Professional Documents
Culture Documents
Janeirah Q. Manalundong
Faculty, College of Health Sciences
September 2020
UNIT I: FUNDAMENTAL CONCEPTS OF PHARMACOLOGY
Nurses have a vital role in drug therapy because their responsibility is not just safe administration
of medications but also adequately performing the nursing process all throughout the drug therapy—
thorough assessment, proper planning, giving the appropriate and necessary nursing interventions, and
evaluation of the expected outcomes of care. For a nurse to be able to adequately perform these vital
roles, one must have a deeper understanding on the fundamental concepts of pharmacology. Topics
included in this unit are the following:
þ Definition of Pharmacology
þ Definition of Key Terms
þ Classes of Drugs
þ Drug Names
þ Drug Information
þ Phases of Drug Evaluation
þ Drug Legislations and Standards
þ Cultural and Ethical Considerations in Pharmacology
þ Pharmaceutics
þ Pharmacokinetics
þ Pharmacodynamics
þ Pharmacotherapeutics
þ Factors Influencing Responses to Drugs
Introduction
In this learning module, we will be focusing on drug action and dynamics which is divided into
different topics—basic areas of pharmacology, pharmacotherapeutics, pharmacokinetics,
pharmacodynamics, and factors influencing responses to drugs. These are salient topics to strengthen and
deepen your knowledge and understanding on what happens after a drug is administered, what then is
the right dose to be administered, what a drug does to our body and how our body affects the drug. Thus,
foundational knowledge on the science of drug action will equip you with the right knowledge, skills, and
attitude toward safe drug administration, appropriate nursing actions/management, and effective patient
education.
Learning Outcomes
Drug Action
Drug action can be illustrated by following the movement of the drug molecule throughout the
body, starting from the time the initial dose of drug enters the patient’s body, to its interaction with its
target site, until finally, the drug has completely moved out of the body. A number of questions arise
from this scenario:
ü How does the drug know where to go? Does it know where to go?
ü Why would the medicine be administered in one manner and not another? When would
a specific route be chosen?
ü What happens to the body after the drug is administered? Where else does the drug go
as it moves throughout the body?
ü After the drug is administered, how long does it take the drug to work?
ü How does the drug get into its intended site of action? Once there, how does it work?
To safely administer medications, a nurse must know the answers to a range of potential questions
about his or her patient’s medication therapy.
The pharmaceutic phase is the first phase of drug action. In the gastrointestinal tract, drugs need
to be in a solution so they can be absorbed. A drug in solid form (tablet, capsule, or powder) must
disintegrate (breakdown) into small particles to dissolve into a liquid, a process known as dissolution.
Drugs in liquid form are already in solution.
& Pharmaceutics. Lilley, L.L., Collins, S.R., & Snyder, J.S. Pharmacology and the Nursing
Process, 8th Ed. Part 1, Chapter 2.
& Routes of Administration. Berman, A., Snyder, S., & Fraudsen, G. (2016). Kozier and
Erb’s Fundamentals of Nursing: Concepts, Process, and Practice. 10th Ed. Pearson
Education, Inc. Chapter 35, pp. 758 – 759.
Absorption
Absorption is the movement of drug particles from the GI tract to body fluids by passive
absorption, active absorption, or pinocytosis. Most oral drugs are absorbed into the surface area of the
small intestine through the action of the extensive mucosal villi. Absorption is
The rate of drug
reduced if the villi are decreased in number because of disease, drug effect, or absorption is dependent
the removal of small intestine. on the route of drug
administration.
The GI membrane is
composed mostly of lipid (fat) and protein, so drugs that are
lipid-soluble pass rapidly through the GI membrane. Water-
soluble drugs need a carrier, either enzyme or protein, to pass
through the membrane. Large particles pass through the cell
membrane if they are nonionized (have no positive or negative
charge). Weak acid drugs such as aspirin are less ionized in the
stomach, and they pass through the stomach lining easily and
rapidly.
