Human Immunodeficiency Virus (HIV) Infection

USES

Antiretroviral (ARV) agents are used in the treatment of HIV infection.

An ARV regimen for treatment-naive patients generally consists of two nucleoside reverse transcriptase inhibitors (NRTIs) in combination with a third ARV medication from one of three drug classes: an integrase inhibitor (INSTI), non-nucleoside reverse transcriptase inhibitor, or a protease inhibitor (PI) with either cobicistat or ritonavir.

ACTION

Nucleoside reverse transcriptase inhibitors compete with natural substrates for formation of proviral DNA by reverse transcriptase inhibiting viral replication.

Nucleotide reverse transcriptase inhibitors (NtRTIs) inhibit reverse transcriptase by competing with the natural substrate deoxyadenosine triphosphate and by DNA chain termination.

Non-nucleoside reverse transcriptase inhibitors directly bind to reverse transcriptase and block RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.

Protease inhibitors (PIs) bind to the active site of HIV-1 protease and prevent the processing of viral gag and gag-pol polyprotein precursors resulting in immature, noninfectious mal particles.

Fusion inhibitors interfere with the entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes. CCR5 coreceptor antagonist selectively binds to human chemokine receptor CCR5 present on cell membrane preventing HIV-1 from entering cells.

Integrase inhibitor inhibits catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme required for viral replication.

