Tensar: Each film coated tablet contains Valsartan USP 80 mg.
Pharmacology: Properties & effects: Valsartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis.
Pharmacokinetics: Absorption: Valsartan peak plasma concentration is reached 2 to 4 hours after dosing. Absolute bioavailability for Tensar is about 25% (range 10%-35%). Food decreases the exposure (as measured by AUC) to valsartan by about 40% and peak plasma concentration (Cmax) by about 50% AUC and Cmax values of valsartan increase approximately linearly with increasing dose over the clinical dosing range. Valsartan does not accumulate appreciably in plasma following repeated administration.
Metabolism and Elimination: Valsartan, when administered as an oral solution, is primarily recovered in feces (about 83% of dose) and urine (about 13% of dose). The recovery is mainly as unchanged drug, with only about 20% of dose recovered as metabolites. The primary metabolite, accounting for about 9% of dose, is valeryl 4-hydroxy valsartan. The enzymes responsible for valsartan metabolism have not been identified but do not seem to be CYP 450 isozymes.
Special Population: Pediatric: The pharmacokinetics of valsartan has not been investigated in patients < 18 years of age.
Geriatric: Exposure (measured by AUC) to valsartan is higher by 70% and the half-life is longer by 35% in the elderly than in the young. No dosage adjustment is necessary.
Gender: Pharmacokinetics of valsartan does not differ significantly between males and females.
Heart Failure: The average time to reach peak concentration and elimination half-life of valsartan in heart failure patients are similar to that observed in healthy volunteers. AUC and Cmax values of valsartan increase linearly and are almost proportional with increasing dose over the clinical dosing range (40 to 160 mg twice a day). The average accumulation factor is about 1.7. The apparent clearance of valsartan following oral administration is approximately 4.5 L/h. Age does not affect the apparent clearance in heart failure patients.
Hypertension: Tensar (valsartan) is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
Heart Failure: Tensar is indicated for the treatment of heart failure (NYHA class II-IV) in patients who are intolerant of angiotensin converting enzyme inhibitors. In a controlled clinical trial, Tensar significantly reduced hospitalizations for heart failure. There is no evidence that Tensar provides added benefits when it is used with an adequate dose of an ACE inhibitor.
Hypertension: The recommended dose of Tensar is 80 mg once daily, irrespective of race, age or gender. The antihypertensive effect is substantially present within 2 weeks and maximal effects are seen after 4 weeks. In patients whose blood pressure is not adequately controlled, the daily dose may be increased to 320 mg daily. Tensar may also be administered with other antihypertensive agents.
No dose adjustment is required for patients with renal impairment or for patients with hepatic insufficiency of non-biliary origin and without cholestasis.
Heart failure: The recommended starting dose of Tensar is 40 mg twice daily. Up titration to 80 mg and 160 mg twice daily should be done to the highest dose, as tolerated by the patient. Consideration should be given to reduce the dose of concomitant diuretics. The maximum daily dose administered in clinical trials is 320 mg in divided doses.
Evaluation of patients with heart failure should always include assessment of renal function.
The safety and efficacy of Tensar have not been established in children.
Limited data are available related to over dosage in humans. The most likely manifestations of over dosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Valsartan is not removed from the plasma by hemodialysis.
Tensar (valsartan) is contraindicated in patients who are hypersensitive to any component of this product.
Renal Insufficiency: There is no apparent correlation between renal function (measured by creatinine clearance) and exposure (measured by AUC) to valsartan in patients with different degrees of renal impairment.
Hepatic Insufficiency: On average, patients with mild-to-moderate chronic liver disease have twice the exposure (measured by AUC values) to valsartan of healthy volunteers (matched by age, sex and weight). In general, no dosage adjustment is needed in patients with mild-to-moderate liver disease. Care should be exercised in patients with liver disease.
Concomitant Therapy in Patients with Heart Failure: In patients with heart failure, concomitant use of Tensar, an ACE inhibitor, and a beta blocker is not recommended. In the Valsartan Heart Failure Trial, this triple combination was associated with an unfavorable heart failure.
Due to the mechanism of action of angiotensin II antagonists, a risk for the fetus can not be excluded. In utero exposure to ACE inhibitors given to pregnant women during the 2nd and 3rd trimesters has been reported to cause injury and death to the developing fetus. As for any drug that also acts directly on the renin-angiotensin-aldosterone system, Tensar should not be used during pregnancy. If pregnancy is detected during therapy, Tensar should be discontinued as soon as possible.
It is not known whether Tensar is excreted in human milk. Valsartan was excreted in the milk of lactating rats. Thus it is not advisable to use Tensar in lactating mothers.
In general treatment with valsartan is well tolerated. Some adverse reaction such as dizziness, insomnia, headache, fatigue, diarrhea, dyspepsia, nausea, abdominal pain, sinusitis, etc. may be observed.
No clinically significant pharmacokinetic interactions were observed when valsartan was co-administered with amlodipine, atenolol, cimetidine, digoxin, furosemide, glyburide, hydrochlorothiazide or indomethacin.
Store in a cool and dry place below 30°C. Protect from light.
C09CA03 - valsartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
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