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Annals of Palliative Medicine Oct 2021Left ventricular (LV) hypertrophy predicts worse cardiac outcomes. Blood pressure lowering is associated with the reduction of LV hypertrophy. This study evaluated the... (Meta-Analysis)
Meta-Analysis
BACKGROUND
Left ventricular (LV) hypertrophy predicts worse cardiac outcomes. Blood pressure lowering is associated with the reduction of LV hypertrophy. This study evaluated the effect of a calcium channel blocker, amlodipine, on LV hypertrophy in patients with hypertension.
METHODS
Studies were identified by conducting a literature survey in electronic databases, and study selection was carried out according to precise eligibility criteria. Meta-analyses of mean change between the follow-up and baseline values of systolic/diastolic blood pressure (SBP/DBP) and LV hypertrophy indices were performed. Meta-regression analyses were performed to examine the factors affecting changes in these indices.
RESULTS
Twenty-three studies [involving 737 patients; age 56.4 years, 95% confidence interval (CI): 53.5-59.2; females 34%, 95% CI: 25-44%; body mass index 26.4 kg/m2, 95% CI: 24.6-28.1] were included. Amlodipine treatment led to a significant reduction in SBP (-24.9 mmHg; 95% CI: -28.3 to -21.6; P<0.0001) and DBP (-14.8; 95% CI: -16.4 to -13.3; P<0.0001), without affecting the heart rate. Amlodipine treatment also significantly reduced the LV mass index. The mean difference (MD) between the follow-up and baseline LV mass index was -12.9; 95% CI: -15.4 to -10.4 (P<0.001). This decrease in LV mass index was positively associated with the follow-up duration [meta-regression coefficient (MC): 0.392; 95% CI: 0.050-0.733; P=0.026] and baseline LV mass index (MC: 0.139; 95% CI: 0.007-0.271; P=0.040). Amlodipine treatment significantly reduced the LV posterior wall thickness, which was also positively associated with the follow-up duration. There was no significant decrease in the LV end-diastolic diameter following amlodipine treatment.
DISCUSSION
Amlodipine treatment in patients with hypertension significantly reduced the LV mass index and LV posterior wall thickness, without notably affecting the LV end-diastolic diameter. Since many of the included studies were non-randomized, open-label, or lacking appropriate comparability, we therefore performed pooled analyses of the changes from baseline, and a comparative account could not be carried out.
Topics: Amlodipine; Blood Pressure; Calcium Channel Blockers; Female; Humans; Hypertension; Hypertrophy, Left Ventricular; Middle Aged
PubMed: 34763438
DOI: 10.21037/apm-21-2455 -
Drugs of Today (Barcelona, Spain : 1998) Mar 2007This review describes the clinical profile and rationale for the development of a single-pill formulation of the calcium channel blocker amlodipine besylate, a... (Review)
Review
This review describes the clinical profile and rationale for the development of a single-pill formulation of the calcium channel blocker amlodipine besylate, a blood-pressure--lowering agent, and atorvastatin calcium, a statin with lipid-lowering antiatherosclerotic properties. Amlodipine and atorvastatin have been demonstrated in numerous clinical trials to be highly effective in lowering blood pressure and low-density lipoprotein cholesterol. Furthermore, both amlodipine and atorvastatin have been demonstrated to reduce cardiovascular events in a broad range of patients' in hypertensive patients with three concomitant cardiovascular risk factors but normal to mildly elevated cholesterol levels, amlodipine combined with atorvastatin demonstrated a reduction in cardiovascular events. The amlodipine/atorvastatin single pill has been shown to improve patients; achievement of national-guideline-recommended blood pressure and lipid target levels and exhibits a safety profile consistent with its parent compounds. The combination pill is now available in parts of Europe in formulations containing either 5 or 10 mg amlodipine and 10 mg atorvastatin. Amlodipine combined with atorvastatin has been demonstrated to reduce cardiovascular events in hypertensive patients at high cardiovascular risk, and the single-pill formulation has the potential to improve adherence and decrease prescription costs. These potential benefits are associated with important implications because hypertensive patients with additional risk factors represent a large proportion of those at risk for cardiovascular events.
