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
|
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
|
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
|
|
Term
| the LOG DOSE EFFECT RELATIONSHIP is described by what type of curve? |
|
Definition
|
|
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
|
|
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 |
|
|
