HIV medications: Difference between revisions

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== Classes ==
 +
==Classes==
   
 
{| class="wikitable"
  
{| class="wikitable"
−
! Class
 +
!Class
−
! Examples
 +
!Examples
  +
!Mechanism of Action
−
! Description
  
  +
!Adverse Effects
 
|-
  
|-
−
| Nucleoside reverse-transcriptase inhibitor (NRTI)
 +
|Nucleoside reverse-transcriptase inhibitor (NRTI)
−
| tenofovir, emtricitabine, abacavir
 +
|[[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.
 +
|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)
−
| Non-NRTI
  
−
| efavirenz
 +
|[[efavirenz]]
−
| Actively inhibit reverse transcriptase at its active site. Resistance develops with a single point mutation.
 +
|Actively inhibit reverse transcriptase at its active site. Resistance develops with a single point mutation.
  +
|
 
|-
  
|-
−
| Protease inhibitor (PI)
 +
|Protease inhibitor (PI)
−
| dirunavir
 +
|[[dirunavir]]
−
| Inhibits protease, which is required for processing proteins in the creation of the virion. Causes a metabolic syndrome.
 +
|Inhibits protease, which is required for processing proteins in the creation of the virion.
  +
|Metabolic syndrome
 
|-
  
|-
−
| Integrase inhibitor (INSTI)
 +
|Integrase strand transfer inhibitor (INSTI)
−
| raltegravir, dolutegravir, bictegravir
 +
|[[raltegravir]], [[dolutegravir]], [[bictegravir]]
  +
|
−
| Extremely potent with few side effects. Take separate from PPIs etc.
  
  +
|Generally very well-tolerated; may cause weight gain and diabetes
 
|-
  
|-
−
| Fusion inhibitor
 +
|Fusion inhibitor
  +
|
 
|
  
|
 
|
  
|
 
|-
  
|-
−
| CCR5 inhibitor
 +
|CCR5 entry inhibitor
  +
|[[maraviroc]]
−
|
  
  +
|Blocks entry of HIV into CD4 cells.
 
|
  
|
 
|-
  
|-
−
| CD4-mAb
 +
|CD4-mAb
−
| ibalizumab
 +
|[[ibalizumab]]
  +
|
−
| Blocks entry of HIV into CD4 cells.
  
  +
|
 
|}
  
|}
   
−
== Specific Medications ==
 +
==Specific Medications==
   
−
{| class="wikitable"
 +
{| class="wikitable sortable"
  +
!Class
−
! Medication
  
  +
!Medication!!Abbr
−
! AKA
  
  +
!Notes
−
! Class
  
−
! Notes
  
 
|-
  
|-
  +
| rowspan="6" |NRTI
−
| lamivudine
  
  +
|[[lamivudine]]||3TC
−
| 3TC
  
−
| NRTI
  
 
|
  
|
 
|-
  
|-
−
| emtricitabine
 +
|[[emtricitabine]]||FTC
−
| FTC
  
−
| NRTI
  
 
|
  
|
 
|-
  
|-
−
| tenofovir disoproxol
 +
|[[tenofovir disoproxol fumarate]]||TDF
−
| TDF
  
−
| NRTI
  
 
|
  
|
 
|-
  
|-
−
| tenofovir alafenamide
 +
|[[tenofovir alafenamide]]||TAF
  +
|Fewer renal and bone effects.
−
| TAF
  
−
| NRTI
  
−
| Fewer renal and bone effects.
  
 
|-
  
|-
−
| zidovudine
 +
|[[zidovudine]]||AZT
−
| AZT
  
−
| NRTI
  
 
|
  
|
 
|-
  
|-
−
| abacavir
 +
|[[abacavir]]||ABC
  +
|Need to check HLA-B*5701 before starting therapy.
−
| ABC
  
−
| NRTI
  
−
| Need to check HLA-B5701 before starting therapy.
  
 
|-
  
|-
  +
| rowspan="4" |NNRTI
−
| efavirenz
  
−
| EFZ
 +
|[[efavirenz]]||EFZ
−
| NNRTI
  
 
|
  
|
 
|-
  
|-
  +
|[[nevirapine]]||NVP
−
| rilpivirine
  
  +
|
−
| RPV
  
−
| NNRTI
  
−
| Take with meal, not with PPI.
  
