Stribild

Stribild is part of the drug class:

• Antivirals for treatment of HIV infections, combinations

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. 

Do not take Stribild if you also take a medicine that contains:

• alfuzosin hydrochloride (Uroxatral)
• cisapride (Propulsid, Propulsid Quicksolv)
• ergot-containing medicines, including:
  • dihydroergotamine mesylate (D.H.E. 45, Migranal)
  • ergotamine tartrate (Cafergot, Migergot, Ergostat, Medihaler Ergotamine, Wigraine, Wigrettes)
  • methylergonovine maleate (Ergotrate, Methergine)
• lovastatin (Advicor, Altoprev, Mevacor)
• oral midazolam
• pimozide (ORAP)
• rifampin (Rifadin, Rifamate, Rifater, Rimactane)
• sildenafil (Revatio), when used for treating the lung problem, pulmonary arterial hypertension (PAH)
• simvastatin (Simcor, Vytorin, Zocor)
• triazolam (Halcion)
• St. John's wort (Hypericum perforatum) or a product that contains St. John's wort

You should not take Stribild if you also take:

• any other medicines to treat HIV-1 infection
• other medicines that contain tenofovir (Atripla, Complera, Viread, Truvada)
• other medicines that contain emtricitabine or lamivudine (Combivir, Emtriva, Epivir, or Epivir-HBV, Epzicom, Trizivir)
• adefovir (Hepsera)

Especially tell your healthcare provider if you take:

• hormone-based contraceptives (birth control pills and patches)
• an antacid medicine that contains aluminum, magnesium hydroxide, or calcium carbonate. Take antacids at least 2 hours before or after you take Stribild.
• medicines to treat depression
• medicines to prevent organ transplant rejection
• medicines to treat high blood pressure
• any of the following medicines:
  • amiodarone (Cordarone, Pacerone)
  • atorvastatin (Lipitor, Caduet)
  • bepridil hydrochloric (Vascor, Bepadin)
  • bosentan (Tracleer)
  • buspirone
  • carbamazepine (Carbatrol, Epitol, Equetro, Tegreto)
  • clarithromycin (Biaxin, Prevpac)
  • clonazepam (Klonopin)
  • clorazepate (Gen-Xene, Tranxene)
  • colchicine (Colcrys)
  • medicines that contain dexamethasone
  • diazepam (Valium)
  • digoxin (Lanoxin)
  • disopyramide (Norpace)
  • estazolam
  • ethosuximide (Zarontin)
  • flecainide (Tambocor)
  • flurazepam
  • fluticasone (Flovent, Flonase, Flovent Diskus, Flovent HFA, Veramyst)
  • itraconazole (Sporanox)
  • ketoconazole (Nizoral)
  • lidocaine (Xylocaine)
  • mexiletine
  • oxcarbazepine (Trileptal)
  • perphenazine
  • phenobarbital (Luminal)
  • phenytoin (Dilantin, Phenytek)
  • propafenone (Rythmol)
  • quinidine (Neudexta)
  • rifabutin (Mycobutin)
  • rifapentine (Priftin)
  • risperidone (Risperdal, Risperdal, Consta)
  • salmeterol (Serevent) or salmeterol when taken in combination with fluticasone (Advair Diskus, Advair HFA)
  • sildenafil (Viagra), tadalafil (Cialis) or vardenafil (Levitra, Staxyn), for the treatment of erectile dysfunction (ED). If you get dizzy or faint (low blood pressure), have vision changes or have an erection that last longer than 4 hours, call your healthcare provider or get medical help right away.
  • tadalafil (Adcirca), for the treatment of pulmonary arterial hypertension
  • telithromycin (Ketek)
  • thioridazine
  • voriconazole (Vfend)
  • warfarin (Coumadin, Jantoven)
  • zolpidem (Ambien, Edluar, Intermezzo, Zolpimist)

Ask your healthcare provider or pharmacist if you are not sure if your medicine is one that is listed above. Do not start any new medicines while you are taking Stribild without first talking with your healthcare provider or pharmacist.

Know the medicines you take. Keep a list of your medicines and show it to your healthcare provider and pharmacist when you get a new medicine.

Stribild can cause serious side effects, including:

New or worse kidney problems, including kidney failure. Your healthcare provider should do blood and urine tests to check your kidneys before you start and while you are taking Stribild. Your healthcare provider may tell you to stop taking Stribild if you develop new or worse kidney problems.

Bone problems can happen in some people who take this medication. Bone problems include bone pain, softening or thinning (which may lead to fractures). Your healthcare provider may need to do tests to check your bones.

