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Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Table 3. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Generic Name
(Abbreviation) /
Trade Name
Formulation
Recommendations
Adverse Events
Abacavir (ABC) /
Hypersensitivity reaction that can be fatal; Ziagen
symptoms may include fever, rash, nausea, vomiting, malaise or fatigue, loss of appetite, and respiratory symptoms (such as sore throat, cough, shortness of breath). Trizivir — with ZDV Trizivir:
Epzicom — with
Didanosine (ddI) / Videx EC:
Pancreatitis, peripheral neuropathy, nausea, Videx, Videx EC,
Lactic acidosis with hepatic steatosis is a rare but same as Videx EC) Videx buffered tabs: potentially life-threatening toxicity associated with Body weight < 60 kg: 250mg daily (buffered tablets or EC capsule) or 125mg twice daily (buffered tablets); with TDF: appropriate dose not established, probably < 250mg/day Emtricitabine
Minimal toxicity; lactic acidosis with hepatic (FTC) / Emtriva
steatosis is a rare but potentially life-threatening Truvada — with
Atripla — with TDF Atripla:
Lamivudine (3TC) / Epivir:
Minimal toxicity; lactic acidosis with hepatic Epivir
150- and 300-mg tablets or daily or 300mg daily steatosis is a rare but potentially life-threatening Combivir — with
Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Generic Name
(Abbreviation) /
Trade Name
Formulation
Recommendations
Adverse Events
Epzicom — with
Trizivir — with ZDV Trizivir:
Stavudine
Peripheral neuropathy; lipodystrophy; rapidly (d4T) / Zerit
progressive ascending neuromuscular weakness (rare); pancreatitis; lactic acidosis with hepatic steatosis (higher incidence with d4T than with Tenofovir
Asthenia, headache, diarrhea, nausea, vomiting, disoproxil
and flatulence; renal insufficiency; lactic acidosis fumarate (TDF) /
with hepatic steatosis is a rare but potentially life-threatening toxicity with use of NRTIs. Viread
Truvada — with
TDF 300mg + FTC 200mg 1 tablet once daily Atripla
Zalcitabine (ddC) / 0.375- or
Peripheral neuropathy; stomatitis; lactic acidosis Hivid
with hepatic steatosis is a rare but potentially life- threatening toxicity with use of NRTIs; pancreatitis Anticipated discontinuation of distribution in 2006 Zidovudine
Bone marrow suppression; macrocytic anemia or (AZT, ZDV) /
neutropenia; gastrointestinal intolerance, Retrovir
headache, insomnia, asthenia; lactic acidosis with hepatic steatosis is a rare but potentially life- threatening toxicity associated with use of NRTIs. Combivir
Trizivir — with 3TC Trizivir:
3TC 150mg + ZDV 300mg + ABC 300mg Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Table 4. Characteristics of Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Generic Name
(Abbreviation) /
Trade Name
Formulation
Dosing Recommendation
Adverse Events
Delavirdine (DLV) 100-mg or 200-mg tablets
400mg 3 times daily; four 100-mg Rash*; increased transaminase / Rescriptor
tablets can be dispersed in >/= 3 levels; headaches oz of water to produce slurry; 200-mg tablets should be taken as intact tablets; separate dosing from buffered didanosine or antacids by 1 hour Efavirenz (EFV) / 50-, 100-, 200-mg capsules or
Sustiva
Atripla
Nevirapine (NVP) 200-mg tablets or
/ Viramune
thereafter, 200mg by mouth twice syndrome*; symptomatic hepatitis, daily including fatal hepatic necrosis, have been reported‡ During clinical trials, NNRTIs were discontinued because of rash among 7% of patients taking nevirapine, 4.3% of patients taking delavirdine, and 1.7% of patients taking efavirenz. Rare cases of Stevens-Johnson syndrome have been reported with the use of all 3 NNRTIs, the highest incidence seen with nevirapine use. Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, confusion, abnormal thinking, impaired concentration, amnesia, agitation, depersonalization, hallucinations, and euphoria. Overall frequency of any of these symptoms associated with use of efavirenz was 52%, as compared with 26% among control subjects; 2.6% of those persons on efavirenz discontinued the drug because of these symptoms; symptoms usually subside spontaneously after 2–4 weeks. Symptomatic, sometimes serious, and even fatal hepatic events (accompanied by rash in approximately 50% of cases) occur with significantly higher frequency in female patients with pre-nevirapine CD4+ T-cell counts > 250 cells/mm³ or in male patients with pre-nevirapine CD4+ T-cell counts > 400 cells/mm³. Nevirapine should not be initiated in these patients unless the benefit clearly outweighs the risk. This toxicity has not been observed when nevirapine is given as single doses to mothers or infants for prevention of mother-to-child HIV transmission. Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Table 5. Characteristics of Protease Inhibitors (PIs)
Generic Name /
Trade Name
Formulation
Dosing Recommendations
Adverse Effects
Amprenavir
Agenerase
Note: APV and RTV oral
Note: APV 150-mg capsule is
Note: Oral solution contains
propylene glycol; contraindicated in pregnant women, children < 4 years old, patients with hepatic or renal failure, and patients treated with disulfiram or metronidazole. Atazanavir (ATV) 100-, 150-, 200-mg capsules
/ Reyataz
asymptomatic first-degree AV block; use with caution in RTV 100mg + ATV 300mg once patients with underlying concomitant medications that can cause PR prolongation; hyperglycemia; fat maldistribution; possible increased bleeding episodes in patients with hemophilia. Darunavir (DRV) / 300-mg tablet
600mg twice daily + RTV 100mg Hyperlipidemia; Prezista
hyperamylasemia transaminase elevation; headache; GI symptoms Fosamprenavir (f- 700-mg tablet
APV) / Lexiva
f-APV 1400mg twice daily; nausea, vomiting; headache; or hyperlipidemia; transaminase elevation; hyperglycemia; fat PI-experienced pts (once-daily regimen not recommended): Co-administration w/EFV (unboosted f-APV not recommended): (f-APV 700mg + RTV 100mg) twice daily; or Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Generic Name /
Trade Name
Formulation
Dosing Recommendations
Adverse Effects
Indinavir (IDV) /
Crixivan
hyperbilirubinemia; headache, asthenia, blurred vision, thrombocytopenia, alopecia, and hemolytic anemia; hyperglycemia; fat maldistribution; possible increased bleeding episodes in patients with hemophilia. Lopinavir +
Each tablet contains LPV 200mg LPV 400mg + RTV 100mg (2 Ritonavir (LPV/r) / + RTV 50mg
Kaletra
tablets or 10mL); Note: once-
daily dosing only recommended elevated scrum transaminases; Note: Oral solution contains
for patients receiving EFV, NVP, increased bleeding episodes in With EFV or NVP: For treatment-experienced pts: LPV 600mg + RTV 150mg (3 oral tablets) twice daily, or LPV 533mg + RTV 133mg (6.7-mL oral solution) twice daily with food Nelfinavir (NFV) / 250-mg tablets or 625-mg
Viracept
maldistribution; possible increased bleeding episodes among patients with hemophilia; serum transaminase elevation. Ritonavir* (RTV) / 100-mg capsules, or
Norvir
hyperglycemia; fat maldistribution; possible increased bleeding episodes in patients with hemophilia. Saquinavir
tablets and hard-
gel capsules
(SQV-hgc) /
Invirase
Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Generic Name /
Trade Name
Formulation
Dosing Recommendations
Adverse Effects
Saquinavir soft- 200-mg capsules
gel capsule
(SQV-sgc) /
Fortovase
maldistribution; possible increased bleeding episodes in patients with hemophilia. Tipranavir
(TPV) / Aptivus
underlying liver diseases; skin rash — TPV has a sulfonamide moiety, use with caution in patients with known sulfonamide allergy; rare cases of fatal and nonfatal intracranial hemorrhage have been reported; hyperlipidemia (especially hypertriglyceridemia); hyperglycemia; fat maldistribution; possible increased bleeding episodes in patients with hemophilia. ARV = antiretroviral; pts = patients; GI = gastrointestinal; AV = atrioventricular Dose escalation for ritonavir when used as sole PI: days 1 and 2, 300mg twice daily; days 3–5, 400mg twice daily; days 6–13, 500mg twice daily; day 14, 600mg twice daily. Medscape's Antiretroviral Pocket Guide
for the Treatment of HIV Infection

Table 6. Characteristics of Fusion Inhibitors
Generic Name /
Trade Name
Formulation
Dosing Recommendations
Adverse Effects
Enfuvirtide (T20) / Injectable — in lyophilized
90mg (1mL) subcutaneous twice Local injection site reactions — Fuzeon
include rash, fever, nausea, vomiting, chills, rigors, hypotension, or elevated serum transaminases; rechallenge is not recommended.

Source: https://law.duke.edu/sites/default/files/migrated_files/dl_file-aidsproject-400_01-GuideAntriRetros_1.pdf

Doi:10.1016/s0002-9343(03)00666-

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