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69 Cards in this Set

  • Front
  • Back
Most drugs target ______
Proteins
True or False
A higher Kd (dissociation constant) means there is a greater affinity
False
Lower Kd=Greater affinity
True or False
Drugs that target transporters will cause the channel to close after binding
True
What are the two types of Ion Channels that exist in the cell membrane?
Ligand Gated
Voltage Gated
Many drugs work by ______ enzymes
Inhibiting
What are the 3 major types of receptors?
Nuclear Hormone Receptors
Receptor Tyrosine Kinases
G-Protein Coupled (GCPRs)
What receptor is found inside the cell cytoplasm? thus, the ligand must be hydrophillic or lipophillic?
Nuclear Hormone Receptors

Ligand is lipophillic
Most common target receptor
Single protein that spans membrane 7 times
G-Protein Coupled Receptor
A single polypeptide that spans the membrane 1 time. Intracellular domain has phosphorylate proteins
Receptor Tyrosine Kinase
Which receptors have an extracellular binding domain?
G-Protein
Tyrosine Kinase
At any point in time, receptors could in their inactive conformation (Ri) up to __%
95%
True or False
Both the active and inactive form of a receptor can link to its G-protein
False
only the active (Ra) can bind
Describe the G-Protein Cycle
G-Protein binds Ra
Conformation change- GDP dissociates
GTP binds to G-protein
alpha subunit dissociates with GTP(from beta,gamma)
alphaGTP binds effector proteins
GTP phosphorylated to GDP and G-protein reassociates
When a ligand Binds a G-protein receptor, it becomes the ______ form
Active
Effector proteins are found on the ____ _____ of the membrane, and interact with the _ subunit
Inner Leaf
Alpha
True or False
Effector proteins are specific to certain G-Proteins
True
Gs stimulates ________
Adenylate Cyclase
Gi inhibits ______
Adenylate Cyclase
Gq stimulates _____
Phospholipase C
Effector proteins activate ______ which cause an effect in the cell
Second messengers
cAMP, IP3, DAG, Ca++
A ligand with a much higher affinity for Ra than Ri
Ra>>>>>Ri
Agonist
A Ligand with a higher affinity for Ra, but some affinity for Ri
Partial Agonist
Can reduce/inhibit effects of a full agonist
A Ligand with a higher affinity for Ri
Ra<<<<<<Ri
Inverse Agonist
(Antagonist)
True or False
An inverse agonist can inhibit basal activity
true
A Ligand that binds to both Ra and Ri without changing the equilibrium
Neutral Antagonist

Resists stimulation
Receptors are _____ due to a varying availability of receptors on the membrane surface
Dynamic
What is the term for "down regulation" where the initial agonist response is largest, followed by desensitization and a recovery time
Tachyphylaxis

receptors are dynamic
why do receptors exhibit tachyphylaxis?
As a defense mechanism for over stimulation
What is the term for when prolonged use of an antagonist causes "up regulation" and the # of receptors can increase
Supersensitivity
______ is the movement of drug molecules from the site of administration to the blood stream
Absorption
what is the process of absorption done by most drugs?
Passive Diffusion

(there is also active trans and carrier mediated)
The intestines are the major site of absorption for both acidic and basic drugs because of the large surface area created by _____ and _____
Villi
Microvilli
food in the stomach _____ the GER
lowers

gastric emptying rate
Process where the drug passes from circulation into the tissues
Distribution
True or False

The drug has effect with its target protein when it is bound to plasma proteins
False

The unbound "free portion" has the effect
_____ cells and tight endothelial cells make the blood brain membrane difficult to pass
Glial
_____ like p-glycoprotein exist in cell membranes and only allow specific structures to pass
Transporters
______ is determined by the percentage of administered dose that makes it to circulation in its active form
bioavailability
Enzyme ______ reduce the metabolism of drugs by inhibiting the activity of CYP450
Inhibitors
Enzyme ______ increase the metabolism of drugs by stimulating more CYP450
Inducers
Flavenoids such as grapefruit
OTC Drug Cimetidine

are ______ _______
Enzyme inhibitors
Barbituates
Poly aromatic hydrocarbons
Broiled meat

Are ____ _______
Enzyme inducers
Inherited difference that influence the response to drugs
can be therapeutic or adverse
Pharmacogenomics
Most pharmacogenomics deal with differences in metabolic enzymes --->
Polymorphic P450

ex:
one patient may have a different 3A4 than another
Term for when a single nucleotide in the sequence is altered
SNP single nucleotide polymorphism

ex: A-T instead of C-G
A _____ Mutation is one that doesnt change the amino acid that is coded
(TCA --> TCC is still serine)
Silent
A _____ mutation results when a SNP causes a different amino acid
Missense

Can be conservative or Non-conservative
What is the difference between conservative and non conservative missense mutations?
Conservative=similar structure
Nonconservative=Completely different
A ______ mutation results when a SNP causes a stop codon to be inserted
Nonsense

function might not be altered if it is not at the binding site
SNP's are more likely to _____ enzyme activity than _____ it
more likely to decrease than increase
True or False
SNP's are inherited and cannot be caused by the environment
True

can be geographical/ethnic
People with low levels of N-Acetyl Transferase NAT are called ______ ________
Slow acetylators lo[NAT]
People with normal levels of NAT are called _____ _______
Fast acetylators [NAT]
A numerical response to a drug is called a _____ response
Graded
A yes/no response
Quantal
When a dose response curve plateau's it has reached maximum ______
efficacy
a drugs ______ is based off the amount the is needed to reach 50% of emax. ED50
potency
Additive effect
1 + 1 = 2
Synergy effect
sum of 2 drugs is greater
1 + 1 = 3
Potentiation effect
inactive drug helps active drug cause effect
1 + 0 = 2
_____ ______ gives an idea about safety of a drug
Therapeutic index
what is the formula for therapeutic index?
ED50 AE/ED50TE

larger # is safer!
What would happen to the curve with competitive antagonism?
shifts right
capable of reaching same Emax
less potent
What would happen to the curve with noncompetitive antagonism?
shifts right
decrease Emax
what nervous system?
non voluntary
rest/digest
glands, smooth muscle
ganglions
Autonomic nervous system
what nervous system?

Voluntary movement
fight/flight
straight path to target
somatic nervous system
CNS-->Ach-->Nicotinic-->Ach-->Muscarinic
Parasympathetic
CNS-->Ach-->Nicotinic-->NE-->Adrenergic
Sympathetic
CNS-->Adrenal Medulla-->E-->blood-->E at Adrenergic receptor
Adrenal Sympathetic