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25 Cards in this Set

  • Front
  • Back

a. Define drug disposition


b. Drug Disposition is an example of Pharmaco___



a. The processes a drug is subjected to by the body upon administration


b. Pharmacokinetics

Name the 4 processes involved in drug disposition

1. Absorption


2. Distribution


3. Metabolism


4. Excretion




ADME

Name the 6 forms of administration (+ what each form is associated with)

1. Rectal/Rectal (Gut)


2. Intramuscular (Muscles)


3. Intravenous (Blood plasma)


4. Percutaneous (Skin)


5. Inhalation (Lungs)


6. Intrathecal (CSF)

The mode of administration has an effect on what?

How much of drug reaches the bood Plasma

How much of the drug that reaches the blood plasma depends on what?

How many membranes the drug has to move through (i.e. the mode of adminstration)

a. Define Bioavailibilty


b. What is the symbol for bioavailability?

a. The Fraction (F) of the administered dose which reaches the Systemic Circulation


b. (F)

a. Which mode of administration has the most efficient bioavailibility?


b. What might a poor bioavailability reflect? (to do with drug)

a. Intravenous (IV) injection = 1


b. High Gastric instability

Briefly describe the phenomenon of First Pass Metabolism

Where the concentration of a drug is significantly reduced (via metabolism by liver + gut wall) before the drug reaches systemic circulation



- When a drug is administered orally, it is absorbed by the __(a)__


- It then enters the __(b)__


- Here it is carried through the __(c)__, into the __(d)__ before it reaches the __(e)__

a. Digestive system


b. Hepatic portal system


c. Portal vein


d. Liver


e. Systemic circuit

Name 5 factors which affect drug absobtion

1. Gastric motility (how quickly drug moves)


2. Nature of drug


3. Area of absorption surface


4. Blood flow at absorption surface


5. Ingestion of food


- Plasma protein binding

- Most drugs are either __(a)__ or __(b)__


- They therefore exhibit __(c)__


- __(d)__ are not lipid soluble

a. Weak acids


b. Weak bases


c. pH dependant ionization


d. Ionized species

a. Name the 4 different routes of absorption across a lipid membrane


b. What is the major route (most common) out of the 4?

a.


1. Diffusion through lipid


2. Diffusion through aqueous channel


3. Carrier mediated


4. Pinocytosis


b.


Diffusion through Lipid

Diffusion through aqueous pores/ion channels:


a. What kind of molecules diffuse via this route?


b. Give an example

a.


- Very small


- Less than 1000Da


- Water soluble


b.


Lithium


(small + monovalent)

Carrier-mediated diffusion:


a. Via what processes do carriers use to cause diffusion?


b. Name 3 examples of important sites of transfer (using this mode of diffusion)


c. Name a downside of this mode of diffusion



a. Facilitated diffusion/Active transport


b.


- Blood-brain barrier


- Renal Tubule


- Gastrointestinal tract


c. Carriers/transporters may become saturated, hence limiting the rate of drug permeation

Pinocytosis:


a. What kind of molecules usually diffuse via thi mode?


b. Give an example

a.


- Macromolecules


- Greater than 1000Da


b.


- Insulin


- Crossing the blood-brain barrier

Diffusion through lipid membranes:


a. What kind of molecules diffuse via this route?


b. Dependent upon what 2 things?


c. Degree of permeation is dictated by what?



a.


- Small


- Lipid soluble


- non-polar


b.


- SA of barrier


- Blood flow at barrier


c. Fick's Law

a. Briefly describe Fick's Law


b. Which factor(s) in Fick's law are inversely proportional?


c. What EXACTLY does Fick's law show?

a. The factors which give an indication of how easily a drug diffuses through a lipid membrane


b. (W) thickness of membrane


c. The amount of drug which diffuses over time


i.e. dQ/dt

e. Which form of a drug is lipid soluble?

e. Which form of a drug is lipid soluble?

a. HA


b. A-


c. BH+


d. B


e. Non-ionized form

- A highly lipid soluble drug is subject to a large __(a)__


- It will diffuse __(b)__ than a drug of lower lipid solubility

a. Transmembrane concentration gradient


b. More rapidly

a. What is the symbol for the dissociation constant?


b. When is the dissociation constant equal to the pH?

a. pKa


b. pKa=pH when 50% of the drug molecules are ionized

Write down the Henderson-Hasselbach equations for both weak acids and weak bases

Describe the phenomenon of ion trapping

When an ionized drug becomes trapped on one side of the membrane which divides compartments with different pHs

a. What are the 5 different body departments?


b. Which body department is the largest


c. WHich body department is the smallest?

a.


- Plasma water


- Interstitial water


- Intracellular water


- Transcellular water


- Fat


b. Intracellular water


c. Transcellular water

a. Define Volume of Distribution


b. What is the formula for volume of distribution?


c. What is the Volume of distribution a measure of?

a.


The volume of water required to contain the total amount of drug in the body at the same concentration as that present in the plasma Cp


b. Vd = Dose/Cp


c. The extent of distribution

If a drug has a high Vd, name 3 things this shows

1. High lipid solubility


2. Low charge (non-polar)


3. Low plasma protein binding