The three major processes of drug absorption.
is chemically changed into inactive metabolites in the liver, then a much smaller Drugs administered via
amount of drug will pass into the circulation (i.e., will be bioavailable). Such drug Intravenous route are 100%
bioavailable.
is said to have a high first-pass effect. First-pass effect reduces the
bioavailability of the drug to less than 100%. Two drug products having the same
bioavailability and same concentration of active ingredient are said to be bioequivalent (e.g., a brand-
name drug and the same generic drug).
Distribution
The process of drug distribution is the movement of the drug from, Drugs are distributed first to those
or “out of”, the systemic circulation to its target site of action. The areas with extensive blood supply.
Areas of rapid distribution: Heart,
physiochemical characteristics of the drug itself dictate where the drug liver, kidneys, and brain.
“goes” as it moves throughout the body. Drug distribution is influenced by Areas of slower distribution:
muscle, skin, fat.
blood flow, the drug’s affinity to the tissue, and the protein-binding effect. In
addition, volume of drug distribution is dependent on the drug dose and its
concentration in the body.
Protein Binding
When two highly protein bound drugs are given concurrently, they
compete for protein-binding sites, thus causing more free drug to be released into the circulation. In this
situation, drug accumulation and possible drug toxicity can result. Also, a low serum protein level
decreases the number of protein-binding sites and can cause an increase in the amount of free drug in
the plasma. Drug toxicity may then result. Drug dose is prescribed according to the percentage in which
the drug binds to protein.
Protein
Bound (%)
>89% Highly protein-bound drugs
61% - 89% Moderately high protein-bound drugs
30% - 60% Moderately protein-bound drugs
<30% Low protein-bound drugs
Metabolism (Biotransformation)
Metabolism is the process by which the body inactivates or biotransforms drugs. Drugs can be
metabolized in several organs; however, the liver is the primary site of metabolism. Most drugs are
inactivated by liver enzymes and are then converted or transformed by Liver cirrhosis and hepatitis alter
hepatic enzymes to inactive metabolites or water-soluble substances for drug metabolism by inhibiting the
drug metabolizing enzymes in the
excretion. liver. When the drug metabolism
rate is decreased, excess drug
Cytochrome P-450 accumulation can occur and lead to
enzymes The half-life (t½) of a drug is the time it toxicity.
The family of enzymes takes for one half of the drug concentration to be
most notable and
eliminated. Metabolism and elimination affect the
responsible for chemically
changing the structure ofhalf-life of a drug. For example, with the liver or kidney dysfunction, the half-life
drug molecules.
of the drug is prolonged and less drug is metabolized and eliminated. A short
half-life is considered to be 4 to 8 hours, and a long one is 24 hours or longer. If
the drug has long half-life, it takes several days for the body to completely eliminate the drug.
A drug goes through several half-lives before more than 90% of the drug is eliminated. If the
patient takes 650mg of aspirin and the half-life is 3 hours, it takes 3 hours for the first half-life to eliminate
325 mg, 6 hours for the second half-life to eliminate an additional 162 mg, and so on until the sixth half-
life (or 18 hours), when 10 mg of aspirin is left in the body (refer to the table below).
The main route of drug elimination is through the kidneys (urine). Other routes include bile, feces,
lungs, saliva, sweat, and breast milk. The kidneys filter free unbound drugs, water-soluble drugs, and drugs
that are unchanged. The lungs eliminate volatile drug substances and products metabolized to carbon
dioxide (CO2) and water (H2O).
The urine pH influences drug excretion. Urine pH varies from 4.5 to Large quantities of cranberry
8. Acidic urine promotes elimination of weak base drugs, and alkaline urine juice can decrease urine pH,
causing acidic urine and thus
promotes elimination of weak acid drugs. Aspirin, a weak acid, is excreted inhibiting elimination of aspirin.
rapidly in alkaline urine. If a person takes an overdose of aspirin, sodium
bicarbonate may be given to change the urine pH to alkaline to promote
excretion of the drug.
