Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Olmesartan medoxomil (Belsar, Olmetec) developed by Sankyo Pharma and proposed by Sankyo Pharma but also Menarini is a new angiotensin II ATI receptor blocker. Its indication is the treatment of hypertension. Olmesartan is indeed an antihypertensive agent with an efficacy dependent on the dose from 10 to 40 mg. It is taken once a day, because of a long duration of action. This prodrug has a dual elimination pathway (biliary and renal). The contraindications are the same as for the other sartans. One of its main advantage, besides its rapidly observed efficacy to lower high blood pressure, is its relatively low cost within this family. It has also cardiovascular and renal protective effects. The recommended usual dosage is 20 mg/day.
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PMID:[The drug of the month: Olmesartan medoxomil]. 1562 83

In most patients with hypertension, especially Stage 2 hypertension, adequate control of blood pressure (BP) is only achieved with combination drug therapy. When using combination therapy, antihypertensive agents with complementary mechanisms of action are recommended, for example, an angiotensin receptor blocker (ARB) in combination with hydrochlorothiazide (HCTZ), a beta-blocker + HCTZ, an ACE inhibitor + HCTZ, or a calcium channel blocker + an ACE inhibitor. One such combination is olmesartan medoxomil + HCTZ, which is available as fixed-dose, single-tablet combinations for once-daily administration. In clinical trials, olmesartan medoxomil/HCTZ reduced systolic BP (SBP) and diastolic BP (DBP) to a greater extent than either component as monotherapy. A clinical study in patients with Stage 1 or 2 hypertension showed that olmesartan medoxomil/HCTZ achieved a similar mean reduction in DBP, but a significantly greater mean reduction in SBP and higher rate of BP control (< 140/90 mmHg) than observed with losartan/HCTZ, at US/European-approved starting doses. In a non-inferiority trial, the antihypertensive efficacy of olmesartan medoxomil/HCTZ was comparable to that of atenolol/HCTZ. Furthermore, indirect comparisons have shown that olmesartan medoxomil/HCTZ compares favorably with other antihypertensive combination therapies, including other ARB/HCTZ combinations and amlodipine besylate/ benazepril. Olmesartan medoxomil/HCTZ is generally well tolerated. In conclusion, olmesartan medoxomil/HCTZ is an effective and well-tolerated combination antihypertensive therapy that results in significant BP reductions and BP control in many patients.
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PMID:Olmesartan medoxomil combined with hydrochlorothiazide for the treatment of hypertension. 1732 94

The therapeutic control of hypertension is still a global challenge and frequently requires combination therapy. Olmesartan medoxomil hydrochlorothiazide (Olmetec plus, Belsar plus) is a fixed-dose combination of olmesartan 20 mg and hydrochlorothiazide 12.5 or 25 mg. Olmesartan is a well known angiotensin II AT1 receptor blocker characterized by a good efficacy, a fast and prolonged duration of action and a placebo-like tolerability. With the combination therapy, no significant change of pharmacokinetics of either component is observed. The fixed-dose combination results in a greater blood pressure reduction compared to monotherapy with either component. This is at least effective as or even more effective than the combination of atenolol or losartan with hydrochlorothiazide, respectively. The responder rate is about 90%. The safety and tolerability remain excellent. Beyond the antihypertensive effect, olmesartan significantly reduces vascular inflammation and the wall-to-lumen ration in arteries. The starting dose is 20/12.5 mg.
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PMID:[Medication of the month. Olmesartan medoxomil hydroclorothiazide (Olmetec Plus or Belsar Plus]. 1751 87

Olmesartan medoxomil is an angiotensin II (Ang II) receptor blocker (ARB) that has been approved by the US Food and Drug Administration (FDA) for the treatment of hypertension. It is a prodrug that is hydrolysed in the gut into its active metabolite, olmesartan (RNH-6270). Olmesartan is highly selective for the Ang II type 1 receptor (AT1) to which it binds completely and insurmountably and has very little affinity for the other receptor subtypes AT2 and AT4. After oral administration, in animals and humans, it achieves a maximal blood drug concentration within a maximal time of approximately 2 h. It is then slowly eliminated in the urine and faeces. His half-life is approximately 13 h, which makes it suitable for once-daily administration. Olmesartan medoxomil given orally in single daily doses of 20-40 mg has demonstrated significant blood pressure (BP) lowering effects in hypertensive patients. A medline search for the preparation of this manuscript was conducted and revealed 128 references, from 2000 to 2007. Of these, only 16 well-designed prospective clinical trials were selected. The remaining were either animal studies, reviews or studies in progress. In well-designed clinical trials, olmesartan medoxomil has demonstrated similar antihypertensive actions to the other antihypertensive drugs, as well as other members of its class given the highest recommended doses. In addition, the BP lowering effect of olmesartan, like the other members of its class, is greatly enhanced in combination with a diuretic. Its safety profile is similar to the other ARBs and no different than placebo.
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PMID:Treatment of hypertension with olmesartan medoxomil, alone and in combination with a diuretic: an update. 1755 45

