HIV drugs Flashcards
Fusion inhibitors - MoA, Eg
Bind HIV fusion protein gp41
Enfuvirtide
Attachment inhibitors
Inhibit HIV co-receptors that enable entry - CCR5 CXCR4
Eg Maraviroc - CCR5
Nucleoside RTIs
Prodrugs that require phosphorylation Then they mimic nucelotide building blocks for DNA Lamivudine Emtricitabine Zidovudine
Nucleotide RTI
Only require one step of phosphorylation (cf 3 in nucleoside)
Tenofovir
NRTI/NtRTI SE
Mitochondrial DNA is more vulnerable to effects of NRTI/NtRTIs
–> lactic acidosis, lipoatrophy in the face and limbs and peripheral neuropathy
Non-NRTIs
Directly bind the HIV RT, not competitive with NRTI/NtRTI as act at different place in pathway
Efavirenz
Nevirapine
Delavirdine
Integration inhibitors
Inhibits viral integrase enzyme - prevents viral DNA integration into host genome
Raltegravir
Elvitegravir
Protease inhibitors
Block protease enzyme, HIV uses this to break up large polyproteins, required for assembly of new viral particles
HIV can still replicate, but produces immature virions that cannot infect new cells
Ritonavir
SE- hyperlipidaemia, fat redistribution, T2DM
Enfvirtide - class, SE
Fusion inhibitor, targets gp41
SE- local rxn to injection
Maraviroc
Attachment inhibitor, targets CCR5
Unknown SE
Zidovudine
NRTI
SE- general- fever, headache, GI disturbance
Specific - BM supression
Lamivudine
NRTI general SEs
Emtricitabine
NRTI - general SEs
Mitochondrial Toxicity
Stavudine
Peripheral Neuropathy
Zalcitabine, Stavudine
Hypersensitivity
Abacavir
Tenofovir
NtRTI
SE bone and renal toxicity
Efavirenz
NNRTI
CNS effects
Nevirapine
NNRTI - Hepatitis and Rash
Delavirdine
NNRTI - rash
Raltegravir
Integration inhibitor
Unknown SE
Protease inhibitor SEs
Hyperlipidaemias
Fat redistribution
T2DM
