Review of Knowledge (ROK): Pharmacology NR291
I I I I I
Course NR293
Exam Exam 1: Week 3 (Chapters on Exam 1 are: 2, 38, 39, 40, 42, 10, 12, 14, 16, & 44)
I I I I I I I I I I I I I I I I I I I
Purpose
The IReview Iof IKnowledge I(ROK) Ifocuses Ion Icourse Ioutcomes, Iunit Ioutcomes Iand Ikey Iconcepts Ito Ienhance Istudent Isuccess
Ion Iexams. IUse Ithis Idocument Ias Ia Ifocused Iguide Ifor Istudy Iin Iconjunction Iwith Iassigned Ireadings, IPowerPoint
Ipresentations, Iand Iother Icourse Iresources. ISupplement Ithis Idocument Iby Ioutlining Iyour Iown Inotes Ifrom Ithe Itextbook
Ichapters Iand Iplace Iyour Iexpanded Imore Idetailed Inotes Iin Ithe IStudent INotes Icolumn. IThis Idocument Ishould INOT Ibe Iused
Ias Ia Isubstitute Ifor Icompleting Ithe Iassigned Ireadings.
Key Concepts
I Chapters Student Notes I
Pharmacologic Chapter I2
IPrinciples
Identify I the I 4 I phases I of I pharmacokinetics, I and I explain I briefly I what I occurs I in I each I phase.
1. Absorption I (p. I 22-25)
2. Distribution I (p.26)
3. Metabolism I (p.27)
4. Excretion I(p. I 27-28)
The I half-life I of I a Idrug Iis I the I time I required Ifor I one-half I (50%) I of I a I given I drug Ito I be I removed I from I the I body.
IIt Iis Ia I measure Iof Ithe Irate I at I which Ithe I drug Iis Ieliminated Ifrom Ithe Ibody. I For Iinstance, Iif Ithe I peak Ilevel Iof I a
Iparticular Idrug Iis I100 I mg/L I & Ithe I measured Idrug Ilevel Iis I 50 I mg/L Iin I 8 Ihours, Ithen Ithe I estimated Ihalf-life Iof
Ithat Idrug Iis I8 Ihours. I(Lilley, ICollins, I& ISnyder, I2014, Ip. I28)
Fill Iin Ithe Iboxes:
Half- Ilife Iis I3 3 Ihours 6 Ihours 9 Ihours 12 Ihours
hours
Drug IX Idose I200 100 50 25 12.5
mg
Drug IX Idose I500 250 125 62.5 31.25
mg
Route I of I Administration: I The I parenteral I route I is I the I fastest I route I by I which I a I drug I can I be I absorbed,
Ifollowed Iby Ithe I enteral I and Itopical Iroutes. I Parenteral I is Ia Igeneral Iterm I meaning I any Iroute I of I administration
Iother Ithan Ithe IGI Itract. IIt Imost Icommonly Irefers Ito Iinjection. IIntravenous Iinjection Idelivers Ithe Idrug Idirectly
,into Ithe Icirculation, Iwhere Iit Iis Idistributed Iwith Ithe Iblood Ithroughout Ithe Ibody. I Drugs Igiven Iby Iintramuscular
Iinjection Iand Isubcutaneous Iinjection I are I absorbed I more I slowly Ithan Ithose I given Iintravenously.
