Unit 1 Chapter 3 Pharmcaokinetics and Phamadynamics Flashcards
What is Pharmacikinetics?
Pharmacokinetics is the process of drug movement throughout the body necessary to achieve drug action. The four processes are
(1) absorption,
(2) distribution,
(3) metabolism (or biotransformation), and
(4) excretion (or elimination).
WHAT THE BODY WILL DO THE DRUG
What two organs are essential to drug metabolism and drug excretion?
A. Anus and esophagus
B. Heart and rectum
C. Liver and kidneys
D. Urethra and oral cavity
C. Liver and kidneys
First pass occurs in liver
What is Drug Absorption
Drug absorption is the movement of the drug into the bloodstream after administration.
What is Disintegration, Dissolution,
Disintegration
Breakdown of oral drug form into small particles
. The rate of dissolution is the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it. Drugs in liquid form are more rapidly available for GI absorption than are solids.
-taken by mouth
Dissolution
Process of combining small drug particles with
liquid to form a solution
For the body to use drugs taken by mouth, a drug in solid form (e.g., tablet or capsule) must disintegrate into small particles and combine with a liquid to form a solution, a process known as dissolution (drugs in liquid form are already in solution), to be absorbed from the gastrointestinal (GI) tract into the bloodstream.
Drug absorption
Drug movement from GI tract into bloodstream
Liver Failure
Medication is absorbed slowly (Jaundice)
Kidney Failure
Drug toxicity can occur (Overdose) .Medication stays longer in the body.
What is half-life
The drug half-life (t1⁄2) is the time it takes for the amount of drug in the body to be reduced by half. The amount of drug administered, the amount of drug remaining in the body from previous doses, metabolism, and elimination affect the half-life of a drug.
For example, with liver or kidney dysfunction, the half-life of the drug is prolonged, and less drug is metabolized and eliminated.
the amount of time it takes a half of the drug to be gone in the body
The shorter the half life the more often the drug is administered
the longer the half life the least often the drug will be administered
What factor affect drug absorption?
Blood flow, pain, stress, hunger, fasting, food, and pH affect drug absorption. Poor circulation to the stomach as a result of shock, vasoconstrictor drugs, or disease hampers absorption. Pain, stress, and foods that are solid, hot, or high in fat can slow gastric emptying time, so drugs remain in the stomach longer. Exercise can decrease gastric blood flow by shunting blood flow to peripheral muscles, thereby decreasing blood circulation to the GI tract.
Which of the following affects drug absorption?
A. food
B. sleep
C. rest
D. adequate nutrition
A. food
Blood flow, pain, stress, hunger, fasting, food, and pH affect drug absorption. Poor circulation to the stomach as a result of shock, vasoconstrictor drugs, or disease hampers absorption. Pain, stress, and foods that are solid, hot, or high in fat can slow gastric emptying time, so drugs remain in the stomach longer. Exercise can decrease gastric blood flow by shunting blood flow to peripheral muscles, thereby decreasing blood circulation to the GI tract.
Different routes of drug absorption
Drugs given intramuscularly are absorbed faster in muscles that have increased blood flow (e.g., deltoid) than in those that do not (e.g., gluteus maximus).
Subcutaneous tissue has decreased blood flow compared with muscle, so absorption is slower when drugs are given subcutaneously.predictable rate of absorption than those given by mouth.
Drugs given rectally are absorbed slower than drugs administered by the oral route. Absorption is slower because the surface area in the rectum is smaller than the stomach, and it has no villi. Additionally, the composition of the suppository base (e.g., fa y bases or water-soluble bases) affects drug absorption.
Where does first pass occur?
A.from the portal vein to the Liver
B. from the esophagus to the Stomach
C. Oral cavity
D. Kidney
A.from the portal vein to the Liver
FIRST PASS ONLY OCCURS IN ORAL MEDICATIONS
After absorption of oral drugs from the GI tract, they pass from the intestinal lumen to the liver via the portal vein. In the liver, some drugs are metabolized to an inactive form and are excreted, thus reducing the amount of active drug available to exert a pharmacologic effect. This is referred to as the first-pass effect or first-pass metabolism.
Most oral drugs are affected to some degree by first-pass metabolism. Lidocaine and some nitroglycerins, for example, are not given orally because they have extensive first-pass metabolism, and most of the drug is inactivated. Drugs that are delivered by other routes (IV, IM, SQ, nasal, sublingual, buccal) do not enter the portal circulation and are not subjected to first-pass metabolism.
Why are some drugs not given orally due to the mechanism of the first pass that takes place in the Liver?
