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Advances in Therapy Nov 2023Patients with hypertension and additional cardiovascular risk factors pose a challenge by requiring more intensive blood pressure (BP) control. Single-pill combination... (Observational Study)
Observational Study
Real-World Effectiveness and Safety of a Single-Pill Combination of Olmesartan/Amlodipine/Hydrochlorothiazide in Korean Patients with Hypertension and Cardiovascular Risk Factors.
INTRODUCTION
Patients with hypertension and additional cardiovascular risk factors pose a challenge by requiring more intensive blood pressure (BP) control. Single-pill combination (SPC) therapy can benefit these patients by improving medication adherence.
METHODS
This prospective, multicenter observational study assessed the real-world safety and effectiveness of an SPC containing olmesartan, amlodipine, and hydrochlorothiazide (O/A/H) in South Korean patients with hypertension and cardiovascular risk factors. BP control rates, defined as the percentage of patients achieving systolic BP (SBP) < 130 mmHg and diastolic BP (DBP) < 80 mmHg for intensive BP control, and < 140 mmHg and < 90 mmHg, respectively, for standard BP control, were investigated across various cardiovascular risk groups, along with changes in SBP and DBP from baseline to week 24.
RESULTS
The most prevalent cardiovascular risk factor was age (≥ 45 years in men, ≥ 55 years in women, 86.1%), followed by cardiovascular diseases (64.4%), dyslipidemia (53.7%), body mass index ≥ 25 kg/m (53.5%), and diabetes mellitus (DM) (46.3%). Switching to O/A/H showed significant BP reduction, with a mean change of - 17.8 mmHg/- 9.3 mmHg in SBP/DBP within 4 weeks. The intensive BP control rate was 41.4% (95% confidence interval [CI] 39.5, 43.4), and the standard BP control rate was 73.3% (95% CI 71.5, 75.1), with better control rates in the risk age group (43.1% and 74.1%, respectively) and cardiovascular disease group (42.0% and 73.8%, respectively). The DM group had relatively lower control rates (37.5% for intensive control and 69.4% for standard control). Common adverse drug reactions included dizziness (2.91%), hypotension (1.51%), and headaches (0.70%).
CONCLUSION
The SPC therapy of O/A/H caused a rapid and sustained reduction in SBP/DBP in patients' hypertension and additional cardiovascular risk factors. The therapy was safe and well tolerated.
STUDY REGISTRATION NUMBER
KCT0003401 ( https://cris.nih.go.kr/cris/search/detailSearch.do/20795 ).
Topics: Male; Humans; Female; Middle Aged; Amlodipine; Hydrochlorothiazide; Cardiovascular Diseases; Antihypertensive Agents; Olmesartan Medoxomil; Prospective Studies; Risk Factors; Hypertension; Tetrazoles; Blood Pressure; Heart Disease Risk Factors; Republic of Korea; Drug Combinations
PubMed: 37651078
DOI: 10.1007/s12325-023-02632-9 -
Nutrients Aug 2021Curcumin, a curcuminoid known as the main bioactive compound of turmeric, is used in foods, cosmetics, and pharmaceutical products. Amlodipine is a general...
Curcumin, a curcuminoid known as the main bioactive compound of turmeric, is used in foods, cosmetics, and pharmaceutical products. Amlodipine is a general antihypertensive drug used in combination with various other antihypertensive agents. To date, no studies have examined the effects of the co-administration of amlodipine with curcumin. In this study, the vasodilatory effects of curcumin, amlodipine, and the co-administration of curcumin with amlodipine on isolated rat aortic rings pre-contracted with phenylephrine were evaluated, and the hypotensive effects were evaluated using the tail cuff method. To measure blood pressure, male spontaneously hypertensive rats were divided into four groups, each containing six rats, as follows: amlodipine 1 mg/kg alone treated, amlodipine 1 mg/kg with curcumin 30 mg/kg treated, amlodipine 1 mg/kg with curcumin 100 mg/kg treated, and amlodipine 1 mg/kg with curcumin 300 mg/kg treated groups. Amlodipine and curcumin were intraperitoneally injected, and systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured at 1, 2, 4, and 8 h after administration. The combined administration of curcumin and amlodipine induced a stronger vasorelaxant effect than amlodipine alone. However, co-administration did not significantly lower SBP and DBP compared to the single administration of amlodipine. The results of this study suggest that hypertensive patients taking amlodipine can consume curcumin or turmeric for food or other medical purposes without inhibiting the blood pressure-lowering effect of amlodipine.
