Term
|
Definition
| drug that binds to the same site as the ligand and makes the same signal |
|
|
Term
| define allosteric agonist |
|
Definition
| drug that binds to different site than drug making no signal but causing drug to be more effective |
|
|
Term
|
Definition
| drug produces lesser response than the ligand and competes for ligand site |
|
|
Term
| define competitive agonist |
|
Definition
| drug binds reversibly to receptor but increase in ligand can overcome it |
|
|
Term
| define non-competitive agonist, what are the two types |
|
Definition
binds to receptor and prevents agonist from producing max effect
irreversible: more common, same receptor
allosteric: different receptor |
|
|
Term
| how can you tell if something on a graph is more potent or effective |
|
Definition
moving left on the X axis is more potent
moving up on the Y axis is more effective |
|
|
Term
| what does a partial agonist graph look like compared to agonist |
|
Definition
less effective
shorter, less high on the Y axis |
|
|
Term
| what does a allosteric agonist graph look like compared to agonist |
|
Definition
same effectiveness (height on Y axis)
increased potency (more left on X axis) |
|
|
Term
| what does a non-competitive agonist graph look like compared to agonist |
|
Definition
very short, sinking
less effective (height on Y axis)
less potent (more right on X axis) |
|
|
Term
| what does a antagonist graph look like compared to agonist |
|
Definition
same effectiveness (height on Y axis)
less potency (more right on X axis) |
|
|
Term
| how does a Gs protein work |
|
Definition
| activates cAMP which increases PKA |
|
|
Term
| how does a Gi protein work |
|
Definition
| decreases cAMP which decreases PKA |
|
|
Term
| how does a Gq protein work |
|
Definition
releases IP3 and DAG
IP3 releases Ca
DAG and Ca activate PKC |
|
|
Term
| what is the point of equal ionization |
|
Definition
|
|
Term
| what happens to an acid and base if you put it in stuff that is lower (more basic) than the pKa |
|
Definition
acid will ionize
base will not ionize |
|
|
Term
| what happens to an acid and base if you put it in stuff that is higher (more acidic) than the pKa |
|
Definition
acid will not ionize
base will ionize |
|
|
Term
| what form of a drug is best excreted |
|
Definition
WA will be excreted beter in a basic enivornment
WB will be excreted better in an acidic enivornment |
|
|
Term
| what form of a drug is best distributed in the body |
|
Definition
the same form
WA likes acid
WB likes base |
|
|
Term
| what is used to fix and WB or WB drug OD |
|
Definition
NaHCO3 is used to alkalize urine and fix WA OD
NH3CL is used to acidify urine and fix WB OD |
|
|
Term
|
Definition
| increases gene expression of P450 metabolizing enzymes which decreases the plasma level of the drug making it less effective and decreasing presence of symptoms |
|
|
Term
| what are 5 examples of inducers |
|
Definition
| rifampin, bensopyrine, chronic ethanol, phenytoin, barbituates |
|
|
Term
|
Definition
| decrease gene expression for metabolizing P450 enzymes increasing plasma concentration of the drug which increases symptoms |
|
|
Term
| what are 4 examples of inhibitors |
|
Definition
| cimetidine, erythromycin, ketonazole, grapefruit |
|
|
Term
| define first order metabolism |
|
Definition
rate of drug metabolism is proportional to concentration of the free drug
constant fraction of drug is metabolized per unit time |
|
|
Term
| define zero order metabolism |
|
Definition
drugs with large doses saturate metabolizing enzymes
constant amount of drug is metabolized per unit time |
|
|
Term
