MN553 Advanced Pharmacology & Pharmacotherapeutics Unit 2 Quiz Study Guide
• Describe the absorption, distribution, metabolism, and elimination process
of drugs in the body.
• Absorption: entering the body
• Parenteral Administration (IV): straight to the bloodstream, but once
administered, the drug absorption cannot be slowed, and the drug
cannot be removed from the body
• Oral: common and most convenient route, keep in mind pH and where
the drug needs to take effect (stomach, intestines, etc.)
• Site of administration: eyes, ears, throat/lungs, skin
• Bioavailability: Not all of the administered dose may be dissolved,
absorbed, or survive liver metabolism, only a fraction of an administered
dose makes it to the bloodstream. 100% bioavailability for IV, 10-90% for
oral.
• Peak Blood Levels: Rapid absorption leads to higher peak blood levels,
with a risk of greater toxicity and side effects. Some drugs (like
aminoglycoside antibiotics) need to be closely monitored for toxicity.
• Distribution: process of drug moving through the body
• Properties that affect distribution: drug size, charge, chemical structure,
pH, molecular size, lipid or water solubility.
• Henderson–Hasselbalch Relationship: the effects of pH and ion
charge/concentration affecting how drugs pass through cell membranes
• Protein binding: the biggest player is albumin.
• Other proteins: alpha-1-acid glycoprotein, cortisol-binding globulin, sex
hormone–binding globulin, and lipoproteins.
• General principle that drug action occurs through free, unbound drug.
Protein binding, which may include binding to proteins that are not in the
plasma, also prevents the interaction of drug molecules with their site of
action. Plasma protein binding creates a reservoir of bound drug
molecules that can dissociate at any time to interact with drug receptors
and produce responses.
• Transport system: membrane proteins that actively move drugs in and out
of the cell.
• Volume of Distribution: the concentration of a drug can vary depending
on where it “sits” in the body’s fluids (plasma, extracellular fluid or
intracellular fluid).
• Metabolism: the chemical alteration of the drugs into metabolites.
• Metabolism of drugs can occur in every biological tissue, but it occurs
mostly in the smooth endoplasmic reticulum of cells in the liver.
, • Metabolism by the liver following oral administration is called first-pass
metabolism and is important in determining whether a drug can be orally
administered.
• Phase I reactions, called non-synthetic reactions, involve oxidation,
reduction, and hydrolysis reactions, which prepare the drug molecule for
further metabolism. (Making the drug more water soluble).
• Phase II reactions are called synthetic or conjugation reactions because
drug molecules are metabolized, and something is added to the drug to
synthesize a new compound. Conjugation to these molecules makes
metabolites more water soluble and more easily excreted by the kidneys.
• Major player CYP P450: catalyzes the metabolism of a large number of
diverse, highly lipid-soluble drugs and chemicals. CYPs transfer electrons
from the oxidation of drugs to the electron transport system of the
endoplasmic reticulum, a cell organelle.
• Single nucleotide polymorphisms (SNPs) are minor mutations in proteins
that can result in metabolic activity changes. These alterations in DNA are
sometimes associated with population groups and help explain why
certain groups of patients are more or less sensitive to certain drugs.
• Drug interactions: some chemicals, foods or drugs can compete, block,
limit, or increase/decrease drug receptor function. (it’s an Affinity War!
Get it? Avengers movie.) Drugs that have a higher affinity will block or be
processed first.
• Excretion: drugs are transferred from inside the body to outside the body
• kidney is the primary organ of excretion for most drugs
• The renal system filters the body’s fluid via the glomerulus in the
nephrons. Controls electrolyte and fluid balance.
• Other points of excretion: liver, pulmonary, skin, sweat, saliva, hair, and
breast
• Discuss the process of a drug reaching steady state concentration in the
body.
• Apply the principles of pharmacokinetics to the elderly, pediatrics, and
pregnant/nursing women.
• Pediatric:
◆ Absorption
• More than in adults;
1 Blood flow at the site of administration (IM) or (SC)
▪ 1st 6 months = increased perfusion to muscles - HOWEVER – decrease
flow during illness = delayed or variable absorption
2 GI function
• Describe the absorption, distribution, metabolism, and elimination process
of drugs in the body.
