CR Pharma Mod. 1-2
CR Pharma Mod. 1-2
CR Pharma Mod. 1-2
Respiratory Therapy
Department
CR Pharmacology
MODULE I
Fundamental Concept of
Pharmacology
OVERVIEW
The purpose of this module is to provide an understanding of the basics of
pharmacology including pharmaceutics, pharmacokinetics, and pharmacodynamics.
Drug reactions in relation to side and adverse effects; hypersensitivity reactions;
drug tolerance, cumulative effects and drug toxicity; drug interactions; precautions
and contraindications, are also addressed to provide the RT with a comprehensive
understanding of the knowledge needed for safe medication administration.
Background
Special populations have also been targeted as high risk in relation to certain
medications and or how medications are administered. One special population is
the pregnant woman due to the potential for maternal or fetal adverse drug
reactions. Some drugs can be teratogenic and cause birth defects if given in the
first trimester. Historically these have been rated according to categories, but a new
system is being developed that allows for more specificity based on research that
supports evidence-based prescribing.
DEFINITION OF TERMS:
Pharmacology is the study of drugs and their effect on the human body.
Drugs can have a positive effect on the body which is called the therapeutic
effect, they can have non-therapeutic effects on the body called side effects,
or they can have negative effects on the body which are called adverse
effects.
When administering drugs one must also watch for contraindications that
would make a drug dangerous to give to a patient, precautions that should be
taken when administering a drug, and interactions, either drug-drug or drug-
food, that can increase or decrease the efficacy of the drug.
Drugs are also called medications when given for therapeutic purposes.
When administering a drug to a patient the term medication is more
commonly used because it is being given to elicit a specific therapeutic
response or to treat a health alteration.
Drugs are also known by two different names: their brand name and their
generic name. A drug’s brand name is a term referring to the advertised
brand name under which the drug is sold and a drug’s generic name is a
term referring to the chemical makeup of a drug rather than the advertised
brand name under which the drug is sold. An example of a drug’s generic
and brand name is PARACETAMOL whose brand name is BIOGESIC. Patient’s
may be more familiar with their medication’s brand names but health care
providers should use the generic form to prevent confusion because brand
names can vary widely.
Some drugs given for pain have addictive properties and can be abused by
patients. Of major concern is the improper use of opioid drugs by patients
that has led to an opioid crisis in our society. Approximately 20% of people
who require pain relief for acute pain such as post-operative pain or have
chronic pain related to a health issue such as low back pain are prescribed
opioids.
Opioids are narcotics and as such have addictive properties. These drugs
are safe if taken over a short period of time however, if taken for extended
periods of time or in higher than prescribed amounts a patient becomes at
risk for developing an addiction. It is critical that nurses give these
medications as prescribed and educate patients on their proper use and
alternative non- opioid drugs that can be taken when pain is subsiding.
A. PHARMACEUTICS
The table below illustrates the absorption rate of various forms of oral medication
based on their form.
Drugs can be given in three dosage forms: enterally, parentally, and topically.
Enteral forms are given via the intestinal tract either orally, sublingually
(under the tongue), buccally (between the gums and cheek), or rectally.
Drugs that require quick absorption may be given sublingually or buccally
because the rich supply of blood vessels in the mouth and the ease of
transport through the mucous membranes supports immediate absorption by
the body.
Parenteral forms are given outside the gastrointestinal tract. They are given
intradermally, intramuscularly, subcutaneously, or intravenously. These forms
allow for immediate absorption by the body bypassing the gastrointestinal
track and the need for dissolution.
Topical forms are given via aerosol, cream, foam, gel, suppository, and
through patches. These drugs may act directly on the skin or may be
absorbed through the skin for a systemic response.
SR Slow release
SA Sustained action
CR Controlled releases
XL Extended release
XT Extended time
B. PHARMACOKINETICS
Pharmacokinetics refers to how drugs travel through the body where they
undergo a variety of biochemical processes that result in absorption,
distribution, metabolism, and excretion.
Oral drugs must pass through a layer of epithelial cells that line the
gastrointestinal tract. The absorption pattern of drugs taken orally varies
due to solubility and stability of the medication, the pH of the
gastrointestinal tract and its motility, the presence of food in the stomach
or intestines, drugs given at the same time, and the form of the medication
in regard to whether a medication is a liquid, capsule, tablet, enteric-
coated, or time-released.
Sublingual and buccal drugs which are placed under the tongue
(sublingual) or between the gums and the cheek (buccal) are absorbed before
swallowing. This prevents the gastric pH from inactivating the medication. It
also enhances the rate of absorption due to its passage through highly
vascular membranes.
Rectal and vaginal drugs are easily absorbed and can precipitate both local
and systemic effects. However, the presence of stool in the rectum or
infectious discharge in the vagina limits tissue contact with the medication.
Inhalation of medication through the mouth or nose is rapidly absorbed
through capillary networks in either the nose or alveoli in the lungs.
Intradermal and topical drugs allow slow, gradual absorption of medication.
The effects of this type of medication is usually local but systemic effects can
occur as well.
Subcutaneous and intramuscular drugs may be absorbed quickly or slowly.
Water-soluble drugs are absorbed rapidly while non water-soluble drugs
have a slower absorption rate. In general, drugs given intramuscularly are
absorbed quickly due to the vascularity of muscles however, patients with
poor peripheral perfusion may experience delayed absorption.
Intravenous drugs are absorbed the most quickly and completely of any of
the other routes. Intravenous medication given directly into the
bloodstream reaches tissues in its original chemical form.
2. Distribution is the transportation of drugs to sites of action by bodily fluids.
The organs that are exposed to the drug first are the heart, liver, kidneys, and
brain due to their vascularity and extensive supply of blood. Many drugs may
be hepatotoxic (can cause liver injury) or nephrotoxic (can cause kidney
injury) because drugs pass through these organs in a higher concentration
increasing their potential to cause damage to these organs. There are
various factors that influence the distribution of drugs.
a. Age is a factor that can affect the metabolism of a drug. Infants have a
limited “medication – metabolizing capacity”. Metabolism by the liver also
tends to decline with age requiring a decrease in dose when older adults
are given drugs to avoid inadvertently causing toxicity.
c. First pass effect results from the liver inactivating a certain amount of a
drug after it leaves the gastrointestinal tract and passes through the liver
for the first time. Drugs that are inactivated by the liver need to be given
by a route that does not pass the gastrointestinal tract.
d. Similar metabolic pathways can alter the metabolism of two drugs given at
the same time. The rate of metabolism can decrease for one or both
drugs leading to toxicity.
HALF LIFE
The half-life of a drug is the time it takes after a drug enters the body to
decrease in amount by half.
This decrease reflects how quickly and efficiently a drug is metabolized and
then excreted.
Drugs are excreted from the body when approximately five half-lives have
occurred.
Drugs with a short half-life may need to administer several times a day as
compared to drugs with a long half-life which may only need to be
administered once a day.
o Since most drugs are metabolized in the liver and are excreted by the
kidneys; a decrease in functioning in either of these organs increases the
half-life of a drug.
o Subsequently, patients with liver or kidney dysfunction may experience
toxic effects of drugs much more easily if the dosage or frequency of
administration is not decreased.
o The nurse should also monitor labs that reflect liver function including alanine
transaminase (ALT), aspartate transaminase, (AST), alkaline phosphatase
(ALP) and kidney function including blood urea nitrogen (BUN) and creatinine.
The provider should be notified should an increase in any of the values occur.
ONSET, PEAK, TROUGH, AND DURATION
Onset of action is the time it takes for a drug to exert its therapeutic effect.
Onset of action is influenced by the route of administration and patency of
patient’s gastrointestinal tract and circulatory system.
Peak level of a drug is the point in time when a drug is at its highest level in
the body.
Duration of action is the length of time a drug is in the blood in sufficient
amounts to elicit a response. Duration of action is influenced by the rate of
excretion from the body.
Trough level of a drug is the point in time when a drug is at its lowest, non-
therapeutic level in the body.
When a drug meets a cell, it can modify its function by either enhancing
or blocking the way in which the cell functions.
The joining or binding of a drug with a cell is called the drug – receptor
interaction. Drugs bind with receptors on a cell through the formation of
chemical bonds between the receptor and the active site on the drug
molecule.
Drugs given to enhance a physiologic response are called agonists.
Agonists are drugs that bind with a receptor and enhance the typical
response. Morphine is an example of an agonist because it binds with
receptors that produce the desirable effect of analgesia.
Antagonists are drugs that bind with receptors and either block or lessen the
typical response. An example is a histamine-2 (H2) blocker such as ranitidine
which blocks the histamine induced gastric acid secretion from the parietal
cell of the gastric mucosa.
C.4DRUG INTERACTIONS
Drug-drug and drug-food interactions can dramatically change the action of a
drug in the body.
Precautions should be taken to limit or restrict certain types of food or
concurrent administration of certain types of drugs rather than restricting the
drug itself.
1. Drug-drug interactions occur when one drug changes the way another drug
affects the body. When the combined effect of two drugs you give together is the
same as each drug you give alone in similar doses an additive effect occurs. An
example would be a patient who ingests two drugs that are central nervous
system depressants, such as alcohol and opioids. Their effects add to each other
putting the patient at risk for significant and possibly fatal central nervous system
depression.
Synergistic effects occur when the effect of one drug is greater if you give it
with another drug. An example would be giving aspirin to a patient who is
taking a blood thinner such as warfarin which would increase the patients risk
of bleeding and hemorrhage.
Antagonistic effects occur when the effect of one drug is decreased or
blocked if you give it with another drug. An example would be giving
ciprofloxacin with an antacid which reduces the absorption of ciprofloxacin
decreasing its efficacy to treat infection.
2. Drug-food interactions occur when a drug is given with a food that can
radically change the action of the drug by reducing absorption or
increasing risk for toxicity. An example would be eating fruit or drinking
fruit juice an hour or two before or after taking fexofenadine. The juice can
inhibit the absorption of fexofenadine decreasing or inhibiting its ability to
block the release of allergy-related histamine.
C.5THERAPEUTIC, SIDE, AND ADVERSE DRUG EFFECTS
Side effects are the unintended effects of a drug that commonly occur in
patients and are mild in nature. Side effects occur as a result of a drug's
effects on the body. For example, side effects of diphenhydramine include
dry mouth and drowsiness. Nurses often help patients cope with common
and often uncomfortable side effects of prescribed drugs. A nurse caring for
a patient who is receiving diphenhydramine and reports having a dry mouth
should ensure water or ice chips are available, offer sugar-free hard candy,
and use a saliva substitute as needed. These patients should also be
instructed to avoid driving a car or using heavy machinery when experiencing
drowsiness.
Adverse effects are the unintended and unexpected effects of a drug that
are more severe and can even be life-threatening at a therapeutic dose.
Adverse effects are also side effects of a drug but are more severe in nature.
For example, adverse effects of diphenhydramine in some older adults
include confusion, incoordination, and dizziness. Another example is the risk
of serotonin syndrome when taking sertraline, a drug prescribed for major
depressive disorder, obsessive compulsive disorder, panic disorder,
posttraumatic stress disorder, social anxiety disorder, and premenstrual
dysphoric disorder. Serotonin syndrome results from concurrent
administration of a selective serotonin reuptake inhibitor (SSRI) or a
monoamine oxidase (MAO) inhibitor or any other drug that potentiates
serotonin neurotransmission. Serotonin syndrome is characterized by
hypertensive crisis, hyperpyrexia, muscle rigidity, seizure, and extreme
agitation that can progress to delirium and coma. Nurses must recognize
when a patient is receiving a drug that has life-threatening side effects and
monitor the patient very closely for the first sign of these adverse effects.
C.6HYPERSENSITIVITY REACTIONS
Hypersensitivity reactions occur secondary to administration of a drug that a
patient’s body sees as a foreign substance.
An allergy to a drug usually occurs after more than one dose of a drug has
been given. It occurs secondary to the release of histamine which can cause
generalized inflammation and swelling of tissues (hives), increased mucous
production, and in severe cases constriction of the bronchioles. Mild to
moderate cases of hypersensitivity reactions can be treated with an
antihistamine such as diphenhydramine.
It is very important for nurses to ask patients if they have any allergies to
drugs. Even minor reactions to a drug are notable.
If a patient admits to having an allergy to a drug, ask them what type of
reaction they had then note this information on the chart.
The patient’s wristband should list all known allergies and be placed on a
patient immediately after admission.
When administering medication be sure to check both the chart and patient’s
wrist band for allergies. When checking new orders review the patient’s chart
for allergies and bring to the provider’s attention any drug that could
precipitate a reaction.
Some drugs can display a cross-sensitivity to another drugs. Patients who
report an allergy to penicillin may have a cross-sensitivity to cephalosporin
drugs.
If the patient has not received a cephalosporin on a prior occasion monitor
the patient very closely during the first few doses for signs of an allergic
reaction.
C.7DRUG TOLERANCE, CUMULATIVE EFFECTS, AND DRUG TOXICITY
Drug tolerance, cumulative effects, and drug toxicity are other undesirable
effects related to safe medication administration that the nurse must monitor
for when caring for a patient receiving drug therapy.
3. Drug toxicity occurs when a drug is given in amounts greater than what the
body can excrete. Drug toxicity may occur when a patient receives drugs in
greater than recommended dosages. It can also occur when impaired
excretion of the drug, secondary to impaired liver or kidney function, allows it
to build up in the body over a period. Eventually a toxic level is reached
causing the patient to experience severe and possibly fatal adverse effects.
Drugs that have a small margin of safety can quickly build up to a toxic level
in the body. Patients on drugs with a small margin of need to have their
serum drug level regularly drawn and be closely monitored for signs and
symptoms of toxicity. The effects of drug toxicity may be irreversible and life-
threatening. For example, vancomycin, given in toxic amounts may cause
permanent damage to cranial
nerve VIII resulting in decreased hearing or deafness. Acetaminophen given in
amounts great than 4,000 milligrams per day may cause temporary damage to
the liver or permanent damage that results in liver failure. Nurses must make
certain when giving a patient acetaminophen that a review of all the drugs has
been done to determine if the patient is receiving additional acetaminophen in
any other drugs. Many drugs for pain are combination drugs that contain an
opioid and acetaminophen. Vicodin is an example of a combination drug which
contains 5 milligrams of hydrocodone and 300 milligrams of acetaminophen.
IMPLICATIONS
Respiratory Therapist must be knowledgeable of all drugs they are
administering to their patients. It is important to understand the
pharmacokinetics and pharmacodynamics of a drug to safely administer the
drug while monitoring for side and adverse effects, signs of an allergic
response, and toxicity.
Patient characteristics such as age, health alterations, and impairment of
liver or kidney function, must also be considered regarding increased risk for
side and adverse effects.
The process of monitoring peak and trough level of drugs that are critical to
be maintained at a therapeutic level is also very important knowledge for RT
caring for patients.
All drugs that are prescribed by a provider should be reviewed in relation to
other drugs that are being given to prevent drug – drug interactions. If a
potential interaction is discovered or two similar drugs are prescribed
increasing the risk for toxicity the provider should be notified and concerns
brought to that individual’s attention so a substitution can be made, or a drug
discontinued.
Foods that could precipitate a drug – food interaction must also be restricted
from a patient’s diet and patient education provided if the medication would
continue to be taken outside of the acute care setting.
In summary, RTs are responsible for a deep understanding of the drugs they are
giving to administer drugs in a safe and evidence-based manner.
KEYPOINTS
SUMMARY
REFERENCES: