When was cozaar introduced




















Comparative effects of losartan and irbesartan on serum uric acid in hypertensive patients with hyperuricemia and gout. J Hypertens. Comparative effects of losartan and irbesartan on serum uric acid in hypertensive patients with hyperuricaemia and gout. Clin Ther. Losartan versus valsartan in the treatment of patients with mild to moderate essential hypertension: data from a multicenter, randomized, double-blind, week trial. Comparative effects of chronic ACE inhibition and AT1 receptor blocked losartan on cardiac hypertrophy and renal function in hypertensive patients.

J Hum Hypertens. Sica D, Schoolwerth A. Part 1. Uricosuric effect of losartan in patients with renal transplants. Efficacy and safety of losartan in treatment of hyperuricemia and posttransplantation erythrocytosis: results of a prospective, open, randomized, case-control study. Transplant Proc. Journal of Physiology and Pharmacology. Losartan inhibits thromboxane A2-induced platelet aggregation and vascular constriction in spontaneously hypertensive rats. J Cardiovasc Pharmacol.

Inhibition of platelet activation in stroke-prone spontaneously hypertensive rats: comparison of losartan, candesartan, and valsartan.

Effect of losartan on human platelet activation. Comparative effects of angiotensin II ATtype receptor antagonists in vitro on human platelet activation. Losartan inhibits in vitro platelet activation: comparison with candesartan and valsartan. Journal of the Renin-Angiotensin-Aldosterone System. Platelet aggregability in patients with hypertension treated with angiotensin II type 1 receptor blockers. J Atheroscler Thromb. Renoprotection with and without blood pressure reduction.

Kidney Int. Long-term effects of losartan on proteinuria and renal function in patients with renal amyloidosis. Scand J Urol Nephrol.

Interim evidence of the renoprotective effect of the angiotensin II receptor antagonist losartan versus the calcium channel blocker amlodipine in patients with chronic kidney disease and hypertension: a report of the japanese losartan therapy intended for global renal protection in hypertensive patients JLIGHT study.

Clin Exp Nephrol. Efficacy of losartan in patients with primary focal segmental glomerulosclerosis resistant to immunosuppressive treatment. J Intern Med. Comparison of the angiotensin II antagonist losartan with the angiotensin converting enzyme inhibitor enalapril in patients with essential hypertension.

Randomised, double-blind, parallel study of the anti-hypertensive efficacy and safety of losartan potassium compared with felodipine ER in elderly patients with mild to moderate hypertension. Renoprotection of optimal antiproteinuric doses ROAD study: a randomized controlled study of benazepril and losartan in chronic renal insufficiency.

Effects of losartan on renal and cardiovascular outcomes in patients with type 2 diabetes and nephropathy. New Eng J Med. Arch Intern Med. Anti-proteinuric effects of combination therapy with enalapril and losartan in patients with nephropathy due to type 2 diabetes. Int J Clin Pract. Coadministration of losartan and enalapril exerts additive antiproteinuric effect in IgA nephropathy.

Am J Kidney Dis. Ann Intern Med. Aliskiren combined with losartan in type 2 diabetes and nephropathy. Randomised trial of losartan versus captopril in patients over 65 with heart failure evaluation of losartan in the elderly study, ELITE Lancet. Effect of losartan compared with captopril on mortality in patients with symptomatic heart failure: randomised trial — the losartan heart failure survival study ELITE II. Hemodynamic and neurohormonal effects of the angiotensin II antagonist losartan in patients with congestive heart failure.

Effects of high-dose versus low-dose losartan on clinical outcomes in patients with heart failure HEAAL study : a randomised, double-blind trial.

Cardiovascular morbidity and mortality in the losartan intervention for endpoint reduction in hypertension study LIFE : a randomised trial against atenolol. Regression of hypertensive left ventricular hypertrophy by losartan compared with atenolol: the losartan intervention for endpoint reduction in hypertension LIFE trial.

Regression of electrocardiographic left ventricular hypertrophy by losartan versus atenolol: the losartan intervention for endpoint reduction in hypertension LIFE study.

Left ventricular filling patterns in patients with systemic hypertension and left ventricular hypertrophy the LIFE study. Losartan intervention for endpoint. Am J Cardiol. The left atrium, atrial fibrillation, and the risk of stroke in hypertensive patients with left ventricular hypertrophy. Ther Adv Cardiovasc Dis. A possible link between endothelial dysfunction and insulin resistance in hypertension. A LIFE substudy. Losartan intervention for endpoint-reduction in hypertension.

