Import Your Data

FAQ

More QuickView FAQs

QuickView

0
Meta-
Analysis

Bookmark Forward

QuickView for Valsartan (compound)

Summary
General Info

PubChem

PubChem Compound 5284633

PubChem Compound 5284633

Name:	valsartan
PubChem Compound ID:	5284633
Molecular formula:	C₂₄H₂₉N₅O₃
Molecular weight:	435.519 g/mol
Synonyms:	137862-53-4; Valsartan

DrugBank

Identification

Name:	valsartan
Name (isomeric):	DB00177
Drug Type:	small molecule
Brand:	Valsarran, Diovan
Category:	Angiotensin II Receptor Antagonists, Antihypertensive Agents
CAS number:	137862-53-4

Pharmacology

Indication:	May be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Losartan may be also used as a second line agent in the treatment of congestive heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.
Pharmacology:	Valsartan belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Valsartan 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 regul... show more » Valsartan belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Valsartan 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. show less «
Mechanism of Action:	Valsartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure.... show more » Valsartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Valsartan is selective for AT1 and has virtually no affinity for AT2. Inhibition of aldosterone secretion may inhibit sodium and water reabsorption in the kidneys while decreasing potassium excretion. The primary metabolite of valsartan, valeryl 4-hydroxy valsartan, has no pharmacological activity. show less «
Absorption:	Absolute bioavailability = 23% with high variability
Protein binding:	94 - 97% bound to serum proteins, primarily serum albumin
Biotransformation:	Valsartan is excreted largely as unchanged drug (80%) and is minimally metabolized in humans. The primary circulating metabolite, 4-OH-valsartan, is pharmacologically inactive and produced CYP2C9. 4-OH-valsartan accounts for approximately 9% of the circulating dose of valsartan. Although valsartan is metabolized by CYP2C9, CYP-mediated drug-drug interactions between valsartan and other drugs is unlikely.
Route of elimination:	83% of absorbed valsartan is excreted in feces and 13% is excreted in urine, primarily as unchanged drug
Half Life:	The initial phase t_{1/2 α} is < 1 hour while the terminal phase t_{1/2 β} is 5-9 hours.
Clearance:	2 L/h [IV administration] 4.5 L/h [heart Failure patients receiving oral administration 40 to 160 mg twice a day]
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Amifostine	Additive hypotensive effects may occur. At chemotherapeutic doses of Amifostine, Valsartan should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
Rituximab	Additive hypotensive effects may occur. Increased risk of hypotension. Consider withholding Valsartan for 12 hours prior to administration of Rituximab.
Tobramycin	Increased risk of nephrotoxicity
Potassium	Increased risk of hyperkalemia
Eltrombopag	Eltrombopag may increase the therapeutic and/or toxic effects of Valsartan. Increased Valsartan serum concentrations may be caused by inhibition of hepatic uptake and decreased metabolism. Consider dose modification, alternate therapy or monitor for changes in the therapeutic and toxic effects of Valsartan if Eltrombopag is initiated, discontinued or dose changed.

Targets

Type-1 angiotensin II receptor

Enzymes

Cytochrome P450 2C9

Transporters

Solute carrier organic anion transporter family member 1B3

Solute carrier organic anion transporter family member 1B1

Carriers