Font size
WorksheetsEnteral Dosage and Drug Absorption
Total questions: 78
Worksheet time: 43mins
Not all Enteral drugs are intended to be absorbed. Some medications are intended to act _______ in the GI tract
locally
Enteral Dosages
Dissolution and absorption rate is reached at 100% within 0 time
Solutions
Suspensions
ODTs
Tablets
Enteral Dosage
Dissolution and absorption rate is slowest in
Tablets
Solutions
Suspensions
ODTs
Enteral Dosage
Stability of drug is highest in
Tablets
Powders
Suspensions
Solutions
______ is the most common ingredients that are used to compound dosage forms
Powders
Solutions
Granules
IR tablets
The smaller the particle size, the more surface area available for ______ API dissolution
Faster
Slower
What is the main downside to divided powder medications?
Slow onset
Slow disintegration step
Decreased compliance
Tasty
Compressed tablets include the (drug + ______) to form
What is the purpose for compressed tablets to have a sugar coat on them?
To improve taste of the tablet.
To protect from moisture, light, or air.
What is the purpose of enteric coated tablets?
Dose dumping or the abrupt release of a large amount of drug can be a problem. Why?
What is the purpose of extended-release tablets
What is the purpose delayed-release tablets
Bioavailability from encapsulated drugs may be better than _______
Why are ODTs ideal for lower dose drugs?
What drugs cannot be crushed
Delayed release
Extended release
Immediate release
Biphosphonates
Solutions have _____ API stability
Poor
Great
What functional groups donate a proton?
Carboxylic acid
Imides
Amines
Phenols
Guanidines
Acidic groups at normal pH levels (7.4) tend to _____ a - charged ion called an anion. Anions tend to be more ________
Leave behind/hydrophilic
Leave behind/lipophilic
Accept/hydrophilic
Accept/lipophilic
Basic group at normal pH (7.4) tend to _____ a proton called a cation. Cations are more _________
Accept/lipophilic
Accept/hydrophilic
Donate/lipophilic
Donate/hydrophilic
Amines are really important for solubility and absorption. Why?
Amines can be ionized or non-ionized based on pH level. This can change how the drug is absorbed and where
Amines at higher pH tend to be _______ and thus more ________
Ionized/lipophilic
Non-ionized/lipophilic
Non-ionized/hydrophilic
Ionized/hydrophilic
Amines at lower pH tend to be ______ thus more _______
Ionized/lipophilic
Ionized/hydrophilic
Non-ionized/lipophilic
Non-ionized/hydrophilic
Which functional group giving that it does NOT ionize increases log P while increasing lipophilicity and decreasing water solubility?
Nonpolar
Polar
Which group given that it does NOT ionize lowers log P and decreases lipophilicity?
Polar
Nonpolar
What category of functional group do the following resemble?
Alkanes
Alkenes
Alkynes
Aramatic
Halogenated
Hydrocarbons
Non-polar, Non-ionized
Non-polar, Ionized
Polar, Non-ionized
Polar, Ionized
What functional group does the following describe?
Alcohols
Ethers
Ketone/Aldehyde
Sugars
Esters
Amides
Non-polar, Non-ionized
Non-polar, Ionized
Polar, Non-ionized
Polar, Ionized
Which functional group does the following describe?
Phenols
Imides
Imines
Sulfo
Aromatic amines
Non-polar, Non-ionized
Non-Polar, Ionized
Polar, Low ionized
Polar, Highly ionized
Which functional group does the following describe?
Carboxylic acid
Amino acid
Enols
Guanidines
Imidazole
Non-polar, Non-ionized
Non-polar, Ionized
Polar, Low ionized
Polar, Highly ionized
Consider an amine (RNH2) with a pKa = 10 at physiologic pH (assume pH=7)
What % is ionized
10^7-10 = -3
10^-3 = 0.001
100-0.001 = 99.9%
10^7-10 = -3
10^-3 = 99
100-99 = 1.0%
10^10-7 = 3
10^3 = 90
100-90 = 10%
Weak Acids
When pH is greater than pKa, the weak acid will be mostly ________
Ionized
Non-ionized
Weak Acids
When pH is lower than pKa, the weak acid will be mostly _______
Ionized
Non-ionized
T/F When the pH is lower than pKa, it enhances a weak acids water solubility.
True
False
Weak Bases
When pH is lower than pKa, it tends to be _________
Ionized
Non-ionized
Weak Bases
When pH is higher than pKa, weak base becomes _______
Non-ionized
Ionized
Weak Bases
Would a weak base be better absorbed in the stomach (low pH) or intestines (higher pH)?
