Valtensin - Valtensin is an angiotensin II receptor antagonist. Valtensin keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow.
Valtensin is used to treat high blood pressure (hypertension). It is sometimes given together with other blood pressure medications.
Valtensin may also be used for purposes not listed in this medication guide.
Pharmacology: Antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the binding of angiotensin II to the AT receptor in vascular smooth muscle and the adrenal gland, producing decreased BP.
Indication: Treatment of hypertension; treatment of heart failure; reduction of CV mortality in clinically stable patients with left ventricular failure or dysfunction after MI.
Valtensin is an antihypertensive drug. This medication is a specific antagonist of angiotensin II. It has a selective antagonistic effect on AT1-receptors, which are responsible for implementing the effects of angiotensin II.
Due to the blockade of AT1-receptors the plasma concentrations of angiotensin II increased, which may stimulate the unblocked AT2-receptors. This medicine has no agonistic activity against AT1-receptor. The affinity of Valtensin for AT1-receptors in about 20 000 times higher than that of AT2-receptors.
Valtensin does not inhibit ACE. This drug has no interaction and does not block other hormone receptors or ion channels important for regulation of the cardiovascular system.
This medication has no effect on total cholesterol, triglycerides, glucose and uric acid in blood plasma.
A start of antihypertensive action of Valtensin after its oral administration in a single dose occurs within 2 h after administration, the maximum effect is achieved within 4-6 h.
Valtensin belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Valtensin is a specific and selective type-1 angiotensin II receptor (AT1) antagonist which blocks the blood pressure increasing effects angiotensin II via the renin-angiotensin-aldosterone system (RAAS). RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from granular cells of the juxtaglomerular apparatus in the kidneys. Renin cleaves circulating angiotensinogen to angiotensin I, which is cleaved by angiotensin converting enzyme (ACE) to angiotensin II. Angiotensin II increases blood pressure by increasing total peripheral resistance, increasing sodium and water reabsorption in the kidneys via aldosterone secretion, and altering cardiovascular structure. Angiotensin II binds to two receptors: AT1 and type-2 angiotensin II receptor (AT2). AT1 is a G-protein coupled receptor (GPCR) that mediates the vasoconstrictive and aldosterone-secreting effects of angiotensin II. Studies performed in recent years suggest that AT2 antagonizes AT1-mediated effects and directly affects long-term blood pressure control by inducing vasorelaxation and increasing urinary sodium excretion. Angiotensin receptor blockers (ARBs) are non-peptide competitive inhibitors of AT1. ARBs block the ability of angiotensin II to stimulate pressor and cell proliferative effects. Unlike ACE inhibitors, ARBs do not affect bradykinin-induced vasodilation. The overall effect of ARBs is a decrease in blood pressure.
Adult: PO HTN Initial: 80 mg once daily, up to 160 mg once daily. Max: 320 mg/day. Heart failure 40 mg twice daily, up to 160 mg twice daily if tolerated. Post-MI Initial: 20 mg twice daily, up to 160 mg bid if tolerated.
Valtensin helps to keep your blood pressure under control. Valtensin relaxes your blood vessels and this helps to lower your blood pressure. It may be used on its own or together with other medicines. Valtensin may also be used to treat other conditions, for example, heart failure.
Adult: Initially, 80 mg once daily, increased to 160 mg once daily. Max: 320 mg daily.
Elderly: > 75 yr: Initially, 40 mg once daily. CrCl (ml/min) Dosage Recommendation <20 Initiate at 40 mg once daily. Hepatic impairment: Mild to moderate impairment: Initial dose 40 mg once daily; max: 80 mg once daily. Severe hepatic impairment, cirrhosis, or biliary obstruction: contra-indicated. Oral Heart failure
Adult: 40 mg bid, may be increased to 160 mg bid if tolerated. Renal impairment: Use with caution. Hepatic impairment: Severe hepatic impairment, cirrhosis, or biliary obstruction: contra-indicated. Oral Post myocardial infarction
Adult: Start as early as 12 hr after MI in stable patients, at an initial dose of 20 mg bid, increased over a few wk up to 160 mg bid if tolerated. Renal impairment: Use with caution. Hepatic impairment: Mild to moderate: max: 80 mg bid. Patients with severe hepatic impairment, cirrhosis or biliary obstruction: Avoid. Special Populations: Care should be exercised with dosing of Valtensin in patients with hepatic or severe renal impairment. Moderate to severe renal impairment (creatinine clearance < 20 mL/min), intravascular vol depletion or hepatic impairment: 40 mg once daily.