NURSING PHARMACOLOGY

PHARMACOKINETICS & PHARMACODYNAMICS

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PHARMACOKINETICS

● How the body acts on the drug including absorption,

distribution, biotransformation, and excretion.
● In clinical practice, it includes the onset of drug action,
drug half- life, timing of the peak effect, duration of drug
effects, metabolism or biotransformation of the drug,
and the site of excretion.

CRITICAL CONCENTRATION
• The amount of a drug that is needed to cause a
therapeutic effect (recommended dose).
• Too much of a drug will produce toxic (poisonous) effects.
• Too little will not produce the desired therapeutic effects.

LOADING DOSE
• Some drugs may take a prolonged period to reach a critical
concentration.
• If their effects are needed quickly, a loading dose is
recommended.
• A higher dose than that usually used for treatment to PHASES OF PHARMACOKINETICS
reach critical concentration.
• The critical concentration is then maintained by using the
recommended dosing schedule.
1. LIBERATION -----------------------------------------------------------------------------
EXAMPLE • The process in which a pharmaceutical substance is
released from the formulation it is delivered in.
❖ Digoxin (Lanoxin) - a drug used to increase the strength of
• The release of the drug from its dosage form.
heart contractions.
• This must occur before the drug can be absorbed into the
❖ Xanthine bronchodilators (e.g., aminophylline, theophylline)-
body.
used to treat asthma attacks are often started with a loading
dose.
2. ABSORPTION ---------------------------------------------------------------------------
DYNAMIC EQUILIBRIUM • It refers to what happens to a drug from the time it is
introduced to the body until it reaches the circulating
• The actual concentration that a drug reaches in the fluids and tissues.
body results from a dynamic equilibrium involving • Site of absorption: GI tract either orally or rectally, mucous
several processes: membranes, skin, lungs, muscles, or subcutaneous
a. Absorption from the site of entry tissues.
b. Distribution to the active site
c. Biotransformation (metabolism) in the liver
d. Excretion from the body
• These processes are key elements in determining the
GENERAL CLASSIFICATION OF ROUTES
amount of drug (dose) and the frequency of dose
repetition (scheduling) required to achieve the critical a. ENTERAL ------------------------------------------------------------------------------------
concentration for the desired length of time. • drugs administered directly in the gastrointestinal tract.
• When administering a drug, the nurse needs to consider the
phases of pharmacokinetics so that the drug regimen can
be made as effective as possible.

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b. PARENTERAL ----------------------------------------------------------------------------- INTRAVENOUS ROUTE -------------------------------------------------------------------------

• drugs administered that by-pass the gastrointestinal • reach their full strength at the time of injection, avoiding
tract. initial breakdown, have an immediate onset and are
fully absorbed at administration because they directly
enter the blood stream.
• These drugs are more likely to cause toxic effects
because the margin for error in dose is much smaller.

INTRAMUSCULAR ROUTE --------------------------------------------------------------------

• absorbed directly into the capillaries in the muscle and
sent into circulation.
• This takes time because the drug must be picked up by
the capillary and taken into the veins.
• Men have more vascular muscles than women do. As a
result, drugs administered to men via the IM route reach
a peak level faster than they do in women.

SUBCUTANEOUS ROUTE -----------------------------------------------------------------

• deposit the drug just under the skin, where it is slowly
absorbed into circulation.
• Timing of absorption varies with subcutaneous injection,
depending on the fat content of the injection site and
the state of local circulation.

TOPICAL ROUTE ----------------------------------------------------------------------------------

• Suitable on intact skin and others that contain a
medication are used for the treatment of broken skin or a
wound.
c. PERCUTANEOUS -----------------------------------------------------------------------
• drugs administered through the skin or mucous
membrane. TRANSDERMAL -----------------------------------------------------------------------------------
• absorbed from the surface of the skin.

OPTHALMIC ROUTE --------------------------------------------------------------------------

• medications are administered and absorbed in the eyes.

