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125 Terms
Pharmacokinetics
How the body affects the drug
Absorption
How the drug enters the bloodstream
Distribution
How the drug spreads throughout the body to the target area
Metabolism
How the body breaks down the drug
Excretion
How the drug leaves the body
Pharmacodynamics
How the drug affects the body
The R’s
Right drug
Right dose
Right patient
Right route
Right time
Examples of a schedule I drug
Heroin
LSD
MDMA
Psilocybin
Marijuana
Examples of a schedule II drug
Opioids
Morphine
Hydrocodone
Fentanyl
Oxycontin
Highest abuse potential, no accepted medical use in the U.S.
Schedule I
High abuse potential, accepted medical use
Schedule II
Less abuse potential than schedule II, moderate dependence liability
Schedule III
Less abuse potential than schedule II drugs; limited dependence liability
Schedule IV
Less abuse potential and very limited dependence
Schedule V
This class of drugs requires a written RX
Schedule II
This class off drugs cannot be prescribed
Schedule I
A patient receives a prescription for morphine. The nurse knows this drug is classified as:
Schedule II
Which phase in clinical testing used healthy volunteers to evaluate drug metabolism, pharmacokinetics and biologic effects?
Phase I
Which phase of drug development occurs after the drug is already on the market and being used by the general population?
Phase IV
A nurse is explaining randomized controlled trials to a student nurse. Which of the following best explains randomization?
A. All subjects receive both the new drug and the placebo
B. Subjects are assigned to groups by diagnosis
C. Subjects are assigned to groups based on age
D. Subjects are assigned to groups by chance to prevent bias
Subjects are assigned to groups by chance to prevent bias
During a randomized controlled trial, only the researchers are aware of who receives the active drug versus placebo. What type of study is this?
Single-blind
A new drug shows promising results in animal testing. What phase comes next before human trials can begin?
Phase I
A nurse is teaching a patient that the drug they are taking was tested on thousands of patients over several months to determine safety and effectiveness. This describes:
A. Phase I
B. Phase II and III
C. Phase IV
D. Preclinical trials
Phase II and III
What is the main purpose of Phase IV in clinical drug testing?
A. To determine metabolism and side effects
B. To test the drug on animals
C. To evaluate drug safety in the general population
D. To assign random groups for comparison
To evaluate drug safety in the general population
Which of the following best describes a double-blind study?
A. Only the subject knows what group they are in
B. The researcher knows the subject’s group, but the subject does not
C. Neither the subject nor the researcher knows the subject’s group
D. Everyone knows the subject’s group
Neither the subject nor the researcher knows the subject’s group
A nurse is reviewing a medication label with a patient and explains that “acetaminophen” is the drug’s:
A. Trade name
B. Chemical name
C. Generic name
D. Controlled substance name
Generic name
Which example is a chemical drug name?
A. Tylenol
B. Acetaminophen
C. N-acetyl-para-aminophenol
D. Excedrin
N-acetyl-para-aminophenol
FDA requires that OTC drugs clearly list the _________ of each active ingredient on the label
generic name
What is the major concern when patients self-treat with multiple OTC products?
A. Cost of medications
B. Product expiration
C. Risk of duplicate drug exposure
D. Lack of dosage instructions
Risk of duplicate drug exposure
A nurse is teaching about herbal supplements under the DSHEA of 1994. Which statement by the patient reflects understanding?
A. “Herbal supplements are tested for safety by the FDA before sale.”
B. “I can assume herbal products are standardized and consistent.”
C. “Herbals are not regulated and don’t need proof of effectiveness.”
D. “All supplements must meet the same standards as prescription drugs.”
“Herbals are not regulated and don’t need proof of effectiveness.”
DSHEA (Dietary Supplement & Health Education Act) does not require pre-market approval, but supplements may be pulled from shelves if harm is proven.
TRUE or FALSE.
True
OTC products are required to clearly list the __________ of drug contained within the product
generic name
You can buy a OTC without a prescription.
TRUE OR FALSE.
True
Which of the following best explains why taking multiple OTC products at once could be harmful?
A. They are too expensive
B. They contain identical trade names
C. They may contain the same active ingredient
D. They’re expired and ineffective
They may contain the same active ingredient
Which of the following characteristics allows a drug to cross the cell membrane via direct membrane penetration?
lipid soluble, nonpolar, nonionized
Which method is used by most drugs to cross cell membranes?
