Losartan

Losartan Brand Name– Cozaar

What is Losartan

Losartan is the first of a unique class of oral antihypertensive agents called angiotensin II (AG II) receptor antagonists.

Losartan and its longer acting active metabolite (E-3174) are specific and selective AT₁ receptor antagonists.

Losartan is indicated to treat essential hypertension, diabetic nephropathy, and proteinuria, and has also been used off-label to treat congestive heart failure.

Compared with the angiotensin converting enzyme (ACE) inhibitors (e.g., captopril, enalapril), losartan is associated with a lower incidence of drug-induced cough, rash, and/or taste disturbances.

Because losartan does not inhibit 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 losartan or other angiotensin II antagonists.

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.

The LIFE outcome trial (conducted in patients with hypertension and left ventricular hypertrophy) shows that losartan is more effective than atenolol in reducing total mortality and cardiovascular morbidity and mortality, and is associated with less drug-related adverse events.

The results of the long-term (mean 3.4 years) RENAAL study reported that losartan (50—100 mg/day) is renoprotective (endpoints: doubling of serum creatinine, development of end-stage renal disease) in patients with type 2 diabetes and nephropathy.

Although it is not FDA approved for the treatment of heart failure, losartan has been shown to lower all-cause mortality and hospitalization to a greater extent than captopril in elderly patients with chronic heart failure (ELITE I trial).

Losartan (Cozaar®) was approved by the FDA for the treatment of hypertension in April 1995 and for the treatment of nephropathy in patients with type 2 diabetes mellitus in September 2002.

Indications

1. diabetic nephropathy
2. heart failure
3. hypertension
4. proteinuria
5. stroke prophylaxis

For the treatment of hypertension, either alone or in combination with other antihypertensive agents

Side Effects

1. abdominal pain
2. alopecia
3. anaphylactoid reactions
4. anemia
5. angina
6. angioedema
7. anorexia
8. anxiety
9. arrhythmia exacerbation
10. arthralgia
11. asthenia
12. ataxia
13. atrial fibrillation
14. AV block
15. azotemia
16. back pain
17. blurred vision
18. bradycardia
19. chest pain (unspecified)
20. confusion
21. conjunctivitis
22. constipation
23. cough
24. dental pain
25. depression
26. diaphoresis
27. diarrhea
28. dizziness
29. drowsiness
30. dysgeusia
31. dyspepsia
32. dyspnea
33. ecchymosis
34. edema
35. elevated hepatic enzymes
36. epistaxis
37. erythema
38. exfoliative dermatitis
39. fatigue
40. fever
41. flatulence
42. flushing
43. gout
44. headache
45. hepatitis
46. hyperbilirubinemia
47. hyperkalemia
48. hypoesthesia
49. hyponatremia
50. hypotension
51. impotence (erectile dysfunction)
52. increased urinary frequency
53. infection
54. insomnia
55. libido decrease
56. malaise
57. memory impairment
58. migraine
59. muscle cramps
60. musculoskeletal pain
61. myalgia
62. myocardial infarction
63. nasal congestion
64. nausea
65. nocturia
66. ocular irritation
67. oliguria
68. orthostatic hypotension
69. palpitations
70. paresthesias
71. peripheral neuropathy
72. pharyngitis
73. photosensitivity
74. pruritus
75. purpura
76. rash
77. renal failure (unspecified)
78. rhabdomyolysis
79. rhinitis
80. sinus tachycardia
81. sinusitis
82. stroke
83. syncope
84. teratogenesis
85. thrombocytopenia
86. tinnitus
87. tremor
88. urticaria
89. vasculitis
90. ventricular fibrillation
91. ventricular tachycardia
92. vertigo
93. visual impairment
94. vomiting
95. weakness
96. xerostomia

Interactions

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