Tivicay 10mg Tablets
It is used to treat HIV infection.
Drug Class
Antiretroviral
Pharmacologic Class
Integrase Strand Transfer Inhibitor (INSTI)
Pregnancy Category
Not applicable (modern labeling)
FDA Approved
Aug 2013
DEA Schedule
Not Controlled
Overview
What is this medicine?
Dolutegravir is a medicine used to treat HIV (Human Immunodeficiency Virus) infection. It works by stopping the virus from making copies of itself inside your body, which helps to reduce the amount of virus and improve your immune system. This specific 10mg tablet is often used for children.
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.
Keep 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.
Keep 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 a day. Do not skip doses.
- If you are taking antacids, laxatives, or supplements containing calcium, iron, magnesium, or aluminum, take dolutegravir at least 2 hours before or 6 hours after these products. Alternatively, if taken with food, dolutegravir and supplements can be taken together.
- Maintain regular appointments with your healthcare provider for blood tests and monitoring.
- Practice safe sex to prevent HIV transmission to others.
- Do not stop taking dolutegravir without consulting your doctor, as this can lead to drug resistance and worsening of your condition.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Not applicable for 10mg tablet. Adult standard dose is 50 mg once daily.
Condition-Specific Dosing:
INSTI_resistance_or_certain_inducers:
Not applicable for 10mg tablet. Adult dose is 50 mg twice daily.
Pediatric Dosing
Neonatal:
Not established for 10mg tablet (typically for older infants/children).
Infant:
Weight-based dosing: 6 to <10 kg: 15 mg once daily (using 5mg or 25mg dispersible tablets or 5mg film-coated tablets). 10 to <14 kg: 20 mg once daily (using 5mg or 25mg dispersible tablets or 5mg film-coated tablets). 14 to <20 kg: 25 mg once daily (using 5mg or 25mg dispersible tablets or 5mg film-coated tablets). The 10mg tablet is for specific weight bands.
Child:
Weight-based dosing: 20 to <30 kg: 30 mg once daily (using 10mg or 25mg film-coated tablets). 30 to <40 kg: 35 mg once daily (using 10mg or 25mg film-coated tablets). âĨ40 kg: 50 mg once daily (using 50mg film-coated tablets).
Adolescent:
Weight-based dosing: âĨ40 kg: 50 mg once daily (using 50mg film-coated tablets).
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment required.
Moderate:
No dosage adjustment required.
Severe:
No dosage adjustment required (CrCl <30 mL/min).
Dialysis:
No dosage adjustment required for patients on dialysis.
Hepatic Impairment:
Mild:
No dosage adjustment required (Child-Pugh A).
Moderate:
No dosage adjustment required (Child-Pugh B).
Severe:
No dosage adjustment required (Child-Pugh C).
Pharmacology
Mechanism of Action
Dolutegravir is an integrase strand transfer inhibitor (INSTI). It inhibits HIV integrase by binding to the active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration, which is essential for the HIV replication cycle. This prevents the integration of viral DNA into the host cell genome.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80%
Tmax:
2-3 hours
FoodEffect:
Food increases the extent of absorption (AUC) and prolongs Tmax, but this is not considered clinically significant for once-daily dosing. Can be taken with or without food.
Distribution:
Vd:
Approximately 17.4 L (apparent volume of distribution)
ProteinBinding:
>99% (primarily to plasma albumin)
CnssPenetration:
Yes (CSF concentrations are approximately 1-2% of unbound plasma concentrations, sufficient to inhibit HIV replication in CSF).
Elimination:
HalfLife:
Approximately 14 hours
Clearance:
Approximately 0.94 L/hr (apparent oral clearance)
ExcretionRoute:
Primarily fecal (approximately 53% as unchanged drug), with renal excretion accounting for less than 1% of the dose.
Unchanged:
Approximately 53% (fecal), <1% (renal)
Pharmacodynamics
OnsetOfAction:
Rapid (viral load reduction observed within days)
PeakEffect:
Not directly applicable for chronic antiviral therapy; sustained viral suppression is the goal.
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 Attention Immediately
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 or seek medical help right away:
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
Additionally, changes in your immune system can occur when starting HIV treatment. If you have an underlying infection, it may become apparent after taking this medication. Inform your doctor immediately if you experience any new symptoms, even if they appear after several months of treatment. 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 have mild 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 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, 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 or seek medical help right away:
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
Additionally, changes in your immune system can occur when starting HIV treatment. If you have an underlying infection, it may become apparent after taking this medication. Inform your doctor immediately if you experience any new symptoms, even if they appear after several months of treatment. 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 have mild 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 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, 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 reaction (hypersensitivity): rash, fever, feeling unwell, muscle or joint aches, blisters, mouth sores, eye redness, swelling of the face or mouth, trouble breathing. Seek immediate medical attention.
