Acute heart failure, Cardiomyopathy, Coronary artery disease, Diabetic nephropathy, Heart failure, Hypertension, Post myocardial infarction
Angiotensin-ll receptor blocker
Valsartan is an oral medication that belongs to a class of drugs called angiotensin receptor blockers (ARBs). It is orally active and specific angiotensin II antagonist acting on the AT1 subtype. Angiotensin's attachment to the receptors cause the blood vessels to narrow (vasoconstrict) which leads to an increase in blood pressure (hypertension). Valsartan blocks the angiotensin II receptor. By blocking the action of angiotensin, Valsartan dilates blood vessels and reduces blood pressure without affecting pulse rate. Valsartan has much greater affinity (about 20,000-fold) for the AT1 receptor than for the AT2 receptor. It does not bind or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Hypertension- Adult: Initially, 80 mg once daily, may be increased to 160 mg once daily if needed. Max: 320 mg once daily. Child: As tab: ≥6 yr <35 kg: Initially, 40 mg once daily. Max: 80 mg once daily; 35-80 kg: Initially, 80 mg once daily. Max: 160 mg once daily; >80 kg: Initially, 80 mg once daily. Max: 320 mg once daily. As oral soln: Started at half the equivalent tab dose in valsartan-naive patients. If switching from tab to oral soln, the dose should be halved; if switching from soln to tab, same dose should be used initially. Dose should be titrated further according to response. Elderly: No dosage adjustment needed. Post-myocardial infarction- Adult: Start as early as 12 hr after MI in stable patients at an initial dose of 20 mg bid, doubled at intervals over a few wk up to 160 mg bid if tolerated. Elderly: No dosage adjustment needed. Heart failure- Adult: Initially, 40 mg bid, may be increased to 160 mg bid if tolerated. Elderly: No dosage adjustment needed.
No drug interactions of clinical significance have been found. Compounds which have been studied in clinical trials include Cimetidine, Warfarin, Furosemide, Digoxin, Atenolol, Indomethacin, Hydrochlorothiazide, Amlodipine and Glibenclamide
As Valsartan is not metabolized to a significant extent, clinically relevant drug-drug interactions in the form of metabolic induction or inhibition of the cytochrome P450 system are not expected with Valsartan. Although valsartan is highly bound to plasma proteins, in vitrostudies have not shown any interaction at this level with a range of molecules which are also highly protein bound, such as Diclofenac, Furosemide, and Warfarin. Concomitant use of potassium sparing diuretics (e.g., Spironolactone, Triamterene, Amiloride) potassium supplements, or salt substitutes containing potassium may lead to increase in serum potassium. If co medication is considered necessary, caution is advisable
Hypersensivity to Valsartan or any of the components of the product. Patients with renal artery stenosis, heart failure, aortic or mitral stenosis, severe Na and/or volume depletion. Renal and mild to moderate hepatic impairment. Lactation.
The overall incidence of adverse experiences with Valsartan was similar to placebo. The common side effects are headache, dizziness, rhinitis, sinusitis, pharyngitis, nausea, gastrointestinal upset, oedema and fatigue. Dose related orthostatic effects were seen in less than 1% of patients. An increase in the incidence of dizziness was observed in patients treated with Valsartan 320 mg compared to 80-160 mg.
Pregnancy: Due to the mechanisms of action of angiotensin II antagonists, a risk for the foetus cannot be excluded. In utero exposure to angiotensin converting enzyme (ACE) inhibitors given to pregnant women during the 2nd and 3rd trimesters has been reported to cause foetal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death. When pregnancy is detected, Valsartan should be discontinued as soon as possible. Lactation: It is not known whether Valsartan is excreted in human milk. Valsartan was excreted in the milk of lactating rats. Thus, it is not advisable to use Valsartan in lactating mothers.
Limited data are available related to overdosage in humans. The most likely manifestations of overdosage would be hypotension and tachycardia, bradycardia could occur from parasympathetic (vagal) stimulation. If excessive hypotension occurs, the patient should be placed in the supine position and if necessary, has to be given an intravenous infusion of normal saline.
Store between 15-30° C. Protect from moisture and heat.