Common tests used to determine renal function are creatinine clearance (CLcr)
Creatinine is a metabolic
and blood urea nitrogen (BUN). The creatinine clearance test compares the level
by-product of muscle that
is excreted by the kidneys.
of creatinine in the urine with the level of creatinine in the blood. It varies with
age and gender. Glomerular filtration rate (GFR) may be the best test, but it is
expensive and not so commonly used. A decrease in GFR results in an increase in serum creatinine level
and a decrease in urine creatinine clearance.
With renal dysfunction either in older adults or as result of kidney disorders, drug dosage usually
needs to be decreased. In these cases, the drug dosage usually needs to be determined to establish
appropriate drug dosage. Continuous dosing according to a prescribed dosing regimen without evaluating
creatinine clearance could result in drug toxicity.
Supplementary Resources
& Pharmacokinetics. Adams, M., Holland, N., & Urban, C. (2014). Pharmacology for Nurses: A
Pathophysiologic Approach, 4th Ed. Pearson. Chapter 4, pp. 37 – 41.
& Pharmacokinetics. Lilley, L.L., Collins, S.R., & Snyder, J.S. Pharmacology and the Nursing
Process, 8th Ed. Part 1, Chapter 2.
& Routes of Drug Administration. Berman, A., Snyder, S., & Fraudsen, G. (2016). Kozier and Erb’s
Fundamentals of Nursing: Concepts, Process, and Practice. 10th Ed. Pearson Education, Inc.
Chapter 35, pp. 758 – 759.
Pharmacodynamics is the study of the way drugs affect the body. It describes qualitatively the
therapeutic activity of a drug once it is in the bloodstream, and characterizes the interaction of the drug
with its target site, known as the mechanism of action (MOA). The MOA describes both where the
interaction (drug’s target) takes place and how the change (therapeutic response) occurs.
Drug response can cause a primary or secondary physiological effect or both. The primary effect
is desirable, and the secondary effect may be desirable or undesirable. An example of a drug with primary
and secondary effect is diphenhydramine (Benadryl), an antihistamine. The primary effect of
diphenhydramine is to treat the symptoms of allergy, and the secondary effect is a central nervous system
depression that causes drowsiness. The secondary effect is undesirable when the patient drives a car, but
at bedtime it could be desirable because it causes mild sedation.
Drugs can exert their actions in three basic ways: through receptors, enzymes, and nonselective
interactions. Not all mechanisms of action have been identified for all drugs. Thus, a drug may be said to
have an unknown mechanism of action, even though it has observable therapeutic effects in the body.
Receptor Interactions
Many agonists and antagonists lack specific and selective effects. A receptor produces a variety
of physiologic responses, depending on where in the body the receptor is located. Cholinergic receptors
are located in the bladder, heart, blood vessels, stomach, bronchi, and eyes. A drug that stimulates or
blocks cholinergic receptors affects all
anatomic sites of location. Drugs that affect
various sites are non-specific drugs and have
properties of nonspecifity.
Enzyme Interactions
Enzymes are substances that catalyzes nearly every biochemical reaction in a cell. Drugs can
produce effects by interacting with these enzyme systems. For a drug to alter a physiologic response in
this way, it may either inhibit (more common) or enhance (less common) the action of a specific enzyme.
This process is called selective interaction. Drug-enzyme interaction occurs when the drug chemically
binds to an enzyme molecule in such a way that it alters (inhibits or enhances) the enzyme’s interaction
with its normal target molecules in the body.
Critical Concentration
After a drug is administered, its molecules first must be absorbed into the body; then make their
way to the reactive tissue. If a drug is going to work properly on these reactive tissues, and thereby have
a therapeutic effect, it must attain a sufficiently high concentration in the body. The amount of a drug
needed to cause a therapeutic effect is called critical concentration.
Drug evaluation studies determine the critical concentration required to cause a desired
therapeutic effect. The recommended dose of a drug is based on the amount that must be given to
eventually reach the critical concentration. Too much of a drug will produce toxic (poisonous) effects, and
too little will not produce the desired therapeutic effect.
