Table 1 Major anti-retroviral drugs
From: Thirty years of the human immunodeficiency virus epidemic and beyond
Properties | Drug class | ||||||
|---|---|---|---|---|---|---|---|
NRTIs/NtRTIs | NNRTIs | PIs | INSTIs | Fusion inhibitors | Entry inhibitors | Multiclass combinations | |
Main formulations | Nucleoside analogs AZT: zidovudine (Retrovir) ddI: didanosine (Videx) ddC: zalcitabine (Hivid) d4T: stavudine (Zerit) 3TC: lamivudine (Epivir) ABC: abacavir (Ziagen) FTC: emtricitabine (Emtriva) Nucleotide Analogs TDF: tenofovir (Viread) Combinations AZT/3TC (Combivir) ABC/3TC (Epzicom) AZT/ABC/3TC (Trizivir) TDF/FTC (Truvada) | First generation DLV: delaviridine (Rescriptor) EFV: efavirenz (Sustiva) NVP: nevirapine (Viramune) Second generation ETR: etravirine (Intelence) RPV: rilpivirine (Edurant) In discovery/trial Lersivirine (UK-453061) | First generation APV: amprenavir (Agenerase) SQV: saquinavir (Invirase) IDV: indinavir (Crixivan) FPV: fosamprenavir (Lexiva) RTV: ritonavir (Norvir) NFV: nelfinavir (Viracept) First generation TPV: tipranavir (Aptivus) DRV: darunavir (Perzista) ATZ: atazanavir (Reyataz) Combination Loprinavir/ RTV (Kaletra) DRV/low dose RTV (boosted Prezista) ATZ/low dose RTV (boosted Reyetaz) | RAL: Raltegravir (Isentress) EVG: Elvitegravir (GS-9137) used only in combo in Stribid In discovery/trial Dolutegravir (S/GSK1349572) | ENF: enfuvirtide (Fuzeon) In discovery/trial Ibalizumab (TMB-355) | Maraviroc (Selzentri) In discovery/trial Vicriviroc (SCH 417690) Cenicriviroc (TAK-652) | Emtricitabine/tenofovir/efavirenz (Atripla) Emtricitabine/tenofovir/rilpivirine (Complera) Emtricitabine/tenofovir/elvitegravir/cobicistat (Stribild) |
Advantages | Easy dosing schedule Long half-life Little food effect Dual NRT established as backbone of combination Tx Fewer drug interactions | Low toxicity Impressive long-term results No food effects Less lipid abnormalities Saves PIs for future use | High genetic threshold Useful for treatment-experienced patients with NNRTI drug resistance | Useful for treatment-experienced patients with multiple drug resistance No food effects Fewer adverse effects and interactions | Useful for treatment-experienced patients with multiple drug resistance | Useful for adult patients infected with only CCR5-tropic HIV-1 | Easy to use Recommended for treatment-naive patients |
Disadvantages | Some members lead to serious side effects Potential for drug interactions, cross resistance, and transmission of resistance Screening for HLA-B*5701 required for abacavir | Low genetic barrier for mutation Cross resistance Potential for drug interactions | Complex food requirements Cross-resistance is common and have severe side effects CYP3A4 inhibitors and substrate Drug interaction Side effects | Lower genetic barrier for mutations than PIs | Effectiveness in treatment-naive patients still being studied | Not recommended in patients with dual/mixed or CXCR4-tropic HIV-1 Requires viral tropism assay Bronchitis Drug interactions | Rilpivirine has higher rate of virological failure if HIV-1 RNA >100 000 copies·mL−1 |
Major side effects | Peripheral neuropathy Myopathy and myositis Cardiomyopathy Lactic acidosis Hepatic steatosis (adiposis) Lipodystrophy Pancreatitis Bone marrow suppression | Hepatic and renal toxicity Neuropsychiatric effects Drug–drug interactions Stevens–Johnson syndrome | Insulin resistance Dyslipidemia Hepatotoxicity Osteonecrosis and osteoporosis Drug–drug interactions Possible increased bleeding risk in hemophiliacs | Depression Suicidal tendencies Myopathy and rhabdomyolysis Reported Stevens–Johnson syndrome and toxic epidermal necrolysis | Risk of kidney dysfunction Injection-site reactions Hypersensitivity reaction Increased risk of bacterial pneumonia | Heaptotoxicity Cardiovascular events Bladder irritation Upper respiratory tract infection | Hepatic and renal toxicity Lactic acidosis With HBV co-infection, discontinuation can lead to severe acute HB exacerbations Neuropsychiatric effects Major drug interactions |
Common side effects | Nausea, vomiting, abdominal pain, diarrhea, loss of appetite, lethargy, muscle weakness, insomnia, headache, dizziness | Nausea, vomiting, diarrhea, insomnia, unusual or vivid dreams, dizziness, rash | Nausea, vomiting, diarrhea, rash, headache | Nausea, diarrhea, fever, headache | Fatigue, numbness in feet or legs, dizziness, insomnia | Nausea, cough, fever, dizziness, headache, bloating and distention | Diarrhea, nausea, fatigue, headache, dizziness, depression, insomnia, abnormal dreams and rash |
