DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

1626 control but also complicates the practice of HIV medicine. Current
Table 59–1
challenges include access to effective long-term treatment in
Antiretroviral Agents Approved for Use in the U.S. resource-poor countries and the continuing need for identification
of new drugs for treatment-experienced patients with resistance to
GENERIC NAME
ABBREVIATION;
approved drugs (Flexner, 2007).
[U.S. TRADE NAME] CHEMICAL NAMES
Nucleoside Reverse Transcriptase Inhibitors
Zidovudine
ZDV; azidothymidine PRINCIPLES OF HIV CHEMOTHERAPY
[RETROVIR, others] a
(AZT)
Current treatment assumes that all aspects of disease
Didanosine [VIDEX; VIDEX ddI; dideoxyinosine
EC, others]
derive from the direct toxic effects of HIV on host cells,
Stavudine
d4T; didehy-
mainly CD4+ T-lymphocytes. All treatment regimens
[ZERIT]
drodeoxythymidine associated with long-term suppression of HIV replication
(as measured by decreased plasma HIV RNA) and
Zalcitabine [HIVID] c DDC; dideoxycytidine
Lamivudine [EPIVIR] a
Abacavir [ZIAGEN] a
3TC; dideoxythiacytidine
ABC; cyclopropylaminopurinylcyclopentene
repletion of peripheral CD4 cells are clinically beneficial
(Lee et al., 2001). The goal of therapy is to suppress
virus replication as much as possible for as long
Tenofovir disoproxil TDF; phosphinyl-
as possible.
[VIREAD] a
methoxypropyladenine
Deciding when to start antiretroviral therapy has
(PMPA)
been a shifting target during the epidemic. Current
Emtricitabine
FTC; fluorooxathiolanyl
guidelines in the U.S. recommend starting therapy in all
[EMTRIVA] a
cytosine
those with a CD4 count of ≤350 cells/mm 3 (Department
Non-nucleoside Reverse Transcriptase Inhibitors
of Health and Human Services, 2010). Treatment is also
Nevirapine [VIRAMUNE] NVP
recommended for HIV-infected pregnant women, those
Efavirenz [SUSTIVA; STOCRIN] a EFV
with HIV nephropathy, and those with concurrent hepatitis
B virus infection requiring treatment regardless of
Delavirdine [RESCRIPTOR] DLV
Etravirine [INTELENCE] ETV
CD4 count. Increasing evidence supports the clinical
Protease Inhibitors
benefit and cost effectiveness of starting treatment at
Saquinavir [INVIRASE] SQV
Indinavir [CRIXIVAN] IDV
higher CD4 counts. With more active drug combinations,
large systematic reviews of observational studies
Ritonavir [NORVIR]
RTV
Nelfinavir [VIRACEPT] NFV
and a few randomized clinical trials suggest measurable
Amprenavir [AGENERASE; APV
clinical benefit the earlier treatment is initiated, beginning
PROZEI] c
Lopinavir [KALETRA;
ALUVIA] b
LPV/r
at CD4 counts ≤500 (Kitahata et al., 2009; When to
Start Consortium, 2009). In the foreseeable future, treatment
may be recommended for all infected adults and
Atazanavir [REYATAZ; ATV
children (Flexner, 2007).
ZRIVADA]
Increasing evidence supports the value of antiretroviral
therapy in preventing transmission of the virus from
Fosamprenavir [LEXIVA; FPV
TELZIR]
person to person. Although most antiretroviral therapy is
Tipranavir [APTIVUS] TPV
Darunavir [PREZISTA] DRV
used in chronic treatment of established infection, these
medications are also used in short courses to prevent
Entry Inhibitors
infection in post-exposure settings and to prevent
Enfuvirtide [FUZEON] T-20
Maraviroc [SELZENTRY; MVC
mother-to-child transmission (Department of Health and
CELSENTRI]
Human Services, 2010). Epidemiological modeling suggests
that overall transmission rates are likely to fall in
Integrase Inhibitor
Raltegravir [ISENTRESS] RAL
endemic areas where antiretroviral therapy is widely
a
used (Granich et al., 2009). The possible value of targeted
antiretroviral therapy to reduce new infections,
A number of fixed-dose co-formulations are available: zidovudine
+ lamivudine (COMBIVIR); zidovidine + lamivudine + abacavir
(TRIZIVIR); abacavir + lamivudine (EPZICOM); tenofovir + emtricitabine
or even to reduce or eliminate epidemic transmission,
(TRUVADA); tenofivir + efavirenz + emtricitabine (ATRIPLA). has not been adequately explored (Dieffenbach and
b
Lopinavir is available only as part of a fixed-dose co-formulation
Fauci, 2009).
with ritonavir (KALETRA/ALUVIA). c No longer marketed worldwide.
A number of studies have confirmed the low likelihood
that HIV can be eradicated with drug therapy.
SECTION VII
CHEMOTHERAPY OF MICROBIAL DISEASES