HIV medications: Difference between revisions
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− | == |
+ | ==Classes== |
{| class="wikitable" |
{| class="wikitable" |
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− | ! |
+ | !Class |
− | ! |
+ | !Examples |
+ | !Mechanism of Action |
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− | ! Description |
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+ | !Adverse Effects |
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|- |
|- |
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− | | |
+ | |Nucleoside reverse-transcriptase inhibitor (NRTI) |
− | | |
+ | |[[tenofovir]], [[emtricitabine]], [[abacavir]] |
− | | |
+ | |Nucleoside/nucleotide analogues that get incorporated into viral DNA by reverse transcriptase, causing missense or non-sense mutations. The backbone of HIV treatments, with a high barrier to resistance. |
+ | | |
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|- |
|- |
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+ | |Non-nucleoside reverse-transcriptase inhibitor (NNRTI) |
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− | | Non-NRTI |
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− | | |
+ | |[[efavirenz]] |
− | | |
+ | |Actively inhibit reverse transcriptase at its active site. Resistance develops with a single point mutation. |
+ | | |
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|- |
|- |
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− | | |
+ | |Protease inhibitor (PI) |
− | | |
+ | |[[dirunavir]] |
− | | |
+ | |Inhibits protease, which is required for processing proteins in the creation of the virion. |
+ | |Metabolic syndrome |
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|- |
|- |
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− | | |
+ | |Integrase strand transfer inhibitor (INSTI) |
− | | |
+ | |[[raltegravir]], [[dolutegravir]], [[bictegravir]] |
+ | | |
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− | | Extremely potent with few side effects. Take separate from PPIs etc. |
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+ | |Generally very well-tolerated; may cause weight gain and diabetes |
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|- |
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− | | |
+ | |Fusion inhibitor |
+ | | |
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| |
| |
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| |
| |
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|- |
|- |
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− | | |
+ | |CCR5 entry inhibitor |
+ | |[[maraviroc]] |
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− | | |
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+ | |Blocks entry of HIV into CD4 cells. |
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| |
| |
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|- |
|- |
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− | | |
+ | |CD4-mAb |
− | | |
+ | |[[ibalizumab]] |
+ | | |
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− | | Blocks entry of HIV into CD4 cells. |
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+ | | |
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|} |
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− | == |
+ | ==Specific Medications== |
− | {| class="wikitable" |
+ | {| class="wikitable sortable" |
+ | !Class |
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− | ! Medication |
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+ | !Medication!!Abbr |
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− | ! AKA |
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+ | !Notes |
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− | ! Class |
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− | ! Notes |
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|- |
|- |
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+ | | rowspan="6" |NRTI |
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− | | [[lamivudine]] |
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+ | |[[lamivudine]]||3TC |
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− | | 3TC |
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− | | NRTI |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[emtricitabine]]||FTC |
− | | FTC |
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− | | NRTI |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[tenofovir disoproxol fumarate]]||TDF |
− | | TDF |
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− | | NRTI |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[tenofovir alafenamide]]||TAF |
+ | |Fewer renal and bone effects. |
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− | | TAF |
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− | | NRTI |
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− | | Fewer renal and bone effects. |
