Dolutegravir (Tivicay): Guide To Uses, Dosing, Side Effects
Comprehensive guide to dolutegravir (Tivicay), an effective integrase inhibitor for HIV-1 treatment in adults and children.
Dolutegravir, sold under the brand name Tivicay, is an integrase strand transfer inhibitor (INSTI) used in combination with other antiretroviral agents to treat HIV-1 infection in adults and children. It works by blocking HIV’s integrase enzyme, preventing the virus from integrating its DNA into human cells, thus limiting viral replication.
About dolutegravir
Dolutegravir is a potent antiretroviral medication specifically designed to combat HIV-1. Approved by the FDA in 2013, it has become a cornerstone of modern HIV therapy due to its high efficacy, favorable resistance profile, and once-daily dosing convenience. Clinical trials like SINGLE, SPRING-2, and FLAMINGO demonstrated its superiority over alternatives such as efavirenz and darunavir/ritonavir in treatment-naïve patients, achieving viral suppression rates of 88-90% at 48 weeks.
The drug exhibits a high genetic barrier to resistance, with tight binding to the integrase active site (EC50 0.5-2.1 nM), making it effective even in integrase-experienced patients when dosed appropriately. It is recommended as a preferred first-line agent by major guidelines from the British HIV Association, US DHHS, and European AIDS Clinical Society.
Key facts
- Drug group: Integrase strand transfer inhibitor (INSTI).
- Breastfeeding: Not recommended; HIV can pass through breast milk, and dolutegravir data in breastfeeding is limited.
- Alcohol: No known interactions, but excessive alcohol can weaken the immune system.
- Available as: Tablets (10 mg, 25 mg, 50 mg) and oral suspension for pediatrics.
About HIV
HIV (human immunodeficiency virus) targets the immune system, specifically CD4 cells, leading to AIDS if untreated. Antiretroviral therapy (ART) like dolutegravir suppresses viral load to undetectable levels, preserving immune function and preventing transmission. Combination regimens are essential as monotherapy leads to rapid resistance.
How dolutegravir works
Dolutegravir inhibits the integrase enzyme, which HIV uses to insert its genetic material into the host cell’s DNA. By blocking the strand transfer step, it halts the viral replication cycle. Its long dissociative half-life provides sustained activity, supporting once-daily dosing in most cases.
In vitro studies show potent activity against HIV-1 subtypes, with minimal impact on host transporters at therapeutic doses, though it inhibits creatinine secretion via OCT2/MATE1, potentially elevating serum creatinine without affecting glomerular filtration rate.
Types of HIV
HIV-1 is the predominant global strain treated by dolutegravir. HIV-2 is rarer, primarily in West Africa, and shows natural resistance to some INSTIs, requiring alternative therapies.
How and when to take dolutegravir
Dosage
Always follow your doctor’s instructions. Standard adult dose is 50 mg once daily. Adjust for inducers or specific regimens.
| Patient Group | Dose |
|---|---|
| Treatment-naïve adults/children ≥40 kg | 50 mg once daily |
| With UGT1A1/CYP3A inducers (e.g., efavirenz) | 50 mg twice daily |
| Virologically suppressed switching to DTG + RPV | 50 mg + 25 mg RPV once daily |
| INSTI-experienced | 50 mg twice daily |
| Pediatrics (≥3 kg) | Weight-based: 3 mg/mL suspension |
How to take
- Swallow tablets whole with or without food.
- Suspension: Mix with water/sweet liquid; use syringe for accuracy.
- Missed dose: Take within 20 hours; if longer, skip and resume schedule.
- Do not adjust dose without medical advice.
Dosage for dolutegravir
Pediatric dosing is weight-based, starting at 4 weeks old and ≥3 kg. For example, 5 mg once daily for 3-5.9 kg children. Tablets dispersible for precise pediatric use.
Common questions about dolutegravir
How long does dolutegravir take to work?
Viral load drops rapidly within days; full suppression in weeks with adherence.
Can you drink alcohol with dolutegravir?
Yes, but moderation advised to support immune health.
How long should you take dolutegravir?
Lifelong, as HIV is chronic; regular monitoring required.
Is dolutegravir safe in pregnancy?
Generally safe (Category B), but discuss risks like neural tube defects with provider.
Using dolutegravir with other medicines and herbal supplements
Dolutegravir interacts with UGT1A1/CYP3A inducers (e.g., rifampicin: increase to 50 mg twice daily) and inhibitors. Contraindicated with dofetilide due to QT prolongation risk. Monitor metformin; avoid high-fat meals impacting absorption slightly.
| Drug Class | Effect | Action |
|---|---|---|
| Cationic drugs (metformin) | Increased levels | Limit metformin to 500 mg BID |
| Oxcarbazepine | Decreased DTG | 50 mg BID |
| Antacids | Decreased absorption | Separate by 2 hours |
Common side effects
Most side effects are mild. Discontinuation rates low (2-4% in trials).
| Side Effect | Frequency |
|---|---|
| Insomnia | Common (>1/10) |
| Headache | Common |
| Fatigue | Common |
| Increased creatinine | Common (benign) |
| Rash | Uncommon |
| Suicidal thoughts | Rare |
Serious side effects
Seek immediate help for:
- Severe rash, fever, blistering (hypersensitivity).
- Signs of liver problems (jaundice, dark urine).
- Muscle pain, weakness (rhabdomyolysis rare).
- Hepatitis B flare upon discontinuation.
- Immune Reconstitution Syndrome (IRIS).
Monitor for neural tube defects in pregnancy; weight gain reported in some.
Reporting side effects
Report to FDA MedWatch or national systems (e.g., Yellow Card in UK). Include details like timing and other meds.
Frequently asked questions
What is dolutegravir used for?
Treatment of HIV-1 in combination therapy.
Who should not take dolutegravir?
Those with prior hypersensitivity or on contraindicated drugs like dofetilide.
Does dolutegravir cause weight gain?
Possible, especially long-term; monitor BMI.
Can dolutegravir be crushed?
Dispersible tablets yes; film-coated no.
What if I miss a dose?
Take ASAP if <20 hours late; otherwise skip.
Warning: Neural tube defects
Pregnancy exposure registry data show increased neural tube defect risk (0.3% vs 0.1% background). Counsel women of childbearing potential; use effective contraception.
Patient info: Neural tube defects
Discuss with doctor if planning pregnancy. Benefits outweigh risks for most, but alternatives may be considered.
Find more resources and support
- HIV.gov: Treatment info.
- CDC HIV resources.
- Local clinics for adherence support.
References
- TIVICAY Prescribing Information — ViiV Healthcare / National HIV PrEP Curriculum. 2023. https://www.hivprep.uw.edu/page/treatment/drugs/dolutegravir/prescribing-information
- Dolutegravir: Uses, Interactions, Mechanism of Action — DrugBank Online. 2024-01-15. https://go.drugbank.com/drugs/DB08930
- Dolutegravir (Tivicay) — aidsmap. 2023-05-20. https://www.aidsmap.com/about-hiv/arv-background-information/dolutegravir-tivicay
- Dolutegravir Tablets: Uses & Side Effects — Cleveland Clinic. 2024. https://my.clevelandclinic.org/health/drugs/20972-dolutegravir-tablets
- Dolutegravir (oral route) — Mayo Clinic. 2023-11-01. https://www.mayoclinic.org/drugs-supplements/dolutegravir-oral-route/description/drg-20061287
- Tivicay Product Monograph — ViiV Healthcare. 2024. https://viivhealthcare.com/content/dam/cf-viiv/viiv-healthcare/en_CA/tivicay.pdf
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