OTIC ROUTE ---------------------------------------------------------------------------------------

• absorbed from the ears.

INHALATION ROUTE ----------------------------------------------------------------------------

• absorbed in the lungs via the nose.

OTHER ROUTES OF ADMINISTRATION

o NGT bolus route
o Intravaginal route
o Intravenous piggyback
o Rectal route
o Buccal and sublingual routes
o Intrathecal
o Intracardial
ROUTES OF ADMINISTRATION o Intra-articular
o Nasal
o Intradermal
ORAL ROUTE ----------------------------------------------------------------------------------------
• slow absorption, most frequently used, less expensive,
safest, and patients can easily continue their drug regimen
at home when they are taking medications.
• It subjects the drug to several barriers aimed at
destroying ingested foreign chemicals.
• When food is present, stomach acidity is higher and the
stomach empties more slowly, thus exposing the drug to the
acidic environment for a longer period.
• Certain foods that increase stomach acidity, such as
milk products, alcohol, and protein, also speed the
breakdown of many drugs.
• Oral drugs ideally are to be given 1 hour before or 2 hours
after a meal.

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FACTORS AFFECTING ABSORPTION IN THE 3. DISTRIBUTION -------------------------------------------------------------------------

DIFFERENT ROUTES • It involves the movement of a drug to the body’s tissues.
• Factors that can affect distribution include the drug’s
lipid solubility and ionization and the perfusion of the
reactive tissue.
• Tissue perfusion is a factor in treating a patient with
ROUTE FACTORS
diabetes who has a lower-leg infection and needs
antibiotics to destroy the bacteria in the area.
• In this case, systemic drugs may not be effective
INTRAVENOUS - None: direct entry into the venous because part of the disease process involves changes
system in the vasculature and decreased blood flow to some
areas, particularly the lower limbs.
• If there is no adequate blood flow to the area, little
- Perfusion or blood flow to the muscle
antibiotic can be delivered to the tissues, and little
- Fat content of the muscle antibiotic effect will be seen.
INTRAMUSCULAR - Temperature of the muscle: cold
• Patients in a cold environment may have constricted
causes vasoconstriction and decreases
blood vessels (vasoconstriction) in the extremities,
absorption; heat causes vasodilation
which would prevent blood flow to those areas.
and increases absorption
• The circulating blood would be unable to deliver drugs
to those areas, and the patient would receive little
therapeutic effect from drugs intended to react with those
- Perfusion or blood flow to the Tissue
tissues.
- Fat content of the tissue Temperature
SUBCUTANEOUS of the tissue: cold causes
vasoconstriction and decreases
absorption; heat causes vasodilation DISTRIBUTION PROCESSES
and increases absorption