Topics: Amlodipine; Antihypertensive Agents; Clinical Trials as Topic; Drug Combinations; Heptanoic Acids; Humans; Hypertension; Pyrroles
PubMed: 17380213
DOI: 10.1358/dot.2007.43.3.1079878 -
American Journal of Hypertension Jul 2020Hypertension is a common comorbidity associated with chronic kidney disease (CKD). Treatment in these patients often involves L-type Ca2+ channel (LTCC) blockers. The...
BACKGROUND
Hypertension is a common comorbidity associated with chronic kidney disease (CKD). Treatment in these patients often involves L-type Ca2+ channel (LTCC) blockers. The effect of chronic LTCC-blockade treatment on resistance vasculature was investigated in a genetic hypertensive rat model of CKD, the Lewis Polycystic Kidney (LPK) rat.
METHODS
Mixed-sex LPK and Lewis control rats (total n = 38) were allocated to treated (amlodipine 20 mg/kg/day p.o. from 4 to 18 weeks) and vehicle groups. Following systolic blood pressure and renal function assessment, animals were euthanized and mesenteric vasculature was collected for functional and structural assessment using pressure myography and histology.
RESULTS
Amlodipine treatment reduced LPK rat blood pressure (untreated vs. treated: 185 ± 5 vs. 165 ± 9 mm Hg; P = 0.019), reduced plasma creatinine (untreated vs. treated: 197 ± 17 vs. 140 ± 16 µmol/l; P = 0.002), and improved some vascular structural parameters (internal and external diameters and wall-lumen ratios); however wall thickness was still increased in LPK relative to Lewis despite treatment (Lewis vs. LPK: 31 ± 2 vs. 41 ± 2 µm, P = 0.047). Treatment improved LPK rats' endothelium dysfunction, and nitric oxide-dependent and endothelium-derived hyperpolarization vasorelaxation components, and downregulated prostanoid contributions. LTCC blockade had no effect on biomechanical properties of compliance and intrinsic stiffness, nor artery wall composition.
CONCLUSIONS
Our results indicate that blockade of LTCCs with amlodipine is effective in improving, to a certain extent, detrimental structural and functional vascular features of resistance arteries in CKD.
Topics: Amlodipine; Animals; Antihypertensive Agents; Drug Evaluation, Preclinical; Endothelium, Vascular; Female; Male; Rats, Inbred Lew; Vascular Remodeling; Vascular Stiffness
PubMed: 32215654
DOI: 10.1093/ajh/hpaa054 -
Headache Sep 1998Migraine is among the most common neurologic disorders encountered in clinical practice. In the general US population, the annual incidence has been calculated to be...
Migraine is among the most common neurologic disorders encountered in clinical practice. In the general US population, the annual incidence has been calculated to be approximately 250 per 100,000 with a point prevalence of 10%. Females are affected more than males. A variety of prophylactic and abortive medications are being used for treatment and several are being studied in clinical trials. Calcium-channel blockers are frequently used prophylactic medications. We report two patients with migraine successfully treated with amlodipine (Norvasc, Pfizer, Inc), a slow calcium-channel blocker. To our knowledge, these are the first reported cases of amlodipine used in migraine prophylaxis.
Topics: Adult; Amlodipine; Calcium Channel Blockers; Female; Humans; Male; Middle Aged; Migraine Disorders
PubMed: 11398308
DOI: 10.1046/j.1526-4610.1998.3808624.x -
Pharmaceutical Development and... 2004This article studies the compatibility of amlodipine besylate in its solid formulations with various drug excipients. The various factors affecting amlodipine besylate...