ROUTE Examples Iof IFormulations
Enteral Tablets, Icapsules, Ioral Isoluble Iwafers, Ipills, Itimed-release Icapsules, Itimed-release Itablets,
elixirs, I suspensions, I syrups, I emulsions, I solutions, I lozenges I or I troches, I rectal I suppositories,
Isublingual Ior Ibuccal Itablets
Parente Injectable I forms, I solutions, I suspensions, I emulsions, I powders I for I reconstitution
Iral
Topical Aerosols, I ointments, I creams, I pastes, Ipowders, I solutions, I foams, I gels, I transdermal I patches,
Iinhalers, Irectal Iand Ivaginal Isuppositories
Why I can’t I extended I release I or I enteric I coated I oral I medications I be I crushed? I “could I cause I accelerated
Irelease Iof Idrug Ifrom Ithe Idosage Iform Iand Ipossible Itoxicity” I(Lilley Iet Ial., Ip. I21)
How Ican Iyou Ihelp Ia Iclient Iwho Ihas Iswallowing Idifficulties Itake Itheir Ioral Imedication? I“The Iability Ito Icrush I a
Itablet Ior I open I a I capsule I can I facilitate I drug I administration I when I patients I are I unable I or I unwilling I to Iswallow I a
Itablet I or I capsule I and I also I when I medications I need I to I be I given I through I an I enteral I feeding I tube. I Capsules,
Ipowder, I or I liquid I contents I can I often I be I added I to I soft I foods I such I as I applesauce I or I pudding, I or I dissolved I in I a
Ibeverage. I Granules I contained I in I capsules I are I usually I for I extended I drug I release I and I normally I should I not I be
Icrushed Ior I chewed I by I the I patient. I However, I they I can I often I be I swallowed I when Isprinkled Ion Ione I of I the I soft
Ifoods. IConsultation Iwith Ia Ipharmacist, Ireading Ithe I product Iliterature, Ior Iuse Iof Iother Isuitable Isource Iis
Inecessary I if I any I question I exists I as I to I whether I a I drug I can I be I crushed Ior I mixed I with I specific I food Ior
Ibeverages”. I(Lilley, Iet Ial. Ipg I21)
First IPass IEffect: I“A Idrug Ithat Iis Iabsorbed Ifrom Ithe Iintestine I Imust I Ifirst I Ipass I Ithrough I Ithe I IliverIbefore
I it Ireaches I the I systemic I circulation. I If I a Ilarge I proportion Iof I a I drug Iis I chemically Ichanged Iinto Iinactive
Imetabolites Iin Ithe Iliver, I then I a I much Ismaller I amount Iof I drug I will I pass Iinto Ithe I circulation I(i.e., I will Ibe
Ibioavailable). ISuch Ia Idrug Iis Isaid Ito Ihave Ia Ihigh Ifirst-pass Ieffect I(e.g., Ioral Initrates)” I(Lilly Ip. I22).
First-Pass IRoutes: IList Iroutes Ithat Iwould Ibe Iconsidered Ifirst-pass.
1. ISEE IBOX I2-2, IPAGE I25
I2.
3.
4.
Non–First-Pass IRoutes: IList Iroutes Ithat Iwould Ibe Iconsidered Ifirst-pass.
1. I SEE IBOX I2-2, IPAGE I25
I2.
3.
4.
5.
6.
Put Ithe Ifollowing Ienteral Iroutes Iin Iorder Iof IFastest Ito ISlowest Iabsorption:
Tablet Buccal/sublingual Itablets Enteric Icoated Itablet Liquids, Ielixirs, I&
Isyrups
1
, 1. IBuccal/sublingual Itablets 2. I Liquids, Ielixirs, I& Isyrups 3. I Tablet 4. IEnteric Icoated Itablet
Put Ithe Ifollowing Iparenteral Iroutes Iin Iorder Iof IFastest Ito ISlowest Iabsorption:
I
Intramuscular Iinjection Subcutaneous I injection Intravenous
1. Intravenous 2. IIntramuscular Iinjection 3. I I Subcutaneous I injection
What Iis Ian Iagonist Iversus Ian Iantagonist? IAgonist: IA Idrug Ithat Ibinds Ito Iand Istimulates Ithe Iactivity Iof Ione Ior
Imore Ireceptors Iin Ithe Ibody. I(p. I30); IAntagonist: IA Idrug Ithat Ibinds Ito Iand Iinhibits Ithe Iactivity Iof Ione Ior Imore Ireceptors IinIthe
Ibody. IAntagonists Iare Ialso Icalled Iinhibitors. I(p. I30)
Matching:
a. IPrototype Idrug 1. I_l I I I I ILength Iof Itime Ithe Iconcentration Iof Ia Idrug Iin Ithe Iblood/tissues Iis Iable Ito Ielicit Ia
response
b. I Drug I nomenclature 2. I _a I I I First Iform Iof Ia Idrug Iin Ia Iclass
c. I Drug I classifications 3. I_h_ IBiochemical Ialteration Iof Ia Idrug Iinto Iinactive Ior Iactive Imetabolite: Ioccurs
after I distribution
d. IPharmacotherapeutics I I I 4. I_b_ IRefers Ito Ia Idrug’s Iname
e. I Pharmacodynamics 5. I_i_ I Elimination Iof Idrugs Ifrom Ithe Ibody.
