Metabolism and Excretion: Metabolized by CYP3A, 94.5% eliminated in feces, 6.7% in urine.
Half-life: Elvitegravir–12.9 hr, with ritonavir–8.7 hr.
TIME/ACTION PROFILE (blood levels)
Should not be used concurrently with cobicistat, efavirenz, nevirapine, rifampin, rifapentine, other elvitegravir-containing agents, norgestimate/ethinyl estradiol or St. John's wort;
Severe hepatic impairment;
Lactation: HIV-infected women should not breast feed due to risk of viral transmission.
Use Cautiously in:
Concurrent use of drugs that induce the CYP3A enzyme system;
Geri: May be more sensitive to drug effects (consider age-related ↓ in renal, hepatic and cardiac function, concurrent medications and medical conditions);
OB: Use only if potential benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
Misc: immune reconstitution syndrome
* CAPITALS indicate life-threatening. Underline indicate most frequent.
Strong CYP3A inducers including carbamazepine, oxcarbazepine, phenobarbital, and phenytoin can ↓ blood levels/effectiveness and ↑ risk of viral resistance (consider other anticonvulsants); similar effects may occur with rifampin and rifapentine (concurrent use not recommended)dexamethasone (consider alternative corticosteroid)cobicistat, efavirenz, and nevirapine(concurrent use should be avoided); and bosentan (discontinue bosentan at least 36 hr prior to starting elvitegravir, wait 10 days before restarting at ↓ dose of 62.5 mg once daily or ever other day with careful titration).
Antacids may ↓ blood levels/effectiveness and ↑ risk of viral resistance by forming complexes in the GI (separate doses by 2 hr).
Blood levels and the risk of toxicity are ↑ by atazanavir/ritonavir and lopinavir/ritonavir (↓ elvitegravir dose).
May ↑ blood levels and risk of toxicity from ketoconazole (daily ketoconazole dose should not exceed 200 mg), rifabutin (↓ rifabutin dose to 150 mg every other day or 3 times weekly), bosentan (initiate bosentan at 62.5 mg once daily or every other day and titrate carefully), and buprenorphine.
May ↓ levels of ethinyl estradiol in hormonal contraceptives leading to ↓ contraceptive efficacy (alternative non-hormonal contraceptive recommended).
St. John's wort can ↓ blood levels/effectiveness and ↑ risk of viral resistance (concurrent use should be avoided).
Didanosine(needs to be given on an empty stomach) should be given 1 hr before or 2 hr after elvitegravir (needs to be given with food).
An additional antiretroviral must be coadministered in addition to elvitegravir, a protease inhibitor, and ritonavir.
PO (Adults) If used with ataznavir 300 mg once daily with 100 mg ritonavir once daily or lopinavir 400 mg once daily with ritonavir 100 mg twice daily–85 mg once daily; If used with darunavir 600 mg once daily with 100 mg ritonavir twice daily or fosamprenavir 700 mg twice daily with ritonavir 100 mg twice daily or tipranavir 500 mg twice daily with ritonavir 200 mg twice daily–150 mg once daily.
Tablets: 85 mg, 150 mg
Assess patient for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
PO Administer once daily with food with a protease inhibitor and with ritonavir.
Administer antacids at least 2 hr before or after elvitegravir.
Explain purpose of elvitegravir to patient; elvitegravir does not treat HIV and must be taken with antiretroviral medications. Instruct patient to take elvitegravir as directed with food and with a protease inhibitor (atazanavir, darunavir, fosamprenavir, lopinavir/ritonavir, or tipranavir) and ritonavir on a regular dosing schedule. Do not stop taking elvitegravir without consulting health care professional. Advise patient to read Patient Information prior to starting therapy and with each Rx refill in case of change.
Inform patient that elvitegravir does not cure AIDS or prevent associated or opportunistic infections. Elvitegravir does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom during sexual contact and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's Wort. Elvitegravir interacts with many other drugs. Follow instructions for specific timing of or avoiding other medications.
Advise patient to notify health care professional if signs and symptoms of immune reconstitution syndrome (signs and symptoms of infection or inflammation) occur.
Rep: Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding. May decrease plasma concentrations of hormonal contraceptives. Use nonhormonal methods of contraception during therapy. Encourage pregnant patient to enroll in Antiretroviral Pregnancy Registry by calling 1-800-258-4263. Advise patient to avoid breast feeding.
Slowed progression of HIV infection and decreased occurrence of sequelae.
elvitegravir is a sample topic from the Davis's Drug Guide.
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