Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.Antihypertensive Agents: Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.Dihydropyridines: Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.TetrazolesHydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.Azetidinecarboxylic Acid: A proline analog that acts as a stoichiometric replacement of proline. It causes the production of abnormal proteins with impaired biological activity.Hypertension: Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.Drug Therapy, Combination: Therapy with two or more separate preparations given for a combined effect.Angiotensin II Type 1 Receptor Blockers: Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS.Mibefradil: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Angiotensin-Converting Enzyme Inhibitors: A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility.Cross-Over Studies: Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed)

Effects of amlodipine on sympathetic nerve traffic and baroreflex control of circulation in heart failure. (1/462)

Short-acting calcium antagonists exert a sympathoexcitation that in heart failure further enhances an already elevated sympathetic activity. Whether this is also the case for long-acting formulations is not yet established, despite the prognostic importance of sympathetic activation in heart failure. It is also undetermined whether in this condition long-acting calcium antagonists favorably affect a mechanism potentially responsible for the sympathetic activation, ie, the baroreflex impairment. In 28 heart failure patients (NYHA functional class II) under conventional treatment we measured plasma norepinephrine and efferent postganglionic muscle sympathetic nerve activity (microneurography) at rest and during arterial baroreceptor stimulation and deactivation induced by stepwise intravenous infusions of phenylephrine and nitroprusside, respectively. Measurements were performed at baseline and after 8 weeks of daily oral amlodipine administration (10 mg/d, 14 patients) or before and after an 8-week period without calcium antagonist administration (14 patients). Amlodipine caused a small and insignificant blood pressure reduction. Heart rate, left ventricular ejection fraction, and plasma renin and aldosterone concentrations were not affected. This was the case also for plasma norepinephrine (from 2.43+/-0.41 to 2.50+/-0.34 nmol/L, mean+/-SEM), muscle sympathetic nerve activity (from 54.4+/-5.9 to 51.0+/-4.3 bursts/min), and arterial baroreflex responses. No change in the above-mentioned variables was seen in the control group. Thus, in mild heart failure amlodipine treatment does not adversely affect sympathetic activity and baroreflex control of the heart and sympathetic tone. This implies that in this condition long-acting calcium antagonists can be administered without untoward neurohumoral effects anytime conventional treatment needs to be complemented by drugs causing additional vasodilatation.  (+info)

Irbesartan reduces QT dispersion in hypertensive individuals. (2/462)

Angiotensin type 1 receptor antagonists have direct effects on the autonomic nervous system and myocardium. Because of this, we hypothesized that irbesartan would reduce QT dispersion to a greater degree than amlodipine, a highly selective vasodilator. To test this, we gathered electrocardiographic (ECG) data from a multinational, multicenter, randomized, double-blind parallel group study that compared the antihypertensive efficacy of irbesartan and amlodipine in elderly subjects with mild to moderate hypertension. Subjects were treated for 6 months with either drug. Hydrochlorothiazide and atenolol were added after 12 weeks if blood pressure (BP) remained uncontrolled. ECGs were obtained before randomization and at 6 months. A total of 188 subjects (118 with baseline ECGs) were randomized. We analyzed 104 subjects who had complete ECGs at baseline and after 6 months of treatment. Baseline characteristics between treatments were similar, apart from a slight imbalance in diastolic BP (irbesartan [n=53] versus amlodipine [n=51], 99.2 [SD 3. 6] versus 100.8 [3.8] mm Hg; P=0.03). There were no significant differences in BP normalization (diastolic BP <90 mm Hg) between treatments at 6 months (irbesartan versus amlodipine, 80% versus 88%; P=0.378). We found a significant reduction in QT indexes in the irbesartan group (QTc dispersion mean, -11.4 [34.5] milliseconds, P=0.02; QTc max, -12.8 [35.5] milliseconds, P=0.01), and QTc dispersion did not correlate with the change in BP. The reduction in QT indexes with amlodipine (QTc dispersion, -9.7 [35.4] milliseconds, P=0.06; QTc max, -8.6 [33.2] milliseconds, P=0.07) did not quite reach statistical significance, but there was a correlation between the change in QT indexes and changes in systolic BP. In conclusion, irbesartan improved QT dispersion, and this effect may be important in preventing sudden cardiac death in at-risk hypertensive subjects.  (+info)

Low-dose combination therapy as first-line hypertension treatment for blacks and nonblacks. (3/462)