A. The liver metabolizes the drug to an inactive form, causing the therapeutic effect of the drug to be lessened.
B. The liver metabolizes the drug which causes a greater effect that can lead to a toxic effect or overdose
C.To create a therapeutic effect
D.To decrease the therapeutic effect
A. The liver metabolizes the drug to an inactive form, causing the therapeutic effect of the drug to be lessened.
Most oral drugs are affected to some degree by first-pass metabolism. Lidocaine and some nitroglycerins, for example, are not given orally because they have extensive first-pass metabolism, and most of the drug is inactivated. Drugs that are delivered by other routes (IV, IM, SQ, nasal, sublingual, buccal) do not enter the portal circulation and are not subjected to first-pass metabolism.
PG 22 PHYSICAL BOOK
What is bioavailability?
Bioavailability refers to the percentage of administered drug available for activity.
For orally administered drugs, bioavailability is affected by absorption and first-pass metabolism.
The bioavailability of oral drugs is always less than 100% and varies based on the rate of first-pass metabolism
(i.e., the bioavailability of rosuvastatin is 20%, whereas the bioavailability of digoxin ranges from 70% to 85%). The bioavailability of intravenous (IV) drugs is 100%(
IV drugs does not have contact with first pass metabolism)
What can liver failure do to an oral drug that is ingested and metabolized in the liver?
A. can increase the bioavailability of the oral medication
B. can decrease the bioavailability of the oral medication
C. can increase urine output
D. Can make the patient cry
A. can increase the bioavailability of the oral medication
A decrease in liver function or a decrease in hepatic blood flow can increase the bioavailability of a drug, but only if the drug is metabolized by the liver. Less drug is destroyed by hepatic metabolism in the presence of a liver disorder.
FACTORS AFFECTING
BIOAVAILABILITY
FACTORS AFFECTING
BIOAVAILABILITY
Absorption
First-pass metabolism
Drug form
Route of administration
Gastric mucosa and motility
Administration with food and other drugs
Changes in liver metabolism
What is Drug Distribution?
Distribution is the movement of the drug from the circulation to body tissues.
from blood to organs, fat, and muscles
Drug distribution is influenced by vascular permeability and permeability of cell membranes, regional blood flow and pH, cardiac output, tissue perfusion, the ability of the drug to bind tissue and plasma proteins (Fig. 3.3), and the drugs lipid solubility. Drugs are easily distributed in highly perfused organs such as the liver, heart, and kidney. Tissues with decreased perfusion, such as muscle, fat, and peripheral organs, result in decreased drug distribution.
As a nurse would you administer two protein binding drugs at the same time?
A. Yes
B. No
B. No
When two highly protein-bound drugs are administered together, they compete for protein-binding sites, leading to an increase in free drug being released into the circulation. For example, if warfarin (99% protein bound) and furosemide (95% protein bound) were administered together, warfarin —the more highly bound drug—could displace furosemide from its binding site. In this situation, it is possible for drug accumulation to occur and for toxicity to result.
What two protein binding drugs should you not give at the same time?
Aspirin and Ibuprofen and warfarin
When a drug(ibuprofen) is binded to a protein there is no action (no therapeutic effect)
The part or percentage of the drug that is not binded to a protein is free to cause an action (therapeutic effect)
If a patient doesn’t have enough protein (Albumin) when taking a protein binding medication it can lead to drug toxicity / overdose
What is a free drug
Free drugs are able to exit blood vessels and reach their site of action, causing a pharmacologic response. TOXIC OR OVERDOSE when using two protein binding drugs
What do older adults have that put them at risk for drug toxicity when it comes to ingesting protein binding medications?
A. hypoalbuminemia
B. hyperalbuminemia
C.hypercalcemia
D. Hypotension
A. hypoalbuminemia
Another factor that may alter protein binding is low plasma protein levels, which potentially decrease the number of available binding sites and can lead to an increase in the amount of free drug available, resulting in drug accumulation and toxicity.
Patients with liver or kidney disease and those who are malnourished may have significantly lower serum albumin levels.
Additionally, older adults are more likely to have hypoalbuminemia, particularly if they have multiple chronic illnesses.
With these factors in mind, it is important for nurses to understand the concept of protein binding and check their patient’s protein and albumin levels when administering drugs.
Why is drug metabolism or biotransformation crucially important?
A. it allows fat-soluble drugs to be altered to water soluble drugs in order to be excreted by the kidneys.
B. it distributes the drug across the body and liver
C. it allows hyperinsulinism
D. it creates a safe space for drug absorption
A. it allows fat-soluble drugs to be altered to water soluble drugs in order to be excreted by the kidneys.
is the process by which the body chemically changes drugs into a form that can be excreted. The liver is the primary site of metabolism.