Topics: Amlodipine; Animals; Antihypertensive Agents; Blood Pressure; Curcumin; Drug Therapy, Combination; Hypertension; Male; Rats; Rats, Inbred SHR; Vasodilator Agents
PubMed: 34444956
DOI: 10.3390/nu13082797 -
Journal of Clinical Hypertension... Sep 2023The authors evaluated the efficacy, safety, and characteristics of patients who respond well to standard dose triple combination therapy including chlorthalidone 25 mg... (Randomized Controlled Trial)
Randomized Controlled Trial
Efficacy and safety of standard dose triple combination of telmisartan 80 mg/amlodipine 5 mg/chlorthalidone 25 mg in primary hypertension: A randomized, double-blind, active-controlled, multicenter phase 3 trial.
The authors evaluated the efficacy, safety, and characteristics of patients who respond well to standard dose triple combination therapy including chlorthalidone 25 mg with telmisartan 80 mg plus amlodipine 5 mg in hypertensive patients. This is a multicenter, double-blind, active-controlled, phase 3, randomized trial. Patients are randomized to triple combination (telmisartan 40 mg/amlodipine 5 mg/chlorthalidone 12.5 mg, TEL/AML/CHTD group) or dual combination (telmisartan 40 mg/amlodipine 5 mg, TEL/AML group) treatment and then dose up titration to TEL 80/AML5/CHTD25mg and TEL80/AML5, respectively. The primary endpoint is the change of mean sitting systolic blood pressure (MSSBP) at week 8. A Target BP achievement rate, a response rate, and the safety endpoints are also evaluated. Total 374 patients (mean age = 60.9 ± 10.7 years, male = 78.3%) were randomized to the study. The baseline MSSBPs/diastolic BPs were 149.9 ± 12.2/88.5 ± 10.4 mm Hg. After 8 weeks treatment, the change of MSSBPs at week 8 are -19.1 ± 14.9 mm Hg (TEL/AML/CHTD) and -11.4 ± 14.7 mm Hg (TEL/AML) (p < .0001). The achievement rates of target BP (53.8% vs. 37.8%, p = .0017) and responder rate (54.8% vs. 35.6%, p = .0001) at week 8 were significantly higher in TEL/AML/CHTD. There are no serious adverse event and no one discontinued medication due to adverse event. Among the TEL 80/AML5/CHTD25mg treatment group, patients of female or age ≥ 65 years old showed higher rate of target BP achievement than relatively young male. (61.4 vs. 46.8%, p = .042) Our study showed standard dose triple combination of telmisartan 80 mg/amlodipine 5 mg/chlorthalidone 25 mg is efficacious and safe in treatment of primary hypertension. Target BP achievement with triple therapy would be facilitated in female or old age.
Topics: Humans; Female; Male; Middle Aged; Aged; Telmisartan; Chlorthalidone; Amlodipine; Hypertension; Essential Hypertension; Leukemia, Myeloid, Acute
PubMed: 37614053
DOI: 10.1111/jch.14707 -
Nutrients Sep 2022High fructose intake has been implicated in obesity and metabolic syndrome, which are related to increased cardiovascular mortality. However, few studies have...
High fructose intake has been implicated in obesity and metabolic syndrome, which are related to increased cardiovascular mortality. However, few studies have experimentally examined the role of renin-angiotensin system blockers and calcium channel blockers (CCB) in obesity. We investigated the effects of valsartan (an angiotensin II receptor blocker) and amlodipine (a CCB) on lipolysis through the potential mechanism of PU.1 inhibition. We observed that high fructose concentrations significantly increased adipose size and triglyceride, monoacylglycerol lipase, adipose triglyceride lipase, and stearoyl-CoA desaturase-1 (SCD1), activating transcription factor 3 and PU.1 levels in adipocytes in vitro. Subsequently, PU.1 inhibitor treatment was able to reduce triglyceride, SCD1, and PU.1 levels. In addition, elevated levels of triglyceride and PU.1, stimulated by a high fructose concentration, decreased with valsartan and amlodipine treatment. Overall, these findings suggest that high fructose concentrations cause triacylglycerol storage in adipocytes through PU.1-mediated activation. Furthermore, valsartan and amlodipine treatment reduced triacylglycerol storage in adipocytes by inhibiting PU.1 activation in high fructose concentrations in vitro. Thus, the benefits of valsartan and amlodipine in lipolysis may be through PU.1 inhibition in fructose-induced adiposity, and PU.1 inhibition might have a potential therapeutic role in lipolysis in fructose-induced obesity.
