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NSG |! 531 |! - |! Advanced |! Pharmacology |! - |!
Exam |! 1 |! with |! verified |! detailed |! solutions |!
– |! Rush |! university
Drug |! - |! Correct |! answer |! ✔a |! substance |! intended |! for |! use |! in |! the |! diagnosis, |! cure, |! mitigation, |! treatment, |! or |! prevention |! of |! disease |! and |! a |! substance, |! other |! than |! food, |! intended |! to |! affect |! the |! structure |! or |! any |! function |! of |! the |! body T/F |! most |! drugs |! are |! strong |! acids |! or |! strong |! bases |! - |! Correct |! answer |! ✔F |! - |! most |! drugs |! are |! weak |! acids |! or |! weak |! bases what |! are |! the |! four |! things |! that |! the |! body |! does |! to |! a |! drug? |! - |! Correct |! answer |! ✔1. |! absorbs |! it
- |! distributes |! it |! (think |! about |! it |! - |! most |! drugs |! don't |! have |! MOA |! in |! the |! stomach |! or |! GI |! tract, |! the |! body |! distributes |! to |! where |! it |! acts)
- |! biotransforms |! or |! metabolizes |! it
- |! eliminates |! it Pharmacokinetics |! - |! Correct |! answer |! ✔what |! the |! body |! does |! to |! the |! drug Describe |! absorption |! - |! Correct |! answer |! ✔drugs |! that |! are |! given |! orally |! have |! to |! get |! out |! of |! the |! gut |! and |! into |! circulation in |! order |! to |! do |! that |! the |! drugs |! have |! to |! pass |! through |! cell |! membranes
this |! means |! there |! has |! to |! be |! some |! form |! of |! solubility |! for |! the |! drug |! to |! pass |! through |! the |! cell |! membrane cell |! membranes |! are |! made |! of |! lipids therefore |! drugs |! have |! to |! have |! some |! form |! of |! lipid |! solubility What |! are |! cell |! membranes |! made |! of? |! - |! Correct |! answer |! ✔phsopholipid |! bilayer What |! is |! the |! only |! route |! of |! drug |! that |! does |! not |! have |! to |! pass |! through |! the |! cell |! membrane? |! - |! Correct |! answer |! ✔IV |! push |! - |! because |! it |! goes |! directly |! into |! circulation What |! are |! the |! four |! mechanisms |! of |! transport |! across |! the |! cell |! membrane? |! - |! Correct |! answer |! ✔1. |! simple |! diffusion
- |! channel-mediated
- |! carrier-mediated
- |! Active |! Transport Simple |! diffusion |! - |! what |! has |! to |! be |! true? |! - |! Correct |! answer |! ✔-drug |! has |! to |! be |! lipid |! soluble -there |! has |! to |! be |! a |! concentration |! gradient |! present -if |! a |! drug |! is |! high |! in |! fat |! solubility |! it |! is |! not |! going |! to |! be |! very |! water |! soluble |! - |! these |! two |! properties |! balance |! each |! other |! out If |! a |! drug |! is |! high |! in |! lipid |! solubility |! and |! it |! is |! able |! to |! be |! transported |! by |! simple |! diffusion, |! what |! will |! happen |! once |! it |! crosses |! the |! cell |! membrane? |! - |!