Direct penetration of the membrane
A patient is taking a drug that is a P-glycoprotein substrate. What does this mean?
A. The drug binds to sodium channels
B. The drug uses active transport into the cell
C. The drug is pumped out of cells by a transport protein
D. The drug crosses membranes via direct diffusion
The drug is pumped out of cells by a transport protein
Why is direct membrane penetration not possible for most polar or ionized drugs?
A. They are too small
B. They move too quickly through pores
C. Cell membranes are water-based
D. They can’t dissolve in the lipid layer of the membrane
They can’t dissolve in the lipid layer of the membrane
Which of the following molecules is most likely to use channels or pores to cross the membrane?
Na+ and K
Transport systems
P-Glycoprotein (PCP) or a carrier protein.
Uses a carrier protein to move the drug.
Channels or pores
Tiny openings in the membrane (very few pass this way)
Lipid soluble =
Lipophilic
Where will an acidic drug accumulate if there is a pH gradient across a membrane?
On the basic (alkaline) side
Where will an basic drug accumulate if there is a pH gradient across a membrane?
on the acidic side
A basic drug is placed in an acidic environment. What is most likely to occur?
A. The drug becomes nonionized and crosses membranes easily
B. The drug becomes ionized and is less absorbed
C. The drug is destroyed by acid
D. The drug binds to enzymes and becomes inactive
The drug becomes ionized and is less absorbed
Which of the following best describes quaternary ammonium compounds?
A. Water-soluble but easily crosses membranes
B. Always carry a positive charge and are poorly absorbed
C. Uncharged and highly lipid-soluble
D. Transported passively through protein channels
Always carry a positive charge and are poorly absorbed
Drugs that are large, ionized, or water-soluble require what mechanism to cross membranes?
A. Active liver metabolism
B. Direct membrane penetration
C. Facilitated diffusion via carrier proteins
D. Passive binding to receptors
Facilitated diffusion via carrier proteins
Absorption is the movement
of a drug from the site of administration into the bloodstream
Rate of absorption
How fast the drug enters the blood
Amount of absorption
How much of the drug moves into the bloodstream
Rate of dissolution
how quickly it absorbs
surface area
how much space available for a drug to absorb
5 factors that affect drug absorption
Rate of dissolution
2. Surface area
3. Blood flow
4. Lipid solubility
5. pH partitioning
bioavailability
The amount of active drug that reaches systemic circulation after administration.
What is chemical equivalence?
When two drugs contain the same amount of the active ingredient, but may differ in bioavailability.
What is the barrier to absorption for intravenous (IV) drugs?
None — IV drugs go directly into the bloodstream.
What is the absorption pattern for IV drugs?
Instant and complete (100% bioavailability).
3 advantages of IV drug administration.
1. Rapid onset
2. Precise control of drug levels
3. Ability to administer large volumes
3 disadvantages of IV drug administration.
Irreversible
2. Risk of infection, embolism
3. Expensive and inconvenient
What is the barrier to absorption for intramuscular (IM) and subcutaneous (SubQ) drugs?
Minimal — must pass through the capillary wall.
What factors affect absorption of IM/SubQ drugs?
Water solubility of the drug and blood flow to the injection site.
What are depot preparations?
IM drugs formulated for slow, sustained release over time.
3 disadvantages of IM/SubQ injections.
1. Pain/discomfort
2. Risk of infection
3. Inconvenient, possible nerve damage
What is the main barrier to absorption for oral (PO) drugs?
Epithelial cells lining the GI tract.
Why is oral drug absorption highly variable?
Affected by solubility, pH, gastric emptying time, food, other drugs, and coatings.
What are enteric-coated tablets?
Oral drugs with a coating that prevents stomach breakdown; do not crush.
What are sustained-release preparations?
Drugs released gradually over time for longer effect; do not crush.
Why should sustained-release and enteric-coated drugs not be crushed?
Crushing alters drug delivery, may cause overdose or destroy protection.
What is distribution in pharmacokinetics?
The movement of drugs from the blood into the interstitial space of tissues and then into cells where the drug acts or is metabolized.
What are the 3 major factors that affect drug distribution?
Blood flow to tissues
Ability of the drug to exit the vascular system
Ability of the drug to enter cells
What is the role of blood flow in distribution?
Tissues with more blood flow receive drugs more rapidly. Poor circulation limits drug delivery.
