Tivicay 50mg Tablets
It is used to treat HIV infection.
Drug Class
Antiretroviral
Pharmacologic Class
Integrase Strand Transfer Inhibitor (INSTI)
Pregnancy Category
Not available
FDA Approved
Aug 2013
DEA Schedule
Not Controlled
Overview
What is this medicine?
Dolutegravir is an antiviral medicine used to treat HIV (Human Immunodeficiency Virus) infection. It works by stopping the virus from multiplying in your body, which helps to reduce the amount of virus and increase your immune system's strength. It is not a cure for HIV.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most out of your treatment, it's essential to follow your doctor's instructions for taking this medication. Carefully read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food.
It's crucial that you don't miss or skip a dose during your treatment. If you take supplements or medications that contain iron, aluminum, calcium, magnesium, or zinc (such as certain antacids or vitamins), or if you take buffered products or sucralfate, you may need to take them at a different time than your prescribed medication. Consult with your doctor or pharmacist to determine the best schedule for your medications.
When you receive a new prescription, double-check the medication to ensure you have the correct one. If you suspect you've been given the wrong medication or are unsure about its appearance, contact your doctor immediately.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature in a dry place, away from the bathroom. Keep the lid tightly closed and store all medications in a secure location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you're unsure about the best way to dispose of your medication, consult with your pharmacist. You may also want to explore drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you're unsure about what to do if you miss a dose, contact your doctor for guidance.
To ensure you get the most out of your treatment, it's essential to follow your doctor's instructions for taking this medication. Carefully read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food.
It's crucial that you don't miss or skip a dose during your treatment. If you take supplements or medications that contain iron, aluminum, calcium, magnesium, or zinc (such as certain antacids or vitamins), or if you take buffered products or sucralfate, you may need to take them at a different time than your prescribed medication. Consult with your doctor or pharmacist to determine the best schedule for your medications.
When you receive a new prescription, double-check the medication to ensure you have the correct one. If you suspect you've been given the wrong medication or are unsure about its appearance, contact your doctor immediately.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature in a dry place, away from the bathroom. Keep the lid tightly closed and store all medications in a secure location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you're unsure about the best way to dispose of your medication, consult with your pharmacist. You may also want to explore drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you're unsure about what to do if you miss a dose, contact your doctor for guidance.
Lifestyle & Tips
- Take dolutegravir exactly as prescribed by your doctor, usually once daily. Do not miss doses.
- It can be taken with or without food.
- If you take antacids, laxatives, iron, or calcium supplements, take dolutegravir at least 2 hours before or 6 hours after these products.
- Continue to practice safe sex and avoid sharing needles to prevent transmitting HIV to others.
- Regular blood tests and doctor visits are important to monitor your health and the effectiveness of the treatment.
- Do not stop taking dolutegravir without talking to your doctor, as this can lead to the virus becoming resistant to the medication.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
50 mg once daily (treatment-naive or INSTI-naive)
Dose Range:
50 - 100 mg
Condition-Specific Dosing:
INSTI-experienced with resistance:
50 mg twice daily
Co-administered with certain UGT1A1/CYP3A inducers (e.g., rifampin):
50 mg twice daily
Pediatric Dosing
Neonatal:
Not established for neonates <4 weeks or <3 kg. For infants âĨ4 weeks and âĨ3 kg, weight-based dosing with Tivicay PD (dispersible tablets) is used.
Infant:
Weight-based dosing for infants âĨ4 weeks and âĨ3 kg (Tivicay PD). For example, 3 to <6 kg: 5 mg once daily; 6 to <10 kg: 10 mg once daily; 10 to <14 kg: 15 mg once daily; 14 to <20 kg: 20 mg once daily.
Child:
Weight-based dosing for children âĨ20 kg (Tivicay tablets or Tivicay PD). For example, 20 to <30 kg: 30 mg once daily; 30 to <40 kg: 35 mg once daily; âĨ40 kg: 50 mg once daily.
