Although the dose of nifedipine CR was increased to 80 mg daily, her blood pressure increased to 151/97 mmHg and urinary test showed proteinuria of 2 + in 35 weeks of gestation. She was diagnosed with superimposed preeclampsia (SPE) and additionally treated with esaxerenone. Her blood pressure decreased to 120–140/98–100 mmHg and the proteinuria improved to +/-. A successful cesarean section at 37 weeks resulted in the delivery of a healthy baby boy. Esaxerenone was discontinued 2 weeks after delivery, because she was eager to breast-feed the baby and no safety data of esaxerenone in breast-feeding woman was available. Her blood pressure has been well controlled by nifedipine CR 80 mg daily even after 100 days of postpartum. Conclusions: This is the first case of a pregnant woman who was successfully treated with esaxerenone despite being an elderly pregnant woman who had been diagnosed with IHA and developed SPE. Further studies are needed to investigate the efficacy and safety of non-steroidal selective MR antagonist in similar pregnant patients with IHA, to establish better treatment strategy for these patients.

Analysis of Efficacy of Valsartan Combined with Nifedipine Controlled-release Tablets in the Treatment of Hypertension in Community

Analysis of Efficacy of Valsartan Combined with Nifedipine Controlled-release Tablets in the Treatment of Hypertension in Community

Analysis of the improvement of serological indexes in patients with diabetic nephropathy and hypertension using Valsartan combined with Nifedipine controlled-release regimen.

Objective:To investigate the effect of valsartan combined with nifedipine controlled-release Tablets on diabetic nephropathy (DN) patients with hypertension.Methods:The clinical records of 80 DN patients with hypertension registered in our hospital from April 2020 to April 2021 were collected. The records showed that 38 patients were treated with oral nifedipine controlled-release tablets (control group) and 42 - with oral valsartan combined with nifedipine controlled-release tablets (observation group). The improvement of serological indexes after treatment was compared and analyzed between the two groups.Results:After treatment, the levels of fasting blood glucose (FBG), systolic and diastolic blood pressure, bone oligomeric matrix protein (COMP), thrombin regulatory protein (TM) and Microalbumin (mALB) in the observation group were lower than those in the control group (P<0.05), while the level of angiopoietin-1 (Ang-1) was higher than those in the control group (P<0.05). After the treatment, the levels of homocysteine (Hcy), Cystatin C (CysC) and transforming growth factor β1(TGF-β1) in the observation group were lower than those in the control group (P<0.05). The levels of adiponectin (APN), aldosterone (ALD) and gastric growth promoting factor (ghrelin) in the observation group after the treatment were lower than those in the control group (P<0.05).Conclusions:A combination of valsartan and nifedipine controlled-release tablets in DN patients with hypertension can effectively control blood glucose and blood pressure, improve the serological indexes such as COMP, TM, mAlb, Ang-1, Hcy, CysC, TGF-β1, APN, ALD and ghrelin, and potentially reduce and delay renal function damage.

Curative effect of indapamide combined with amlodipine in the treatment of hypertension complicated with coronary heart disease

Objective To explore the clinical effect of indapamide combined with amlodipine in the treatment of hypertension complicated with coronary heart disease (CHD). Methods From January 2015 to January 2017, 62 hypertension patients complicated with CHD in the First People's Hospital of Daishan County were selected in the research.The patients were randomly divided into two groups according to the digital table, with 31 cases in each group.The observation group received indapamide combined with amlodipine therapy, and the control group received nifedipine controlled release tablets.The curative effect was compared between the two groups. Results After treatment, the treatment effective rate of the observation group was 93.55%, the incidence rate of adverse reactions of the observation group was 9.68%, which of the control group were 83.87%, 25.81%, respectively.The differences were significant in therapeutic effect, total cholesterol, angina frequency, triglycerides, systolic pressure, diastolic blood pressure between the two groups(χ2=8.226, t=8.226, 6.223, 7.112, 5.012, 5.348, all P<0.05). Conclusion Amlodipine in combination with indapamide in the treatment of hypertension complicated with CHD can reduce blood pressure, better auxiliary lower total cholesterol and triglyceride levels, avoid attack frequency of angina pectoris, and with no increase in adverse drug reactions, it has a certain clinical significance. Key words: High artery pressure; Coronary heart disease; Indapamide; Amlodipine

