Drugs Five Last Time Flashcards
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5 drug classes to act on HIV
1) Reverse transcriptase inhibitors (NRTIs and NNRTIs)
2) protease inhibitors
3) HIV fusion inhibitors
4) Integrase strand transfer inhibitors
5) CCR5 antagonists
Drug interactions with anti HIV drugs
Many are inducors or inhibitors for one or more CYP450 enzymes and might intensify effects to harmful degree
Nucleoside/nucleotide reverse transcriptase inhibitors mech of action
Inhibit ability of virus to use reverse transcriptase to incorportae RNA into host cell’s DNA, preventing replication
Nucleoside/nucleotide reverse transcriptase inhibitors ADRS
- Lactic acidosis (rare accumulation)
- hepatic steatosis (fatty degeneration of liver)
Abacavir
Analog of guanine commonly used in antiretrovirals
Abacavir mech of action
Taken up by host cells and converted to active form, compees for binding reverse transcriptase
HLA-B 5701
Specific genetic variation that makes patients susceptibe to abacavir hypersensitivity
Zidovudine (ZDV or AZT)
First antiretroviral drug for HIV, not recommended because of adverse effects
Zidovudine mech of action
Converted to active form in cell and acts as substrate for reverse transcriptase blocking and terminating further growth
Zidovudine ADRs
Anemia and neutropenia
Non nucleoside reverse transcriptase inhibitors
Differ from NRTI’s in struture and mech of action,
Non nucleoside reverse transcriptase inhibitors mech of action
Active as administered bind directly to reverse transcriptase and cause active inhibition
Efavirenz
NNRTI for treating HIV
Efavirenz ADRs
CNS compications
Rash, steven johnson
Teratogenicity
Protease inhibitors
Active against HIV 1 and 2 most effective especially when used in combo with others
Protease inhibtors mech of action
Prevention of HIv maturation by blocking HIV enzyme protease, preventing cleaving of HIV polyproteins
Protease inhibitors ADRs
- Hyperglycemia
- Diabetes
- hyperlipidemia
- decreased cardiac conductio velocity
Ritanovir boosting
Ritanovir is a Protesase inhibitor routinely combined with other PIs specifically to increase plasma level (one protease inhiibotr can metabolism of the other) to increase therapuetic use
Fusion inhibitors
Prevent entracnce of HIV into CD4T cells
Enfuviritide aka T-20
First fusion inhibitor, reserved for treatment experienced patients who have evidence of HIV replication despite ongoing ART
Enfuviritide aka T-20 resistance
-Structural changes to gp41 (subunit embedded in HIV envelope)
HIV-1 Integrase strand transfer inhibitors
PO HIV drugs received accelerated approval for combo therapy for treatment expereinced adults infected wth HIV 1 strains resistant to antiretroviral drugs
Example of HIV-1 Integrase strand transfer inhibitor
Raltegravir
Raltegravir mech of action
Inhibits enzyme that catylzes the process that results in viral DNA insertion into host genome
Other examples of HIV-1 Integrase strand transfer inhibitors
- Elvitegravir
- Dolutegravir
CCR5 antagonists
Restricted to use in adults with CCR5 tropic HIV 1 (found in some individuals not others)
CCR5 antagonist mech of action
CCR5 tropic HIV-1 strains predominate during early stages of infection, drugs bind CCR5 cco receptor preventing from virus entering host cell
Zidovudine/iamivudine
2 nucleoside reverse transcriptase inhibitors administered togethers
Juluca (dolutgravir and rilpivirone)
first 2 regimen drug complete regiment approved for treatment of HIV-1 infection
Ilbazumab-uiyk
IV treatment for multi drug resistant HIV 1, blocks entry of HIv into CD4 cell
ART therapy
Usually contains 3 drugs, attack HIV via 2 different mechanisms, the other 4 are class sparing so if resistance is developed can switch class