ANTIRETROVIRAL AGENTS FOR TREATMENT OF HIV INFECTION

Name	Availability	Dosage Range	Side Effects
Nucleoside Analogues
Abacavir (Ziagen)	T: 300 mg OS: 20 mg/mL	A: 300 mg 2 times/day or 600 mg once daily	Nausea, vomiting, malaise, rash, fever, headaches, asthenia, fatigue, hypersensitivity reactions
Didanosine (Videx EC)	DR: 125 mg, 200 mg, 250 mg, 400 mg OS: 2 g/bottle, 4 g/bottle	DR (weighing 60 kg or more): 400 mg once daily; (weighing 25–59 kg): 250 mg once daily; (weighing 20–24 kg): 200 mg once daily OS (weighing more than 60 kg): 200 mg q12h or 400 mg once daily; (weighing less than 60 kg): 125 mg q12h or 250 mg once daily	Peripheral neuropathy, pancreatitis, diarrhea, nausea, vomiting, headaches, insomnia, rash, hepatitis, seizures
Emtricitabine (Emtriva)	C: 200 mg OS: 10 mg/mL	A: 200 mg/day (C) 240 mg/day (OS)	Headaches, insomnia, depression, diarrhea, nausea, vomiting, rhinitis, asthenia, rash
Lamivudine (Epivir)	T: 100 mg, 150 mg, 300 mg OS: 5 mg/mL, 10 mg/mL	A: 150 mg 2 times/day or 300 mg once daily C: 4 mg/kg 2 times/day	Diarrhea, malaise, fatigue, headaches, nausea, vomiting, abdominal pain, peripheral neuropathy, arthralgia, myalgia, skin rash
Stavudine (Zerit)	C: 15 mg, 20 mg, 30 mg, 40 mg OS: 1 mg/mL	A (weighing more than 60 kg): 40 mg 2 times/day (20 mg 2 times/day if peripheral neuropathy occurs); (weighing 60 kg or less): 30 mg 2 times/day (15 mg 2 times/day if peripheral neuropathy occurs)	Peripheral neuropathy, anemia, leukopenia, neutropenia
Zidovudine (Retrovir)	C: 100 mg T: 300 mg Syrup: 50 mg/5 mL, 10 mg/mL	A: 300 mg 2 times/day	Anemia, granulocytopenia, myopathy, nausea, malaise, fatigue, insomnia
Nucleotide Analogues
Tenofovir TAF (Vemlidy)	T: 25 mg	A: 25 mg once daily	Headache, abdominal pain, fatigue, cough, nausea, back pain
Tenofovir TDF (Viread)	T: 300 mg	A: 300 mg once daily	Nausea, vomiting, diarrhea, headache, fatigue
Non-nucleoside Analogues
Delavirdine (Rescriptor)	T: 100 mg, 200 mg	A: 200 mg 3 times/day for 14 days, then 400 mg 3 times/day	Rash, nausea, headaches, elevated hepatic function tests
Efavirenz (Sustiva)	C: 50 mg, 200 mg T: 600 mg	A: 600 mg/day C: 200–600 mg/day based on weight	Headaches, dizziness, insomnia, fatigue, rash, nightmares
Etravirine (Intelence)	T: 100 mg, 200 mg	A: 200 mg 2 times/day	Skin reactions (e.g., Stevens-Johnson syndrome, erythema multiforme), nausea, abdominal pain, vomiting
Nevirapine (Viramune, Viramune XR)	T: 200 mg T (ER): 400 mg S: 50 mg/mL	A: 200 mg/day for 14 days, then (if no rash) 200 mg 2 times/day	Rash, nausea, fatigue, fever, headaches, abnormal hepatic function tests
Rilpivirine (Edurant)	T: 25 mg	A: 25 mg once daily with a meal	Depression, insomnia, headache, rash
Protease Inhibitors
Atazanavir (Reyataz)	C: 100 mg, 150 mg, 200 mg, 300 mg	A: 400 mg/day or 300 mg (with 100 mg ritonavir) once daily	Headaches, diarrhea, abdominal pain, nausea, rash
Darunavir (Prezista)	T: 400 mg, 600 mg	A: 600 mg 2 times/day (with ritonavir 100 mg) or 800 mg once daily with ritonavir 100 mg	Diarrhea, nausea, vomiting, headaches, skin rash, constipation
Fosamprenavir (Lexiva)	T: 700 mg OS: 50 mg/mL	A: 1,400–2,800 mg/day with 100 mg ritonavir	Headaches, fatigue, rash, nausea, diarrhea, vomiting, abdominal pain
Indinavir (Crixivan)	C: 200 mg, 400 mg	A: 800 mg q8h or 800 mg 2 times/day with ritonavir 100 mg	Nephrolithiasis, hyperbilirubinemia, abdominal pain, asthenia, fatigue, flank pain, nausea, vomiting, diarrhea, headaches, insomnia, dizziness, altered taste
Lopinavir/ritonavir (Kaletra)	C: 133/33 mg OS: 80/20 mg	A: 400 mg/100 mg 2 times/day or 800 mg/200 mg once daily C (4–12 yrs): 10–13 mg/kg 2 times/day	Diarrhea, nausea, vomiting, abdominal pain, headaches, rash
Nelfinavir (Viracept)	T: 250 mg Oral Powder: 50 mg/g	A: 750 mg q8h or 1,250 mg 2 times/day C: 20–25 mg/kg q8h	Diarrhea, fatigue, asthenia, headaches, hypertension, impaired concentration
Ritonavir (Norvir)	C: 100 mg OS: 80 mg/mL	A: Titrate up to 800 mg/day based on protease inhibitor	Nausea, vomiting, diarrhea, altered taste, fatigue, elevated LFTs and triglyceride levels
Saquinavir (Invirase)	C: 200 mg T: 500 mg	A: 1,000 mg 2 times/day with ritonavir 100 mg	Diarrhea, elevated LFTs, hypertriglycerides, cholesterol, abnormal fat accumulation, hyperglycemia
Tipranavir (Aptivus)	C: 250 mg OS: 100 mg/mL	A: 500 mg (with 200 mg ritonavir) 2 times/day	Diarrhea, nausea, fatigue, headaches, vomiting
Fusion Inhibitors
Enfuvirtide (Fuzeon)	I: 108 mg (90 mg when reconstituted)	Subcutaneous: 90 mg 2 times/day	Insomnia, depression, peripheral neuropathy, decreased appetite, constipation, asthenia, cough
CCR5 Antagonists
Maraviroc (Selzentry)	T: 150 mg, 300 mg	A: 300 mg 2 times/day CYP3A4 inducers: 600 mg 2 times/day CYP3A4 inhibitors: 150 mg 2 times/day	Cough, pyrexia, upper respiratory tract infections, rash, musculoskeletal symptoms, abdominal pain, dizziness
Integrase Inhibitor
Raltegravir (Isentress)	T: 400 mg	A: 400 mg 2 times/day	Nausea, headache, diarrhea, pyrexia
Dolutegravir (Tivicay)	T: 50 mg	A: 50 mg once daily or 50 mg bid (with CYP3A inducers or resistance)	Insomnia, headache
Monoclonal Antibody
Ibalizumab-uiyk (Trogarzo)	I: 200 mg	IV: Initially, 2000 mg as a single dose, then 800 mg q14days	Dizziness, diarrhea; decreased Hgb, leukocytes, neutrophils, platelets; increased serum bilirubin, creatinine

