Valsartan

What is Valsartan

Valsartan is a specific angiotensin II antagonist which selectively and competitively blocks the AT₁ receptor, which mediates the vasopressor and aldosterone effects of angiotensin II.

Unlike losartan, valsartan does not have an active metabolite or possess uricosuric effects. Valsartan is used to treatment hypertension in adults and children >= 6 years of age; it is also FDA-approved to treat heart failure in patients who are intolerant to ACE inhibitors.

Because valsartan does not inhibit angiotensin converting enzyme (ACE), it does not result in bradykinin accumulation which is theorized to cause the cough and angioedema associated with ACE inhibitors.

However, angioedema has been rarely associated with valsartan or other angiotensin II antagonists. Valsartan is effective for hypertension, either alone or in combination with other antihypertensive agents. Because AT₁ receptors are nearly saturated at the starting dose for most angiotensin II antagonists, the antihypertensive dose-response curve of these drugs are nonlinear, with proportionally small decreases in blood pressure attained with increased dosage. Greater antihypertensive efficacy is achieved by adding a small dose of a diuretic to the angiotensin II antagonist.

Modest reduction in blood pressure is achieved by increasing the dose of valsartan over the dosage range of 80—320 mg. Valsartan reduces left ventricular hypertrophy (LVH), although the clinical benefit associated with reducing LVH is not well established.

Limited data show that valsartan also reduces proteinuria in patients with hypertension and renal disease; however, larger clinical trials are needed to evaluate the comparative renoprotective efficacy and long-term benefits of valsartan versus ACE inhibitors in patients with renal disease or nephropathy. In addition to antihypertensive actions, the angiotensin II antagonists have been effective in the treatment of heart failure.

Another angiotensin receptor antagonist, losartan, has been shown to lower all-cause mortality and hospitalization to a greater extent than captopril in elderly patients with chronic CHF.

Brand Name

Diovan

Indications

• heart failure
• hypertension
• reduction of cardiovascular mortality

• Valsartan oral solution (Prexxartan) is not therapeutically equivalent to the tablet formulation (Diovan)

Side Effects

1. abdominal pain
2. alopecia
3. anaphylactoid reactions
4. anemia
5. angioedema
6. anorexia
7. anxiety
8. arthralgia
9. asthenia
10. azotemia
11. back pain
12. blurred vision
13. bullous rash
14. chest pain (unspecified)
15. constipation
16. cough
17. diarrhea
18. dizziness
19. drowsiness
20. dyspepsia
21. dyspnea
22. edema
23. elevated hepatic enzymes
24. fatigue
25. flatulence
26. headache
27. hepatitis
28. hyperkalemia
29. hypotension
30. impotence (erectile dysfunction)
31. insomnia
32. muscle cramps
33. myalgia
34. nausea
35. neutropenia
36. oliguria
37. orthostatic hypotension
38. palpitations
39. paresthesias
40. pharyngitis
41. pruritus
42. rash
43. renal failure (unspecified)
44. rhabdomyolysis
45. rhinitis
46. sinusitis
47. syncope
48. teratogenesis
49. thrombocytopenia
50. vasculitis
51. vertigo
52. vomiting
53. xerostomia

Monitoring Parameters

• blood pressure
• LFTs
• serum bilirubin (total and direct)

Contraindications

• ACE-inhibitor induced angioedema
• angioedema
• Black patients
• breast-feeding
• children
• geriatric
• heart failure
• hepatic disease
• hyperkalemia
• hypotension
• hypovolemia
• infants
• neonates
• pregnancy
• renal artery stenosis
• renal failure
• renal impairment
• surgery

Interactions

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