PHARMACEUTICS

The study of how various drug forms influence

pharmacokinetic and pharmacodynamic activities.

PHARMACOTHERAPEUTICS
The use of drugs and the clinical indications for drugs to
prevent and treat diseases.

PHARMACOGNOSY
The study of natural (plant and animal) drug sources.
Formerly called materia medica (medicinal materials) and is
concerned with botanical or zoologic origin.

PHARMACOKINETICS
The study of what the body does to the drug molecules.

Administering medications, supervising medication,

self-administration, and assisting other health personnel with
the administration of medications are common functions of the
nurse. These functions require a variety of skills.

Drugs are capable of exerting a wide variety of effects in

the human body. Knowing the actions, both intended and
unwanted,, of drugs taken by clients under the nurse’s care is
essential, even when the nurse is not personally responsible for
administering the drugs.

Pharmacokinetics derived from the Greek words

pharmakon (drug) and kinetikos (movement), is used to describe
the absorption, distribution, metabolism, and excretion of a
compound. Although pre-clinical studies require the
determination of acceptable in vitro activity and in at least two
animal species, pharmacokinetic studies must be performed in
man to correlate blood concentrations with particular
biological effects.

Pharmacokinetic studies of natural products are

challenging because they typically involve the administration of
complex mixtures of substances, in many instances of unknown
components.
parenteral
❖ Four steps for pharmacokinetics
➢ Absorption - through oral, topical, injections
■ Bioavailability is the proportion of a drug
that is successfully absorbed into systemic
circulation
➢ Distribution - the way that drugs move through
the bloodstream
■ Anatomical barriers → blood-brain barrier
& blood-placental barrier
➢ Metabolism - reactions that inactive the drug
and target for excretion
■ Drugs travelling through the bloodstream
are likely to be metabolized to some degree
■ Drugs taken orally will enter the hepatic
portal system
■ First-pass effect: first pass of a drug
through the liver; the bioavailability is
greatly reduced and 90% of the drug may
be inactivated
■ Drugs are metabolized after reaching their
targest
➢ Excretion - how the drug exits; blood filtration,
defecation, urination, sweating, and exhalation
■ Drugs are excreted through bile via
enterohepatic circulation
ABSORPTION
❖ A drug to produce a pharmacologic effect, it must be
absorbed or transported from its site of administration (GI
tract, muscle, skin) into the bloodstream
❖ The rate at which drugs are absorbed determines the
onset of effect.
❖ In turn, the amount of drug absorbed determines the
intensity of effects
 ❖ Both drug-related & patient-related factors influence drug
absorption.
❖ First pass effect
➢ The metabolism of a drug and its passage from the
first pass effect can also occur
in the lungs, vasculature
liver into the circulation
(veins), gastrointestinal tract,
and other metabolically active
■ A drug given via the oral route may be
tissues in the body extensively metabolized by the liver before
reaching the systemic circulation (high first-pass
major site of drug
effect) metabolism
■ The same drug — given IV — bypasses the liver,
preventing the first-pass effect from taking
place, and more drug reaches the circulation.
❖ Factors that affect the absorption of the medication in teh
stomach:
➢ Acidity of the stomach
➢ The presence or absence of food or fluid
➢ Age of the patient
➢ Presence of other types of medication
❖ Drugs administered sublingually or in buccal mucosa, they
are absorbed in the highly vascularized (large blood
supply) tissue like under the tongue.
❖ Bypassed the liver
❖ Absorbed rapidly in the bloodstream and delivered at the
site of action
❖ Parenteral
➢ It is the general term meaning any route other than
the stomach, most commonly it refers to injection like
subcutaneous, intradermal, and intramuscular
➢ Advantage of bypassing the first pass effect
➢ Absorbed at the site of injection
➢ Intravenous
■ Delivers drug directly in the bloodstream
■ Fastest absorption
❖ Topical drugs
➢ Absorbed locally and effect is non-systemic.
 ❖ Inhaled drugs will be transported and absorbed in the
airsacs of alveoli.

