Valsartan


Generic Medicine Info
Indications and Dosage
Oral
Heart failure
Adult: For the treatment of NYHA class II-IV cases in patients who cannot tolerate ACE inhibitors: Initially, 40 mg bid, may be increased at intervals of at least 2 weeks up to 160 mg bid according to the patient's tolerability.

Oral
Post-myocardial infarction
Adult: For the reduction of CV mortality in clinically stable patients with left ventricular dysfunction or failure after a recent MI: Therapy may be initiated as early as 12 hours following MI. Initially, 20 mg bid, may be doubled at intervals over the next few weeks up to Max of 160 mg bid according to the patient's tolerability.

Oral
Hypertension
Adult: Initially, 80 mg once daily, may be increased to 160 mg once daily according to clinical response. Max: 320 mg once daily.
Child: ≥6 years As tab: 18-<35 kg: Initially, 40 mg once daily, may be increased up to a Max of 80 mg once daily if needed; ≥35 kg: Initially, 80 mg once daily. Max: 35-<80 kg: 160 mg daily; ≥80 kg: 320 mg daily. As oral solution: <35 kg: Initially, 20 mg once daily. Max: 40 mg once daily; ≥35 kg: Initially, 40 mg once daily. Max: 80 mg once daily. Doses should be adjusted according to clinical response and tolerability. If switching from tab to the oral solution is clinically essential, the dose should be halved; if switching from oral solution to tab, initially the same dose in mg must be used then titrated further based on blood pressure response. Dosage recommendations may vary among individual products or between countries (refer to specific product or local guidelines).
Hepatic Impairment
Mild to moderate: Max: 80 mg daily. Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Biliary cirrhosis, cholestasis. Severe hepatic impairment. Pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2).
Special Precautions
Patient with aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy, post-MI, heart failure; bilateral or unilateral renal artery stenosis, volume and/or Na depletion; ascites due to cirrhosis or refractory ascites, primary hyperaldosteronism; history of angioedema. Patients undergoing surgery. Black patients. The oral solution of valsartan has higher bioavailability and peak plasma concentration than the tab/cap preparation; therefore, tab/cap and oral solution are not bioequivalent on a mg:mg basis. Renal and mild to moderate hepatic impairment. Children. Lactation.
Adverse Reactions
Significant: Acute kidney injury, increased serum creatinine, hyperkalaemia, hypotension, angioedema.
Blood and lymphatic system disorders: Neutropenia, thrombocytopenia.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea.
General disorders and administration site conditions: Fatigue, asthenia.
Immune system disorders: Hypersensitivity including serum sickness.
Investigations: Increased liver enzymes, increased BUN, decreased Hb and haematocrit.
Metabolism and nutrition disorders: Hyponatraemia.
Musculoskeletal and connective tissue disorders: Back pain, myalgia, arthralgia.
Nervous system disorders: Dizziness, headache, orthostatic dizziness.
Respiratory, thoracic and mediastinal disorders: Cough.
Skin and subcutaneous tissue disorders: Rash, pruritus, dermatitis bullous.
Vascular disorders: Syncope, orthostatic hypotension, vasculitis.
Patient Counseling Information
This drug may cause dizziness or weariness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure, electrolytes (e.g. serum K levels), and renal function regularly during therapy. Assess for signs of angioedema.
Overdosage
Symptoms: Marked hypotension that may result in a depressed level of consciousness, circulatory collapse and/or shock; tachycardia or bradycardia. Management: Symptomatic and supportive treatment. Induce vomiting for recent ingestion. If hypotension occurs, place the patient in a supine position, then administer normal saline IV infusion to facilitate blood volume correction as needed.
Drug Interactions
Increased serum K levels with K-sparing diuretics (e.g. spironolactone, triamterene, amiloride), K supplements, K-containing salt substitutes, or other agents that may elevate serum K levels (e.g. heparin). May increase serum lithium concentration and toxicity. May reduce the antihypertensive effect and increase the risk of worsening renal function with NSAIDs including aspirin and selective COX-2 inhibitors. Systemic exposure may be increased with inhibitors of OATP1B1 (e.g. rifampicin, ciclosporin) and multidrug resistance protein 2 (MRP2) such as ritonavir.
Potentially Fatal: Increased risk of hypotension, hyperkalaemia and reduced renal function (including acute renal failure) with aliskiren and ACE inhibitors.
Food Interaction
Reduced exposure and peak plasma concentration with food; however, reduced exposure is not accompanied by clinically significant decrease in therapeutic effect.
Lab Interference
May result in false-negative aldosterone/renin ratio (ARR).
Action
Description:
Mechanism of Action: Valsartan is an angiotensin II receptor antagonist. It selectively inhibits the binding of angiotensin II to the angiotensin II type 1 (AT1) receptors found within many tissues (e.g. vascular smooth muscle, adrenal gland), thereby blocking the vasoconstricting and aldosterone-secreting effects of angiotensin II. Additionally, this action leads to a more efficient inhibition of the angiotensin II CV effects and fewer adverse effects than ACE inhibitors.
Onset: Approx 2 hours.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed after oral administration. Reduced exposure and peak plasma concentration with food. Absolute bioavailability: Approx 23% (tab/cap); approx 39% (oral solution). Time to peak plasma concentration: 2-4 hours (tab/cap); 1-2 hours (oral solution).
Distribution: Plasma protein binding: 94-97%, mainly to serum albumin.
Metabolism: Metabolised minimally in the liver by CYP2C9 into the inactive valeryl 4-hydroxy valsartan metabolite.
Excretion: Via faeces (approx 83%) and urine (approx 13%) as unchanged drug. Elimination half-life: Approx 6 hours.
Chemical Structure

Chemical Structure Image
Valsartan

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 60846, Valsartan. https://pubchem.ncbi.nlm.nih.gov/compound/Valsartan. Accessed Oct. 25, 2023.

Storage
Store between 15-30°C. Protect from moisture.
MIMS Class
Angiotensin II Antagonists
ATC Classification
C09CA03 - valsartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
References
Anon. Valsartan. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 19/09/2023.

Anon. Valsartan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/09/2023.

Buckingham R (ed). Valsartan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/09/2023.

Diovan 3 mg/mL Oral Solution (Novartis Ireland Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/01/2023.

Diovan 40 mg Film-coated Tablet (Novartis Corporation [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 05/01/2023.

Joint Formulary Committee. Valsartan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/09/2023.

Paediatric Formulary Committee. Valsartan. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 26/09/2023.

Valsartan 160 mg Capsules (Teva UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 26/09/2023.

Valsartan 80 mg Film-coated Tablets (Crescent Pharma Limited). https://products.mhra.gov.uk. MHRA. Accessed 21/09/2023.

Valsartan Oral Solution (Lifsa Drugs LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 05/01/2023.

Valsartan Tablets (Lupin Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 19/09/2023.

Disclaimer: This information is independently developed by MIMS based on Valsartan from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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