Adolescent:
For adolescents âĨ40 kg: 50 mg once daily. If INSTI-experienced with resistance or co-administered with certain inducers, 50 mg twice daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required (CrCl âĨ30 mL/min)
Moderate:
No dose adjustment required (CrCl âĨ30 mL/min)
Severe:
No dose adjustment required (CrCl <30 mL/min)
Dialysis:
No dose adjustment required; dolutegravir is highly protein bound and not significantly removed by dialysis.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
No dose adjustment required (Child-Pugh B)
Severe:
Not available (No data for Child-Pugh C)
Pharmacology
Mechanism of Action
Dolutegravir is an integrase strand transfer inhibitor (INSTI). It inhibits HIV-1 integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration, which is essential for the HIV-1 replication cycle.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 50-70%
Tmax:
2-7 hours
FoodEffect:
Food increases the extent of dolutegravir absorption (AUC and Cmax) but does not significantly affect Tmax. Can be taken with or without food.
Distribution:
Vd:
Approximately 17.4 L
ProteinBinding:
>99% (primarily to plasma albumin)
CnssPenetration:
Yes (detectable in cerebrospinal fluid, CSF)
Elimination:
HalfLife:
Approximately 14 hours
Clearance:
Not available
ExcretionRoute:
Primarily fecal (approximately 53% as unchanged drug), with renal excretion being a minor pathway (approximately 32% as metabolites, <1% as unchanged drug).
Unchanged:
Approximately 53% (fecal), <1% (renal)
Pharmacodynamics
OnsetOfAction:
Rapid (achieves steady-state concentrations within days)
PeakEffect:
Not applicable for chronic antiviral effect; viral load reduction is gradual over weeks.
DurationOfAction:
Sustained viral suppression with once-daily dosing due to long half-life and potent activity.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Fever
Muscle or joint pain
Mouth sores
Eye irritation
When starting HIV treatment, changes in your immune system can occur, and hidden infections may become apparent. If you experience any new symptoms after starting this medication, even after several months, inform your doctor right away. These symptoms may include:
Fever
Sore throat
Weakness
Cough
Shortness of breath
Other Possible Side Effects
Most medications can cause side effects, but many people do not experience any or only have mild symptoms. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Headache
Feeling tired or weak
Trouble sleeping
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Fever
Muscle or joint pain
Mouth sores
Eye irritation
When starting HIV treatment, changes in your immune system can occur, and hidden infections may become apparent. If you experience any new symptoms after starting this medication, even after several months, inform your doctor right away. These symptoms may include:
Fever
Sore throat
Weakness
Cough
Shortness of breath
Other Possible Side Effects
Most medications can cause side effects, but many people do not experience any or only have mild symptoms. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Headache
Feeling tired or weak
Trouble sleeping
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of a severe allergic (hypersensitivity) reaction: rash, fever, tiredness, muscle or joint aches, blisters, mouth sores, red or swollen eyes, swelling of the face, lips, or mouth, trouble breathing.
- Signs of liver problems: dark urine, pale stools, yellowing of your skin or the whites of your eyes (jaundice), nausea, vomiting, stomach pain.
- New or worsening mental health problems: severe depression, anxiety, agitation, suicidal thoughts or actions.
- Signs of Immune Reconstitution Inflammatory Syndrome (IRIS): new or worsening symptoms of an infection you had in the past (e.g., tuberculosis, herpes zoster) or new inflammatory conditions.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease, as this may affect the medication's safety and efficacy.
If you are currently taking any of the following medications: Dofetilide, etravirine, nevirapine, oxcarbazepine, phenobarbital, phenytoin, or St. John's wort, as these may interact with this medication.
Additionally, if you are:
Pregnant, planning to become pregnant, or breastfeeding, you will need to discuss the potential benefits and risks of this medication with your doctor. This conversation will also include the best methods for preventing the transmission of HIV to your baby.
Please note that this is not an exhaustive list of all potential interactions or health concerns related to this medication. Therefore, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor to ensure it is safe to take this medication.
* Never start, stop, or change the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease, as this may affect the medication's safety and efficacy.
If you are currently taking any of the following medications: Dofetilide, etravirine, nevirapine, oxcarbazepine, phenobarbital, phenytoin, or St. John's wort, as these may interact with this medication.
Additionally, if you are:
Pregnant, planning to become pregnant, or breastfeeding, you will need to discuss the potential benefits and risks of this medication with your doctor. This conversation will also include the best methods for preventing the transmission of HIV to your baby.
Please note that this is not an exhaustive list of all potential interactions or health concerns related to this medication. Therefore, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor to ensure it is safe to take this medication.
* Never start, stop, or change the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you have a history of hepatitis B or C, discuss this with your doctor to ensure safe treatment.
