抗病毒藥品 HIV infection

Raltegravir potassium is an HIV-1 integrase inhibitor. It prevents viral replication by inhibiting viral DNA insertion into the host's cellular genome. Specifically, raltegravir prevents integrase insertion essential for endonucleolytic processing of the viral DNA ends, and the subsequent strand transfer or integration of viral and cellular DNA.

Absorption:
1. Tmax: 1 to 3 hours
2. Bioavailability: 32% or more; Effect of food: Not significant
Distribution:
Protein binding: 83% bound to human plasma protein
Metabolism:
1. Liver: primary site, uridine diphosphate glucuronosyltransferase-mediated glucuronidation
2. Metabolite: raltegravir glucuronide (major, inactive)
3. Elimination Half Life: 9 hours
Excretion:
1. Renal clearance: 60.5 mL/min
2. Renal excretion: 32% (9% unchanged; 23% changed); Fecal: 51% (unchanged )
3. Dialyzable: (hemodialysis) 82% removed

Pecific contraindications have not been determined.

Fetal risk cannot be ruled out.

Infant risk cannot be ruled out.

Common: Nausea, Headache, Insomnia, Fatigue
Serious: Stevens-Johnson syndrome, Toxic epidermal necrolysis, Hypersensitivity reaction, Rhabdomyolysis, Suicidal, Renal failure

Treatment-naive or treatment-experienced:
400 mg orally twice daily
Non-occupational exposure; Prophylaxis:
400 mg orally twice daily, in combination with emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg orally once daily

Use is not recommended in preterm neonates
1. >25 kg: 400 mg twice daily
2. >40 kg, Treatment-naive: 400 mg twice daily

No dosage adjustment is necessary; Avoid administration before dialysis session

1. Mild-to-moderate impairment: No dosage adjustment necessary
2. Severe impairment: There are no dosage adjustments provided in manufacturer's labeling (has not been studied)