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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