Clinical effect of combined controlled-release nifedipine tablets-valsartan therapy on elderly patients suffering from type II diabetic nephropathy with hypertension

Objective: This study aims to discuss the clinical effect of the combined therapy of nifedipine controlledrelease tablets-valsartan on elderly patients who have Type II Diabetic Nephropathy (T2DN) with Hypertension (HTN). Methods: We recruited 130 elderly patients who have T2DN with HTN and who were admitted to our hospital over the period of April, 2015 to February, 2017. We divided the patients into the control (n=65) and observation groups (n=65) through the odd-even method. The control group received controlledrelease nifedipine tablets and the observation group received controlled-release nifedipine tablets– valsartan. We compared the blood pressure level, total therapeutic efficiency, treatment satisfaction, and BUN level of the two groups. Results: The blood pressure level of the observation group significantly improved relative to that of the control group (P<0.05). The total therapeutic efficiency of the control group was 80.00%, which was significantly lower than that of the observation group (98.46%) (P<0.05). The treatment satisfaction of the observation group was 96.92%, which was significantly higher than that of the control group (75.38%) (P<0.05). The BUN level of the observation group was considerably higher than that of the control group (P<0.05). Conclusions: Elderly patients who received controlled-release nifedipine tablets-valsartan for the clinical treatment of T2DN with HTN exhibited significantly improved blood pressure level, total therapeutic efficiency, treatment satisfaction, and BUN levels. Therefore, the reasonable application of controlled-release nifedipine tablets-valsartan therapy can improve the life quality of elderly patients who have T2DN with HTN.

Comparison of ambulatory blood pressure-lowering effects of higher doses of different calcium antagonists in uncontrolled hypertension: the Calcium Antagonist Controlled-Release High-Dose Therapy in Uncontrolled Refractory Hypertensive Patients (CARILLON) Study

Background: Data are sparse regarding ambulatory blood pressure (BP) reduction of up-titration from a standard dose to a high dose in both nifedipine controlled-release (CR) and amlodipine. This was a prospective, randomized, multicenter, open-label trial.Patients and methods: Fifty-one uncontrolled hypertensives medicated by two or more antihypertensive drugs including a renin-angiotensin system inhibitor and a calcium antagonist were randomly assigned to either the nifedipine CR (80 mg)/candesartan (8 mg) group or the amlodipine (10 mg)/candesartan (8 mg) group.Results: The changes in 24-hr BP were comparable between the groups. The nifedipine group demonstrated a significant decrease in their urinary albumin creatinine ratio, whereas the amlodipine group demonstrated a significant decrease in their NTproBNP level. However, there was no significant difference in any biomarkers between the two groups.Conclusion: Nifedipine showed an almost equal effect on ambulatory blood pressure as amlodipine. Their potentially differential effects on renal protection and NTproBNP should be tested in larger samples.

P-015 - Formulation development of nifedipine controlled-release coated tablets

P-015 - Formulation development of nifedipine controlled-release coated tablets

Determination of nifedipine in dog plasma by high‐performance liquid chromatography with tandem mass spectrometric detection

Nifedipine is a dihydropyridine calcium channel blocker used widely in the management of hypertension and other cardiovascular disorders. In this work, a simple, rapid and sensitive liquid chromatography/tandem mass spectrometry method was developed and validated to determine nifedipine in dog plasma using nimodipine as the internal standard. Chromatographic separation was carried out on a C₈ column. The mobile phase consisted of a mixture of acetonitrile, water and formic acid (60:40:0.2, v/v/v) at a flow rate of 0.5 mL/min. Detection was performed on a triple quadrupole tandem mass spectrometer in selected reaction monitoring mode via an atmospheric pressure chemical ionization source. The method has a lower limit of quantification of 0.20 ng/mL with consumption of plasma as low as 0.05 mL. The linear calibration curves were obtained in the concentration range of 0.20-50.0 ng/mL (r = 0.9948). The recoveries of the liquid extraction method were 74.5-84.1%. Intra-day and inter-day precisions were 4.1-8.8 and 6.7-7.4%, respectively. The quantification was not interfered with by other plasma components and the method was applied to determine nifedipine in plasma after a single oral administration of two controlled-release nifedipine tablets to beagle dogs.

The ‘physical-mental’ treatment of cardiovascular disease co-morbid with mental disorders

A 47-year-old woman complained of sudden chest tightness, shortness of breath, palpitations and a severe headache. Her highest blood pressure had reached 200/120 mmHg before and was diagnosed as hypertension. One month ago, the results of her cranial CT scan showed multiple lacunar cerebral infarctions. She then complained of insomnia, extreme fatigue, poor appetite, loss of interest in everything and paid more attention to her blood pressure and measured blood pressure over five times per day at home. The patient went to visit a psychologist who drew the conclusion of depression. She took sertraline (50 mg once a day) and followed up with the psychologist in the following 2 weeks. During the last month, she has taken 30-mg nifedipine controlled-release tablets once a day and the blood pressure was well-controlled. More attention should be paid to the mental status of patients with cardiovascular disease. There are many screening tools to assess depression in cardiovascular disease patients. The ‘physical-mental’ treatment of cardiovascular disease cannot be conducted at one time and follow-ups are necessary.

Feasibility of Regression of Hypertension Using Contemporary Antihypertensive Agents

Recently, we reported that transient treatment of genetically hypertensive rats with high-dose angiotensin receptor blocker (ARB) causes regression of established hypertension. In this study, we investigated whether treatment with candesartan or nifedipine controlled-release (CR) resulted in a sustained regression of hypertension in humans. Patients aged 30 to 59 years with untreated stage 1 essential hypertension and a family history of hypertension were treated with the antihypertensive agents candesartan (n = 124) or nifedipine CR (n = 120). After 1 year of treatment (phase 1), the medications were tapered and discontinued (phase 2). During phase 2, home and office blood pressures were monitored for another year to assess posttreatment reoccurrence of stage 1 hypertension. In phase 1, after 1 year of treatment a similarly substantial BP decrease was seen in the candesartan (-24.5/16.1 mm Hg) and nifedipine (-26.8/18.0 mm Hg) groups. In phase 2 there was a substantial reoccurrence of hypertension; at the study end, only 1 patient was able to continue without antihypertensive medication. However, a Kaplan-Meier analysis revealed a significant delay of reoccurrence of hyper tension (P = 0.0001) in the candesartan group. One year of treatment with candesartan or nifedipine CR was not associated with marked regression of hypertension in humans at the standard doses used in this trial. However, withdrawal of candesartan was associated with a slightly longer delay before restarting medications. Further studies with larger doses of candesartan given over a longer time are required to determine whether such a regimen may induce sustainable and clinically relevant reversal of hypertension and alteration in its natural history.

Nifedipine controlled-release 40 mg b.i.d. in Japanese patients with essential hypertension who responded insufficiently to nifedipine controlled-release 40 mg q.d.: a phase III, randomized, double-blind and parallel-group study

This phase III, multicenter, randomized, double-blind, parallel-group study compared the efficacy and safety of nifedipine controlled-release (CR) 40 mg twice daily (b.i.d.) and once daily (q.d.) in 325 Japanese patients with essential hypertension uncontrolled with nifedipine CR 40 mg q.d. (ClinicalTrials.gov record: NCT01287260). The primary endpoint was the change from baseline in trough seated diastolic blood pressure (DBP) after 8 weeks. Nifedipine CR 40 mg b.i.d. showed significantly greater reductions in trough seated DBP (-7.7±0.6 mm Hg vs. -3.6±0.6 mm Hg) and trough seated systolic blood pressure (BP) (-11.1±0.9 mm Hg vs. -3.7±0.9 mm Hg) after 8 weeks of treatment compared with nifedipine CR 40 mg q.d. (both P<0.0001). At week 8, BP target achievement and responder rates were higher with nifedipine CR 40 mg b.i.d. (21.5% and 42.4% vs. 10.3% and 19.5%, respectively). Adverse events considered related to the study drug were reported in 9.0 and 9.7% of patients receiving nifedipine CR 40 mg b.i.d. and q.d., respectively. The frequency of drug-related adverse events commonly reported with nifedipine CR (headache, hot flush, palpitations, peripheral edema, hypotension, dizziness, tachycardia) was low and the results were similar between the treatment groups. In conclusion, a higher dose of nifedipine CR was associated with greater efficacy and a safety profile similar to that of the currently approved dose (40 mg q.d.) in Japanese patients with essential hypertension, and it may offer a valuable treatment choice for patients who do not achieve target BP levels with standard treatment.

Comparison of the effect of nifedipine controlled-release tablet and nifedipine sustained-release tablet in the treatment of hypertension

Objective To investigate the clinical efficacy of nifedipine sustained-release formulation(SR)and nifedipine controlled-release(GITS)in the treatment of essential hypertension.Methods 160 patients with essential hypertension were randomly divided into two groups.The SR group was treated with SR 20 mg twice a day;GITS group was treated with GITS 30 mg once a day.All patients were given ambulatory blood pressure monitoring(ABPM)and observed the 24-hour average blood pressure,heart rate,changes in the trough/peak(T/P)values,and adverse reactions before and after treatment in two groups.Results The T/P value of systolic blood pressure(SBP)and diastolic(DBP)in the GITS group was 68.5％,74.6％,respectively,which were higher than those of SR group(57.2％,61.1％)(x2=6.32,7.05,all P＜0.05);GITS group was significantly lower than the SR group in heart rate(t=4.17,P＜0.05);Adverse reactions between two groups had no significant difference(x2=0.16,P＞0.05).Conclusion SR and GITS can effectively lower blood pressure,but GITS is more efficient,stable,safe,small impact on the heart rate. Key words: Nifedipine; Formulations; Hypertension; Efficacy

Metabolic effect of combined telmisartan and nifedipine CR therapy in patients with essential hypertension

BackgroundIn addition to exerting a blood pressure (BP)-lowering effect, telmisartan produces favorable metabolic effects via peroxisome proliferator-activated receptor γ activation. While a combination of telmisartan and a calcium channel blocker is often used to achieve a target BP level, the metabolic effects of this drug combination remain unclear. Therefore, this study evaluated the metabolic effects of telmisartan plus nifedipine controlled release (CR) therapy, in hypertensive patients without metabolic disease.MethodsSixteen patients with essential hypertension, who had not undergone antihypertensive therapy in the previous 6 months, were studied. Patients were initiated on telmisartan (40 mg/day). If their office BP was not reduced to 140/90 mmHg after 6 weeks, nifedipine CR (20–40 mg per day) was added for 18 weeks. The other patients whose BP had achieved the target of 140/90 mmHg, continued only telmisartan.ResultsTelmisartan reduced BP (174 ± 13/92 ± 10 to 143 ± 22/78 ± 11 mmHg; P < 0.01) at 6 weeks in 16 patients, but eight patients did not achieve target BP levels and required addition of nifedipine. Telmisartan also resulted in a reduction in the homeostatic model assessment of insulin resistance (HOMA-IR) (1.30 ± 0.65 to 1.10 ± 0.42; P < 0.05) at 6 weeks, but did not affect adiponectin or leptin levels. Addition of nifedipine (n = 8) resulted in a reduction in BP (158 ± 18/80 ± 13 to 131 ± 8/73 ± 13 mmHg; P < 0.01) at 18 weeks, but did not affect the HOMA-IR (1.10 ± 0.40 to 1.02 ± 0.56; ns). In patients who did not require addition of nifedipine (n = 8), BP levels remained nearly identical at 18 weeks (127 ± 13/73 ± 9 to 128 ± 13/68 ± 8 mmHg; ns), and HOMA-IR also remained nearly identical.ConclusionsTelmisartan produced a favorable metabolic effect in hypertensive patients without preexisting metabolic disorders. Addition of nifedipine CR produced further BP-lowering effects, and resulted in maintenance of metabolic indices.

Comparison between Two Calcium Antagonists: Blood Pressure Reduction and Renal Effects in Hypertensive Patients with Type 2 Diabetes

Several types of Ca channel blockers (CCBs) which have unique organ protective effects are commercially available all over the world. However, the hypotensive and pleotropic effect in CCBs are not sufficiently assessed in the diabetic patient with refractory hypertension for angiotensin receptor blocker (ARB). We conducted a pilot study to compare the efficacy of two different CCBs (azelnidipine and nifedipine controlled release (CR)) in 55 hypertensive patients with type 2 diabetes who had not achieved their target blood pressure (BP) with ARB monotherapy. Patients were randomly assigned to receive azelnidipine (8–16 mg/day) or nifedipine CR (10–40 mg/day) concomitantly with valsartan (80 mg/day). There were no significant differences in baseline characteristics between the two groups. The final dose of azelnidipine and nifedipine CR was 13.3±3.9 and 17.1±9.4 mg/day, respectively. However the target BP (<130/80mmHg) achievement rate was higher in the earlier phase of the combination therapy with nifedipine CR than that of the azelnidipine group, the rates after 6 months were comparable between the groups (83 vs. 66%). The systolic blood pressure was significantly lower in the nifedipine CR group from 2 to 6 months after the combination therapy (P<0.05, respectively). Both groups showed no significant changes in blood glucose and hemoglobin A1c. There were no significant differences in the urinary albumin/creatinine ratio and estimated Glomerular Filtration Rate (eGFR). In conclusion, the adjunctive therapy of nifedipine CR was superior to that of azelnidipine for decreasing blood pressure and achieving the target blood pressure, especially in the earlier phase of the diabetic patient with refractory hypertension for ARB. However the nephroprotective effect of nifedipine CR combination therapy was comparable to that of azelnidipine. Keywords: Angiotensin-converting enzyme inhibitor, angiotensin receptor blocker, albumin creatinine ratio, calcium channel blocker, estimated Glomerular Filtration Rate, diabetes, Glucose metabolism, hypertension, Renal function

Effects of combination therapy with angiotensin II type I receptor blockers and calcium channel blockers on renal function in hypertensive patientsA retrospective, “real-world” comparative study

Combination therapies with angiotensin II type I receptor blockers (ARBs) and calcium channel blockers (CCBs) are frequently administered to hypertensive patients, because these regimens have renoprotective and antihypertensive effects. However, few studies have focused on the renoprotective effects of individual CCBs when combined with ARBs for hypertension. Two hundred eighty-six outpatients prescribed three different CCBs (benidipine [CAS 91599-74-5], amlodipine [CAS 111470-99-6] and controlled release nifedipine (nifedipine CR) [CAS 21829-25-4]) for hypertension in combination with ARBs during a 4-year period were registered in a retrospective comparative study. The factors that influenced the appearance of renal events defined as doubling of serum creatinine were investigated. The renal event rate was significantly lower in the benidipine than in the amlodipine (p < 0.05) and nifedipine CR (p < 0.01) groups. Multivariate analysis revealed hazard ratios for renal events to be significantly higher with chronic kidney disease (CKD) and lower with benidipine. Moreover, among patients with CKD, the benidipine group showed a significantly lower renal event rate than the amlodipine (p < 0.05) and nifedipine groups (p < 0.05). In hypertensive patients treated with ARB and CCB, benidipine exhibits a better renoprotective effect than other drugs of this class (amlodipine and nifedipine CR).