To assess the efficacy and safety of bisoprolol/6.25-mg hydrochlorothiazide (HCTZ), amlodipine, and enalapril in black and nonblack patients, data from two comparative studies were pooled and subgroup analyses performed. Both studies had similar designs and included all three active treatments. The second study also included a placebo group. Subjects (n = 541) with a sitting diastolic blood pressure of 95-114 mmHg were titrated to achieve a diastolic blood pressure < or = 90 mmHg. The studies included 114 blacks and 427 nonblacks. Results of an intention-to-treat analysis of mean change from baseline after 12 weeks of treatment showed the following: 1) blood pressure was significantly lowered by all three active drugs compared with baseline or placebo; 2) in blacks, bisoprolol/6.25-mg HCTZ resulted in significantly greater reductions of systolic and diastolic blood pressure than enalapril or placebo, but was not significantly different from amlodipine; 3) in nonblacks, bisoprolol/6.25-mg HCTZ resulted in significantly greater reduction of diastolic blood pressure than amlodipine, enalapril, or placebo. The placebo-corrected change in blood pressure was greater for blacks than whites on the bisoprolol/6.25-mg HCTZ combination, but this was not statistically significant. Bisoprolol/6.25-mg HCTZ controlled diastolic blood pressure to < or = 90 mmHg in significantly more patients than enalapril or placebo in blacks and nonblacks. The difference in control rates was not significant versus amlodipine. The incidence of drug-related adverse events was similar between treatments; however, bisoprolol/6.25-mg HCTZ had a lower discontinuation rate due to lack of blood pressure control or adverse experiences in both blacks and nonblacks.  (+info)

Renal effects of amlodipine in normotensive renal transplant recipients. (4/462)

Renal effects of amlodipine in normotensive renal transplant recipients. The use of cyclosporin A (CsA) has improved the success of renal transplantation, but is associated with hypertension and significant renal toxicity. Previous reports suggest that calcium channel blockers may be useful in opposing the adverse effects of CsA. We have evaluated the effects of amlodipine (5 mg, once daily for 8 weeks) on renal function in 27 normotensive renal transplant recipients with stable renal function, in a double-blind, placebo-controlled, multicentre, cross over study. Amlodipine significantly reduced serum creatinine concentration relative to placebo (mean+/-SD: 168+/-65 vs 177+/-66 micromol/l; P=0.002) and there was a strong trend towards an increase in effective renal plasma flow on amlodipine relative to placebo (238+/-92 vs 217+/-87 ml/min; P=0.055). Glomerular filtration rate and lithium clearance were unaffected. Trough CsA blood concentration was unaffected. Amlodipine was well tolerated, with a low incidence of adverse events, and did not affect blood pressure or heart rate. In conclusion, amlodipine reduced serum creatinine in normotensive renal transplant recipients after only 8 weeks treatment, and was well tolerated in concomitant administration with CsA.  (+info)

Beneficial effect of myocardial angiogenesis on cardiac remodeling process by amlodipine and MCI-154. (5/462)

The present study examined the effect of long-term treatment with amlodipine and MCI-154 (a Ca2+ sensitizer) on progressive cardiac dysfunction and microvasculature in the dilated cardiomyopathic (DCM) hamster heart. After treatment of DCM hamsters (Bio 53.58) with amlodipine or MCI-154 for 15 wk from the age of 5 wk, amlodipine and MCI-154 were found to cause an increase in left ventricular percent fractional shortening and decreases in left ventricular diastolic dimension and isovolumic relaxation time in echocardiograms (P < 0.01). A hemodynamic study showed that the diastolic time constant decreased in the amlodipine-treatment group (P < 0.05). In a morphometric study employing a double-staining method that discriminated arteriolar and venular capillaries, amlodipine and MCI-154 caused increases in total capillary density (P < 0.05) and the proportion of venular capillaries (P < 0.05). Moreover, Northern blot analysis showed that the expression of mRNA for vascular endothelial growth factor was significantly increased by amlodipine and MCI-154. They preserve coronary microvasculature in the DCM hamster and might induce angiogenesis of small vessels, thereby contributing to preservation of cardiac systolic and diastolic function.  (+info)

Increased NADH-oxidase-mediated superoxide production in the early stages of atherosclerosis: evidence for involvement of the renin-angiotensin system. (6/462)

BACKGROUND: Angiotensin II activates NAD(P)H-dependent oxidases via AT1-receptor stimulation, the most important vascular source of superoxide (O2*-). The AT1 receptor is upregulated in vitro by low-density lipoprotein. The present study was designed to test whether hypercholesterolemia is associated with increased NAD(P)H-dependent vascular O2*- production and whether AT1-receptor blockade may inhibit this oxidase and in parallel improve endothelial dysfunction. METHODS AND RESULTS: Vascular responses were determined by isometric tension studies, and relative rates of vascular O2*- production were determined by use of chemiluminescence with lucigenin, a cypridina luciferin analogue, and electron spin resonance studies. AT1-receptor mRNA was quantified by Northern analysis, and AT1-receptor density was measured by radioligand binding assays. Hypercholesterolemia was associated with impaired endothelium-dependent vasodilation and increased O2*- production in intact vessels. In vessel homogenates, we found a significant activation of NADH-driven O2*- production in both models of hyperlipidemia. Treatment of cholesterol-fed animals with the AT1-receptor antagonist Bay 10-6734 improved endothelial dysfunction, normalized vascular O2*- and NADH-oxidase activity, decreased macrophage infiltration, and reduced early plaque formation. In the setting of hypercholesterolemia, the aortic AT1 receptor mRNA was upregulated to 166+/-11%, accompanied by a comparable increase in AT1-receptor density. CONCLUSIONS: Hypercholesterolemia is associated with AT1-receptor upregulation, endothelial dysfunction, and increased NADH-dependent vascular O2*- production. The improvement of endothelial dysfunction, inhibition of the oxidase, and reduction of early plaque formation by an AT1-receptor antagonist suggests a crucial role of angiotensin II-mediated O2*- production in the early stage of atherosclerosis.  (+info)

