Raltegravir

ISENTRESS

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

FDA dosing	Population	Start	Target
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

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

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

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.

NO BOXED WARNINGS

Principal riskCations block absorption; lower resistance barrier

Cost, est. cash$300–$2,000/month

Generic entry2032 est.

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.