PHARMACOLOGY Aspirin is an analgesic, antipyretic, anti-

Purpose inflammatory, and anti-platelet

The purpose of studying PHARMACOLOGY is to MEDICATION FORMS
help you learn about medicines and the why, what, Medications are available in a variety of forms and
how, when, and where they are used in daily life. preparations
The form of the med will determine its route of
NURSING PHARMACOLOGY administration
Pharmacology Composition of med is designed to enhance its
pharmacon - meaning drug absorption & metabolism
logos - meaning science Medication Forms
is the study of drugs (chemicals) that alter Tablet
functions of living organisms? Capsule
Drug therapy Caplet
also called pharmacotherapy, is the use of Elixir
drugs to prevent, diagnose, or treat signs, Enteric-coated
symptoms, and disease processes. Suppository
Medication Suspension
Drugs given for therapeutic purposes. Transdermal patch
Nursing pharmacology Drops
Pharmacoeconomics Injections
involves the costs of drug therapy, Ointment
including those of purchasing, dispensing, Tincture
storage, administration, laboratory and Liniment
other tests used to monitor client Aerosol
responses, and losses from expiration. Subcutaneous Injection
Drug Intramuscular or IM
Any chemical that affects the physiologic Ointment
processes of a living organism Patch
NOMENCLATURE/Drugs Eye Drops or Eye Ointment
Chemical name Ear Drops
• Describes the drug’s chemical composition and Suppositories
molecular structure
Generic name (non-proprietary name) PHARMACOLOGIC PRINCIPLES
• Name given by the country or Adopted Phases
Name Council Pharmacotherapeutic
Trade name (proprietary name) Pharmacokinetics
• The drug has a registered trademark; use of the Pharmacodynamics
name restricted by the drug’s patent owner Pharmacognosy
(usually the manufacturer) Pharmaceutics'
Drugs
Chemical name
• (+/-)-2-(p-isobutylphenyl) propionic acid
Generic name
• Ibuprofen
Trade name
• Alaxan®, Advil®

CLASSIFICATION
Classification:
Functional Class vs. Chemical Class
Medication classification indicates:
effect of the medicine
symptom the medicine relieves
medicine desired effect (e.g. oral
hypoglycemics) Pharmaceutics
The study of how various drug forms
Classification influence pharmacokinetic and
A medication may also be part of more than one pharmacodynamics activities
class

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Figure 2-1 The chemical, generic, and trade names for the common analgesic
ibuprofen are listed next to the chemical structure of the drug.
DRUG TRANSPORT
What does this have to do with drug
administration? Oral
Drugs must reach and interact with or cross the • Pills, capsules, tablets, liquids
cell membrane to stimulate or inhibit cellular • SL, Buccal, NGT, Gastrostomy, Duodenostomy
function tubes
NOTE:
Pharmacokinetics Assess client’s ability to take oral medications
The study of what the body does to the drug,
process of drug movement throughout the body ORAL DRUGS
that is necessay to achieve drug action. Dosage is determined by how much of the drug is
– Absorption required to be taken by mouth to given the
– Distribution desired affect.
– Metabolism Time in the stomach – is the stomach empty –
– Excretion full – does it make a difference on how drug is
Remember:” ADME” absorbed
Small intestine – large surface area for
Pharmacokinetics: absorption of nutrients and minerals
ABSORPTION
The rate at which a drug leaves its site of WHAT ELSE MIGHT INFLUENCE ORAL DRUG
administration, and the extent to which ABSORPTION?
absorption occurs. movement of a drug into the • Food in stomach
bloodstream after administration. • Certain juices – grapefruit juice
Bioavailability- proportion of a drugs which • Milk – binds with molecules of some drugs so
enters the circulation when introduced into the that the drug is never absorbed
body and so is able to have an active effect • Orange juice – enhances absorption of iron
Bioequivalent- means that the active ingredients taken orally
of 2 drugs has the same rate and extent of • The coating on the tablet: chewable, enteric
absorption coated (breakdown occurs in small intestine),
slow release capsules
Factors That Affect Absorption Intradermal Sites
• Administration route of the drug • Ventral forearm
• Ability of Medicine to Dissolve • Upper chest
• Food or fluids administered with the drug • Shoulder
• Body Surface Area Subcutaneous Sites
• Status of the absorptive surface • Outer aspects of the arms & thighs
• Rate of blood flow to the small intestine • Hip & lower abdomen
• Lipid Solubility of Medicine • Above the iliac crest
• Status of GI motility Intramuscular
• Ventrogluteal
Factors Affecting Pharmacokinetics - for 1 year and above
• Age • Vastus lateralis
• Diseases - below 1-year-old
• Individual Differences • Dorsogluteal
• Psychological Factors clients w/ well-developed gluteal
• Type & Amount of Drug Prescribed muscles
• Social Factors • Deltoid
Intravenous
R (IV) is the installation of fluid and/or
o electrolytes, or nutrient, medication
u substances into a vein.
t Topical Agent
e skin, ophthalmic, otic, nasal, vaginal,
s rectal
Inhalation

