Tivicay 25mg 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 HIV and increase your immune system's strength.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most out of your medication, follow these guidelines:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
You can take this medication with or without food.
It's crucial that you don't miss or skip a dose during treatment. If you're taking products that contain iron, aluminum, calcium, magnesium, or zinc (such as certain antacids or vitamins), a buffered product, or sucralfate, you may need to take them at a different time than your medication. Consult with your doctor or pharmacist to determine the best schedule.
When you receive a new prescription, verify that you have the correct medication. If you're unsure or think you've been given the wrong medication, contact your doctor immediately.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding the bathroom.
Keep the lid tightly closed.
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 have access to drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, follow these steps:
Take the missed dose as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and resume your regular 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 medication, follow these guidelines:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
You can take this medication with or without food.
It's crucial that you don't miss or skip a dose during treatment. If you're taking products that contain iron, aluminum, calcium, magnesium, or zinc (such as certain antacids or vitamins), a buffered product, or sucralfate, you may need to take them at a different time than your medication. Consult with your doctor or pharmacist to determine the best schedule.
When you receive a new prescription, verify that you have the correct medication. If you're unsure or think you've been given the wrong medication, contact your doctor immediately.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding the bathroom.
Keep the lid tightly closed.
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 have access to drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, follow these steps:
Take the missed dose as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and resume your regular 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 the medication exactly as prescribed by your doctor, usually once daily. Do not miss doses.
- It can be taken with or without food.
- If you are taking antacids, laxatives, iron supplements, or calcium supplements, take dolutegravir at least 2 hours before or 6 hours after these products.
- Do not stop taking dolutegravir without talking to your doctor, as this can lead to the virus becoming resistant to the medication.
- Maintain regular doctor appointments and laboratory tests to monitor your HIV infection and medication effectiveness.
- This medication does not cure HIV infection or prevent its transmission to others. Continue to practice safe sex and avoid sharing needles.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
50 mg once daily
Dose Range:
25 - 100 mg
Condition-Specific Dosing:
treatmentNaiveOrExperiencedINSTINaive:
50 mg once daily
withCertainInteractingDrugs:
50 mg twice daily (e.g., rifampin, carbamazepine, efavirenz, nevirapine, tipranavir/ritonavir, fosamprenavir/ritonavir, etravirine without boosted PIs)
INSTIExperiencedWithResistance:
50 mg twice daily (with certain INSTI resistance mutations or clinical suspicion of resistance)
Pediatric Dosing
Neonatal:
Not established (Tivicay tablets)
Infant:
Not established (Tivicay tablets)
Child:
Weight-based dosing for children weighing at least 14 kg. For 25mg/50mg tablets: 20 to <30 kg: 35 mg once daily (using 25mg tablet + 10mg from dispersible or 5mg tablets). âĨ30 kg: 50 mg once daily.
Adolescent:
âĨ30 kg: 50 mg once daily
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed (CrCl >10 mL/min). Not studied in ESRD on dialysis.
Dialysis:
No specific recommendations; unlikely to require adjustment due to minimal renal excretion.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A)
Moderate:
No dose adjustment needed (Child-Pugh B)
Severe:
Not studied (Child-Pugh C). Use with caution.
Pharmacology
Mechanism of Action
Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration. This step is essential for the HIV replication cycle.
Pharmacokinetics
Absorption:
Bioavailability:
Not formally established, but high. Food increases AUC and Cmax.
Tmax:
2-7 hours
FoodEffect:
Food (especially high-fat meal) increases dolutegravir exposure (AUC and Cmax) but is not required for administration. Can be taken with or without food.
Distribution:
Vd:
Approximately 17.4 L
ProteinBinding:
>99% (primarily to plasma albumin)
CnssPenetration:
Yes, dolutegravir penetrates the cerebrospinal fluid (CSF) with CSF concentrations therapeutically relevant.
Elimination:
HalfLife:
Approximately 14 hours
Clearance:
Not available (systemic clearance is approximately 1 L/hr)
ExcretionRoute:
Primarily fecal (53% of total dose, 32% as unchanged drug); renal excretion is minimal (<1% as unchanged drug).
Unchanged:
32% (feces), <1% (urine)
Pharmacodynamics
OnsetOfAction:
Rapid (viral load reduction observed within days of initiation)
PeakEffect:
Steady-state concentrations achieved within approximately 5 days of once-daily dosing.
DurationOfAction:
Sustained viral suppression with once-daily dosing due to long half-life and high barrier to resistance.
