NCM 212 - PHARMACOLOGY

PHARMACOKINETICS & PHARMACODYNAMICS 🧑‍⚕️ DESIATA, LYRIZZA

INTRODUCTION TO PHARMACOLOGY
PHARMACOKINETICS & PHARMACODYNAMICS AREAS OF PHARMACOLOGY
(1) Pharmaceutics
(2) Pharmacokinetics
Administering medications, supervising
(3) Pharmacodynamics
medication self-administration and assisting other
health personnel with the administration of
Pharmaceutics
medications are common functions of the nurse.
● Study of how various drug forms
These functions require a variety of skills.
influence pharmacokinetic (what the
Drugs are capable of exerting a wide
body does to the drug) and
variety of effects in the human body. Knowing the
pharmacodynamic (what the drug does
actions, both intended and unwanted, of drugs
to the body) activities
taken by clients under the nurse's care is essential,
Pharmacokinetics
even when the nurse is not personally responsible
● The study of what the body does to the
for administering the drugs.
drug molecules.
PHARMACOKINETICS
4 Phases
● Derived from the Greek words pharmakon
(1) Absorption
(drug) and kinetikos (movement)
(2) Distribution
● Used to describe the absorption, distribution,
(3) Metabolism
metabolism, and excretion of a compound
(4) Excretion
● Although pre clinical studies require the
Pharmacodynamics
determination of acceptable in vitro activity
● The study of what the drug does to the
and in at least two animal species,
body.
pharmacokinetic studies must be performed
● The mechanism of drug actions in living
in man to correlate blood concentrations
tissues
with particular biological effects
Pharmacotherapeutics
● Pharmacokinetic studies of natural products
● Use of drugs and the clinical indications
are challenging because they typically
for drugs to prevent and treat diseases.
involve the administration of complex
Pharmacognosy
mixtures of substances, in many instances of
● The study of natural (plant and animal)
unknown components
drug sources.
PHARMACODYNAMICS ● Formerly called materia medica
● The study of the biochemical and physiologic (medicinal materials) and is concerned
effects of drugs (especially pharmaceutical with botanical or zoologic origin
drugs).
● The effects can include those manifested
within animals (including humans),
microorganisms, or combinations of
organisms (for example, infection)
● Pharmacodynamics places particular
emphasis on dose–response relationships,
that is, the relationships between drug
concentration and effect
 PHARMACOKINETICS ABSORPTION
● For a drug to produce a pharmacologic
Pharmacokinetics derived from the
effect, it must be absorbed or transported
Greek words pharmakon (drug) and kinetikos
from its site of administration (GI tract, muscle,
(movement), is used to describe the absorption,
skin) into the bloodstream
distribution, metabolism, and excretion of a
● The rate at which drugs are absorbed
compound. Although pre clinical studies require
determines the onset of effect
the determination of acceptable in vitro activity
● In turn, the amount of drug absorbed
and in at least two animal species,
determines the intensity of effects
pharmacokinetic studies must be performed in
● Both drug-related & patient-related factors
man to correlate blood concentrations with
influence drug absorption
particular biological effects.
● Drugs administered sublingually or in buccal
Pharmacokinetic studies of natural
mucosa, they are absorbed in the highly
products are challenging because they typically
vascularized (large blood supply) tissue like
involve the administration of complex mixtures of
under the tongue
substances, in many instances of unknown
● Bypassed the liver
components
● Absorbed rapidly in the bloodst
PHARMACOKINETIC PHASE (ADME PROCESS)
Absorption: when a drug is released from its Absorption of Drugs via Route
formulation/admin site and enters the ● PARENTERAL
bloodstream
○ Is the general term meaning any route
Distribution: movement of a drug once in the
other than the stomach, most commonly it
bloodstream
Metabolism: the body using the drug and refers to injection like subcutaneous,
giving off a byproduct intradermal and intramuscular
Excretion: getting rid of by product ○ Advantage of bypassing the first pass

PHASES OF SOLID DRUG ABSORPTION effect

○ Absorbed at the site of injection
○ Intravenous
■ Delivers drug directly into the
bloodstream
■ Fastest absorption
● TOPICAL DRUGS
○ Absorbed locally and effect is non-systemic
● INHALED DRUGS
○ Inhaled drugs will be transported and
absorbed in the air sacs or alveoli
FIRST PASS EFFECT DISTRIBUTION
● The metabolism of a drug and its ● It refers to the transportation of drug via the
passage from the liver into the bloodstream to its site of action
circulation ● For a drug to achieve its therapeutic effect, it
must proceed to the part of the body or
tissue with which it will react
● At this point some drugs are eliminated in the
liver and kidney

