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S3.M1.Pharm6,7
Pharmacodynamics
30
Pharmacology
Professional
05/20/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
The site of action is not an indication of the quality of the effect
Definition
Term
what are the two SITES OF DRUG ACTION?
Definition
1) NON CELLULAR SITES (actions occurring mainly in the extracellular fluids of the body)
2) CELLULAR SITES
Term
Drugs cause characteristic effects in some tissue and don't in others suggesting that-
Definition
RECEPTORS in tissue=characteristic effect
no receptor in tissue= no effect
Term
what is a DRUG RECEPTOR?
Definition
any cell component to which a drug binds to initiate the chain of biochemical events leading to the drug’s observed effects
Term
what are the main classes of DRUG RECEPTORS?
Definition
1) Regulatory proteins
2) Ion channel proteins
3) Enzymes
4) Carrier proteins
5) Structural proteins
Term
what are some PROPERTIES of RECEPTORS?
Definition
1. SPECIFICITY-few drugs can bind one receptro
2. STEREO SELECTIVITY-only one isomer binds
3. SENSITIVITY-elictis effects at low concentrations
4. VARIABILITY-number of receptors fluctuates
Term
what are the types of CHEMICAL BONDS that can be made between drugs and receptors?
Definition
covalent, ionic, hydrogen, hydrophobic, van der waals forces (hydrogen and van der waals most common)
Term
what is the AFFINITY of a drug?
Definition
tendency of a drug to bind to a receptor
Term
what are the two DRUG RECEPTOR INTERACTIONS
Definition
1. ACTIVATION-->results in biological response
2. BLOCKADE-->blocks other responses
Term
what are the AGONIST CLASSES?
Definition
1. FULL-produces maximal response
2. PARTIAL-response below maximum
3. INVERSE-decreases basal activity
Term
what is an ANTAGONIST?
Definition
A drug which, when bound to the receptor, fail completely to produce any activation of that receptor
Term
the DOSE-EFFECT RELATIONSHIP is described by what type of curve?
Definition
hyperbolic curve
Term
the LOG DOSE EFFECT RELATIONSHIP is described by what type of curve?
Definition
sigmoid curve
Term
what does it mean when a system has SPARE RECEPTORS? what effect do they have on the system?
Definition
the receptor pool of the system is larger than the number needed to evoke a full response-->increase sensitivity to a drug
Term
what is CHEMICAL ANTAGONISM?
Definition
drug combines chemically with the drug to be antagonized so making that drug pharmacologically inactive
Term
what is PHARMACOKINETIC ANTAGONISM?
Definition
when a drug prevents the absorption or stimulates the elimination of the drug to be antagonized, so reducing its concentration at the site of action
Term
what is PHYSIOLOGICAL ANTAGONISM?
Definition
occurs when a drug response mediated by the activation of a receptor is antagonized by an opposite response produced by another drug acting on a DIFFERENT RECEPTOR
Term
what is PHARMACOLOGICAL ANTAGONISM?
Definition
agonist and antagonist compete for the same receptor type and therefore the antagonist prevents in some way the activation of the receptor normally activated by the agonist
Term
characteristic of RECEPTOR BLOCK COMPETITIVE ANTAGONISM?
Definition
-agonist and antagonists compete for receptors -decreases affinity of agonist
-antagonism is surmountable by increasing agonist
-shifts log/dose effect curve to the RIGHT
Term
how is RECEPTOR-BLOCK IRREVERSIBLE ANTAGONISM different than competitive antagonism?
Definition
-antagonist binds irreversibly--> cant be surmounted, is uncompetitive
-increased antagonist binding decreases maximal effect of agonist (decreased slope of log dose effect curve)
Term
The lower the dose required to produce the effect, the higher the ______?
Definition
potency
Term
EFFICACY of a drug is directly proportional to what?
Definition
INTRINSIC ACTIVITY (ability of drug to produce biological response)
Term
what does the SLOPE of the LOG DOSE RESPONSE CURVE indicate?
Definition
the range of doses that are useful for achieving a given effect
Term
what is the THERAPEUTIC DOSE?
Definition
the ratio between an harmful dose and an
effective dose of a drug
Examples: LD50 / ED50 ; TD50 / ED50 ; TD1/ED99
Term
what is the THERAPEUTIC WINDOW?
Definition
the range between the minimum therapeutic dose (or plasma concentration) and the minimum toxic dose (or plasma concentration) of a drug
Term
what are the five classes of REGULATORY RECEPTORS?
Definition
-intracellular receptors
-ion channel linked receptors (ionotropic)
-transmembrane enzyme linked receptor
-Janus kinase linked receptor
-G protein linked receptor (metabotropic)
Term
how are drug receptors regulated with time and use?
Definition
chronic activation of receptors=desensitization and down regulation
CHRONIC INHIBITION = up regulation and hypersensitivity
Term
what are some things that lead to NONCOMPLIANCE of patients with medications?
Definition
-poor physician relationship
-side effects
-variable symptoms
-patient doesn't believe the disease is serious, or the treatment is effective
Term
what is POTENTIATION in terms of DRUG DRUG interactions?
Definition
0+1>1 -A drug which has no effect by itself enhances the effect of another drug
Term
what are some features of DRUG TOLERANCE?
Definition
not all drugs, variable in rate of development or person, related to a given dose, may disappear or be reversed
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