Confidence:
Medium
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
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
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
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
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:
- Severe skin rash or allergic reaction (e.g., rash with fever, blistering, mouth sores, swelling of face/lips/tongue, muscle/joint aches, general ill feeling)
- Signs of liver problems (e.g., yellowing of skin or eyes, dark urine, pale stools, severe stomach pain, nausea, vomiting)
- New or worsening mood changes, depression, anxiety, or thoughts of self-harm, especially if you have a history of mental health issues.
- New or worsening muscle pain or weakness.
- Symptoms of immune reconstitution inflammatory syndrome (IRIS) such as fever, swollen lymph nodes, worsening of existing infections, or new infections.
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 allergic reaction 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 includes exploring the best ways to prevent transmitting HIV to your baby.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, 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 verify that it is safe to take this medication in conjunction with your other treatments.
* Never start, stop, or modify 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 allergic reaction 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 includes exploring the best ways to prevent transmitting HIV to your baby.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, 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 verify that it is safe to take this medication in conjunction with your other treatments.
* Never start, stop, or modify 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 other medications, it may be necessary to adjust the timing of their administration to avoid interactions with this drug. Consult 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.
This medication is not a cure for HIV, and it is vital to continue taking it as directed by your doctor or healthcare provider, even if you feel well. Maintain regular appointments with your doctor to ensure ongoing care and monitoring.
This drug works by reducing the amount of HIV in your blood. By lowering the viral load to undetectable levels, you can significantly decrease 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 the sharing of needles and injection equipment. Consult your doctor or healthcare provider to discuss the most effective ways to prevent the spread of HIV.
When taking other medications, it may be necessary to adjust the timing of their administration to avoid interactions with this drug. Consult 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.
This medication is not a cure for HIV, and it is vital to continue taking it as directed by your doctor or healthcare provider, even if you feel well. Maintain regular appointments with your doctor to ensure ongoing care and monitoring.
This drug works by reducing the amount of HIV in your blood. By lowering the viral load to undetectable levels, you can significantly decrease 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 the sharing of needles and injection equipment. Consult your doctor or healthcare provider to discuss the most effective ways to prevent the spread of HIV.
Overdose Information
Overdose Symptoms:
- Limited experience with overdose. Symptoms are likely an exaggeration of known side effects (e.g., gastrointestinal upset, rash, headache).
What to Do:
There is no specific antidote for dolutegravir overdose. Treatment should be symptomatic and supportive. Contact a poison control center immediately (e.g., 1-800-222-1222 in the US).
Drug Interactions
Contraindicated Interactions
- Dofetilide (increases dofetilide concentrations, risk of life-threatening arrhythmias)
Major Interactions
- Polyvalent cation-containing antacids, laxatives, iron supplements, calcium supplements (reduce dolutegravir absorption; separate administration by at least 2 hours before or 6 hours after)
- Rifampin (requires dolutegravir 50 mg twice daily)
- Carbamazepine (requires dolutegravir 50 mg twice daily)
- Etravirine (without boosted protease inhibitors; requires dolutegravir 50 mg twice daily)
- Efavirenz (requires dolutegravir 50 mg twice daily)
- Nevirapine (requires dolutegravir 50 mg twice daily)
- Tipranavir/ritonavir (requires dolutegravir 50 mg twice daily)
- Fosamprenavir/ritonavir (requires dolutegravir 50 mg twice daily)
- Metformin (increases metformin concentrations; monitor renal function, consider metformin dose reduction)
Moderate Interactions
- St. John's Wort (may decrease dolutegravir levels; avoid co-administration)
- Orlistat (may decrease dolutegravir absorption; separate administration)
- Dexamethasone (systemic, may decrease dolutegravir levels; monitor for efficacy)
Minor Interactions
- No clinically significant minor interactions requiring dose adjustment or specific monitoring are commonly cited beyond the major interactions.
Monitoring
Baseline Monitoring
HIV-1 viral load
Rationale: To establish baseline disease activity and monitor treatment response.
Timing: Prior to initiation of therapy
CD4+ T-cell count
Rationale: To assess immune status and monitor immune reconstitution.
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 like metformin.
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
Hepatitis B and C serology
Rationale: To identify co-infection, which may influence treatment decisions and monitoring for liver toxicity.
Timing: Prior to initiation of therapy
Pregnancy test (for females of childbearing potential)
Rationale: To rule out pregnancy due to potential risk of neural tube defects if taken at conception.