f. IAbsorption 6. I_k I I I I I Maximum I concentration I of I a I drug I in I the I body
g. IDistribution 7. I_c I I I Class I or I chemical I name I of I a I drug
h. I Metabolism 8. I_g I I I Transport Iof Idrug Iby Ithe Ibloodstream Ito Iits Isite Iof Iaction
i. IExcretion 9. I_j I I I ITime Irequired Ifor Ia Idrug Ito Ielicit Ia Itherapeutic Iresponse Iafter Idosing
j. IOnset Iof Iaction 10. I_d_ I Clinical I use I of I drugs Ito I prevent I and Itreat Idiseases
K. IPeak Ilevel 11. I_e_ I The Istudy Iof Iwhat Ithe Idrug Idoes Ito Ithe Ibody.
l. IDuration 12. I _m_ I The I study I of I the I what I the I body I does I to I the I drug
m. I Pharmacokinetics 13. I f_Movement Iof Idrug Ifrom Isite Iof Iadministration Iinto I bloodstream Ifor
distribution Ito I tissues
n. ITherapeutic Ieffect 14. I_n_ I Desired Ior Iintended Ieffect Iof Ia Iparticular Imedication
0. ITrough ILevel 15. Io ILowest Iconcentration Iof Imedication Iwithin Ithe Ibody Iafter Iit Iis Ireduced Ifrom
Ithe Ipeak Ilevel
The I organ I that I is I most I responsible I for I drug I metabolism I is: I I I Liver I (p I 27)
List I other I routes I of I metabolism: I muscle, I kidneys, I lungs, I plasma, I and I intestinal I mucosa.
The Iorgan Ithat Iis Imost Iresponsible Ifor I drug Ielimination I(excretion) Iis: I Kidney I(p I27)
I
List Iother Iroutes Iof Ielimination I(excretion): Iliver Iand Ithe Ibowel
“Metabolism I is I also I referred I to I as I biotransformation. I It I involves I the I biochemical I alteration Iof I a I drug Iinto
I an I inactive I metabolite, Ia Imore Isoluble I compound, Ia Imore I potent I active I metabolite I(as Iin Ithe I conversion Iof
Ian Iinactive I prodrug Ito Iits I active Iform), I or I a Iless I active Imetabolite. I Hepatic I metabolism Iinvolves Ithe I activity
Iof I a I very I large I class I of I enzymes I known I as I cytochrome I P-450 I enzymes I (or I simply I P-450 I enzymes), I also
Iknown Ias Imicrosomal Ienzymes” I(Lilley Ip I27).
“A Ireceptor: I can Ibe Idefined Ias Ia Ireactive Isite Ion Ithe Isurface Ior Iinside Iof Ia Icell” I(Lilley, Ip I30).
“Enzymes: I the I substance I that I catalyze I nearly I every I biochemical I reaction I in I a I cell. I Drugs I produce I effects
by Iinteracting Iwith Ithese Ienzyme Isystems” I(Lilley, Ip I30).