○ A drug given via the oral route may be

extensively metabolized by the liver before
reaching the systemic circulation (high
first-pass effect)
○ The same drug—given IV—bypasses the
liver, preventing the first-pass effect from
taking place, and more drug reaches the
circulation

METABOLISM
Factors that affect the absorption of the
● Biotransformation in the liver
medication in the stomach:
● It involves biochemical alteration of the drug
● Acidity of the stomach
to inactive metabolite, a more soluble
● The presence or absence of food or fluid
compound or to a more potent active
● Age of the patient
metabolite
● Presence of other types of medication
● Other metabolic tissue: skeletal muscle,
kidney, lungs, intestinal mucosa
Delayed drug metabolism results in:
● Accumulation of drugs
● Prolonged action of the drugs
Stimulating drug metabolism causes:
● Diminished pharmacologic effects
EXCRETION
● Elimination of drug in the body
PHARMACODYNAMICS
Pharmacodynamics (PD) is the study of
● Whether active or inactive, drugs must
the biochemical and physiologic effects of drugs
eventually be removed from the body
(especially pharmaceutical drugs). The effects
● Kidney ( main organ)
can include those manifested within animals
Other organ of excretion:
(including humans), microorganisms, or
● the bowel and liver
combinations of organisms (for example,
Other routes of excretion:
infection).
● through sweat and saliva
Pharmacodynamics places particular
emphasis on dose–response relationships, that is,
the relationships between drug concentration and
effect.

PHARMACODYNAMIC
● Study of the mechanism of drug actions in
living tissue
● What a drug does to the body
○ relates to the site of drug action
● The site of drug action is the specific cell,
tissue, or organ where the drug works
Drugs-induced alterations to normal physiologic
function

3 PRINCIPLES ABOUT DRUG ACTION

(1) Drugs do not create new function or
response but modify or alter existing
physiologic activity within the body;
(2) Drugs interact with the body in several
different ways. No drug has a single action
(3) Drug effects are determined by the drug’s
interaction with the body.
MECHANISM OF ACTION Parameters of Drug Action
● Ways in which a drug can produce a Onset of Action
therapeutic effect ● interval between time drug is
○ The effects that a particular drug has administered & first sign of its effect.
depends on the cells or organ targeted Duration of Action
by the drug. ● length of time the drug exerts
○ Once the drug hits its “site of action” it pharmacologic effect.
can modify the rate at which a cell or Peak Action
tissue functions. ● drug reaches its highest blood/plasma
RECEPTOR INTERACTION concentration
● Drug structure is essential
● Involves the selective joining of drug ENZYME INTERACTION
molecule with a reactive site on the cell ● Enzymes-
surface that elicits a biological effect ○ are substances that catalyze
● Receptor nearly every biochemical
○ is the reactive site on a cell or tissue reaction in a cell
● Once the substance binds to and interacts ● Drugs can interact with enzyme systems
with the receptor, a pharmacologic response to alter a response
is produced ● Inhibits action of enzymes-enzyme is
● Affinity “fooled” into binding to drug instead of
○ used to describe the strength of the drug’s target cell
binding to receptors ● Protects target cell from enzyme’s action
● The drug with the best “fit” or affinity will elicit (ACE Inhibitors)
the best response
Drug Action NON-SPECIFIC INTERACTION
● Interaction between the drug and ● Not involving a receptor site or alteration
molecular, cellular components in enzyme function
(mechanism of action) ● Main site of action is cell membrane or
cellular process
● Drugs will physically interfere or
chemically alter cell process
● Final product is altered causing defect or
cell death
● Cancer drugs, Antibiotics

