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HIV-1 integrase inhibitor

ISENTRESS (raltegravir) is a prescription medicine used along with other drugs to treat HIV-1 infection in adults and children aged 4 weeks and older. It works by blocking a specific enzyme that the virus needs to replicate.

How it worksRaltegravir is an HIV-1 integrase strand transfer inhibitor. It stops the virus from being able to complete its life cycle by blocking a key enzyme.

Brand names:ISENTRESS

Used for
Treatment of HIV-1 infection in combination with other medicines
Conditions
Human immunodefiiciency virus type 1 (HIV-1)
Class
AntiretroviralIntegrase InhibitorHIV-1 integrase inhibitorImmune System

How to take

FormsFilm-coated tablets, Chewable tablets, Oral suspension
RoutesOral

Adults typically take 400 mg twice daily. If taking rifampin, the dose increases to 800 mg twice daily. Children's doses depend on their weight.

Do not swap different types of ISENTRESS (like switching from a swallowable tablet to a chewable one) without guidance, as they are not identical in how the body uses them.

Key warnings

  • ·Severe and potentially fatal skin reactions like Stevens-Johnson syndrome have been reported.
  • ·Stop using ISENTRESS immediately if you develop a severe rash, fever, or signs of a serious allergic reaction.
  • ·Use caution if you have a history of muscle disease or are taking other drugs that affect muscles.
  • ·Patients with phenylketonuria (PKU) should be aware that the 100 mg and 25 mg chewable tablets contain phenylalanine.

Do not use if

  • ·None listed

Side effects

Common

InsomniaHeadacheDizzinessNauseaFatigue

Serious

  • ·Severe, life-threatening skin reactions (such as Stevens-Johnson syndrome)
  • ·Severe allergic reactions (rash, fever, or swelling)
  • ·Muscle problems (myopathy or rhabdomyolysis)
  • ·Liver issues

Seek help if

  • ·Severe rash
  • ·Fever
  • ·Muscle aches
  • ·Blisters
  • ·Facial swelling

Interactions

  • ·Rifampin (can make ISENTRESS less effective)
  • ·DDAVP
  • ·DIALANTIN
  • ·OMEPRAZOLE
  • ·PREZISTA
  • ·EQUETRO
  • ·INTELENCE
  • ·FEMRING
  • ·SUSTIVA
  • ·RIFADIN
  • ·XATMEP
FoodISENTRESS can be taken with or without food.

Special populations

PregnancyISENTRESS should only be used during pregnancy if the benefit to the mother outweighs the potential risk to the baby. There are no large, controlled studies on pregnant women.

BreastfeedingBreastfeeding is not recommended while taking ISENTRESS. HIV-positive mothers are advised not to breastfeed to prevent passing the virus to the infant.

PediatricISENTRESS is used in children and adolescents from 4 weeks of age up to 18 years old. Dosing is based on weight for younger children.

GeriatricThere isn't enough data to know if older adults respond differently, but doctors should use caution due to potential changes in liver or kidney function.

Talk to your doctor

Monitor

  • ·Skin/rash appearance
  • ·Liver aminotransferase levels
  • ·Muscle symptoms
  • ·Immune reconstitution inflammatory syndrome

Questions to ask

  • ·Should I be concerned about muscle pain while taking ISENTRESS?
  • ·How should I manage my other medications while on ISENTRESS?
  • ·What should I watch for regarding skin rashes?

Pharmacokinetics

OnsetSteady state is achieved within about 2 days of twice-daily dosing.
BioavailabilityAbsolute bioavailability has not been established.
MetabolismRaltegravir does not appear to affect drugs metabolized by CYP3A4.

Practical

OverdoseNo specific treatment is listed for an overdose, but standard medical support should be used. In studies, doses up to 1600 mg once or 800 mg twice daily were generally well-tolerated.

StorageStore at 20-25°C (68-77°F). Keep chewable tablets in the original package with the moisture-protecting desiccant.

Ingredients

Allergens

lactose

Inactive

calcium phosphate dibasic anhydroushypromellose 2208lactose monohydratemagnesium stearatemicrocrystalline cellulosepoloxamer 407sodium stearyl fumarateblack iron oxidepolyethylene glycol 3350butylated hydroxytoluenepolyvinyl alcoholferric oxide redtalctitanium dioxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.