Blood Press. Opposite effects of losartan and atenolol on natriuretic peptides in patients with hypertension and left ventricular hypertrophy: a LIFE substudy. The impact of serum uric acid on cardiovascular outcomes in the LIFE study.

Effects of losartan compared with atenolol on lipids in patients with hypertension and left ventricular hypertrophy: the losartan intervention for endpoint reduction in hypertension study.

Does albuminuria predict cardiovascular outcome on treatment with losartan versus atenolol in hypertension with left ventricular hypertrophy? Incidence of atrial fibrillation in relation to changing heart rate over time in hypertensive patients: the LIFE study. Circ Arrhythm Electrophysiol.

Risk of new-onset diabetes in the losartan intervention for endpoint reduction in hypertension study. Economic evaluation of angiotensin receptor blockers in type 2 diabetes, hypertension, and nephropathy.

The impact of losartan on the lifetime incidence of ESRD and costs in mexico. Cost effectiveness of angiotensin receptor blocker monotherapy in patients with hypertension in the netherlands: a comparative analysis using clinical trial and drug utilization data.

Am J Cardiovas Drugs. Support Center Support Center. Information from references 5 through 9 , and Estimated cost to the pharmacist based on average wholesale prices rounded to the nearest dollar in Red book.

Montvale, N. Cost to the patient will be higher, depending on prescription filling fee. Information from references 5 through 9. Losartan was the first angiotensin-II receptor antagonist to be introduced Compared with the parent drug, the active metabolite EXP has a longer half-life and antihypertensive effects that correlate more with plasma concentration.

The starting dosage of losartan is 50 mg once daily. The duration of activity for a dose is 24 hours. Twice-daily dosing can be used if the antihypertensive effect measured at a trough is inadequate. A hydrochlorothiazide-losartan combination Hyzaar is also available. This combination drug contains Some investigators advocate the use of this combination instead of escalation of a single drug, because dose-dependent adverse effects are less likely to occur.

Placebo-controlled trials have found valsartan to be both safe and effective for the treatment of hypertension. The affinity of valsartan for the AT 1 receptor is about 20, times greater than its affinity for the AT 2 receptor. Valsartan is also available as a combination product with hydrochlorothiazide Diovan HCT. This combination drug contains 80 or mg of valsartan and With the addition of hydrochlorothiazide, blood pressure decreases even more i. Dosing is once daily. Irbesartan is a safe and effective angiotensin-II receptor antagonist with an affinity for the AT 1 receptor that is more than 8, times greater than its affinity for the AT 2 receptor.

In one study, patients with mild to moderate hypertension were given placebo, losartan in a dosage of mg per day or irbesartan in a dosage of or mg per day. Placebo-controlled trials have shown that irbesartan in a dosage of to mg per day lowers mean systolic blood pressure by 8 to 12 mm Hg and mean diastolic pressure by 5 to 8 mm Hg.

Candesartan cilexetil has been shown to be effective for the treatment of hypertension. Candesartan itself is poorly absorbed after oral administration; the ester prodrug, candesartan cilexetil, improves bioavailability Table 2.

With oral administration of candesartan cilexetil, conversion to the active compound occurs rapidly and completely during gastrointestinal absorption. Candesartan is both safe and well tolerated in dosages of 8 to 32 mg per day.

With these dosages, systolic blood pressure is reduced by 8 to 12 mm Hg and diastolic pressure is reduced by 4 to 8 mm Hg. Comparable reductions of diastolic blood pressure have been achieved with candesartan in a dosage of 8 mg per day and enalapril in a dosage of 10 mg per day. The same study compared losartan in a dosage of 50 mg per day with candesartan in dosages of 8 and 16 mg per day.

Telmisartan is the most recently labeled angiotensin-II receptor antagonist. Its affinity for the AT 1 receptor is more than 3, times greater than its affinity for the AT 2 receptor. Nonlinear pharmacokinetics yield a greater than proportional increase in plasma telmisartan concentrations with increasing dosages.

The efficacy of telmisartan in the treatment of hypertension has been demonstrated in placebo-controlled trials. A three-month study of patients showed that telmisartan in a dosage of 40, 80, or mg per day produced a slightly greater antihypertensive effect than enalapril in a dosage of 20 mg per day.

The decreases in diastolic and systolic blood pressures for enalapril were 7. Like the other angiotensin-II receptor antagonists, telmisartan has been shown to have a side effect profile similar to that of placebo. Clinical trials have demonstrated no rebound hypertension or first-dose orthostatic effect. The side effects of angiotensin-II receptor antagonists are comparable to those of placebo. Unlike ACE inhibitors, the angiotensin-II receptor antagonists are not significantly associated with cough.

