Varenicline

What is Varenicline

Varenicline is a nicotine receptor agonist for aid in smoking cessation. Varenicline is a potent and competitive partial agonist at nicotinic receptors.

Varenicline is effective because it provides some nicotine effects to help with nicotine withdrawal symptoms while also blocking the effects of nicotine if the user were to relapse.

Most other smoking cessation therapies either try to replace nicotine or mimic the effects of nicotine by inhibiting dopamine reuptake. Varenicline was evaluated in 3,659 chronic smokers (about 21 cigarettes per day for 25 years) in 6 premarketing clinical trials.

Brand Name

Chantix

Indications

  • tobacco cessation

For use as an adjunct to psychosocial interventions for tobacco cessation (smoking cessation)

Side Effects

  1. abdominal pain
  2. abnormal dreams
  3. acne vulgaris
  4. agitation
  5. amnesia
  6. anemia
  7. angina
  8. angioedema
  9. anorexia
  10. anxiety
  11. appetite stimulation
  12. arthralgia
  13. atopic dermatitis
  14. atrial fibrillation
  15. atrial flutter
  16. back pain
  17. blurred vision
  18. bradycardia
  19. bronchospasm
  20. cataracts
  21. chest pain (unspecified)
  22. chills
  23. cholecystitis
  24. complex sleep-related behaviors
  25. conjunctivitis
  26. constipation
  27. depression
  28. diabetes mellitus
  29. diarrhea
  30. dizziness
  31. drowsiness
  32. dysarthria
  33. dysgeusia
  34. dyspepsia
  35. dysphagia
  36. dyspnea
  37. edema
  38. elevated hepatic enzymes
  39. emotional lability
  40. epistaxis
  41. eructation
  42. erythema
  43. erythema multiforme
  44. esophagitis
  45. ethanol intoxication
  46. euphoria
  47. fatigue
  48. fever
  49. flatulence
  50. gastritis
  51. gastroesophageal reflux
  52. GI bleeding
  53. GI obstruction
  54. hallucinations
  55. headache
  56. hearing loss
  57. hostility
  58. hot flashes
  59. hyperglycemia
  60. hyperhidrosis
  61. hyperlipidemia
  62. hypoglycemia
  63. hypokalemia
  64. impotence (erectile dysfunction)
  65. insomnia
  66. irritability
  67. laryngeal edema
  68. lethargy
  69. leukocytosis
  70. libido decrease
  71. lymphadenopathy
  72. mania
  73. menstrual irregularity
  74. migraine
  75. muscle cramps
  76. musculoskeletal pain
  77. myalgia
  78. myocardial infarction
  79. nausea
  80. nephrolithiasis
  81. night blindness
  82. nightmares
  83. nocturia
  84. nystagmus
  85. ocular irritation
  86. ocular pain
  87. oral ulceration
  88. osteoporosis
  89. palpitations
  90. pancreatitis
  91. paranoia
  92. parosmia
  93. peptic ulcer
  94. peripheral edema
  95. photophobia
  96. photosensitivity
  97. polyuria
  98. pruritus
  99. psoriasis
  100. psychomotor impairment
  101. psychosis
  102. pulmonary embolism
  103. rash
  104. renal failure (unspecified)
  105. restless legs syndrome (RLS)
  106. restlessness
  107. rhinorrhea
  108. seizures
  109. sinus tachycardia
  110. somnambulism
  111. splenomegaly
  112. Stevens-Johnson syndrome
  113. stroke
  114. suicidal ideation
  115. syncope
  116. thrombocytopenia
  117. thrombosis
  118. tinnitus
  119. tremor
  120. urinary retention
  121. urticaria
  122. vertigo
  123. visual impairment
  124. vomiting
  125. weight gain
  126. xerophthalmia
  127. xerosis
  128. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • angioedema
  • behavioral changes
  • bipolar disorder
  • breast-feeding
  • cardiac disease
  • children
  • complex sleep-related behaviors
  • depression
  • dialysis
  • driving or operating machinery
  • ethanol ingestion
  • ethanol intoxication
  • geriatric
  • infants
  • myocardial infarction or stroke
  • pregnancy
  • psychiatric event
  • renal failure
  • renal impairment
  • schizophrenia
  • seizures
  • serious rash
  • suicidal ideation

Interactions

  • Cimetidine
  • Ethanol
  • Lamotrigine
  • Ranolazine
  • Tafenoquine
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