I
Matching: I Pharmacotherapeutics
2
I I I I I
Course NR293
Exam Exam 1: Week 3 (Chapters on Exam 1 are: 2, 38, 39, 40, 42, 10, 12, 14, 16, & 44)
I I I I I I I I I I I I I I I I I I I
Purpose
The IReview Iof IKnowledge I(ROK) Ifocuses Ion Icourse Ioutcomes, Iunit Ioutcomes Iand Ikey Iconcepts Ito Ienhance Istudent Isuccess
Ion Iexams. IUse Ithis Idocument Ias Ia Ifocused Iguide Ifor Istudy Iin Iconjunction Iwith Iassigned Ireadings, IPowerPoint
Ipresentations, Iand Iother Icourse Iresources. ISupplement Ithis Idocument Iby Ioutlining Iyour Iown Inotes Ifrom Ithe Itextbook
Ichapters Iand Iplace Iyour Iexpanded Imore Idetailed Inotes Iin Ithe IStudent INotes Icolumn. IThis Idocument Ishould INOT Ibe Iused
Ias Ia Isubstitute Ifor Icompleting Ithe Iassigned Ireadings.
Key Concepts
I Chapters Student Notes I
Pharmacologic Chapter I2
IPrinciples
Identify I the I 4 I phases I of I pharmacokinetics, I and I explain I briefly I what I occurs I in I each I phase.
1. Absorption I (p. I 22-25)
2. Distribution I (p.26)
3. Metabolism I (p.27)
4. Excretion I(p. I 27-28)
The I half-life I of I a Idrug Iis I the I time I required Ifor I one-half I (50%) I of I a I given I drug Ito I be I removed I from I the I body.
IIt Iis Ia I measure Iof Ithe Irate I at I which Ithe I drug Iis Ieliminated Ifrom Ithe Ibody. I For Iinstance, Iif Ithe I peak Ilevel Iof I a
Iparticular Idrug Iis I100 I mg/L I & Ithe I measured Idrug Ilevel Iis I 50 I mg/L Iin I 8 Ihours, Ithen Ithe I estimated Ihalf-life Iof
Ithat Idrug Iis I8 Ihours. I(Lilley, ICollins, I& ISnyder, I2014, Ip. I28)
Fill Iin Ithe Iboxes:
Half- Ilife Iis I3 3 Ihours 6 Ihours 9 Ihours 12 Ihours
hours
Drug IX Idose I200 100 50 25 12.5
mg
Drug IX Idose I500 250 125 62.5 31.25
mg
Route I of I Administration: I The I parenteral I route I is I the I fastest I route I by I which I a I drug I can I be I absorbed,
Ifollowed Iby Ithe I enteral I and Itopical Iroutes. I Parenteral I is Ia Igeneral Iterm I meaning I any Iroute I of I administration
Iother Ithan Ithe IGI Itract. IIt Imost Icommonly Irefers Ito Iinjection. IIntravenous Iinjection Idelivers Ithe Idrug Idirectly
,into Ithe Icirculation, Iwhere Iit Iis Idistributed Iwith Ithe Iblood Ithroughout Ithe Ibody. I Drugs Igiven Iby Iintramuscular
Iinjection Iand Isubcutaneous Iinjection I are I absorbed I more I slowly Ithan Ithose I given Iintravenously.
