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American Journal of Cardiovascular... Apr 2013Combination therapy is often required in patients with hypertension, and fixed-dose single-pill combinations have been shown to provide an easier regimen for patients,... (Review)
Review
Combination therapy is often required in patients with hypertension, and fixed-dose single-pill combinations have been shown to provide an easier regimen for patients, improving adherence. Irbesartan/amlodipine (Aprovasc®) is an angiotensin-receptor blocker/calcium-channel blocker fixed-dose single-pill combination, whose constituent drugs exert additive effects when coadministered. In two randomized, open-label, multicentre, phase III trials, fixed-dose combination therapy with irbesartan/amlodipine was more effective than continuation of irbesartan or amlodipine monotherapy in patients with hypertension not adequately controlled with initial irbesartan or amlodipine monotherapy; there was a significantly greater decrease from baseline in mean seated home systolic blood pressure (primary endpoint) with the fixed-dose combination. The fixed-dose combination was also associated with a greater decrease in mean seated home diastolic blood pressure and mean seated office systolic and diastolic blood pressure than monotherapy. The fixed-dose combination of irbesartan/amlodipine was well tolerated in these patients; most treatment-emergent adverse events were of mild or moderate severity. The most frequent adverse event was peripheral oedema, generally associated with amlodipine treatment.
Topics: Adult; Amlodipine; Antihypertensive Agents; Biphenyl Compounds; Blood Pressure; Drug Therapy, Combination; Humans; Hypertension; Irbesartan; Tetrazoles; Treatment Outcome
PubMed: 23516133
DOI: 10.1007/s40256-013-0014-7 -
Journal of Avian Medicine and Surgery Jul 2021Amlodipine is a calcium channel blocker shown to be effective in lowering blood pressure with minimal adverse effects in mammals. To provide a retrospective evaluation...
Amlodipine is a calcium channel blocker shown to be effective in lowering blood pressure with minimal adverse effects in mammals. To provide a retrospective evaluation of amlodipine use in psittacine birds, medical records were reviewed for all avian patients prescribed amlodipine for treatment for the presumptive diagnosis of hypertension, based on clinical signs and indirect blood pressure measurements. Five birds were treated with amlodipine between 2010 and 2018. The median age was 33 years (range, 22-37 years) and 3/5 birds presented for ataxia or seizures. The median indirect systolic blood pressure at diagnosis was 243 mm Hg (range, 200-275 mm Hg). In 3/5 birds, amlodipine was the only drug prescribed, whereas, in 2/5 birds, enalapril was also prescribed in addition to amlodipine. In addition to the prescription of enalapril, blood pressure measurements were obtained indirectly, which are variables to be considered in this report. The initial median dose of amlodipine prescribed was 0.4 mg/kg (range, 0.1-0.4 mg/kg) PO q24h. In 3/5 birds, amlodipine administration was increased either in dose or frequency. Median follow-up time was 25 months (range, 2-55 months) after the initiation of amlodipine treatment. Owners in all 5 cases reported improvement of clinical signs by a median time of 2 months (range, 1-15 months). Three of 5 birds (60%) demonstrated a decreasing trend in blood pressure during the first 6 months after treatment with amlodipine was started (average, ≥20% decrease). Prospective, controlled studies are needed to investigate the efficacy of amlodipine in psittacine birds.
Topics: Amlodipine; Animals; Birds; Hypertension; Prospective Studies; Psittaciformes; Retrospective Studies
PubMed: 34256545
DOI: 10.1647/19-00016 -
Journal of Cardiovascular Pharmacology 1993Although it has long been recognized that many antihypertensive drugs exhibit large intersubject variability in their disposition characteristics, the concept that this... (Comparative Study)
Comparative Study Review
Although it has long been recognized that many antihypertensive drugs exhibit large intersubject variability in their disposition characteristics, the concept that this translates into a high variability in response has largely been ignored. Thus, too often in the past, research into antihypertensive drugs has ignored the importance of underlying plasma drug concentrations and has sought to attribute the variability in antihypertensive response to factors such as age and plasma renin activity. In studies with hypertensive patients in which pharmacokinetic and pharmacodynamic indices have been integrated, we have demonstrated that the intersubject variability in the pharmacokinetics of verapamil, nifedipine, enalapril, and amlodipine is directly related to the variability in blood pressure response at steady state. The characteristic low variability in the peak and predose, steady-state plasma concentrations associated with amlodipine are reflected in a correspondingly low variability in the blood pressure response. In addition, using the trough-to-peak, steady-state, blood pressure response as an index of 24-h duration of action, amlodipine exhibited significantly higher values with lower variability (66 +/- 11%) when compared to verapamil (47 +/- 13%), nifedipine (48 +/- 9%) and enalapril (44 +/- 15%). Concentration-effect analyses of all four drugs revealed that the antihypertensive response could be related to circulating drug concentrations and that the response following administration of the first dose correlated well with the response following long-term treatment.
