Raltegravir
ISENTRESS
Pronunciation: ral-TEG-ra-veer
What it isThe first HIV integrase inhibitor; HIV.
Why this oneVery few drug interactions, so it suits transplant patients and complex polypharmacy.
What limits itTwice-daily dosing and a lower resistance barrier than dolutegravir. Cations block absorption; rare rhabdomyolysis.
FDA-approved for
- HIV infection (2007)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection | Adults | 400 mg BID | 400 mg BID (800 mg BID with rifampin) | |
| HIV-1 infection | Children/Adolescents >=25 kg | 400 mg BID | 400 mg BID | |
| HIV-1 infection | Children 3 to <25 kg | weight-based dosing | weight-based (see label tables) |
Renal Undefined
Hepatic Undefined
Instructions
- May be administered with or without food
- Do not substitute chewable tablets or oral suspension for the 400 mg film-coated tablet (not bioequivalent)
- With rifampin in adults, use 800 mg BID
Available strengths
- tab 400, 600 mg
- chew tab 25, 100 mg
- powder 100 mg/packet
- susp 100 mg
Cautions
- Severe, potentially fatal skin reactions (Stevens-Johnson syndrome, TEN) and hypersensitivity reactions — discontinue immediately
- Immune reconstitution syndrome
- Chewable tablets (100 mg, 25 mg) contain phenylalanine — caution in phenylketonuria
- Myopathy/rhabdomyolysis — caution in at-risk patients
Adverse reactions
- Insomnia, headache, dizziness, nausea, fatigue
- Creatine kinase elevations; myopathy and rhabdomyolysis reported
Pregnancy Use only if potential benefit justifies potential risk to the fetus; no adequate well-controlled human studies.
Lactation Breastfeeding is not recommended while taking raltegravir.
Cost
| Strength | #/mo | generic $ | brand $ | CostPlus | |
|---|---|---|---|---|---|
| 400 mg | tab | 60 BID | — | $2,072.33/mo | not offered |
| 600 mg | tab | 60 BID | — | $2,070.90/mo | not offered |
| 25 mg | chew tab | 60 BID | — | not offered | |
| 100 mg | chew tab | 60 BID | — | not offered | |
| 100 mg/packet | powder | per unit | — | not offered |
Generic entry2032 est.
NO BOXED WARNINGS
Principal riskCations block absorption; lower resistance barrier
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.