Standard DoseOne 50 mg tablet once daily without regard to food, for individuals on HIV therapy for the first time (treatment-naïve) or treatment-experienced individuals who have never had treatment failure with an INSTI. One 50 mg tablet twice daily, without regard to food, for adults who have or who are suspected of having certain INSTI drug resistance or who are taking certain other medications. Must be taken in combination with another antiretroviral(s) that does not contain this medication or medication from the same drug class.
For adults and children weighing more than 44 pounds (20 kg), use standard dose listed above or see package labeling. New Tivicay PD tablets (5 mg), taken without regard to food, were approved in June and are dispersible in water (oral suspension) for pediatric patients age four weeks and older weighing at least 6.6 pounds (3 kg). Children weighing at least 30.8 pounds (14 kg) may take either Tivicay or Tivicay PD, but Tivicay PD is preferred for those weighing 30.8 up to 44 pounds. Dosing under 44 pounds is weight-based; Tivicay is also available in 10 mg and 25 mg tablets. Do not chew, cut, or crush Tivicay PD tablets. If dose is more than one Tivicay PD tablet, swallow one tablet at a time. If using a dispersible dose, see package insert for mixing instructions. Dosing of Tivicay and Tivicay PD for oral suspension cannot be interchanged on a milligram per milligram basis.
Take missed dose as soon as possible, unless it is closer to the time of your next dose. Do not double up on your next dose. Not recommended for people with severe liver impairment. Use with caution in people with severe kidney impairment who have INSTI drug resistance or suspected resistance, because Tivicay levels may be decreased.
- See package insert for more complete information on potential side effects and interactions.
AWP50 mg tablets: $2,300.04/month
Potential Side Effects and Toxicity
In general, Tivicay is well tolerated with infrequent side effects. The most common moderate to severe side effects in clinical studies were insomnia (3%), headache (2%), and fatigue (2%). Mild insomnia was observed in 7% of participants in one study. Increased CPK (creatine kinase, a lab value indicating muscle damage), rhabdomyolysis (breakdown of muscle), and myopathy or myositis (muscle pain) were also reported. New data associate INSTIs with weight gain. See weight gain in “More information;” go to positivelyaware.com/articles/weighty-concerns and positivelyaware.com/articles/fatty-tissues. There have been rare reports of depression and suicidal ideation, primarily among patients with a history of psychiatric illnesses, in people receiving INSTI-based regimens. DHHS guidelines recommend closely monitoring patients on an INSTI who have pre-existing psychiatric conditions. Tivicay can cause a small, reversible increase in kidney function test (serum creatinine) within the first few weeks of treatment without affecting actual kidney function. Liver enzymes should be monitored in people with hepatitis B or C.
Potential Drug Interactions
Do not take with the anti-arrhythmic dofetilide. Intelence decreases Tivicay levels by 88%, therefore, these two medications must be co-administered with Kaletra, boosted Prezista, or boosted Reyataz. Tivicay should be taken two hours before or six hours after taking laxatives or antacids, the ulcer medication sucralfate, oral iron or calcium supplements, or buffered medications. It can be taken with iron- or calcium-containing supplements if taken together with food. Acid reducers (Pepcid, Zantac, Tagamet) and proton pump inhibitors (for example, Aciphex, Dexilant, Prilosec, Prevacid, Protonix, and Nexium) are okay to use. Avoid taking with Viramune, oxcarbazepine, phenytoin, phenobarbital, or St. John’s wort. Start metformin at lowest dose and titrate based on tolerability and clinical effect. Monitor for metformin adverse effects. Use alternatives to rifampin, carbamazepine, efavirenz, Aptivus/Norvir, and Lexiva/Norvir when possible in people with confirmed or suspected INSTI drug resistance, but these medications can be taken with Tivicay 50 mg twice daily. No known interactions with Epclusa, Harvoni, or Zepatier. Tell your provider or pharmacist about all medications, herbals, and supplements you are taking or thinking of taking, prescribed or not, as there are other drug interactions which are not listed here.