ROUTE Examples Iof IFormulations
Enteral Tablets, Icapsules, Ioral Isoluble Iwafers, Ipills, Itimed-release Icapsules, Itimed-release Itablets,
elixirs, I suspensions, I syrups, I emulsions, I solutions, I lozenges I or I troches, I rectal I suppositories,
Isublingual Ior Ibuccal Itablets
Parente Injectable I forms, I solutions, I suspensions, I emulsions, I powders I for I reconstitution
Iral
Topical Aerosols, I ointments, I creams, I pastes, Ipowders, I solutions, I foams, I gels, I transdermal I patches,
Iinhalers, Irectal Iand Ivaginal Isuppositories
Why I can’t I extended I release I or I enteric I coated I oral I medications I be I crushed? I “could I cause I accelerated
Irelease Iof Idrug Ifrom Ithe Idosage Iform Iand Ipossible Itoxicity” I(Lilley Iet Ial., Ip. I21)
How Ican Iyou Ihelp Ia Iclient Iwho Ihas Iswallowing Idifficulties Itake Itheir Ioral Imedication? I“The Iability Ito Icrush I a
Itablet Ior I open I a I capsule I can I facilitate I drug I administration I when I patients I are I unable I or I unwilling I to Iswallow I a
Itablet I or I capsule I and I also I when I medications I need I to I be I given I through I an I enteral I feeding I tube. I Capsules,
Ipowder, I or I liquid I contents I can I often I be I added I to I soft I foods I such I as I applesauce I or I pudding, I or I dissolved I in I a
Ibeverage. I Granules I contained I in I capsules I are I usually I for I extended I drug I release I and I normally I should I not I be
Icrushed Ior I chewed I by I the I patient. I However, I they I can I often I be I swallowed I when Isprinkled Ion Ione I of I the I soft
Ifoods. IConsultation Iwith Ia Ipharmacist, Ireading Ithe I product Iliterature, Ior Iuse Iof Iother Isuitable Isource Iis
Inecessary I if I any I question I exists I as I to I whether I a I drug I can I be I crushed Ior I mixed I with I specific I food Ior
Ibeverages”. I(Lilley, Iet Ial. Ipg I21)
First IPass IEffect: I“A Idrug Ithat Iis Iabsorbed Ifrom Ithe Iintestine I Imust I Ifirst I Ipass I Ithrough I Ithe I IliverIbefore
I it Ireaches I the I systemic I circulation. I If I a Ilarge I proportion Iof I a I drug Iis I chemically Ichanged Iinto Iinactive
Imetabolites Iin Ithe Iliver, I then I a I much Ismaller I amount Iof I drug I will I pass Iinto Ithe I circulation I(i.e., I will Ibe
Ibioavailable). ISuch Ia Idrug Iis Isaid Ito Ihave Ia Ihigh Ifirst-pass Ieffect I(e.g., Ioral Initrates)” I(Lilly Ip. I22).
First-Pass IRoutes: IList Iroutes Ithat Iwould Ibe Iconsidered Ifirst-pass.
1. ISEE IBOX I2-2, IPAGE I25
I2.
3.
4.
Non–First-Pass IRoutes: IList Iroutes Ithat Iwould Ibe Iconsidered Ifirst-pass.
1. I SEE IBOX I2-2, IPAGE I25
I2.
3.
4.
5.
6.
Put Ithe Ifollowing Ienteral Iroutes Iin Iorder Iof IFastest Ito ISlowest Iabsorption:
Tablet Buccal/sublingual Itablets Enteric Icoated Itablet Liquids, Ielixirs, I&
Isyrups
1
, 1. IBuccal/sublingual Itablets 2. I Liquids, Ielixirs, I& Isyrups 3. I Tablet 4. IEnteric Icoated Itablet
Put Ithe Ifollowing Iparenteral Iroutes Iin Iorder Iof IFastest Ito ISlowest Iabsorption:
I
Intramuscular Iinjection Subcutaneous I injection Intravenous
1. Intravenous 2. IIntramuscular Iinjection 3. I I Subcutaneous I injection
What Iis Ian Iagonist Iversus Ian Iantagonist? IAgonist: IA Idrug Ithat Ibinds Ito Iand Istimulates Ithe Iactivity Iof Ione Ior
Imore Ireceptors Iin Ithe Ibody. I(p. I30); IAntagonist: IA Idrug Ithat Ibinds Ito Iand Iinhibits Ithe Iactivity Iof Ione Ior Imore Ireceptors IinIthe
Ibody. IAntagonists Iare Ialso Icalled Iinhibitors. I(p. I30)
Matching:
a. IPrototype Idrug 1. I_l I I I I ILength Iof Itime Ithe Iconcentration Iof Ia Idrug Iin Ithe Iblood/tissues Iis Iable Ito Ielicit Ia
response
b. I Drug I nomenclature 2. I _a I I I First Iform Iof Ia Idrug Iin Ia Iclass
c. I Drug I classifications 3. I_h_ IBiochemical Ialteration Iof Ia Idrug Iinto Iinactive Ior Iactive Imetabolite: Ioccurs
after I distribution
d. IPharmacotherapeutics I I I 4. I_b_ IRefers Ito Ia Idrug’s Iname
e. I Pharmacodynamics 5. I_i_ I Elimination Iof Idrugs Ifrom Ithe Ibody.
