Valsartan GPO

Valsartan GPO





Full Prescribing Info
80 mg: Each tablet contains 80 mg of valsartan.
160 mg: Each tablet contains 160 mg of valsartan.
Excipients/Inactive Ingredients: 80 mg: Spray-dried mannitol, microcrystalline cellulose, povidone, croscarmellose sodium, magnesium stearate, hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol, iron oxide red, iron oxide yellow, iron oxide black.
160 mg: Spray-dried mannitol, microcrystalline cellulose, povidone, croscarmellose sodium, magnesium stearate, hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol, iron oxide yellow, sunset yellow aluminium lake, iron oxide red, indigo carmine aluminium lake.
Pharmacology: Pharmacodynamics: Mechanism of action: Valsartan is angiotensin II receptor (type AT1) antagonists (AIIRAs). Angiotensin II is a potent vasoconstrictor, the primary vasoactive hormone of renin-angiotensin system, and an important component in the pathophysiology of hypertension. Its effects are vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. 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 (e.g., vascular smooth muscle and the adrenal gland). The primary metabolite of valsartan is essentially inactive with an affinity for the AT1 receptor about 1/200 of valsartan itself.
Dose/concentration/time-pharmacodynamic response relationship: Data is not available.
Pharmacokinetics: Absorption: Bioavailability of valsartan is about 25%. Time to peak plasma concentration of valsartan is 2-4 hours. Food decreases Cmax of valsartan by about 50% and its AUC by about 40%.
Distribution: Volume of distribution of valsartan is 17 L. Protein binding of valsartan is 95%, primarily with albumin.
Metabolism: Approximately 20% of valsartan is converted to metabolites.
Elimination: Valsartan is recovered in feces by approximately 83% and in urine by 13%. The terminal half-life of valsartan is approximately 6 hours. The total plasma clearance and renal clearance are about 2 L/h and 0.62 L/h, respectively.
Special populations: Renal function impairment: Valsartan is not removed from the plasma by hemodialysis. In the case of severe renal disease, exercise care with dosing of valsartan.
Hepatic function impairment: On average, patients with mild to moderate chronic liver disease have twice the exposure (measured by AUC values) to valsartan of healthy volunteers.
Elderly: AUC of valsartan is 70% higher and the half-life is 35% longer in elderly patients than in younger patients.
Toxicology: Mechanism of toxicity: Data is not available.
Hypertension: Valsartan is indicated for the treatment of hypertension, to lower blood pressure. It may be used alone or in combination with other antihypertensive agents.
Heart failure: Valsartan is indicated for the treatment of heart failure (New York Heart Association [NYHA] class II-IV).
Post-myocardial infarction (MI): Valsartan is indicated to reduce cardiovascular mortality in clinically stable patients with left ventricular failure or left ventricular dysfunction following MI.
Dosage/Direction for Use
Recommended dose: Adults: Hypertension: Usual dosage: 80 to 320 mg once daily.
Maximum dose: 320 mg/day.
Initial dosage: 80 or 160 mg once daily when used as monotherapy in patients who are not volume depleted. Patients requiring greater reductions may be started at a higher dose.
Dosage adjustment: If additional antihypertensive effect is required, the dose may be increased to a maximum of 320 mg/day, or a diuretic may be added.
Heart failure: Maximum dose: 320 mg/day.
Initial dosage: 40 mg twice daily.
Dosage titration: Up titration to 80 and 160 mg twice daily should be done to the highest dose as tolerated by the patient.
Concomitant therapy: Consider reducing the dose of concomitant diuretics.
Post-myocardial infarction: Initial dosage: 20 mg twice daily initiated as early as 12 hours after an MI.
Dosage titration: Patients may be up-titrated within 7 days to 40 mg twice daily, with subsequent titrations to a target maintenance dosage of 160 mg twice daily, as tolerated by the patient. If symptomatic hypotension or renal function impairment occurs, consider a dosage reduction.
Concomitant therapy: Valsartan may be given with other standard post-MI treatments, including thrombolytics, aspirin, beta-blockers, and statins.
Children 6 to 16 years of age: Hypertension: Initial dosage: 1.3 mg/kg once daily (up to 40 mg total).
Dosage adjustment: Adjust dosage according to blood pressure response. Dosages higher than 2.7 mg/kg (up to 160 mg) once daily have not been studied.
Elderly: Modification of valsartan dosage is not necessary for elderly patients.
Renal function impairment: Modification of valsartan dosage is not necessary for patients with mild to moderate renal impairment. Valsartan has not been studied in patients with creatinine clearances (CrCl) of less than 10 mL/minute and should be used with caution in adults with severe renal impairment.
Hepatic function impairment: Modification of valsartan dosage is not necessary for patients with mild to moderate chronic liver disease. Valsartan should be used with caution in patients with hepatic impairment.
Mode of administration: Valsartan GPO tablet is administered orally and may be administered with or without food.
Data is not available.
Valsartan GPO tablet is contraindicated in patients with hypersensitivity to valsartan or any component of this product. Do not coadminister aliskiren with Valsartan GPO tablet in patients with diabetes mellitus.
Special Precautions
Hypotension/volume- or salt-depleted patients: In patients who are intravascularly volume depleted (e.g., those treated with diuretics), symptomatic hypotension may occur. Correct these conditions prior to administration or start treatment under close medical supervision with a reduced dose.