DISTRIBUTION
❖ It refers to the transportation of drug via the bloodstream
to its site of action.
❖ 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 drug are eliminated in the liver or
kidney.
❖ Distribution
➢ Protein-binding
➢ Blood flow
➢ Body tissue affinity
➢ Lipid solubility

METABOLISM
❖ Biotransformation in the liver
❖ It involves biochemical alteration of the drug to inactive
metabolite, a more soluble compound or to a more potent
active metabolite
❖ Other metabolic tissue: skeletal muscle, kidney, lungs,
intestinal mucosa
❖ Delayed drug metabolism results in:
➢ Accumulation of drugs
➢ Prolonged action of th drug
❖ Stimulating drug metabolism causes:
➢ Diminished pharmacologic effects

EXCRETION
❖ Elimination of drug in the body
❖ Whether active or inactive, drugs must eventually be
removed from the body
❖ Kidney (main organ)
 ❖ Other organ of excretions
➢ The bowel and the liver (as bile)
❖ Other routs of excretion
➢ Through sweat and saliva

PHARMACODYNAMICS
It is the study of the biochemical and physiologic effects of
drugs (especially pharmaceutical drugs). The effects can
include those manifested within animals (including humans),
microorganisms, or combinations of organisms (for example,
infection).

Pharmacodyamics places particular emphasis on

dose–responses relationships, that is, the relationships between
drug concentration and effect.

❖ It is the study of the mechanism of drug actions in living

tissue;
❖ What the 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

THREE 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.

❖ Drugs are induced alterations to normal physiologic

function
❖ Positive change → Therapeutic effect → Goal of Therapy
MECHANISM OF ACTION
They are ways in which a drug can produce a therapeutic
effect.
❖ The effects that a particular drug has depends on the
cells or organ targeted by the drug.
❖ Once the drug hits its “site of action” it can modify the rate
at which a cell or tissue functions.

1. Receptor Interaction
○ Drug structure is essential.
○ It involves the selective joining of drug molecule
with a reactive site on the cell surface that elicits
a biological effect.
○ Receptor is the reactive site on a cell or tissue.
○ Once the substance binds to and interacts with
the receptor, a pharmacologic response is
produced.

A. Drugs act by forming a chemical bond with specific receptor

sites, similar to a key and lock B. The better the “fit” the better
the response. Drugs with complete attachment and response
are called agonists. C. Drugs that attach but do not elicit a
response are called antagonists. D. Drugs that attach, elicit
some response, and also block other responses are called
partial agonists or agonist-antagonists.
RECEPTOR INTERACTION
❖ Affinity is used to describe the strength of the drug’s
binding to receptors.
❖ The drug with the best “fit” or affinity will elicit the best
response.

DRUG ACTION
It is the interaction between the drug and molecular,
cellular components (mechanism of action). Drug action may
be:
❖ Agonist — Drug binds to receptor → There is a response.
(Adrenergic Agents)
❖ Antagonist — Drug binds to receptor → There is no
response. → It 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.

PARAMETERS OF DRUG ACTION

❖ Onset of Action – interval between time drug is
administered and first sign of its effect.
❖ Dureaction
Duration of Action – length of time the drug exerts
pharmacologic effect.
❖ Peak Action – drug reaches its highest blood/plasma
concentration
 cause or accelerate a
biological process to begin

2. 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)
3. Non-Specific Interaction
○ Not involving a receptor site or alteration in
enzyme function
○ 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
HALF-LIFE
A measure of the time required for elimination.

❖ It 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 100mg of a drug that
has a half-life of 12 hours, it will show like this:

The nurse is giving a medication that has a high first-pass

effect. The physician has changed the route from IV to PO. The
nurse expects the oral dose to be:
1. Higher because of the first-pass effect.
2. Lower because of the first pass effect.
3. The same as the IV dose.
4. Unchanged.