When taking this drug, it may be necessary to adjust the timing of other medications to avoid interactions. Consult with your doctor or pharmacist to determine the best schedule for taking your medications.
Regular blood tests and laboratory evaluations are crucial to monitor your condition. Adhere to the schedule recommended by your doctor to ensure your health is properly tracked.
Although this medication helps manage HIV, it is not a cure. Continue taking this drug as directed by your doctor or healthcare provider, even if you feel well, to maintain its effectiveness. Regular appointments with your doctor are vital to monitor your progress and adjust treatment as needed.
This medication works by reducing the amount of HIV in your blood. By lowering the viral load to undetectable levels, you can significantly reduce the risk of transmitting HIV to others. However, it is crucial to combine this treatment with other preventive measures, such as using condoms during sexual activity and avoiding shared use of needles and injection equipment. Consult with your doctor or healthcare provider to discuss the most effective ways to prevent HIV transmission and develop a comprehensive prevention plan.
When taking this drug, it may be necessary to adjust the timing of other medications to avoid interactions. Consult with your doctor or pharmacist to determine the best schedule for taking your medications.
Regular blood tests and laboratory evaluations are crucial to monitor your condition. Adhere to the schedule recommended by your doctor to ensure your health is properly tracked.
Although this medication helps manage HIV, it is not a cure. Continue taking this drug as directed by your doctor or healthcare provider, even if you feel well, to maintain its effectiveness. Regular appointments with your doctor are vital to monitor your progress and adjust treatment as needed.
This medication works by reducing the amount of HIV in your blood. By lowering the viral load to undetectable levels, you can significantly reduce the risk of transmitting HIV to others. However, it is crucial to combine this treatment with other preventive measures, such as using condoms during sexual activity and avoiding shared use of needles and injection equipment. Consult with your doctor or healthcare provider to discuss the most effective ways to prevent HIV transmission and develop a comprehensive prevention plan.
Overdose Information
Overdose Symptoms:
- Limited data on acute overdose. Symptoms may include exaggerated adverse effects such as gastrointestinal upset, rash, or headache.
What to Do:
Call 1-800-222-1222 (Poison Control Center) immediately. Treatment is generally supportive, as dolutegravir is highly protein bound and not significantly removed by dialysis.
Drug Interactions
Contraindicated Interactions
- Dofetilide (risk of increased dofetilide concentrations and severe arrhythmias)
Major Interactions
- Polyvalent cation-containing antacids, laxatives, sucralfate, iron supplements, calcium supplements (decreased dolutegravir absorption; separate administration by at least 2 hours before or 6 hours after)
- Rifampin (decreased dolutegravir concentrations; increase dolutegravir dose to 50 mg twice daily)
- Carbamazepine, Oxcarbazepine, Phenobarbital, Phenytoin (potential for decreased dolutegravir concentrations; consider alternative or increase dolutegravir dose to 50 mg twice daily)
- Etravirine (without boosted protease inhibitors or other INSTIs; decreased dolutegravir concentrations; increase dolutegravir dose to 50 mg twice daily)
- Metformin (increased metformin concentrations; monitor for metformin-related adverse effects, consider dose reduction of metformin)
Moderate Interactions
- St. John's Wort (potential for decreased dolutegravir concentrations; avoid co-administration)
- Tipranavir/ritonavir (potential for decreased dolutegravir concentrations; monitor viral load)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
HIV-1 viral load
Rationale: To establish baseline disease activity and monitor treatment efficacy.
Timing: Prior to initiation of therapy
CD4+ T-cell count
Rationale: To assess immune status and monitor treatment efficacy.
Timing: Prior to initiation of therapy
Renal function (serum creatinine, eGFR)
Rationale: To assess baseline kidney function and monitor for potential changes, especially with co-administered drugs.
Timing: Prior to initiation of therapy
Liver function tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function and monitor for potential hepatotoxicity.
Timing: Prior to initiation of therapy
Pregnancy test
Rationale: For females of childbearing potential, due to potential risk of neural tube defects.