1. PROTEIN BINDING
- Acidity of stomach • Some drugs are tightly bound and are released very
PO (ORAL) - Length of time in stomach slowly.
- Blood flow to gastrointestinal tract • These drugs have a very long duration of action
- Presence of interacting foods or drugs because they are not free to be broken down or
excreted and are released very slowly into the
reactive tissue
PR (RECTAL) - Perfusion or blood flow to the rectum • Some drugs are loosely bound; they tend to act
- Lesions in the rectum quickly and to be excreted quickly.
- Length of time retained for absorption • Some drugs compete with each other for protein
binding sites, altering effectiveness or causing
toxicity when the two drugs are given together.
MUCOUS - Perfusion or blood flow to the area
MEMBRANES - Integrity of the mucous membranes
(SUBLINGUAL, - Presence of food or smoking 2. BLOOD- BRAIN BARRIER
BUCCAL) - Length of time retained in area
• It is a cellular activity that keeps foreign invaders,
poisons and similar materials away from the CNS.
• Drugs that are more likely to pass through the blood–
TOPICAL (SKIN) - Perfusion or blood flow to the area
brain barrier and reach the CNS.
- Integrity of skin
• Almost all antibiotics are not lipid soluble and
cannot cross the blood– brain barrier. Effective
antibiotic treatment can occur only when the infection
- Perfusion or blood flow to the area
is severe enough to alter the blood brain barrier and
INHALATION - Integrity of lung lining
allow antibiotics to cross
- Ability to administer drug properly
• Although many drugs can cause adverse CNS effects,
these are often the result of indirect drug effects
and not the actual reaction of the drug with CNS
tissue.
ABSORPTION PROCESSES • For example, alterations in glucose levels and
electrolyte changes can interfere with nerve
functioning and produce CNS effects such as
a. PASSIVE DIFFUSION ------------------------------------------------------------------ dizziness, confusion, or changes in thinking ability.
• movement of drug from higher to lower concentration
and does not require energy.
• Occurs quickly in smaller molecules, soluble in water & 3. PLACENTA & BREAST MILK
lipids, and has no electrical charge that could repel it • Many drugs readily pass through the placenta and
from the cell membrane. affect the developing fetus in pregnant women.
• It is best not to administer any drugs to pregnant
women.
b. ACTIVE TRANPOST ------------------------------------------------------------------- • Drugs should be given only when the benefit
• That uses energy to actively move a molecule across a clearly outweighs any risk.
cell membrane.
• The molecule may be large, or it may be moving against
a concentration gradient. 4. METABOLISM/ BIOTRANSFORMATION ----------------------------------
• It is a very important process in drug excretion in the kidney. • The liver is the most important site of this process
wherein drugs are changed into new, less active
chemicals.
c. FILTRATION -------------------------------------------------------------------------------
• Everything that is absorbed from the GI tract first
• involves movement through pores in the cell enters the liver to be “treated.”
membrane, either down a concentration gradient or as • The liver detoxifies many chemicals and uses
a result of the pull of plasma proteins (when pushed by others to produce needed enzymes and structures.
hydrostatic, blood, or osmotic pressure).
• It is another process the body commonly uses in drug
excretion.

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FIRST- PASS EFFECT DRUG HALF- LIFE

• The phenomenon in which drugs given orally are carried • The time it takes for drug in the body to decrease to one
directly to the liver after absorption, where they may be half of the peak level it previously achieved.
largely inactivated by liver enzymes before they can • This information is important in determining the appropriate
enter the general circulation. timing for a drug dose or determining the duration of a
• Oral drugs frequently are given in higher doses than drug’s effect on the body.
drugs given by other routes because of this early • The half-life that is indicated in any drug monograph is the
breakdown. half-life for a healthy person.
• Using this information, one can estimate the half-life of a
drug for a patient with kidney or liver dysfunction
HEPATIC ENZYME SYSTEM allowing the prescriber to make changes in the dosing
• Phase I biotransformation- involves oxidation- schedule.
reduction, or hydrolysis of the drug via the cytochrome
P450 system of enzymes.
• Phase II biotransformation- usually involves a DETERMINING THE IMPACT OF HALF-LIFE ON DRUG LEVELS
conjugation reaction that makes the drug more polar
and more readily excreted by the kidneys. A patient is taking a drug that has a half-life of 12 hours.
• Increased activity in an enzyme system speeds the You are trying to determine when a 50-mg dose of the drug will
metabolism of the drug. be gone from the body:
• This explains why some drugs cannot be taken together ✓ In 12 hours, half of the 50 mg (25 mg) would be in the body.
effectively. ✓ In another 12 hours (24 hours), half of 25 mg (12.5 mg)
• The presence of one drug speeds the metabolism of would remain in the body.
others, preventing them from reaching their ✓ After 36 hours, half of 12.5 mg (6.25 mg) would remain.
therapeutic levels. ✓ After 48 hours, half of 6.25 mg (3.125 mg) would remain.
• Some drugs inhibit an enzyme system, making it less ✓ After 60 hours, half of 3.125 (1.56 mg) would remain.
effective. ✓ After 72 hours, half of 1.56 (0.78 mg) would remain.
• Therefore, any drug that is metabolized by that system will ✓ After 84 hours, half of 0.78 (0.39 mg) would remain.
not be broken down for excretion, and the blood levels of ✓ Twelve more hours (for a total of 96 hours) would reduce
that drug will increase, often to toxic levels. the drug amount to 0.195 mg.
✓ Finally, 12 more hours (108 hours) would reduce the
• These actions also explain why liver disease is often a
contraindication or a reason to use caution when amount of the drug in the body to 0.097 mg, which would
be quite negligible.
administering certain drugs. If the liver is not functioning
✓ Therefore, it would take 472 to 5 days to clear the drug from
effectively, the drug will not be metabolized as it should be,
and toxic levels could develop rather quickly. the body.

