Term
Define and describe on graph:
Potency
----------------------
Efficacy |
|
Definition
1) the size of the dose nec to produce a certain effect
often defined by ED(50) - the EFFECTIVE DOSE tat results in 50% maximal effect
***Potency is the first slope to rise off the graph
-----------------------------------
the maximal effect obtained by the drug
HIGHEST value on graph |
|
|
Term
| If a graph has A rise at a lover dose, but B rise higher, describe the EFFICACY and POTENCY |
|
Definition
| A has greater potency, but B has greater EFFICACY |
|
|
Term
What is importaint to remember when looking @ a graph:
X = DOSE
Y = Responce |
|
Definition
that we can judge POTENCY (fist to arrise at lower dose)
BUT
CANNOT judge Efficacy
here, the "efficacy" refers to percentage of individuals who respond to drug |
|
|
Term
| Potency can be used to dtr. ______, but cannot be said to determine _____ |
|
Definition
dose size
CANNOT dtr BETTER DRUG |
|
|
Term
D+R --> DR --> K(2)
K(1) K(2)
What is another term for k(2)? |
|
Definition
|
|
Term
| Name two drugs that increase the force of contraction of the heart; |
|
Definition
| ePINEPHRINE AND bETA ADRENERGIC RECEPTOR |
|
|
Term
| Trace the pathway of Epinephrine binding |
|
Definition
Epi binds Beta Adrenergic Receptor
G protein
Adenylyl Cyclase
CAMP (Cyclic Amp)
CAMP activates PHOSPHORELATION OF PROTEiNS
Thesphosphorelates quiescent calcium channel, allowing membrane depolarization
Therefore, more Ca enters cell, and SARCOMERE sees more Ca --> GREATER CONTRATION of heart musc |
|
|
Term
| Full agonists and partial agonists differ in ____ |
|
Definition
efficacy
They may or may NOT differ in potency |
|
|
Term
| ______ is a drug that produces a ceiling effect NOT exceeded by other similar drugs |
|
Definition
FULL AGONIST
drugs whose maximal effects are less, regardless of dose, are called partial agonists |
|
|
Term
Functional drug interactions with at TWO STATE RECEPTOR (active and inactive state):
1) NO preference for states
2) Extreme preference for active state
3)relative preference for active states
4)preference for INACTIVE STATE |
|
Definition
1)Inactive compound (often a functional antagonist)
2) Full Agonist
3)Partial Agonist
4) Inverse Agonist (Functionally significant only if the receptor has INHERENT ACTIVITY) |
|
|
Term
| T/F - Do drugs create denovo physiological effects? |
|
Definition
| NO -- they merely modify underlying processes |
|
|
Term
MAJOR RECEPTOR FAMILIES: 1 Cholinergic nicotinic receptors and GABA 2 A and B Adenergic Receptors 3 Insulin Recetor 4 Steroid Recptor |
|
Definition
1 Ligand - Gated ion chanel Rapid Responce Stimulation of Nicotinic Receptor by Acetylcholine results in Na influx and contraction of musc. 2 G Protein coupled Receptor 3 Enzyme Linked Receptor 4 Intracellular Receptor much longer time needed |
|
|
Term
| Enzyme linked receptors often have ___ in their structure: |
|
Definition
|
|
Term
|
Definition
the phenomenon of repeat admin of a drug results in diminished effect:
Can occur by receptor DOWNREGULATION, DESINSITIZATION, |
|
|
Term
| T/F: A competitive ANTAGONIST increases the ED(50) |
|
Definition
| True! in the presence of a compet. antagonist, a higher conc of drug is req to elicit a given responce. |
|
|
Term
| Variation in the sensitivity of a pop of individuals to increasing doses of a drug is best dtrmined by : |
|
Definition
| Quantal dose-response curves: |
|
|
Term
____ = a measure of a drugs safety
A large value indicates that these is a wide margin between doses that are effective and doses that are toxic. |
|
Definition
|
|
Term
| what is the significance of SPARE RECEPTORS? |
|
Definition
More receptors are present that are required for maximal resp.
This decreases the conc of agonist req for full effect
a single drug receptor interaction results in many cellular response elements being activated
***Noncompetitive antagoinsists can behaive like competative antagoinists with spare receptors |
|
|
Term
| name a competitive antagoinist for epinephrine |
|
Definition
|
|
Term
____ can be overcome by increasing the agonist
while
_____ ALWAYS decreases the maximal resp. |
|
Definition
Competitive antagonist
Nonocompetative antagoinist |
|
|
Term
give an example of IRREVERSIBLE BINDING of a competitive antagonist
explain mech |
|
Definition
Aspirin inhib of cyclo-oxygenase
blocks formation of PROSTOGLANDIN from Arach Acid
Req new synth of protein to overcome
Imp for using aspirin to prevent MI |
|
|
Term
t/f:
Noncomp. antagonists can behaive like comp. antag with spare receptors |
|
Definition
|
|
Term
| Formula for therapeutic index: |
|
Definition
lethal dose 50 / effective dose 50
higher number = safer |
|
|
Term
| In a dose percentage curve, EFFICACY ______ |
|
Definition
| is replaced by the maximum percent of patients responding to the drug |
|
|
Term
| Potency is DETERMINED in part by ______ |
|
Definition
| the affinity of the receptor for the drug |
|
|
Term
| formula for therapeutic index: |
|
Definition
|
|
Term
| List three drug mechanisms not involving a drug receptor |
|
Definition
Neut of GASTRIC ACID with base (antiacid)
MANNITOL - increases osmolarity of body fluids
Nucleotide analogs that are inc. into DNA |
|
|
Term
| _____ = special class of proteins whose role is to receive signals from other cells or to sense the outside environment of the cell |