- Signs of liver problems: yellowing of the skin or eyes (jaundice), dark urine, pale stools, nausea, vomiting, stomach pain.
- New or worsening mental health problems: severe depression, anxiety, agitation, suicidal thoughts or actions (especially if you have a history of mental illness).
- 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 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 conversation will also include the best methods 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 conversation will also include the best methods 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 this drug, be aware that other medications may need to be taken at a different time to avoid interactions. Consult your doctor or pharmacist to determine the best schedule for taking your medications.
Regular blood work and laboratory tests are crucial to monitor your condition. Adhere to the testing schedule recommended by your doctor to ensure the medication's effectiveness and your overall health.
It is important to understand that this medication is not a cure for HIV. Continue taking this drug as directed by your doctor or healthcare provider, even if you feel well, to maintain control over the virus. Regular appointments with your doctor are necessary to monitor your condition and adjust treatment as needed.
This medication helps reduce the amount of HIV in your blood, which can lower the risk of transmitting the virus 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 to others.
When taking this drug, be aware that other medications may need to be taken at a different time to avoid interactions. Consult your doctor or pharmacist to determine the best schedule for taking your medications.
Regular blood work and laboratory tests are crucial to monitor your condition. Adhere to the testing schedule recommended by your doctor to ensure the medication's effectiveness and your overall health.
It is important to understand that this medication is not a cure for HIV. Continue taking this drug as directed by your doctor or healthcare provider, even if you feel well, to maintain control over the virus. Regular appointments with your doctor are necessary to monitor your condition and adjust treatment as needed.
This medication helps reduce the amount of HIV in your blood, which can lower the risk of transmitting the virus 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 to others.
Overdose Information
Overdose Symptoms:
- Limited experience with overdose. Symptoms may include exaggeration of known adverse effects such as headache, insomnia, nausea, or rash.
What to Do:
There is no specific antidote for dolutegravir overdose. Treatment should be supportive, with monitoring of vital signs and observation of the patient's clinical status. Hemodialysis is unlikely to be effective due to high protein binding. Contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Major Interactions
- Dofetilide (increased dofetilide levels, risk of serious arrhythmias)
- Certain polyvalent cation-containing antacids/laxatives/supplements (e.g., calcium, iron, magnesium, aluminum) if not separated in time
- Rifampin (decreased dolutegravir levels, requires dolutegravir dose adjustment to 50 mg twice daily)
- Carbamazepine, Oxcarbazepine, Phenytoin, Phenobarbital (decreased dolutegravir levels, requires dolutegravir dose adjustment to 50 mg twice daily)
- Etravirine (without boosted protease inhibitors or other INSTIs, decreased dolutegravir levels, requires dolutegravir dose adjustment to 50 mg twice daily)
- Efavirenz, Nevirapine, Tipranavir/ritonavir (decreased dolutegravir levels, requires dolutegravir dose adjustment to 50 mg twice daily)
Moderate Interactions
- Metformin (dolutegravir increases metformin exposure; consider dose reduction of metformin)
- St. John's Wort (potential for decreased dolutegravir levels)
Confidence Interactions
Monitoring
Baseline Monitoring
HIV-1 RNA (viral load)
Rationale: To establish baseline and monitor treatment efficacy.
Timing: Prior to initiation of therapy.
CD4+ T-cell count
Rationale: To establish baseline and monitor immune status.
Timing: Prior to initiation of therapy.
Liver function tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function and monitor for drug-induced liver injury.
Timing: Prior to initiation of therapy.
Renal function (serum creatinine, eGFR)
Rationale: To assess baseline renal function. Dolutegravir can cause a small, reversible increase in serum creatinine due to inhibition of tubular secretion, without affecting GFR.
Timing: Prior to initiation of therapy.
Pregnancy test (for females of childbearing potential)
Rationale: To rule out pregnancy before starting therapy due to potential (though low) risk of neural tube defects.
Timing: Prior to initiation of therapy.
Routine Monitoring
HIV-1 RNA (viral load)
Frequency: Every 4-8 weeks after initiation until undetectable, then every 3-6 months.
