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Chapter 1 - Drug Action
Pharmaceutic, Pharmacokinetic, and Pharmacodynamic Phases
104
Pharmacology
Undergraduate 3
09/06/2011

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Term
A drug taken orally goes through three phases:
Definition
1. Pharmaceutic
2. Pharmacokinetic
3. Pharmacodynamic
Term
What happens in the pharmaceutic phase?
Definition
The drug becomes a solution so it can cross the biologic membrane
Term
What phase is absent when a drug is administered using the subQ, IM, or IV route?
Definition
Pharmaceutic
Term
What are the four processes of the pharmacokinetic phase?
Definition
1. Absorption
2. Distribution
3. Metabolism (biotransformation)
4. Excretion (elimination)
Term
A biologic or physiologic response occurs in which phase of drug action?
Definition
Pharmacodynamic phase
Term
What percentage of drugs are taken by mouth?
Definition
80%
Term
What is another term for the pharmaceutic phase?
Definition
Dissolution
Term
Drugs in solid form must disintegrate into small particles to dissolve into a liquid. These two processes are known as
Definition
1. Disintegration
2. Dissolution
Term
What form of drugs are already dissoluted?
Definition
Drugs in liquid form
Term
Fillers and inert substances found in tablets are termed:
Definition
Excipients.
These allow a drug to take on a particular size and shape, and enhance dissolution
Term
Adding K or Na to sodium enhances its absorption. T/F
Definition
True. Penicillin is poorly absorbed in the GI tract b/c of gastric acid. Adding these substances allows it to be absorbed.
Term
Infants gastric secretions are more acidic, therefore they can absorb more penicillin. T/F
Definition
False. Infants gastric secretions are more alkaline, causing them to absorb more of the penicillin.
Term
The breakdown of a tablet into smaller particles:
Definition
Disintegration
Term
Dissolving of small particles in the GI fluid before absorption:
Definition
Dissolution
Term
The time it takes the drug to disintegrate and dissolve to become available for the body to absorb it:
Definition
Rate limiting
Term
A lower pH causes a slower disintegration and absorption. T/F
Definition
False. A lower pH will cause drugs to be disintegrated and absorbed faster (in a pH of 1 or 2). The very young and older adults generally have slower rates of disintegration and absorption for drugs that are absorbed primarily in the stomach.
Term
What type of drugs resist disintegration in gastric acid of the stomach?
Definition
Enteric-coated. Disintegration does not occur until the drug reaches the alkaline environment of the small intestine.
Term
The process of drug movement to achieve drug action.
Definition
Pharmacokinetics
Term
Movement of drug particles from the GI tract to body fluids.
Definition
Absorption
Term
What are the three methods of absorption?
Definition
Passive
Active
Pinocytosis
Term
What happens to protein-based drugs in the small intestine?
Definition
They are DESTROYED by digestive enzymes
Term
Diffusion is an example of
Definition
Passive absorption
Term
Movement by using a carrier such as an enzyme or protein to move a drug against a concentration gradient is
Definition
Active absorption. This requires energy.
Term
Process by which cells carry a drug across their membrane by engulfing the drug particles:
Definition
Pinocytosis
Term
The Gi membrane is composed mostly of ____ & ____
Definition
Lipid and protein
Term
Water-soluble drugs pass readily through the lipid bilayer of cell membranes. T/F
Definition
False. Water-soluble drugs need a carrier, such as an enzyme or protein, to pass through the membrane.
Term
What type of particles can pass through the cell membrane? (the answer has to do with electrical charge)
Definition
Nonionized (no positive or negative charge)
Term
What administration methods bypass the GI tract or liver?
Definition
Parenteral drugs
Eyedrops
Eardrops
Nasal sprays
Respiratory inhalants
Transdermal drugs
Sublingual drugs
Term
What drugs are absorbed faster than water-soluble and ionized drugs?
Definition
Lipid soluble and non-ionized drugs.
Term
What factors affect drug absorption?
Definition
Blood flow,
pain,
stress,
hunger,
fasting,
food,
and pH.
