Dolutegravir

What is Dolutegravir?

• Dolutegravir (TIVICAY) is a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI) used , together with other medication, to treat HIV/AIDS.

What are the uses of this medicine?

This medicine is used to treat Human Immunodeficiency Virus-1 (HIV-1) infection together with:

• other antiretroviral medicines in adults and children who weigh at least 66 pounds (30 kg).
• rilpivirine in adults to replace their current anti-HIV-1 medicines when their healthcare provider determines that they meet certain requirements.

How does this medicine work?

• Dolutegravir (doe" loo teg' ra vir) is relatively new antiretroviral drug that targets the HIV integrase, one of the three viral enzymes involved in replication.
• Dolutegravir blocks the binding site of the HIV integrase and prevents the strand transfer activity and integration of the provirus into the host genome.
• Dolutegravir has both in vitro and in vivo activity against HIV, and several randomized controlled trials have shown that it can cause significant declines in HIV RNA levels and rises in peripheral CD4 T cell counts.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have ever had an allergic reaction to a medicine that contains dolutegravir.
• take dofetilide.

What drug interactions can this medicine cause?

• TIVICAY should be taken 2 hours before or 6 hours after taking cation-containing antacids or laxatives, sucralfate, oral supplements containing iron or calcium, or buffered medications. Alternatively, TIVICAY and supplements containing calcium or iron can be taken together with food.
• Drugs that are metabolic inducers may decrease the plasma concentrations of dolutegravir.
• Dolutegravir is metabolized by UGT1A1 with some contribution from CYP3A. Dolutegravir is also a substrate of UGT1A3, UGT1A9, BCRP, and P-gp in vitro.

Is this medicine FDA approved?

• FDA approved this drug in the year of 2013.

How should this medicine be used?

• Perform pregnancy testing before initiation of TIVICAY in adolescents and adults of childbearing potential.

Recommended Dosage: Adult Population

• Treatment-naïve or treatment-experienced INSTI-naïve or virologically suppressed (HIV-1 RNA <50 copies per mL) adults switching to dolutegravir plus rilpivirine:50 mg once daily
• Treatment-naïve or treatment-experienced INSTI-naïve when coadministered with certain UGT1A or CYP3A inducers: 50 mg twice daily
• INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50 mg twice daily

Pediatric Patients: Treatment-naïve or treatment-experienced INSTI-naïve patients weighing at least 30 kg:

• If at least 40 kg: The recommended dose is TIVICAY 50 mg once daily.
• Patients 30 kg to less than 40 kg: The recommended dose is TIVICAY 35 mg once daily.
• If certain UGT1A or CYP3A inducers are coadministered, then adjust the weight-based dose of TIVICAY to twice daily.

Administration

• Take TIVICAY exactly as your healthcare provider tells you to take it.
• Take TIVICAY with or without food.
• Do not change your dose or stop taking TIVICAY without talking with your healthcare provider.
• If you take antacids, laxatives, or other medicines that contain aluminum, magnesium, or buffered medicines, TIVICAY should be taken at least 2 hours before or 6 hours after you take these medicines.
• If you need to take iron or calcium supplements by mouth during treatment with TIVICAY:
• If you take TIVICAY with food, you may take these supplements at the same time that you take TIVICAY.
• If you do not take TIVICAY with food, take TIVICAY at least 2 hours before or 6 hours after you take these supplements.
• Do not miss a dose of TIVICAY.
• If you miss a dose of TIVICAY, take it as soon as you remember. Do not take 2 doses at the same time or take more than your prescribed dose.
• Stay under the care of a healthcare provider during treatment with TIVICAY.
• Do not run out of TIVICAY. The virus in your blood may increase and the virus may become harder to treat. When your supply starts to run low, get more from your healthcare provider or pharmacy.
• If you take too much TIVICAY, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 10 mg, 25 mg, and 50 mg

This medicine is available in fallowing brand namesː

• TIVICAY

What side effects can this medication cause?

The most common side effects of this medicine include:

• trouble sleeping
• tiredness
• headache

TIVICAY can cause serious side effects including:

• Allergic reactions
• Liver problems
• Changes in your immune system (Immune Reconstitution Syndrome)

What special precautions should I follow?

• Hypersensitivity reactions characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury, have been reported. Discontinue TIVICAY and other suspect agents immediately if signs or symptoms of hypersensitivity reactions develop, as a delay in stopping treatment may result in a life-threatening reaction.
• Hepatotoxicity has been reported in patients receiving dolutegravir-containing regimens. Patients with underlying hepatitis B or C may be at increased risk for worsening or development of transaminase elevations. Monitoring for hepatotoxicity is recommended.
• Embryo-fetal toxicity may occur when used at the time of conception and in early pregnancy. Avoid use of TIVICAY at the time of conception through the first trimester of pregnancy due to the risk of neural tube defects. Advise adolescents and adults of childbearing potential to use effective contraception.
• Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy.

What to do in case of emergency/overdose?

Management of overdosage:

• There is no known specific treatment for overdose with TIVICAY.
• If overdose occurs, the patient should be monitored and standard supportive treatment applied as required.
• As dolutegravir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by dialysis.

Can this medicine be used in pregnancy?

• There are insufficient human data on the use of TIVICAY during pregnancy to definitively assess a drug-associated risk for birth defects and miscarriage.

Can this medicine be used in children?

• The safety, virologic, and immunologic responses in subjects who received TIVICAY were evaluated in 46 treatment-experienced, INSTI-naïve, HIV‑1–infected subjects aged 6 to less than 18 years.
• It is not known if TIVICAY is safe and effective in children who weigh less than 66 pounds (30 kg) or in children who have received certain types of medicine for HIV-1 infection.

What are the active and inactive ingredients in this medicine?

• Active ingredient: dolutegravir.
• Inactive ingredients: D-mannitol, microcrystalline cellulose, povidone K29/32, sodium starch glycolate, and sodium stearyl fumarate. The tablet film‑coating contains the inactive ingredients iron oxide yellow (for the 25-mg and 50-mg tablets only), macrogol/PEG, polyvinyl alcohol-part hydrolyzed, talc, and titanium dioxide.

Who manufactures and distributes this medicine?

Manufactured for: ViiV Healthcare Research Triangle Park

Manufactured by: GlaxoSmithKline Research Triangle

What should I know about storage and disposal of this medication?

• Store TIVICAY at room temperature between 68°F to 77°F (20°C to 25°C).
• Store TIVICAY 10-mg tablets in the original bottle. Keep the bottle tightly closed and protected from moisture.
• The bottle of TIVICAY (10-mg tablets) contains a desiccant packet to help keep your medicine dry (protect it from moisture). Do not remove the desiccant packet from the bottle.
• Keep TIVICAY and all medicines out of the reach of children.

• Dailymed label info on Dolutegravir
• FDA Dolutegravir

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