i.e. |! carrier-mediated |! transport |! where |! the |! protein |! accepts |! the |! drug, |! then |! flips, |! orienting |! the |! open |! side |! of |! the |! protein |! to |! the |! opposite |! side |! of |! the |! cell |! membrane what |! are |! the |! three |! types |! of |! passive |! transport |! - |! Correct |! answer |! ✔simple |! diffusion, |! channel-mediated, |! carrier-mediated Does |! a |! lipid |! soluble |! or |! water |! soluble |! drug |! get |! absorbed |! more |! quickly? |! - |! Correct |! answer |! ✔lipid |! soluble what |! does |! solubility |! of |! a |! drug |! depend |! on? |! - |! Correct |! answer |! ✔-whether |! the |! drug |! is |! an |! acid |! or |! a |! base -the |! pH |! of |! the |! environment |! in |! which |! the |! drug |! is |! located what |! does |! pH |! measure? |! - |! Correct |! answer |! ✔hydrogen |! ion |! concentration pH |! = |! -log |! (H+) what |! happens |! when |! you |! put |! an |! acidic |! drug |! in |! solution? |! - |! Correct |! answer |! ✔it |! gives |! up |! its' |! hydrogen |! ion |! and |! releases |! it |! into |! solution what |! happens |! when |! you |! put |! a |! basic |! drug |! in |! solution? |! - |! Correct |! answer |! ✔it |! accepts |! a |! hydrogen |! ion |! sitting |! in |! solution What |! is |! the |! equation |! for |! acid? |! - |! Correct |! answer |! ✔HA |! --><-- |! H+ |! + |! A-
What |! is |! the |! equation |! for |! Base? |! - |! Correct |! answer |! ✔BH+ |! --><-- |! B |! + |! H+ HA is |! this |! acid |! associated |! or |! dissociated? |! - |! Correct |! answer |! ✔associated |! - |! it |! has |! its' |! hydrogen |! ion HA is |! this |! acid |! protonated |! or |! unprotonated? |! - |! Correct |! answer |! ✔protonated |! - |! a |! hydrogen |! ion |! is |! a |! positively |! charged |! particle |! and |! the |! positively |! charged |! particle |! is |! bound |! to |! it H+ |! + |! A- is |! this |! acid |! protonated |! or |! unprotonated? |! - |! Correct |! answer |! ✔unprotonated |! - |! no |! longer |! bound |! to |! the |! hydrogen |! ion H+ |! + |! A- is |! this |! acid |! associated |! or |! dissociated? |! - |! Correct |! answer |! ✔dissociated |! - |! when |! the |! acid |! is |! dissociated |! it |! picks |! up |! a |! charge weak |! acids |! and |! weak |! bases |! are |! buffers, |! what |! does |! this |! mean? |! - |! Correct |! answer |! ✔-if |! you |! take |! a |! weak |! base |! buffer |! and |! put |! it |! in |! a |! highly |! acidic |! environment |! that |! buffer |! is |! going |! to |! pick |! up |! the |! excess |! hydrogen |! ions |! and |! try |! to |! minimize |! the |! change |! in |! pH -if |! the |! pH |! gets |! too |! alkaline |! or |! high, |! and |! you |! add |! a |! weak |! acid |! buffer, |! it |! will |! donate |! the |! hydrogen |! ion |! to |! try |! and |! minimize |! the |! change |! in |! pH
you |! add |! a |! weak |! base |! as |! a |! buffer, |! which |! direction |! is |! the |! reaction |! favored? |! - |! Correct |! answer |! ✔Favored |! to |! the |! left |! - |! base |! will |! accept |! hydrogen |! to |! neutralize |! acidic |! environment Let's |! say |! the |! pH |! of |! the |! environment |! is |! 8 you |! add |! a |! weak |! base |! as |! a |! buffer, |! which |! direction |! is |! the |! reaction |! favored? |! - |! Correct |! answer |! ✔Favored |! to |! the |! right |! - |! gives |! away |! its' |! hydrogen |! ion T/F if |! a |! drug |! is |! highly |! ionized |! it |! is |! going |! to |! be |! highly |! water |! soluble |! - |! Correct |! answer |! ✔True Water |! is |! a |! polar |! molecule |! - |! it |! has |! a |! negatively |! and |! positively |! charged |! pole imagine |! an |! unprotonated |! acid |! - |! it's |! negatively |! charged |! so |! it |! can |! form |! an |! electrical |! bond |! with |! the |! positive |! pole |! of |! water same |! with |! an |! unprotonated |! base |! - |! it |! is |! positively |! charged |! and |! can |! form |! an |! electrical |! bond |! with |! the |! negative |! pole |! of |! water If |! a |! drug |! is |! highly |! ionized |! what |! does |! this |! mean |! for |! its' |! ability |! to |! enter |! the |! cell |! membrane? |! - |! Correct |! answer |! ✔it |! will |! be |! highly |! water |! soluble |! because |! it |! bonds |! to |! water water |! does |! not |! enter |! the |! cell |! membrane drugs |! that |! are |! charged |! are |! not |! lipid |! soluble |! and |! they |! won't |! passively |! diffuse this |! means |! they |! will |! need |! channel |! mediated |! or |! carrier |! mediated
what |! type |! of |! acid |! and |! base |! will |! be |! lipid |! soluble? |! - |! Correct |! answer |! ✔an |! uncharged |! one |! that |! is |! unable |! to |! bond |! to |! water this |! would |! mean |! a |! protonated |! acid |! or |! an |! unprotonated |! base what |! is |! a |! drug's |! pKa |! - |! Correct |! answer |! ✔When |! pH |! = |! pKa, |! 50% |! of |! the |! drug |! is |! ionized |! and |! 50% |! in |! non-ionized |! form. |! Lower |! pKa |! stronger |! acid; |! Higher |! pKa |! stronger |! base. What |! do |! we |! need |! to |! know |! when |! the |! two |! sides |! of |! the |! reaction |! are |! equal? |! - |! Correct |! answer |! ✔the |! drug |! will |! see |! the |! pH |! as |! neutral no |! net |! gain |! or |! loss |! of |! hydrogen |! ion we |! need |! to |! know |! the |! drug's |! pKa Say |! you |! have |! a |! drug |! where |! pKa |! = |! 6 |! and |! the |! pH |! of |! the |! environment |! is |! 7.4. |! What |! will |! happen? |! - |! Correct |! answer |! ✔The |! drug |! will |! see |! the |! environment |! as |! basic |! so |! it |! will |! favor |! it |! to |! the |! right |! giving |! up |! its' |! hydrogen |! ion what |! does |! ALAN |! stand |! for? |! - |! Correct |! answer |! ✔Acidic |! environment |! moves |! reaction |! to Left |! and |! makes Acid Nonionized (base |! is |! opposite |! or |! ionized) HA |! --><-- |! H+ |! + |! A-
the |! pH |! in |! the |! GI |! tract |! varies |! from |! 1 |! - |! 8 How |! will |! the |! reaction |! be |! favored |! throughout |! the |! GI |! tract? |! - |! Correct |! answer |! ✔We |! know |! that |! all |! across |! the |! GI |! tract |! the |! pH<pKa acidic |! environment Use |! ALAN Favored |! to |! the |! left |! throughout However |! when |! you |! are |! in |! the |! stomach |! (more |! acidic) |! it |! will |! be |! favored |! strongly |! to |! the |! left compared |! to |! distally |! in |! the |! GI |! tract |! (closer |! to |! pH |! of |! 8) |! it |! will |! only |! sightly |! be |! favored |! to |! the |! left may |! be |! 90% |! nonionized |! form |! and |! 10% |! ionized |! form |! in |! the |! stomach |! compared |! to |! 55% |! nonionized |! form |! and |! 45% |! ionized |! form |! in |! the |! distal |! reaches |! of |! the |! gut What |! happens |! as |! you |! have |! a |! bigger |! discrepancy |! in |! pH |! and |! pKa, |! what |! will |! happen? |! - |! Correct |! answer |! ✔there |! will |! be |! a |! bigger |! difference |! in |! the |! ionized |! and |! nonionized |! sides |! of |! the |! reaction When |! is |! it |! to |! our |! advantage |! to |! make |! drugs |! less |! absorbed? |! Shifting |! the |! fraction |! of |! drug |! from |! a |! lipid |! soluble |! dominance |! to |! a |! water |! soluble |! dominance? |! - |! Correct |! answer |! ✔If |! someone |! overdoses! We |! want |! to |! change |! the |! reaction |! and |! cause |! the |! drug |! to |! be |! more |! water |! soluble |! so |! that |! the |! kidneys |! will |! excrete |! the |! drug |! instead |! of |! reabsorbing |! it |! back |! into |! the |! blood making |! a |! drug |! more |! water |! soluble |! enhances |! this |! process we |! alter |! the |! pH |! of |! the |! blood |! to |! alter |! the |! pH |! of |! the |! filtrate |! to |! favor |! the |! dominance |! of |! water |! solubility
