Review Flashcards

1
Q

P-glycoprotein

A

Efflux transporter

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2
Q

ABC

A

Efflux transporter (Active Transport)
- Found on apical membrane
- Found along Brush Border Membrane

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3
Q

SLC

A

Influx transporters (Facilitated Transport)
- Found along basolateral membrane (faces blood)
- Found along Sinusoidal Space

Ex. OAT, GLUT, SGLT2

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4
Q

Transporters
- Highest concentration in liver and kidney

A
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5
Q

Tumour cells have increased P-gp resulting increased efflux of drugs
- Need to inhibit P-gp to have drug effect

A
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6
Q

Total Clearance

A

Renal Liver and Other

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7
Q

Rate of elimination

A

Rate of renal elimination + Rate of liver metabolism + other

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8
Q

Cheapatic

A

Hepatic Clearance

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9
Q

Clint

A

Clearance of both bound and unbound drug

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10
Q

Clint’

A

Clearance of unbound drug

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11
Q

Order of Vd

A

In multi-compartment model

Vbeta > Vss > Vc > Vplasma

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12
Q

What body organ has the highest perfusion rate

A

Kidneys
- Liver, Heart, Brain

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13
Q

What body organ has the lowest perfusion rate

A

Bone, Muscle, Skin

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14
Q

Intrinsic Tissue Permeabulity

A

Dependent on physiochemical properties
- LogP
- Molecular size
- Pka

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15
Q

How to monitor renal clearance

A

Creatinine Clearance

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16
Q

How to monitor hepatic clearance

A

Liver Function Tests

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17
Q

How to know if drug is High E or Low E

A

CLhepatic / Qhepatic

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18
Q

Non-Linear Kinetics
- Vmax

A

Affected by inhibitors and inducers
Non-competitive

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19
Q

Non-Linear Kinetics
- Km

A

Affected by displacement
Competitive

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20
Q

Renal Clearance Table
- Clrenal = Clcr

A

Glomerular Filtration

20
Q

Renal Clearance Table
- Clrenal < Clcr

A

Reabsorption

20
Q

Renal Clearance Table
- Clrenal > Clcr

21
Q

Low E Drug
- CLh Dependency

22
Q

High E Drug
- CLh Dependency

23
Moderate E Drug - CLh Dependency
Q + Clint'
24
What is Vd beta
Represents Elimination + Central + Peripheral + Transfer between Central/Peripheral
25
What is Vd steady state
Represents Central + Peripheral + Transfer between Central/Peripheral
26
What is Vc
Represents the volume in central compartment
27
What is Vplasma
Represents the volume of the plasma
28
Exogenous
NSAIDS kick off warfarin Phenytoin kicks off valproic
29
Endogenous
Uremia kicks off phenytoin
30
High Vd drugs favour tissues
31
Low Vd drugs favour plasma proteins
32
25% of cardiact output is to the kidneys
33
Anatomy of Kidney
Urine Space Capillary Basement Membrane Mesangium(Smooth muscle contraction of glomerulus) - Has phagocytes Bowman's capsule Macula Densa Proximal Tubular
34
Anatomy of Kidney Basement Membrane
Slit Diaphragm Glycosialo Protein Coat - Keeps charged particles out Foot Process/podocytes Solute Fenestra - Allows for filtration Epithelial Cells
35
Capillary in Bowmans Capsule has 3x the pressure of normal capillary
36
Normal GFR in healthy patient
120-125 mL/min
37
0.9 Fraction Bound 0.1 Fraction Unbound
38
Adujusted Body Weight Formula
IBW + 0.4 * (ABW - IBW)
39
Drug Drug Interactions
Same drug can kick off the same drug - Probability of interaction is high
40
Ionized vs Uniuonized
Ionized drugs are excreted Unionized drugs are reabsorbed
41
Liver Anatomy
Mesenteric Circulation - Drug goes from gut lumen into the liver Portal Vein - Drug that is carried from gut Hepatic Artery - Drug that is carreied into the liver from systemic Hepatic Vein - Carries drug to rest of the body Metabolism and Bilary Excretion
42
Portal Vein - intro lobules Hepatic Artery - into lobule Bile duct - from lobule Hepatic Vein and Inferior Vena Cava - From liver
43
Sinusoidal Space Kupffer Cells Hepatocytes Space of Disse Canalicular Space
44
Average Q in healthy adult in a 70 kg man
1500 mL/min
45
80% of blood is form portal vein 20% is from hepatic artery/
46
Zero Order
High Dose/Concentration Always saturated Not concentration dependent
47
First Order
Low Dose/Concentrations Concentrations are well below saturation Concentration dependent