Pharmacokinetics:
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DISTRIBUTION
Transportation of drug molecules within the body. METABOLISM
distribution is the movement of the drug from the
circulation to body tissue. DD is influenced by the
rate of blood flow to the tissue, the drugs affinity
to the tissue and chon binding.
Drug needs to be carried to the site of the action.
Need blood to circulate the drug WHAT CAN STOP THIS PROCESS?
Heart, liver, kidneys
KEY CONCEPTS OF DISTRIBUTION
Protein binding – drug molecules need to get
from the blood plasma into the cell
Protein binding allows part of the drug to be
stored and released as needed
Some of the drug is stored in muscle, fat and other
body tissues and is gradually released into the
plasma
An important concept!
HOW DOES THE DRUG GET INTO THE CELL?
Drug must pass though the capillary wall
Blood brain barrier – very effective in keeping
drugs from getting into the central nervous
system or CNS – limits movement of drug
molecules into brain tissue
Blood Brain Barrier
This is especially important when treating
infections of the brain such as meningitis, Pharmacokinetics:
encephalitis, or brain abscess EXCRETION
Medications must be able to penetrate the blood
brain barrier
Medications usually given intravenous
THREE WAYS TO GET IN!
Direct penetration of the membrane
Protein channels
Carrier proteins
# 1 Lipid Soluble Drugs
Lipid soluble drugs are able to dissolve in the lipid
Laboratory Values
layer of the cell membrane
No energy expended by the cell
Passive diffusion
Oral tablets or capsules must be water
soluble to dissolve in fluids of the
stomach and small intestine
# 2 Protein Channels
Most drug molecules are too big to pass in to the
cell via the channels – small ions such as sodium
and potassium use the protein channels but their
movement is regulated by gating mechanisms –
only small amounts allowed
# 3 Carrier Proteins
Molecule needs to bind with a protein that will
transport it from one side of the cell membrane to
another – a drugs structure determines which
carrier will transfer it.
Pharmacokinetics:
Method by which the drugs are inactivated or bio
transformed by the body.
Active drugs contain metabolites that are
excreted – skin, urine, stool
Most drugs metabolized in the liver
Enzyme inhibition
 Other drugs
 Combination drugs
 Liver disease
 Impaired blood circulation in person with
heart disease
 Infant with immature livers
 Malnourished people or those on low-
protein diets
First-pass effect – some drugs are extensively
metabolized or broken down in the liver and only
a part of the drug is released into the systemic
circulation
This is why dosage is important – how much
drug needs to be taken in to give the desired effect
and how often does it need to be taken
Refers to the elimination of the drug from the
body
Requires adequate functioning of the circulatory
system and organs of excretion
 Kidneys
 Bowels
 Lungs
 Skin
Laboratory values reflecting function of liver and
kidneys need to be looked at.
BUN and Creatinine – kidney function
Liver function tests:
 ALT – alamine aminotransferase
(elevated in hepatitis)
 AST or SGOT– aspartate
aminotransferase – elevated in
liver disease
 Bilirubin levels – infants –
gallstones in adults
Serum Drug Levels
 Laboratory measurement of the amount of
drug in the blood at a particular time
 A minimum effective concentration (MEC)
must be present before a drug exerts its action
on a cell.
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 Toxic Levels
Excessive level of a drug in the body
 Single large dose
 Repeated small doses
 Slow metabolism which allows drug to
accumulate in the body
 Slow excretion from the body by the
kidneys or gastrointestinal tract
Laboratory values are important!
Serum drug levels indicate the onset, peak and
duration of the drug action
DO WE DO SERUM DRUG LEVELS FOR ALL DRUGS?
No
When do we need them?
 Drugs with narrow margin of safety
(digoxin, aminoglycoside antibiotics,
lithium)
 To check to see if the drug is at
therapeutic levels – seizure medications
 When drug overdose is suspected
Important concept!
Serum half-life or elimination half-life is the time it
takes the serum concentration of the drug to reach
50%
 A drug with a short half-life requires
more frequent administration
 A drug with a long half-life requires less
frequent administration
1. Inhibit
2. Activate
3. Replace
Enzyme Interaction
Enzymes are substances that catalyze nearly every
biochemical reaction in a cell
Drugs can interact with enzyme systems to alter a
response
Inhibits action of enzymes-enzyme is “fooled” into
binding to drug instead of target cell
Protects target cell from enzyme’s action (ACE
Inhibitors)
Receptor theory
Most drugs exert their effects by chemically
binding with receptors at the cellular level.
Receptors are proteins located
 on the surfaces of cell membranes
 within the cells
WHAT DO THE RECEPTORS DO?
The receptors are often described as the lock into
which the drug molecule fits as a key.
All body cells do not respond to all drugs even
when all the cells are exposed to the drug.
RECEPTOR

Why is this important?

