Valsartan

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Valsartan.jpg

[edit] MECHANISM OF ACTION

Valsartan is a member of a family of drugs called angiotensin receptor blockers (ARBs).

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include 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, such as vascular smooth muscle and the adrenal gland.

[edit] INDICATIONS

  • Treatment of hypertension (To reduce the risk of cardiovascular events, primarily strokes and myocardial infarctions)
  • Treatment of heart failure
  • Reduction of cardiovascular mortality in clinically stable patients with left ventricular failure or left ventricular dysfunction following myocardial infarction

[edit] DOSAGE

  • Hypertension:
    • Adult: 80-320 mg once daily
    • Pediatric (6-16 years): 1.3-2.7 mg/kg once daily (up to 40-160 mg total)
  • Heart Failure: starting dose is 40 mg twice daily, dosage range from 40-160 mg twice daily
  • Post-Myocardial Infarction: starting dose is 20 mg twice daily, dosage range from 20-160 mg twice daily

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 40 mg, 80 mg, 160 mg, 320 mg

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to any component
  • Contraindicated in patients with severe hepatic impairment.
  • Pregnancy and lactation
  • Do not coadminister Aliskiren with Valsartan in patients with diabetes (see interactions)

[edit] WARNINGS AND PRECAUTIONS

[edit] INTERACTIONS

  • Aliskiren: Dual blockade of the renin-angiotensin-aldosterone system like taking an Angiotensin II receptor antagonist plus a direct renin inhibitors (Aliskiren) is associated with increased risks of hypotension, syncope, hyperkalemia, and kidney damage compared to monotherapy.
  • Drugs that inhibit the renin-angiotensin system including Valsartan can cause hyperkaliemia. Potassium-sparing diuretics (Amiloride, Eplerenone, Potassium canrenoate, Spironolactone, Triamterene) and potassium supplements may have an additive effect on potassium retention, resulting in hyperkalemia and, in heart failure patients may lead to increases in serum creatinine. If co-medication is considered necessary, monitoring of serum potassium is advisable.
  • NSAIDS: Caution is advised if non steroidal antiinflammatory drugs NSAIDs are prescribed with angiotensin II receptor antagonists, including Valsartan. (Concomitant use of NSAIDS may result in decreased angiotensin II receptor antagonists effectiveness). In some patients with compromised renal function who are being treated with NSAIDS, the co-administration of angiotensin II receptor antagonists may result in further deterioration of renal function. Cases of acute renal failure, usually reversible, have also been reported.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus, thus Valsartan should not be used during pregnancy or in women planning to become pregnant and is not advisable to use in breast-feeding mothers. If pregnancy is detected during therapy, Valsartan should be discontinued as soon as possible.

[edit] SIDE EFFECTS

hypotension, headache, dizziness, fatigue, hyperkalemia, abdominal pain, neutropenia, elevated liver enzymes and cough.

[edit] RELATED LINKS

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)