Irbesartan

Irbesartan Brand Name– Avapro

What is Irbesartan

Irbesartan is an oral angiotensin II receptor antagonist used to treat hypertension.

It is also indicated to treat diabetic nephropathy and proteinuria. Irbesartan has a longer half-life than losartan and valsartan; however, all three agents can be effectively dosed once daily for hypertension.

Compared to losartan, irbesartan does not require dosage adjustment for hepatic insufficiency, is not metabolized to an active metabolite, and lacks uricosuric effects. Because AT₁ receptors are nearly saturated at the starting doses for most angiotensin II antagonists, the antihypertensive dose-response curve for these drugs is nonlinear, with proportionally small decreases in blood pressure attained with increased dosage.

Greater antihypertensive efficacy is generally achieved by adding a small dose of hydrochlorothiazide to the angiotensin II antagonist.

Irbesartan tends to reverse the potassium loss associated with hydrochlorothiazide. Because irbesartan 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 irbesartan or other angiotensin II antagonists.

Irbesartan has been associated with reduced proteinuria in patients with nephropathy, and has been shown to have long-term renoprotective effects in patients with diabetic renal disease.

Irbesartan delays the onset of diabetic nephropathy independently of its antihypertensive effects in patients with Type 2 diabetes and microalbuminuria.

In addition, irbesartan delays the progression of renal disease in patients with pre-existing diabetic nephropathy.

Comparative clinical trials are needed to evaluate the comparative renoprotective efficacy and long-term benefits of irbesartan (or other AII-receptor antagonists) versus ACE inhibitors in patients with renal disease or diabetic nephropathy.

Preliminary data support a short-term hemodynamic benefit of irbesartan in heart failure patients. Irbesartan is being evaluated in large outcome trials for the treatment of heart failure.

Irbesartan (Avapro®) was granted final FDA approval for the treatment of hypertension on 9/30/97.

It is also available in combination with HCTZ. The manufacturer for irbesartan has updated the prescribing information to remove previously suggested dosage guidelines for use in pediatric patients

Indications

1. diabetic nephropathy
2. hypertension
3. proteinuria

Side Effects

1. abdominal pain
2. anaphylactic shock
3. angina
4. angioedema
5. anxiety
6. arrhythmia exacerbation
7. azotemia
8. cardiac arrest
9. chest pain (unspecified)
10. chills
11. conjunctivitis
12. constipation
13. cough
14. depression
15. diarrhea
16. dizziness
17. drowsiness
18. dyspepsia
19. dyspnea
20. ecchymosis
21. edema
22. elevated hepatic enzymes
23. epistaxis
24. erythema
25. fatigue
26. fever
27. flatulence
28. flushing
29. gout
30. headache
31. heart failure
32. hepatitis
33. hyperkalemia
34. hypertension
35. hypertensive crisis
36. hypotension
37. impotence (erectile dysfunction)
38. influenza
39. jaundice
40. libido decrease
41. libido increase
42. muscle cramps
43. musculoskeletal pain
44. myocardial infarction
45. nausea
46. neutropenia
47. oliguria
48. orthostatic hypotension
49. paresthesias
50. pharyngitis
51. pruritus
52. pyrosis (heartburn)
53. rash
54. renal failure (unspecified)
55. rhabdomyolysis
56. rhinitis
57. serious hypersensitivity reactions or anaphylaxis
58. sinus tachycardia
59. stroke
60. syncope
61. teratogenesis
62. thrombocytopenia
63. tinnitus
64. tremor
65. urticaria
66. vertigo
67. visual impairment
68. vomiting
69. weakness
70. wheezing

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
• pregnancy
• renal artery stenosis
• surgery

Interactions

• Acarbose
• Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
• Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
• Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
• Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
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• Acetaminophen; Dextromethorphan; Pseudoephedrine
• Acetaminophen; Dichloralphenazone; Isometheptene
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• Aliskiren; Valsartan
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