Drug information of Elvitegravir

Elvitegravir

Drug group:

Mechanism of effect

Integrase is an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II.

Pharmacokinetics

Absorption

AUC increases with food

Metabolism

Hepatic via CYP3A enzymes and also hepatic glucuronidation mediated by UGT1A1/3

Excretion

Feces (~95%); urine (~7%)

Time to Peak

Plasma: ~4 hours

Half-Life Elimination

Terminal: ~9 hours

Protein Binding

99%

Drug indications

HIV-1 infection: In combination with an HIV protease inhibitor coadministered with ritonavir and with other antiretroviral drug(s) for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults

Dosage

Usual Adult Dose for HIV Infection

With once-daily atazanavir/ritonavir or twice-daily lopinavir-ritonavir: 85 mg orally once a day with food
With twice-daily darunavir/ritonavir, fosamprenavir/ritonavir, or tipranavir/ritonavir: 150 mg orally once a day with food

Comments:
-The manufacturer product information should be consulted for the recommended dosing regimen for atazanavir/ritonavir, lopinavir-ritonavir, darunavir/ritonavir, fosamprenavir/ritonavir, or tipranavir/ritonavir; this drug should not be used with other dose regimens or HIV-1 protease inhibitors.
-This drug should not be used with cobicistat and protease inhibitors.

Use: In combination with a ritonavir-boosted HIV protease inhibitor and at least 1 other antiretroviral drug, for the treatment of HIV-1 infection in antiretroviral therapy-experienced patients.

Side effects

Gastrointestinal

Very common (10% or more): Increased lipase (14%), diarrhea (up to 13%)

Common (1% to 10%): Abdominal pain, vomiting, nausea, increased serum amylase

Uncommon (0.1% to 1%): Dyspepsia, abdominal distension, flatulence[Ref]

Increased serum amylase (greater than 2 times the upper limit of normal [2 x ULN]) has been reported in 6% of patients.

If serum amylase was greater than 1.5 x ULN, lipase was also measured. Increased lipase (grades 3 to 4) has been reported in 14% of patients.[Ref]

Hepatic

Increased total bilirubin (greater than 2.5 x ULN), GGT (greater than 5 x ULN), ALT (greater than 5 x ULN), and AST (greater than 5 x ULN) have been reported in 6%, 3%, 2%, and 2% of patients, respectively.[Ref]

Common (1% to 10%): Increased total bilirubin, increased ALT, increased AST[Ref]

Musculoskeletal

Common (1% to 10%): Increased creatine kinase, back pain, arthralgia, pain in extremity

Frequency not reported: Osteonecrosis[Ref]

Increased creatine kinase (at least 10 x ULN) has been reported in 6% of patients.[Ref]

Genitourinary

Hematuria (greater than 75 RBC/high power field) and urine glucose (4+) have been reported in 6% and 4% of patients, respectively.

Common (1% to 10%): Hematuria, urine glucose

Metabolic

Increased total cholesterol (greater than 300 mg/dL), increased total triglycerides (greater than 750 mg/dL), and hyperglycemia (greater than 250 mg/dL) have each been reported in 5% of patients.

Common (1% to 10%): Increased total cholesterol, increased total triglycerides, hyperglycemia

Nervous system

Common (1% to 10%): Headache

Uncommon (0.1% to 1%): Dizziness, paresthesia, somnolence, dysgeusia

Hematologic

Decreased neutrophils (less than 750/mm3) has been reported in 3% of patients.

Common (1% to 10%): Decreased neutrophils[

Psychiatric

Common (1% to 10%): Depression

Uncommon (0.1% to 1%): Suicidal ideation, suicide attempt, insomnia

Suicidal ideation and suicide attempt were reported in patients with history of depression or psychiatric illness.[Ref]

Dermatologic

Common (1% to 10%): Rash[Ref]

Other

Common (1% to 10%): Fatigue[Ref]

Immunologic

Frequency not reported: Autoimmune disorders (e.g., Graves' disease)

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like 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; or swelling of the mouth, face, lips, tongue, or throat.
  • Changes in your immune system can happen when you start taking drugs to treat HIV. If you have an infection that you did not know you had, it may show up when you take this drug. Tell your doctor right away if you have any new signs after you start this drug, even after taking it for several months. This includes signs of infection like fever, sore throat, weakness, cough, or shortness of breath.

    All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

    • Diarrhea.

    These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

rifapentinest. john's wort , zinc acetate  , zinc chloride , zinc gluconate ,

Alerts

Concerns related to adverse effects:

  • Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.

Disease-related concerns:

  • Hepatic impairment: No dosage adjustment is required in mild or moderate (Child-Pugh class A or B) hepatic impairment. Use is not recommended in severe hepatic impairment (Child-Pugh class C); has not been studied in this population.

Concurrent drug therapy issues:

  • Appropriate use: Not recommended in combination with a protease inhibitor and cobicistat due to lack of dosing recommendations, potential suboptimal plasma concentrations, loss of therapeutic effect, or development of resistance.
  • Concurrent therapy: Avoid concurrent use with other elvitegravir-containing products.
  • Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

 

Before taking this medicine

  • If you are allergic to elvitegravir; any part of elvitegravir; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
  • If you have liver disease.
  • If you are taking cobicistat and you are also taking certain other drugs to treat HIV. There are many drugs that are not to be taken if you are taking elvitegravir along with cobicistat. Ask your doctor or pharmacist if you are not sure.
  • If you are taking any of these drugs: Boceprevir, carbamazepineefavirenznevirapineoxcarbazepinephenobarbitalphenytoinrifampin, rifapentine, or St. John's wort.
  • If you are taking another drug that has the same drug in it.
  • If you are breast-feeding. Do not breast-feed while you take elvitegravir.

Points of recommendation

  • Tell all of your health care providers that you take elvitegravir. This includes your doctors, nurses, pharmacists, and dentists.
  • This medicine interacts with many other drugs. The chance of elvitegravir's side effects may be raised or how well elvitegravir 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 elvitegravir with all of your other drugs (prescription or OTC, natural products, vitamins).
  • 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.
  • 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 elvitegravir.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using elvitegravir while you are pregnant.
  • Take elvitegravir with food.
  • If you are also taking didanosine, take it at least 1 hour before or 2 hours after elvitegravir.
  • Do not take antacids within 2 hours before or 2 hours after taking elvitegravir.
  • Keep taking elvitegravir as you have been told by your doctor or other health care provider, even if you feel well.
  • It is important that you do not miss or skip a dose of elvitegravir during treatment.
  • Store in the original container at room temperature.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.
  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about elvitegravir, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Storage

Store below 30°C (86°F). Dispense only in original container.

 

Pregnancy level

B

Use is recommended only if clearly needed and the benefit outweighs the risk to the fetus.

AU TGA pregnancy category: B2
US FDA pregnancy category: B

Comments: Use of effective contraception during therapy has been recommended.

Breast feeding warning

Breastfeeding is not recommended during use of this drug.

Excreted into human milk: Unknown
Excreted into animal milk: Yes

Comments:
-The effects in the nursing infant are unknown.
-The US CDC, American Academy of Pediatrics, and manufacturer advise HIV-infected women not to breastfeed to avoid postnatal transmission of HIV to a child who may not yet be infected.

Related drugs

Dolutegravir

Drug forms

Vitekta

Ask a Pharmacist


User's questions
    No comments yet.