|
Definition
|
|
Term
| List 3 edx of PANCRINE hormones |
|
Definition
Angiotensin II Somatostatin Prostoglandin |
|
|
Term
** this mechanism has an extracellular Receptor with Intracellular Enzymatic Activity.
It has IMMEDIATE response time, but longer term effects |
|
Definition
Receptor Tyrosine Kinases
common mech of hormones that reg growth and differentiation. |
|
|
Term
difference between: *********************** Nicotinic and Muscarinic |
|
Definition
* Muscarinic receptors are o found at the: post-ganglionic neurons of the parasympathetic nervous system, and o on many neurons in the brain (e.g. the ventral tegmental area). Glands. Bladder. Ciliary Muscle (relax) G Protein
muscarine (a toxin produced by certain mushrooms) is an agonist. o atropine is an antagonist (hence its use in acetylcholinesterase poisoning)
================================== * Nicotinic receptors are o found at the neuromuscular junctions of cardiac and smooth muscle as well as on o -the post-ganglionic neurons of the sympathetic nervous system. Ion Channel activated -nicotine is an agonist (hence the name) -curare is an antagonist (hence its ability to paralyze skeletal muscles) |
|
|
Term
Talk about inactivation of Norepinephrine, once released from synaptic vesicles by depolarization of an action potential:
2 PARTS*** |
|
Definition
MAO in mitochondria and COMT (in Cytoplasm) have MINOR roles in inactivation of NE
an Active TP system rapidly reuptakes Norepi back into the nerve terminal
**major mech for the inactivation of norepi transmitter takes place at adrenergic neuroeffector unctions |
|
|
Term
| talk @ MAO and COMT's role in NOREPI in nerve terminals |
|
Definition
MAO - Mitochondria
***Norepi that leaks out of vesicle is inactivated by MAO***
COMT - Cytoplasm of effector cells, liver, and kidney
Both have minor role in inactivating NE release from nerve ending by exocytosis |
|
|
Term
|
Definition
the MAJOR urinary metabolite of both EPI and NOREPI
**
(the major urinary metabolite of dopamine is HVA - Homovanillic Acid) |
|
|
Term
The major urinary metabolie of DOPA is _____
The major metabolite of NOREPI and EPI is ____ |
|
Definition
HVA - Homovanillic Acid
VMA - Vanillyl Mandelic Acid |
|
|
Term
| Norepi release at neuroeffector junct is inactivated mainly by : |
|
Definition
| the reuptake in the nerve ending |
|
|
Term
| ACH release at the neuroeffector junction is inactivated primarily by: |
|
Definition
degredation of ACH
Acetylcholinesterase cleaves ACH to choline and acetate in synaptic cleft |
|
|
Term
| List the responces of : B1 B2 A1 |
|
Definition
B1: SA - inc HR AV - inc conduction Atria and ventricles - inc contractility kidney - renin B2: Relax skel musc Bladder - Relax detrusor relax cilia of eye relax uterus relax BRONCH A1: Contract bv and skel musc Contract skin Trigone and sphinctor contract Iris contract Uterus contract |
|
|
Term
Muscarinic Receptor : ?Where? Describe the subtypes: |
|
Definition
| M1,3,5 are cellular EXCITATION M2,4 INHIBIT EXCITATION Post gang parasympathetic |
|
|
Term
What is ACH affect on heart and BV if injected? ** what drug inhibits this affect on BV?** ** what is another drug that counteracts the Nicotinic effects of poison gas?** |
|
Definition
Leads to a temporary DECREASE in heart rate and stroke volume, Mimics the VAGAL STIMULATION which uses ach Also causes VASODIALATION, lowering BP this is caused by inc. in intracell CA+ **ATROPINE blocks muscarinic receptors** Counteracts the effect of deficient ACH Cholinesterase, which result in an increase of ACH in nerve terminals, leading to too much muscarinic (Parasympathetic) activation Pralidoxine -- Helps at NICOTINIC SITES Promotes reactivation of ACH cholinesterase that has been phosphorylated-- Helps alieviate nueromusc junct --must be administered soon after poisoning!!!! |
|
|
Term
Which type of ion channel is: 1)G Protein Activated? 2) Ligand ion channel? |
|
Definition
1) Muscarinic Postgang parasympathetic ----------------------------- 2) Nicotinic Skelital, etc. |
|
|
