Kwon Exam 2 Flashcards
After administration, a drug must be _____ and _____ to its site of action.
absorbed; distributed
What part of ‘ADME’ represents systemic circulation?
absorption
What part of ‘ADME’ represents equilibration?
distribution
Which route of drug administration is the most complex?
oral administration
What part of ‘ADME’ does the drug go from the gut into the blood stream?
absorption
Drugs may be _____ to inactive (sometimes active) products to aid elimination from the body.
metabolized
The drug and its metabolites must be _____ from the body after it has brought about its effects.
excreted
What is the difference between heparin and warfarin?
- heparin stays in plasma (central compartment)
- warfarin is 99% albumin bound
What is the passage of a drug through cell layers into the general circulation?
absorption
What is the passage of a drug from the blood through the capillary tubes into extracellular fluid, cells, and tissues?
distribution
What is the passage of drugs into hepatic tissues (site of biotransformation)?
metabolism
What is the passage of a drug through nephron units in kidney for removal from the body?
excretion
What does the drug passage through cell membranes depend on? (hint: 4 things)
- molecular size/shape
- degree of ionization
- relative lipid solubility (of ionized + nonionized forms)
- binding to serum and tissue properties
What determines the kinetic properties of a drug?
polarity (water solubility)
What measures the relative affinity of an agent for a polar aqueous medium versus a non polar, oil-like medium? (hint: water soluble versus lipid soluble)
partition coefficient
Membranes are lipids and drugs must cross several membrane (lipid) barriers in order to reach their site of action. What is this called?
lipid solubility
Why don’t large molecules readily cross membranes?
because of their molecular weight
T/F uncharged drugs readily crosses membranes, charged molecules do not.
TRUE
The more charged a drug molecule, the more water soluble and the less lipid soluble it is. What is this called?
ionization
Many drugs are ____ acids or ____ bases and their charge at any given moment depends on the pH of the medium they are in.
weak acids; weak bases
Absorption rate and efficiency is dependent on what?
route of administration
Which type of diffusion shows low structural specificity?
aqueous (passive) diffusion
Which type of diffusion requires specific carrier proteins and can be inhibited?
facilitated diffusion
What are the 4 primary mechanisms for the passage of a drug through cell membranes?
- aqueous (passive) diffusion
- facilitated diffusion
- active transport
- endocytosis and exocytosis
Which primary mechanism for the passage of drug absorption through cell membranes is spontaneous and bidirectional and cannot be inhibited?
aqueous (passive) diffusion
Which primary mechanism for the passage of drug absorption through cell membranes can be saturated and is driven by a concentration gradient (high to low)?
facilitated diffusion
Which primary mechanism for the passage of drug absorption through cell membranes can be saturated and is energy dependent requiring ATP that can be inhibited?
active transport
Which primary mechanism for the passage of drug absorption through cell membranes is an energy dependent, saturable process? (hint: carries drugs of exceptionally large size >1000)
endocytosis and exocytosis
Lizness (linaclotide) is indicated in adults for the treatment of what?
irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC)
Drugs must be absorbed from the site of administration unless _____ ______.
injected intravenously
Which two routes of administration take effect in 30-60 seconds? (hint: fastest)
- intravenous (#1)
- intraosseous (#2)
Which two routes of administration take effect in 2-3 minutes? (hint: second fastest)
- endotracheal (#3)
- inhalation (#4)
Which is the only route of administration that takes effect in 3-5 minutes?
sublingual (#5)
Which two routes of administration take effect between 10-30 minutes?
- intramuscular (#6) (10-20 min)
- subcutaneous (#7) (15-30 minutes)
Which route of administration take effect in 5-30 minutes?
rectal (#8)
Which route of administration takes the longest (30-90 minutes)?
ingestion (#9)
Which route of administration varies from minutes to hours?
transdermal (topical) (#10)
What are the 3 types of parenteral injection?
- intravenous (IV)
- subcutaneous (SC)
- Intramuscular (IM)
Which route of administration is fastest and allows for systemic circulation immediately?
intravenous (IV)
List several disadvantages of intravenous injection:
- toxic reactions can be seen immediately
- most dangerous route
- drug must be in aqueous solution
- must be performed slowly
- once injected, drug cannot be removed
List several advantages of intravenous injection:
- extremely rapid
- initial absorption step is by-passed
- drug levels are more accurately controlled
- good for irritant drugs
- suitable for large volumes
The rate of parenteral injection is limited by what 3 things?
- area of absorbing capillary membranes
- solubility of the substance in interstitial fluid
- large molecules gain access to the circulation (biologics)
The ‘time until effect’ that refers to route of administration is based on what?
plasma concentration curve
Route of administration determines the ____ and ____ of absorption.
rate; efficiency
The more charged a drug molecule, the ____ water soluble and the ____ lipid soluble it is.
more; less
Which functional groups are acids?
- carboxylic acids
- beta-dicarbonyls
- sulfonamides and sulfonylureas
- tertrazoles
- phenols
- thiols
- sulfates, phosphates, phosphonates
Which functional groups are bases?
- aliphatic and alicyclic amines
- aromatic amines
- imines and hydrazines
- aromatic heterocycles (nitrogen)
T/F amides are bases:
FALSE amides are neutral !!
T/F sulfonamides are acids:
TRUE
What is an amphoteric molecule?
a molecule with acidic + basic groups
What is the most abundant protein in blood?
serum albumin (lipid binding sites)
Ionization of acidic/basic groups affect plasma protein binding and tissue binding, what does this affect?
distribution
What type of group can be in a benzo ring?
amine group
An imide is when X is a ___ atom.
NITROGEN
(X = N)
What functional group has a pKa slightly higher than carboxylic acids (less acidic) and is more lipophilic than carboxylic acids?
tetrazoles
What type of drug contains a tetrazole in its structure? (hint: not an actual drug name)
angiotensin II receptor blockers
Is phenol predominantly ionized in blood?
no, its unionized
What amino acid has a phenolic side chain?
tyrosine
Which functional group (that was listed in the acid/base powerpoint) is the strongest base?
guanidine (pKa = 12-13)
The acid/base nature of a drug molecule influences what? (this is long, sorry)
- overall water solubility of drug molecule
- oral absorption of drug molecule
- passive reabsorption of drug molecule w/in urinary tract
- ability of drug molecule to interact w biological target
- metabolism and elimination of drug molecule
- ability to form water or lipid-soluble salts
- suitability of drug molecule for given pharmaceutical formulation and route of administration
SHORTENED VERSION
- water solubility
- oral absorption
- passive reabsorption
- integration w target
- metabolism/elimination
- formation of water/lipid soluble salts
- suitability for formulation/administration
What is #1 in the image?
peak effect
What is #2 in the image?
onset of effect
What is #3 in the image?
lag period
What is #4 in the image?
duration of action
What is #5 in the image?
MEC for adverse response
What is #6 in the image?
therapeutic window
What is #7 in the image?
MEC for desired response
What does “Drug Effect (CP)” in the image refer to?
plasma concentration
The therapeutic window of a drug is related to what?
related to drug effect
What functional group is pictured?
alkane
What functional group is pictured?
alkene
What functional group is pictured?
alkyne
What functional group is pictured?
benzene ring (phenyl)
What functional group is pictured?
amine
What functional group is pictured?
alcohol (hydroxyl group)
What functional group is pictured?
ether
What functional group is pictured?
alkyl halide
What functional group is pictured?
thiol
What functional group is pictured?
aldehyde
What functional group is pictured?
ketone
What functional group is pictured?
ester
What functional group is pictured?
carboxylic acid
What functional group is pictured?
amide
