Saquinavir

What is Saquinavir

Saquinavir is an antiretroviral protease inhibitor, indicated for use in combination with ritonavir and other antiretroviral medications to treat HIV-1 infection in patients 16 years and older.

To obtain adequate plasma concentrations, saquinavir MUST always be ‘boosted’ with ritonavir; cobicistat is NOT interchangeable with ritonavir to increase the exposure of saquinavir.

Dose-dependent QT and PR prolongation, as well as torsades de pointes, have been reported with use; thus, saquinavir is contraindicated for use in patients with congenital long QT syndrome, refractory hypokalemia or hypomagnesemia, in combination with drugs that both increase saquinavir plasma concentrations and prolong QT interval, and in patients with or at risk for complete atrioventricular (AV) block.

Brand Name

  • Fortovase
  • Invirase

Indications

  • human immunodeficiency virus (HIV)
  • human immunodeficiency virus (HIV) infection

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. alopecia
  4. anemia
  5. anorexia
  6. anxiety
  7. arthralgia
  8. ascites
  9. asthenia
  10. AV block
  11. back pain
  12. bleeding
  13. bullous rash
  14. chest pain (unspecified)
  15. confusion
  16. constipation
  17. cough
  18. Cushingoid features
  19. dehydration
  20. depression
  21. diabetes mellitus
  22. diabetic ketoacidosis
  23. diaphoresis
  24. diarrhea
  25. dizziness
  26. drowsiness
  27. dysgeusia
  28. dyspepsia
  29. dysphagia
  30. dyspnea
  31. eczema vaccinatum
  32. edema
  33. elevated hepatic enzymes
  34. eructation
  35. erythema
  36. fatigue
  37. fever
  38. flatulence
  39. gastritis
  40. GI bleeding
  41. GI obstruction
  42. gynecomastia
  43. headache
  44. hematoma
  45. hemolytic anemia
  46. hepatitis
  47. hepatomegaly
  48. hyperamylasemia
  49. hyperbilirubinemia
  50. hypercholesterolemia
  51. hyperglycemia
  52. hyperlipidemia
  53. hypertension
  54. hypertriglyceridemia
  55. hypoesthesia
  56. hypotension
  57. infection
  58. influenza
  59. insomnia
  60. intracranial bleeding
  61. jaundice
  62. lethargy
  63. leukopenia
  64. lipodystrophy
  65. lymphadenopathy
  66. myalgia
  67. nausea
  68. nephrolithiasis
  69. neutropenia
  70. pancreatitis
  71. pancytopenia
  72. paresthesias
  73. peripheral neuropathy
  74. peripheral vasoconstriction
  75. phlebitis
  76. PR prolongation
  77. pruritus
  78. psychosis
  79. QT prolongation
  80. rash
  81. seizures
  82. sinusitis
  83. Stevens-Johnson syndrome
  84. syncope
  85. thrombocytopenia
  86. tinnitus
  87. torsade de pointes
  88. tremor
  89. urticaria
  90. visual impairment
  91. vomiting
  92. xerosis
  93. xerostomia

Monitoring Parameters

  • blood glucose
  • CBC with differential
  • CD4+ T cell count
  • hepatitis B serology
  • LFTs
  • plasma hepatitis C RNA
  • plasma HIV RNA
  • pregnancy testing
  • serum bilirubin (total and direct)
  • serum cholesterol
  • serum lipid profile
  • urinalysis

Contraindications

  • alcoholism
  • autoimmune disease
  • AV block
  • bradycardia
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • cardiomyopathy
  • coronary artery disease
  • diabetes mellitus
  • diabetic ketoacidosis
  • females
  • galactosemia
  • geriatric
  • Graves’ disease
  • Guillain-Barre syndrome
  • heart failure
  • hemophilia
  • hepatic disease
  • hepatitis
  • hepatitis B and HIV coinfection
  • hepatitis C and HIV coinfection
  • human immunodeficiency virus (HIV) infection resistance
  • hypercholesterolemia
  • hyperglycemia
  • hyperlipidemia
  • hypertension
  • hypertriglyceridemia
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • immune reconstitution syndrome
  • malnutrition
  • myocardial infarction
  • pancreatitis
  • pregnancy
  • QT prolongation
  • thyroid disease
  • torsade de pointes

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