| what are 3 examples of drugs with zero order kinetics |
|
Definition
| aspirin, ethanol, phenytoin |
|
|
Term
| what is a maintience dose for, how is it calculated |
|
Definition
adjust rate so input equals rate of loss to keep a steady plasma level
(Cs)(Cl)/(F) |
|
|
Term
| what is loading dose for, how is it calculated |
|
Definition
load initial volume of drug needed
(Cp)(Vd)/(F) |
|
|
Term
| how long does it take to get to steady state, what is it dependent on(2) |
|
Definition
4-5 half lives
depends on half life and steady state is determined by first order kinetics |
|
|
Term
|
Definition
zidovudine
lamivudine
entricitabine |
|
|
Term
|
Definition
| host adds 3P then drug terminates DNA elongation |
|
|
Term
|
Definition
peripherial neuropathy
lactic acidosis
marrow supression - zidovudine |
|
|
Term
|
Definition
|
|
Term
|
Definition
| host adds 2P, drug terminates DNA elongation |
|
|
Term
|
Definition
|
|
Term
|
Definition
maculopapular rash
CNS effects - enfavirenz |
|
|
Term
|
Definition
| binds reverse transcriptase causing inactivation |
|
|
Term
| name a protease inhibitor, what is the MOA |
|
Definition
ritonavir
inhibits protease stopping viral replication |
|
|
Term
| protease inhibitor side effects (5) |
|
Definition
central fat deposition
insulin release
hyperglycemia
P450 inhibitor - increased in infants |
|
|
Term
|
Definition
| in combination with out PI because it is an extra good P450 inhibitor |
|
|
Term
| name an integrase inhibitor |
|
Definition
|
|
Term
|
Definition
| inhibits viral genetic integration into host chromosomes |
|
|
Term
| name three anti-herpes drugs |
|
Definition
acyclovir
gencyclovir
foscarnet |
|
|
Term
|
Definition
| TK adds 1P, host adds 2P, DNA chain termination |
|
|
Term
| acyclovir side effects (4) |
|
Definition
delerium
tremor
seizure
nephrotoxicity (crystal urea, drink water) |
|
|
Term
|
Definition
| TK adds 1P, host adds 2P, DNA chain termination |
|
|
Term
|
Definition
|
|
Term
|
Definition
| stops reverse transcriptase and DNA polumerase |
|
|
Term
| fascarnet side effects (2) |
|
Definition
nephrotoxicity
altered Ca and P balance |
|
|
Term
| what two herpes drugs treat CMV |
|
Definition
|
|
Term
| name and influenza a and b drug |
|
Definition
|
|
Term
|
Definition
| neuroaminidase inhibitor that stopps viral budding |
|
|
Term
|
Definition
|
|
Term
|
Definition
| stops mycolic acid assembly |
|
|
Term
|
Definition
| peripherial neuritis (take B6 to fix) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| rifampin side effects (5) |
|
Definition
P450 inhibitor
pseudomembrane colitis
renal failure
anemia
red/orange urine |
|
|
Term
|
Definition
|
|
Term
| which antibiotics should be adjusted with renal dysfunction |
|
Definition
|
|
Term
|
Definition
| inhibit transpeptidation in cross linking |
|
|
Term
| what are the side effects of B-lactams |
|
Definition
|
|
Term
| what are the side effects of imipenem |
|
Definition
| seizures with renal dysfunction |
|
|
Term
| how can something become resistant to B-lactams |
|
Definition
| alter PBP, product B-lactaminase |
|
|
Term
| how can you avoid B-lactaminase |
|
Definition
| clavulamic acid: B lactaminase inhibitor |
|
|
Term
| which penicillin is the most B-lactaminase resistant, what group is it in |
|
Definition
|
|
Term
| which cephalosporin is the most B-lactaminase resistant, which group is it in |
|
Definition
| cephtriaxone (3 and 4th generation) |
|
|
Term
|
Definition
| binds d-alanine terminal to inhibit peptidoglycan elongation |
|
|
Term
|
Definition
| red man syndrome (upper body flushing due to histamin release and infusion too fast) |