This article studies the compatibility of amlodipine besylate in its solid formulations with various drug excipients. The various factors affecting amlodipine besylate stability were studied using high-performance liquid chromatography (HPLC). It has been found that binary 1:1 mixtures of amlodipine besylate and an excipient are stable at 65 degrees C and 40 degrees C/75% RH. Further investigations were conducted to study the stability of amlodipine besylate in multicomponent mixtures, including mixtures with actual formulations. The study reveals that mixtures of lactose, magnesium stearate, and water induce some instability on amlodipine besylate. The major degradation product confirmed by HPLC-mass spectrometry is amlodipine besylate glycosyl. This is in conformity with the well-known Maillard reaction between primary amines and lactose. Thus, lactose-free amlodipine formulations are recommended from the safety, quality, efficacy, and process cost points of view.
Topics: Amlodipine; Dosage Forms; Drug Interactions; Drug Stability; Excipients
PubMed: 15000463
DOI: 10.1081/pdt-120027414 -
The Medico-legal Journal Sep 2023Incorrect dispensing of medications by community pharmacies can lead to accidental poisonings. This may not be considered by emergency medicine physicians in patients...
Incorrect dispensing of medications by community pharmacies can lead to accidental poisonings. This may not be considered by emergency medicine physicians in patients describing vague symptoms. We present a case of a paediatric ingestion of amlodipine, resulting from a community pharmacy dispensing error, that was recognized by the child's mother, and consider the liability implications.
Topics: Female; Humans; Child; Amlodipine; Pharmacies; Mothers; Pharmacy; Eating
PubMed: 35993220
DOI: 10.1177/00258172221116499 -
American Journal of Cardiovascular... Oct 2013This article discusses racial/ethnic disparities in hypertension, with particular focus on non-white populations including blacks, Hispanics/Latinos, and Asians.... (Review)
Review
This article discusses racial/ethnic disparities in hypertension, with particular focus on non-white populations including blacks, Hispanics/Latinos, and Asians. Hypertension and its related morbidity and mortality affect a disproportionate number of black patients compared with white patients. Blacks, Hispanics/Latinos, and Asians have poor rates of hypertension awareness, treatment, and control. Given the high prevalence of comorbidities (e.g., obesity, diabetes, and metabolic syndrome) in these populations, renin-angiotensin-aldosterone system blockers are a good choice for foundation therapy. This review also discusses the importance of adherence and persistence with antihypertensive medication, which remain suboptimal in these non-white populations. Evidence suggests improvement with the use of single-pill combination therapy. Lastly, clinical trial data on the antihypertensive efficacy and safety of the combination of a dihydropyridine calcium channel blocker and an angiotensin receptor blocker, a widely utilized combination, in non-white populations are presented. PubMed was searched using the title/abstract key words (amlodipine AND valsartan AND [hypertension OR hypertensive] AND [black(s) OR African American(s) OR Hispanic(s) OR Latino(s) OR Mexican(s) OR Asian(s)]). In total, eight studies in patients with stage 1 or 2 hypertension were identified (n = 1,111 black, n = 389 Hispanic/Latino, and n = 3,094 Asian). Results showed that treatment with the combination of amlodipine plus valsartan is a reasonable choice for initial therapy or in patients who fail to respond to monotherapy. These drug classes have complementary mechanisms of action and, when used concomitantly, the magnitude of blood pressure lowering in these non-white populations is generally comparable with that seen in non-Hispanic white patients.
Topics: Black or African American; Amlodipine; Amlodipine, Valsartan Drug Combination; Antihypertensive Agents; Asian People; Drug Combinations; Health Status Disparities; Hispanic or Latino; Humans; Hypertension; Medication Adherence; Tetrazoles; Treatment Outcome
PubMed: 23784267
DOI: 10.1007/s40256-013-0033-4 -
Molecules (Basel, Switzerland) May 2021Amlodipine, a unique long-lasting calcium channel antagonist and antihypertensive drug, has weak fluorescence in aqueous solutions. In the current paper, we show that...