Hyperkalemia: Hyperkalemia may occur in patients receiving valsartan, especially in those with heart failure and preexisting renal impairment. Dosage reduction or discontinuance of valsartan therapy may be required. Risk factors include renal dysfunction, diabetes mellitus, or concomitant use of potassium-sparing diuretics, potassium supplements, and/or potassium containing salts.
Surgery: Hypotension may occur during major surgery and anesthesia in patients treated with angiotensin II receptor antagonists due to blockade of the renin-angiotensin system.
Aortic/mitral stenosis: Use caution in patients with significant aortic/mitral stenosis.
ACE inhibitors and renin inhibitors: Concomitant use of an ACE inhibitor or renin inhibitor (e.g., Aliskiren) is associated with an increased risk of hypotension, hyperkalemia, and renal dysfunction. Concomitant use with aliskiren should be avoided in patients with glomerular filtration rate (GFR) less than 60 mL/minute and is contraindicated in patients with diabetes mellitus (regardless of GFR).
Renal effects: As a consequence of inhibiting the renin-angiotensin system, changes in renal function, including acute renal failure, may occur. Consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function.
Renal artery stenosis: Use with caution in patients with unstented unilateral/bilateral renal artery stenosis.
Renal function impairment: Use caution with preexisting renal insufficiency.
Hepatic function impairment: Valsartan should be used with caution in patients with obstructive biliary disease or hepatic impairment since the drug is eliminated primarily by biliary excretion and clearance of the drug may be reduced.
Sensitivity reactions: Sensitivity reactions, including various anaphylactoid reactions and/or angioedema, have been reported in patients receiving angiotensin II receptor antagonists, including valsartan. These drugs should be used with extreme caution in patients with a history of angioedema associated with or unrelated to ACE inhibitor or angiotensin II receptor antagonist therapy. Valsartan should not be readministered to patients with a history of angioedema. Prolonged frequent monitoring may be required, especially if tongue, glottis, or larynx are involved. Discontinue therapy immediately if angioedema occurs.
Effect on ability to drive and use machine: Data is not available.
Use in Pregnancy: Fetal toxicity: Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. When pregnancy is detected, discontinue valsartan as soon as possible.
Use in Children: Valsartan is not recommended for pediatric patients younger than 6 years.
Use In Pregnancy & Lactation
Pregnancy: US Pregnancy category: D.
Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected.
There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Labor and delivery: Data is not available.
Lactation: It is not known if valsartan is excreted in human breast milk. Because of the potential for adverse effects on breast-feeding infants, decide whether to discontinue breast-feeding or discontinue valsartan, taking into account the importance of the drug to the mother.
Adverse Reactions
The following adverse reactions were found in patients treated with valsartan (Pooled data from separate studies, n = 2,316).
Common adverse events (1-10%): Central nervous system (CNS): Dizziness (>1%), fatigue (2%), headache (>1%).
Gastrointestinal tract system (GI): Abdominal pain (2%), diarrhea (>1%), nausea/vomiting (>1%).
Musculoskeletal: Arthralgia (>1%).
Respiratory: Cough (>1%), pharyngitis (>1%), rhinitis (>1%), sinusitis (>1%), upper respiratory tract infection (>1%).
Miscellaneous: Edema (>1%), viral infection (3%).
Uncommon adverse events (0.1-1%): Cardiovascular system (CVS): Dose-related orthostatic effects (<1%).
Central nervous system (CNS): Anxiety/nervousness (>0.2%), insomnia (>0.2%), paresthesia (>0.2%), somnolence (>0.2%).
Gastrointestinal tract system (GI): Constipation (>0.2%), dry mouth (>0.2%), dyspepsia/heartburn (>0.2%), flatulence (>0.2%).
Musculoskeletal: Muscle cramp (>0.2%), myalgia (>0.2%), pain (>0.2%).
Miscellaneous: Allergic reaction (>0.2%), asthenia (>0.2%), dyspnea (>0.2%), impotence (>0.2%), palpitations (>0.2%), pruritus (>0.2%), rash (>0.2%), vertigo (>0.2%).
Less frequently adverse events: Angioedema, anorexia, chest pain, syncope, and vomiting.
Lab test abnormalities: Hepatic: Occasional elevations (more than 150% in valsartan-treated patients) of liver enzymes or serum bilirubin have occurred. Three patients (less than 0.1%) treated with valsartan discontinued treatment for elevated liver chemistries.
Renal: Minor increases in BUN or serum creatinine were observed in 0.8% of patients taking valsartan.
Hematologic: Decreases of more than 20% in hemoglobin and hematocrit were observed in 0.4% and 0.8%, respectively, of valsartan patients versus 0.1% and 0.1% with placebo. One valsartan patient discontinued treatment for microcytic anemia. Neutropenia was observed in 1.9% of patients treated with valsartan and 0.8% of patients treated with placebo.
Serum potassium: Increases of more than 20% in serum potassium were observed in 4.4% of valsartan-treated patients versus 2.9% of placebo-treated patients.
Drug Interactions
See Table.

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Drug/Food interactions: Food decreases the peak plasma concentration and extent of absorption of valsartan by 50% and 40%, respectively.
Do not store above 30°C. Store in the original container.
ATC Classification
C09CA03 - valsartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
FC tab 80 mg (pink, biconvex, round, one side debossed with "80" and the other side bisected) x 3 x 10's. 160 mg (orange, biconvex, oblong, one side debossed with "160" and the other side bisected) x 3 x 10's.
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