Table of Contents
What is Valsartan?
Valsartan is an active ingredient used for the treatment of High blood pressure, Heart Failure, Heart Attack and Left Ventricular Dysfunction.
The brand names of Valsartan in the United States are: Diovan, Prexxartan.
Valsartan Mechanism of Action (MOA)
Inhibits the effect of angiotensin II on blood pressure, renal blood flow and aldosterone secretion.
Therapeutic indications, uses and benefits of Valsartan
High blood pressure essential (adults) and arterial hypertension (children and adolescents from 6-18 years).
Recent acute myocardial infarction (clinically stable patients with symptomatic heart failure or asymptomatic left ventricular systolic dysfunction after recent AMI within the last 12 h-10 days).
Symptomatic heart failure in adults when ACEi cannot be used, or as an added treatment to ACEi when ß-blockers cannot be used.
Dosage of Valsartan
Valsartan (Solution 4 mg/1mL, Tablet: 40 mg, 80 mg, 160 mg, 320 mg).
Oral.
Adults:
– High blood pressure essential: 80 mg/day.
If control is not obtained, increase to 160 mg/day; maximum 320 mg.
– High blood pressure (children and adolescents 6-18 years).
Tablets: 40 mg/day (p.c. <35 kg); 80 mg/day (p.c. 35 kg or more). Maximum recommended: ≥18 kg to <35 kg: 80 mg; ≥35 kg to <80 kg: 160 mg; ≥80 kg to ≤160 kg: 320 mg.
Oral solution (children unable to swallow tablets): 20 mg/day (body weight <35 kg); 40 mg/day (body weight 35 kg or more); maximum 80 mg. The oral solution is not bioequivalent to the tablet formulation.
Mild-moderate liver failure: maximum 80 mg.
– Recent AMI (clinically stable): start 12 hours into AMI with 20 mg/2 times daily, adjusted to 40 mg, 80 mg and 160 mg/2 times daily in subsequent weeks; maximum 160 mg/2 times daily.
– Heart failure: initial 40 mg/2 times daily, adjust up to 80 mg and 160 mg/2 times daily at intervals of 2 weeks depending on tolerance; maximum 320 mg/day (in divided doses).
Mild-moderate liver failure without cholestasis: do not exceed 80 mg.
Mode of administration of Valsartan
Oral use.
Administer independently of meals and should be administered with water.
Contraindications of Valsartan
- Hypersensitivity.
- Severe liver failure.
- Biliary cirrhosis.
- Cholestasis.
- Second and third trimester of pregnancy.
- Concomitant use with aliskirene in patients with diabetes mellitus or renal insufficiency (TFG <60 ml/min/1,73m 2).
Warnings and precautions with Valsartan
- Kidney failure.
- Liver failure.
- Severe heart failure.
- Dialysis.
- Aortic or mitral stenosis or hypertrophic obstructive cardiomyopathy.
- Bilateral stenosis of the renal arteries or stenosis of the renal artery of a single functioning kidney increase the risk of hypotension and renal failure.
- Risk of symptomatic hypotension in patients with decreased Na and/or volume.
- Not recommended in recent renal transplant.
- Not recommended in primary hyperaldosteronism.
- Risk of hyperkalaemia (concomitant use with K-sparing diuretics, K supplements and salt substitutes containing K).
- Monitor serum K levels and kidney function.
- Not recommended triple combination (ACEi, ß-blocker and valsartan).
- Dual blockade of the renin-angiotensin-aldosterone system by combining aliskirene with an ACEi or AIIRA is not recommended.
- The use of aliskirene in combination with valsartan is contraindicated in patients with diabetes mellitus or renal failure (TFG <60 l/min/1,73m 2 ).
- Not recommended in children with renal insufficiency (Clcr <30 ml/min), nor undergoing dialysis.
- In children with mild-moderate liver failure (limited experience) not to exceed 80 mg.
- Risk of angioedema (including swelling of face, lips, pharynx and/or tongue).
Liver failure
Contraindicated in severe liver failure, biliary cirrhosis and cholestasis. Caution in mild-moderate liver failure without cholestasis, dose should not be > 80 mg. In children with mild to moderate liver failure should not exceed 80 mg.
Renal insufficiency
Caution in renal insufficiency and undergoing dialysis (lack of studies). Not recommended in children with renal insufficiency (Clcr <30 ml/min), nor undergoing dialysis; control renal function and K levels. Contraindicated in renal insufficiency (TFG <60 ml/min/1,73m 2 ) concomitant with aliskirene.
Interactions with Valsartan
- Increases toxicity of: lithium.
- Antihypertensive effect increased by: other antihypertensive.
- Antihypertensive effect attenuated by: NSAIDs (e.g. selective COX-2 inhibitors, ASA at doses > 3 g/day and non-selective NSAIDs).
- Concomitant administration with NSAIDs, monitoring of renal function and adequate hydration increase the risk of renal function impairment.
Pregnancy and Valsartan
Not recommended in first trimester. Contraindicated in the second and third trimester.
Induces fetotoxicity (decreased renal function, oligohydramnios, delay in cranial ossification) and neonatal toxicity (renal insufficiency, hypotension, hyperkalemia).
Breastfeeding
Since there is no information regarding use during lactation, it is recommended not to administer during this period. It is preferable to switch to a treatment with a better known safety profile during lactation, especially in newborns or premature infants.
Effects on driving ability
No studies have been conducted on the effect on driving ability. When driving or using machinery, it should be noted that occasional dizziness or fatigue may occur.
Adverse reactions and side effects of Valsartan
- Dizziness.
- Postural dizziness.
- Hypotension.
- Orthostatic hypotension.
- Renal failure and deterioration.
⭐⭐⭐⭐⭐ VIDEO OF VALSARTAN/DIOVAN (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: 80M03YXJ7I
ChemIDplus
DrugPortal
PubChem CID: 60846
NCI Thesaurus: C47781