Topics: Activating Transcription Factor 3; Adiposity; Amlodipine; Angiotensin Receptor Antagonists; Antihypertensive Agents; Blood Pressure; Calcium Channel Blockers; Fructose; Humans; Hypertension; Lipase; Lipolysis; Monoacylglycerol Lipases; Obesity; Stearoyl-CoA Desaturase; Tetrazoles; Triglycerides; Valsartan
PubMed: 36145135
DOI: 10.3390/nu14183759 -
Journal of Veterinary Internal Medicine May 2022Activity of the circulating renin-angiotensin-aldosterone system (RAAS) has not been comprehensively characterized in cats with systemic hypertension (SH) or...
BACKGROUND
Activity of the circulating renin-angiotensin-aldosterone system (RAAS) has not been comprehensively characterized in cats with systemic hypertension (SH) or cardiomyopathy (CM), and the effects of furosemide or amlodipine treatment on the RAAS have not been fully evaluated in cats.
HYPOTHESIS/OBJECTIVES
To document RAAS activity in cats with SH or CM compared to healthy cats and determine how RAAS profiles change with furosemide or amlodipine treatment.
ANIMALS
Sixty-six client-owned cats: 15 with SH (7 amlodipine-treated, 8 untreated), 17 with advanced CM (7 furosemide-treated, 10 not furosemide-treated), and 34 healthy cats.
METHODS
Equilibrium concentrations of RAAS peptides and aldosterone were quantified in serum samples by liquid chromatography-mass spectrometry. Variables were compared between groups using Kruskal-Wallis analysis with post hoc Holms-corrected Dunn's testing.
RESULTS
Compared with healthy cats, cats with CM had higher concentrations of angiotensin I, aldosterone, and plasma renin activity (all P < .01), and these differences remained significant (P < .03) after considering subgroups of untreated or furosemide-treated cats. Compared with healthy cats, untreated cats with SH showed no differences in RAAS biomarkers, whereas amlodipine-treated cats had higher concentrations of angiotensins I, II, III, IV, and 1-7, aldosterone, and plasma renin activity (all P < .03). Multivariable analysis determined that furosemide and amlodipine treatments were independent predictors of increased RAAS biomarker concentrations.
CONCLUSIONS AND CLINICAL IMPORTANCE
Cats with CM had increased RAAS activity, whereas cats with untreated SH did not. Furosemide and amlodipine both led to nonspecific activation of both classical and alternative RAAS pathways in cats.
Topics: Aldosterone; Amlodipine; Animals; Biomarkers; Cardiomyopathies; Cat Diseases; Cats; Furosemide; Hypertension; Renin; Renin-Angiotensin System
PubMed: 35285549
DOI: 10.1111/jvim.16401 -
The Journal of Pharmacy and Pharmacology Aug 2021To study the effect of Zingiber officinale and Hibiscus sabdariffa on pharmacokinetics and pharmacodynamics of amlodipine.
OBJECTIVES
To study the effect of Zingiber officinale and Hibiscus sabdariffa on pharmacokinetics and pharmacodynamics of amlodipine.
METHODS
Hypertension was induced in rats (SBP 173.2 ± 1.7 mmHg, mean, 1-24 h). Systolic blood pressure (SBP), diastolic blood pressure (DBP), mean blood pressure (MBP) and heart rate (HR) of group-I (amlodipine treated), group-II (Z. officinale, and Z. officinale + amlodipine) and group-III (H. sabdariffa, and H. sabdariffa + amlodipine) animals were measured by "tail-cuff system". Pharmacokinetics of amlodipine with and without herbs (Z. officinale or H. sabdariffa) was also investigated.
RESULTS
Z. officinale as well as H. sabdariffa decreased the SBP, DBP and MBP. Concurrent treatment with Z. officinale + amlodipine (SBP 129.4 ± 4.5) or H. sabdariffa + amlodipine (SBP 130.4 ± 3.9) showed higher decrease in BP (mean, 1-24h), than individually administered amlodipine (SBP 149.5 ± 2.4) or Z. officinale (SBP 150.2 ± 3.1) or H. sabdariffa (SBP 139.1 ± 1.2). These herbs also influenced the Cmax, AUC0-t, and Tmax of amlodipine. H. sabdariffa increased AUC0-t of amlodipine from 81.8 ± 14.7 to 125.0 ± 10.6 (ng h/mL).