Loading Dose
When immediate drug response is desired, large initial dose, known as the loading dose, of drug
is given to achieve a rapid minimum effective concentration in plasma. Digoxin—a drug used to increase
the strength of heart contractions—is often started with a loading dose (a higher dose than that usually
used for treatment) to reach the critical concentration. The critical concentration then is maintained by
using the recommended dosing schedule.
Dose response is the relationship between the minimal versus the maximal amount of drug dose
needed to produce the desired drug response. The drug dose is usually adjusted to achieve the desired
response. All drugs have a maximum drug effect (maximal efficacy). For example, morphine and tramadol
hydrochloride are prescribed to relieve pain. The maximum efficacy of morphine is greater than tramadol
hydrochloride, regardless of how much tramadol hydrochloride is given. The pain relief with the use of
tramadol hydrochloride is not as great as it is with morphine.
The amount of drug it takes to elicit a maximum therapeutic response of the drug is a measure of
the drug’s potency; a separate and distinctive parameter, easily confused with efficacy.
þ Efficacy is the maximal response produced by a drug and depends on the number of drug-
receptor complexes formed.
þ Potency is a measure of the amount of drug necessary to produce a therapeutic response; the
lower the amount of drug needed, the greater the potency.
One important aspect of pharmacodynamics is knowing the drug’s onset, peak, and duration of
action.
Supplementary Resources
Before drug therapy is initiated, an end point or expected outcome of therapy needs to be
established. This desired therapeutic outcome is patient-specific, established in collaboration with the
patient, and, if appropriate determined with other members of the healthcare team. Outcome goals must
be realistic and prioritized so that drug therapy begins with interventions that are essential to the patient’s
well-being. Examples are:
A contraindication for a
Items to be considered in patient therapy
assessment are: medication is any patient condition,
- Drugs currently used (prescription, over- especially a disease state that makes the
the-counter, herbal, etc.),
- Pregnancy and breastfeeding status,
use of the given medication dangerous to
and the patient.
- Concurrent illness that could
contraindicate a given medication.
The implementation of a treatment
plan can involve several types and
combinations of therapies. The type of
therapy can be categorized as acute,
maintenance, supplemental (or
replacement), palliative, supportive,
prophylactic, or empiric.
Acute Therapy
Acute therapy often involves more intensive drug treatment and is implemented in the
acutely ill (those with rapid onset of illness) or the critically ill. It is often needed to sustain
life or treat disease. Examples are the administration of vasopressors to maintain blood
pressure, the use of volume expanders for a patient who is in shock, and intensive
chemotherapy for a patient with newly diagnosed cancer.
Maintenance Therapy
Maintenance therapy does not eradicate pre-existing problems the patient may have, but
it will prevent progression of a disease or condition. It is used for the treatment of chronic
illnesses such as hypertension. In this case, maintenance therapy maintains the patient’s
blood pressure within given limits, which prevents certain end-organ damage. Another
example is the use of oral contraceptives for birth control.
Supplemental (or replacement) therapy supplies the body with a substance needed to
maintain normal function. This substance may be needed either because it cannot be
made by the body or because it is produced in insufficient quantity. Examples are the
administration of insulin to diabetic patients and of iron to patients with iron-deficiency
anemia.
Palliative Therapy
Supportive Therapy
Supportive therapy maintains the integrity of body functions while the patient is recovering
from illness or trauma. Examples are provision of fluids and electrolytes to prevent
dehydration in a patient who is vomiting and has diarrhea, administration of fluids, volume
expanders, or blood products to a patient who has lost blood during surgery.
Effects of Drugs
þ Therapeutic Effects – also referred to as the desired effect; is the primary effect intended,
that is, the reason the drug is prescribed.
þ Side Effects – or secondary effect, of a drug is one that is unintended. Side effects are usually
predictable and may be either harmless or potentially harmful. Some side effects are
tolerated for the drug’s therapeutic effects.
þ Adverse Effects of Reactions – more severe side effects; may justify the discontinuation of a
drug.
o The nurse should monitor for dose-related side or adverse effects and report these
to the healthcare provider who may discontinue the medication or change the
dosage.
