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63 Cards in this Set

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What the drug does to the body. (biochemical/physiological effects, mechanism of action, and interaction with receptors)
What is pharmacodynamics
What the body does to the drug. (Absorption, distribution, biotransformation, and excretion)
What is pharmacokinetics.
What is 1st pass metabolism?
When drugs are metabolized extensively by the liver before being delivered to the systemic circulation.
Describe the distribution of free drugs from the circulatory. x 3
1. Bind to receptor (or site of action)
2. Bind to tissue for storage
3. Bind to plasma components for storage.
What is 1st pass metabolism?
When drugs are metabolized extensively by the liver first before being delivered to the systemic circulation.
Define absorption.
The rate and the extent to which a drug leaves its site of administration.
Two types of administration routes for drug absorption.
1. Enteral
2. Parenteral
Examples of enteral.
oral, sublingual, and rectal
Examples of parenteral.
IV, SQ, IM, inhalation, and topical.
What are the characters required for passage across cell membrane? x 4
1. Nonpolar
2. Unionized
3. Low MW
4. Lipid Soluble
What is the major physical difference between non-brain capillaries and brain capillaries?
Brain capillaries do NOT have fenestrations.
Role of pinocytosis and tight junctions in brain capillaries.
Greatly reduced
In order to cross the blood brain barrier, solutes must to what?
Cross two membranes.
According to Fick's law, what would increase absorption of drugs? x 2
Increase absorption area.

Decrease thickness of membrane.
What would define a low molecular weight electrolyte that is able to circumlocute?
Water solube, weak electrolyte smaller than 100 Daltons
In an ACIDIC environment, a weak acid would become what?
Unionized.
In a NEUTRAL, BASIC environment, a weak acid would become what?
Ionized.
In a strong BASIC environment, a weak base becomes what?
Unionized
In a NEUTRAL, ACIDIC environment, a weak base would become what?
Ionized.
What is the HH equation for weak acids?
pKa - pH = log (U/I)
What is the HH equation for weak bases?
pKa - pH = log (I/U)
Aspirin is an example of a weak _______?
Acid
Pyrimethamine is an example of a weak ______?
Base
Codeine's onset of action depends on what?
GI motility
What are the advantages of IV administration? x 2
1. Absorption is circumvented

2. Bioavailability is complete
Why should IV drugs have a short half life?
Once injected, there is no turning back.
What is the most common form of drug administration?
PO
What are the benefits of PO? x 3
1. Safest
2. Most convenient
3. Most economical
What are disadvantages of PO?
1. Slow onset of action
2. 1st pass metabolism
3. Irregularities in absorption (by food or other drugs)
Nitroglycerine has special significance in what type of drug administration?
Sublingual
Advantages of SL? x 3
1. NO FIRST PASS EFFECT - drains directly to SVC

2. HIGH POTENCY - only few molecules needed

3. HIGH LIPID SOLUBILITY - very rapid absorption.
Advantages of rectal administration. x 3
1. When oral ingestion is not possible (infant or unconscious)

2. Greater portion bypasses the first pass effect

3. Onset of action is faster than oral.
Disadvantages of rectal administration. x 2
1. Patient compliance

2. Absorption irregular and often incomplete
Advantages of SQ?
1. Absorption is quick, but slow enough for sustained effect.
What is the best administration technique for durgs that irritate?
IV
What effects the rate of absorption for SQ?
Vasodilators and Vasoconstrictors.
Steroids, Heparin, Insulin, and Epinephrine are administered how?
SQ.
Describe absorption for water soluble and oil-based drugs in IM.
Water soluble is fast

Oil based is slow
What administration method is best for optimizing the effects of a drug in the CNS when it cannot pass the blood brain barrier?
Intrathecal
What would be the purpose of intra-arterial administration? x 2
1. Minimize systemic effects

2. Diagnostic drugs
Advantages of Inhalation/Intranasal. x 2
1. Lung area is large

2. Hepatic 1st pass is minimized.
T/F - Drugs bound to plasma membrane are INACTIVE.
TRUE
T/F - Drugs in the free form are ACTIVE.
TRUE
Give an example of a plasma protein for acidic drugs.
Albumin
Give an example of a plasma protein for basic drugs.
Alpha 1 acid glycoprotein
Describe the affinity and capacity of albumin.
Affinity - LOW

Capacity - HIGH
Hypoalbuminemia (liver/kidney failure) can lead to what on drugs?
Elevated level of free drug
Describe the affinity and capacity of alpha 1 acid glycoprotein.
Affinity - HIGH

Capacity - LOW
Plasma protein binding can be described as? x 3
1. Non-selective
2. Non-linear
3. Saturable
Drugs compete with binding sites with?
Each other and endogenous ligands.
Compare fetal plasma with mother's plasma. Why important?
Fetal plasma is slightly more acidic, thus ion trapping of BASIC drugs can occur (b/c it is ionized).
If concentration of drug in plasma is low, then Volume of Distribution is what?
High
Volume of distribution is what type of variable?
Independent.

Does NOT depend on clearance, half-life, or bioavailability.
Excretory organs (including lungs) excrete what kind of compounds more efficiently?
Polar compounds.
Glomerular filtration is regulated by what?
1. GFR
2. CV performance
3. Blood Volume
4. Renal Blood flow
Acidification of urine increases the excretion of what kind of drugs?
Basic
Alkalinization of urine increases the excretion of what kind of drugs?
Acidic
Describe the half-life and elimination rates for FIRST ORDER kinetics.
Half-life is constant.

Elimination rate changes.
How many half lives to acheive steady state after dosage?
4-5
What variables are needed for designing a rational dose regimen? x 4
1. Bioavailability
2. Volume of Distribution
3. Half life
4. Clearance
T/F - Clearance is amount of drug removed.
FALSE - it is th evolume of fluid that would have to be completely freed of drug to account for the elimination.
With increase in age, what happens to clearance and drug half-life?
Clearance decreases.

Half-life increases
T/F - At steady state, amount in = amount out, for both first and zero order.
FALSE - only true for first order.