Changes in body fat can happen in people who take HIV-1 medicine. These changes may include increased amount of fat in the upper back and neck ("buffalo hump"), breast, and around the middle of your body (trunk). Loss of fat from the legs, arms and face may also happen. The exact cause and long-term health effects of these conditions are not known.

Changes in your immune system (Immune Reconstitution Syndrome) can happen when you start taking HIV-1 medicines. Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time. Tell your healthcare provider right away if you start having any new symptoms after starting your HIV-1 medicine.

• Do not run out of Stribild. Refill your prescription or talk to your healthcare provider before your it is all gone.
• Do not stop taking Stribild without first talking to your healthcare provider.
• If you stop taking Stribild, your healthcare provider will need to check your health often and do blood tests regularly for several months to check your HBV infection. Tell your healthcare provider about any new or unusual symptoms you may have after you stop taking this medication.

• feel very weak or tired
• have unusual (not normal) muscle pain
• have trouble breathing
• have stomach pain with nausea or vomiting
• feel cold, especially in your arms and legs
• feel dizzy or lightheaded
• have a fast or irregular heartbeat

• your skin or the white part of your eyes turns yellow (jaundice)
• dark "tea-colored" urine
• light-colored bowel movements (stools)
• loss of appetite for several days or longer
• nausea
• stomach pain

You may be more likely to get lactic acidosis or severe liver problems if you are female, very overweight (obese), or have been taking Stribild for a long time.

• alfuzosin hydrochloride (Uroxatral)
• cisapride (Propulsid)
• lovastatin (Advicor, Altoprev, Mevacor)
• oral midazolam
• pimozide (Orap)
• rifampin (Rifadin, Rifamate, Rifater, Rimactane)
• sildenafil (Revatio), when used for treating the lung problem, pulmonary arterial hypertension (PAH)
  simvastatin (Simcor, Vytorin, Zocor)
• triazolam (Halcion)
• St. John's wort (Hypericum perforatum) or a product that contains St. John's wort
• ergot-containing medicines, including:
  • ​dihydroergotamine mesylate (DHE 45, MIgranal)
  • ergotamine tartrate (Cafergot, Migergot, Ergostat, Medihaler Ergotamine, Wigraine, Wigrettes)
  • methylergonovine maleate (Ergotrate, Methergine)

Do not take this medication if you are allergic to it or to any of the inactive ingredients.

Tell your healthcare provder if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Stribild falls into category B. There are no well-done studies that have been done in humans with but in animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

There is a pregnancy registry for women who take antiviral medicines during pregnancy. The purpose of this registry is to collect information about the health of you and your baby. Talk with your healthcare provider about how you can take part in this registry.

Many drugs can interact with this medicine and some should not be used at the same time. Tell your doctor about all the medicines you use.

This medicine may cause a serious condition called lactic acidosis. Get emergency medical help if you have even mild symptoms such as: muscle pain or weakness, numb or cold feeling in your arms and legs, trouble breathing, stomach pain, nausea with vomiting, fast or uneven heart rate, dizziness, or feeling very weak or tired.

This medicine can harm your liver. Call your doctor at once if you have: nausea, upper stomach pain, loss of appetite, dark urine, clay-colored stools, or yellowing of your skin or eyes.

If you have hepatitis B you may develop liver symptoms after you stop taking this medicine. Your doctor may want to check your liver function for several months.

Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Early symptoms of lactic acidosis may get worse over time and this condition can be fatal. Get emergency medical help if you have even mild symptoms: muscle pain or weakness, numb or cold feeling in your arms and legs, trouble breathing, stomach pain, nausea with vomiting, fast or uneven heart rate, dizziness, or feeling very weak or tired.

Call your doctor at once if you have:

• kidney problems--little or no urination; painful or difficult urination; swelling in your feet or ankles; feeling tired or short of breath; or

• liver problems--nausea, swelling around your midsection, upper stomach pain, unusual tiredness, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

This medicine may increase your risk of certain infections or autoimmune disorders by changing the way your immune system works. Symptoms may occur weeks or months after you start treatment. Tell your doctor if you have:

• signs of a new infection--fever, night sweats, swollen glands, mouth sores, diarrhea, stomach pain, weight loss;

• chest pain (especially when you breathe), dry cough, wheezing, feeling short of breath;

• cold sores, sores on your genital or anal area;

• rapid heart rate, feeling anxious or irritable, weakness or prickly feeling, problems with balance or eye movement;

• trouble speaking or swallowing, severe lower back pain, loss of bladder or bowel control; or

• swelling in your neck or throat (enlarged thyroid), menstrual changes, impotence, loss of interest in sex.