Although achieving blood pressure (BP) control is critical to improve cardiovascular prognosis in hypertensive patients, many of them fail to attain the targets. Most patients with hypertension need more than one antihypertensive agent to achieve the goals. Combination therapy is required when monotherapy fails to attain BP objectives (< 140/90 mmHg in general hypertensive population; < 130/80 mmHg in high-risk groups) and as a first-line treatment in certain situations, such as markedly elevated BP values, high or very high cardiovascular risk patients or when lower targets are warranted. The advantages of combination therapy are well documented with the potential for increased antihypertensive efficacy as a result of different mechanisms of action, and a lower incidence of adverse effects because of the lower doses used and the possible compensatory responses. The inhibition of the renin-angiotensin system appears to be very beneficial in the treatment of patients with hypertension. Olmesartan medoxomil 20 mg/hydrochlorothiazide 12.5 mg is the latest combination of an angiotensin receptor blocker and a diuretic approved for treatment of hypertension. The aim of this manuscript is to update the published data about the efficacy and safety of this fixed combination.
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PMID:Olmesartan medoxomil plus hydrochlorothiazide for treating hypertension. 1807 44

Olmesartan medoxomil (Olmetec, Benicar) is an angiotensin II type 1 (AT(1)) receptor antagonist (angiotensin receptor blocker [ARB]) that inhibits the actions of angiotensin II on the renin-angiotensin-aldosterone system, which plays a key role in the pathogenesis of hypertension. Oral olmesartan medoxomil 10-40 mg once daily is recommended for the treatment of adult patients with hypertension. In those with inadequate BP control using monotherapy, fixed-dose olmesartan medoxomil/hydrochlorothiazide (HCTZ) [Olmetec plus, Benicar-HCT] combination therapy may be initiated. Extensive clinical evidence from several large well designed trials and the clinical practice setting has confirmed the antihypertensive efficacy and good tolerability profile of oral olmesartan medoxomil, as monotherapy or in combination with HCTZ, in patients with hypertension, including elderly patients with isolated systolic hypertension (ISH). Notably, BP control is sustained throughout the 24-hour dosage interval, including during the last 4 hours of this period. In clinical trials, olmesartan medoxomil monotherapy provided better antihypertensive efficacy than losartan, candesartan cilexetil or irbesartan monotherapy, and was at least as effective as valsartan treatment, with a faster onset of action than other ARBs in terms of reductions from baseline in diastolic BP (DBP) and, in most instances, systolic BP (SBP). Combination therapy with olmesartan medoxomil plus HCTZ was superior to that with benazepril plus amlodipine, as effective as that with losartan plus HCTZ, noninferior to that with atenolol plus HCTZ, but less effective than that with telmisartan plus HCTZ, in individual trials. Data from ongoing clinical outcome trials are required to more fully determine the relative position of olmesartan medoxomil therapy in the management of hypertension. In the meantime, the consistent antihypertensive efficacy during the entire 24-hour dosage interval and good tolerability profile of olmesartan medoxomil, with or without HCTZ, make it a valuable option for the treatment of adult patients with hypertension, including the elderly.
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PMID:Olmesartan medoxomil: a review of its use in the management of hypertension. 1854 34

black triangle Olmesartan medoxomil/amlodipine is a fixed-dose combination of olmesartan medoxomil and amlodipine, both established antihypertensive agents. Dose titration with the individual constituent drugs is recommended before switching to the equivalent fixed-dose combination. black triangle In a randomized, double-blind, factorial trial in patients with mild to severe hypertension, 8 weeks of olmesartan medoxomil/amlodipine was more effective in reducing diastolic BP (DBP) and systolic BP (SBP) than placebo or equivalent dosages of olmesartan medoxomil or amlodipine as monotherapy. black triangle In two randomized, double-blind trials in patients with moderate to severe hypertension not adequately treated with amlodipine or olmesartan medoxomil monotherapy, 8 weeks of olmesartan medoxomil/amlodipine 20 mg/5 mg, 40 mg/5 mg or 40 mg/10 mg per day was more effective in reducing DBP and SBP than continuing treatment with olmesartan medoxomil 20 mg/day or amlodipine 5 mg/day monotherapy. black triangle More patients receiving olmesartan medoxomil/amlodipine at approved dosages than monotherapy recipients at equivalent dosages reached BP goals (42.5-51.0% vs 21.1-36.3% in the factorial trial and 44.5-54% vs 28.5-30% in the monotherapy comparisons). black triangle In the comparison with amlodipine monotherapy, >70% of olmesartan medoxomil/amlodipine recipients, some requiring upwards dosage adjustment, met BP goals. black triangle Olmesartan medoxomil/amlodipine was generally well tolerated in clinical trials. Peripheral oedema was significantly less common in olmesartan medoxomil/amlodipine 40 mg/10 mg per day than amlodipine monotherapy 10 mg/day recipients.
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PMID:Olmesartan medoxomil/amlodipine. 1940 51