Target: Undetectable (<20-50 copies/mL)
Action Threshold: Persistent detectable viral load or viral rebound indicates treatment failure or resistance.
CD4+ T-cell count
Frequency: Every 3-6 months (less frequent once immune reconstitution is stable).
Target: Increasing towards normal range
Action Threshold: Declining CD4 count may indicate treatment failure or other immune compromise.
Liver function tests (ALT, AST, bilirubin)
Frequency: Periodically, or as clinically indicated, especially in patients with pre-existing liver disease.
Target: Within normal limits
Action Threshold: Significant elevations may require investigation and potential drug discontinuation.
Renal function (serum creatinine, eGFR)
Frequency: Periodically, or as clinically indicated.
Target: Stable, within acceptable limits (acknowledging slight increase from DTG)
Action Threshold: Significant or progressive increase in creatinine may warrant further investigation.
Weight
Frequency: Periodically
Target: Stable or healthy weight gain
Action Threshold: Significant or rapid weight gain should be monitored.
Symptom Monitoring
- Hypersensitivity reactions (rash, fever, malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, eosinophilia, angioedema, dyspnea, liver enzyme elevations)
- Liver toxicity (nausea, vomiting, abdominal pain, dark urine, jaundice)
- Neurological symptoms (insomnia, headache, dizziness, depression, anxiety, suicidal ideation, particularly in patients with pre-existing psychiatric conditions)
- Signs of immune reconstitution inflammatory syndrome (IRIS) (worsening of pre-existing opportunistic infections or new infections/inflammatory conditions)
Special Patient Groups
Pregnancy
Dolutegravir is a preferred antiretroviral in pregnancy. Initial concerns about a potential association with neural tube defects (NTDs) when initiated at conception have largely been mitigated by subsequent data showing a very low risk, comparable to other antiretrovirals. The benefits of viral suppression in pregnancy generally outweigh the low theoretical risk.
Trimester-Specific Risks:
First Trimester:
Low, but slightly elevated theoretical risk of neural tube defects if initiated at the time of conception. Current data suggest this risk is very low and comparable to other ARTs. Continued use is generally recommended if already on therapy.
Second Trimester:
Generally considered safe and recommended for initiation or continuation.
Third Trimester:
Generally considered safe and recommended for initiation or continuation.
Lactation
Breastfeeding is generally not recommended for mothers with HIV in developed countries due to the risk of HIV transmission to the infant. However, if breastfeeding occurs, dolutegravir is excreted into human milk at low concentrations. The potential for adverse effects in breastfed infants is low, but long-term effects are unknown.
Infant Risk:
Low systemic exposure in infants; potential for adverse effects is low, but long-term data are limited. Risk of HIV transmission remains the primary concern.
Pediatric Use
Dolutegravir is approved for use in pediatric patients weighing at least 3 kg. Dosing is weight-based and specific formulations (dispersible tablets, 5mg film-coated, 10mg film-coated, 25mg film-coated, 50mg film-coated) are available to facilitate accurate dosing across different weight bands. The 10mg tablet is specifically for children weighing 20 to <40 kg.
Geriatric Use
No specific dosage adjustment is required for elderly patients. However, caution should be exercised due to the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Dolutegravir has a high barrier to resistance, making it a robust component of initial HIV regimens.
- Generally well-tolerated, with common side effects including insomnia, headache, and nausea.
- Can be taken with or without food, but polyvalent cation-containing antacids/supplements require separation or co-administration with food.
- Monitor for neuropsychiatric symptoms, especially in patients with pre-existing mental health conditions.
- While initial concerns about neural tube defects in pregnancy have largely been alleviated, discuss risks and benefits with pregnant patients.
- Dolutegravir can cause a small, reversible increase in serum creatinine due to inhibition of tubular secretion of creatinine, which is not indicative of true renal dysfunction.
Alternative Therapies
- Other Integrase Strand Transfer Inhibitors (INSTIs): Bictegravir, Raltegravir, Elvitegravir (co-formulated with cobicistat)
- Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs): Efavirenz, Rilpivirine, Doravirine
- Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs): Tenofovir alafenamide (TAF), Tenofovir disoproxil fumarate (TDF), Emtricitabine, Lamivudine, Abacavir
- Protease Inhibitors (PIs): Darunavir, Atazanavir, Lopinavir/ritonavir (usually boosted)
- Entry Inhibitors: Enfuvirtide, Maraviroc
Cost & Coverage
Average Cost:
Varies widely, typically several hundred to over a thousand USD per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.