Valsartan

Brand names: Diovan®

Chemical formula:

Español:
• Valsartán, Tableta oral

Valsartan Oral tablet

What is this medicine?

VALSARTAN is used to treat high blood pressure. This drug is also used to treat patients with heart failure and patients who have had a heart attack.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•heart failure
•kidney disease
•liver disease
•an unusual or allergic reaction to valsartan, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. This medicine can be taken with or without food. Take your medicine at regular intervals. Do not take it more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 6 years for selected conditions, precautions do apply.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

•blood pressure medicines
•diuretics, especially triamterene, spironolactone or amiloride
•potassium salts or potassium supplements

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Check your blood pressure as directed. Ask your doctor or health care professional what your blood pressure should be and when you should contact him or her. Call your doctor or health care professional if you notice an irregular or fast heart beat.

Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child, particularly in the second or third trimester. Talk to your health care professional or pharmacist for more information.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this drug affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can make you more drowsy and dizzy. Avoid alcoholic drinks.

Avoid salt substitutes unless you are told otherwise by your doctor or health care professional.

Do not treat yourself for coughs, colds, or pain while you are taking this medicine without asking your doctor or health care professional for advice. Some ingredients may increase your blood pressure.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•confusion, dizziness, light headedness or fainting spells
•decreased amount of urine passed
•difficulty breathing or swallowing, hoarseness, or tightening of the throat
•fast or irregular heart beat, palpitations, or chest pain
•skin rash, itching
•swelling of your face, lips, tongue, hands, or feet

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•cough
•decreased sexual function
•headache
•nausea or stomach pain

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep your medicine container tightly closed and protect from moisture. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Valsartan
Systematic (IUPAC) name
(S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acid
Identifiers
CAS number	137862-53-4
ATC code	C09CA03
PubChem	60846
DrugBank	APRD00133
Chemical data
Formula	C24H29N5O3
Mol. mass	435.519 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	25%
Protein binding	95%
Metabolism	?
Half life	6 hours
Excretion	Renal 30%, biliary 70%
Therapeutic considerations
Pregnancy cat.	D
Legal status	℞ Prescription only
Routes	oral
Y(what is this?)  (verify)

Valsartan is an angiotensin II receptor antagonist (more commonly called an "ARB", which stands for angiotensin receptor blocker), with particularly high affinity for the type I (AT₁) angiotensin receptor. In the U.S., valsartan is indicated for treatment of high blood pressure, congestive heart failure (CHF), or post-myocardial infarction (MI).^{[citation needed]}

Valsartan is marketed by Novartis under the trade name Diovan. In India, it is marketed by CIPLA under the trade name Valtan and by Torrent Pharmaceuticals under the trade name Valzaar. In 2005, Diovan was prescribed more than 12 million times in the United States. Global sales approx $6.0bn.^{[citation needed]} Patent expires in 2012.^{[citation needed]}

A study released by the Journal of Clinical Investigation in 2007 found some efficacy in the use of valsartan in the treatment and prevention of Alzheimer's Disease although such use is considered to be highly experimental.^[1]

Contents 1 Administration 2 Myocardial infarction controversy 3 Side effects 4 See also 5 References 6 External links

Administration

Oral tablets, containing 40 mg (scored), 80 mg, 160 mg or 320 mg of valsartan. Usual dosage ranges from 40–320 mg daily.

In some markets available as a hard gelatin capsule, containing 40 mg, 80 mg, or 160 mg of valsartan.

Diovan HCT contains a combination of valsartan and hydrochlorothiazide but, unlike Diovan, is only indicated for hypertension, not for CHF or post-MI.^{[citation needed]}

Myocardial infarction controversy

Whether angiotensin receptor blockers may or may not increase the risk of myocardial infarction was announced in the BMJ^[2] and was more recently debated in the medical journal of the American Heart Association.^[3][4] To date^[when?], there is no consensus on whether ARBs have a tendency to increase MI, but there is also no substantive evidence to indicate that ARBs are able to reduce MI.