Common side effects may include:

• diarrhea;

• nausea; or

• changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

• Tell all of your health care providers that you take Stribild. This includes your doctors, nurses, pharmacists, and dentists.
• This medicine interacts with many other drugs. The chance of this medicine's side effects may be raised or how well Stribild works may be lowered. The chance of the other drugs' side effects may also be raised. This may include very bad, life-threatening, or deadly side effects. Check with your doctor and pharmacist to make sure that it is safe for you to take this medicine with all of your other drugs (prescription or OTC, natural products, vitamins).
• Bone problems like bone pain, soft bones, and thin bones have happened with Stribild (elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate). This may lead to broken bones. You may need to have a test to check your bones. Talk with your doctor.
• Take calcium and vitamin D as you were told by your doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• Have your urine checked as you have been told by your doctor.
• This medicine is not a cure for HIV. Stay under the care of your doctor.
• This medicine does not stop the spread of diseases like HIV or hepatitis that are passed through blood or having sex. Do not have any kind of sex without using a latex or polyurethane condom. Do not share needles or other things like toothbrushes or razors. Talk with your doctor.
• This medicine may rarely cause swollen liver and an acid health problem in the blood. This may be deadly in some cases. The chance may be higher in women, in overweight people, and in people who have taken drugs like this one for a long time. Talk with your doctor.
• Birth control pills and other hormone-based birth control may not work as well to prevent pregnancy. Use some other kind of birth control also like a condom when taking this medicine.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using Stribild while you are pregnant.

Stribild tablets are green, capsule shaped, film coated, and debossed with "GSI" on one side and the number "1" surrounded by a square box ( ) on the other side. Each bottle contains 30 tablets (NDC 61958-1201-1) and a silica gel desiccant, and is closed with a child-resistant closure.

Store at 25 °C (77 °F), excursions permitted to 15–30 °C (59–86 °F) (See USP Controlled Room Temperature).

• Keep container tightly closed.
• Dispense only in original container.

You should not take Stribild if you are allergic to cobicistat, elvitegravir, emtricitabine, or tenofovir.

Some medicines can interact with Stribild and should not be used at the same time. Your doctor may need to change your treatment plan if you use any of the following drugs:

• alfuzosin;

• lovastatin, simvastatin;

• oral midazolam, triazolam;

• rifampin;

• sildenafil (Revatio, for treating pulmonary arterial hypertension);

• St. John's wort;

• antipsychotic medicine - lurasidone, pimozide;

• ergot medicine - dihydroergotamine, ergotamine, ergonovine, methylergonovine; or

• seizure medicine - carbamazepine, phenobarbital, phenytoin.

Stribild is a complete combination treatment and should not be used with other antiviral medications, especially those that contain adefovir, cobicistat, elvitegravir, emtricitabine, lamivudine, ritonavir, or tenofovir: Atripla, Combivir, Complera, Emtriva, Epivir, Epzicom, Hepsera, Kaletra, Norvir, Triumeq, Trizivir, Truvada, Tybost, Viread, or Viekira.

To make sure Stribild is safe for you, tell your doctor if you have:

• liver or kidney disease;

• osteopenia (low bone mineral density); or

• a history of hepatitis B or C infection.

Some people taking Stribild develop a serious condition called lactic acidosis. This may be more likely in women, in people who are overweight or have liver disease, and in people who have taken HIV/AIDS medication for a long time. Talk with your doctor about your risk.

Stribild is not expected to be harmful to an unborn baby. However, HIV can be passed to your baby if you are not properly treated during pregnancy. Take all of your HIV medicines as directed to control your infection.

If you are pregnant, your name may be listed on a pregnancy registry. This is to track the outcome of the pregnancy and to evaluate any effects of Stribild on the baby.

Women with HIV or AIDS should not breast feed a baby. Even if your baby is born without HIV, the virus may be passed to the baby in your breast milk.

