DRUG ACTIONS AND THE BODY Flashcards
drug becomes a solution so that it can
cross the biologic membrane.
PHARMACEUTIC PHASE
Approximately 80% of drugs are taken by
mouth
PHARMACEUTIC PHASE
PHARMACEUTIC PHASE Is also called
Dissolution Phase
Drugs that DON’T HAVE PHARMACEUTIC
PHASE
*SQ
* IM
* IV
3 Phases of Drug Action
- Pharmaceutic
- Pharmacokinetic
- Pharmacodynamics
Breakdown of tablets in smaller particles
DISINTEGRATION
Dissolving of the smaller particles in the GI
fluid before absorption.
DISSOLUTION
Drug in solid form must disintegrate into
small particles to dissolve in liquid.
DISSOLUTION
Process of drug movement to achieve a
drug action.
PHARMACOKINETIC PHASE
Describes how the body handles the
medication
PHARMACOKINETIC PHASE
2 PROCESSES to cross body
membranes
- Diffusion or Passive Movement
- Active Transport Movement
movement of chemical from higher to lower
concentration.
Diffusion or Passive Movement
movement of chemical
against a concentration or electrochemical
gradient.
Active Transport Movement
4 PROCESSES INVOLVED IN
PHARMACOKINETICS
- Absorption
- Distribution
- Metabolism/Biotransformation
- Excretion/Elimination
Movement of drug particles from GI tract to
body fluids
ABSORPTION
this absorption occurs by diffusion thus drug doesn’t require energy to move across a membrane.
Passive absorption
Requires a carrier such as enzyme of
protein to move the drug against a
concentration gradient thus energy is required
Active absorption
Process by which cells carry a drug
across their membrane by engulfing
the drug particle.
Pinocytosis
drug passes to the liver first.
First-Pass/Hepatic First Pass
o Blood flow
o Pain
o Stress
o Hunger
o Fasting
o Food
o pH
FACTORS THAT AFFECT DRUG ABSORPTION
Drug administered through this have the most rapid onset of action
IV
Drug in ________are absorbed faster than tablets of capsules
elixir or syrup formulation
Drug administered in______are absorbed quickly and have more rapid onset of action than those given in opposite
high doses
Subcategory of absorption
BIOAVAILABILITY
percentage of the administered drug
dose that reaches the systematic
circulation
BIOAVAILABILITY
bioavailability of this route occurs after absorption and first pass metabolism
oral route
Percentage of Bioavailability for Oral route
always less than 100%
Percentage of Bioavailability for IV route
100%
Percentage of Bioavailability of Oral drugs that have high first pass hepatic metabolism
20% to 40%.
o Drug form
o Route of administration
o GI mucosa and motility
o Food and other drugs
o Changes in liver metabolism
FACTORS THAT AFFECT BIOAVAILABILITY
caused by
liver dysfunction or inadequate hepatic
blood flow
Changes in liver metabolism
Process by which the drugs become
available to body fluids and body tissues.
DISTRIBUTION
Drugs with a_____of drug distribution have a longer half-life and stays in the body longer
larger volume
Drugs with a_____of drug distribution have a longer half-life and stays in the body longer
larger volume
Heart, liver, kidney, and brain receives the_____blood supply
MOST
Skin, bone, and adipose tissues receive a
_________ blood flow or supply
LOWER
They possess the special anatomical barriers that inhibit many chemicals and medication from entering
Blood – brain barrier and Fetal – placental
barrier
o Blood flow
o Drug’s affinity to the tissue
o Protein binding effect
FACTORS THAT AFFECT DISTRIBUTION
Drugs that are greater than 89% bound to
protein are known as
Diazepam 98%
HIGHLY PROTEIN-BINDING DRUGS
61%-89% bound to protein are
Ex: Erythromycin 70/5
MODERATELY HIGH PROTEIN BOUNDS.
30%-60% drugs bound to protein are
Ex: Aspirin 49%
MODERATELY PROTEIN BOUNDS
Less than 30% drugs bound to protein are
Ex: Amoxicillin 20%
LOW PROTEIN BOUND DRUGS.
This lead to drug toxicity.
Low Serum Albumin Level
Prevent some medication from entering
certain body organs.
BARRIERS TO DRUG DISTRIBUTION
- Blood Brain Barrier
- Placental Barrier
BARRIERS TO DRUG DISTRIBUTION
– to pass this barrier, drug must be lipid soluble and loosely attached to plasma protein
Blood Brain Barrier
shields from possibility of adverse effects but many substances like drugs, nicotine, and alcohol do cross
Placental Barrier
Process of chemically converting a drug to be easily removed from the body.
METABOLISM OR BIOTRANSFORMATION
A process by which the body inactivates, or biotransforms drugs
METABOLISM OR BIOTRANSFORMATION
primary site of drug metabolism
LIVER
makes drug more water soluble and excreted by the kidneys
CONJUGATES
Metabolized the lipid soluble drugs to water soluble for excretion
ROLE OF LIVER IN METABOLISM &
BIOTRANSFORMATION
Some drugs are transformed in active metabolites causing increased pharmacologic response
ROLE OF LIVER IN METABOLISM &
BIOTRANSFORMATION
Time it takes for ½ of the drug concentration to be eliminated.