A large percentage of drugs are lipid soluble, thus the liver metabolizes the lipid-soluble drug substance to a water-soluble substance for renal excretion.
Liver diseases such as cirrhosis and hepatitis alter drug metabolism by inhibiting the drug-metabolizing enzymes in the liver. When the drug metabolism rate is decreased, excess drug accumulation can occur and can lead to toxicity.
What is the half-life of a drug
The drug half-life (t1⁄2) is the time it takes for the amount of drug in the body to be reduced by half.
For example, with liver or kidney dysfunction, the half-life of the drug is prolonged, and less drug is metabolized and eliminated.
By knowing the half-life, the time it takes for a drug to reach a steady state (plateau drug level) can be determined.
A drug goes through several half-lives before complete elimination occurs, and drug half-life is used to determine dosing interval.
This is best understood with an example: ibuprofen has a half-life of about 2 hours. If a person takes 200 mg, in 2 hours, 50% of the drug will be gone, leaving 100 mg. Two hours later, another 50% of the drug will be gone, this time leaving 50 mg; in another 2 hours, 50% more will be gone, so only 25 mg will remain.
This process continues such that 10 hours after 200 mg of ibuprofen has been taken, if no additional doses are administered, 6.25 mg of the drug remains
What is a loading dose
By giving a large initial dose, known as a loading dose, that is significantly higher than maintenance dosing, therapeutic effects can be obtained while a steady state is reached. It bears repeating that the loading dose is larger than the dose needed to maintain the drug at steady state; it would produce toxic side effects if given in repeated doses. After the loading dose, maintenance dosing is begun; this is the dose needed to maintain drug concentration at steady state when given repeatedly at a consistent dose and constant dosing interval.
NORMAL RANGE OF BLOOD UREA NITROGEN
Both Sexes: 10-20 mg/dL
Common tests used to determine renal function include creatinine and blood urea nitrogen (BUN).
NORMAL RANGE FOR CREATNINE
Male: 0.6-1.2 mg/dL Female: 0.5-1.1 mg/dL
Common tests used to determine renal function include creatinine and blood urea nitrogen (BUN).
WHAT DOES AN ELEVATED BLOOD UREA NITROGEN INDICATE
Acute glomerulonephritis
Congestive heart failure
Diabetes mellitus
High-protein diet
Nephrotic syndrome
Renal disease
Severe dehydration
Severe infection
Shock
WHAT DOES AN DECREASE BLOOD UREA NITROGEN INDICATE
Alcohol abuse
Diet inadequate in protein
Hepatitis
Liver failure
Malnutrition
WHAT DOES AN ELEVATED CREATNINE INDICATE
Congestive heart failure
Dehydration
Diabetes mellitus
Glomerulonephritis
Renal failure
Rheumatoid arthritis
Shock
Uremia
Serum creatinine is a waste product of skeletal muscle metabolism. It is excreted by the kidneys. Because creatinine is excreted at a more consistent rate than BUN, serum-level values tend to be more sensitive in detecting renal impairment.
WHAT DOES AN DECREASED CREATNINE INDICATE
Atrophy of muscle
Pregnancy
Serum creatinine is a waste product of skeletal muscle metabolism. It is excreted by the kidneys. Because creatinine is excreted at a more consistent rate than BUN, serum-level values tend to be more sensitive in detecting renal impairment.
Which routes can drug be excreted?
The main route of drug excretion, elimination of drugs from the body, is through the KIDNEYS to become urine.
Drugs are also excreted through
bile,
the lungs,
saliva,
sweat, and
breast milk.
What is Pharmacodynamics
Pharmacodynamics is the study of the effects of drugs on the body.
Drugs act within the body to mimic the actions of the body’s own chemical messengers.
A drugs Primary effect is..
A drug’s primary effect is the desirable response
THERAPEUTIC EFFECT
example
An example of a drug with a primary and secondary effect is diphenhydramine, an antihistamine. The primary effect of diphenhydramine is to treat the symptoms of allergy;. desired effect, ,at bedtime it could be desirable because it causes mild sedation.
A drugs Secondary effect is..
secondary effect may be desirable or undesirable.
SIDE EFFECT
An example of a drug with a primary and secondary effect is diphenhydramine, an antihistamine. the secondary effect is a central nervous system (CNS) depression that causes drowsiness. The secondary effect is undesirable when the patient drives a car