f. IAbsorption 6. I_k I I I I I Maximum I concentration I of I a I drug I in I the I body
g. IDistribution 7. I_c I I I Class I or I chemical I name I of I a I drug
h. I Metabolism 8. I_g I I I Transport Iof Idrug Iby Ithe Ibloodstream Ito Iits Isite Iof Iaction
i. IExcretion 9. I_j I I I ITime Irequired Ifor Ia Idrug Ito Ielicit Ia Itherapeutic Iresponse Iafter Idosing
j. IOnset Iof Iaction 10. I_d_ I Clinical I use I of I drugs Ito I prevent I and Itreat Idiseases
K. IPeak Ilevel 11. I_e_ I The Istudy Iof Iwhat Ithe Idrug Idoes Ito Ithe Ibody.
l. IDuration 12. I _m_ I The I study I of I the I what I the I body I does I to I the I drug
m. I Pharmacokinetics 13. I f_Movement Iof Idrug Ifrom Isite Iof Iadministration Iinto I bloodstream Ifor
distribution Ito I tissues
n. ITherapeutic Ieffect 14. I_n_ I Desired Ior Iintended Ieffect Iof Ia Iparticular Imedication
0. ITrough ILevel 15. Io ILowest Iconcentration Iof Imedication Iwithin Ithe Ibody Iafter Iit Iis Ireduced Ifrom
Ithe Ipeak Ilevel
The I organ I that I is I most I responsible I for I drug I metabolism I is: I I I Liver I (p I 27)
List I other I routes I of I metabolism: I muscle, I kidneys, I lungs, I plasma, I and I intestinal I mucosa.
The Iorgan Ithat Iis Imost Iresponsible Ifor I drug Ielimination I(excretion) Iis: I Kidney I(p I27)
I
List Iother Iroutes Iof Ielimination I(excretion): Iliver Iand Ithe Ibowel
“Metabolism I is I also I referred I to I as I biotransformation. I It I involves I the I biochemical I alteration Iof I a I drug Iinto
I an I inactive I metabolite, Ia Imore Isoluble I compound, Ia Imore I potent I active I metabolite I(as Iin Ithe I conversion Iof
Ian Iinactive I prodrug Ito Iits I active Iform), I or I a Iless I active Imetabolite. I Hepatic I metabolism Iinvolves Ithe I activity
Iof I a I very I large I class I of I enzymes I known I as I cytochrome I P-450 I enzymes I (or I simply I P-450 I enzymes), I also
Iknown Ias Imicrosomal Ienzymes” I(Lilley Ip I27).
“A Ireceptor: I can Ibe Idefined Ias Ia Ireactive Isite Ion Ithe Isurface Ior Iinside Iof Ia Icell” I(Lilley, Ip I30).
“Enzymes: I the I substance I that I catalyze I nearly I every I biochemical I reaction I in I a I cell. I Drugs I produce I effects
by Iinteracting Iwith Ithese Ienzyme Isystems” I(Lilley, Ip I30).
I
Matching: I Pharmacotherapeutics
2
