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44 Cards in this Set
- Front
- Back
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What are 7 common and useful assay detection methods? |
Colorimetric Fluorometric Chemiluminescent Radiometric GFP ELISA FRET |
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What are 3 assay limitations? |
Accuracy Reproducibility Log Scale |
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The body has developed a sophisticated method for dealing with xenobiotics. What is Absorption? (ADME) |
How the “drug” gets into the bloodstream |
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The body has developed a sophisticated method for dealing with xenobiotics. What is Distribution? (ADME) |
How the “drug” gets from the bloodstream to the rest of the body |
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The body has developed a sophisticated method for dealing with xenobiotics. What is Metabolism? (ADME) |
How the “drug” is chemically transformed in the body |
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The body has developed a sophisticated method for dealing with xenobiotics. What is Excretion? (ADME) |
How the “drug” is eliminated from the body |
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What are the primary methods of drug Absorption? |
iv – intravenous
p.o. – per os (by mouth – oral)
inh - inhalation
ip – intraperitoneal (only relevant in animal models) |
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How do oral “drugs” get into the bloodstream? |
They don’t pass between the epithelial cells. They have to go THROUGH the epithelial cells of the small intestine. |
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Xenobiotics that can pass through the epithelial cells of the small intestine are deposited into the _________ ________ vein |
Xenobiotics that can pass through the epithelial cells of the small intestine are deposited into the hepatic portal vein |
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The portal vein takes these xenobiotics to the _______. |
The portal vein takes these xenobiotics to the liver |
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How do inhaled “drugs” get into the bloodstream? |
The alveoli are lined with epithelial cells, drugs pass THROUGH those cells. Inhaled “drugs” pass from the alveoli into the pulmonary vein. |
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What is a huge difference between oral and inhaled drugs? |
Inhaled xenobiotics do not have to pass through the liver before entering the heart. |
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Ultimately, all non-injected routes of administration have to pass through ____ to be absorbed |
Ultimately, all non-injected routes of administration have to pass through cells to be absorbed |
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What is Albumin? |
The most abundant plasma protein. With its deep hydrophobic clefts that often contain charged residues, albumin binds to most xenobiotic compounds and prevents them from passing through the pores in the capillaries |
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Xenobiotics pass from _____ to ____. |
Xenobiotics pass from plasma to cells. |
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What are the four factors that contribute to the overall pharmacokinetics of a drug? |
ADME! Absorption, Distribution, Metabolism, and Excretion. |
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What is the site for all metabolism? |
The liver. |
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What are three mechanisms the liver has to chemically modify drugs in the body? |
The liver has several mechanisms to perform biological oxidations
Cytochrome P450 (CYP)
Monoamine oxidase
Dehydrogenation |
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What does Cytochrome P450 do to hydrocarbons? |
Cytochrome P450 typically oxidizes hydrocarbons, providing more polar and more reactive functionalities. |
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What does Monoamine oxidase do to amines in the liver? |
Monoamine oxidase oxidizes amines in the liver to effectively perform a Hoffmann elimination |
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What does alcohol dehydrogenase convert? |
Alcohol dehydrogenase is another metabolic enzyme in the liver that converts primary alcohols to aldehydes and secondary alcohols to ketones |
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What are the two main methods of metabolism that occur in the liver? |
Oxidation and bioconjugation. |
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What are the two prominent bioconjugation reactions? |
Glucuronidation and Sulfation. These processes work together to functionalize, solubilize and target xenobiotics for elimination/excretion |
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Glucuronidation can occur at any ___________ site on a xenobiotic compound. Glucuronidation both makes xenobiotic compounds more _____ ______ and “marks” them for ________ |
Glucuronidation can occur at any nucleophilic site on a xenobiotic compound. Glucuronidation both makes xenobiotic compounds more water soluble and “marks” them for elimination |
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True or False? Sulfatination has the same effects of Glucuronidation. |
True. |
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What is first pass metabolism? |
The processes in the liver that takes place before the compound enters the rest of the circulatory system. |
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What flow rate must be known to completely measure the effects of first pass metabolism? |
It is possible to completely measure the effects of first pass metabolism by knowing the hepatic blood flow rates. |
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Albumin is the most abundant plasma protein. It binds to most xenobiotic molecules and prevents them from passing through the ___________. |
Albumin is the most abundant plasma protein. It binds to most xenobiotic molecules and prevents them from passing through the capillaries. |
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What is the Depot effect? |
When Albumin binding actually protects some xenobiotics from metabolism by keeping them in the bloodstream and not releasing them into the liver |
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How are drugs eliminated from the body? |
The metabolized xenobiotics leave the liver via the bile duct, which transports them back into the intestines. Ultimately, they are transported to the heart via the hepatic vein. |
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Upon entering the circulatory system, these metabolized compounds begin to pass through the _______. |
Upon entering the circulatory system, these metabolized compounds begin to pass through the kidneys |
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Via a similar process to diffusion out of capillaries, the blood is filtered through the kidneys and the metabolites are _____________ for excretion |
Via a similar process to diffusion out of capillaries, the blood is filtered through the kidneys and the metabolites are concentrated for excretion |
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True or False? Pharmacokinetics do not occur in a static system. |
True. |
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What is the definition of Dose? |
The amount of “drug” that is administered to the organism (mg/kg or mpk) |
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What is the definition of Clearance? |
The rate of elimination of the “drug” |
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What is the formula for CL? |
CL = Rate of elimination/[drug]
Ex: CL = Dose/AUC0→∞ |
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What is the formula for AUC0→∞? |
AUC0→∞ = [drug]*t
Ex: M*h |
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What is the definition of the Cmax? |
The highest concentration of the “drug”. For iv dosing, effectively occurs instantly. Critical to know from an overdose perspective
[drug] |
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What is the definition of the Tmax?
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Time required to achieve Cmax
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What is the definition of Half life? How is it calculated? |
Half life is how long it takes the concentration of the “drug” to decrease by half.
Ex: t1/2 = T([max drug]/2) - Tmax |
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What is the definition of the Volume of distribution? (V) |
Volume of distribution (V) relates the amount of drug in the body to the blood concentration
Ex: V = (Dose/[drug])*e&(-kt) |
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Solid State Volume is an attempt to quantify what? |
V(SS) is an attempt to quantify how well distributed the drug is throughout the tissues of the body |
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True or False? Oral drugs have to enter the bloodstream before their concentration can be measured |
True. |
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What is the definition of bioavailability? |
Bioavailability is the fraction of the drug that reaches the bloodstream (F)
Ex for IV: F(IV) = 100
Bioavailability via other routes is often presented as %F |