Tivicay is considered a second-generation INSTI—it may work in many individuals whose virus has developed resistance to other INSTIs, but they will need twice-daily dosing. Compared to other INSTIs, Tivicay has a high genetic barrier against the development of resistance, similar to the protease inhibitors (such as Prezista). Weight gain is becoming more widely recognized as a side effect of INSTIs. In the community, enlargement of the stomach and waist area can be distressing. According to DHHS HIV treatment guidelines, “Weight gain has been associated with initiation of ART [antiretroviral therapy] and subsequent viral suppression. The increase appears to be greater with INSTIs than with other drug classes.” Other factors have been associated with weight gain, including race, sex, and previous overweight status. There is no word yet on reversibility, but the race is on to find more answers. Pediatric HIV guidelines include Tivicay as part of a preferred regimen. Tivicay is particularly useful when drug interactions are a concern with the HIV protease inhibitor (PI) drugs. Tivicay is a small tablet, a benefit for patients who have difficulty swallowing.
Another ART (antiretroviral therapy) switch strategy for people who are virally suppressed, backed by some supporting evidence, is moving them to a boosted protease inhibitor + integrase inhibitor. In two small observational studies, individuals were switched from their current ART regimens to Prezista + Norvir + Tivicay, and viral suppression was maintained in over 97% of participants. Dolutegravir is now a preferred medication at the time of conception as well as during pregnancy, per DHHS perinatal guidelines updated in December. See the online version of this page.
Dr. Melanie Thompson:
Dolutegravir is recommended as a first-line option for initial treatment, in combination with TDF or TAF, and FTC or 3TC. It also can be taken with ABC/3TC, or with 3TC alone in STR formulations.
Resistance to dolutegravir can occur but is less common than to raltegravir and elvitegravir.
Weight gain was higher with dolutegravir than raltegravir in the large NA-ACCORD cohort study, and higher than with elvitegravir/cobicistat in a pooled analysis.
Early data from the Tsempano study in Botswana suggested that persons on dolutegravir at the time they became pregnant were more likely to have infants with neural tube defects (birth defects affecting the developing nervous system) than those not taking dolutegravir at conception. Based on that, dolutegravir-containing regimens were recommended as alternatives for persons planning pregnancy or those not using adequate contraception. Updated data, however, now show only a very small increase in risk for neural tube defects in those on dolutegravir at the time of conception, suggesting that the benefits of improved viral suppression on dolutegravir may outweigh the risks. While the risk is small, providers should discuss with people capable of pregnancy before starting dolutegravir. There have been no concerns about using dolutegravir in the second or third trimesters of pregnancy.
This clears preliminary concerns over the potential for birth defects with dolutegravir raised in 2018 by a study in Botswana. In the latest study data reported in July 2020, it was found that 0.3% of infants exposed to dolutegravir were diagnosed with neural tube defects, compared to 0.1% of infants born to women with HIV on non-dolutegravir containing regimens, and 0.08% of infants born to women without HIV. These data show that the prevalence of the birth defect is not significantly different when taking dolutegravir around the time of conception or during pregnancy compared to other HIV drugs (see summary of data on page 19 of package insert).
There are fewer drug interactions with dolutegravir than with boosted drugs, but several are notable. Dofetilide, a heart rhythm medication, should never be taken with dolutegravir. Dolutegravir can increase levels of metformin, and levels of dolutegravir are decreased by etravirine and efavirenz when no booster is present. Calcium, magnesium, zinc, aluminum, and iron supplements can lower INSTI levels and dosing recommendations should be observed.
Activist Bridgette Picou:
Tivicay is to be used as part of an HIV cocktail or regimen. Side effects may include headache and diarrhea. It can be taken with or without food, and is dosed as once a day, or twice a day if there is resistance to other integrase inhibitors.