Reduction of sympathetic hyperactivity by enalapril in patients with chronic renal failure. (7/462)

BACKGROUND: Inhibition of angiotensin-converting enzyme (ACE) reduces the risk of cardiovascular problems in patients with chronic renal failure. This effect may be due in part to a decrease in sympathetic nervous activity, but no direct evidence of such an action is available. METHODS: We studied muscle sympathetic-nerve activity in 14 patients with hypertension, chronic renal failure, and increased plasma renin activity before, during, and after administration of the ACE inhibitor enalapril. Ten other patients with similar clinical characteristics were studied before and during treatment with the calcium-channel blocker amlodipine. Normal subjects matched for age and weight were included in both studies. RESULTS: At base line, mean (+/-SD) muscle sympathetic-nerve activity was higher in the group of patients who received enalapril than in the control subjects (35+/-17 vs. 19+/-9 bursts per minute, P=0.004). The baroreflex curve, which reflects changes in muscle sympathetic-nerve activity caused by manipulations of blood pressure with sodium nitroprusside and phenylephrine, was shifted to the right in the patients, but baroreflex sensitivity was similar to that in the control subjects (-2.1+/-1.9 and -2.7+/-1.3 bursts per minute per mm Hg, respectively; P=0.36). A single dose of the sympatholytic drug clonidine caused a greater fall in blood pressure in the patients than in the control subjects. Treatment with enalapril normalized blood pressure and muscle sympathetic-nerve activity (at 23+/-10 bursts per minute) in the patients and shifted the baroreflex curve to the left, reflecting normal blood-pressure levels, without significantly changing sensitivity (-2.3+/-1.8 bursts per minute per mm Hg, P=0.96). In the patients who received amlodipine, treatment also lowered blood pressure but increased muscle sympathetic-nerve activity, from 41+/-19 to 56+/-14 bursts per minute (P=0.02). CONCLUSIONS: Increased sympathetic activity contributes to hypertension in patients with chronic renal disease. ACE inhibition controls hypertension and decreases sympathetic hyperactivity.  (+info)

Combination of calcium channel blockers and beta-adrenoceptor blockers for patients with exercise-induced angina pectoris: a double-blind parallel-group comparison of different classes of calcium channel blockers. Netherlands Working Group on Cardiovascular Research (WCN). (8/462)

AIMS: The combination of calcium channel blockers and beta-adrenoceptor blockers is more effective for the treatment of exercise-induced angina pectoris than beta-adrenoceptor blocker monotherapy. As ischaemia in exercise-induced angina is preceded by increase in heart rate, calcium channel blockers with negative chronotropic properties may perform better for this purpose than nonchronotropic compounds. METHODS: A 335 patient double-blind parallel-group study comparing 14 day treatment with amlodipine 5 and 10 mg, with diltiazem 200 and 300 mg, and mibefradil 50 and 100 mg added to baseline beta-adrenoceptor blocker treatment was performed. Exercise testing (ETT) was performed by bicycle ergometry. RESULTS: Although none of the calcium channel blockers improved duration of exercise or amount of workload, all significantly delayed onset of 1 mm ST-segment depression on ETT (P<0.001 for any treatment vs baseline). In addition, mibefradil, both low and high dose treatment, produced the longest delays (low dose: different from diltiazem and amlodipine by 24.1 and 29.8 s, respectively, P<0. 003 and <0.001; high dose: different from diltiazem and amlodipine by 33.7 and 37.0 s, respectively, P<0.001 and <0.001). These effects were linearly correlated with the reduction in rate pressure product (RPP). Serious symptoms of dizziness occurred significantly more frequently on mibefradil (P<0.05), and 19 patients on mibefradil withdrew from trial. CONCLUSIONS: Calcium channel blockers with negative chronotropic properties provide greater delay of ischaemia in patients with exercise-induced angina, but the concomitant risk of intolerable dizziness attenuates this benefit.  (+info)

*Candesartan

"Comparative effect of candesartan and amlodipine, and effect of switching from valsartan, losartan, telmisartan and olmesartan ... Candesartan showed significantly early morning Blood Pressure decreased over amlodipine, and also to ARBs, valsartan, losartan ...