Term
Drugs given IM are absorbed faster in muscles that have more blood vessels such as the _______ than in those that have fewer blood vessels, such as the _____.
Definition
Deltoids

Gluteals
Term
Subcutaneous tissue has few blood vessels, so absorption is ____.
Definition
Slow
Term
The process in which drugs pass to the liver first
Definition
First-pass effect
or
hepatic first pass
Term
If a drug has an extensive first-pass metabolism, what happens to it?
Definition
Most of the dose is destroyed.
Term
The percentage of the administered dose that reaches systemic circulation
Definition
Bioavailability
Term
For the oral route, bioavailability occurs:
Definition
After absorption and hepatic drug metabolism.
Term
T/F - The bioavailability for the oral route is never 100%.
Definition
True. But for the IV route it IS usually 100%.
Term
To obtain the desired drug effect, the oral dose could be _ to _ times larger than the drug dose for IV use.
Definition
3 to 5
This is because oral drugs that have a high first-pass hepatic metabolism may have a bioavailability of only 20-40% upon entering systemic circulation.
Term
Drug form, route, GI mucose and motility, food and other drugs, and changes in liver metabolism are all factors that alter
Definition
Bioavailability
Term
What happens to a drug that is primarily metabolized by the liver in the presence of a liver disorder?
Definition
Its' bioavailability increases.
Term
The process by which the drug becomes available to body fluids and body tissues
Definition
Distribution
Term
Drug distribution is influenced by
Definition
Blood flow
the drug's affinity to the tissue, and
the protein binding effect
Term
What are protein-bound drugs primarily bound to?
Definition
Albumin
Term
The portion of the drug that is bound to the protein is considered ______, as it is not available to receptors.
Definition
Inactive
Term
Only ____ _____ are active and can cause a pharmacologic response.
Definition
Free drugs
Term
What happens when free drug in circulation decreases?
Definition
More bound drug is released from protein to maintain the balance of free drug.
Term
When two highly protein-bound drugs are given concurrently, what happens?
Definition
They compete for protein-binding sites, causing more free drug to be released into circulation
Term
How is drug dose prescribed?
Definition
It is prescribed according to the percentage in which the drug binds to protein.
Term
In what form must a drug be metabolized to be excreted by the kidneys?
Definition
Water-soluble
Term
Half life (t1/2):
Definition
The time it takes for one half of the drug concentration to be eliminated.
Term
A short half life is considered to be
Definition
4-8 hours
Term
A long half life is considered to be
Definition
longer than 24 hours
Term
What is the main route of drug elimination?
Definition
Kidneys
Term
What are routes of drug elimination other than the urine?
Definition
Bile,
feces,
saliva,
lungs,
sweat,
breast milk.
Term
T/F The kidneys filter free unbound drugs, water-soluble drugs, and drugs that are unchanged.
Definition
True
Term
T/F Protein-bound drugs can be filtered through the kidneys.
Definition
False. Once the drug is released from the protein, it is a free drug and is eventually excreted in the urine.
Term
With a kidney disease what happens to glomerular filtration rate?
Definition
It is decreased, and drug excretion is slowed or impaired.
Term
What's the most accurate test to determine renal function?
Definition
Creatinine clearance (CLcr)
Term
Creatinine is:
Definition
a metabolic byproduct of muscle that is excreted by the kidneys.
Term
A _____ in renal GFR results in an increase in serum creatinine levels and decrease in uring creatinine clearance.
Definition
Decrease
Term
The CLcr should be determined to establish appropriate drug doses in those with ____.
