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1.20 Pharmacology
By Dr. Backes
70
Pharmacology
Professional
01/20/2012

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Cards

Term
Where in the body are reductases found?
Definition
ER, cytosol, anaerobic gut microorganisms
Term
What are the different types of reduction reactions?
Definition
azoreduction, nitroreduction, ketoreduction
Term
Where do hydrolysis reactions take place?
Definition
plasma, liver, kidney, and all tissues
Term
What types of enzymes catalyze hydrolysis reactions?
Definition
esterase, amidase, and epoxide hydrolase
Term
What is succinylcholine apnea?
Definition
dut to an esterase deficiency, enzyme appears to have an altered affinity for esters, affects about 1/3000
Term
Where is epoxide hydrolase found?
Definition
liver and all tissues
Term
What are the two forms of epoxide hydrolase?
Definition
microsomal and soluble forms
Term
What induces epoxide hydrolase?
Definition
phenobarbital and 3 methylcholanthrene
Term
What induces epoxide hydrolase?
Definition
phenobarbital and 3 methylcholanthrene
Term
What types of reactions happen in phase 2 conjugation reactions?
Definition
glucouronidation, sulfate conjugation, acetylation, glutathione conjugation, methylation, glycine conjugation
Term
What enzyme is used for glucuronide conjugation?
Definition
UDP-glucuronyl-transferase
Term
What enzyme is used for sulfate conjugation?
Definition
sulfotransferase
Term
What enzyme and substrate are used for acetylation?
Definition
acetyl CoA, N-acetyltransferase
Term
What enzyme is used for glutathione conjugation?
Definition
glutathione S transferase
Term
What enzymes perform methylation?
Definition
methyltransferases
Term
Where are methyltransferases located within the cell?
Definition
cytoplasm and ER
Term
What activated molecule is used for methylation?
Definition
S-adenosylmethionine
Term
Which amino acid is most often used in conjugation reactions?
Definition
glycine
Term
Where in the cell does amino acid conjugation occur?
Definition
mitochondria and cytoplasm
Term
What factors of an organism will affect drug metabolism?
Definition
genetics, aging, species differences
Term
Why do the elderly have a lower drug clearance?
Definition
decreased absorption, altered distribution, decreased metabolism, decreased excretion
Term
What is the equation for the rate of elimination?
Definition
Vel = Kel * [A]
Term
What value is equal to the slope of the line plotted on a log [drug] over time?
Definition
Kel
Term
What functional groups does glucuronidation react with?
Definition
hydroxyl, amine, or carboxylic acid
Term
Where in the cell does glucuronidation occur?
Definition
ER
Term
What fuctional groups does sulfate conjugation occur with?
Definition
alcohols, phenols, and aromatic amines
Term
Where does sulfate conjugation occur?
Definition
the cytosol
Term
Where does acetylation occur?
Definition
the cytosol
Term
Name 2 conjugation reactions that are saturable.
Definition
sulfate and glycine conjugation
Term
What functional groups does acetylation occur with?
Definition
primary amines
Term
Are most people in the US slow or fast acetylators?
Definition
slow
Term
What racial groups are rapid acetylators? slow acetylators?
Definition
japanese are rapid acetylators
middle eastern, scandanavians, finns are slow
Term
W
Definition
Term
Slow acetylators are at risk for:
Definition
isoniazid-induced neurotoxicity, drug-induced SLE, and arylamine induced bladder cancer
Term
Fast acetylators are at risk for:
Definition
isoniazid induced hepatitis, and colorectal cancer (esp with rapid CYP1A2 type)
Term
What functional groups react in methylation reactions?
Definition
hydroxyl, sulfhydryl, and amine
Term
Where do glutathione conjugation reactions take place?
Definition
cytosol and mitochondria of liver and numerous other tissues
Term
Describe the structure of glutathione conjugation enzymes:
Definition
functional dimer
Term
What type of conjugation reactions can ultimately form mercapturic acids?
Definition
glutathione conjugation
Term
What types of functional groups participate in glutathione conjugations?
Definition
aromatic hydrocarbons (epoxides), arylamines, organic halides, phenols, and ligand binidng cpabilities (ligandins)
Term
How do you induce alpha class GSTs?
Definition
ingestion of high levels of brussel sprouts
Term
What are the polymorphisms of glutathione conjugation?
Definition
four classes (GSTM1-4)
Term
Describe GSTM1.
Definition
polymorphic (*0, 8a, and *b); null gene (increased risk of cancer), essentially absent in 20-50% of all individuals
Term
How many variants of GSTP1 are there?
Definition
four
Term
GSTM1 null phenotype is linked to what cancers?
Definition
pituitary adenomas, head and neck cancer, malignant melanoma, colorectal cancer, and bladder carcinoma
Term
Is GSTM1 null phenotype associated with lung cancer?
Definition
yes but only in heavy smokers
Term
What functional groups participate in glycine conjugation?
Definition
aliphatic acids and aromatic carboxylic acids
Term
Name a type of conjugation reaction that is developmentally induced
Definition
glycine conjugation
Term
What effect do ethanol and cimantidine have on drug metabolism
Definition
inhibition
Term
Name drugs that induce P450 and other drug metabolizing enzymes.
Definition
phenobarbital and other drugs, polycyclic hydrocarbons and carcinogenesis
Term
What dietary elements can affect drug metabolism?
Definition
charcoal broiled beef, vitamin deficiencies, brussel sprouts, grapefruit
Term
What is the relationship between the half life and the elimination constant?
Definition
t1/2= .693/kel
Term
What is the volume of distribution?
Definition
apparent volume into which a drug distributes in the body
Term
How do you calculate a volume of distribution?
Definition
inject a known quantity of drug as an IV bolus. take blood samples at various times after injection. Plot data on a semilogarithmic plot and extrapolate back to t=0 to calculate the concentration prior to elimination. VD= amount of drug/plasma concentration = X0/Cp
Term
List three equations that equal total clearance.
Definition
ClT = Kel * VD
CLT = X0/area under the curve
CLT = Cl(liver) + CL(kidney) + Cl(other)
Term
Describe an equation for rate of absorption.
Definition
V(abs) = K(abs) + [A]
Term
What is bioavailability?
Definition
area under the curve of drug [] over time
Term
What is the C(ss)?
Definition
infusion rate/Cl(T)
Term
How do you calculate teh total clearance of a drug administered IV.
Definition
ClT= X0/AUC
Term
How do you calculate total clearance in a drug that is administered extravascularly?
Definition
F*X0/AUC
Term
What is the extraction ratio for hepatic clearance?
Definition
E= (Q*Cin - Q*Cout)/Cin
Term
What is the hepatic clearance for first order drugs?
Definition
Cl(H) = Q*E
Term
What is the hepatic clearance for zero order drugs?
Definition
ClH = Fu * Cl(int), where Cl(int) = Vmax/Km
Term
Renal clearance is related to the rates of...
Definition
glomerular filtration, passive reabsorption, and active secretion
Term
Which type of drug reaches a steady state faster, those with a long half life or those with a short half life?
Definition
short half life
Term
If renal clearance is greater than GFR, the the drug is being excreted by...
Definition
tubular secretion
Term
If renal clearance is less than GFR then several mechanisms may be responsible such as...
Definition
protein binding, tubular reabsorption, depressed GFR
Term
T/F The area under the curve for a drug given IV is greater than the area under the curve of the same drug given extravenously.
Definition
true
Term
What is the equation for continuous IV infusion
Definition
Vin=K0
Term
The inital dose of a medicine which is greater than the following doses is termed a ________.
Definition
loading dose
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