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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