||
|- |
|- |
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− | | |
+ | |[[zidovudine]]||AZT |
− | | AZT |
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− | | NRTI |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[abacavir]]||ABC |
+ | |Need to check HLA-B*5701 before starting therapy. |
||
− | | ABC |
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− | | NRTI |
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− | | Need to check HLA-B*5701 before starting therapy. |
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|- |
|- |
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+ | | rowspan="4" |NNRTI |
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− | | [[efavirenz]] |
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− | | |
+ | |[[efavirenz]]||EFZ |
− | | NNRTI |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[nevirapine]]||NVP |
+ | | |
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− | | RPV |
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− | | NNRTI |
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− | | Take with meal, not with PPI. |
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|- |
|- |
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− | | |
+ | |[[rilpivirine]]||RPV |
+ | |Take with meal, not with PPI. |
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− | | DOR |
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+ | |- |
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− | | NNRTI |
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+ | |[[doravirine]]||DOR |
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| |
| |
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|- |
|- |
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+ | | rowspan="3" |PI |
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− | | [[lopinavir/ritonavir]] |
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+ | |[[lopinavir/ritonavir]]||LPV/r |
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− | | LPV/r |
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+ | |GI side effects. |
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− | | PI |
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− | | GI side effects. |
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|- |
|- |
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− | | |
+ | |[[darunivir]]||DRV |
− | | DRV |
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− | | PI |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[ritonavir]]||RTV |
+ | | |
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− | | DTG |
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− | | INSTI |
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− | | Increases metformin levels. Avoid in pregnancy. |
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|- |
|- |
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+ | | rowspan="5" |INSTI |
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− | | [[elvitegravir/cobicistat]] |
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+ | |[[dolutegravir]]||DTG |
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− | | EVG/c |
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+ | |Increases metformin levels. Avoid in pregnancy. |
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− | | INSTI |
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− | | Requires booster that has drug interaction. |
||
|- |
|- |
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+ | |[[elvitegravir/cobicistat]]||EVG/c |
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− | | [[raltegravir]] |
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+ | |Requires booster that has drug interaction. |
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− | | RAL |
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− | | INSTI |
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− | | First INSTI. BID dosing. Only INSTI that can be used in pregnancy. |
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|- |
|- |
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− | | |
+ | |[[raltegravir]]||RAL |
+ | |First INSTI. BID dosing. Only INSTI that can be used in pregnancy. |
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− | | BIC |
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+ | |- |
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− | | INSTI |
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+ | |[[bictegravir]]||BIC |
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| |
| |
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|- |
|- |
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− | | |
+ | |[[cabotegravir]]||CAB |
+ | |Long-acting injectable available. |
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− | | CAB |
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− | | INSTI |