|
|
Term
|
Definition
| altering d-alanine terminal |
|
|
Term
| tetracyclines work on what subunit |
|
Definition
|
|
Term
| what are two tetracyclines |
|
Definition
| tetracycline + docycycline |
|
|
Term
|
Definition
| unable to bind receptor site |
|
|
Term
| tetracycline side effects |
|
Definition
metals (antacids) cause chelation
concentrations in bone and teeth
phototoxicity |
|
|
Term
| aminoglycosides work on what subunit |
|
Definition
|
|
Term
| what are two aminoglycosides |
|
Definition
| doxycycline and gentamycin |
|
|
Term
|
Definition
| need O2 to get into bacteria (will never work on anaerobes) |
|
|
Term
| aminoglycocide side effects |
|
Definition
nephrotoxicity
ototoxiticy
muscle weakness due to decreased ACh release |
|
|
Term
| macrolides work on what subunit |
|
Definition
|
|
Term
| what are three macrolides |
|
Definition
| erythromycin, azithromycin, clathromycin |
|
|
Term
|
Definition
|
|
Term
|
Definition
| bind to motilin receptor increasing GI motility (used in gastroperosis in diabetics) |
|
|
Term
| what drug is an antifolate |
|
Definition
|
|
Term
|
Definition
pteridine + PABA use DHPS to make DHF
DNF uses DHFR to make THF |
|
|
Term
|
Definition
| inhibit DHPS (dihydrofolate synthase) |
|
|
Term
|
Definition
| inhibit dihydrofolate reductase (DHPR) |
|
|
Term
|
Definition
hypersensitivity, SJS
in G6PDH deficiency get hemolytic anemia
marrow supression because it stops THF causing anemia
phototoxicity |
|
|
Term
|
Definition
| ciproflaxcin and levoflaxcin |
|
|
Term
|
Definition
| inhibit topoisomerae 2 (DNA gyrase) stopping positive supercoils |
|
|
Term
| flouroquinolone side effects |
|
Definition
tendon and cartiladge: tendinitis, tears
phototoxicity |
|
|
Term
| function of flouroquinolones |
|
Definition
kill all geam negatives
levoflaxcin kills gram positive too (good for atypical pneumonia) |
|
|
Term
|
Definition
| cannot have O2 present (works on anaerobes only) |
|
|
Term
| side effects metronidazole |
|
Definition
|
|
Term
|
Definition
giardia
entomebia
trichomonas
bacterioides
clostridium
gardnerella |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| doxycyclin or azithromycin |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
pen G
if using a cephalosporin: cephalexin |
|
|
Term
|
Definition
| anti-steph penicillin (naficillin) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| tetracycline or macrolide |
|
|
Term
| what microbes cause atypical pneumonia |
|
Definition
chalmydia
mycoplasma
legionella |
|
|
Term
|
Definition
| cephtriaxone (+ampicillin for listeria) |
|
|
Term
|
Definition
|
|
Term
|
Definition
| binds ergosterol opening pores killing fungi |
|
|
Term
|
Definition
| serious systemic infection, too toxic for regular use |
|
|
Term
| amphotericin B side effects |
|
Definition
|
|
Term
| fluconazole and voraconazole MOA |
|
Definition
| inhibit 14a-demythelase stopping lenosterol conversion to ergosterol |
|
|
Term
|
Definition
routine fungal infection
less serious fungal infection
anti-fungal (candidia) |
|
|
Term
|
Definition
|
|
Term
|
Definition
| stops squaline exopidase stopping squaline conversion to squaline epoxidase |
|
|
Term
|
Definition
| dermatophic infection (tinea), oncomycosis (nails) |
|
|
Term
| terbinafine administration |
|
Definition
|
|
Term
|
Definition
| prophylaxis and tx DOC for blood schizonticide (malaria in blood) |
|
|
Term
|
Definition
| add to chloroquine for p. vivax and p. ovale because they chill in liver (tissue schizonicide) |
|
|
Term
| side effects of primaquine |
|
Definition
| in people with G6PDH deficiency causes hemolytic anemia |
|
|
