Valsartan

Valsartan is an angiotensin II receptor antagonist, that is selective for the type I angiotensin receptor.

Valsartan

Valsartan; Diovan; Provas; Tareg; L-Valsartan

Co-Diovan, Diovan, Nebicard-V, Starval, Valent, Valent R, Valent R-5, Valent-H, Valfect, Valfect-H, Valzaar, Valzaar-H, Valzaar-SM

(2S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acid

Oral bioavailability 23%, Protein bound 94-97%.

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. Valsartan 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

NA

• May be used as a first line agent to delay progression of diabetic nephropathy.
• May be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. 

Angioedema; dizziness; headache; dose-related orthostatic hypotension; rash; hyperkalaemia; myalgia; respiratory tract disorders; back pain; GI disturbances; fatigue; increase in BUN and serum creatinine; abdominal pain; dry cough; LFT elevations.

• Increased risk of renal impairment and hyperkalemia with NSAIDs and cyclosporine.
• Increased risk of lithium toxicity.
• Increased risk of hypotension with general anaesthetics, clozapine, dopamine agonists and other antihypertensives.
• Increased risk of hyperkalaemia with potassium-sparing diuretics, potassium supplements, ACE inhibitors, and heparin.

Hypersensitivity; severe hepatic impairment, cirrhosis or biliary obstruction; primary hyperaldosteronism. Pregnancy (2nd and 3rd trimesters) and lactation.

Store between 15-30°C (59 - 86<249>F).

Molecular weight

435.5188

Molecular formula

C24H29N5O3

CAS number

137862-53-4

Precautions

Volume depletion; renal artery stenosis; monitor serum potassium concentrations; severe CHF; renal impairment; mild to moderate hepatic impairment. Elderly.