Stomach (ionized)
Intestines (non-ionized)
What are criteria for Lipinski's rule of 5s
MW less than 500
Less than 15 polar-H bonds
Log P in between -1 and 5
More than 15 polar-H bonds
Log P greater than 5
Log P between 0-3 is optimal for ______
Distribution
Metabolism
Excretion
Absorption
Transporters typically carry ____ substrates that cannot passively diffuse across cell membranes
Polar
Non-polar
Type of Transporters
Which type of substrates do OATS typically carry?
hydrophilic
Acids
Bases
Anions (-)
Cations (+)
Type of Transporters
Which type of substrates do OCTS typically carry?
Acids
Bases
Cations (+)
Anions (-)
Type of Transporters
What type of substrates do OATPS typically carry?
Hydrophobic
Anions (-)
Large
Small
Type of Transporters
What type of substrates do CNTS typically carry?
Nucleosides
Protein
Peptides
Aminoacids
Type of Transporters
What type of substrates do PEPT typically carry?
Nucelosides
Protein
Peptides
Amino Acids
High solubility and High permeability indicates what classification in the BCS system?
Class I
Class II
Class III
Class IV
Low solubility and High permeability indicates which classification in the BCS system?
Class I
Class II
Class III
Class IV
High solubility and low permeability indicates which classification in the BCS system?
Class I
Class II
Class III
Class IV
Low solubility and low permeability indicates which classification in the BCS system?
Class I
Class II
Class III
Class IV
T/F in most cases drugs have nearly 100% bioavailability
Absorption Profiles
Metoprolol fall in class I of BCS
with a MW of 261, 9 H bonds, and Log P of 1.8
Does this profile meet lipinski criteria?
Yes
No
Absorption Profiles
Metformin fall in class III of BCS
with a MW of 165, 10 H bonds, and Log P of -1.43
Does this profile meet lipinski criteria?
Yes
No
What is the major plasma transport protein?
Protein Binding
Which best describes the characteristic of the following?
Distribute quicker
Short half life
Metabolized quicker
Low protein binding
High protein binding
Protein Binding
Which best describes the characteristic of the following?
Distribute slower
long half life
Metabolized slower
Low protein binding
High protein binding
Free Drug
Drug A is 99% bound with 0.1% free drug
Drug B is 90% bound with 10% free drug
Which drug has an increased risk of toxicity and why?
Drug B has an increased risk of toxicity. Has a 100 fold increase of free drug
Drug A has an increased risk of toxicity. Has a 100 fold increase of free drug
Which section of organs have the highest rate of permeability?
Kidney, Liver, Gut
Muscle, Brain, Nerve
Drugs with less than 1000 MW can diffuse through most _________ ____ _________
(a)
Where must drugs distribute to produce its therapeutic effect?
(a)
Acidic drugs accumulate in tissues with pH ______ than plasma pH
Higher
Less
Basic drugs accumulate in tissues with pH ______ than plasma pH
Higher
Less
Volume Distribution
VD below __ is not getting into tissues (big and highly bound)
10
50
100
Volume Distribution
VD ____ than 10 can distribute on both planes
lower
greater
Volume Distribution
VD above __ indicates passive diffusion
10
50
100
If Km value is low it means the drug (does/does not) stick well to the enzyme
Does
Does not
Which of the following are characteristics of low extraction rate?
Not easily removed or metabolized
Good oral bioavailability
Very little first pass metabolism
Poor oral bioavailability
Easily removed or metabolized
Which of the following are characteristics of high extraction rate?
Not easily removed or metabolized
Good oral bioavailability
IV administration prefered
Poor oral bioavailability
Easily removed or metabolized
Phase I metabolism is functionally _______ and primarily an _______ process used to _______ substrates
irreversible/oxidation/ build
reversible/oxidation/ break down
irreversible/oxidation/ break down
reversible/oxidation/ build
Phase II metabolism is functionally _______ and primarily enhances ___________ used to _______ functional groups
irreversible/water solubility/ build
reversible/water solubility/ build
irreversible/oxidation/ break down
reversible/oxidation/ build
The following enzymes are primarily apart of which phase?
CYP3A4
CYP2D6
MAO
DAO
ADH
AIDH
FMOs
Phase I
Phase II
The following enzymes are primarily apart of which phase?
UGT
SULT
GST
COMT
Phase I
Phase II
CYP3A4 is typically most abundant in the ______
ADME
Which excipient adds bulk to the product?
Diluents
Binders
Glidants
Disintegrants
ADME
Which excipient promotes adhesion of powder into granules into tablets
Diluents
Binders
Gildants
Disintegrants
Being more soluble in water than lipid membranes describes…
Ionized
Non-ionized
BCS
If low solubility, it requires ______ liquid to be soluble
More
Less
Drugs with many _____ groups typically indicates hydrophilicity
Polar
Non-polar
Drugs with many _____ groups typically indicates lipophilicity
Polar
Nonpolar
solubility controls _______
Permeability
Absorption