Topics: Amlodipine; Antihypertensive Agents; Blood Pressure; Half-Life; Humans; Hypertension; Metabolic Clearance Rate
PubMed: 7522286
DOI: No ID Found -
Expert Opinion on Pharmacotherapy Jan 2001Myocardial infarction, stroke, heart failure and end-stage renal disease have all been linked to inadequate control of blood pressure. Despite overwhelming evidence that... (Comparative Study)
Comparative Study Review
Myocardial infarction, stroke, heart failure and end-stage renal disease have all been linked to inadequate control of blood pressure. Despite overwhelming evidence that uncontrolled hypertension is responsible for a sizeable number of adverse health-related outcomes, control of the disease remains considerably suboptimal. Available data demonstrate that in order to achieve adequate blood pressure control, a large number of patients require therapy with more than one medication. Fixed dose combination antihypertensive therapy has many advantages over other treatment options. Positive effects on blood pressure control, rates of adherence, adverse effects and cost have been identified. Amlodipine/benazepril (Lotrel), Novartis) is a fixed dose combination product indicated for the treatment of hypertension. Although not currently recommended as first-line therapy, studies confirm that this combination of a long-acting calcium antagonist and an angiotensin-converting enzyme (ACE) inhibitor possesses substantial blood pressure lowering capabilities. Whereas adverse events tend to become more frequent with increasing doses of antihypertensive monotherapy, the rate of adverse events attributed to amlodipine/benazepril in clinical trials often correlates with rates ascribed to placebo. Amlodipine/benazepril is capable of sustaining blood pressure control over a 24 h period and appears to be minimally affected by an occasional dose omission. Unlike the older calcium antagonists, amlodipine is unlikely to cause alterations in myocardial contractility. Additionally, the amlodipine/benazepril combination product costs less than the same therapy administered as the individual components. It is, therefore, reasonable to consider therapy with amlodipine/benazepril in appropriate patients after an adequate trial of antihypertensive monotherapy.
Topics: Amlodipine; Antihypertensive Agents; Benzazepines; Blood Pressure; Clinical Trials as Topic; Drug Combinations; Humans; Hypertension; Treatment Outcome
PubMed: 11336577
DOI: 10.1517/14656566.2.1.165 -
Journal of Clinical Periodontology Apr 1994Amlodipine is a calcium channel blocker used in the management of angina and hypertension. We report 3 cases of gingival overgrowth in adult dentate patients associated...
Amlodipine is a calcium channel blocker used in the management of angina and hypertension. We report 3 cases of gingival overgrowth in adult dentate patients associated with chronic usage of this drug. Gingival changes occurred within 3 months of dosage and appeared to be compounded by the patient's existing periodontal condition. In all 3 patients, there was sequestration of amlodipine in their crevicular fluid. The significance of this finding in relation to the pathogenesis of this unwanted effect remains to be elucidated.
Topics: Adult; Aged; Amlodipine; Collagen; Dental Plaque Index; Epithelium; Female; Fibroblasts; Gingival Crevicular Fluid; Gingival Hyperplasia; Humans; Male; Middle Aged; Periodontal Index; Periodontal Pocket
PubMed: 8195445
DOI: 10.1111/j.1600-051x.1994.tb00318.x -
The American Journal of Cardiology Jan 1994Amlodipine is an intrinsically long-acting, vasoselective calcium antagonist structurally related to nifedipine, but with unique binding and pharmacologic properties... (Review)
Review
Amlodipine is an intrinsically long-acting, vasoselective calcium antagonist structurally related to nifedipine, but with unique binding and pharmacologic properties that distinguish it from other agents of this class. Pharmacokinetic studies in animal models demonstrate a more prolonged half-life, high volume of distribution, and gradual elimination of amlodipine compared with that of other calcium antagonists. The presence of a basic side chain at the 2-position of the dihydropyridine ring renders the molecule > 90% ionized at physiologic pH and is believed to be primarily responsible for its markedly different pharmacologic and pharmacokinetic properties. Amlodipine has slow receptor binding kinetics that result in a gradual onset of action and may allow for less dependence on instantaneous plasma levels. Although amlodipine appears to bind to additional calcium channel recognition sites blocked by diltiazem and verapamil, it does not significantly depress heart rate nor does it produce significant negative inotropic effects or electrophysiologic disturbances. Preclinical studies indicate that amlodipine is a potent antihypertensive agent with natriuretic and diuretic properties that may enhance its ability to reduce blood pressure without attendant fluid retention.
