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105 Cards in this Set

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Determines the duration of action of Drug.
Biotransformation
Main Organ of biotransformation
Liver
Important for orally administered drugs to be metabolized.
Gi tract, Upper Intestine
Participates in entero-hepatic cycling of glucoronides.
Liver and upper intestine
Important site for basic drugs and inhaled drugs
Lungs
Biotransforms dermally applied drugs
Skin
Helps eliminate some drugs in urine
Kidney
May be important for CNS active drugs
Brain
Age and gentic make up effect on metabolism
Internal ( intrinsic)
How Nutrition, Food, Disease state, other drugs effect metabolism.
External ( environmental )
Discovered with debrisoquine, metabolizes many N-containing drugs, 1-15 % are poor metabolizers, low doses given to those who are lacking this enzyme.
CYP2D6
First shown with mephenytoin, Oriental poor metabolizers have less of this enzyme.
CYP2C19
Low rates of conjugation of bilirubin are because lack of this enzyme.
UGT-1 family
Newborns have low levels of this enzyme.
UGT
Metabolism decreases when this number increases.
Age ( as you get older metabolism decreases.)
First recognized polymorphism, affects the metabolism of drugs like isoniazid.
NAT-2
Asian and natives have a low incidence of this.
Slow acetylators
Swedish have 70% and US has 50 % of this.
Slow acetylators
Omeprazole induces this enzyme
CYP1A2
Phenobarbital and Carbamezpine induce this enzyme
CYP2 and 3
Isoniazid induces this enzyme
CYP2E1
What you do with hot tea or coffee
CYP slowly
Rifampicin induces this enzyme
CYP3A4 and 5
Clofibrate induces this enzyme
CYP4
UGT and GST are induced by this drug
Phenobarbital and othe barbiturates
Oltipraz can induce this enzyme
GST
CYP1A2 can be induced by these
Tobacco, Charbroiled foods
CYP1 and 2 can be induced by these
PCBs and DDT
Alcohol can induce this CYP
2E1
St. Johns wart is an inducer of this enzyme
CYP3A4
Bioflavaniods and garlic and onion are weak inducers of these enzymes
CYP, GST
Perservatives can induce these enzymes
GST and UGT
Green tea and black tea can induce 3 enzymes name them
CYP, UGT, GST
Can down regulate CYP2 and 3 family members during viral infections
Interferons or cytokines
This liver disease leads to lowered levels of enzymes
Cirrhosis
Most variable of all CYP enzymes
2D6
Least variable of the CYP enzymes
2E1 and 3A4/5
Present in higher concentration than PAPS
UDP- glucoronic acid
These are usually present in high concentrations
GSH and NADPH and NADH
GSH level decrease when this decreases
Nutrition
Malnutrion of aa can lead to this
Reduced aa conjugation
Ethanol consumptions lowers this
NADPH
Indinavir and saquinavir are both substrates for this enzyme
CYP3A4
Inhibits CYP3A4 by binding to it
Erythromycin metabolites
Ketoconazole and other imiidizole containing drugs inhibit this enzyme
CYP
The products in Grapefuit that inhibit CYP3A4
Furnocoumarins and flavanoids
This is when a receptor binding causes a biological activity
Intrinsic activity (alpha factor)
GABA-A is this type of channel
Cl- gated
All glutamate receptor types
Cation channels
Inhibits Calcium channels
Go
Activates potassium channels
Gi
Activates Calcium channels
Gs
Gq activates this
PLC
PLC makes
IP3 and DAG
Gq uses this for of energy to activate this
GDP becomes GTP to activate PLC
IP3 frees this cation
Calcium
Calcium activates this
Protein Kinases
DAG activates this
PKC
Activates AC to increase cAMP
Gs
Does the opposite of Gs
Gi
Gs uses this ase energy form to activate AC
GTP
cAMP is inactivated by this (Viagra)
Phosphodiesterases
PKA is activated by cAMP when this energy form is used
ATP
Is activated by Gi to make PG
PLA2
When proteins are modified by this they do things
Phosphorylation
Decreases the chance of an AP, and is located on the dendrites or cell bodies.
Impulse modulating autoreceptors
Autoreceptor located on presynaptic terminals and inhibits NT syn
Synthesis modulating autoreceptor
Autoreceptor located on presynaptic terminals inhibits NT release
Release modulating autoreceptors
What the body does to the drugs (ADME)
Pharmacokinetic
What the body does to the drug (DDC)
Pharmacodynamics
Means Poison or Drug
Pharmakon
Drugs for different folks
Pharmacogenomics
Adverse effects of chemical compounds. Includes environmental exposure.
Toxicology
This act required that safety testing and labels be accurate and complete
1938: Federal Food, Drug and Cosmetic Act
Amendment responsible for the "Caution: Federal law prohibits dispensing without prescription" on Rx bottles
1951: Durham-Humphrey
Kefhauver-Harris Amendment: Required testing for both safety and effectiveness for new drugs and ones between1938 and _____
1962
Drugs come from different sources this is the main source
Plant or Animals
Most drugs are used to
Treat symptoms
13000
RX drugs available
2-3 weeks
New drug approved
Most of the times people see doctors they get this
RX
Old people take this
25% of RX
Ptenet life for a drug in US
20 years
To do clinical trials you submit this to fda
IND
When you submit NDA to FDA it takes this long for them to approve
20-24 months
CAST looked at
PVC-premature ventricular contractions
Rezulin taken of market because
Heart and Liver failures
Vioxx pulled of market for this
Increased risk of MI or Heart problems
Not approved for use by FDA
Combo of Phen-Fen
Full agonist
Alpha = ?
alpha = 1
Partial agonist
Alpha = ?
0 < alpha < 1
Antagonist
Alpha = ?
alpha = 0
Full agonist elicits?
Emax at Bmax
Partial agonist never elicits?
Emax
Noncompetitive shifts?
Emax downward
NO effect on EC50 or slope
Competitive shifts?
EC50 to the right
NO effect on Emax or slope
Inverse agonist
Alpha = ?
-1 < alpha < 0
Inverse agonist can resemble?
Antagonist
Bmax =?
Max number of binding sites in tissue sample
Bmax found when?
Drug concentration has saturated the receptors
Bmax measures?
Occupancy
NOT activity
Kd =?
Drug concentration occupies half of Bmax
2 things that can change Kd?
Structural specificity
Stereoselectivity
Hill Plot: ?
Determines if dose response or binding curve has a normal slope
Hill plot is a ?
linear version of log-dose graph