In the VALUE trial, the angiotensin II receptor blocker valsartan produced a statistically significant 19% (p=0.02) relative increase in the prespecified secondary end point of myocardial infarction (fatal and non-fatal) compared with amlodipine.^[5]

The CHARM-alternative trial showed a significant +52% (p=0.025) increase in myocardial infarction with candesartan (versus placebo) despite a reduction in blood pressure.^[6]

Indeed, as a consequence of AT1 blockade, ARBs increase Angiotensin II levels several-fold above baseline by uncoupling a negative-feedback loop. Increased levels of circulating Angiotensin II result in unopposed stimulation of the AT2 receptors, which are, in addition upregulated. Unfortunately, recent data suggest that AT2 receptor stimulation may be less beneficial than previously proposed and may even be harmful under certain circumstances through mediation of growth promotion, fibrosis, and hypertrophy, as well as proatherogenic and proinflammatory effects.^[7][8][9]

Side effects

Most commonly, headache and dizziness. Sensitivity to sun light and bright artificial light.

There is a case report of a stillbirth in which valsartan is implicated.^[10]

See also

Angiotensin Receptor Blockers: Drug discovery and development

References

1. ^ Wang J, Ho L, Chen L, et al. (November 2007). "Valsartan lowers brain beta-amyloid protein levels and improves spatial learning in a mouse model of Alzheimer disease". J. Clin. Invest. 117 (11): 3393–402. doi:10.1172/JCI31547. PMID 17965777. PMC 2040315. http://content.the-jci.org/articles/view/31547. Retrieved 2009-11-11. 
2. ^ Verma S, Strauss M (November 2004). "Angiotensin receptor blockers and myocardial infarction". BMJ 329 (7477): 1248–9. doi:10.1136/bmj.329.7477.1248. PMID 15564232. 
3. ^ Strauss MH, Hall AS (August 2006). "Angiotensin receptor blockers may increase risk of myocardial infarction: unraveling the ARB-MI paradox". Circulation 114 (8): 838–54. doi:10.1161/CIRCULATIONAHA.105.594986. PMID 16923768. 
4. ^ Tsuyuki RT, McDonald MA (August 2006). "Angiotensin receptor blockers do not increase risk of myocardial infarction". Circulation 114 (8): 855–60. doi:10.1161/CIRCULATIONAHA.105.594978. PMID 16923769. 
5. ^ Julius S, Kjeldsen SE, Weber M, et al. (June 2004). "Outcomes in hypertensive patients at high cardiovascular risk treated with regimens based on valsartan or amlodipine: the VALUE randomised trial". Lancet 363 (9426): 2022–31. doi:10.1016/S0140-6736(04)16451-9. PMID 15207952. 
6. ^ Granger CB, McMurray JJ, Yusuf S, et al. (September 2003). "Effects of candesartan in patients with chronic heart failure and reduced left-ventricular systolic function intolerant to angiotensin-converting-enzyme inhibitors: the CHARM-Alternative trial". Lancet 362 (9386): 772–6. doi:10.1016/S0140-6736(03)14284-5. PMID 13678870. 
7. ^ Levy BI (September 2005). "How to explain the differences between renin angiotensin system modulators". Am. J. Hypertens. 18 (9 Pt 2): 134S–141S. doi:10.1016/j.amjhyper.2005.05.005. PMID 16125050. 
8. ^ Levy BI (January 2004). "Can angiotensin II type 2 receptors have deleterious effects in cardiovascular disease? Implications for therapeutic blockade of the renin-angiotensin system". Circulation 109 (1): 8–13. doi:10.1161/01.CIR.0000096609.73772.C5. PMID 14707017. 
9. ^ Reudelhuber TL (December 2005). "The continuing saga of the AT2 receptor: a case of the good, the bad, and the innocuous". Hypertension 46 (6): 1261–2. doi:10.1161/01.HYP.0000193498.07087.83. PMID 16286568. 
10. ^ Briggs GG, Nageotte MP (2001). "Fatal fetal outcome with the combined use of valsartan and atenolol". The Annals of Pharmacotherapy 35 (7-8): 859–61. doi:10.1345/aph.1A013. PMID 11485133. 

External links

• PubMed:Valsartan
• Official Diovan Site

v • d • e Antihypertensives: agents acting on the renin-angiotensin system (C09) ACE inhibitors ("-pril") Sulfhydryl-containing: Captopril • Zofenopril Dicarboxylate-containing: Enalapril# • Ramipril • Quinapril • Perindopril • Lisinopril • Benazepril Phosphonate-containing: Fosinopril Other/ungrouped: Alacepril • Cilazapril • Delapril • Imidapril • Moexipril • Rentiapril • Spirapril • Temocapril • Trandolapril AIIRAs/ ("-sartan") Azilsartan • Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan Renin inhibitors/ ("-kiren") Aliskiren • Remikiren #WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III

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