*Cilnidipine

Peripheral edema, a common side effect from the use of amlodipine, was reduced when patients were shifted to cilnidipine. ... "Excellent Tolerance to Cilnidipine in Hypertensives with Amlodipine - Induced Edema". North American Journal of Medical ...

*Amlodipine

... can be given as a combination therapy with a variety of medications: Amlodipine/atorvastatin, where amlodipine is ... Amlodipine/perindopril if using amlodipine alone caused edema. Perindopril is a long-lasting ACE inhibitor. Amlodipine/ ... Amlodipine/aliskiren or amlodipine/aliskiren/hydrochlorothiazide if amlodipine alone cannot reduce blood pressure. Aliskiren is ... Amlodipine/olmesartan or amlodipine/olmesartan/hydrochlorothiazide if amlodipine is insufficient in reducing blood pressure. ...

*Amlodipine/benazepril

Amlodipine Benazepril Faulkner, Michele A; Hilleman, Daniel E (2005). "Amlodipine/benazepril: fixed dose combination therapy ... Amlodipine/benazepril, marketed in the U.S. as Lotrel by Novartis and manufactured as a generic drug by Teva and Sandoz, is an ... antihypertensive medication which combines a calcium channel blocker (amlodipine besilate) with an angiotensin converting ...

*Aliskiren/amlodipine

... aliskiren 300 mg/amlodipine 10 mg) being more effective than olmesartan/amlodipine with comparable tolerability. Pfeiffer, ... "Efficacy and Tolerability of Aliskiren/Amlodipine Single-Pill Combinations in Patients who did not Respond Fully to Amlodipine ... Clinical trials have shown it to be more effective than amlodipine on its own, with a high dosing regime ( ... The drug combination aliskiren/amlodipine (INNs, trade name Tekamlo) is an antihypertensive. ...

*Atorvastatin/amlodipine

"CADUET (amlodipine besylate/atorvastatin calcium) Tablets" (PDF). NDA 21-540/S-009. United States Food and Drug Administration ... The drug combination atorvastatin/amlodipine (trade names Caduet in the US, Australia and Russia, and Envacar elsewhere) is a ... It is a fixed-dose combination drug containing the calcium channel blocker amlodipine and the statin atorvastatin being ...

*Aliskiren/amlodipine/hydrochlorothiazide

The drug combination aliskiren/amlodipine/hydrochlorothiazide (INNs, trade name Amturnide) is an antihypertensive approved by ...

*DMOZ - Health: Pharmacy: Drugs and Medications: A: Amlodipine

Amlodipine is a calcium channel blocker used in the treatment of hypertension. ... Amlodipine is a calcium channel blocker used in the treatment of hypertension. ...

*Medochemie

"Amlodipine Medochemie". Drugs.com. 2013. Retrieved 2013-08-04. "Medochemie Cyprus exports reach €100 mln". FinancialMirror.com ...

*Valsartan

Amlodipine and valsartan are combination drugs for hypertension. The combination is not approved for use by anyone younger than ... "amlodipine and valsartan". Retrieved September 2, 2016. Valsartan National Library of Medicine: Drug Information Portal. ... In one study of people without diabetes, valsartan reduced the risk of developing diabetes mellitus over amlodipine, mainly for ... "Progressive effects of valsartan compared with amlodipine in prevention of diabetes according to categories of diabetogenic ...

*Dysgeusia

In a second case, a fifty-nine-year-old man was prescribed amlodipine in order to treat his hypertension. After eight years of ... When he ran out of his medication, he decided not to obtain a refill and stopped taking amlodipine. Following this self-removal ... Once he refilled his prescription and began taking amlodipine a second time, his taste disturbance reoccurred. These two cases ... There are few case reports claiming calcium channel blockers like Amlodipine also cause dysguesia by blocking calcium sensitive ...

*Pfizer

... amlodipine), an antihypertensive drug of the dihydropyridine calcium channel blocker class. Amlodipine is on the World Health ... Caduet (amlodipine/atorvastatin) for cholesterol and hypertension. Camptosar (irinotecan) for cancer and Chemotherapeutic ...

*Felodipine

... amlodipine 5, and verapamil 0.2. Felodipine is a member of the 1,4-dihydropyridine class of calcium channel blockers. It is a ...

*Drug-related gingival hyperplasia

Srivastava, AmitKumar; Kundu, Debabrata; Bandyopadhyay, Prasanta; Pal, AsitKumar (2010). "Management of amlodipine-induced ...

*Lercanidipine

By comparison, amlodipine has a lower potential for CYP3A4 mediated interactions. Lercanidipine increases plasma levels of ... but switching from amlodipine, felodipine or nitrendipine (all at least second generation) to lercanidipine significantly ... "Lack of effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of amlodipine". British Journal of Clinical ...

