Raltegravir

What is Raltegravir

Raltegravir is an antiretroviral agent approved for the treatment of human immunodeficiency virus (HIV) infection.

It was the first in a class of antiretroviral agents called HIV integrase strand transfer inhibitors, which were designed to slow the advancement of HIV infection by blocking the HIV integrase enzyme needed for viral multiplication. As compared with only optimized background therapy (OBT), oral raltegravir 400 mg twice daily plus OBT was significantly more effective at both reducing HIV viral RNA concentrations and increasing CD4 cell counts among treatment-experienced adults with documented resistance to at least one nucleoside reverse transcriptase inhibitor (NRTI), one non-nucleoside reverse transcriptase inhibitor (NNRTI), and one protease inhibitor (PI).

In the raltegravir group (n = 462), 55% of patients achieved an HIV viral RNA load less than 50 copies/mL compared with 27% of patients in the only OBT group (n = 237). Virologic failure occurred in 35% of patients in the raltegravir group compared with 66% of patients in the only OBT group.

The mean increases in CD4 cell counts from baseline were 118 cells/mm3 for raltegravir recipients and 47 cells/mm3 for recipients of only OBT. The use of other active agents with raltegravir was associated with a greater likelihood of treatment response.

In treatment-naive patients, receipt of raltegravir, tenofovir, and lamivudine for 48 weeks led to rapid, potent, and durable reductions in viral load.

Creatine phosphokinase (CPK) elevation, muscle weakness, and rhabdomyolysis have been reported with raltegravir therapy.

Brand Name

  • Isentress
  • Isentress HD

Indications & Dosage

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

Side Effects

  1. abdominal pain
  2. anemia
  3. angioedema
  4. anxiety
  5. arthralgia
  6. asthenia
  7. conjunctivitis
  8. depression
  9. diarrhea
  10. dizziness
  11. dyspepsia
  12. elevated hepatic enzymes
  13. eosinophilia
  14. fatigue
  15. fever
  16. gastritis
  17. headache
  18. hepatic failure
  19. hepatitis
  20. hyperamylasemia
  21. hyperbilirubinemia
  22. hyperglycemia
  23. infection
  24. insomnia
  25. malaise
  26. myalgia
  27. myopathy
  28. nausea
  29. nephrolithiasis
  30. neutropenia
  31. oral ulceration
  32. paranoia
  33. rash
  34. renal failure (unspecified)
  35. rhabdomyolysis
  36. Stevens-Johnson syndrome
  37. suicidal ideation
  38. thrombocytopenia
  39. toxic epidermal necrolysis
  40. vomiting
  41. weight gain

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

  • autoimmune disease
  • Black patients
  • breast-feeding
  • depression
  • females
  • geriatric
  • Graves’ disease
  • Guillain-Barre syndrome
  • hepatic disease
  • hepatitis
  • hepatitis B and HIV coinfection
  • hepatitis C and HIV coinfection
  • Hispanic patients
  • human immunodeficiency virus (HIV) infection resistance
  • immune reconstitution syndrome
  • lactase deficiency
  • phenylketonuria
  • pregnancy
  • serious rash
  • suicidal ideation

Interactions

  • Aluminum Hydroxide
  • Aluminum Hydroxide; Magnesium Carbonate
  • Aluminum Hydroxide; Magnesium Hydroxide
  • Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
  • Aluminum Hydroxide; Magnesium Trisilicate
  • Amlodipine; Atorvastatin
  • Antacids
  • Aspirin, ASA; Pravastatin
  • Atorvastatin
  • Atorvastatin; Ezetimibe
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Calcium Carbonate
  • Calcium Carbonate; Magnesium Hydroxide
  • Calcium Carbonate; Risedronate
  • Calcium Carbonate; Simethicone
  • Carbamazepine
  • Etravirine
  • Ezetimibe; Simvastatin
  • Fenofibrate
  • Fenofibric Acid
  • Fibric acid derivatives
  • Fluvastatin
  • Fosamprenavir
  • Fosphenytoin
  • Gemfibrozil
  • HMG-CoA reductase inhibitors
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Lovastatin
  • Lovastatin; Niacin
  • Magnesium Hydroxide
  • Niacin; Simvastatin
  • Phenobarbital
  • Phenytoin
  • Pitavastatin
  • Pravastatin
  • Primidone
  • Rifampin
  • Rosuvastatin
  • Simvastatin
  • Simvastatin; Sitagliptin
  • Tipranavir
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