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Chapter 3
Pharmacodynamics
49
Psychology
Graduate
02/10/2017

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Term
Pharmacodynamics
Definition
Exploring the mechanisms of a drug action that occur at the molecular level. "What the drug does to the body."
Term
Principle of Pharmacology
Definition
The pharmacological, physiological, or behavioral effects induced by a drug follow from their interaction with receptors.
Term
Pharmacokinetics
Definition
The study of what the body does to a drug.
Term
Receptor
Definition
Fairly large molecule at which endogenous transmitters or modulars produce their biological effects.
Term
Affinity
Definition
Strength of attachment.
Term
Ion Channel
Definition
The central portion of the receptros spans the membrane of the neuron and forms a pore, which enlarges when either an endogenous neurotransmitter or exogenous drug attaches to the receptor- binding site.
Term
G-Protein-Coupled Receptors
Definition
The activation of these receptors induces the release of an attached intracellular protein that, in turn, controls enzymatic functions within the post-synaptic neuron.
Term
1. Ionotropic 2. G-Protein 3. Carrier Proteins 4. Enzymes
Definition
The four types of receptor proteins
Term
Second Messengers
Definition
Intracellular enzymes.
Term
Carrier Proteins
Definition
Receptor that transports small organic molecules across cell membranes against concentration gradients.
Term
(Reuptake) Carrier Proteins
Definition
Pre-synaptic carrier proteins that bring dopamine, epinephrine, serotonin, etc. back into the pre-synaptic nerve terminal.
Term
Enzymes
Definition
Regulate the synaptic availability of certain neurotransmitters. Inhibition of these increase the availability of neurotransmitters.
Term
Isomers
Definition
Molecules formed around a carbon atom that have the same molecular formula but have different arrangement of their atoms in space.
Term
Enantiomers
Definition
Simple substances that show optical isomerism exist as two (or more) isomers.
Term
Racemic Mixture or Racemate
Definition
Most medicines are manufactured this way. Medications are often produced as a 50/50 mixture of their two enantiomers. It is the mixture of 50% active and 50 % inactive that is marketed. Although only the (-) half of the medicine will be biologically active in the body.
Term
Total effect of the drug
Definition
1. On one specific type of receptor 2. At different types of receptors.
Term
Side Effects
Definition
Additional responses to the drug.
Term
Down Regulation (Desensitization)
Definition
In the presence of chronic stimulation the number of receptor sites decreases.
Term
Up Regulation (Super Sensitivity)
Definition
When the number of transmitter molecules available at postsynaptic receptors is decreased.
Term
Dose-Response Curve (DRC)
Definition
A function that describes the relationship between the dose of a drug and the magnitude of the drug's effect.
Term
Potency
Definition
The amount of drug required to produce a given effect.
Term
Variability
Definition
Refers to individual differences in drug response; some patients respond at very low doses and some require much more drug.
Term
Slope
Definition
The relationship between the dose of a drug and its effect, as measured within the more or less linear (straight) central portion of the dose-response curve.
Term
Flat/Shallow Slope
Definition
Large increases in dose do not produce big changes in effect.
Term
Steep Slope
Definition
There is only a small difference between the dose that produces a barely discernible effect and the dose that causes a maximal effect.
Term
Efficacy
Definition
The ability to produce a desired effect. The dose that exerts the maximum effects obtainable has 100% _______.
Term
Agnositic Action
Definition
Binding to a receptor site can initiate a cellular response similar or identical to that exerted by the natural transmitter.
Term
Full Agonist
Definition
Drug capable of eliciting the maximum response from a receptor system.
Term
Partial Agonist
Definition
Agonist that is unable to induce maximal activation of a receptor population, regardless of the amount of drug applied.
Term
Allosteric Action
Definition
This drug may not produce an effect by itself, but, in the presence of the natural transmitter.
Term
Positive allosteric effect
Definition
Increase the response of the transmitter.
Term
Inhibitory allosteric effect
Definition
Decrease the response of the transmitter.
Term
Antagonistic Action
Definition
Drug that blocks access of the transmitter to the site, preventing the normal effect of the transmitter or displaces transmitters.
Term
Inverse Agonist
Definition
Drug that binds to a receptor site that produces the opposite pharmacological effect of an agonist
Term
Competitive Antagonist
Definition
Bind in a reversible way. They attach to the receptor yet do not stimulate the effector system for the receptors.
Term
Noncompetitive Antagonist
Definition
Irreversible. THe actions of a non-competitive antagonist cannot be overcome by increasing the dose of agnonist because they have different binding sites.
Term
Core Parts of Pharmacodynamics
Definition
1. Agonists bind to receptors to produce a functional response
2. Agonists can be full, partial, or inverse.
3.Antagonists block or reverse the effects of agonists.
4. Antagonists can be competitive or noncompetitive/irreversible.
Term
Therapeutic Index
Definition
The ratio of the LD50 to the ED 50 is used as an index of the relative safety of the drug.
Term
Margin of Safety
Definition
The ratio of LD1 to ED 99.
Term
Polypharmacy
Definition
Combining medications to improve therapeutic outcome.
Term
Principles for "Irrational Polypharmacy"
Definition
1. Pharmacodynammic Redundancy 2. Pharmacodynamic interactions 3. Pharmacokinetic Interactions
4. Inadequate Dosing
5. Clinical Evaluation and Oversight.
Term
Pharmacodynamic Redundancy
Definition
Two drugs have the same or overlapping mechanism of action
Term
Pharmacodynamic Interactions
Definition
When the effect of two medications oppose each other.
Term
Pharmacokinetic Interactions
Definition
Certain drugs might either increase or decrease the rate of hepatic metabolism of other drugs and how this interaction can affect the plasma levels of other drugs metabolized by the same enzymes.
Term
Inadequate Dosing
Definition
Dose are too low beacuase of side effects. Sometimes the medication is given at a dose that is sufficient for one action, but not high enough for a second pharmacological action to be effective. Possible cause: Polypharmacy.
Term
Clinical Evaluation and Oversight
Definition
Drugs started during exacerbation of an illness might need to be reassessed after the patient has restablized. The natural history of the disorder might produce spontaneous remission, allowing dose reduction or elimination. The appearance of new symptoms might be a result of long-term drug exposure which would be better treated by reassessment of the medication instead of adding a new agent.
Term
Serotonin Syndrome
Definition
Rare, but potentially serious untoward response caused by excess serotinergic action at 5-HT2A and 5_HT1A receptors in the central and peripheral nervous system.
Term
Symptoms of Serotonin Syndrome
Definition
Altered mental states: delirium, clonus, tremor, hyperthermia, tachycardia, akathisia
Term
Serious Drug Reactions
Definition
Allergies, blood disorders, liver or kidney toxicity, abnormalities in fetal development.
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