if |! they |! OD |! on |! an |! acidic |! drug |! we |! give |! them |! a |! base |! if |! they |! OD |! on |! a |! basic |! drug |! we |! give |! them |! an |! acid What |! do |! we |! give |! when |! someone |! overdoses |! on |! aspirin |! and |! why? |! - |! Correct |! answer |! ✔we |! give |! bicarb this |! corrects |! the |! metabolic |! acidosis |! in |! the |! blood |! and |! it |! raises |! the |! pH |! in |! the |! filtrate |! to |! make |! it |! more |! basic |! in |! order |! to |! make |! the |! aspirin |! ionized |! so |! that |! it |! binds |! to |! water |! and |! is |! not |! reabsorbed |! back |! in |! the |! kidneys |! and |! is |! instead |! excreted if |! the |! pH>pKa a |! basic |! drug |! will |! exist |! in |! predominantly |! which |! form? |! - |! Correct |! answer |! ✔BRAIN moves |! to |! the |! right makes |! the |! basic |! drug |! nonionized if |! the |! pH |! > |! pKa |! an |! acidic |! drug |! will |! exist |! predominantly |! in |! which |! form? |! - |! Correct |! answer |! ✔BRAIN reaction |! to |! the |! right makes |! the |! acidic |! drug |! ionized what |! is |! the |! effect |! of |! administering |! an |! H2 |! blocker |! such |! as |! zantac |! on |! the |! absorption |! of |! ibuprofen |! a |! weak |! acid |! - |! Correct |! answer |! ✔you're |! not |! necessarily |! flipping |! the |! pH |! you |! could |! give |! on |! and |! the |! pH |! would |! still |! be |! less |! than |! the |! pKa
Describe |! the |! relationship |! of |! blood |! flow |! with |! drug |! distribution |! - |! Correct |! answer |! ✔highly |! perfused |! organs |! get |! the |! lion |! share |! of |! a |! drug the |! kidneys |! then |! for |! example |! get |! a |! lot |! of |! a |! drug cartilage |! does |! not |! it |! is |! not |! highly |! perfused |! and |! that |! is |! why |! when |! we're |! trying |! to |! treat |! something |! like |! joints |! or |! ligaments |! we |! often |! give |! injections |! straight |! to |! the |! sight the |! brain |! is |! highly |! perfused |! however |! it |! doesn't |! get |! the |! lion |! share |! because |! a |! drug |! has |! to |! be |! lipid |! soluble Describe |! the |! relationship |! between |! solubility |! and |! drug |! distribtuion |! - |! Correct |! answer |! ✔say |! that |! a |! drug |! is |! highly |! water |! soluble, |! it |! will |! do |! great |! when |! it |! gets |! through |! the |! channels |! and |! into |! the |! blood |! stream |! or |! the |! tissue say |! that |! a |! drug |! is |! highly |! lipid |! soluble, |! it |! is |! going |! to |! do |! great |! in |! the |! cell |! membrane |! but |! not |! in |! the |! blood |! or |! tissues |! because |! it |! will |! need |! a |! carrier |! transporter describe |! the |! relationship |! between |! plasma |! protein |! binding |! and |! drug |! distribution |! - |! Correct |! answer |! ✔albumin |! for |! example |! - |! it |! is |! sticky |! so |! drugs |! stick |! to |! them so |! if |! a |! drug |! sticks |! to |! albumin |! it |! gets |! stuck |! in |! the |! blood |! stream. |! plasma |! proteins |! don't |! leave |! the |! plasma the |! first |! few |! doses |! given |! are |! just |! saturating |! the |! plasma |! proteins, |! once |! they |! are |! saturated |! the |! drug |! can |! then |! leave |! the |! bloodstream drug |! that |! is |! bound |! to |! plasma |! proteins |! are |! inactive |! as |! long |! as |! they |! are |! bound |! they |! can't |! get |! to |! their |! site |! of |! action