þ Drug Toxicity – harmful effects of a drug on an organism or tissue; it results from overdosage,
ingestion of a drug intended for external use, or buildup of drug in the blood because of
impaired metabolism or excretion (cumulative effect).
þ Drug Allergy – an immunologic reaction to a drug. When a client is first exposed to a foreign
substance (antigen) the body may react by producing antibodies. A client can react to a drug
in the same manner as an antigen and thus develop symptoms of an allergic reaction.
o Allergic reactions can be either mild or severe. A mild reaction has a variety of
symptoms, from skin rashes to diarrhea.
o Can occur anytime from a few minutes to 2 weeks after the administration of the
drug.
þ Anaphylactic Reaction – severe allergic reaction that occurs immediately after the
administration of the drug. This response is fatal if the symptoms are not noticed immediately
and treatment is not obtained promptly.
o The earliest symptoms are subjective feeling of swelling in the mouth and tongue,
acute shortness of breath, acute hypotension, and tachycardia.
þ Potentiating and Inhibiting Effects – the effect of one or both drugs may either be increased
(potentiating) or decreased (inhibiting).
o Potentiating effects may be additive or synergistic. (Refer to key terms for definitions)
þ Iatrogenic Disease – disease caused unintentionally by medical therapy; can be due to drug
therapy.
o Examples: Hepatic toxicity resulting in biliary obstruction, renal damage, and
malformation of the fetus as a result of specific drugs taken during pregnancy.
When administering a drug to a patient, the nurse must be aware that the human factor has a
tremendous influence on what actually happens to a drug when it enters the body. No two people react
in exactly the same way to any given drug. Before administering a drug, the nurse must consider a number
of factors such as:
Weight
þ The recommended dose of a drug is based on drug evaluation studies and is targeted at a
150-lb person.
þ 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.
þ Toxic effects may occur at the recommended dose if the person is very small.
Age
þ Age is a factor primarily in children and older adults.
þ Children metabolize drugs differently than adults do, and they have immature systems for
handling drugs.
þ Older adults undergo many physical changes that are part of the aging process.
Gender
þ Physiological differences between men and women can influence drug’s effect.
þ Men have more vascular muscles than women, so the effects of the drug will be seen sooner
in men than in women when giving IM injections.
þ Women have more fat cells than men do, so drugs that deposit in fact may be slowly
released and cause effects for a prolonged period.
Physiological factors
þ Physiological differences such as diurnal rhythms of the nervous and endocrine systems,
acid-base balance, hydration, and electrolyte balance can affect the way that a drug works
on the body and the way that the body handles the drug.
þ If a drug does not produce the desired effect, one should review the patient’s acid-base and
electrolyte profiles and the timing of the drug.
Pathological factors
þ Other pathological conditions can change the basic pharmacokinetics of a drug.
þ For example: GI disorders can affect the absorption of many oral drugs.
þ Liver and kidney diseases affect the way that a drug is biotransformed and excreted
and can lead to toxic reactions when the usual dose is given.
Immunological factors
þ After exposure to its proteins, a person can develop antibodies to a drug.
þ With future exposure to the same drug, that person may experience a full-blown allergic
reaction.
þ Sensitivity to a drug can range from mild (e.g., dermatological reactions such as a rash) to
more severe (e.g., anaphylaxis, shock, and death).
Psychological factors
þ The patient’s attitude about a drug has been shown to have an effect on how that drug
works.
þ Placebo effect: when a drug is more likely to be effective if the patient thinks it will work
than if the patient believes it will not work.
þ The patient’s personality also influences compliance with drug regimen.
þ The nurse is in a position to influence the patient’s attitude about drug effectiveness as
nurses are most often involved in drug administration.
Environmental factors
þ Some drugs are enhanced by a quiet, cool, non-stimulating environment.
þ For example: 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.
þ Other drug effects may be influenced by temperature.
þ For example, antihypertensives that work well during cold, winter months may become
too effective in warmer environments, when natural vasodilation may lead to a release of
heat that tends to lower the blood pressure.