Agonist
● Drug binds to receptor-there is a response
(Adrenergic Agents)
● drug binds to receptor-no response-prevents
binding of agonists (Alpha & Beta Blockers)
Competitive Antagonist
● act with receptor sites to block normal
stimulation producing no effect
Noncompetitive Antagonist
● prevent reaction of another chemical with
different receptor site on that cell
HALF-LIFE
● A measure of the time required for
elimination
● Is determined by an individual’s ability to
metabolize and excrete a particular
drug
● When the half-life of the drug is known,
dosages and frequency of
administration can be calculated.
For example: if a patient is given 100 mg of a drug
that has a half-life of 12 hours, it will show like this:
EFFECTS OF DRUGS IN THE HUMAN BODY
TOXIC EFFECTS OF DRUGS
ADVERSE EFFECTS
● Predictable or unpredictable
○ Excessive pharmacologic
effects
○ most predictable and are often
the easiest to prevent or
counteract
○ May be unpleasant or even
dangerous
● Occur for many reasons, including the
following:
○ The drug may have other
effects on the body besides the
therapeutic effect
○ The patient is sensitive to the
drug given
○ The drug’s action on the body
causes other responses that are
undesirable or unpleasant
○ The patient is taking too much
or too little of the drug, leading
to adverse effects
Primary actions
● One of the most common occurrences
in drug therapy is the development of
adverse effects from simple overdose
● can be extensions of the desired effect
Secondary actions
● Secondary actions of the drug are
effects that the drug causes in the body
that are not related to the therapeutic
effect
● In addition to the desired
pharmacological effect
HYPERSENSITIVITY
● Some patients are excessively responsive
to either the primary or the secondary
effects of a drug
● It may result from a pathological or
underlying condition
Gell and Coombs Classification System
Type I reactions
● immediate hypersensitivity reactions
that are mediated by immunoglobulin E
(IgE) antibodies
● Eg: urticaria (hives), atopic dermatitis,
anaphylactic shock
Type II reactions
● cytolytic reactions that involve
complement are mediated by
immunoglobulins G and M (IgG and IgM)
● Eg: hemolytic
anemia,thrombocytopenia, and
drug-induced lupus erythematosus
Type III reactions
● mediated by immune complexes
● The deposition of antigen antibody
complexes in vascular endothelium
leads to inflammation,
lymphadenopathy, and fever (serum
sickness)
● Eg: severe skin rash seen in patients with
a life-threatening form of drug-induced
immune vasculitis that is known as
StevensJohnson syndrome
Type IV reactions
● delayed hypersensitivity reactions that
are mediated by sensitized lymphocytes
● Eg: ampicillin-induced skin rash that
occurs in patients with viral
mononucleosis
DRUG ALLERGY
● Occurs when the body forms antibodies
to a particular drug, causing an immune
response when the person is re-exposed
to the drug.
Four main classifications:
I. Anaphylactic reaction
● this allergy involves an antibody that
reacts with specific sites in the body to
cause the release of chemicals,
including histamine that produce
immediate reactions(mucous membrane
swelling & constricting bronchi) that can
lead to respiratory distress and even
respiratory arrest
II. Cytotoxic reaction
● this allergy involves antibodies that
circulate in the blood and attack
antigens(the drug)on cell sites, causing
death of that cell. This reaction is not
immediate but may be seen over a few
days
III. Serum reaction
● this allergy involves antibodies that
circulate in the blood and cause
damage to various tissues by depositing
in blood vessels. This reaction may occur
up to a 1 week or more after exposure to
the drug
IV. Delayed reaction
● this reaction occurs several hours after
exposure and involves antibodies that
are bound to specific white blood cells.
DRUG-INDUCED TISSUE AND ORGAN DAMAGE SUPERINFECTION
● One of the body’s protective mechanisms is
provided by the wide variety of bacteria that
DERMATOLOGICAL REACTION
live within or on the surface of the body.
● They adverse reactions involving the skin
● This bacterial growth is called the normal flora
● It range from a simple rash to potentially fatal
● Several kinds of drugs especially antibiotics
exfoliative dermatitis
destroy the normal flora, leading to
○ Rashes, Hives
development of superinfection
● Rash, scaling, fever, enlarged lymph nodes,
ASSESSMENT
enlarged liver and the potentially fatal
● Symptoms can include fever, diarrhea, black
erythema multiforme exudativum or known as
or hairy tongue, inflamed and swollen tongue
Stevens-Johnson syndrome.
(glossitis), mucous membrane lesions and
INTERVENTION
vaginal discharge with or without itching
● In mild cases, or when the benefit of the drug
INTERVENTIONS
outweighs the discomfort of the skin lesion,
● Provide supportive measures like frequent