Timing: Prior to initiation of therapy
Routine Monitoring
HIV-1 viral load
Frequency: Every 4-8 weeks after initiation until undetectable, then every 3-6 months
Target: <20-50 copies/mL (undetectable)
Action Threshold: Persistent detectable viral load or viral rebound indicates potential treatment failure or resistance; investigate adherence or resistance.
CD4+ T-cell count
Frequency: Every 3-6 months (or as clinically indicated once stable)
Target: Increasing or stable
Action Threshold: Significant decline may indicate treatment failure or other immune-compromising conditions.
Renal function (serum creatinine, eGFR)
Frequency: Every 3-6 months, or more frequently if co-administered with metformin or other nephrotoxic agents
Target: Stable or within normal limits
Action Threshold: Significant increase in creatinine or decrease in eGFR may warrant investigation or dose adjustment of co-medications.
Liver function tests (ALT, AST, bilirubin)
Frequency: Every 3-6 months, or as clinically indicated
Target: Within normal limits
Action Threshold: Significant elevation may indicate hepatotoxicity; investigate and consider treatment modification.
Symptom Monitoring
- Hypersensitivity reactions (rash, fever, fatigue, myalgia, arthralgia, blistering, oral lesions, conjunctivitis, facial edema, angioedema, hepatitis, eosinophilia)
- Signs/symptoms of hepatotoxicity (e.g., jaundice, dark urine, nausea, vomiting, abdominal pain)
- Neuropsychiatric symptoms (e.g., depression, anxiety, insomnia, suicidal ideation, especially in patients with pre-existing psychiatric conditions)
- Signs of immune reconstitution inflammatory syndrome (IRIS)
- New or worsening muscle pain or weakness (rhabdomyolysis, though rare)
Special Patient Groups
Pregnancy
Dolutegravir is generally recommended for use in pregnancy due to its efficacy and high barrier to resistance, particularly after the first trimester. However, there was an initial signal of a small increased risk of neural tube defects when dolutegravir was taken at the time of conception. Current data suggests this risk is very low, but counseling should occur.
Trimester-Specific Risks:
First Trimester:
Small, but increased, risk of neural tube defects if initiated at the time of conception. For women already on dolutegravir and becoming pregnant, continuation is generally recommended. For women initiating ART in the first trimester, alternative regimens may be considered, but dolutegravir remains an option with informed consent.
Second Trimester:
Generally considered safe and recommended for initiation or continuation.
Third Trimester:
Generally considered safe and recommended for initiation or continuation.
Lactation
Not recommended. Dolutegravir is excreted in human milk. The potential for HIV transmission through breast milk and the unknown effects of dolutegravir on breastfed infants outweigh the benefits of breastfeeding.
Infant Risk:
Potential for drug exposure in infant, unknown long-term effects, and risk of HIV transmission.
Pediatric Use
Dolutegravir is approved for use in pediatric patients weighing at least 14 kg. Dosing is weight-based. Dispersible tablets (Tivicay PD) are available for younger children and those weighing less than 20 kg, allowing for more precise dosing.
Geriatric Use
No dose adjustment is required for patients >65 years of age. However, geriatric patients may have reduced renal or hepatic function, and co-morbidities or co-medications should be considered.
Clinical Information
Clinical Pearls
- Dolutegravir has a high barrier to resistance, making it a robust option for initial HIV treatment.
- Generally well-tolerated, with common side effects including insomnia, headache, and nausea.
- Important to counsel patients on the need to separate dolutegravir from polyvalent cation-containing products (antacids, iron, calcium supplements).
- Monitor for neuropsychiatric symptoms, especially in patients with pre-existing psychiatric conditions, as these can occur.
- There is a potential for weight gain with dolutegravir-containing regimens, which should be monitored.
- Consider 50 mg BID dosing in patients with certain drug interactions or documented INSTI resistance.
Alternative Therapies
- Bictegravir (e.g., Biktarvy)
- Raltegravir (Isentress)
- Elvitegravir/cobicistat (e.g., Genvoya, Stribild)
- Other classes of antiretrovirals (e.g., NNRTIs like doravirine, PIs like darunavir, NRTIs like tenofovir/emtricitabine)
Cost & Coverage
Average Cost:
Varies widely, typically $1,500 - $2,500+ per 30 tablets
Insurance Coverage:
Tier 3 or Specialty Tier (requires prior authorization)
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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 details about the medication taken, the amount, and the time it happened.