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48 Cards in this Set
- Front
- Back
What is pharmacokinetics?
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The study of plasma and tissue drug concentrations by examining the effects of drug dosage and timing.
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What is the enteral tract?
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The GI tract (glottis to anus). Enteral routes of administration include oral, rectal, and any tube that feed into the GI tract.
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What are some factors influencing the degree of absorption from orally- administered drugs?
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Solubility, disintegration, pH of tract, variability in gastric emptying and GI motility, GI blood flow, first pass effect through hepatic portal circulation.
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What is "bioavailability"? What factors can influence it?
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It is the % of the dose reaching the systemic circulation. It is influenced by the metabolism, excretion, different formulations, and liver function.
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What are some advantages of giving drugs through the oral route?
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Sterility/purity is not an issue, formulations are cheap and convenient.
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What are some disadvantages of giving drugs through the oral route?
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Patient must be conscious and cooperative, absorption and bioavailability are variable, potential loss through vomiting, potential for upper GI tract irritation.
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What are some advantages of giving drugs through the rectal route?
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Rapid absorption, less first-pass effect, good for patients with swallowing problems.
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What is a parenteral route of administration?
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Anything that is not the enteral route.
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What is the sublingual route of administration? What are some of its advantages?
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It is placing the drug under the tongue. It provides direct entry to the systemic circulation, often absorbs rapidly, has a neutral pH, and is fast, easy, and comfortable.
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What is the difference between an IV "push" and an IV "drip"?
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A push is a bolus injection; a drip is a continuous infusion.
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What are some factors that affect drug distribution?
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Solubility in fat or tissue, pH of compartments, plasma protein binding, and redistribution.
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What difference creates the gradient through the placenta? What effect does this gradient have in terms of drug distribution?
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The fetus has a lower pH than the mother. This can cause more drugs to accumulate at the fetus than the rest of the body.
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What is "biotransformation," as it concerns pharmaceuticals?
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Metabolism of the drug.
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What is Phase I of drug metabolism?
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The drug is made more polar by the cytochrome P450 enzyme (CYP) family.
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What is Phase II of drug metabolism?
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The conjugation of the drug to endogenous compounds from the liver.
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What are metabolites?
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The intermediates and products of metabolism.
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Discuss the number and activity of drug metabolites.
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They can be very numerous for a drug, and are usually inactive.
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What are some factors that affect the rate of excretion of drugs from the kidney?
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Renal blood flow, urinary pH, protein binding, MW of drug.
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What role does the gallbladder play in drug excretion?
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Some drugs are secreted into bile by the liver - some of these are reabsorbed by the stomach.
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Define "first order elimination" of drugs. What does the log C vs. time plot look like?
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The loss of a constant proportion of a drug over time. The plot is a straight line.
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What are some factors that affect drug distribution?
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Solubility in fat or tissue, pH of compartments, plasma protein binding, and redistribution.
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What difference creates the gradient through the placenta? What effect does this gradient have in terms of drug distribution?
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The fetus has a lower pH than the mother. This can cause more drugs to accumulate at the fetus than the rest of the body.
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What is "biotransformation," as it concerns pharmaceuticals?
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Metabolism of the drug.
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What is Phase I of drug metabolism?
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The drug is made more polar by the cytochrome P450 enzyme (CYP) family.
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What is Phase II of drug metabolism?
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The conjugation of the drug to endogenous compounds from the liver.
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What are metabolites?
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The intermediates and products of metabolism.
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Discuss the number and activity of drug metabolites.
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They can be very numerous for a drug, and are usually inactive.
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What are some factors that affect the rate of excretion of drugs from the kidney?
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Renal blood flow, urinary pH, protein binding, MW of drug.
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What role does the gallbladder play in drug excretion?
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Some drugs are secreted into bile by the liver - some of these are reabsorbed by the stomach.
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Define "first order elimination" of drugs. What does the log C vs. time plot look like?
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The loss of a constant proportion of a drug over time. The plot is a straight line.
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What are some factors that affect drug distribution?
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Solubility in fat or tissue, pH of compartments, plasma protein binding, and redistribution.
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What difference creates the gradient through the placenta? What effect does this gradient have in terms of drug distribution?
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The fetus has a lower pH than the mother. This can cause more drugs to accumulate at the fetus than the rest of the body.
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What is "biotransformation," as it concerns pharmaceuticals?
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Metabolism of the drug.
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What is Phase I of drug metabolism?
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The drug is made more polar by the cytochrome P450 enzyme (CYP) family.
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What is Phase II of drug metabolism?
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The conjugation of the drug to endogenous compounds from the liver.
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What are metabolites?
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The intermediates and products of metabolism.
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Discuss the number and activity of drug metabolites.
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They can be very numerous for a drug, and are usually inactive.
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What are some factors that affect the rate of excretion of drugs from the kidney?
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Renal blood flow, urinary pH, protein binding, MW of drug.
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What role does the gallbladder play in drug excretion?
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Some drugs are secreted into bile by the liver - some of these are reabsorbed by the stomach.
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Define "first order elimination" of drugs. What does the log C vs. time plot look like?
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The loss of a constant proportion of a drug over time. The plot is a straight line.
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After how many half-lives is a drug considered to be "gone"?
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4 to 5 half-lives.
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What is "zero order elimination" of a drug? What does its log Cp vs. time scale look like?
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It is when a constant amount of drug is eliminated per unit time. The plot is a parabola which points downwards.
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What is the "volume of distribution"? What does a high Vd signify?
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It is the volume in which a drug "seems" to be dissolved, based on the amount of drug given and the plasma concentration. A high Vd signifies that a lot of drug has been bound in the tissue, leaving behind little free drug.
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What is drug clearance?
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It indicates the volume of plasma that is cleared of a drug per unit time.
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How does a double-compartment model of clearance differ in concept and in its log Cp vs. time graph from a single compartment model?
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It includes a second compartment representing the tissues, not just a single compartment representing the bloodstream. Its graph has a steep, negatively-sloped "distribution phase," followed by a flatter "elimination phase."
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Give the formulas for concentration of drug and for half-life of a drug.
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Ct = Co * e ^ (Kel * t)
t1/2 = 0.693 / Kel |
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What is a "loading dose"?
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A high dose of a substance given right at the beginning of a drug course.
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What is a good way to keep very stable drugs levels in an individual from the beginning of the course?
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Use a loading dose and continuous infusion.
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