*Peripheral edema

Some medicines (e.g. amlodipine, pregabalin) may also cause or worsen the condition. Successful treatment depends on control of ...

*Simvastatin

High doses of simvastatin are also contraindicated with the widely used antihypertensive amlodipine. A lower dose is also ... amlodipine, and ranolazine. All statins act by inhibiting 3-hydroxy-3-methylglutaryl (HMG) coenzyme A reductase. HMG-CoA ...

*Olmesartan

Teva Pharmaceuticals produces a formulation containing olmesartan, amlodipine, and hydrochlorothiazide for once daily use. ...

*P-type calcium channel

Some of these calcium antagonists include verapamil, diltiazem, amlodipine, benidipine, cilnidipine, nicardipine, and ...

*Feline hyperaldosteronism

Specific therapy for treating high blood pressure (e.g., amlodipine), should be added if necessary. Most affected cats are over ...

*Levamlodipine

... also known as levoamlodipine or S-amlodipine is a pharmacologically active enantiomer of amlodipine. Amlodipine belongs to the ... "Clinical Trial of S-Amlodipine 2.5 mg versus Amlodipine 5 mg in the Treatment of Hypertension". Indian Journal of Clinical ... Pathak L, Hiremath, Kerkar PG, Manade VG (March 2004). "Multicentric, clinical trial of S-Amlodipine 2.5 mg versus Amlodipine 5 ... Comparative Clinical Trial of S-Amlodipine 2.5 mg vs Amlodipine 5 mg in the Treatment of mild to moderate Hypertension". JAMA- ...

*Alkem Laboratories

In 2007 the company filed its first ANDA for drug Amlodipine which was approved in 2009. Alkem has developed a portfolio of 705 ...

*Efonidipine

These incremental microcirculatory benefits of efonidipine over the conventional L-type Ca2+ channel blockers (Amlodipine) are ... One common adverse effect of the L-type Ca2+ channel blockers like Amlodipine is vasodilatory Pedal edema. Combined L-/T-type ... Ca2+ channel blockers, such as Efonidipine, display antihypertensive efficacy similar to their predecessors (Amlodipine) with ...

*Combination drug

... atorvastatin/amlodipine) or Exforge (amlodipine/valsartan). In cases of FDCs targeting multiple conditions, such conditions ...