5. EXCRETION ------------------------------------------------------------------------------
• It is the removal of a drug from the body.
PHARMACOERGONOMICS
• The kidneys, skin, saliva, lungs, bile and feces are some
of the routes used to excrete drugs. • It is an area of study that explores the unique differences
• Drugs that have been made water soluble in the liver in response to drugs that each individual possesses
are often readily excreted from the kidney by glomerular based on genetic makeup.
filtration—the passage of water and water-soluble • Predictable differences in the pharmacokinetics and
components from the plasma into the renal tubule. pharmacodynamic effects of drugs can be anticipated
• Kidney dysfunction and urine acidity are factors to with people of cultural backgrounds.
consider in drug toxicity due to inability to excrete
poisonous substances.
• Dose adjustment needs to be considered if a patient has
problems with either the liver or the kidneys. FACTORS AFFECTING RESPONSES TO DRUG
• Assessment should be done before starting drug
therapy.
A. WEIGHT --------------------------------------------------------------------------------------
• People who are much heavier may require larger doses
to get a therapeutic effect from a drug because they
have increased tissues to perfuse and increased receptor
sites in some reactive tissue.
• Toxic effects may occur at the recommended dose if
the person is very small.

B. AGE ----------------------------------------------------------------------------------------------
• Older adults undergo many physical changes that are
a part of the aging process.
• Their bodies may respond very differently in all aspects
of pharmacokinetics—less effective absorption,
distribution, perfusion, altered biotransformation or
metabolism and less effective excretion.
• Children metabolize many drugs differently than adults
do, and they have immature systems for handling drugs.
• Many drugs come with recommended pediatric doses,
and others can be converted to pediatric doses.

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G. IMMUNOLOGIC FACTORS -----------------------------------------------------------

• People can develop an allergy to a drug.
• After exposure to its proteins, a person can develop
antibodies to a drug.
• With future exposure to the same drug, that person may
experience a full- blown allergic reaction.

H. PSYCHOLOGICAL FACTORS --------------------------------------------------------

• The patient’s attitude about a drug has an effect on how
that drug works.
• A drug is more likely to be effective if the patient thinks
it will work than if the patient believes it will not work.
• This is called the PLACEBO EFFECT.
• The patient’s personality also influences compliance
with the drug regimen.
• Some people willingly follow a prescribed regimen.
• Others do not trust the medical system.