HALF-LIFE (t1/2)
The time it takes for a drug to reach a
steady state of serum concentration can
be computed
HALF-LIFE (t1/2)
Process where the drug is removed from
the body.
EXCRETION
main route of drug elimination.
KIDNEY
main route of drug elimination.
KIDNEY
a process where some of the drugs is secreted in the bile
BILIARY EXCRETION
- Hepatic metabolism
- Bile
- Feces
- Lungs
- Saliva
- Sweat
- Breastmilk
ROUTES FOR EXCRETION
Common test used to determine renal function
CREATININE CLEARANCE AND BLOOD UREA
NITROGEN (BUN)
A metabolic by-product of muscle that is excreted by the kidney.
CREATININE
Creatinine level can be tested by obtaining urine collection for
12–24-hour
normal creatinine level
85-135 ml/min
therapeutic response of most drugs related to
their level in the plasma
DRUG PLASMA CONCENTRATION
- Minimum effective concentration
- Toxic concentration
PLASMA DRUG LEVELS
amount of drug required to produce a therapeutic effect
Minimum effective concentration
level of drug that will result in serious adverse effects.
Toxic concentration
Plasma drug concentration between the minimum effective drug concentration and toxic concentration.
THERAPEUTIC RANGE
Refers to how the medicine changes the body
PHARMACODYNAMIC PHASE
Refers to how the medicine changes the body
PHARMACODYNAMIC PHASE
During this phase, drug response can cause primary and
secondary effect
PHARMACODYNAMIC PHASE
relationship between the minimal vs the maximal amount of drug dose needed to produce desired drug response
DOSE RESPONSE
time it takes to reach the minimum effective concentration (MEC) after the drug administered
ONSET OF ACTION
occurs when the drug reaches its highest blood or plasma concentration
PEAK ONSET
length of time the drug has a pharmacologic effect
DURATION OF ACTION
drug acts through receptors to initiate a response or to prevent a response.
RECEPTOR THEORY
- Kinase
- Ligand
- G protein
- Nuclear receptors
4 RECEPTOR SYSTEMS
linked receptor
Kinase
Drug activates enzyme inside the cell and the response is INITIATED.
Kinase
Ligand-binding domain for drugbinding is on the cell surface.
Kinase
gated ion channels
Ligand
Channel spans the cell membrane and with this type of receptor, THE CHANNEL OPENS, allowing for the flow of ions into and out of the cell
Ligand
coupled receptor systems.
G protein
- Receptor
- G-protein that binds with
guanosine triphosphate. - Effector that is either and
enzyme or ion channel.
3 COMPONENTS to G protein receptor response
cell nucleus and not on the surface of the cell membrane
Nuclear receptors
Drugs that produce a response.
AGONISTS
Drugs that produce same type of response as the endogenous substance.
AGONISTS
describes a medication that produces a weaker or less efficacious response than an agonist.
PARTIAL AGONISTS
Drug that blocks a response.
ANTAGONISTS
Drugs will occupy a receptor and prevent the endogenous chemical from acting
ANTAGONISTS
- Stimulation or Depression
- Replacement
- Inhibition or killing of organism
- Irritation
4 CATEGORIES OF DRUG ACTION
rate of cell activity or the secretion from the gland increases.
STIMULATES
cell activity and function of a specific organ are reduced
DEPRESSES
replace essential body compound like INSULIN.
REPLACEMENT
drugs that inhibit or kill organisms interfere with bacterial cell growth.
INHIBITION OR KILLING
irritate a specific body part.
IRRITATION
Highest plasma concentration of drug in the px bloodstream
PEAK DRUG LEVEL
Indicates the rate of absorption of a drug.
PEAK DRUG LEVEL
Lowest plasma concentration of a drug.
TROUGH DRUG LEVEL
Indicate the rate of elimination of the drug
TROUGH DRUG LEVEL
Large initial dose of a drug is given when immediate drug response is desired.
LOADING DOSE
A drug is given to achieve a rapid minimum effective concentration in the plasma
LOADING DOSE
Physiologic effects not related to desired drug effects.
SIDE EFFECTS
this can be desirable or undesirable
SIDE EFFECTS
More severe than side effects.
Always undesirable
ADVERSE REACTIONS
Range of untoward effects of drugs that cause mild to severe side effect, including anaphylaxis (cardiovascular
collapse)
ADVERSE REACTIONS
When drug level exceeds the therapeutic range
TOXIC EFFECT/TOXICITY
Happens when overdosing or drug accumulation occur.
TOXIC EFFECT/TOXICITY
A way to compare the doses of two independently administered drugs in terms of how much is needed to produce a response.
POTENCY
Magnitude of maximal response that can be produced from a particular drug.
EFFICACY
Area of pharmacology that examine the role of heredity in drug response.
PHARMACOGENETICS
unpredictable and unexplained drug reactions
IDIOSYNCRATIC RESPONSE
refers to decrease responsiveness over the course of the
therapy.
TOLERANCE
refers to rapid decrease response to the drug.
TACHYPHYLAXIS
a physiological benefit from a compound that may not have the chemical structure of a drug effect
PLACEBO EFFECT