Drug tolerance
þ Tolerance may arise because of increased biotransformation of the drug, increased
resistance to its effects, or other pharmacokinetic factors.
þ The drug no longer causes the same reaction. Therefore, increasingly larger doses are
needed to achieve a therapeutic effect.
þ Example: morphine, an opiate used for pain relief. The longer morphine is taken, the more
tolerant the body becomes to the drug, so that larger and larger doses are needed to
relieve pain.
Interactions
þ Usually this is an increase or decrease in the desired therapeutic effect of one or all of
the drugs or an increase in adverse effects.
þ Drug – Drug Interactions. When two or more drugs or substances are taken together,
there is a possibility that an interaction can occur, causing unanticipated effects in the
body.
þ Drug – Alternative Interactions. Alternative therapies, such as herbal products, act as
drugs in the body and can cause these same interactions.
þ Drug – Food Interactions. Certain foods can also interact with drugs. Food is known to
increase, decrease, or delay drug absorption; can bind with drug, causing less or slower
drug absorption.
Other drug-related effects that must be considered during drug therapy are teratogenic,
mutagenic, and carcinogenic effects. These can result in devastating patient outcomes and may be
prevented in many instances by appropriate monitoring.
þ Teratogenic Effects of drugs or other chemicals result in structural defects in the fetus.
Compounds that produce such effects are called teratogens.
þ Mutagenic Effects are permanent changes in genetic composition of living organisms and
consist of alterations in chromosome structure, the number of chromosomes, or the genetic
code of the DNA molecule. Drugs that are capable of inducing mutations are called mutagens.
o Radiation, viruses, chemicals (e.g., industrial chemicals such as benzene)
þ Carcinogenic Effects are the cancer-causing effects of drugs, other chemicals, radiation, and
viruses. Agents that produce such effects are called carcinogens.
Toxicology
The study of poisons and unwanted responses to both drugs and other chemicals is
known as toxicology. Clinical toxicology deals specifically with the care of the poisoned
patient. Poisoning can result from a variety of causes, ranging from drug overdose to
ingestion of household cleaning agents to snakebite. Poison control centers are
healthcare institutions equipped with sufficient personnel and information resources to
recommend appropriate treatment for the poisoned patient.
Effective treatment of the poisoned patient is based on a system of priorities, the first of which
is to preserve the patient’s vital functions by maintaining airway, ventilation, and circulation. The second
priority is to prevent absorption of the toxic substance and/or speed its elimination from the body using
one or more of the varieties of clinical methods available.
& Toxicology. Smith, B.T. & Pacitti, D.F. (2020). Pharmacology for Nurses. 2nd Ed. Jones and
Barlett Learning, LLC. Chapter 2, pp. 24 – 25.
Resources
Adams, M., Holland, N., & Urban, C. (2014). Pharmacology for Nurses: A Pathophysiologic
Approach, 4th Ed. Pearson.
Berman, A., Snyder, S., & Fraudsen, G. (2016). Kozier and Erb’s Fundamentals of Nursing:
Concepts, Process, and Practice. 10th Ed. Pearson Education, Inc.
Hayes, F.R., Kee, J.L., & McCuistion, L.E. (2015). Pharmacology: A Patient-Centered Nursing
Process Approach, 8th ed. Saunders, USA.
Karch, A. (2013). Focus on Nursing Pharmacology, 6th ed. Lippincott Williams and Wilkins, USA.
Lilley, L.L., Collins, S.R., & Snyder, J.S. Pharmacology and the Nursing Process, 8th Ed.
Pharmacodynamics.
https://info.xanedu.com/hubfs/OpenRN_Nursing_Pharmacology_ISBN_9781734914115
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Smith, B.T. & Pacitti, D.F. (2020). Pharmacology for Nurses. 2nd Ed. Jones and Barlett Learning, LLC.
Zerwekh, J. & Miller, C.J. (2019). Mosby’s Pharmacology Memory NoteCards: Visual, Mnemonic,
and Memory Aids for Nurses, 5th Ed. Elservier, Inc. ISBN: 978-0-323-54951-6