I. ENVIRONMENTAL FACTORS -------------------------------------------------------

• Some drug effects are enhanced by a quiet, cool, non-
stimulating environment.
• Other drug effects may be influenced by temperature.
• EXAMPLE # 1: Sedating drugs are given to help a
patient relax or to decrease tension. Reducing external
stimuli to decrease tension and stimulation help the drug be
more effective.
• EXAMPLE # 2: Antihypertensives that work well during
C. GENDER ------------------------------------------------------------------------------------- cold, winter months may become too effective in
• When giving IM injections, for it is important to remember warmer environments, when natural vasodilation may
that men have more vascular muscles, so the effects of lead to a release of heat that tends to lower the blood
the drug will be seen sooner in men than in women. pressure.
• Women have more fat cells than men do, so drugs that
deposit in fat may be slowly released and cause effects for
a prolonged period. J. TOLERANCE ---------------------------------------------------------------------------------
• EXAMPLE, gas anesthetics have an affinity for depositing • Tolerance may arise because of increased
in fat and can cause drowsiness and sedation sometimes biotransformation of the drug, increased resistance to
weeks after surgery. its effects, or other pharmacokinetic factors.
• When tolerance occurs, the drug no longer causes the
same reaction.
D. PHYSIOLOGIC FACTORS -------------------------------------------------------------- • Therefore, increasingly larger doses are needed to
• Physiological differences such as diurnal rhythm of the achieve a therapeutic effect.
nervous and endocrine systems, acid–base balance,
hydration, and electrolyte balance can affect the way that EXAMPLE:
a drug works on the body and the way that the body handles • Morphine is an opiate used for pain relief. The longer
the drug. morphine is taken, the more tolerant the body becomes to
• If a drug does not produce the desired effect, one the drug, so that larger and larger doses are needed to
should review the patient’s acid- base and electrolyte relieve pain.
profiles and the timing of the drug • It should be given in smaller doses or in combination with
other drugs that may also relieve pain.
• CROSS-TOLERANCE—or resistance to drugs within
E. PATHOLOGIC FACTORS -------------------------------------------------------------- the same class may also occur in some situations.
• The disease that the drug is intended to treat can
change the functioning of the chemical reactions within
the body and thus change the response to the drug. K. CUMULATION ------------------------------------------------------------------------------
• Body conditions can change the basic pharmacokinetics of • If a drug is taken in successive doses at intervals that
a drug are shorter than recommended, or if the body is unable
to eliminate a drug properly, the drug can accumulate
EXAMPLES: in the body, leading to toxic levels and adverse effects.
✓ GI disorders can affect the absorption of many oral This can be avoided by following the drug regimen
drugs. precisely.
✓ Vascular diseases and low blood pressure alter the .
distribution of a drug, preventing it from being
delivered to the reactive tissue, thus rendering the L. CUMULATION ------------------------------------------------------------------------------
drug nontherapeutic. • When two or more drugs or substances are taken
✓ Liver or kidney diseases affect the way that a drug together, there is a possibility that an interaction can
is biotransformed and excreted and can lead to toxic occur, causing unanticipated effects in the body.
reactions when the usual dose is given.

F. GENETICS ------------------------------------------------------------------------------------
• Some people lack certain enzyme systems necessary
for metabolizing a drug, whereas others have overactive
enzyme systems that cause drugs to be broken down
more quickly.
• Others have differing metabolisms or slightly different
enzymatic makeups that alter their chemical reactions and
the effects of a given drug.

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DRUG-DRUG OR DRUG-ALTERNATIVE THERAPY INTERACTIONS DRUG-FOOD INTERACTIONS

