Module 3: Chapter 46 HIV drugs Flashcards
what cells are necessary for normal immune fn
CD4
what is the fn of the CDR4 cell
recognizes foreign antigens and infected cells
helps activate the antibody-producing B lymphocytes
what cells induce cell-mediated immunity
CD4
is HIV bacteria or a virus
retrovirus
how can you tell the difference btw. a retrovrius and virus
difference is in the genetic material
How does CD4 activate T cells to destroy antigens
activate B lymphocytes
which produce antibodies activating T cell
T8 Killer cell attacks antigen
Binding between what two things begins an HIV infection
gp120 on HIV virus to CD4 receptor on a cell
what happens one the virus is bound to the cell
viral envelope and the plasma membrane fuse
What types of cells have a CD4 protein receptor site
monocytes
macrophages
certain nerve cells
what happens in the cell once GP120 attaches to a CD4 receptor
in the cell viral RNA is transcribed into a single strand of viral DNA
what cells does the HIV virus have an infinity for
CD4 cells
how is HIV infection tested
initially made by a screening test followed by a confirmatory assay
Are screening tests highly sensitive or highly specific
highly sensitive
are confirmatory assays highly sensitive or highly specific?
highly specific
combination use of screening tests and confirmatory assays produces results thatare
highly accurate
what was the first class of drugs approved by the FDA to treat HIV infection and AIDS
nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)
what are NRTIs chemically similar to
human nucleotides “building blocks” of DNA
what must NRTI’s do to be effective?
convert to their active forms.
what do NRTIs do?
inhibit reverse transcriptase an enzyme critical to HIV replication
what is the prototype drug for NRTI’s
zidovuidine (AZT, ZDV, Retrovir)
what 3 conditions is zidovudine commonly used to treat
epstein-Barr Virus
hepatitis B virus
HIV infection
how is zidovudine administered
parenterally or orally
where is zidovudine commonly metabolized? excreted?
liver
kidneys
the usual
how does zidovudine work
inhibits the synthsis of DNA by reverse transcriptase
are there any contraindications or precautions to zidovudine therapy
hypersensitivity
breast-feeding
lactic acidosis
what are some adverse effect of zidovudine
GI symptoms headache seizures somnolence hematologic toxicities
what are known drug interactions for zidovudine
ganciclovir acetaminophen interferon beta-1b probenecid rifampin trimethoprim valproic acid
what do you need to assess for regarding female patients and zidovudine
assess pregnancy and lactation
understanding of HIV transmission
when should zidovudine be administered
1 hour before meals
what type of diet should a patient undergoing zidovudine have
low fat
what should be done to minimize adverse effects regarding patients zidovudine
IM injections
how often should laboratory data be obtained for a patient receiving zidovudine
every 2-4 weeks
what are absolute contraindications regarding zidovudine use
hypersensitivity
breast-feeding
existing lactic acidosis
what is the second class of drugs used to treat HIV infection
nonnucleoside reverse transcriptase inhibitors (NNRTIs)
NNRTI’s stand for
nonnucleoside reverse transciptase inhibitors
Do NNRTI’s only affect HIV-1 or HIV-2
HIV-1
how do NNRTIs work
inhibit a specific site on the reverese transciptase that is required to carry out the process of DNA synthesis
what is the prototype drug for NNRTIs
efavirenz (Sustiva)
What is Sustiva used for
to treat HIV-1 infection
why do NNRTIs not work on HIV-2
, they do not reverse transciptase in HIV-2
How is efavirenz administered
orally
is efavirenz protein bound?
yes
where does efavirenz metabolized?
excreted?
liver
urine and feces
how does efavirenz work?
inhibits HIV reverse transciptase
what are some adverse effects for efavirenz
diziness impaired concentration insomnia abnormal dreams hallucinations
what drugs interact with efavirenz
drugs that are metabolized by P-450 CYP3A4
What pregnancy class is efavirenz
category D
how many times a day is efavirenz administered? is there a preferred time(s)?
once
at bedtime
what should a patient do if they miss a dose of efavirenz
take the next dose as soon as they remember unless it’s for the next day
what is one way that the adverse effects of efavirnez can be minimized
on an empty stomach
what is important patient and family education regarding efavirenz therapy
importance of adherence to drug therapy
advise pts. experienceing depression, anxiety, behavior changes, and those feeling paranoid or manic to contact the health care provider immediately
what ongoing assessment is necessary in a patient being treated with efavirenz
periodic examinations and blood monitoring
What pregnancy category is efavirenz
D
teratogenic during all trimesters
What is the third major class of drugs used in treating HIV infection and AIDs
protease inhibitors
what class of drugs has changed the opinion of experts as to the ultimate fatality of HIV and AIDS
preotease inhibitors
what class of HIV drugs is the most potent anti-HIV drugs
Preotease Inhibitors
what is the prototype drug for protease inhibitors
saquinavir (Invirase)
What is the purpose of saquinavir
treating HIV infection in adults
how is saquinavir administered
orally
true or false: saquinavir has great bioavailability
false, poor bioavailability
where is saquinavir exreted
feces and urine
how does saquinavir work?
competetive inhibitor or HIV protease, an enzyme required for HIV replication
are there any precautions or contraindications regarding saquinavir
hypersensitivity
children under age 16
What are the adverse effects of squinavir
Nausea diarrhea stomach discomfort insomnia headahce
are there any drug interactions for squinavir?
interacts with drugs that are metabolized by P-450 CYP3A4
what things should be assessed for regarding saquinavir
pregnancy or lactation
patients ability to adhere to drug therapy
When shoudl saquinavir tablets be administered
2 hours after eating a full meal
what should be administered with each dose of squinavir
ritonavir
what can be done to decrease GI distress if it is experienced during saquinavir treatment
small frequent meals
if a patient complains of headahces during saqunavir treatment what should be adminsitered
acetaminophen
What are two key pieces of information that the patient and family need to be educated on regarding squinavir
periodic clinical and blood monitoring
S & S of diabetes
due to the poor bioavailability of squinavir given alone , what medication is commonly given in combination with saquinavir to increase bioavailability
ritonavir: significantly inhibits squinivars metabolism resulting in an increased serum concentration of squinavir
what does HAART stand for
highly active antiretroviral therapy (for HIV)
what is the newest class of HAART therapy approved for management of HIV disease
Integrase inhibitors
what is integrase
enzyme that is a key component that allows converted HIV viral DNA to enter the host cell
how do integrase inhibitors work?
block or inhibit the host cell DNA to produce genetic material for new viruses
what is the prototype for integrase inhibitors
raltegravir (Isentress)
what is raltegravir commonly used for
HIV strains that are resistant to multiple antiretroviral regimens and epereince ongoing viral replication while reciving HAART
what is the half life for raltegravir
9 hours
how is raltegravir metabolized? excreted?
liver
feces, urine
How does raltegravir work?
HIV virus integrase strand transfer inhibitor
known contraindications for raltegravir?
use cautiously with drugs that can cause muscle problems
what are the adverse effects of raltegravir?
diarrhea nausea abdominal distension pain flatulence headache fatigue
known drug interactions with ratlegravir
many HAART medications
firampin
proton pump inhibitors
what should be assessed for regarding raltegravir
wheterhe treatment expereinced or treatment naive
what pregnancy category is raltegravir
C
what needs to be stressed with raltegravir?
need for safe sex
does raltevir need to be given with food
with or without is fine
true or false: RAltegravir should not be used as monotherapy
true
what should a patient taking raltegravir take for common adverse effects
OTC medications
what should be monitored for during raltegravir treatemtn
opportunistic diseases
What pregnancy category is raltegravir
C - no well controlled studies, women should contact their prescriber immediately if they believe they are pregnant
what are entry inhibitors also known as
fusion inhibitors
what new class of drugs inhibits the HIV virus from binding to it, fusing with it and entering a human cell
entry inhibitors
what is the prototype drug for entry inhibitors
enfuvirtide (Fuzeon)
What is the purpose of enfuvirtide?
managing HIV infection in pts who have expereicend treatment failure
how is enfuvirtide administered
SC
how does enfuvirtide work
binds to the pg41 protein on the surface of HIV
what are the adverse effects of enfuvirtide
injection site rxn anorexia nausea weight loss fatigue anxiety headache insomnia peripheral neuropathy infections
what pregnancy category is enfuvirtide
category B
what lifestyle, diet and habit teaching should be done with patients on enfuvirtide therapy
avoid risk factors that predispose him or her to infection
how can therapeutic effects be maximized for enfuvirtide
reconstitute it with sterile water and then allow the solution to sit for 10 mintues to ensure that the powder dissolves completely
aseptic technique important
what ongoing assessment should be done for a patient taking enfuvirtide
assess the patient taking enfuvirtide for signs of infectious disorders such as pneumonia, sinusitis, herpes simplex, influenza and conjunctivitis
what is a major adverse effect of enfuvirtide
injection site rxn