RALTEGRAVIR POTASSIUM

Clinical safety rating: safe

Animal studies have demonstrated safety

How it works

Raltegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration, which is essential for viral replication.

What the body does with it

Metabolism	Primarily metabolized by glucuronidation via UGT1A1; minor metabolism by CYP3A4.
Excretion	Primarily hepatic metabolism via UGT1A1-mediated glucuronidation; <2% excreted unchanged in urine; approximately 51% of dose recovered in feces (as parent and metabolites) and 32% in urine (as metabolites); biliary/fecal elimination accounts for the majority.
Half-life	Terminal elimination half-life is approximately 9 hours (range 7–12 hours); supports twice-daily dosing; t1/2 is prolonged in hepatic impairment (Child-Pugh B/C) but no dose adjustment recommended.
Protein binding	Approximately 83% bound to human plasma proteins, predominantly albumin.
Volume of Distribution	Volume of distribution at steady state (Vss/F) is approximately 0.6 L/kg (total body water), indicating distribution into intracellular compartments; penetrates cerebrospinal fluid (CSF) achieving concentrations ~5–10% of plasma levels.
Bioavailability	Oral bioavailability is not precisely determined but is estimated to be high (≥60–70%) based on absorption and metabolism data; food may increase Cmax (up to 2-fold) but not AUC significantly; thus can be taken with or without food.
Onset of Action	Oral: Time to maximal plasma concentration (Tmax) is about 0.5–1.5 hours; antiviral effect typically observed within 1–2 weeks of therapy, with maximal viral suppression achieved by week 4–6.
Duration of Action	The drug is administered twice daily due to half-life; clinical effect on viral load maintained over dosing interval with sustained suppression; suboptimal adherence leads to rapid rebound of viremia.

Classification & Brands

Dosing & administration

400 mg orally twice daily, with or without food. Administered as two 200 mg tablets or one 400 mg tablet.

Dosage form	TABLET
Renal impairment	No dose adjustment required for any degree of renal impairment, including end-stage renal disease on hemodialysis.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh Class A or B). Not studied in severe hepatic impairment (Child-Pugh Class C); use with caution.
Pediatric use	For weight <3 kg: insufficient data. 3 kg to <4 kg: 50 mg twice daily. 4 kg to <6 kg: 80 mg twice daily. 6 kg to <10 kg: 100 mg twice daily. 10 kg to <14 kg: 150 mg twice daily. 14 kg to <20 kg: 200 mg twice daily. 20 kg to <28 kg: 250 mg twice daily. 28 kg to <40 kg: 300 mg twice daily. ≥40 kg: 400 mg twice daily. For children ≥2 years: can use oral granules for suspension or tablets.
Geriatric use	No specific dose adjustment recommended. Clinical studies did not include sufficient numbers of patients aged ≥65 years to determine if they respond differently. Use with caution due to potential comorbidities and renal/hepatic function decline.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Strong UGT1A1 inducers may decrease levels Can cause severe and potentially fatal skin reactions.

Breastfeeding	Raltegravir is present in human breast milk with a milk-to-plasma (M/P) ratio of approximately 0.5-0.6. Limited data suggest low risk to the infant; however, because of potential for HIV transmission and adverse effects, breastfeeding is not recommended in HIV-infected women regardless of antiretroviral therapy.
Teratogenic Risk	First trimester: No increased risk of major birth defects based on data from >1000 exposed pregnancies; however, neural tube defects have been reported in animal studies at doses exceeding human exposure. Second and third trimesters: No evidence of fetal harm; raltegravir crosses the placenta with cord blood concentrations approximately equal to maternal plasma.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Common Effects	Headache
Serious Effects

Absolute Contraindications

["None."]

Clinical Precautions

Precautions

["Severe skin and hypersensitivity reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reaction with eosinophilia and systemic symptoms (DRESS) have been reported.","Immune reconstitution syndrome may occur.","Increased risk of creatine kinase elevation and myopathy/rhabdomyolysis.","May cause liver enzyme elevations in patients with hepatitis B or C coinfection."]

Clinical Tips & Counseling

Drug interactions

Loading safety data…