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90 Cards in this Set
- Front
- Back
- 3rd side (hint)
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The study of Rx distribution in the body and focuses on the change in Rx plasma concentration in tissues and body fluids over time
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Pharmacokinetics
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Detailed mechanism of action by which Rx produce their pharmacological effects on target organs.
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Pharmacodynamics
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Effective for administering potent Rx at low dosages
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Skin patches advantages
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Effective for treating respiratory problems
delivered directly to the site of action minimize side effects |
Aerosols -Advantages
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Distribution across the BBB is affected by what Rx property?
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Lipid solubility
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Enzyme- catalyzed conversion of Rx is known as what?
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Metabolism
aka Biotransformation |
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Where does most biotransformation take place?
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Liver
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What organs besides the liver have enzymes for Rx metabolism?
5ct |
~Brain
~Lungs ~Kidneys ~Intestines ~Skin |
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What other routes of excretion exist besides the kidneys?
7ct |
~Air
~Bile ~Breast Milk ~Feces ~Saliva ~Sweat ~Tears |
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First step in renal Rx excretion?
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Glomerular filtration
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How are
-weak acids -bases -charged particles excreted? |
Active tubular secretion
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How are non-electrolytes excreted?
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Passively
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How are compounds with large molecular weights excreted?
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In the bile
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How are most Rx absorbed?
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Passive diffusion
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Where are weak acids absorbed?
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In the stomach
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Where are weak bases absorbed?
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In the intestine
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How does molecular size affect the distribution of heparin
for example? |
Heparin is confined to the plasma because of its large size
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How can the first pass effect be bypassed?
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Orally or sublingually
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This group of substances catalyzes the biotransformation of many Rx.
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Cytochrome P450 enzyme system
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The fraction of the administered dose of a Rx that reaches the systemic circulation in an active form.
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Bioavailability
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The time required to reduce the plasma Rx concentration by 50%.
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Half-life
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The point at which the rate of Rx elimination reaches the rate of Rx administration
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Steady state
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How long does it take to reach steady state?
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5 half-lives for a first order process
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A dose given to rapidly establish a therapeutic plasma concentration?
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Loading dose
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Term for a dose given to establish or maintain the desired steady-state plasma Rx concentration
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Maintenance dose
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Specific cell molecules by which Rx molecules interact to produce their desired effects.
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Receptors
They are typically ________ Molecules ? |
Typically Protein Molecules
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This is not always related to receptor affinity and differs among various Rx that bind to a receptor and start the signal transduction pathway.
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Intrinsic activity
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Rx that have both receptor affinity and efficacy are called:
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Agonists
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This term indicates that the Rx can produce maximal response obtainable in a tissue.
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Full agonists
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The study of Rx distribution in the body and focuses on the change in Rx plasma concentration in tissues and body fluids over time
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Pharmacokinetics
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These can produce only a submaximal response.
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Partial agonists
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Detailed mechanism of action by which Rx produce their pharmacological effects on target organs.
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Pharmacodynamics
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These reduce the rate of signal transduction.
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Inverse agonists
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Effective for administering potent Rx at low dosages
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Skin patche advantages
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Rx that have receptor affinity but lack efficacy.
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Antagonists
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Effective for treating respiratory problems
delivered directly to the site of action minimize side effects |
Aerosols -Advantages
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The concentration of a Rx at the receptor site and the magnitude of the response.
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Intrinsic activity
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Distribution across the BBB is affected by what Rx property?
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Lipid solubility
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A continuous response when elicited that is described in terms of a percentage of the maximal response plotted against the log dose of the Rx.
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Graded dose-response relationship
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Enzyme- catalyzed conversion of Rx is known as what?
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Metabolism aka biotransformation
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An all or none response that is described as a cumulative percentage of subjects exhibiting a defined all-or-none effect and is plotted against the log dose of the Rx
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Quantal
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Where does most biotransformation take place?
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Liver
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T or F: some Rx can cause damage to specific organs while not damaging others.
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T
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What organs besides the liver have enzymes for Rx metabolism?
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Intestines
kidneys brain lungs and skin |
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List some ways in which Rx can interfere with each other
7ct |
Altered Absorption
Biotransformation Distribution Excretion Pharmacodynamic Interactions Rx <--> Food Interactions Rx <--> Rx Reaction |
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What other routes of excretion exist besides the kidneys?
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Bile
sweat saliva tears feces breast milk and exhaled air |
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In this population
the capacity to metabolize and excrete Rx is greatly reduced because of low levels of Rx biotransformation enzymes. |
Neonates and premature infants
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First step in renal Rx excretion?