Amlodipine, a unique long-lasting calcium channel antagonist and antihypertensive drug, has weak fluorescence in aqueous solutions. In the current paper, we show that direct visualization of amlodipine in live cells is possible due to the enhanced emission in cellular environment. We examined the impact of pH, polarity and viscosity of the environment as well as protein binding on the spectral properties of amlodipine in vitro, and used quantum chemical calculations for assessing the mechanism of fluorescence quenching in aqueous solutions. The confocal fluorescence microscopy shows that the drug readily penetrates the plasma membrane and accumulates in the intracellular vesicles. Visible emission and photostability of amlodipine allow confocal time-lapse imaging and the drug uptake monitoring.
Topics: Amlodipine; Cell Survival; HEK293 Cells; Humans; Indoles; Microscopy, Confocal; Microscopy, Fluorescence; Models, Biological; Molecular Conformation; Solutions
PubMed: 34070063
DOI: 10.3390/molecules26102997 -
Sudebno-meditsinskaia Ekspertiza 2019The purpose of the work is to determine the optimal conditions for isolating amlodipine, to purify it by the method of column chromatography and to develop a method for...
The purpose of the work is to determine the optimal conditions for isolating amlodipine, to purify it by the method of column chromatography and to develop a method for detecting it in biological material. TLC, GC-MS, low pressure column chromatography, and HPLC were used for analysis. We studied the comparative isolation of amlodipine from biological material using 13 isolating agents of organic nature, water, and aqueous solutions. The use of acetone as an insulating agent for the extraction of amlodipine from tissues of cadaver organs has been substantiated. The possibility of purification of the analyzed compound from the endogenous substances of the biomaterial is shown by the method of reversed phase chromatography in a column of the Silasorp S-18 sorbent of 30 μm. A technique has been developed for detecting amlodipine in the tissues of cadaveric organs (liver), which corresponds to the necessary parameters of linearity, selectivity, accuracy, precision and stability. The limits of detection and quantification of amlodipine by the proposed method are 0.25·10 and 4.0·10 g, respectively, in 1 g of the biomaterial.
Topics: Acetone; Amlodipine; Cadaver; Chromatography, High Pressure Liquid; Gas Chromatography-Mass Spectrometry; Humans; Reproducibility of Results
PubMed: 31407706
DOI: 10.17116/sudmed20196204147 -
Arteriosclerosis, Thrombosis, and... Dec 2003Calcium channel blockers (CCBs) were developed as vasodilators, and their use in cardiovascular disease treatment remains largely based on that mechanism of action. More... (Review)
Review
Calcium channel blockers (CCBs) were developed as vasodilators, and their use in cardiovascular disease treatment remains largely based on that mechanism of action. More recently, with the evolution of second- and third-generation CCBs, pleiotropic effects have been observed, and at least some of CCBs' benefit is attributable to these mechanisms. Understanding these effects has contributed greatly to elucidating disease mechanisms and the rationale for CCB use. Furthermore, this knowledge might clarify why drugs are useful in some disease states, such as atherosclerosis, but not in others, such as heart failure. Although numerous drugs used in the treatment of vascular disease, including statins and angiotensin-converting-enzyme inhibitors, have well-described pleiotropic effects universally accepted to contribute to their benefit, little attention has been paid to CCBs' potentially similar effects. Accumulating evidence that at least 1 CCB, amlodipine, has pharmacologic actions distinct from L-type calcium channel blockade prompted us to investigate the pleiotropic actions of amlodipine and CCBs in general. There are several areas of research; foci here are (1) the physicochemical properties of amlodipine and its interaction with cholesterol and oxidants; (2) the mechanism by which amlodipine regulates NO production and implications; and (3) amlodipine's role in controlling smooth muscle cell proliferation and matrix formation.
Topics: Amlodipine; Animals; Calcium Channel Blockers; Calcium Channels, L-Type; Cardiovascular Diseases; Cardiovascular Physiological Phenomena; Humans
PubMed: 14512371
DOI: 10.1161/01.ATV.0000097770.66965.2A