PHARM: Anti-HIV drugs Flashcards
What does p24 in ELISA indicate?
HIV (p24 is a capsule protein that incr viral load)
What are two other sx in primary HIV syndrome
HAND: HIV assoc neurologic dysfxn
Seroconversion: HIV ab negative for first few months then converts to positive
What are the four types of HIV therapy
Reverse Transcriptase Inhibs
Entry inhibs
Protease inhibs
Integrase inhibs
Which type of HIV drug is involved in salvage therapy?
Entry inhibitors!
What are the 2 entry inhibitors?
Enfuvirtide and Maraviroc
Which drugs end in “navir”?
Protease inhibitors!
Which drugs end in “gravir”?
Integrase inhibitors
Which drug besides protease inhibs suppresses Cytochrome P450?
Colbicisat
What do NRTIs do?
Disrupt chain elongation (inhib DNA poly)
Main toxicity of NRTI?
Mitochondrial toxicity
What is Tenofovir?
only nucleotide RT inhib phosphorylated once
What do entry inhibitors Enfuvirtide and Maraviroc do?
Enfuvirtide- changes gp40 (proteolytic hydrolysis met, not 450)
Maraviroc- CCR5 costim inhib
Integrase inhibs sxe
Steven johnsons
met by glucor not 450
HAART tx?
need at least THREE drugs from at least 2 diff categories
Which drug should we use first in HAART, but what if pt has obesity/CV issues?
protease inhibs, unless CV issues then use NRTI (2) + NNRTI etc
Whats an example of a combo of HAART to avoid?
avoid 2 NNRTIs
An ex of a sxe with a protease inhib
insulin resistance
Which drug is v strong inhib of P450 so can use w PI to make it stronger?
ritonavir
Adv to phenotype testing? Disadv?
Adv: direct, can do partial res
Disadv: cutoffs not standardized, less sensitive than geno, $$$
What conversion rxn is inv in dTMP synth
DHF to THF via DHF reductase (produces deoxythymy, a DNA synth component)
Hematochromatosis
Chronic excess of total body iron (eg issue with abs or frequent transfusions)
Which defs cause microcytic vs megaloblastic anemia?
Microcytic-iron def
Megaloblastic-B12 and folate def
What is pernicious anemia caused by?
defect in INTRINSIC FACTOR which helps with B12 absorption
What to G-CSF and GM-CSF do?
tx, hematopo GFs which improve rbc count, stim granulocytes (neutros) and myleoid cells
Why would renal failure cause anemia
kidneys produce EPO!
What is epoeitin-alpha?
Recomb EPO for renal failure, acts on receptors on ery progens in bone marrow to stim rbc prod (receptor agonist)
2 forms of EPO that have longer half lives?
Darbepoeitin alpha (glycosylated form) Methoxy.......beta
EPO tox/complications?
HTN and thrombosis
What do u treat with EPO?
chronic and end stage renal dis
who gets iron def
women bc blood loss and vegetarians/malnourished
iron supplements
ferrous sulfate gluconate and fumaarate
IV iron
iron dextran, sodium ferric gluconate complex, iron sucrose
Why cant iron be given in hemolytic anemia
iron stores elev in this
in which anemia should iron NOT be given
hemolytic anemia
which ppl shoudl have folate supp
pregnancy!
If megaloblastic anemia, what should be ruled out before dx with folic acid def?
b12 def
B12 is produced by gut bacteria and needs ___produced by ____ to absorb iron in the ____
IF, gastric parietal cells, intestine
which def causes neuro issues
b12
2 forms of b12 and which has longer half life
hydroxycobalamin
what conversions does b12 do
homocystine AND methylmalonyl coa
How is iron conv and abs by ints
iron abs as ferrous Fe2+ hem via DMT1 transporter in int.
stored as ferritin
when iron needed, ferrious iron transf across BL by ferroportin then oxidized to ferric Fe3 by ferroxidase
-ferric complexed with transferrin and transp to blood
Tx of acute iron intox
DEFEROXAMINE (common in kdis)
Tx of chronic iron intox
DEFERASIROX or above iron chelators
what do b12 and folic acid help w
DNA SYNTH OF RBC
Why is folic acid monoTx contraind in tx of pernicious anemia?
bc doesnt tx b12 neuro issues!