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− | | Long-acting injectable available. |
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|- |
|- |
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− | | [[ibalizumab]] |
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| |
| |
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+ | |[[ibalizumab]]|| |
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− | | |
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− | | |
+ | |CD4-receptor antibody. |
|} |
|} |
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− | == |
+ | ==Single-Tablet Regimens== |
− | {| class="wikitable" |
+ | {| class="wikitable sortable" |
− | ! |
+ | !Brand name |
− | ! |
+ | !NRTIs |
− | ! |
+ | !Non-NRTI |
+ | !First-line? |
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− | ! Notes |
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+ | !Notes |
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|- |
|- |
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+ | |Atripla |
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− | | Triumeq |
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+ | |[[tenofovir disoproxil fumarate]] / [[emtricitabine]] |
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− | | ABC/3TC |
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+ | |[[efavirenz]] (NNRTI) |
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− | | DTG (INI) |
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+ | |No |
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− | | Highest barrier to resistance. Need to test for HLA-B5701 allele before starting. Avoid in hepatitis B coinfection. |
||
+ | |Older regimen. Neuropsychiatric symptoms, possibly including suicide. No dose adjustment with [[rifampin]]. |
||
|- |
|- |
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+ | |Biktarvy |
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− | | Atripla |
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+ | |[[tenofovir alafenamide]] / [[emtricitabine]] |
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− | | TDF/FTC |
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+ | |[[bictegravir]] (INI) |
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− | | EFZ |
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+ | |Yes |
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− | | Older regimen. Neuropsychiatric symptoms, possibly including suicide. |
||
+ | | |
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|- |
|- |
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− | | |
+ | |Complera |
+ | |[[tenofovir disoproxil fumarate]] / [[emtricitabine]] |
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− | | TDF/FTC |
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+ | |[[rilpivirine]] (NNRTI) |
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− | | RPV |
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+ | |No |
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− | | Avoid with viral loads (>100,000) or low CD4 (<200). Pill must be taken with food (>400kcal) and without PPIs. |
||
+ | |Avoid with viral loads (>100,000) or low CD4 (<200). Pill must be taken with food (>400kcal) and without PPIs. |
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|- |
|- |
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+ | |Delstrigo |
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− | | Stribild |
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+ | |[[tenofovir disoproxil fumarate]] / [[lamivudine]] |
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− | | TDF/FTC |
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+ | |[[doravirine]] (NNRTI) |
||
− | | EVG/c (INI) |
||
+ | |No |
||
− | | Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70. |
||
+ | | |
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|- |
|- |
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+ | |Dovato |
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− | | Genvoya |
||
+ | |[[emtricitabine]] |
||
− | | TAF/FTC |
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− | | |
+ | |[[dolutegravir]] (INI) |
+ | |Yes |
||
+ | |Two-medication regimen |
||
+ | |- |
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+ | |Genvoya |
||
+ | |[[tenofovir alafenamide]] / [[emtricitabine]] |
||
+ | |[[elvitegravir]]/[[cobicistat]] (INI) |
||
+ | |No |
||
+ | |See Stribild, above. |
||
+ | |- |
||
+ | |Odefsey |
||
+ | |[[tenofovir alafenamide]] / [[emtricitabine]] |
||
+ | |[[rilpivirine]] (NNRTI) |
||
+ | |No |
||
| |
| |
||
|- |
|- |
||
+ | |Stribild |
||
− | | Biktarvy |
||
+ | |[[tenofovir disoproxil fumarate]] / [[emtricitabine]] |
||
− | | TAF/FTC |
||
+ | |[[elvitegravir]]/[[cobicistat]] (INI) |
||
− | | BIC (INI) |
||
+ | |No |
||
+ | |Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70. |
||
+ | |- |
||
+ | |Symfi |
||
+ | |[[tenofovir disoproxil fumarate]] / [[emtricitabine]] |
||