*Gynecomastia

Medications that are probably associated with gynecomastia include calcium channel blockers such as verapamil, amlodipine, and ...
Cadila Pharmaceuticals is a one of the foremost pharma companies in synthesizing APIs. We are bulk drug manufacturer of Amlodipine Besylate. The CAS number of Amlodipine Besylate is 88150-42-9.. Amlodipine is used to treat high blood pressure. Lowering high blood pressure helps to prevent heart attack, strokes and kidney problems. Amlodipine Besylate is a calcium channel blocker drug. It relaxes blood vessels so blood can flow easily. It is also used to prevent certain types of chest pain.. Cadila Pharmaceuticals Limited is one of the top USFDA approved pharmaceutical companies based in India. It is respected as a best Active Pharmaceutical Ingredients (APIs) manufacturing company in India. One of our core expertises is to synthesize APIs of the highest quality at inexpensive price.. We are major Amlodipine Besylate manufacturer and supplier. We export Amlodipine Besylate to Asian countries like; Japan, China, Georgia, Singapore, Malaysia, Vietnam, South Korea etc., and Middle East countries ...
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After oral administration of therapeutic doses of amlodipine besylate tablets, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability has been estimated to be between 64 and 90%. The bioavailability of amlodipine besylate tablets is not altered by the presence of food.. Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. Elimination from the plasma is biphasic with a terminal elimination half-life of about 30 to 50 hours. Steady-state plasma levels of amlodipine are reached after 7 to 8 days of consecutive daily dosing.. The pharmacokinetics of amlodipine are not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose.. Elderly patients and ...
The combination of benazepril plus amlodipine was shown to be more effective than benazepril plus hydrochlorothiazide in reducing cardiovascular events in the Avoiding Cardiovascular Events through Combination Therapy in Patients Living with Systolic Hypertension (ACCOMPLISH) trial. There was a small difference in clinic systolic blood pressure between the treatment arms favoring benazepril plus amlodipine. Ambulatory blood pressure monitoring provides a more rigorous estimate of blood pressure effects. A subset of 573 subjects underwent ambulatory blood pressure monitoring during year 2. Readings were obtained every 20 minutes during a 24-hour period. Between-treatment differences (benazepril plus amlodipine versus benazepril plus hydrochlorothiazide) in mean values were analyzed using ANOVA. Treatment comparisons with respect to categorical variables were made using Pearsons χ2. At year 2, the treatment groups did not differ significantly in 24-hour mean daytime or nighttime blood pressures ...
Amlodipine. No evidence of teratogenicity or other embryo/fetal toxicity was found when pregnant rats and rabbits were treated orally with amlodipine maleate at doses of up to 10 mg amlodipine/kg/day (respectively about 10 and 20 times the maximum recommended human dose of 10 mg amlodipine on a mg/m2 basis) during their respective periods of major organogenesis. (Calculations based on a patient weight of 60 kg). However, litter size was significantly decreased (by about 50%) and the number of intrauterine deaths was significantly increased (about 5-fold) in rats receiving amlodipine maleate at a dose equivalent to 10 mg amlodipine/kg/day for 14 days before mating and throughout mating and gestation. Amlodipine maleate has been shown to prolong both the gestational period and the duration of labor in rats at this dose. There are no adequate and well-controlled studies in pregnant women. Amlodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the ...
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Background: Endothelial cell (EC) dysfunction is causally related to atherosclerosis and hypertension. Aliskiren, a direct renin inhibitor, and amlodipine, a calcium channel blocker, have each been shown to improve vascular function; however, their combined effects are not understood. In this study, we tested the separate versus combined effects of aliskiren and amlodipine on aortic and glomerular EC function.. Methods: Spontaneously hypertensive (SH) rats were assigned to four treatment groups: (1) vehicle; (2) 40 mg/kg/day aliskiren; (3) 5 mg/kg/day amlodipine; and (4) combined aliskiren and amlodipine treatment (at 40 and 5 mg/kg/day, respectively). Each group contained 8 animals and treatments were administered for 8 weeks. Endothelial nitric oxide (NO) and peroxynitrite (ONOO-) release from aortic and glomerular ECs were measured ex vivo using amperometric nanosensors and correlated with systemic blood pressure (BP) measurements.. Results: Aliskiren and amlodipine improved NO release in a ...
Part 1: After aliskiren treatment (period 2), each patient was entered into a second washout period (4 weeks) during which blood pressure was required to be ≤ 140/90 mmHg. If blood pressure exceeded 140/90 mmHg on two consecutive days (home monitoring) and was confirmed at the study center, the patient was entered into the amlodipine treatment period (period 3). In period 3, all patients received 5 mg amlodipine o.d.. The length of the amlodipine period varied from 4 to 7 weeks.. Part 2: Eligible patients randomized to part 2 received amlodipine 5 mg o.d. and aliskiren placebo for 12 weeks ...
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We very much appreciate the comments and hypotheses of Balligand and Godfraind.1 Our quantitative overview on amlodipine and angiotensin receptor blockers demonstrated that calcium channel blockade by the use of amlodipine substantially reduced the risk of stroke and myocardial infarction.2 Blood pressure gradients between randomized groups of trials largely account for the benefit of amlodipine versus other antihypertensive agents. However, amlodipine indeed produced benefits beyond brachial blood pressure measured in the clinic, particularly against stroke. We believe that the benefit of amlodipine beyond brachial blood pressure to a large extent could be attributable to the better blood pressure control in the whole circulatory system and over 24 hours, although other mechanisms, such as the prevention of intima-media thickening by calcium channel blockade,3 may also play a role. In the Conduit Artery Function Evaluation substudy of the Anglo-Scandinavian Cardiac Outcomes Trial-Blood Pressure ...