Timing: Prior to initiation of therapy
Routine Monitoring
HIV-1 viral load
Frequency: Every 4-8 weeks after initiation, then every 3-6 months once suppressed
Target: Undetectable (<20-50 copies/mL)
Action Threshold: Persistent detectable viral load or viral rebound
CD4+ T-cell count
Frequency: Every 3-6 months (or less frequently if stable and suppressed)
Target: Increasing or stable
Action Threshold: Significant decline
Renal function (serum creatinine, eGFR)
Frequency: Every 6-12 months, or more frequently if co-morbidities or co-medications warrant
Target: Stable within normal limits
Action Threshold: Significant increase in creatinine or decrease in eGFR
Liver function tests (ALT, AST, bilirubin)
Frequency: Periodically, or if symptoms of liver dysfunction develop
Target: Within normal limits
Action Threshold: Significant elevation (e.g., >5x ULN)
Weight
Frequency: Periodically
Target: Stable
Action Threshold: Significant unexplained weight gain
Symptom Monitoring
- Hypersensitivity reactions (rash, fever, malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, eosinophilia, angioedema, difficulty breathing)
- Hepatotoxicity (dark urine, pale stools, yellowing of skin or eyes, nausea, vomiting, abdominal pain)
- Neuropsychiatric symptoms (depression, anxiety, insomnia, suicidal ideation or attempts, particularly in patients with pre-existing mental health conditions)
- Immune Reconstitution Inflammatory Syndrome (IRIS) (worsening of pre-existing opportunistic infections or inflammatory conditions)
- Weight gain
Special Patient Groups
Pregnancy
Dolutegravir is a preferred antiretroviral option for most pregnant individuals with HIV. However, there was an initial signal of a potential increased risk of neural tube defects (NTDs) when dolutegravir was initiated at the time of conception. Current guidelines recommend discussing this risk with patients who are pregnant or planning to become pregnant. For those already pregnant, continuing dolutegravir is generally recommended.
Trimester-Specific Risks:
First Trimester:
Potential small increased risk of neural tube defects if initiated at conception or in early first trimester. Risk appears to be very low with continued use.
Second Trimester:
Generally considered safe and effective.
Third Trimester:
Generally considered safe and effective.
Lactation
Breastfeeding is not recommended for mothers with HIV in developed countries due to the risk of HIV transmission to the infant. Additionally, dolutegravir is excreted in human milk, and the effects on a breastfed infant are unknown.
Infant Risk:
L5 (Contraindicated/High Risk) - Risk of HIV transmission, unknown effects of dolutegravir exposure.
Pediatric Use
Dolutegravir is approved for use in pediatric patients aged âĨ4 weeks and weighing âĨ3 kg. Dosing is weight-based, with dispersible tablets (Tivicay PD) available for younger/lighter children. Close monitoring for adverse effects is important.
Geriatric Use
No specific dose adjustment is required for elderly patients. However, caution is advised due to the higher likelihood of decreased renal, hepatic, or cardiac function, and concomitant disease or other drug therapy. Monitor for age-related decline in organ function.
Clinical Information
Clinical Pearls
- Dolutegravir is a highly effective and generally well-tolerated INSTI, often used as a cornerstone of first-line HIV regimens.
- Counsel patients on the importance of strict adherence to prevent resistance development.
- Emphasize the need to separate dolutegravir from polyvalent cation-containing products (antacids, iron/calcium supplements) to ensure adequate absorption.
- Be aware of the potential for neuropsychiatric adverse events, especially in patients with pre-existing mental health conditions. Monitor and counsel patients on these symptoms.
- Monitor for signs of hypersensitivity reaction, which can be severe and involve multi-organ dysfunction.
- Dolutegravir can increase metformin concentrations; monitor patients on metformin for adverse effects and consider metformin dose reduction.
- While the neural tube defect signal in pregnancy has been largely mitigated by more data, it's crucial to discuss this with women of childbearing potential and those planning pregnancy.
Alternative Therapies
- Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) (e.g., efavirenz, rilpivirine, doravirine)
- Protease Inhibitors (PIs) (e.g., darunavir, atazanavir, lopinavir/ritonavir)
- Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) (e.g., tenofovir, emtricitabine, lamivudine, abacavir)
- Fusion Inhibitors (e.g., enfuvirtide)
- CCR5 Antagonists (e.g., maraviroc)
- Post-attachment Inhibitors (e.g., fostemsavir)
Cost & Coverage
Average Cost:
Varies widely, typically $1,000 - $2,000+ per 30 tablets
Insurance Coverage:
Tier 2 or Tier 3 (Specialty Drug)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened.