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NSG 105 PHARMACOLOGY

Module 3: Drug Action


1st Semester, A.Y. 2020 – 2021

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:

Module 1: Drug Definitions and Classifications

þ Definition of Pharmacology
þ Definition of Key Terms
þ Classes of Drugs
þ Drug Names

Module 2: Drug Standard and Drug Information

þ Drug Information
þ Phases of Drug Evaluation
þ Drug Legislations and Standards
þ Cultural and Ethical Considerations in Pharmacology

Module 3: Drug Action

þ Pharmaceutics
þ Pharmacokinetics
þ Pharmacodynamics
þ Pharmacotherapeutics
þ Factors Influencing Responses to Drugs

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 2


Janeirah Q. Manalundong
Faculty, College of Health Sciences
UNIT I: FUNDAMENTAL CONCEPTS OF PHARMACOLOGY
Module III: Drug Action

Introduction

Greetings dear learners!

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

þ Discuss what is drug action in terms of pharmaceutics, pharmacokinetics, and


pharmacodynamics.
þ Differentiate the three phases of drug action.
þ Discuss the two processes that occur before tablets are absorbed into the body.
þ Describe the four phases of pharmacokinetics.
þ Explain the meaning of pharmacodynamics in drug action.
þ Describe the determinants that affect drug therapy.
þ Discuss the nursing implications of the different phases of drug action.

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?

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 3


Janeirah Q. Manalundong
Faculty, College of Health Sciences
ü How much of the drug is needed to affect an observable change in the patient’s
symptoms?
ü What dose of drug is “too much”, and what happens if too much drug is given?
ü How often does the medication need to be given to the patient, and how long should
the therapy regimen continue?
ü Which patient parameters should be monitored while the patient is taking this
medication?
ü How does the body eliminate the drug?
ü How long will it take for the drug to be completely removed from the body?

To safely administer medications, a nurse must know the answers to a range of potential questions
about his or her patient’s medication therapy.

Basic Areas of Pharmacology

A tablet or capsule taken by mouth goes through three phases—pharmaceutics,


pharmacokinetics, and pharmacodynamics—as drug actions occur. In pharmaceutic phase, the drug
becomes a solution so that it can cross the biologic membrane. The second phase, the pharmacokinetic
phase, is composed of four processes: absorption, distribution, metabolism (or biotransformation), and
excretion (or elimination). In the pharmacodynamic phase,
a biologic or physiologic response results.

The aforementioned areas of pharmacology


describe the relationship between the dose of a drug and
the activity of that drug in treating the disorder.
Pharmaceutics is the study of how various dosage forms
influence the way in which the drug affects the body.
Pharmacokinetics is the study of what the body does to the
drug. Lastly, pharmacodynamics is the study of what the
drug does to the body. It involves drug-receptor
relationships.

Pharmacotherapeutics (also called therapeutics)


focuses on the clinical use of drugs to prevent and treat
diseases. It defines the principles of drug action. Some drug
mechanisms of action are more clearly understood than
others. The study of natural (versus synthetic) drug sources
(i.e., plants, animals, minerals) is called pharmacognosy.
Pharmacoeconomics focuses on the economic aspects of
drug therapy.

In summary, pharmacology is a very dynamic science that incorporates different disciplines,


including chemistry, physiology, and biology.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 4


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Pharmaceutics

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.

Different dosage forms have different pharmaceutical


properties. Dosage form determines the rate at which
dissolution (dissolving of solid dosage forms and their Figure 2-1. The two pharmaceutic phases
absorption, e.g., from GI tract) occurs. Oral drugs that are liquids
(e.g. elixirs, syrups) are already dissolved and are usually absorbed more quickly than solid dosage forms.

Enteric-coated drugs, on the other hand, have a


coating that prevents them from being broken down in
the acidic pH environment of the stomach and are not
absorbed until they reach the higher (more alkaline) pH of
intestines. This results in slower dissolution and therefore
slower absorption. Enteric-coated tablets or capsules and
sustained-release (beaded) capsules should NOT be
crushed. This would cause disruption of the coating designed to protect the stomach lining from the local
effects of the drug and/or protect the drug from being prematurely disrupted by stomach acid.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 5


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Supplementary Resources

: Enteric coating: An Overview https://www.pharmapproach.com/enteric-coating-2/

& 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.

Pharmacokinetics: “What the body does to the drug?”


The nurse applies
Pharmacokinetics is the process of drug knowledge of
movement to achieve drug action. It is the study of what pharmacokinetics when
assessing the patient for
happens to a drug from the time it is put into the body
possible adverse drug
until the parent drug and all metabolites have left the effects.
body. The four processes are absorption, distribution,
metabolism (or biotransformation), and excretion (or The nurse communicates
assessment findings to
elimination), often referred to by the acronym ADME. members of health care
þ Absorption: The process of drug team in a timely manner to
movement, from site of administration, promote safe and effective
drug therapy for the
into the systemic circulation. patient.
þ Distribution: The process of drug
movement, from the systemic circulation,
to the site of drug action.
þ Metabolism: Chemical alteration(s) to the structure of the drug molecule.
þ Excretion (or elimination): Process(es) of irreversible drug removal from the body.

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 6


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Bioavailability is the term used to express the extent of drug Many drugs administered
absorption. A drug that is absorbed from the intestine must first pass through by mouth have a
the liver before it reaches the systemic circulation. If a large proportion of a drug bioavailability of <100%.

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

As drugs are distributed in the plasma, many are bound to varying


degrees (percentages) with protein (primarily albumin). The portion of the
drug that is bound is inactive because it is not available to receptors, and
the portion that remains unbound is free, active drug. Only free drugs
(drugs not bound to protein) are active and can cause a pharmacologic
response. Drugs bound to proteins cannot leave the systemic circulation
to get to the site of action. This is why only free drug is active.

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

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 7


Janeirah Q. Manalundong
Faculty, College of Health Sciences
The blood-brain barrier (BBB) is a semipermeable membrane in
the CNS that protects the brain from foreign substances. Highly
lipid-soluble drugs are able to cross the BBB. Drugs that are not
bound to proteins and are not lipid-soluble are not able to cross
the BBB, which makes it difficult to distribute the drug.

During pregnancy, both lipid-soluble and lipid-insoluble drugs are


able to cross the placental barrier, which can affect the fetus and
Drug movement across blood-brain barrier.

the mother. The risk-benefit ratio should be considered before


drugs are given during pregnancy. During lactation, drugs can be secreted into the breastmilk, which could
affect the nursing infant. The nurse needs to check which drugs may cross into breastmilk before
administering to a lactating patient.

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).

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 8


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Excretion (or Elimination)

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.

: Watch Pharmacology – Pharmacokinetics (Made Easy) at


https://www.youtube.com/watch?v=NKV5iaUVBUI

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 9


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Pharmacodynamics: “What the drug does to the body?”

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

A receptor can be defined as the reactive site on


the surface or inside a cell. If the mechanism of action of a
drug involves a receptor interaction, then the molecular
structure of the drug is critical. Drug-receptor interaction is
the joining of the drug molecule with a reactive site on the
surface of a cell or tissue. Most commonly, this site is a
protein structure within the cell membrane. Once a drug
binds to and interacts with the receptor, a pharmacologic
response is produced. The degree to which a drug attaches
to and binds with a receptor is called its affinity. The drug
with the best “fit” and strongest affinity for the receptor will elicit the greatest response.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 10


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Nonspecific and Nonselective 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.

Drugs may act on different receptors.


Drugs that affect various receptors are
nonselective drugs or have properties of
nonselectivity. Chlorpromazine (Thorazine)
acts on the norepinephrine, dopamine,
acetylcholines, and histamine receptors, and a variety of responses result from action of these receptor
sites. Drugs that produce a response but do not act on a receptor may act by stimulating or inhibiting
enzyme activity or hormone production.

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 11


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Dose Response and Maximal Efficacy

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.

Potency vs. Efficacy

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.

Therapeutic Index and Therapeutic Range


(Therapeutic Window)

The safety of drugs is a major concern. The


therapeutic index estimates the margin of safety of a
drug through the use of a ratio that measures the
effective (therapeutic) dose in 50% of people and the
lethal dose in 50% of people. The closer the ratio is to 1,
the greater the danger of toxicity.

Drugs with a low therapeutic index have a


narrow margin of safety. Drug dosage might need
adjustment, and plasma (serum) drug levels need to be
monitored because of small safety between effective
dose and lethal dose.

The therapeutic range (therapeutic window) of


a drug concentration in plasma is the level of drug
between the minimum effective concentration in the
plasma for obtaining desired drug action and the
minimum toxic concentration (toxic effect). When the
therapeutic range is given, it includes both protein-
bound and unbound portions of the drug. If the therapeutic range is narrow, such as for digoxin (0.5 to 1
ng/mL), the plasma drug level should be monitored periodically to avoid drug toxicity.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 12


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Onset, Peak, and Duration of Action

One important aspect of pharmacodynamics is knowing the drug’s onset, peak, and duration of
action.

Onset of Action Peak of Action Duration of Action

•The time it takes •Occurs when the •The length of


to reach the drug reaches its time the drug has
minimum highest blood or a pharmacologic
effective plasma effect.
concentration concentration.
after a drug is
administered.

Peak and Trough Drug Levels

Peak and trough levels are requested for


drugs that have a narrow therapeutic index and are
considered toxic, such as aminoglycosides
antibiotics. If either the peak and trough level is too
high, toxicity can occur. If the peak is too low, no
therapeutic effect is achieved.

Peak drug level is the highest plasma


concentration of drug at a specific time. Peak drug
levels indicate the rate of absorption. If a peak drug
level is ordered, a blood sample should be drawn at
the proposed peak time, according to the route of
administration.

The trough drug level is the lowest plasma


concentration of a drug, and it measures the rate at
which the drug is eliminated. Trough levels are
drawn immediately before the next dose of drug is
given, regardless of route of administration.

Supplementary Resources

: Pharmacodynamics, Chapter 1, pp. 20 – 21.


https://info.xanedu.com/hubfs/OpenRN_Nursing_Pharmacology_ISBN_9781734914115
_order_print_copies_from_XanEdu_call_toll_free_888_212_3121.pdf

: Watch Pharmacology – Pharmacodynamics (Made Easy) at https://youtu.be/tobx537kFaI

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 13


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Pharmacotherapeutics

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:

þ Curing a disease, These goals and


þ Eliminating or reducing preexisting symptom, outcomes are
þ Arresting or slowing a disease process, NOT the same as
nursing goals and
þ Preventing disease or unwanted condition, or
outcomes.
þ Otherwise improving quality of life.

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 14


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Supplemental Therapy

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

The goal of palliative therapy is to make the patient as comfortable as possible.


Palliative therapy focuses on providing patients with relief from the symptoms, pain,
and stress of a serious illness. The goal is to improve quality of life for both the patient
and the family. It is typically used in the end stages of an illness when attempts at
curative therapy have failed; however, it can be provided along with curative treatment.
An example is the use of high-dose opioid analgesics to relieve pain in the final stage of cancer.

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.

Prophylactic Therapy and Empiric Therapy

Prophylactic therapy is drug therapy provided to prevent illness or other undesirable


outcome during planned events. A common example is the use of preoperative antibiotic
therapy for surgical procedures. The antibiotic is given before incision is made, so that
the antibiotic can kill any potential pathogens. Another example is the administration of
disease-specific vaccines to individuals traveling to geographic areas where a given
disease is known to be endemic.

Empiric therapy is based on clinical probabilities. It involves drug administration when a


certain pathologic condition has a high likelihood of occurrence based on the patient’s initial
presenting symptoms. A common example is use of antibiotics against the organism most
commonly associated with a specific infection before the results of the culture and sensitivity
reports are available.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 15


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Factors Influencing Responses to Drugs

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 16


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Factors Influencing Drug Effects

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 17


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Genetic factors
þ Some people lack certain enzymes necessary for metabolizing a drug, whereas others have
overreactive enzyme systems that cause drugs to be broken down more quickly.
þ Predictable differences in the pharmacokinetics and pharmacodynamic effects of drugs can
be anticipated with people of particular culture backgrounds because of their genetic
makeup.
þ Pharmacogenomics is a new area of study that explores the unique differences in response
to drugs that each individual possesses based on genetic makeup.

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 18


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Cumulation effects
þ If a drug is taken in successive doses at intervals that are shorter than recommended, or
if the body is unable to eliminate a drug properly, the drug can accumulate in the body,
leading to toxic levels and adverse effects.
þ This can be avoided by following the drug regimen precisely.
þ If a drug is causing serious adverse effects, review the drug regimen with the patient to
find out how the drug is being taken, and then educate the patient appropriately.

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.

þ Drug – Laboratory Interactions. Abnormal plasma or serum electrolyte concentrations


can affect certain drug therapies.

þ Drug – Induced Photosensitivity. It is a skin reaction caused by exposure to sunlight. It


is caused by the interaction of a drug and exposure to ultraviolet A (UVA) light, which
can cause cellular damage.
o Photoallergy occurs when a drug undergoes activation in the skin by UV light to
a compound more allergenic than the parent compound.
o Phototoxicity occurs when a photosensitive drug undergoes photochemical
reactions within the skin to cause damage. This type of reaction is different from
photoallergy in that it is not immune-mediated.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 19


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Other Drug Effects

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.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 20


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Supplementary Resource

& Toxicology. Smith, B.T. & Pacitti, D.F. (2020). Pharmacology for Nurses. 2nd Ed. Jones and
Barlett Learning, LLC. Chapter 2, pp. 24 – 25.

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 21


Janeirah Q. Manalundong
Faculty, College of Health Sciences
Learning Checkpoint

Proceed to our Google classroom for our learning activity.

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
_order_print_copies_from_XanEdu_call_toll_free_888_212_3121.pdf

Smith, B.T. & Pacitti, D.F. (2020). Pharmacology for Nurses. 2nd Ed. Jones and Barlett Learning, LLC.

Pharmacology – Pharmacodynamics (Made Easy) at https://youtu.be/tobx537kFaI

Pharmacology – Pharmacokinetics (Made Easy) at


https://www.youtube.com/watch?v=NKV5iaUVBUI

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

NSG 105 PHARMACOLOGY COURSE GUIDE DRUG ACTION 22


Janeirah Q. Manalundong
Faculty, College of Health Sciences

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