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 |
|
|