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. 2016 Aug 18;5(3):329–352. doi: 10.1007/s40121-016-0126-x

Table 2.

Approved and investigational single-tablet regimens (STR)

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