- Clinically significant drug-drug interactions occur with drugs • For the most part, a drug-food interaction occurs when the
that have small margins of safety. drug and the food are in direct contact in the stomach.
- If there is very little difference between a therapeutic dose and Some foods increase acid production, speeding the
a toxic dose of the drug, interference with the drug's breakdown of the drug molecule and preventing
pharmacokinetics or pharmacodynamics can produce serious absorption and distribution of the drug. Some foods
problems. For example, drug-drug interactions can occur in the chemically react with certain drugs and prevent their
following situations: absorption into the body.
• The antibiotic tetracycline cannot be taken with iron
products for this reason. Tetracycline also binds with
a. AT THE SITE OF ABSORPTION: One drug prevents or calcium to some extent and should not be taken with foods
accelerates absorption of the other drug. For example, or other drugs containing calcium.
the antibiotic tetracycline is not absorbed from the GI tract • Grapefruit juice has been found to affect liver enzyme
if calcium or calcium products (milk) are present in the systems for up to 48 hours after it has been ingested. This
stomach. can result in increased or decreased serum levels of certain
drugs. Many drugs come with the warning that they should
-------------------------------------------------------------------------------------------------------------- not be combined with grapefruit juice. This drug-food
interaction does not take place in the stomach, so the
b. DURING DISTRIBUTION: One drug competes for the grapefruit juice needs to be avoided the entire time the drug
protein-binding site of another drug, so the second is being used, not just while the drug is in the stomach.
drug cannot be transported to the reactive tissue. For • In most cases, oral drugs are best taken on an empty
example, aspirin competes with the drug methotrexate stomach. If the patient cannot tolerate the drug on an
(Rheumatrex) for protein-binding sites. Because aspirin is empty stomach, the food selected for ingestion with the
more competitive for the sites, the methotrexate is drug should be known not to interact with it. Drug
bumped off, resulting in increased release of methotrexate monographs usually list important drug- food interactions
and increased toxicity to the tissues. and give guidelines for avoiding problems and optimizing
the drug's therapeutic effects.
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c. DURING BIOTRANSFORMATION: One drug stimulates or
blocks the metabolism of the other drug. For DRUG-LABORATORY TEST INTERACTIONS
example, warfarin (Coumadin), an oral anticoagulant, is • As explained previously, the body works through a series of
bio- transformed more quickly if it is taken at the same time chemical reactions. Because of this, administration of a
as barbiturates, rifampin, or many other drugs. Because particular drug may alter results of tests that are done
the warfarin is biotransformed to an inactive state more on various chemical levels or reactions as part of a
quickly, higher doses will be needed to achieve the diagnostic study. This drug-laboratory test interaction
desired effect. Patients who use St. John's wort may is caused by the drug being given and not necessarily
experience altered effectiveness of several drugs that are by a change in the body's responses or actions. Keep
affected by that herb's effects on the liver. Digoxin, these interactions in mind when evaluating a patient's
theophylline, oral contraceptives, anti- cancer drugs, diagnostic tests. If one test result is altered and does not fit
drugs used to treat HIV, and antidepressants are all in with the clinical picture or other test results, consider the
reported to have serious interactions with St. John's wort. possibility of a drug-laboratory test interference.
• For example, dalteparin (Fragmin), a low-molecular- weight
-------------------------------------------------------------------------------------------------------------- heparin used to prevent deep vein thrombosis after
abdominal surgery, may cause increased levels of the liver
d. DURING EXCRETION: One drug competes for excretion enzymes aspartate aminotransferase and ala- nine
with the other drug, leading to accumulation and toxic aminotransferase with no injury to liver cells or hepatitis.
effects of one of the drugs. For example, digoxin
(Lanoxin) and quinidine are both excreted from the same
sites in the kidney. If they are given together, the quinidine
is more competitive for these sites and is excreted,
OPTIMAL THERAPEUTIC EFFECT
resulting in increased serum levels of digoxin, which • As overwhelming as all this information may seem, most
cannot be excreted. patients can follow a drug regimen to achieve optimal
therapeutic effects without serious adverse effects.
-------------------------------------------------------------------------------------------------------------- • Avoiding problems is the best way to treat adverse or
ineffective drug effects. One should incorporate basic
history and physical assessment factors into any plan
e. AT THE SITE OF ACTION: One drug may be an of care so that obvious problems can be spotted and
antagonist of the other drug or may cause effects that handled promptly. If a drug just does not do what it is
oppose those of the other drug, leading to no expected to do, further examine the factors that are known
therapeutic effect. This is seen, for example, when an to influence drug effects.
antihypertensive drug is taken with an antiallergy drug that • Frequently, the drug regimen can be modified to deal
also increases blood pressure. The effects on blood with that influence. Rarely is it necessary to completely
pressure are negated, and there is a loss of the anti- stop a needed drug regimen because of adverse or
hypertensive effectiveness of the drug. If a patient is taking intolerable effects. In many cases, the nurse is the
antidiabetic medication and also takes the herb ginseng, caregiver in the best position to assess problems early.
which lowers blood glucose levels, he or she may
experience episodes of hypoglycemia and loss of blood
glucose control. Whenever two or more drugs are being
given together, first consult a drug guide for a listing of
clinically significant drug-drug interactions. Sometimes
problems can be avoided by staggering the administration
of the drugs or adjusting their doses.

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SUMMARY PHARMACODYNAMICS
• Pharmacodynamics is the study of the way that drugs affect • Study of interactions between chemical components of
the body. living systems and the foreign chemicals including
• Most drugs work by replacing natural chemicals, by drugs, that enter those systems
stimulating normal cell activity, or by depressing normal cell • “How drugs affect the body”
activity.
• Chemotherapeutic agents work by interfering with normal
cell functioning, causing cell death. The most desirable THERAPEUTIC INDEX
chemotherapeutic agents are those with selective toxicity to
• Therapeutic window/ ratio
foreign cells and foreign cell activities.
• Comparison between amount of drug that causes harm/
• Drugs frequently act at specific receptor sites on cell
toxicity and the amount of drug promoting therapeutic
membranes to stimulate enzyme systems within the cell
effect.
and to alter the cell's activities.
• Mathematically expressed as TD50/ ED50
• Pharmacokinetics—the study of the way the body deals
➢ TD= Toxic dose, dose where 50% experience toxicity
with drugs-includes absorption, distribution,
is reached
biotransformation, and excretion of drugs.
➢ ED= Median effective dose, a dose where 50%
• The goal of established dosing schedules is to achieve a
critical concentration of the drug in the body. This critical
concentration is the amount of the drug necessary to
achieve the drug's therapeutic effects.
• Arriving at a critical concentration involves a dynamic
equilibrium among the processes of drug absorption,
distribution, metabolism or biotransformation, and
excretion.
• Absorption involves moving a drug into the body for
circulation. Oral drugs are absorbed from the small
intestine, undergo many changes, and are affected by
many things in the process. IV drugs are injected directly
into the circulation and do not need additional absorption.
• Drugs are distributed to various tissues throughout the body
depending on their solubility and ionization. Most drugs are
bound to plasma proteins for transport to reactive tissues.
• Drugs are metabolized or biotransformed into less toxic
chemicals by various enzyme systems in the body. The liver LOW THERAPEUTIC INDEX = UNSAFE, Needs monitoring
is the primary site of drug metabolism or biotransformation. HIGH/ WIDE THERAPEUTIC INDEX = Safe drugs
The liver uses the cytochrome P450 enzyme system to alter
the drug and start its biotransformation.
• The first-pass effect is the breakdown of oral drugs in the GRADE DOSE RESPONSE RELATIONSHIP
liver immediately after absorption. Drugs given by other
routes often reach reactive tissues before passing through
the liver for biotransformation.
DOSE RESPONSE CURVE ---------------------------------------------------------------------
• Drug excretion is removal of the drug from the body. This
occurs mainly through the kidneys. • Illustration that evaluates and compares the efficacy and
• The half-life of a drug is the period of time it takes for an potency of related drugs
amount of drug in the body to decrease to one half of the
peak level it previously achieved. The half-life is affected by
all aspects of pharmacokinetics. Knowing the half-life of a DRUG POTENCY -----------------------------------------------------------------------------------
drug helps in predicting dosing schedules and duration of • Refers to concentration/ amount of drug need to
effects. achieve therapeutic effect
• The actual effects of a drug are determined by its • Lesser amount needed to achieve therapeutic effect, the
pharmacokinetics, its pharmacodynamics, and many more potent the drug is (LESSER THE BETTER)
human factors that can change the drug's effectiveness.
• To provide the safest and most effective drug therapy, the
nurse must consider all of the possible factors that influence DRUG EFFICACY -----------------------------------------------------------------------------------
drug concentration and effectiveness. • Level to which the drug reaches the therapeutic effect
• HIGHER EFFECT= More efficacious the drug is

