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Raltegravir

Antiretroviral · HIV infection

Also known as RAL

AntiretroviralHIV infection
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
9 major
SEVERE in our sources
PREGNANCY
g Management of HIV infection in pregnancy should
FDA category + note
Top interactionssee all 12
  • Aluminum HydroxideSevereDatabaseDDInter
  • Calcium CarbonateSevereDatabaseDDInter
  • MagaldrateSevereDatabaseDDInter
  • Magnesium HydroxideSevereDatabaseDDInter

Mechanism

Raltegravir is an HIV integrase strand transfer inhibitor (INSTI) that blocks the catalytic activity of HIV integrase by chelating the essential divalent metal ions (Mg²⁺) at the enzyme's active site, preventing the integration of viral DNA into the host cell chromosome. This arrests the HIV replication cycle at a step after reverse transcription but before proviral DNA establishment, providing a mechanism distinct from all other antiretroviral classes. It has activity against both HIV-1 and HIV-2.

Indications

HIV infectionHIV infection, post-exposure prophylaxis (off-label)HIV-infected adults and children weighing 2 kg or moreHIV (addition to optimized background therapy in repeatedly treated patients)untreated patients as a component of initial triple drug regimen (with two NRTIs)

Dosing

Adult
adults with antiretroviral therapy available at www.bhiva.org/ guidelines. There can be variation in the licensing of different medicines containing the same drug.…

Pharmacokinetics

Onset
Orally active
Half-life
9
Bioavailability
≥31.8 ± 9.4%
Protein binding
83%
Metabolism
UGT1A1
Excretion
9% (renal, unchanged)

Side effects

Common
headachenauseaastheniafatiguecreatine kinase elevationsmyopathyrhabdomyolysisexacerbation of depressionnonspecific side effects (otherwise well tolerated)
Serious
  • drug reaction with eosinophilia and systemic symptoms (DRESS)
  • myopathy (potential toxicity)

Pregnancy & lactation

Pregnancy

g Management of HIV infection in pregnancy should

Drug interactions

Aluminum Hydroxide
Severe
Database

Clinical effect not specified

Source: DDInter

Calcium Carbonate
Severe
Database

Clinical effect not specified

Source: DDInter

Magaldrate
Severe
Database

Clinical effect not specified

Source: DDInter

Magnesium Hydroxide
Severe
Database

Clinical effect not specified

Source: DDInter

Rifampicin
Severe
Database

.

Source: DDInter

Zinc Acetate
Severe
Database

Clinical effect not specified

Source: DDInter

Zinc Chloride
Severe
Database

Clinical effect not specified

Source: DDInter

Zinc Gluconate
Severe
Database

Clinical effect not specified

Source: DDInter

Zinc Sulfate
Severe
Database

Clinical effect not specified

Source: DDInter

Aluminum Containing Antacids
Moderate
Textbook

Reduced bioavailability of raltegravir.

Magnesium- or aluminum-containing antacids and sucralfate must be taken 6 h before or 2 h after raltegravir.

Source: G&G 14e · p1245-1266

Calcium Containing Supplements
Moderate
Textbook

Reduced bioavailability of raltegravir.

Administration of calcium- and iron-containing supplements should be separated from raltegravir by at least 2 h, unless given with food.

Source: G&G 14e · p1245-1266

Iron Containing Supplements
Moderate
Textbook

Reduced bioavailability of raltegravir.

Administration of calcium- and iron-containing supplements should be separated from raltegravir by at least 2 h, unless given with food.

Source: G&G 14e · p1245-1266

Related guidelines

Other Antiretroviral drugs

Ask House about Raltegravir

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team