Endothelial dysfunction is the common link between cardiovascular disease risk factors and the earliest event in the cascade of incidents that results in target organ damage. Angiotensin II, the terminal pressor effector arm of the renin-angiotensin-aldosterone system, increases blood pressure (BP) by vasoconstriction and sodium and fluid retention, and has a pro-oxidative action that induces endothelial dysfunction and contributes to vascular remodeling. Angiotensin receptor blockers (ARBs) reduce BP and morbidity and mortality in patients with hypertension, ventricular hypertrophy, diabetes mellitus, and renal disease. Olmesartan medoxomil is a long-acting, well-tolerated, effective ARB that prevents or reverses endothelial dysfunction in animal models of atherosclerosis, hypertension, diabetes, nephropathy, and retinopathy. Olmesartan medoxomil, a prodrug of olmesartan approved for the treatment of hypertension, has been shown to ameliorate endothelial dysfunction in patients with hypertension or diabetes. In randomized studies, the drug reduces vascular inflammation and the volume of large atherosclerotic plaques, increases the number of regenerative endothelial progenitor cells in the peripheral circulation, improves endothelium-dependent relaxation, and restores the normal resistance vessel morphology. Importantly, the impact of olmesartan medoxomil on endothelial dysfunction is thought to be independent of BP lowering.
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PMID:Effect of angiotensin receptor blockade on endothelial function: focus on olmesartan medoxomil. 1943 55

Serum cystatin C concentration is an alternative measure of kidney function that is less affected by age, sex or muscle mass, and is a more sensitive indicator of early renal dysfunction than creatinine-based estimations of glomerular filtration rate. Cardiovascular sequela increases progressively with the increase in left ventricular mass. Our goal was to evaluate the effect of olmesartan medoxomil on cystatin C levels and left ventricular hypertrophy (LVH) in patients with hypertension. Forty-four newly diagnosed hypertensive patients (27 women and 17 men) were recruited in the study. Olmesartan medoxomil (20mg/day) was started and the patients were followed up for 6 months. Baseline echocardiographic findings (i.e. left ventricular mass index), serum creatinine, urine albumin/creatinine ratio (ACR) and serum cystatin C levels were compared with the levels of these variables measured at the end of 6-month follow-up period. After 6 months of treatment with olmesartan medoxomil, there was a significant reduction in systolic and diastolic blood pressure (p<0.001) and in urine ACR (p=0.04). Mean serum cystatin C levels decreased from 1.61+/-0.24 mg/l to 1.31+/-0.29 mg/l (p<0.001). Olmesartan medoxomil treatment also reduced left ventricular mass index (p<0.001) and LVH (p<0.001). Our findings indicate that olmesartan medoxomil decreases serum cystatin C levels, urine ACR and reduces LVH in patients with hypertension. To our knowledge, this study is the first to show that olmesartan medoxomil decreases serum cystatin C levels, indicating that in patients with essential hypertension it may counteract end organ damage.
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PMID:Effect of olmesartan medoxomil on cystatin C level, left ventricular hypertrophy and diastolic function. 1952 88

National and international guidelines recommend the use of combination drugs as a first-line therapy for persons with stage 2 hypertension (blood pressure > or =160/100 mmHg). Although hypertension is common (30% of adults in the USA), its control to recommended blood pressure levels of under 140/90 mmHg remains low, at 36.8%. In the past, fixed-drug combinations included a diuretic with another antihypertensive drug. Recently, combinations of angiotensin-converting enzyme inhibitors or angiotensin receptor blockers mostly with dihydropyridine calcium channel blockers have been developed and approved for the treatment of hypertension. One of these, olmesartan medoxomil in combination with amlodipine besylate has been shown to be effective and safe for the treatment of hypertension. In a large, randomized, placebo-controlled study (Combination of Olmesartan medoxomil and Amlodipine besylate in Controlling High blood pressure [COACH]) of 1940 patients, the high-dose combinations of olmesartan medoxomil and amlodipine besylate 40/10 mg/day reduced the sitting systolic and diastolic blood pressure by 29/19 mmHg from baseline (p < 0.001) and resulted in 54% of patients achieving blood pressure goals. It also decreased the pedal edema induced by amlodipine monotherapy 10 mg/day by 36.1%. This drug combination, besides being effective, is also safe and well tolerated.
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PMID:Amlodipine besylate/olmesartan medoximil fixed combination for the treatment of hypertension. 1967 66


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