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PERCENT ADHERENCE
• The extent to which a person’s behavior when taking
medication following a diet or executing lifestyle
changes, corresponds with agreed recommendations
from health care provider.
• Non- adherent behaviors include missing doses, taking
drug holidays, taking extra doses when not feeling well,
changing the timing of doses, or inconsistently not taking
medications= liver damage

RESONS FOR NON- ADHERENCE

a) Complex instructions (Educate patients; they should clearly
understand, answer questions)
b) Asymptomatic diseases- no more symptoms so they stop
the medication.
c) Side effects of medications
d) Cognitive impairment- Alzheimer’s
e) Poor insight to illness- Educated abt. Their illness
f) Cost of medication
g) Poor nurse-patient relationship
h) Inadequate discharge planning
i) Lack of follow up
j) Lack of belief in the regimen

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CELLULAR RECEPTOR SITES AND DRUG ACTION D. NON-COMPETITIVE ANTAGONST -----------------------------------------------

• Drugs that react with specific receptor sites on a cell
DRUGS USUALLY WORK IN ONE OF FOUR WAYS: and by reacting there, prevent the reaction of another
✓ To replace or act as substitutes for missing chemicals. chemical with a different receptor site on that cell.
✓ To increase or stimulate certain cellular activities.
✓ To depress or slow cellular activities.
✓ To interfere with the functioning of foreign cells, such
as invading microorganisms or neoplasms.

RECEPTOR SITES ---------------------------------------------------------------------------------

• Areas on the cell membrane where drugs or chemical
react to cause an effect within the cell.
• Nearby enzymes break down the reacting chemicals
and open the receptor site for further stimulation.
• The interaction between the chemical and the receptor
site affects enzyme systems within the cell.
• The activated enzyme systems then produce certain
effects, such as increased or decreased cellular activity,
changes in cell membrane permeability, or alterations in
cellular metabolism.

A. AGONIST --------------------------------------------------------------------------------------
• These are drugs that interact directly with receptor
sites to cause the same activity that natural chemicals DRUG - ENZYME INTERACTION ----------------------------------------------------------
would cause at that site. • Drugs can interfere with the enzyme systems that act as
• For example, insulin reacts with specific insulin-receptor catalysts for various chemical reactions.
sites to change cell membrane permeability, thus promoting • Enzyme systems work in a cascade fashion, with one
the movement of glucose into the cell. enzyme activating another until a cellular reaction
eventually occurs.
• If a single step in one of the many enzyme systems is
blocked, normal cell function is disrupted.
✓ Acetazolamide (Diamox) is a diuretic that blocks
the enzyme carbonic anhydrase, which
subsequently causes alterations in the hydrogen
ion and water exchange system in the kidney, as
well as in the eyes.
B. ANTAGONIST -------------------------------------------------------------------------------
• These are drugs act to prevent the breakdown of natural
chemicals that are stimulating the receptor site.
✓ Monoamine oxidase (MAO) inhibitors block the
breakdown of norepinephrine by the enzyme
MAO. Normally, MAO breaks down
norepinephrine. The blocking action of MAO
inhibitors allows norepinephrine to stay on the
receptor site, stimulating the cell longer and
leading to prolonged norepinephrine effects.
✓ Those effects can be therapeutic (e.g., relieving
depression) or adverse (e.g., increasing heart
rate and blood pressure).

C. COMPETITIVE ANTAGONIST -------------------------------------------------------

• Drugs react with receptor sites to block normal
stimulation, producing no effect.
• Curare occupies receptor sites for acetylcholine, which is
necessary for muscle contraction and movement.
• Curare causing paralysis.

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NURSING PHARMACOLOGY | PHARMACOKINETICS & PHARMACODYNAMICS

SELECTIVE TOXICITY ---------------------------------------------------------------------------

• The ability of a drug to attack only those systems found in
foreign cells.
• Penicillin, an antibiotic affects an enzyme system unique to
bacteria, causing bacterial cell death without disrupting
normal human cell functioning.

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