 
|-
  
|-
  +
|[[rilpivirine]]||RPV
−
| doravirine
  
  +
|Take with meal, not with PPI.
−
| DOR
  
  +
|-
−
| NNRTI
  
  +
|[[doravirine]]||DOR
 
|
  
|
 
|-
  
|-
  +
| rowspan="3" |PI
−
| lopinavir/ritonavir
  
  +
|[[lopinavir/ritonavir]]||LPV/r
−
| LPV/r
  
  +
|GI side effects.
−
| PI
  
−
| GI side effects.
  
 
|-
  
|-
−
| darunivir
 +
|[[darunivir]]||DRV
−
| DRV
  
−
| PI
  
 
|
  
|
 
|-
  
|-
  +
|[[ritonavir]]||RTV
−
| dolutegravir
  
  +
|
−
| DTG
  
−
| INSTI
  
−
| Increases metformin levels. Avoid in pregnancy.
  
 
|-
  
|-
  +
| rowspan="5" |INSTI
−
| elvitegravir/cobicistat
  
  +
|[[dolutegravir]]||DTG
−
| EVG/c
  
  +
|Increases metformin levels. Avoid in pregnancy.
−
| INSTI
  
−
| Requires booster that has drug interaction.
  
 
|-
  
|-
  +
|[[elvitegravir/cobicistat]]||EVG/c
−
| raltegravir
  
  +
|Requires booster that has drug interaction.
−
| RAL
  
−
| INSTI
  
−
| First INSTI. BID dosing. Only INSTI that can be used in pregnancy.
  
 
|-
  
|-
  +
|[[raltegravir]]||RAL
−
| bictegravir
  
  +
|First INSTI. BID dosing. Only INSTI that can be used in pregnancy.
−
| BIC
  
  +
|-
−
| INSTI
  
  +
|[[bictegravir]]||BIC
 
|
  
|
 
|-
  
|-
−
| cabotegravir
 +
|[[cabotegravir]]||CAB
  +
|Long-acting injectable available.
−
| CAB
  
−
| INSTI
  
−
| Long-acting injectable available.
  
 
|-
  
|-
−
| ibalizumab
  
 
|
  
|
  +
|[[ibalizumab]]||
−
|
  
−
| CD4-receptor antibody.
 +
|CD4-receptor antibody.
 
|}
  
|}
   
−
== Single-Tablet Regimens ==
 +
==Single-Tablet Regimens==
   
−
{| class="wikitable"
 +
{| class="wikitable sortable"
−
! Brand name
 +
!Brand name
−
! NRTIs
 +
!NRTIs
−
! Non-NRTI
 +
!Non-NRTI
  +
!First-line?
−
! Notes
  
  +
!Notes
 
|-
  
|-
  +
|Atripla
−
| Triumeq
  
  +
|[[tenofovir disoproxil fumarate]] / [[emtricitabine]]
−
| ABC/3TC
  
  +
|[[efavirenz]] (NNRTI)
−
| DTG (INI)
  
  +
|No
−
| 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]].
 
|-
  
|-
  +
|Biktarvy
−
| Atripla
  
  +
|[[tenofovir alafenamide]] / [[emtricitabine]]
−
| TDF/FTC
  
  +
|[[bictegravir]] (INI)
−
| EFZ
  
  +
|Yes
−
| Older regimen. Neuropsychiatric symptoms, possibly including suicide.
  
  +
|
 
|-
  
|-
−
| Complera
 +
|Complera
  +
|[[tenofovir disoproxil fumarate]] / [[emtricitabine]]
−
| TDF/FTC
  
  +
|[[rilpivirine]] (NNRTI)
−
| RPV
  
  +
|No
−
| 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.
 
|-
  
|-
  +
|Delstrigo
−
| Stribild
  
  +
|[[tenofovir disoproxil fumarate]] / [[lamivudine]]
−
| TDF/FTC
  
  +
|[[doravirine]] (NNRTI)
−
| EVG/c (INI)
  
  +
|No
−
| Includes a P450 inhibitor to boost elvitegravir levels, with resultant drug-drug interactions. Avoid if CrCl <70.
  
  +
|
 
|-
  
|-
  +
|Dovato
−
| Genvoya
  
  +
|[[emtricitabine]]
−
| TAF/FTC
  
−
| ELV/c (INI)
 +
|[[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
−
| 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.
 
|}
  
|}
   
−
== Considerations ==
 +
== 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 ==
 +
==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.
 +
*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.
 +
*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

Further Reading

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