• Absorption: entering the body
• Parenteral Administration (IV): straight to the bloodstream, but once
administered, the drug absorption cannot be slowed, and the drug
cannot be removed from the body
• Oral: common and most convenient route, keep in mind pH and where
the drug needs to take effect (stomach, intestines, etc.)
• Site of administration: eyes, ears, throat/lungs, skin
• Bioavailability: Not all of the administered dose may be dissolved,
absorbed, or survive liver metabolism, only a fraction of an administered
dose makes it to the bloodstream. 100% bioavailability for IV, 10-90% for
oral.
• Peak Blood Levels: Rapid absorption leads to higher peak blood levels,
with a risk of greater toxicity and side effects. Some drugs (like
aminoglycoside antibiotics) need to be closely monitored for toxicity.
• Distribution: process of drug moving through the body
• Properties that affect distribution: drug size, charge, chemical structure,
pH, molecular size, lipid or water solubility.
• Henderson–Hasselbalch Relationship: the effects of pH and ion
charge/concentration affecting how drugs pass through cell membranes
• Protein binding: the biggest player is albumin.
• Other proteins: alpha-1-acid glycoprotein, cortisol-binding globulin, sex
hormone–binding globulin, and lipoproteins.
• General principle that drug action occurs through free, unbound drug.
Protein binding, which may include binding to proteins that are not in the
plasma, also prevents the interaction of drug molecules with their site of
action. Plasma protein binding creates a reservoir of bound drug
molecules that can dissociate at any time to interact with drug receptors
and produce responses.
• Transport system: membrane proteins that actively move drugs in and out
of the cell.
• Volume of Distribution: the concentration of a drug can vary depending
on where it “sits” in the body’s fluids (plasma, extracellular fluid or
intracellular fluid).
• Metabolism: the chemical alteration of the drugs into metabolites.
• Metabolism of drugs can occur in every biological tissue, but it occurs
mostly in the smooth endoplasmic reticulum of cells in the liver.
, • Metabolism by the liver following oral administration is called first-pass
metabolism and is important in determining whether a drug can be orally
administered.
• Phase I reactions, called non-synthetic reactions, involve oxidation,
reduction, and hydrolysis reactions, which prepare the drug molecule for
further metabolism. (Making the drug more water soluble).
• Phase II reactions are called synthetic or conjugation reactions because
drug molecules are metabolized, and something is added to the drug to
synthesize a new compound. Conjugation to these molecules makes
metabolites more water soluble and more easily excreted by the kidneys.
• Major player CYP P450: catalyzes the metabolism of a large number of
diverse, highly lipid-soluble drugs and chemicals. CYPs transfer electrons
from the oxidation of drugs to the electron transport system of the
endoplasmic reticulum, a cell organelle.
• Single nucleotide polymorphisms (SNPs) are minor mutations in proteins
that can result in metabolic activity changes. These alterations in DNA are
sometimes associated with population groups and help explain why
certain groups of patients are more or less sensitive to certain drugs.
• Drug interactions: some chemicals, foods or drugs can compete, block,
limit, or increase/decrease drug receptor function. (it’s an Affinity War!
Get it? Avengers movie.) Drugs that have a higher affinity will block or be
processed first.
• Excretion: drugs are transferred from inside the body to outside the body
• kidney is the primary organ of excretion for most drugs
• The renal system filters the body’s fluid via the glomerulus in the
nephrons. Controls electrolyte and fluid balance.
• Other points of excretion: liver, pulmonary, skin, sweat, saliva, hair, and
breast
• Discuss the process of a drug reaching steady state concentration in the
body.
• Apply the principles of pharmacokinetics to the elderly, pediatrics, and
pregnant/nursing women.
• Pediatric:
◆ Absorption
• More than in adults;
1 Blood flow at the site of administration (IM) or (SC)
▪ 1st 6 months = increased perfusion to muscles - HOWEVER – decrease
flow during illness = delayed or variable absorption
2 GI function