In controlled trials using these drugs, the incidence of dry cough was comparable to that with placebo i. Life-threatening angioedema has been associated with both ACE inhibitors and angiotensin-II receptor antagonists. The incidence of angioedema appears to be lower with angiotensin-II receptor antagonists than with ACE inhibitors.

However, these agents have been in clinical use for a much shorter time than ACE inhibitors. Postmarketing surveillance should help to further define the overall incidence of angioedema in patients treated with the newer drugs.

Dizziness is a drug-related side effect that occurs in about 2 to 4 percent of patients taking angiotensin-II receptor antagonists. Infrequent adverse effects with a possible causal association include nausea, headache, upper respiratory tract infection, back pain, fatigue, diarrhea, dyspepsia, nasal congestion, sinusitis and pharyngitis. Rarely, liver function tests and serum bilirubin concentrations may become elevated in patients treated with angiotensin-II receptor antagonists.

When administered during the second and third trimesters of pregnancy, medications that act directly on the renin-angiotensin-aldosterone system have been associated with fetal and neonatal injury or death. Therefore, angiotensin-II receptor antagonists should not be used in pregnant women. In addition, none of these agents should be taken by patients who are breast-feeding because it is not certain how much drug is secreted in breast milk.

Clinically significant drug interactions have been reported with losartan, which undergoes extensive first-pass metabolism by cytochrome P enzymes. Drugs such as ketoconazole Nizoral and troleandomycin Tao inhibit cytochrome P and thus may reduce formation of the active metabolite of losartan.

The concomitant use of losartan and cimetidine Tagamet has been found to increase the bioavailability of losartan by 18 percent. The clinical implications of potential interactions with angiotensin-II receptor blockers are still uncertain. No significant drug interactions have been reported with valsartan, irbesartan or candesartan. A drug interaction can occur between telmisartan and digoxin Lanoxin.

In this interaction, the peak plasma concentrations of digoxin are increased, and the trough digoxin levels are elevated by 20 percent. The AT 1 receptor is found throughout the kidneys, including the renal vessels, afferent and efferent arterioles, and tubular and juxta-glomerular cells.

One study on the use of losartan in patients with kidney disease demonstrated an increase in renal plasma flow with a stable glomerular filtration rate. Candesartan has been shown to have vasodilator effects within the renal circulation by decreasing renal vascular resistance. The occurrence of microalbuminuria has also been studied in patients treated with angiotensin-II receptor antagonists. In small studies, irbesartan, losartan and candesartan have been associated with a reduction in urine protein excretion.

Angiotensin-II receptor antagonists should be used cautiously in patients with renal dysfunction, and potassium levels should be monitored. These agents have the potential to elevate potassium concentrations, especially in patients who are also taking potassium-sparing diuretics.

In patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system, such as those with severe congestive heart failure, the use of angiotensin-II receptor antagonists may result in oliguria, progressive azotemia and, rarely, acute renal failure or death.

Data are accumulating on the use of angiotensin-II receptor antagonists in the treatment of congestive heart failure. However, none of the drugs in this class has been labeled by the FDA for this indication. Studies have compared the use of losartan and placebo in patients with New York Heart Association classes II through IV congestive heart failure and an ejection fraction of less than 40 percent. The Evaluation of Losartan in the Elderly ELITE study was a week investigation conducted in patients with congestive heart failure who were 65 years of age or older.

The mg tablet is priced similarly to losartan 25 mg and 50 mg, valsartan 80 mg and mg, and enalapril 10 mg. Gemfibrozil treatment of post-CABG patients with isolated low HDL has been associated with marked reduction in subsequent clinical events despite lack of any demonstrated angiographic benefit. It has been shown to be effective for congestive heart failure and diabetic nephropathy.

Reprints Share. Angiotensin Receptor Blockers for Hypertension. Options expand for women: FDA approves a new intrauterine device. Indications Irbesartan is indicated for the treatment of hypertension. Potential Advantages Angiotensin II receptor blockers, as a class, have not been associated with cough or angioedema, which can be problematic with ACE inhibitors.

Comments Angiotensin II is substance that regulates blood pressure and plasma volume. Report Abusive Comment Thank you for helping us to improve our forums. Is this comment offensive? Please tell us why. Restricted Content You must have JavaScript enabled to enjoy a limited number of articles over the next days.



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