How do abscesses affect drug distribution?
Abscesses have no blood supply, so drugs can’t reach them through circulation.
How do solid tumors affect drug distribution?
Blood flow is higher at the edges but poor in the center, limiting drug penetration and reducing effectiveness.
What is the memory trick for poor blood flow in abscesses/tumors?
“No flow, no go” — if blood can’t get there, neither can the drug.
How easily do drugs exit through capillary beds?
Easily — most drugs pass through capillary walls with little resistance.
What is the blood-brain barrier (BBB)?
A protective structure with tight junctions that prevents most drugs from entering the brain.
What kind of drugs can pass through the blood-brain barrier?
Lipid-soluble, non-ionized drugs, or those using a transport system.
Is the blood-brain barrier fully developed at birth?
No — it is not fully developed in infants, making them more vulnerable to CNS drug effects.
Can drugs cross the placenta?
Yes — the placenta is not a complete barrier; many drugs can pass and affect the fetus.
What is plasma albumin?
A protein in the blood that drugs can bind to; it restricts drug movement out of the bloodstream.
What happens when a drug is protein-bound?
It is inactive — cannot leave the bloodstream, cannot reach target tissues, and cannot be metabolized or excreted.
What is a “free drug”?
A drug that is not bound to albumin and is free to act on target tissues or be metabolized.
Why is protein binding reversible?
Drugs can unbind and become active again when needed.
What happens when two drugs compete for protein binding sites?
One drug may be displaced, increasing the level of free (active) drug and the risk of toxicity.
What are the three key barriers to drug distribution?
Blood-brain barrier
Placental barrier
Protein binding (to albumin)
Which part of distribution affects how long a drug stays in the system?
Protein binding — bound drugs stay in circulation longer and are released slowly.
Where does most drug metabolism take place?
Liver
Which enzyme system is responsible for most drug metabolism in the liver?
Cytochrome P450 system
What happens to most drugs after CYP450 metabolism?
hey become more water-soluble
What are the two common CYP450 inhibitors?
acute alcohol use and grapefruit juice
What effect do CYP450 inducers have on drug levels?
A. Increase drug levels in the blood
B. Slow drug metabolism
C. Decrease drug levels by speeding metabolism
D. Stop the drug from binding to proteins
Decrease drug levels by speeding metabolism
A drug is metabolized by CYP450 and given with an inducer. What should the nurse expect?
A. The drug will be inactivated more slowly
B. The drug may require a lower dose
C. The patient may experience toxicity
D. The drug may need a higher dose
The drug may need a higher dose
What is a prodrug?
A drug that becomes active after metabolism
Which of the following describes the activation of a prodrug?
A. The drug is immediately active when swallowed
B. The drug is detoxified in the stomach
C. The drug becomes active after enzymatic conversion in the liver
D. The drug bypasses the first-pass effect
The drug becomes active after enzymatic conversion in the liver
Which of the following best explains how metabolism supports renal drug excretion?
A. It turns drugs into fat for excretion
B. It reduces the number of protein-bound drugs
C. It makes drugs more water-soluble
D. It concentrates drugs in the bladder
It makes drugs more water-soluble
A patient takes Drug A, which is metabolized by CYP450. Drug B is a strong inhibitor of that enzyme. What happens to Drug A?
A. It is excreted more quickly
B. It becomes less effective
C. Its concentration in the blood increases
D. It binds more tightly to albumin
Its concentration in the blood increases
What effect does a CYP450 inducer have on a substrate drug?
A. It slows the drug's metabolism
B. It increases the drug's half-life
C. It accelerates the drug’s breakdown
D. It improves protein binding
It accelerates the drug’s breakdown
Which situation may require a higher dose of a drug to remain effective?
A. The patient has liver failure
B. The patient is taking a CYP450 inhibitor
C. The patient is taking a CYP450 inducer
D. The drug is highly protein-bound
The patient is taking a CYP450 inducer
What happens when a CYP450 inducer is taken with a drug metabolized by that enzyme?
A. Drug levels increase
B. Drug is metabolized faster → levels decrease
C. Drug is unchanged
D. Drug becomes toxic
Drug is metabolized faster → levels decrease
Why might a provider switch a medication from oral to IV?
A. IV is more convenient
B. IV avoids first-pass effect in the liver
C. Oral drugs are toxic
D. The patient prefers IV
IV avoids first-pass effect in the liver