Describe |! the |! relationship |! between |! drug |! size |! and |! drug |! distribution |! - |! Correct |! answer |! ✔large |! molecules |! cannot |! cross |! the |! cell |! membrane. |! Drugs |! are |! therefore |! generally |! small |! in |! molecule |! size What |! is |! volume |! of |! distribution? |! - |! Correct |! answer |! ✔The |! theoretical |! volume |! into |! which |! the |! drug |! disperses. |! A |! volume |! of |! distribution |! of |! around |! 7L |! indicates |! that |! the |! drug |! is |! staying |! in |! the |! blood |! compartment. |! A |! large |! volume |! of |! distribution |! indicates |! that |! the |! drug |! is |! leaving |! the |! blood |! compartment |! and |! may |! be |! bound |! to |! tissues. Used |! to |! determine |! loading |! dose ex. |! 3L |! may |! stay |! in |! the |! plasma |! which |! has |! a |! capacity |! of |! 4L |! because |! the |! plasma |! is |! large |! enough |! to |! hold |! it the |! volume |! required |! to |! contain |! a |! given |! drug |! dose |! if |! it |! were |! distributed |! equally |! throughout |! the |! body |! at |! the |! same |! concentration |! as |! in |! the |! plasma it |! is |! a |! hypothetical |! volume |! that |! doesn't |! relate |! to |! any |! real |! volume |! in |! the |! body think |! of |! VD |! as |! a |! bucket |! that |! we |! are |! putting |! the |! drug |! in Say |! we |! give |! 50 |! mg |! of |! a |! drug |! IV, |! wait |! a |! minute, |! then |! measure |! the |! plasma |! concentration |! of |! that |! drug |! and |! it |! is |! 2 |! mg/L what |! is |! the |! VD? |! - |! Correct |! answer |! ✔ 25 |! L if |! this |! drug |! distributes |! across |! the |! tissues |! at |! the |! same |! concentration |! as |! it |! does |! in |! the |! plasma |! then |! we |! need |! 25 |! L |! to |! hold |! that |! drug
What |! does |! this |! say |! about |! the |! drug |! when |! in |! cell? |! - |! Correct |! answer |! ✔when |! it |! is |! in |! the |! cell |! pH<pKa |! making |! the |! environment |! acidic |! moving |! the |! reaction |! to |! the |! left |! making |! the |! acid |! nonionized |! and |! the |! base |! ionized in |! the |! cell |! hydralazine |! is |! going |! to |! be |! more |! ionized |! than |! nonionized |! causing |! it |! to |! get |! trapped |! in |! the |! cell if |! it |! didn't |! flip |! like |! that |! it |! would |! move |! back |! out |! into |! the |! plasma |! but |! that |! is |! not |! how |! this |! drug |! works in |! the |! plasma |! it |! is |! very |! lipid |! soluble |! in |! the |! cell |! it |! is |! not Say |! we |! have |! Thiopental |! an |! acid pKa |! = |! 7. VD |! = |! 2L/kg VW |! = |! 136 |! L plasma |! pH |! = |! 7. cell |! pH |! = |! 7. Describe |! the |! reaction |! - |! Correct |! answer |! ✔plasma |! pH |! < |! pKa use |! ALAN reaction |! to |! the |! left |! making |! the |! acid |! nonionized will |! cross |! over |! into |! the |! cells cellular |! pH |! is |! less |! than |! pKa once |! the |! concentration |! gradient |! is |! flipped |! the |! drug |! is |! going |! to |! move |! out |! which |! means |! that |! this |! must |! be |! a |! short |! acting |! drug
what |! are |! the |! three |! key |! reasons |! VD |! is |! so |! important? |! - |! Correct |! answer |! ✔1. |! it |! tells |! us |! where |! the |! drug |! distributes
- |! it's |! related |! to |! elimination |! - |! higher |! VD |! = |! longer |! time |! to |! eliminate |! the |! drug |! because |! the |! drug |! is |! outside |! of |! the |! plasma |! and |! therefore |! can't |! be |! circulated |! to |! liver |! and |! kidneys |! for |! excretion