Half-life determines how often a drug is given
 OD-Daily in the morning
 H. S.-At bedtime
 Q.I.D - four times a day
 T.I.D – three times a day
 Q4 hours – every four hours
 Q 12 hours – 9 am and 9 pm
 Q6hours- every 6 hours
 BID- two times a day
 Q8 hours- every 8 hours Nursing pharmacology

Pharmacodynamics
The study of what the drug does to the body the
mechanism of drug actions in living tissues

“WHAT THE DRUG DOES TO THE BODY”

Cellular Physiology
What does a cell do?
 Exchange material
 Obtain energy from nutrients
 Synthesize hormones, neurotransmitters,
enzymes, structural proteins and other
complex molecules LOCKS
 Duplicate themselves

Drugs can:
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THE THREE DISTINCT PHASES OF A DOSE–RESPONSE
CURVE.
RECEPTORS ARE REGULATED IN TWO WAYS:
1. Agonists (activators)
– bind to the receptor and act to produce a
pharmacologic effect
2. Antagonists (blockers)
– bind to the receptor and prevent the cell from
producing an effect
Agonist-Antagonist
POTENCY AND EFFICACY
More is not better!
Number of receptors site available will effect drug
action so giving a higher dose does not necessarily
produce additional pharmacological effects.
Drug Dosing
Often the first dose is higher in an effort to bring
the therapeutic blood serum levels up quicker
NURSING PHARMACOLOGY
THERAPEUTIC INDEX AND DRUG SAFETY
 Administering a dose that produces an optimum
therapeutic response for each individual patient is
only one component of effective
pharmacotherapy. Nurses must also be able to
predict whether the dose is safe for the patient.
 The larger the difference between the two
doses, the greater the therapeutic index.
 The therapeutic index offers the nurse
practical information on the safety of a drug
and a means to compare one drug with
another.
THE GRADED DOSE–RESPONSE RELATIONSHIP AND
THERAPEUTIC RESPONSE
The graded dose–response relationship is a
fundamental concept in pharmacology. The
graphical representation of this relationship is
called a dose–response curve.
By observing and measuring the patient’s
response obtained at different doses of the drug,
one can explain several important clinical
relationships.
Phase 1 occurs at the lowest doses. The flatness
of this portion of the curve indicates that few
target cells have yet been affected by the drug.
Phase 2 is the straight-line portion of the
curve. This portion often shows a linear
relationship between the amount of drug
administered and the degree of response obtained
from the patient.
Phase 3, a plateau is reached in which
increasing the drug dose produces no
additional therapeutic response. This may
occur for a number of reasons.
Within a pharmacologic class, not all drugs are
equally effective at treating a disorder. Nurses
need a method to compare one drug with another
in order to administer treatment effectively.
There are two fundamental ways to compare
medications within therapeutic and
pharmacologic classes. First is the concept of
POTENCY. A drug that is more potent will produce
a therapeutic effect at a lower dose, compared
with another drug in the same class.
CELLULAR RECEPTORS AND DRUG ACTION
Drugs act by modulating or changing existing
physiological and biochemical processes. To exert
such changes requires that drugs interact with
specific molecules and chemicals normally found
in the body.
A cellular macromolecule to which a medication
binds in order to initiate its effects is called a
RECEPTOR. The concept that a drug binds to a
receptor to cause a change in body chemistry or
physiology is a fundamental theory in
pharmacology. Receptor theory explains the
mechanisms by which most drugs produce their
effects.
Not all receptors are bound to plasma
membranes; some are intracellular molecules
such as DNA or enzymes in the cytoplasm. By
interacting with these types of receptors,
medications are able to inhibit protein synthesis
or regulate cellular events such as replication and
metabolism. Examples of agents that bind
intracellular components include steroid
medications, vitamins, and hormones.
Some drugs act independently of cellular
receptors. These agents are associated with other
mechanisms, such as changing the permeability of
cellular membranes, depressing membrane
excitability, or altering the activity of cellular
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 pumps. Actions such as these are described as Supplemental therapy
nonspecific cellular responses. Palliative therapy
Supportive therapy
TYPES OF DRUG–RECEPTOR INTERACTIONS Prophylactic therapy
When a drug binds to a receptor, several Type of Medication Action
therapeutic consequences can result. In simplest Therapeutic Effect
terms, a specific activity of the cell is either Side Effects
enhanced or inhibited. The actual biochemical Adverse Effects
mechanism underlying the therapeutic effect, Toxic Effect
however, may be extremely complex. In some Idiosyncratic Reactions
cases, the mechanism of action is not known. Allergic Reaction
When a drug binds to its receptor, it may produce Medication Interactions
a response that mimics the effect of the Iatrogenic Response
endogenous regulatory molecule.
Therapeutic Effect
Drug – Diet interaction The expected or predictable physiological
Food can slow absorption response a medication causes
Food substances can react with certain drugs A single med can have several therapeutic effects
How to give medication is information provided in
you drug manual Side Effects
‘A drug that does not cause side-effects is a drug that does
Drug – Drug Interaction not work.’
Some drugs taken together will enhance each Unintended secondary effects a medication
other predictably will cause
Tylenol with codeine May be harmless or serious
Some drugs taken together will interfere with If side effects are serious enough to negate the
another drugs actions beneficial effect of meds therapeutic action, it may
Some drugs are given to decrease or reverse the be D/C
toxic effects of a drug People may stop taking medications because of
Narcotic antidote is naloxone the side effects