A, adults; C, capsules; C (dosage), children; DR, delayed-release; ER, extended-release; I, injection; IV, intravenous; OS, oral solution; S, suspension; T, tablets; TAF, tenofovir alafenamide; TDF, tenofovir disoproxil fumarate.

FIXED-COMBINATION THERAPIES

Brand Name	Generic Name	Dosage
Atripla	Efavirenz 600 mg Emtricitabine 200 mg Tenofovir (TDF) 300 mg	1 tablet once daily
Biktarvy	Bictegravir 50 mg Emtricitabine 200 mg Tenofovir (TAF) 25 mg	1 tablet once daily
Cabenuva	Cabotegravir 400 mg, 600 mg Rilpivirine 600 mg, 900 mg	IM: 600/900 mg once, then 400/600 mg once/mo or 600/900 mg for 2 consecutive mos, then continue with injections q2mos starting on month 4
Cimduo	Lamivudine 300 mg Tenofovir (TDF) 300 mg	1 tablet once daily
Combivir	Lamivudine 150 mg Zidovudine 300 mg	1 tablet twice daily
Complera	Emtricitabine 200 mg Rilpivirine 27.5 mg Tenofovir (TDF) 300 mg	1 tablet once daily
Delstrigo	Doravirine 100 mg Lamivudine 300 mg Tenofovir 300 mg	1 tablet once daily
Descovy	Emtricitabine 200 mg Tenofovir (TAF) 25 mg	1 tablet once daily
Dovato	Dolutegravir 50 mg Lamivudine 300 mg	1 tablet once daily
Epzicom	Abacavir 600 mg Lamivudine 300 mg	1 tablet once daily
Evotaz	Atazanavir 300 mg Cobicistat 150 mg	1 tablet once daily
Genvoya	Cobicistat 150 mg Elvitegravir 150 mg Emtricitabine 200 mg Tenofovir (TAF) 10 mg	1 tablet once daily
Juluca	Dolutegravir 50 mg Rilpivirine 25 mg	1 tablet once daily
Odefsey	Emtricitabine 200 mg Rilpivirine 25 mg Tenofovir (TAF) 25 mg	1 tablet once daily
Prezcobix	Cobicistat 150 mg Darunavir 800 mg	1 tablet once daily
Stribild	Cobicistat 150 mg Elvitegravir 150 mg Emtricitabine 200 mg Tenofovir (TDF) 300 mg	1 tablet once daily
Symfi	Efavirenz 400 mg Lamivudine 300 mg Tenofovir (TDF) 300 mg	1 tablet once daily
Symtuza	Cobicistat 150 mg Darunavir 800 mg Emtricitabine 200 mg Tenofovir 10 mg	1 tablet once daily
Triumeq	Abacavir 600 mg Dolutegravir 50 mg Lamivudine 300 mg	1 tablet once daily
Trizivir	Abacavir 300 mg Lamivudine 150 mg Zidovudine 300 mg	1 tablet twice daily
Truvada	Emtricitabine 200 mg Tenofovir (TDF) 300 mg	1 tablet once daily

TAF, Tenofovir alafenamide; TDF, tenofovir disoproxil fumarate.

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Drug classification