Table 2.
Approved STR | HIV viral load/CD4 restrictions | Testing requirements | CrCl restrictions | Drug–drug interactions | Genetic barrier to resistance and dosing considerations |
---|---|---|---|---|---|
Dolutegravir/abacavir/lamivudine | None | HLA-B*5701a | CrCl <50 ml/min: use is not recommended |
Carbamazepine, efavirenz, fosamprenavir/r, rifampin tipranavir/r: administer 50 mg PO BID Al, Ca, Fe, Mg containing products: administer DTG-containing product 2 h before or 6 h after. Alternatively, DTG and supplements with Ca or Fe can be taken together with food Metformin: limit daily dose of metformin to 1000 mg daily Etravirine: use not recommended unless administered with boosted-PI (atazanavir, darunavir, or lopinavir) Avoid use with nevirapine, oxcarbazepine, phenobarbital, phenytoin, St. John’s wort |
High barrier to resistance May be taken with or without food |
Darunavir/cobicistat/tenofovir alafenamide/emtricitabineb | None | None | CrCl <30 ml/min: use likely not recommended |
Numerous interactions exist since DRV and COBI are metabolized by CYP3A4 Avoid use with alfuzosin, amiodarone, apixaban, carbamazepine, cisapride, dronedarone, ergot derivatives, lurasidone, oral midazolam, lovastatin, phenobarbital, phenytoin, quinidine, pimozide, ranolazine, rifampin, rivaroxaban, salmeterol, sildenafild, simvastatin, St. John’s wort, ticagrelor, triazolam |
High barrier to resistance Recommended to take with food |
Elvitegravir/cobicistat/tenofovir disoproxil fumarate/emtricitabine | None | None |
CrCl <70 ml/min at initiation of therapy: Initial use is not recommended CrCl <50 ml/min during therapy: Continued use is not recommended |
Numerous interactions exist since EVG and COBI are metabolized by CYP3A4c Al, Ca, Mg-containing antacids: separate by 2 h from antacid administration Avoid use with alfuzosin, carbamazepine, ergot derivatives, oral midazolam, lovastatin, phenobarbital, phenytoin, pimozide, rifampin, sildenafild, simvastatin, St. John’s wort, triazolam |
Low-medium barrier to resistance Recommended to take with food |
Elvitegravir/cobicistat/tenofovir alafenamide/emtricitabine | None | None | CrCl <30 ml/min: use is not recommended | Refer to section above |
Low-medium barrier to resistance Recommended to take with food |
Rilpivirine/tenofovir disoproxil fumarate/emtricitabine |
Use is not recommended if: CD4 count <200 cells/mm3 OR HIV RNA >100,000 copies/ml |
None | CrCl <50 ml/min: use is not recommended |
Al, Ca, Mg-containing antacids: Administer antacids at least 2 h before or 4 h after RPV H2RA: Administer H2RA at least 12 h before RPV or at least 4 h after RPV Rifabutin: administer an additional 25 mg dose of RPV daily while on rifabutin Avoid use with carbamazepine, dexamethasone, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, St. John’s wort |
Low barrier to resistance Recommended to take with food (at least 400 kcal) |
Rilpivirine/tenofovir alafenamide/emtricitabine |
Use is not recommended if: CD4 count <200 cells/mm3 OR HIV RNA >100,000 copies/ml |
None | CrCl <30 ml/min: Use is not recommended | Refer to section above |
Low barrier to resistance Recommended to take with food (at least 400 kcal) |
Efavirenz/tenofovir disoproxil fumarate/emtricitabine | None | None | CrCl <50 ml/min: use is not recommended |
Numerous interactions exist since EFV induces CYP3A and CYP2B6c Once-daily fosamprenavir: add an additional 100 mg or RTV daily (for a total daily dose of 300 mg) Oral ethinyl estradiol/norgestimate or etonogestrel implant: a reliable method of barrier contraception must be used in addition to hormonal contraceptives. Methadone: monitor for signs of withdrawal Rifabutin: dose of rifabutin needs to be increased in the presence of EFV Rifampin: an additional dose of EFV 200 mg daily is needed Avoid use with atazanavir, lopinavir, and other NNRTIs Avoid use with voriconazole because the dose of EFV has to be reduced to 300 mg daily |
Low barrier to resistance Take at bedtime on an empty stomach |
Al aluminum, Ca Calcium, COBI cobicistat, CrCl creatinine clearance, DRV darunavir, DTG dolutegravir, EFV efavirenz, Fe iron, H 2 RA histamine2-receptor antagonist, Mg magnesium, NNRTI non-nucleoside reverse transcriptase inhibitor, PI protease inhibitor, RPV rilpivirine, r or RTV Ritonavir
aAll patients should receive allele testing (HLA-B*5701) prior to initiating therapy to minimize the likelihood of a hypersensitivity reaction characterized by rash, fever, shortness of breath, and generalized malaise. If the patient tests positive for HLA-B*5701, abacavir-containing regimens should be avoided
bCurrently an investigational drug
cRefer to package insert for a complete listing of drug-drug interactions
dWhen used for the treatment of pulmonary arterial hypertension