Dolutegravir
An integrase strand transfer inhibitor, recommended by WHO as the preferred drug for first- and second-line HIV treatment.
Also called DTG (abbreviation).
Drug card
- Class
- Integrase inhibitor
- How it works
- Blocking HIV integrase, so viral DNA cannot enter the host chromosome
- Used for
- HIV-1 infection, with other antiretrovirals
- Known for
- Trouble sleeping (insomnia)
- Weight gain
- Its name
- -vir means an antiviral; -tegravir means an HIV integrase inhibitor
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does dolutegravir work?
Binds the active site of HIV integrase and blocks the strand transfer step, so viral DNA is not inserted into the host chromosome. It has a high genetic barrier to resistance. It also blocks the kidney transporter OCT2, which raises serum creatinine slightly without lowering kidney filtration, and raises metformin levels.
Uses
What is dolutegravir used for?
- HIV-1 infection, with other antiretrovirals
Side effects
Side effects of dolutegravir
- Trouble sleeping (insomnia)Known for
- Weight gainKnown for
- Headache
- Tiredness
- Nausea and diarrhea
- Hypersensitivity: rash, fever, liver injurySerious
- Hepatitis and acute liver failureSerious
- Suicidal thoughts, mainly with past mental illnessSerious
- Sideroblastic anemiaSerious
- Joint and muscle aches
- Immune reconstitution syndromeSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Antacids, laxatives, sucralfate and iron or calcium supplements bind it in the gut and cut its absorption, so it is taken well apart from them.
- Strong enzyme inducers such as rifampicin lower its levels.
- Contraindicated with dofetilide; it raises metformin levels.
- A small early rise in serum creatinine reflects blocked secretion, not kidney damage.
Good to know: An early signal of neural tube defects with use at conception was not confirmed by larger studies, and WHO recommends it for all populations, pregnant women included.
Remember it
A way to remember it
Integrase is the glue gun: block it and viral DNA never sticks to the chromosome.
HIV integrase pastes the DNA copy of the viral genome into the host chromosome. Dolutegravir and its relatives block that strand transfer step, so the provirus is never formed.
Written for biofideX
Its name
-vir means antiviral
Sub-stems name the target: -ciclovir, -amivir, -fovir, -tegravir, -navir, -buvir, -virine (NNRTIs). Lamivudine and zidovudine are antivirals without it.
-tegravir means HIV integrase inhibitor
Dolutegravir, raltegravir, bictegravir and cabotegravir stop HIV integrase from inserting viral DNA into the host cell's chromosomes.
- Every drug name stem
Its class
Integrase inhibitors
After reverse transcription, HIV integrase inserts the DNA copy of the viral genome into the host cell's chromosome. Integrase inhibitors bind the enzyme's active site and block this strand transfer step, so the viral DNA is never integrated and the virus cannot replicate. Dolutegravir has a high genetic barrier to resistance.
Easily mixed up with HIV protease inhibitors and nucleoside reverse transcriptase inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Dolutegravir tablets: label (DailyMed)
- Dolutegravir (NCI Thesaurus)
- WHO recommends dolutegravir as preferred HIV treatment option in all populations (WHO)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Antivirals
Dolutegravir is one of 10 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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