Definition
Renal dysfunction
Term
Normal creatinine clearance is
Definition
85 - 135 mL/min
Term
Older clients may have a CLcr of
Definition
60 mL/min
Term
The study of drug concentration and its effects on the body
Definition
Pharmacodymnamics
Term
The primary effect of a drug is _____
Definition
desirable
Term
The secondary effects of a drug are
Definition
Desirable or undesirable
Term
The relationship between the minimal versus the maximal amount of drug dose needed to produce the desired drug response
Definition
Dose response
Term
Maximal efficacy - aka
Definition
Maximum drug effect
Term
Onset of action
Definition
the time it takes to reach the minimum effective concentration (MEC) after a drug is administered
Term
Peak action
Definition
Occurs when the drug reaches its highest blood or plasma concentration
Term
Duration of action
Definition
the length of time the drug has a pharmacologic effect
Term
A time response curve evaluates
Definition
Onset of action
Peak action
and Duration
Term
Too high a drug level above the ________ _____ _____________ can result in toxicity.
Definition
Minimum toxic concentration (MTC)
Term
Where are most receptors found?
Definition
In cell membranes
Term
What are the 4 receptor families?
Definition
1. Kinase-linked
2. Ligand-gated ion channels
3. G protein-coupled
3. Nuclear
Term
Drugs act through receptors by binding to the receptor to ______ a response or to ______ a response.
Definition
Produce (initiate)
Block (prevent)
Term
Agonist
Definition
Drug that produces a response
Term
Antagonist
Definition
Drug that blocks a response
Term
IC50 is the antagonist drug concentration required to inhibit __% of the maximum biological response.
Definition
50%
Term
Nonspecific drugs affect
Definition
Various sites and have properties of nonspecifity.
Term
Nonselective drugs affect
Definition
various receptors
Term
What are the four categories of drug action?
Definition
1. Stimulation or depression
2. Replacement
3. Inhibition or killing of organisms
4. Irritation
Term
The length of action of a drug depends on
Definition
Its half life
Term
Therapeutic index (TI) estimates
Definition
the margin of safety of a drug through the use of a ratio that measures the effective dose in 50% of persons or animals, and the lethal dose in 50% of animals.
Term
The closer the therapeutic index is to _, the greater the danger of toxicity.
Definition
1
Term
Drugs with a ___ ______ _____ have a narrow margin of safety.
Definition
Low therapeutic index
Term
Drugs with a ___ ______ _____ have a narrow margin of safety.
Definition
Low therapeutic index
Term
The therapeutic range (window) of a drug concentration in plasma should be between
Definition
the minimum effective concentration and minimum toxic concentration.
Term
T/F If the therapeutic range is narrow, the plasma drug level should be monitored periodically to avoid drug toxicity.
Definition
True. Monitoring the theraptutic range is not necessary if the drug is not considered highly toxic
Term
Peak drug level
Definition
The highest plasma concentration of drug at a specific time. This indicates the rate of absorption.
Term
__ peak time is faster than __ peak time.
Definition
IV; oral
Term
T/F A urine sample should be evaluated at the proposed peak time, according to the route of administration.
Definition
False. A blood sample should be drawn.
Term
What is the lowest plasma concentration of a drug that measures the rate at which the drug is eliminated?
Definition
Trough drug level
Term
When are trough levels drawn?
Definition
Immediately before the next dose of drug is given.
Term
Peak levels indicate the rate of _____ and trough levels indicate the rate of _____.
Definition
Absorption; elimination
Term
What happens if peak is too low?
Definition
No therapeutic effect is achieved.
Term
What is a loading dose?
Definition
A large initial dose to initiate an immediate drug response. This achieves a rapid minimum effective concentration in the plasma.
Term
Side effects are
Definition
Physiological effects not related to desired drug effects
Term
Adverse reactions are
Definition
more severe than side effects. They are unintended and occur at normal doses. They are always undesirable
Term
How can toxicity be identified?
Definition
By monitoring the plasma (serum) therapeutic range of the drug.
Term
Pharmacogenetics
Definition
Studying how the effect of a drug action varies from a predicted drug response because of genetic factors or hereditary influence. Genetic factors can alter the metabolism of the drug.
Term
Decreased responsiveness over the course of therapy
Definition
Tolerance
Term
Tachyphalaxis
Definition
A rapid decrease in response to the drug. An acute tolerance.
Term
Placebo effect
Definition
Psychological benefit from a compound that may not have the chemical structure of a drug effect.
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