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48 Cards in this Set

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What is pharmacokinetics?
The study of plasma and tissue drug concentrations by examining the effects of drug dosage and timing.
What is the enteral tract?
The GI tract (glottis to anus). Enteral routes of administration include oral, rectal, and any tube that feed into the GI tract.
What are some factors influencing the degree of absorption from orally- administered drugs?
Solubility, disintegration, pH of tract, variability in gastric emptying and GI motility, GI blood flow, first pass effect through hepatic portal circulation.
What is "bioavailability"? What factors can influence it?
It is the % of the dose reaching the systemic circulation. It is influenced by the metabolism, excretion, different formulations, and liver function.
What are some advantages of giving drugs through the oral route?
Sterility/purity is not an issue, formulations are cheap and convenient.
What are some disadvantages of giving drugs through the oral route?
Patient must be conscious and cooperative, absorption and bioavailability are variable, potential loss through vomiting, potential for upper GI tract irritation.
What are some advantages of giving drugs through the rectal route?
Rapid absorption, less first-pass effect, good for patients with swallowing problems.
What is a parenteral route of administration?
Anything that is not the enteral route.
What is the sublingual route of administration? What are some of its advantages?
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.
What is the difference between an IV "push" and an IV "drip"?
A push is a bolus injection; a drip is a continuous infusion.
What are some factors that affect drug distribution?
Solubility in fat or tissue, pH of compartments, plasma protein binding, and redistribution.
What difference creates the gradient through the placenta? What effect does this gradient have in terms of drug distribution?
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.
What is "biotransformation," as it concerns pharmaceuticals?
Metabolism of the drug.
What is Phase I of drug metabolism?
The drug is made more polar by the cytochrome P450 enzyme (CYP) family.
What is Phase II of drug metabolism?
The conjugation of the drug to endogenous compounds from the liver.
What are metabolites?
The intermediates and products of metabolism.
Discuss the number and activity of drug metabolites.
They can be very numerous for a drug, and are usually inactive.
What are some factors that affect the rate of excretion of drugs from the kidney?
Renal blood flow, urinary pH, protein binding, MW of drug.
What role does the gallbladder play in drug excretion?
Some drugs are secreted into bile by the liver - some of these are reabsorbed by the stomach.
Define "first order elimination" of drugs. What does the log C vs. time plot look like?
The loss of a constant proportion of a drug over time. The plot is a straight line.
What are some factors that affect drug distribution?
Solubility in fat or tissue, pH of compartments, plasma protein binding, and redistribution.
What difference creates the gradient through the placenta? What effect does this gradient have in terms of drug distribution?
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.
What is "biotransformation," as it concerns pharmaceuticals?
Metabolism of the drug.
What is Phase I of drug metabolism?
The drug is made more polar by the cytochrome P450 enzyme (CYP) family.
What is Phase II of drug metabolism?
The conjugation of the drug to endogenous compounds from the liver.
What are metabolites?
The intermediates and products of metabolism.
Discuss the number and activity of drug metabolites.
They can be very numerous for a drug, and are usually inactive.
What are some factors that affect the rate of excretion of drugs from the kidney?
Renal blood flow, urinary pH, protein binding, MW of drug.
What role does the gallbladder play in drug excretion?
Some drugs are secreted into bile by the liver - some of these are reabsorbed by the stomach.
Define "first order elimination" of drugs. What does the log C vs. time plot look like?
The loss of a constant proportion of a drug over time. The plot is a straight line.
What are some factors that affect drug distribution?
Solubility in fat or tissue, pH of compartments, plasma protein binding, and redistribution.
What difference creates the gradient through the placenta? What effect does this gradient have in terms of drug distribution?
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.
What is "biotransformation," as it concerns pharmaceuticals?
Metabolism of the drug.
What is Phase I of drug metabolism?
The drug is made more polar by the cytochrome P450 enzyme (CYP) family.
What is Phase II of drug metabolism?
The conjugation of the drug to endogenous compounds from the liver.
What are metabolites?
The intermediates and products of metabolism.
Discuss the number and activity of drug metabolites.
They can be very numerous for a drug, and are usually inactive.
What are some factors that affect the rate of excretion of drugs from the kidney?
Renal blood flow, urinary pH, protein binding, MW of drug.
What role does the gallbladder play in drug excretion?
Some drugs are secreted into bile by the liver - some of these are reabsorbed by the stomach.
Define "first order elimination" of drugs. What does the log C vs. time plot look like?
The loss of a constant proportion of a drug over time. The plot is a straight line.
After how many half-lives is a drug considered to be "gone"?
4 to 5 half-lives.
What is "zero order elimination" of a drug? What does its log Cp vs. time scale look like?
It is when a constant amount of drug is eliminated per unit time. The plot is a parabola which points downwards.
What is the "volume of distribution"? What does a high Vd signify?
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.
What is drug clearance?
It indicates the volume of plasma that is cleared of a drug per unit time.
How does a double-compartment model of clearance differ in concept and in its log Cp vs. time graph from a single compartment model?
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."
Give the formulas for concentration of drug and for half-life of a drug.
Ct = Co * e ^ (Kel * t)

t1/2 = 0.693 / Kel
What is a "loading dose"?
A high dose of a substance given right at the beginning of a drug course.
What is a good way to keep very stable drugs levels in an individual from the beginning of the course?
Use a loading dose and continuous infusion.