METHODS: Twelve mild-to-moderate essential hypertensives were investigated in this open, randomized cross-over study. Blood pressure and heart rate were measured by use of ambulatory blood pressure monitoring after a wash-out period of 1 week and after treatment schedules with 5 mg amlodipine once a day either. Amlodipine is a calcium channel blocker that dilates blood vessels and improves blood flow. Amlodipine is used to treat chest pain (angina) and other conditions caused by coronary artery disease. Amlodipine is also used to treat high blood pressure. It does not matter what time of day you take amlodipine.. You may have to take what time of day should i take amlodipine blood pressure medicine for the breakdown of your life. If estoque blood pressure is not treated, it can cure serious problems such as other failure, blood pressure disease, stroke, or kidney disease. You may take this morning with or without food. Take this medicine at the same situation each day. Their doctor will discuss ...
Patients with end-stage renal failure have a markedly higher mortality because of cardiovascular events in comparison with the normal population. Disorders in the calcium metabolism, such as calcification of the vessel walls, occur very frequently. There are indications that calcium channel blockers are capable of lowering the cardiovascular mortality in patients with end-stage renal failure.. It is intended to carry out a prospective, randomized, double-blind, placebo-controlled, multicenter study in order to find out if the calcium channel blocker amlodipine is able to reduce the mortality of patients with end-stage renal failure.. The investigation will be carried out after suitable explanation and written informed consent in 356 patients aged between 18 and 90 years with end-stage renal failure and chronic haemodialysis treatment. The patients will be randomized to either treatment with amlodipine 10 mg/day or placebo. The occurrence of events will be documented and evaluated prospectively ...
In male Wistar rats [light(L): 07:00-19:00 h, dark(D): 19:00-07:00 h], the effects of the calcium channel blocker amlodipine (1, 3, 10 mg/kg i.p.) on blood pressure, heart rate, and motor activity were studied by telemetric monitoring. Amlodipine was
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Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice. ...
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Backround Multidrug resistance (MDR) is a major obstacle to successful cancer chemotherapy as the over-expressed MDR protein acts as an efflux pump, which leads to a reduction in the uptake of the anticancer agent by tumour cells. We combined topotecan and amlodipine together into the stealthy liposomes, in which amlodipine was applied as a MDR reversing agent to overcome the resistance.. Materials and methods Cytotoxicity, apoptosis and the signalling pathway assays were performed on human chronic myelogenous leukaemia K562, promyelocytic leukaemia HL-60 and MDR HL-60 cells, respectively. Pharmacokinetics and antitumour activity studies were performed on normal Kunming mice and female BALB/c nude mice with MDR HL-60 xenografts, respectively.. Results Topotecan alone was effective in inhibiting the growth of non-resistant leukaemia cells, K562 and HL-60 cells but not the growth of MDR HL-60 cells. The resistance of topotecan in MDR HL-60 cells was potently reversed by the addition of amlodipine. ...
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Chronic electric activation of the carotid baroreflex produces sustained reductions in sympathetic activity and arterial pressure and is currently being evaluated as hypertension therapy for patients with resistant hypertension. However, the chronic changes in renal function associated with natural suppression of sympathetic activity are largely unknown. In normotensive dogs, we investigated the integrative cardiovascular effects of chronic baroreflex activation (2 weeks) alone and in combination with the calcium channel blocker amlodipine, which is commonly used in the treatment of resistant hypertension. During baroreflex activation alone, there were sustained decreases in mean arterial pressure (17±1 mmHg) and plasma (norepinephrine; ≈35%), with no change in plasma renin activity. Despite low pressure, sodium balance was achieved because of decreased tubular reabsorption, because glomerular filtration rate and renal blood flow decreased 10% to 20%. After 2 weeks of amlodipine, arterial ...
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A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO) for the precipitation of, respectively, a DMSO solvate of an L-tartrate salt of R-(+)-amlodipine, or a DMSO solvate of a D-tartrate salt of S-(-)-amlodipine. ##STR1##
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Drug manufacturer deviates from the appropriate comparator therapy specified by the G-BA. The fixed drug combination of aliskiren and amlodipine (trade name: Rasilamlo®) was approved in April 2011 for the treatment of people with hypertension in whom aliskiren or amlodipine alone has an insufficient effect. In an early benefit assessment pursuant to the "Act on the Reform of the Market for Medicinal Products" (AMNOG), the German Institute for Quality and Efficiency in Health Care (IQWiG) examined whether this drug combination offers an added benefit compared with the present standard drug therapy in people with essential hypertension. However, such an added benefit cannot be inferred from the dossier, as the drug manufacturer deviated from the specifications of the Federal Joint Committee (G-BA) and chose a different comparator therapy.. Calcium channel blocker and ACE inhibitor specified as comparator therapy. Aliskiren interferes with the production of blood-pressure controlling hormones (the ...
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The distinctive pharmacokinetic and pharmacodynamic activity of amlodipine, including long onset and duration of activity as a calcium channel antagonist, may be related to its interactions with membranes. We have used X-ray crystallography and small-angle X-ray scattering to examine and compare the crystal structure of amlodipine and its location in cardiac sarcolemmal lipid bilayers with that of uncharged dihydropyridines (DHPs) such as nimodipine. Crystallographic analysis demonstrated that the DHP ring of amlodipine is considerably more planar than that of nimodipine, that amlodipine has a greater torsion angle between the DHP and aryl rings, and that the protonated amino group extends away from the DHP ring structure. Despite the positive charge of amlodipine at physiological pH, membrane electron density profile structures showed amlodipine to have a time-averaged location near the hydrocarbon core/water interface similar to that observed for several uncharged DHPs. However, unlike ...
