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69 Cards in this Set
- Front
- Back
Most drugs target ______
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Proteins
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True or False
A higher Kd (dissociation constant) means there is a greater affinity |
False
Lower Kd=Greater affinity |
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True or False
Drugs that target transporters will cause the channel to close after binding |
True
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What are the two types of Ion Channels that exist in the cell membrane?
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Ligand Gated
Voltage Gated |
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Many drugs work by ______ enzymes
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Inhibiting
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What are the 3 major types of receptors?
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Nuclear Hormone Receptors
Receptor Tyrosine Kinases G-Protein Coupled (GCPRs) |
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What receptor is found inside the cell cytoplasm? thus, the ligand must be hydrophillic or lipophillic?
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Nuclear Hormone Receptors
Ligand is lipophillic |
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Most common target receptor
Single protein that spans membrane 7 times |
G-Protein Coupled Receptor
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A single polypeptide that spans the membrane 1 time. Intracellular domain has phosphorylate proteins
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Receptor Tyrosine Kinase
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Which receptors have an extracellular binding domain?
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G-Protein
Tyrosine Kinase |
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At any point in time, receptors could in their inactive conformation (Ri) up to __%
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95%
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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 |
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Describe the G-Protein Cycle
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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 |
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When a ligand Binds a G-protein receptor, it becomes the ______ form
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Active
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Effector proteins are found on the ____ _____ of the membrane, and interact with the _ subunit
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Inner Leaf
Alpha |
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True or False
Effector proteins are specific to certain G-Proteins |
True
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Gs stimulates ________
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Adenylate Cyclase
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Gi inhibits ______
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Adenylate Cyclase
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Gq stimulates _____
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Phospholipase C
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Effector proteins activate ______ which cause an effect in the cell
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Second messengers
cAMP, IP3, DAG, Ca++ |
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A ligand with a much higher affinity for Ra than Ri
Ra>>>>>Ri |
Agonist
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A Ligand with a higher affinity for Ra, but some affinity for Ri
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Partial Agonist
Can reduce/inhibit effects of a full agonist |
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A Ligand with a higher affinity for Ri
Ra<<<<<<Ri |
Inverse Agonist
(Antagonist) |
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True or False
An inverse agonist can inhibit basal activity |
true
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A Ligand that binds to both Ra and Ri without changing the equilibrium
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Neutral Antagonist
Resists stimulation |
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Receptors are _____ due to a varying availability of receptors on the membrane surface
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Dynamic
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What is the term for "down regulation" where the initial agonist response is largest, followed by desensitization and a recovery time
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Tachyphylaxis
receptors are dynamic |
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why do receptors exhibit tachyphylaxis?
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As a defense mechanism for over stimulation
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What is the term for when prolonged use of an antagonist causes "up regulation" and the # of receptors can increase
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Supersensitivity
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______ is the movement of drug molecules from the site of administration to the blood stream
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Absorption
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what is the process of absorption done by most drugs?
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Passive Diffusion
(there is also active trans and carrier mediated) |
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The intestines are the major site of absorption for both acidic and basic drugs because of the large surface area created by _____ and _____
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Villi
Microvilli |
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food in the stomach _____ the GER
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lowers
gastric emptying rate |
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Process where the drug passes from circulation into the tissues
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Distribution
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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 |
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_____ cells and tight endothelial cells make the blood brain membrane difficult to pass
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Glial
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_____ like p-glycoprotein exist in cell membranes and only allow specific structures to pass
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Transporters
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______ is determined by the percentage of administered dose that makes it to circulation in its active form
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bioavailability
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Enzyme ______ reduce the metabolism of drugs by inhibiting the activity of CYP450
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Inhibitors
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Enzyme ______ increase the metabolism of drugs by stimulating more CYP450
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Inducers
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Flavenoids such as grapefruit
OTC Drug Cimetidine are ______ _______ |
Enzyme inhibitors
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Barbituates
Poly aromatic hydrocarbons Broiled meat Are ____ _______ |
Enzyme inducers
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Inherited difference that influence the response to drugs
can be therapeutic or adverse |
Pharmacogenomics
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Most pharmacogenomics deal with differences in metabolic enzymes --->
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Polymorphic P450
ex: one patient may have a different 3A4 than another |
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Term for when a single nucleotide in the sequence is altered
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SNP single nucleotide polymorphism
ex: A-T instead of C-G |
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A _____ Mutation is one that doesnt change the amino acid that is coded
(TCA --> TCC is still serine) |
Silent
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A _____ mutation results when a SNP causes a different amino acid
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Missense
Can be conservative or Non-conservative |
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What is the difference between conservative and non conservative missense mutations?
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Conservative=similar structure
Nonconservative=Completely different |
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A ______ mutation results when a SNP causes a stop codon to be inserted
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Nonsense
function might not be altered if it is not at the binding site |
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SNP's are more likely to _____ enzyme activity than _____ it
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more likely to decrease than increase
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True or False
SNP's are inherited and cannot be caused by the environment |
True
can be geographical/ethnic |
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People with low levels of N-Acetyl Transferase NAT are called ______ ________
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Slow acetylators lo[NAT]
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People with normal levels of NAT are called _____ _______
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Fast acetylators [NAT]
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A numerical response to a drug is called a _____ response
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Graded
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A yes/no response
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Quantal
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When a dose response curve plateau's it has reached maximum ______
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efficacy
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a drugs ______ is based off the amount the is needed to reach 50% of emax. ED50
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potency
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Additive effect
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1 + 1 = 2
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Synergy effect
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sum of 2 drugs is greater
1 + 1 = 3 |
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Potentiation effect
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inactive drug helps active drug cause effect
1 + 0 = 2 |
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_____ ______ gives an idea about safety of a drug
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Therapeutic index
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what is the formula for therapeutic index?
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ED50 AE/ED50TE
larger # is safer! |
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What would happen to the curve with competitive antagonism?
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shifts right
capable of reaching same Emax less potent |
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What would happen to the curve with noncompetitive antagonism?
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shifts right
decrease Emax |
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what nervous system?
non voluntary rest/digest glands, smooth muscle ganglions |
Autonomic nervous system
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what nervous system?
Voluntary movement fight/flight straight path to target |
somatic nervous system
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CNS-->Ach-->Nicotinic-->Ach-->Muscarinic
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Parasympathetic
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CNS-->Ach-->Nicotinic-->NE-->Adrenergic
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Sympathetic
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CNS-->Adrenal Medulla-->E-->blood-->E at Adrenergic receptor
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Adrenal Sympathetic
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