Drug Tolerance ADVERSE RECTION

Body becomes accustomed to drug over period of • Medication misadventures
time – Adverse drug events
Adverse Effects – Adverse drug reactions
Undesired response – Medication errors
Allergic reaction Adverse Effects
Drowsiness  Undesirable response of a medication
Nausea / vomiting / GI upset  Unexpected effects of drug not related to
Liver or kidney damage therapeutic effect
Fevers  Must be reported to FDA
Drug dependency  Can be a side effect or a harmful effect
Cancinogenicity – ability to cause cancer  Can be categorized as pharmacologic,
Teratogenicity – cause damage to fetus idiosyncratic, hypersensitivity, or drug
interaction
Pharmacotherapeutics
The use of drugs and the clinical indications for TOXIC EFFECT
drugs to prevent and treat diseases Toxicology
The study of poisons and unwanted responses to
Monitoring therapeutic agents
The effectiveness of the drug therapy must be
evaluated. Toxic Effect
One must be familiar with the drug’s intended May develop after prolonged intake or when a
therapeutic action (beneficial) and the drug’s medicine accumulates in the blood because of
unintended but potential side effects (predictable, impaired metabolism or excretion, or excessive
adverse drug reactions). amount taken
Toxic levels of opioids can cause respiratory
Types of Therapies depression
Acute therapy Antidotes available to reverse effects
Maintenance therapy
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Idiosyncratic Reactions
Unpredictable effects-overreacts or under reacts
to a medication or has a reaction different from
normal
Normal effect is produce by a small fraction of the
standard dose.
Allergic Reaction
Unpredictable response to a medication
Makes up greater than 10% of all medication
reactions
Client may become sensitized immunologically to
the initial dose, repeated administration causes an
allergic response to the medicine, chemical
preservative or a metabolite
Medication acts as an antigen triggering the
release of the body’s antibodies
May be mild or severe
• Lower doses are needed when the drugs are
given together.
• Similar therapeutic activity can cause
problems if administered together
SYNERGISTIC EFFECT
• Effect of 2 meds combined is greater than the
meds given separately
• Alcohol & Antihistamines, antidepressants,
barbiturates, narcotics
ANTAGONIST EFFECT
• Combined effect is less than each of them
alone.
• Drugs with opposite action to that of another
drug or natural body chemical
• Examples: Beta-blockers the ‘olol’ drugs
INCOMPATIBILITY EFFECT
• Drugs are incompatible when combining
them causes chemical deterioration of
one or both

OTHER DRUG REACTIONS

Teratogenic- Structural effect in unborn fetus
Carcinogenic-Causes cancer
Mutagenic- Changes genetic composition
(radiation, chemicals)

Iatrogenic Responses
Unintentional adverse effects that occur during
therapy
Treatment Induced Dermatologic
rash, hives, acne
Renal Damage
Aminoglycoside antibiotics, NSAIDS,
contrast medium
Blood Dyscrasias
Destruction of blood cells
(Chemotherapy)
Hepatic Toxicity
Elevated liver enzymes

DRUG INTERACTIONS
Interactions
• Additive effect
• Synergistic effect
• Antagonistic effect
• Incompatibility

ADDITIVE EFFECT
• Drugs are said to have an additive effect when
they have similar actions.
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