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Objectives Clinical studies have indicated the beneficial effect of an L/N-type calcium channel blocker (CCB) cilnidipine around the progression of proteinuria in hypertensive patients compared with an L-type CCB amlodipine. in an age-dependent manner. Cilnidipine suppressed the proteinuria greater than amlodipine did. The immunohistochemical analysis showed that N-type calcium channel and Wilms tumor factor a marker of podocyte were co-expressed. SHR/ND had significantly greater desmin staining an indication of podocyte injury with lower podocin and nephrin expression in the glomeruli than Wistar-Kyoto rat or SHR. Cilnidipine significantly prevented the increase in desmin staining and restored the glomerular podocin and nephrin expression compared with amlodipine. Cilnidipine also prevented the increase in renal angiotensin II content the expression and membrane translocation of NADPH oxidase subunits and dihydroethidium staining in SHR/ND. In contrast amlodipine failed MUC12 to switch these ...
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The optimum antihypertensive treatment for prevention of hypertensive stroke has yet to be elucidated. This study was undertaken to examine the benefit of a combination of valsartan, an AT1 receptor blocker, and amlodipine, a calcium channel blocker, in prevention of high-salt-induced brain injury in hypertensive rats. High-salt-loaded stroke-prone spontaneously hypertensive rats (SHRSPs) were given (1) vehicle, (2) valsartan (2 mg/kg/day), (3) amlodipine (2 mg/kg/day), and (4) a combination of valsartan and amlodipine for 4 weeks. The effects on brain injury were compared between all groups. High-salt loading in SHRSPs caused the reduction of cerebral blood flow (CBF), cerebral hypoxia, white matter lesions, glial activation, AT1 receptor upregulation, eNOS uncoupling, iNOS induction, and nitroxidative stress. Valsartan, independently of blood pressure, enhanced the protective effects of amlodipine against brain injury, white matter lesions, and glial activation in salt-loaded SHRSPs. These ...
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The Localization of the Phenylalkylamine Binding Sites of the Alpha} Subunit The phenylalkylamine-based calcium antagonists (prototype, verapamil), resemble their dihydropyridine-based equivalents (e. g. nifedipine, amlodipine) in that their primary pharmacological activity is due to their ability to interact with "receptors" which reside in the (lj subunit of the L-type Ca 2 + channel complex (Glossman and Striessnig, 1990). , 1982; Valdivia and Coronado, 1989). , 1990). According to Striessnig and his colleagues, the receptor region for these particular calcium antagonists involves three negatively charged aspartic acid residues at positions of 1382, 1385 and 1390 of the 1873 amino acid sequence of the (ll subunit. 1). The detailed biochemistry of these channels has been described elsewhere (Nayler, 1990). , 1989) or, (b) as in cardiac and smooth muscle cells, in response to Ca2+ ions crossing the sarcolemma by way of the voltage-activated Ca 2 + -selective channels (Cleemann and Morad, ...
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The increased viscosity of blood of hypertensive patients can be assumed to be a risk factor for the development of cardiovascular diseases. The aim of the present study was to elucidate whether anti-hypertensive treatment has any impact on blood theology.. Twenty patients with previously untreated hypertension who consecutively attended our outpatient hypertension clinic were included in this prospective, open, cross-over study. The patients were randomly selected to treatment with amlodipine or metoprolol. The antihypertensive therapy was switched after 4 months. Haemorheological and haemodynamic variables were measured with rotational viscometry and impedance cardiography, respectively.. Fifteen and 16 patients could be evaluated after amlodipine or metoprolol treatment respectively. The mean blood pressure (BP) decreased from 159 +/- 22/105 +/- 7 to 139 +/- 21/91 +/- 6 mm Hg on amlodipine and from 162 +/- 22/104 +/- 5 to 145 +/- 24/90 +/- 8 mm Hg on metoprolol therapy. After amlodipine ...
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Objective To investigate the efficacy of taking in valsartan hydrochlorothiazide at the different time points on a blood pressure variability( BPV),carotid intima media thickness( CIMT),notric oxide( NO) and endothelin 1( ET-1). Methods Enrolled 80 hypertensive subjects with stage 1 to 2 essential hypertension,who were treated in Hebei general hospital between June 2015 and February 2017. These subjects were randomly assigned to receive valsartan hydrochlorothiazide( 80 mg/12. 5 mg) either on awakening( Ⅰgroup) or at bedtime( Ⅱgroup). All cases received 24 hours ambulatory blood pressure monitoring and CIMT before and after 12 weeks of treatment. NO and ET-1 were monitored before the treatment and12 weeks after the treatment. Results Compared with the baseline level,24 h mean systolic blood pressure( 24 h MSBP),24 h diastolic blood pressure( 24 h MDBP),24 h systolic blood pressure variability( 24 h SBPV),24 h diastolic blood pressure variability( 24 h DBPV),day SBPV,day DBPV,night SBPV,night DBPV
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Cilnidipine (INN) is a calcium channel blocker. It is a calcium antagonist accompanied with L-type and N-type calcium channel blocking functions. It was jointly developed by Fuji Viscera Pharmaceutical Company and Ajinomoto, and was approved to enter the market and be used as an anti-hypertensive in 1995.[citation needed] Unlike other calcium antagonists, cilnidipine can act on the N-type calcium channel in addition to acting on the L-type calcium channel. Cilnidipine is approved for use in Japan, China, India, Korea, and some European countries to treat hypertension. Cilnidipine decreases blood pressure and is used to treat hypertension and its comorbidities. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, reducing the pressure in the capillary bed. Cilnidipine is vasoselective and has a weak direct dromotropic effect, a strong vasodepressor effect, and an arrhythmia-inhibiting effect. Blood pressure control with cilnidipine ...

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