Topics: Amlodipine; Animals; Aorta; Calcium Channel Blockers; Delayed-Action Preparations; Dogs; Hypertension; In Vitro Techniques; Kidney; Muscle Contraction; Myocardial Reperfusion Injury; Nifedipine; Portal Vein; Rats; Rats, Inbred SHR; Rats, Inbred WKY; Vascular Resistance
PubMed: 8310972
DOI: 10.1016/0002-9149(94)90268-2 -
Deutsche Medizinische Wochenschrift... Jan 1998
Topics: Amlodipine; Angina Pectoris; Antihypertensive Agents; Calcium Channel Blockers; Coronary Disease; Heart Failure; Humans; Hypertension; Vasodilator Agents
PubMed: 9465851
DOI: 10.1055/s-0029-1233207 -
Expert Review of Cardiovascular Therapy Jan 2011Hypertension is an increasingly prevalent cardiovascular risk factor associated with high rates of morbidity and mortality. Lowering blood pressure (BP) to recommended... (Review)
Review
Hypertension is an increasingly prevalent cardiovascular risk factor associated with high rates of morbidity and mortality. Lowering blood pressure (BP) to recommended levels reduces the risk of hypertension-associated cardiovascular events. Despite current treatment options and recommendations, the BP of many patients remains suboptimally controlled. There is a need for more effective management in patients not achieving BP goals on current monotherapy or combination therapy. Regimens combining three or more antihypertensive agents have been shown to increase the proportion of patients achieving BP goals. Recent data suggest that the combination of olmesartan medoxomil, amlodipine and hydrochlorothiazide is a rational treatment option offering safe and effective BP reductions and goal attainment in a greater proportion of patients compared with dual-combination regimens. As the understanding of the importance of BP control grows, treatment options that enable patients to achieve BP goals quickly and safely will become increasingly important in hypertension management.
Topics: Amlodipine; Antihypertensive Agents; Drug Combinations; Drug Therapy, Combination; Humans; Hydrochlorothiazide; Hypertension; Imidazoles; Olmesartan Medoxomil; Tetrazoles
PubMed: 21166525
DOI: 10.1586/erc.10.163 -
Canadian Family Physician Medecin de... Apr 2011
Topics: Adolescent; Amlodipine; Calcium Channel Blockers; Gingival Hypertrophy; Humans; Hypertension; Male
PubMed: 21490356
DOI: No ID Found -
Drugs Dec 2011Despite the well documented benefits conferred by adequate control of hypertension, the majority of hypertensive patients display suboptimal control and few patients... (Review)
Review
Despite the well documented benefits conferred by adequate control of hypertension, the majority of hypertensive patients display suboptimal control and few patients achieve blood pressure (BP) levels <140/90 mmHg. As a consequence, combination therapy will be required in the majority of patients to achieve target BP. Fixed-dose combinations of antihypertensives not only simplify treatment regimens, contributing to enhanced patient adherence, they provide superior BP-lowering efficacy and an improved tolerability profile. Fixed-dose combinations have become the strategy of choice in high-risk patients or those with stage 2-3 hypertension. The combination of a renin-angiotensin system inhibitor (RASI) with a calcium channel blocker (CCB) is a first-line combination that, in addition to its antihypertensive efficacy, reduces oedema, the main adverse effect of the dihydropyridine CCB and the main factor limiting their use. In morbidity/mortality studies, this fixed-dose combination has also demonstrated superiority over a RASI combined with a diuretic. The single-pill combination of telmisartan and amlodipine has been shown to produce a dose-dependent BP-lowering effect significantly greater than that of either agent administered as monotherapy. These findings have been confirmed by ambulatory BP monitoring in patients with stage 1 and 2 hypertension, which demonstrated that single-pill telmisartan/amlodipine provides substantial 24-hour BP-lowering efficacy. A higher proportion of patients achieved 24-hour BP goals of <130/80 mm Hg on combination therapy. The superior efficacy of combination therapy has been demonstrated across a broad range of patients, including those with moderate-to-severe hypertension, diabetes mellitus and obesity. Moreover, combined use of telmisartan and amlodipine reduces the incidence of amlodipine-induced oedema, making it a preferred combination for the treatment of hypertension.
Topics: Amlodipine; Antihypertensive Agents; Benzimidazoles; Benzoates; Clinical Trials as Topic; Drug Combinations; Humans; Hypertension; Telmisartan
PubMed: 22085386
DOI: 10.2165/11594510-000000000-00000