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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 200mg1 tablet once dailyAtripla 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 300mgMedscape'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.
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