Stribild not approved for use by a child younger than 12 years old or weighing less than 77 pounds.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Absorption

Bioavailability

Pharmacokinetics in healthy individuals similar to those in individuals with HIV-1 infection.1

Tenofovir DF is a diester prodrug of tenofovir.1

Oral bioavailability of tenofovir from tenofovir DF is approximately 25%; peak plasma concentrations attained in about 1 hour in fasting HIV-infected patients.1

Peak plasma concentrations and AUC in pediatric patients 2 to <12 years of age receiving 8 mg/kg (up to 300 mg) once daily as an oral powder or in pediatric patients 12 to <18 years of age receiving 300 mg once daily as tablets were similar to peak plasma concentrations and AUC reported in adults receiving 300 mg once daily.1 Exposures in HBV-infected pediatric patients 12 to <18 years of age receiving 300 mg once daily as tablets were similar to those in HIV-1-infected adults and adolescents receiving 300 mg once daily.1

In nonfasting individuals, mean peak plasma concentrations were 26% lower when administered as an oral powder compared with administration as tablets; mean AUC was similar with both preparations.1

Fixed-combination tablet containing efavirenz 600 mg, emtricitabine 200 mg, and tenofovir DF 300 mg (efavirenz/emtricitabine/tenofovir DF; Atripla) is bioequivalent to a 600-mg efavirenz tablet, 300-mg tenofovir DF tablet, and 200-mg emtricitabine capsule given simultaneously.232

Fixed-combination tablet containing emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir DF 300 mg (emtricitabine/rilpivirine/tenofovir DF; Complera) taken with a meal is bioequivalent to a 200-mg emtricitabine capsule, 25-mg rilpivirine tablet, and 300-mg tenofovir DF tablet taken simultaneously with a meal.233

Fixed-combination tablet containing emtricitabine 200 mg and tenofovir DF 300 mg (emtricitabine/tenofovir DF; Truvada) is bioequivalent to a 200-mg emtricitabine capsule and 300-mg tenofovir DF tablet given simultaneously.230

Food

Food delays time to peak plasma tenofovir concentrations by approximately 1 hour.1 Administration with a high-fat meal increases oral bioavailability of tenofovir (14% increase in peak plasma concentrations; 40% increase in AUC);1 pharmacokinetics not appreciably affected by administration with a light meal.1

Distribution

Extent

Tenofovir distributed into semen35 and vaginal tissue and cervicovaginal fluid in low concentrations following oral administration.30 31 32 36 Very low concentrations may be distributed into saliva.33

Tenofovir crosses human placenta.32 202

Tenofovir distributed into human milk in low concentrations.1 34 202

Plasma Protein Binding

In vitro binding to plasma or serum proteins is <0.7 or 7.2%, respectively, over tenofovir concentrations of 0.01–25 mcg/mL.1

Elimination

Metabolism

Tenofovir DF requires initial diester hydrolysis for conversion to tenofovir and subsequent phosphorylation by cellular enzymes to form the active tenofovir diphosphate.1

Tenofovir and its prodrug are not substrates of CYP enzymes.1

Elimination Route

Tenofovir eliminated principally by kidneys using glomerular filtration and active tubular secretion; approximately 32% of an oral dose eliminated in urine within 24 hours.1

Tenofovir removed by hemodialysis.1

Half-life

Approximately 17 hours.1

Special Populations

No substantial changes in tenofovir pharmacokinetics in individuals with moderate to severe hepatic impairment compared with those with normal hepatic function.1

Moderate to severe renal impairment results in increased tenofovir plasma concentrations and AUC.1 (See Renal Impairment under Dosage and Administration.)

• Tenofovir DF is an HIV NRTI.1 2 3 Prodrug that is inactive until hydrolyzed in vivo to tenofovir which is then phosphorylated to the active metabolite (tenofovir diphosphate).1 2 3

• Active in vitro and in vivo against HIV-11 and HBV;1 26 200 some activity against HIV-2.1

• Inhibits replication of retroviruses, including HIV-1, by interfering with viral RNA-directed DNA polymerase (reverse transcriptase).1 2 3

• Inhibits HBV replication through competitive inhibition of viral reverse transcriptase.1

• Weak inhibitor of mammalian DNA α- and β-polymerases and mitochondrial DNA γ-polymerase.1 4 Low potential to induce mitochondrial toxicity.4

• HIV-1 resistant to tenofovir can be selected in vitro and have been reported in clinical isolates.1 HIV-1 strains with reduced susceptibility to tenofovir have K65R and K70E substitutions in reverse transcriptase.1

• HIV resistant to tenofovir may be cross-resistant to some NRTIs.1 Cross-resistance with HIV PIs or NNRTIs unlikely.7

• May be active against HBV resistant to adefovir and/or lamivudine.1 26 29 Some adefovir-, entecavir-, lamivudine-, or telbivudine-resistant HBV may have reduced susceptibility to tenofovir.1