+ | |[[efavirenz]] (NNRTI) |
||
+ | |No |
||
| |
| |
||
+ | |- |
||
+ | |Symtuza |
||
+ | |[[tenofovir alafenamide]] / [[emtricitabine]] |
||
+ | |[[darunavir]]/[[cobicistat]] (PI) |
||
+ | |No |
||
+ | | |
||
+ | |- |
||
+ | |Triumeq |
||
+ | |[[abacavir]] / [[lamivudine]] |
||
+ | |[[dolutegravir]] (INI) |
||
+ | |Yes |
||
+ | |Highest barrier to resistance. Need to test for HLA-B5701 allele before starting. Avoid in hepatitis B coinfection. |
||
|} |
|} |
||
− | == |
+ | == Crushing Medications == |
+ | * See https://www.hivclinic.ca/main/drugs_extra_files/Crushing%20and%20Liquid%20ARV%20Formulations.pdf |
||
− | * Hepatitis B: Avoid Triumeq; use TDF/FTC-based regimen instead |
||
− | * CKD: Avoid Stribild in CrCl <70 |
||
− | == |
+ | ==Further Reading== |
− | * |
+ | *Andany N and Gold WL. [https://doi.org/10.1503/cmaj.151412 Five things to know about single-tablet antiretroviral treatment (once daily)]. ''CMAJ''. 2016;188(13)971. |
− | * |
+ | *Gandhi M and Gandhi RT. [https://doi.org/10.1056/NEJMct1215532 Single-Pill Combination Regimens for Treatment of HIV-1 Infection]. ''N Engl J Med''. 2014;371:248-259. |
[[Category:HIV]] |
[[Category:HIV]] |
Latest revision as of 08:32, 25 January 2024
Classes
Class | Examples | Mechanism of Action | Adverse Effects |
---|---|---|---|
Nucleoside reverse-transcriptase inhibitor (NRTI) | tenofovir, emtricitabine, abacavir | Nucleoside/nucleotide analogues that get incorporated into viral DNA by reverse transcriptase, causing missense or non-sense mutations. The backbone of HIV treatments, with a high barrier to resistance. | |
Non-nucleoside reverse-transcriptase inhibitor (NNRTI) | efavirenz | Actively inhibit reverse transcriptase at its active site. Resistance develops with a single point mutation. | |
Protease inhibitor (PI) | dirunavir | Inhibits protease, which is required for processing proteins in the creation of the virion. | Metabolic syndrome |
Integrase strand transfer inhibitor (INSTI) | raltegravir, dolutegravir, bictegravir | Generally very well-tolerated; may cause weight gain and diabetes | |
Fusion inhibitor | |||
CCR5 entry inhibitor | maraviroc | Blocks entry of HIV into CD4 cells. | |
CD4-mAb | ibalizumab |
Specific Medications
Class | Medication | Abbr | Notes |
---|---|---|---|
NRTI | lamivudine | 3TC | |
emtricitabine | FTC | ||
tenofovir disoproxol fumarate | TDF | ||
tenofovir alafenamide | TAF | Fewer renal and bone effects. | |
zidovudine | AZT | ||
abacavir | ABC | Need to check HLA-B*5701 before starting therapy. | |
NNRTI | efavirenz | EFZ | |
nevirapine | NVP | ||
rilpivirine | RPV | Take with meal, not with PPI. | |
doravirine | DOR | ||
PI | lopinavir/ritonavir | LPV/r | GI side effects. |
darunivir | DRV | ||
ritonavir | RTV | ||
INSTI | dolutegravir | DTG | Increases metformin levels. Avoid in pregnancy. |
elvitegravir/cobicistat | EVG/c | Requires booster that has drug interaction. | |
raltegravir | RAL | First INSTI. BID dosing. Only INSTI that can be used in pregnancy. | |
bictegravir | BIC | ||
cabotegravir | CAB | Long-acting injectable available. | |
ibalizumab | CD4-receptor antibody. |
Single-Tablet Regimens
Brand name | NRTIs | Non-NRTI | First-line? | Notes |
---|---|---|---|---|
Atripla | tenofovir disoproxil fumarate / emtricitabine | efavirenz (NNRTI) | No | Older regimen. Neuropsychiatric symptoms, possibly including suicide. No dose adjustment with rifampin. |
Biktarvy | tenofovir alafenamide / emtricitabine | bictegravir (INI) | Yes | |
Complera | tenofovir disoproxil fumarate / emtricitabine | rilpivirine (NNRTI) | No | Avoid with viral loads (>100,000) or low CD4 (<200). Pill must be taken with food (>400kcal) and without PPIs. |
Delstrigo | tenofovir disoproxil fumarate / lamivudine | doravirine (NNRTI) | No | |
Dovato | emtricitabine | dolutegravir (INI) | Yes | Two-medication regimen |
Genvoya | tenofovir alafenamide / emtricitabine | elvitegravir/cobicistat (INI) | No | See Stribild, above. |
Odefsey | tenofovir alafenamide / emtricitabine | rilpivirine (NNRTI) | No | |
Stribild | tenofovir disoproxil fumarate / emtricitabine | elvitegravir/cobicistat (INI) | No | Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70. |
Symfi | tenofovir disoproxil fumarate / emtricitabine | efavirenz (NNRTI) | No | |
Symtuza | tenofovir alafenamide / emtricitabine | darunavir/cobicistat (PI) | No | |
Triumeq | abacavir / lamivudine | dolutegravir (INI) | Yes | Highest barrier to resistance. Need to test for HLA-B5701 allele before starting. Avoid in hepatitis B coinfection. |
Crushing Medications
- See https://www.hivclinic.ca/main/drugs_extra_files/Crushing%20and%20Liquid%20ARV%20Formulations.pdf
Further Reading
- Andany N and Gold WL. Five things to know about single-tablet antiretroviral treatment (once daily). CMAJ. 2016;188(13)971.
- Gandhi M and Gandhi RT. Single-Pill Combination Regimens for Treatment of HIV-1 Infection. N Engl J Med. 2014;371:248-259.