- |! It's |! necessary |! to |! calculate |! the |! loading |! dose |! of |! a |! drug association |! constant |! (Ka) |! - |! Correct |! answer |! ✔the |! inverse |! of |! the |! dissociation |! constant |! - |! tells |! us |! the |! affinity |! for |! plasma |! protein |! receptors drugs |! that |! are |! very |! highly |! bound |! to |! proteins |! are |! going |! to |! be |! favored |! to |! the |! left dissociation |! constant |! (Kd) |! - |! Correct |! answer |! ✔the |! inverse |! of |! the |! association |! constant |! - |! tells |! us |! the |! affinity |! for |! plasma |! protein |! receptors drugs |! that |! don't |! have |! a |! very |! high |! affinity |! are |! going |! to |! be |! favored |! to |! the |! right k1 |! - |! Correct |! answer |! ✔the |! rate |! of |! the |! reaction |! that |! favors |! the |! drug |! binding |! to |! the |! plasma |! protein k2 |! - |! Correct |! answer |! ✔the |! rate |! of |! the |! reaction |! that |! favors |! the |! drug |! dissociating |! from |! the |! plasma |! protein Ka |! - |! Correct |! answer |! ✔k1/k
c. |! drug's |! therapeutic |! index |! - |! if |! ratio |! between |! therapeutic |! and |! toxic |! doses |! is |! low, |! displacement |! may |! be |! important t/f Kd |! is |! positively |! associated |! with |! free |! drug |! in |! the |! plasma |! - |! Correct |! answer |! ✔true what |! might |! decreased |! free |! drug |! in |! the |! plasma |! mean? |! - |! Correct |! answer |! ✔an |! increase |! in |! plasma |! albumin |! concentration what |! might |! increased |! total |! drug |! concentration |! mean? |! - |! Correct |! answer |! ✔increased |! free |! drug |! in |! the |! plasma |! when |! the |! protein |! binding |! sites |! are |! saturated Biotransformation |! - |! Correct |! answer |! ✔One |! or |! more |! biochemical |! reactions |! involving |! a |! parent |! drug; |! occurs |! mainly |! in |! the |! liver |! and |! produces |! a |! metabolite |! that |! is |! either |! inactive |! or |! active. |! Also |! known |! as |! metabolism. what |! is |! the |! relationship |! between |! biotransformation |! reactions |! in |! the |! body |! and |! the |! solubility |! of |! the |! drug? |! - |! Correct |! answer |! ✔makes |! the |! drug |! more |! water |! soluble |! so |! that |! we |! can |! get |! rid |! of |! it because |! the |! body |! does |! something |! to |! the |! drug |! to |! change |! them |! that |! is |! why |! we |! have |! to |! keep |! giving |! it |! because |! the |! body |! is |! always |! trying |! to |! get |! rid |! of |! something |! that |! is |! not |! self
How |! come |! drugs |! don't |! initiate |! an |! immune |! reaction? |! - |! Correct |! answer |! ✔In |! order |! for |! something |! to |! stimulate |! an |! immune |! response |! they |! have |! to |! be |! somewhat |! large |! and |! drugs |! by |! design |! are |! somewhat |! small What |! are |! the |! two |! major |! routes |! by |! which |! drugs |! are |! eliminated? |! - |! Correct |! answer |! ✔Liver |! - |! makes |! it |! water |! soluble Kidneys |! - |! get |! rid |! of |! it How |! does |! the |! liver |! prepare |! drugs |! for |! excretion? |! - |! Correct |! answer |! ✔by |! making |! them |! more |! water |! soluble |! and |! generally |! by |! making |! them |! more |! polar if |! they |! are |! more |! polar |! what |! happens |! when |! they |! are |! filtered |! into |! the |! kidneys |! is |! that |! they |! bind |! to |! water |! and |! get |! excreted |! in |! the |! urine |! and |! don't |! get |! filtered |! back |! into |! the |! systemic |! sirculation phase |! I |! reactions |! - |! Correct |! answer |! ✔mediated |! by |! enzymes |! in |! the |! liver at |! the |! end |! of |! this |! reaction |! the |! substance |! is |! more |! polar the |! major |! reaction |! that |! occurs |! in |! a |! phase |! I |! reaction |! is |! oxidation What |! are |! the |! family |! of |! enzymes |! that |! mediate |! phase |! I |! reactions |! in |! the |! liver? |! - |! Correct |! answer |! ✔cytochrome |! p450 |! enzymes their |! sole |! purpose |! is |! to |! get |! rid |! of |! something |! that |! we |! didn't |! mean |! to |! consume evolutionarily |! speaking |! this |! might |! be |! poisonous |! berries |! for |! example what |! is |! the |! major |! reaction |! that |! occurs |! in |! a |! phase |! I |! reaction? |! - |! Correct |! answer |! ✔oxidation