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Glomerular filtration
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In this population
first pass inactivation may be increased as well as a higher biotransformation rate. |
Children
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How are weak acids
bases and other charged particles excreted? |
Active tubular secretion
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In this age group
there is a higher volume of distribution for fat- soluble Rx. |
The elderly
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How are non-electrolytes excreted?
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Passively
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In this age group
there is a reduced capacity to excrete Rx. |
Neonates
Infants Elderly |
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How are compounds with large molecular weights excreted?
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In the bile
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Disease in these organs can result in reduced Rx clearance.
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Liver and kidneys
as well as heart failure |
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How are most Rx absorbed?
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Passive diffusion
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In the very young and the very old
what adjustment should be made in Rx prescribing? |
Dosage per kilogram should be reduced
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Where are weak acids absorbed?
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In the stomach
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What can result if dosages aren't reduced for liver and kidney disease patients?
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Toxicity
because of :reduced: ~Metabolism ~Excretion |
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Where are weak bases absorbed?
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In the intestine
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Is conjugation
oxidation or both usually reduced in liver disease? |
Oxidation
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How does molecular size affect the distribution of heparin
for example? |
Heparin is confined to the plasma because of its large size
|
|
|
|
How can the first pass effect be bypassed?
|
Orally or sublingually
|
|
|
|
This group of substances catalyzes the biotransformation of many Rx.
|
Cytochrome P450 enzyme system
|
|
|
|
The fraction of the administered dose of a Rx that reaches the systemic circulation in an active form.
|
Bioavailability
|
|
|
|
The time required to reduce the plasma Rx concentration by 50%.
|
Half-life
|
|
|
|
The point at which the rate of Rx elimination reaches the rate of Rx administration
|
Steady state
|
|
|
|
How long does it take to reach steady state?
|
5 half-lives for a first order process
|
|
|
|
A dose given to rapidly establish a therapeutic plasma concentration?
|
Loading dose
|
|
|
|
Term for a dose given to establish or maintain the desired steady-state plasma Rx concentration
|
Maintenance dose
|
|
|
|
Specific cell molecules by which Rx molecules interact to produce their desired. Effects. They are typically protein molecules
|
Receptors
|
|
|
|
This is not always related to receptor affinity and differs among various Rx that bind to a receptor and start the signal transduction pathway.
|
Intrinsic activity
|
|
|
|
Rx that have both receptor affinity and efficacy are called:
|
Agonists
|
|
|
|
This term indicates that the Rx can produce maximal response obtainable in a tissue.
|
Full agonists
|
|
|
|
These can produce only a submaximal response.
|
Partial agonists
|
|
|
|
These reduce the rate of signal transduction.
|
Inverse agonists
|
|
|
|
Rx that have receptor affinity but lack efficacy.
|
Antagonists
|
|
|
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The concentration of a Rx at the receptor site and the magnitude of the response.
|
Intrinsic activity
|
|
|
|
A continuous response when elicited that is described in terms of a percentage of the maximal response plotted against the log dose of the Rx.
|
Graded dose-response relationship
|
|
|
|
An all or none response that is described as a cumulative percentage of subjects exhibiting a defined all-or-none effect and is plotted against the log dose of the Rx
|
Quantal
|
|
|
|
T or F: some Rx can cause damage to specific organs while not damaging others.
|
T
|
|
|
|
List some ways in which Rx can interfere with each other.
|
Pharmacodynamic interactions
altered Rx absorption or distribution or biotransformation or excretion Rx- food interactions reaction between Rx |
|
|
|
In this population
the capacity to metabolize and excrete Rx is greatly reduced because of low levels of Rx biotransformation enzymes. |
Neonates and premature infants
|
|
|
|
In this population
first pass inactivation may be increased as well as a higher biotransformation rate. |
Children
|
|
|
|
In this age group
there is a higher volume of distribution for fat- soluble Rx. |
The elderly
|
|
|
|
In this age group
there is a reduced capacity to excrete Rx. |
Neonates
infants and the elderly |
|
|
|
Disease in these organs can result in reduced Rx clearance.
|
Liver and kidneys
as well as heart failure |
|
|
|
In the very young and the very old
what adjustment should be made in Rx prescribing? |
Dosage per kilogram should be reduced
|
|
|
|
What can result if dosages aren't reduced for liver and kidney disease patients?
|
Toxicity because of reduced metabolism and exertion
|
|
|
|
Is conjugation
oxidation or both usually reduced in liver disease? |
Oxidation
|
|
