Carvedilol

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Carvedilol Brand Name– Coreg | Coreg CR

What is Carvedilol

Carvedilol is a combined alpha- and nonselective beta-blocker. Although it has some pharmacologic similarities to labetalol, the ratio of beta to alpha-1 effects is much greater for carvedilol than for labetalol.

Carvedilol is a lipophilic beta-blocker, and lacks intrinsic sympathomimetic activity (ISA).

Carvedilol also possesses antioxidant properties. The commercial product is a racemic mixture of two enantiomers, R(+) and S(-), both of which are important for the desired clinical effect.

Carvedilol (Coreg®) was approved in the US in September 1995 for the treatment of hypertension, either alone or in combination with other antihypertensive agents. In comparative studies in elderly hypertensive patients, blood pressure lowering effects of carvedilol were similar to other antihypertensives.

Carvedilol is appropriate therapy for treating hypertension in patients with renal disease or diabetes mellitus. A study in the treatment of heart failure was prematurely stopped in April 1995 due to early evidence of a beneficial effect on morbidity and mortality; results revealed a 65% decrease in risk of death in patients assigned to carvedilol.

Only 1.6% of patients who were randomized had to discontinue carvedilol due to worsening heart failure.

The FDA granted final approval for carvedilol use in mild-moderate heart failure in May 1997. An indication for use in severe heart failure received approval in November 2001 based on the COPERNICUS trial findings; carvedilol reduced mortality and hospitalization rate in patients with severe chronic heart failure.

Subsequently, the COMET trial evaluated carvedilol vs. metoprolol in patients with chronic heart failure (NYHA Class II—IV), and demonstrated a significantly lower all-cause mortality for carvedilol (34% vs. 40% for metoprolol).

However, the COMET study has been criticized for utilizing the immediate-release form of metoprolol (tartrate) vs. the extended-release formulation (succinate), which has been FDA-approved for heart failure based on the favorable findings of the MERIT-HF trial.

The COMET trial has also been criticized for evaluating a substantially lower metoprolol target dosage (50 mg PO twice daily) than the FDA-approved target dosage for heart failure (200 mg PO once daily) supported by the MERIT-HF trial. In March 2003, carvedilol received approval for use to prevent cardiovascular mortality in stable patients with left ventricular dysfunction following acute myocardial infarction.

This approval was based on the results of the CAPRICORN trial.

Carvedilol has been studied in stable angina pectoris. The 2007 AHA guidelines for the management of hypertension state beta-blockers should not be used as first-line therapy for the treatment of hypertension, as several comparative clinical trials have shown beta blockers to be inferior to ACE inhibitors, angiotensin-receptor blockers, or calcium channel blockers for preventing both stroke and coronary artery disease complications.

These guidelines do, however, recommend the use of beta-blockers for the treatment of hypertension in patients with angina, prior myocardial infarction, or heart failure.

Carvedilol has been marketed in Europe since the 1980s under the trade name Kredex™.

Extended-release carvedilol tablets (Coreg CR™) were approved by the FDA in October 2006 for the same indications approved for regular-release carvedilol tablets (Coreg®).

Indications

  1. acute myocardial infarction
  2. angina
  3. atrial fibrillation
  4. atrial flutter
  5. cardiomyopathy
  6. heart failure
  7. hypertension
  8. reduction of cardiovascular mortality
  9. unstable angina

For the treatment of essential hypertension, either as a single agent or in combination with other antihypertensive agents

Side Effects

  1. abdominal pain
  2. alopecia
  3. amnesia
  4. anaphylactoid reactions
  5. anemia
  6. angina
  7. angioedema
  8. anxiety
  9. aplastic anemia
  10. arthralgia
  11. asthenia
  12. asthma-related death
  13. AV block
  14. blurred vision
  15. bradycardia
  16. bronchospasm
  17. bundle-branch block
  18. confusion
  19. cough
  20. depression
  21. diabetes mellitus
  22. diaphoresis
  23. diarrhea
  24. dizziness
  25. drowsiness
  26. dyskinesia
  27. dyspnea
  28. edema
  29. elevated hepatic enzymes
  30. emotional lability
  31. erythema
  32. erythema multiforme
  33. exfoliative dermatitis
  34. fatigue
  35. fever
  36. floppy iris syndrome
  37. GI bleeding
  38. glycosuria
  39. gout
  40. headache
  41. heart failure
  42. hematuria
  43. hyperbilirubinemia
  44. hypercholesterolemia
  45. hyperglycemia
  46. hyperhidrosis
  47. hyperkalemia
  48. hypertension
  49. hypertriglyceridemia
  50. hyperuricemia
  51. hypervolemia
  52. hypoesthesia
  53. hypoglycemia
  54. hypokalemia
  55. hyponatremia
  56. hypoprothrombinemia
  57. hypotension
  58. hypotonia
  59. hypovolemia
  60. impaired cognition
  61. impotence (erectile dysfunction)
  62. increased urinary frequency
  63. insomnia
  64. jaundice
  65. leukopenia
  66. libido decrease
  67. maculopapular rash
  68. malaise
  69. melena
  70. migraine
  71. muscle cramps
  72. myocardial infarction
  73. nasal congestion
  74. nausea
  75. neuropathic pain
  76. nightmares
  77. orthostatic hypotension
  78. palpitations
  79. pancytopenia
  80. paresis
  81. paresthesias
  82. peripheral edema
  83. peripheral vasoconstriction
  84. pharyngitis
  85. photosensitivity
  86. pneumonitis
  87. proteinuria
  88. pruritus
  89. psoriaform rash
  90. pulmonary edema
  91. purpura
  92. rash
  93. sinus tachycardia
  94. Stevens-Johnson syndrome
  95. stroke
  96. syncope
  97. thrombocytopenia
  98. tinnitus
  99. toxic epidermal necrolysis
  100. tremor
  101. urinary incontinence
  102. urticaria
  103. vertigo
  104. visual impairment
  105. vomiting
  106. weakness
  107. weight gain
  108. weight loss
  109. wheezing
  110. withdrawal
  111. xerostomia

Monitoring Parameters

  • blood pressure
  • heart rate

Contraindications

  • abrupt discontinuation
  • acute bronchospasm
  • acute heart failure
  • asthma
  • AV block
  • beta-blocker hypersensitivity
  • bradycardia
  • breast-feeding
  • bronchitis
  • cardiogenic shock
  • cerebrovascular disease
  • children
  • chronic obstructive pulmonary disease (COPD)
  • contact lenses
  • depression
  • diabetes mellitus
  • driving or operating machinery
  • emphysema
  • geriatric
  • hepatic disease
  • history of angioedema
  • hyperthyroidism
  • hypoglycemia
  • hypotension
  • infants
  • myasthenia gravis
  • neonates
  • orthostatic hypotension
  • peripheral vascular disease
  • pheochromocytoma
  • pregnancy
  • psoriasis
  • pulmonary disease
  • pulmonary edema
  • renal disease
  • renal failure
  • renal impairment
  • sick sinus syndrome
  • surgery
  • thyroid disease
  • thyrotoxicosis
  • vasospastic angina
  • ventricular dysfunction

Interactions

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