CONCLUSION
Simultaneous administration of Z. officinale or H. sabdariffa with amlodipine, improves its pharmacodynamic response.
Topics: Amlodipine; Animals; Antihypertensive Agents; Area Under Curve; Blood Pressure; Drug Therapy, Combination; Zingiber officinale; Heart Rate; Herb-Drug Interactions; Hibiscus; Hypertension; Male; Phytotherapy; Plant Extracts; Rats, Wistar; Rats
PubMed: 34383955
DOI: 10.1093/jpp/rgaa062 -
Current Medical Research and Opinion Jul 2022Hypertension is a major cause of morbidity and mortality worldwide. Although current drug therapies can be effective, management of hypertension is closely linked to... (Review)
Review
OBJECTIVES
Hypertension is a major cause of morbidity and mortality worldwide. Although current drug therapies can be effective, management of hypertension is closely linked to patient adherence to therapy. A fixed-dose combination (FDC) of bisoprolol and amlodipine has shown to be effective and convenient, and to significantly improve patient adherence.
METHODS
This narrative review evaluates recent evidence from four studies which explore the efficacy, safety, and adherence of FDC bisoprolol and amlodipine in patients with hypertension: one observational study; two randomized clinical trials (RCTs); and one indirect comparison analysis.
RESULTS
All four studies support the efficacy of FDC bisoprolol and amlodipine in the management of hypertension, highlighting clinically meaningful reductions in systolic and diastolic blood pressure (BP), and high adherence. In a large cohort study exploring FDC bisoprolol and amlodipine in daily practice, high adherence improved BP and heart rate control versus baseline. In a Phase 3 RCT, FDC bisoprolol and amlodipine demonstrated superiority over monotherapies in BP control and a positive tolerability profile, further supporting its use to manage hypertension in second line following monotherapy. In another Phase 3 RCT, the combination of bisoprolol and amlodipine led to significant BP reductions versus monotherapy with amlodipine with a comparable safety profile. Finally, in the indirect treatment comparison, a low dose combination of bisoprolol and amlodipine showed a similar decrease in systolic BP compared with a maximum dose of amlodipine.
CONCLUSIONS
This review adds to growing evidence supporting the efficacy, safety, and tolerability of FDC bisoprolol and amlodipine in managing hypertension.
Topics: Amlodipine; Antihypertensive Agents; Bisoprolol; Blood Pressure; Drug Combinations; Humans; Hypertension; Observational Studies as Topic; Randomized Controlled Trials as Topic; Treatment Outcome
PubMed: 35510372
DOI: 10.1080/03007995.2022.2072087 -
Recent Advances in Anti-infective Drug... 2023Considering the role of calcium in the replication and morphogenesis of rotaviruses, it is hypothesized that decreased cytosolic calcium levels by using calcium channel...
BACKGROUND
Considering the role of calcium in the replication and morphogenesis of rotaviruses, it is hypothesized that decreased cytosolic calcium levels by using calcium channel blockers can subsequently interfere with rotavirus replication.
OBJECTIVE
The present study investigated the effects of two calcium ion channel blockers, amlodipine and diltiazem, against human rotavirus infection.
METHODS
Cytotoxic effects of the drugs on MA-104 cells were evaluated using the neutral red assay. The effects of amlodipine and diltiazem at non-toxic concentrations on human rotavirus were examined using cytopathic effect inhibition, TCID, and real-time PCR assays.
RESULTS
The highest inhibitory effect was obtained at concentrations of 0.5 μg/ml of amlodipine and 3 μg/ml of diltiazem, leading to 4.6 and 5.5 logarithmic reductions in infectious rotavirus titer and four- and a five-fold increase in the C values compared to the virus control, respectively (-value < 0.001). Conversely, infectious rotavirus titers were significantly elevated compared to the virus control at concentrations above 0.9 μg/ml of amlodipine and above 25 μg/ml of diltiazem.
CONCLUSION
Our study suggests that in addition to cardiovascular diseases, calcium channel blockers at their optimal doses may also be used to treat gastroenteritis caused by rotavirus infection.
