test undergraduate – 24 questions: multiple choice, fill-in and t/f – 3 problems ms – 3...
DESCRIPTION
EXTRAVASCULAR DOSE KINETICS Lecture #13TRANSCRIPT
![Page 1: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/1.jpg)
Test
• Undergraduate– 24 Questions: Multiple Choice, Fill-in and T/F– 3 Problems
• MS– 3 Questions: Multiple Choice, Fill-in and T/F– MS grade: Undergrad Part * 0.9 + MS Part
• Check out the point number per question.– Not all questions are created equally.
![Page 2: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/2.jpg)
Tips for working out problems
1. (30%) Write out the equations. Be sure to use the correct symbols from the book or my lectures.
Do not put unnecessary equations in.2. (40%) Show all your work. Each step.3. (20%) Correct answer4. (10%) Correct units with the answer
![Page 3: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/3.jpg)
EXTRAVASCULAR DOSE KINETICSLecture #13
![Page 4: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/4.jpg)
Extravascular Routes of Administration
• Enteral (GI Tract)– oral, sub-lingual, buccal, rectal
• Parenteral (injection/infusion)– Not IV or IA– IM, SC, ID
• Skin (Patch)• Lungs
– Inhalation• Vaginal (local)• Eye (local)
X
![Page 5: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/5.jpg)
Oral Dosage Forms
• Immediate release• Modified release– Extended Release– Delayed Release– Targeted Release– Oral disintegrating tablets (ODT)
Drug
Abs
orbe
dDr
ug A
bsor
bed
Drug
Abs
orbe
d
Time
Time
Time
A
B
C
![Page 6: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/6.jpg)
Kinetics of Absorption
Liver
GI Tract
AortaVena Cava
HepaticArteryHepatic
Vein
HepaticPortalVein
HepaticPortalVein
Gall Bladder
BileDuct
Heart
skinfat
ka
![Page 7: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/7.jpg)
Absorption Kinetics: First Versus ZeroFr
actio
n Dr
ug R
emai
ning
in th
e GI
Tra
ct
Not Concentration Dependent
Concentration Dependent
![Page 8: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/8.jpg)
Absorption Kinetics: First Versus ZeroFr
actio
n Dr
ug R
emai
ning
in th
e GI
Tra
ct
Cartesian Plot Semilogarithmic Plot
![Page 9: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/9.jpg)
Absorption Kinetics without EliminationGI Tract Blood Plasma
1st Order
Zero Order
![Page 10: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/10.jpg)
First Order Absorption Kinetics
Half-time of Absorption
Absorption Rate Constant
Amount being Absorbed
![Page 11: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/11.jpg)
First Order Absorption Kinetics with Elimination
1st Order
![Page 12: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/12.jpg)
Absorption Kinetics with EliminationGI Tract Blood Plasma
1st Order
Zero Order
EliminationPhase
EliminationPhase
Absorption Phase
Absorption Phase
![Page 13: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/13.jpg)
Oral vs IV
IV
Oral
![Page 14: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/14.jpg)
“Intestines”
“Blood Plasma”
“Liver”
![Page 15: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/15.jpg)
Bioavailability (F)
• Fraction of the oral dose systemic circulation
AUC = Area under the Curve ((mg*hr)/L)F = BioavailabilityAdose= Dose (mg)CL=Clearance (L/hr)
![Page 16: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/16.jpg)
Increasing Dose
AUC?Cmax?Tmax?ka?k?
Dose (A) AUC CMAX tmax ka k
increase increase increase no effect no effect no effect
decrease
decrease
decrease
no effect no effect no effect
![Page 17: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/17.jpg)
Absorption vs. Elimination
Blood Plasma
Abso
rptio
n
Elim
inati
on
![Page 18: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/18.jpg)
Absorption vs. Elimination
Blood PlasmaAbsorptionElimination
AbsorptionElimination
Blood Plasma
Elimination Rate Limiting
Absorption Rate Limiting
Confusing thing in the Book: Disposition Limited, when disposition refers to ADME according to several references.
![Page 19: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/19.jpg)
Elimination is “Rate” LimitingAbsorption >> Elimination Absorption > Elimination
Cmax
Cmax
AUC=0.42 (mg*hr)/L AUC=0.32 (mg*hr)/L
AUC (IV) = 0.48 (mg*hr)/L
ka=0.7 /hrk=0.1 /hr
ka=0.2 /hrk=0.1 /hr
![Page 20: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/20.jpg)
Absorption is “Rate” Limiting
ka=0.05 /hrk=0.1 /hr
Absorption < Elimination
AUC=0.16 (mg*hr)/L
AUC (IV)=0.48 (mg*hr)/L
Cmax Cmax
Absorption = Elimination
ka=0.1 /hrk=0.1 /hr
AUC=0.24 (mg*hr)/L
Absorption Phase?
![Page 21: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/21.jpg)
Distinguishing effects on absorption and elimination
• Strategies– Different Dosage Forms– Different Routes
![Page 22: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/22.jpg)
Absorption vs. Elimination
chronic obstructive pulmonary disease (COPD)asthma
*Similar compounds in Chocolate
500 ml water in Empty Stomach
20 ml water in Empty Stomach
20 ml water in Full Stomach
![Page 23: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/23.jpg)
Absorption vs. Elimination
oil
oil + aluminum monostearate
aqueous
![Page 24: Test Undergraduate – 24 Questions: Multiple Choice, Fill-in and T/F – 3 Problems MS – 3 Questions:…](https://reader036.vdocument.in/reader036/viewer/2022062601/5a4d1c107f8b9ab0599f66e7/html5/thumbnails/24.jpg)
Distinguishing between absorption and elimination rate limitations
Increasing ka
Increasing ka
Increasing k
Increasing k
Elimination rate constant (k) is constant Absorption rate constant (ka) is constant