provide frequent skin care; instruct the
mouth care, skin care, access to bathroom,
patient to avoid rubbing, wearing tight or
small and frequent meals
rough clothing, and using harsh soap, or
● Administer antifungal therapy as appropriate
perfumed lotions
● Administer antihistamines as needed
BLOOD DYSCRASIA
● In severe cases, discontinue the drug
● It is bone marrow suppression caused by drug
● Notify the prescriber
effects
● Application of topical corticosteroids or
ASSESSMENT
emollient are frequently used
● Fever, chill, sore throat, weakness, back pain,
dark urine, agranulocytosis, anemia,
STOMATITIS
thrombocytopenia (low platelet), leukopenia
● Inflammation of the mucous membranes,
(low WBC) or a combination of these
can occur because of a direct toxic reaction
(pancytopenia)
to the drug or because the drug deposits in
● Most serious is aplastic anemia
the end capillaries in the mucous
INTERVENTION
membranes, leading to inflammation.
● Monitor blood counts
○ Eg: Antineoplastic drugs
● Provide supportive measures (rest, protection
ASSESSMENT
from exposure to infection, injury, or bleeding)
● It includes swollen gums, inflamed gums
● In severe cases, discontinue the drug or stop
(gingivitis) and swollen and red tongue
administration until the bone marrow recovers
(glossitis)
to safe level, but may have serious
INTERVENTIONS
consequences before toxicity can be
● Provide frequent mouth care with a non
detected
irritating solution
● Offer nutrition evaluation
TOXICITY
● Development of tolerated diet
● Introducing chemical into the body can
sometimes affect the body in a very noxious
or toxic way
LIVER INJURY (HEPATOTOXICITY)
● Cholestatic hepatotoxicity is often
caused by a hypersensitivity mechanism
producing inflammation and stasis of the
biliary system.
● Hepatocellular toxicity is sometimes
caused by a toxic drug metabolite.
ASSESSMENT
● Fever, malaise, nausea, and vomiting,
jaundice, change in color of urine or
stools, abdominal pain or colic, elevated
liver enzymes (serum transaminase level)
INTERVENTIONS
● Discontinue the drug and notify the
prescriber
● Offer supportive measures (small,
frequent, meals, skin care, cool
environment, rest periods)
RENAL INJURY (NEPHROTOXICITY)
● Classified according to site and
mechanism and include interstitial
nephritis, renal tubular necrosis and
crystalluria (the precipitation of insoluble
drug in the renal tubules)
BLADDER TOXICITY
● It is less common than renal toxicity, but it
may occur as an adverse effect of a few
drugs.
● One example is cyclophosphamide, an
antineoplastic drug whose metabolite
causes hemorrhagic cystitis.
ASSESSMENT
● Elevated blood urea nitrogen (BUN),
elevated creatinine concentration,
decreased hematocrit, electrolyte
imbalances, fatigue, malaise, edema,
irritability, and skin rash
INTERVENTIONS
● Notify the prescriber
● Discontinue the drug as needed
● Offer supportive measures (diet & fluid
restrictions, skin care, electrolyte therapy,
rest)
● In severe cases, dialysis may be required
for survival
OTHER ORGAN TOXICITIES
● Pulmonary toxicity occurs through a
variety of mechanisms. Some drugs
cause respiratory depression via their
effects on the brain stem respiratory
centers.
● Relatively few drugs produce
cardiotoxicity. Some may cause skeletal
muscle damage evidenced by muscle
pain and sometimes leading to
rhabdomyolysis.
POISONING
● Occurs when an overdose of a drug
damages multiple body systems, leading
to the potential for fatal reactions.
● Emergency and life support measures
often are needed in severe cases
SKIN RASHES OF ALL VARIETIES
● These can range from a simple rash to
potentially fatal exfoliative dermatitis.
Adverse reactions involve the skin
because many drugs can deposit there
or cause direct irritation to the tissue.
Reactions
● It includes macular, papular,
maculopapular & urticarial rashes, and
potentially fatal erythema multiforme
exudativum (Stevens-Johnson syndrome)
may be produced by drug
hypersensitivity reactions.
IDIOSYNCRATIC REACTIONS
● Unexpected drug reactions caused by a
genetically determined susceptibility
results:
● Extreme sensitivity to a low dose
● Extreme insensitivity to a high dose
● Unpredictable or unexplainable
symptoms
● Results in paradoxical reactions
(opposite of desired)
○ Eg: a sedative is given for
insomnia, but instead keeps the
patient awake
DRUG INTERACTIONS
Additive effect
● 2 drugs with similar actions are taken for
a doubled effect (1 + 1 = 2)
● Ibuprofen + paracetamol = added
analgesic effect
Synergistic effect
● Combined effect of 2 drugs is greater
than sum of the effect or each drug
given alone (1+1=3)
● Aspirin + codeine = greater analgesic
effect
Potentiation
● A drug that has no effect enhances the
effect of a 2nd drug (0+1=2)

Antagonistic
● One drug inhibits the effect of another
drug (1+1=0)
● Tetracycline + antacid = decreased
absorption of tetracycline