Topics: Humans; Diltiazem; Calcium Channel Blockers; Amlodipine; Rotavirus; Rotavirus Infections
PubMed: 36345239
DOI: 10.2174/2772434418666221107105624 -
The Science of the Total Environment Aug 2022Wastewater treatment plants (WWTPs) are the important source of microplastics (MPs) in the environment, and disinfection processes bear high potential to degrade MPs....
Wastewater treatment plants (WWTPs) are the important source of microplastics (MPs) in the environment, and disinfection processes bear high potential to degrade MPs. This study investigated the physicochemical degradation, dissolved organic products and interaction with co-existed pollutants (heavy metal and pharmaceutical) on polyethylene (PE), polypropylene (PP) and polystyrene (PS) MPs during simulated disinfection processes. Compared to photo or chlorination, photochlorination significantly resulted in the physicochemical degradation, including morphology alteration, fragmentation, and chemical oxidation on PP and PS MPs, but showed relatively low effect on PE, indicating the different resistance among polymers to disinfected treatment. Photochlorination also caused the formation of chain-scission organic compounds and even chlorinated products from MPs (e.g. CHOCl for PP and monochlorophenol, dichlorophenol, chloroacetophenone and chlorobenzoic acid for PS), which may form disinfection byproducts to induce healthy risk. The adsorption potentials of MPs for Cr(VI) or amlodipine were enhanced by photochlorination since the cracking and formed oxygen functional groups enhanced the pore filling and surface precipitation of Cr(VI), and the electrostatic attraction and hydrogen bonding with amlodipine. The findings indicated the physicochemical degradation of MPs and the combined pollution with co-existed pollutants, highlighting the health risks of MP-derived organic products during the disinfection treatments (even in normal dosage) in WWTPs.
Topics: Adsorption; Amlodipine; Chromium; Microplastics; Plastics; Polystyrenes; Water Pollutants, Chemical
PubMed: 35472361
DOI: 10.1016/j.scitotenv.2022.155499 -
Journal of Periodontal Research Oct 2020Amlodipine, a calcium channel blocker derivative, is frequently used by patients with high blood pressure. Studies reported that it can induce gingival overgrowth....
BACKGROUND AND OBJECTIVES
Amlodipine, a calcium channel blocker derivative, is frequently used by patients with high blood pressure. Studies reported that it can induce gingival overgrowth. However, the underlying mechanism is not fully described yet. Interleukin-17A (IL-17A) is known as a proinflammatory cytokine, but current studies indicate that it has a role in fibrotic disorders and epithelial-mesenchymal transition (EMT). The aim of this study was to figure out the possible role of IL-17A in amlodipine-induced gingival overgrowth.
MATERIALS AND METHODS
Twenty-nine (29) individuals participated in the study, and they were assigned into 3 groups based on medical status and clinical periodontal examination; 9 patients with amlodipine-induced gingival overgrowth, 11 patients with inflammatory gingival overgrowth, and 9 healthy individuals as a control group. Clinical periodontal parameters including plaque index (PI), gingival index (GI), and gingival overgrowth index (GOI) were recorded. Blood and gingival crevicular fluid (GCF) samples were obtained. Gingival tissues were taken by appropriate periodontal surgery following initial periodontal therapy. To detect IL-17A on tissue samples, immunohistochemistry (IHC) was performed. Quantitative analysis was done, and the expression level of IL-17A was given as the percent positively stained cells. Enzyme-linked immunosorbent assay (ELISA) kits were used to analyze IL-17A in serum and GCF samples.
RESULTS
All recorded clinical parameters were significantly higher in gingival overgrowth groups compared with control. Evaluation of inflammation on tissue sections did not show any significant change within the groups. Immunohistochemistry findings showed that IL-17A expression was increased in amlodipine samples (81.90%) compared with control samples (42.35%) (P < .001). There was an increase in the inflammatory group (66.08%) which is significantly less than the amlodipine group (P < .05). IL-17A levels in serum and GCF samples were not different within the study groups.
CONCLUSION
In this study, elevated IL-17A expression regardless of inflammation shows that amlodipine might cause an increase of IL-17A in gingival tissues. This increase might induce fibrotic changes and EMT in gingival overgrowth tissues. The association of IL-17A with fibrosis and EMT in gingival tissues requires further investigation.
Topics: Amlodipine; Antihypertensive Agents; Dental Plaque Index; Gingival Crevicular Fluid; Gingival Overgrowth; Humans; Interleukin-17
PubMed: 32173874
DOI: 10.1111/jre.12747