Kwon Exam 2 Flashcards by tara tritsch

After administration, a drug must be _____ and _____ to its site of action.

absorbed; distributed

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What part of ‘ADME’ represents systemic circulation?

absorption

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What part of ‘ADME’ represents equilibration?

distribution

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Which route of drug administration is the most complex?

oral administration

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What part of ‘ADME’ does the drug go from the gut into the blood stream?

absorption

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Drugs may be _____ to inactive (sometimes active) products to aid elimination from the body.

metabolized

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The drug and its metabolites must be _____ from the body after it has brought about its effects.

excreted

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What is the difference between heparin and warfarin?

heparin stays in plasma (central compartment)
warfarin is 99% albumin bound

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What is the passage of a drug through cell layers into the general circulation?

absorption

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What is the passage of a drug from the blood through the capillary tubes into extracellular fluid, cells, and tissues?

distribution

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What is the passage of drugs into hepatic tissues (site of biotransformation)?

metabolism

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What is the passage of a drug through nephron units in kidney for removal from the body?

excretion

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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

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What determines the kinetic properties of a drug?

polarity (water solubility)

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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

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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

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Why don’t large molecules readily cross membranes?

because of their molecular weight

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T/F uncharged drugs readily crosses membranes, charged molecules do not.

TRUE

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The more charged a drug molecule, the more water soluble and the less lipid soluble it is. What is this called?

ionization

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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

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Absorption rate and efficiency is dependent on what?

route of administration

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Which type of diffusion shows low structural specificity?

aqueous (passive) diffusion

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Which type of diffusion requires specific carrier proteins and can be inhibited?

facilitated diffusion

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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

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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?