MODULE ONE STUDYING PHARMACOLOGY

At the end of this module, you will be able to:

 Define the phases of pharmacology and drug therapy.

 Perform a learning styles inventory to reveal your preferred learning style(s).

 Determine which methods for learning pharmacology are compatible with you
learning style(s).

 Described major drug classes, controlled substances schedules, pregnancy

categories, prescription vs over-the-counter regulations, and how drugs are
classified by brand/generic names.

 Identify the main principles of organic chemistry, pharmacodynamics, and

pharmacokinetics.

 Describe how atoms combine to form different kinds of molecules.

 Distinguish how pH affects behavior of acidic and basic drug molecules.

 Identify the key components of the dose response curve that represent
therapeutic range, efficacy, potency, and steady state.

 Describe factors that influence absorption, distribution, metabolism, and

excretion of drugs from the body.

Pharmacology – the study of how drugs from various sources work inside the body for their intended
purposes.

Physiology – the study of normal body function.

Pathophysiology – the study of abnormal body processes or disease.

Phases of Pharmacology
Each phase focuses on a different part of the way the drug works, how they
are introduced into the body, and how they behave in it.
Pharmaceutics – the study of how drugs are introduced into the body.

Pharmacokinetics – the study of how drugs are absorbed into the

bloodstream (absorption), circulated to tissues throughout the body
(distribution), inactivated (metabolized), and eliminated (metabolism and
excretion). Pharmacokinetic processes affect a drug’s effectiveness, dosing
schedule, and use.
 Pharmacodynamics – the study of drugs and their receptors on the molecular
level.

Pharmacotherapeutics – the study of how drugs are used in clinical practice

for individual patients.
Determining what will be most beneficial and appropriate for use for an
individual patient.

Strategies for Learning Pharmacology

 This is not going to be easy, it’s like learning a new language.

 Break up the material into categories – drug classes.

 Memorize brand & generic drug names.

 Learn commonalities that apply to drugs in a class

Develop methods that work best for you so that you can understand and
remember all you need.
Learning styles – your preferred learning methods.

 Intrapersonal (independent)

 Interpersonal (group)

 Drug Classifications
 Drugs are categorized in a variety of ways. When a molecule is first
discovered for medicinal properties, its name is based on molecular
structure and traditional chemical nomenclature.
 During phase I clinical trials – 1st tried on healthy human subjects –
drugs are given a generic drug name – assigned by a government
agency.
 Phase II & III clinical trials – drugs are tested on humans having the
condition or disease the drug is supposed to treat. Near the end of
Phase III, a proprietary or brand name is assigned by the company that
will manufacture and sell the drug.
 Phase IV clinical trials – postmarketing.

 Generic substitution
 Often a drug’s class, mechanism of action, and common uses can be
easily determined by simply knowing a drugs generic name.
 Major Drug Classes
 Medications are grouped by major drug classes according to their
mechanism of action. Drugs that work in the same way are put into a
particular class and usually given names with a common stem. Drug
classes are then lumped into therapeutic classes – use on a particular
body system.

 “Look-alike” and “sound-alike” drug names
 Prescription vs OTC Medications
 Legend or prescription drugs - only available by prescription and are
dispensed from the pharmacy upon receipt of a valid prescription from
a prescriber.
 Over-the-counter (OTC) - medications that can be purchased without a
prescription.

 Controlled vs Non-Controlled Substances
 Controlled substances - medications that have been categorized by the
Drug Enforcement Agency (DEA) to have the potential for abuse and
dependence.
 Schedule I – illegal substances or only available for research or
experimental purposes.
 Schedule II – V – medications that can be legally dispensed with
certain restrictions.

 Pregnancy Categories
 Pregnancy categorization - developed to assess safety during
pregnancy; determining potential benefits and risks involved when a
woman takes a medication while pregnant.
 Some drugs are considered safe during pregnancy because they do not
significantly cross through the placenta and enter the bloodstream of
the developing fetus.
 Teratogenic – drugs that can cause birth defects or malformations in a
developing fetus; degree of teratogenicity may depend on the stage of
development.
 Alternative and Complementary Treatments
 Western medicine – traditional medicine; treatments generally
recognized and accepted; relies on the scientific method.
 Eastern medicine – older type of medicine that used herbs and
alternative therapies and recognizes a person’s spiritual being and
balance.
 Dietary and nutritional supplements – are regulated as foods; not
regulated for safety and efficacy as are prescription and OTC products
by the FDA.
  Homeopathy – treating an ailment with a substance, that can cause an
effect similar to the ailment itself.
 Chinese medicine – uses Eastern medical philosophies.
 Acupuncture – insertion of needles at specific points on the body to
unblock energy channels.
 Acupressure – applies pressure to those points to enhance energy flow.
 Chiropractic therapy – non-drug modalities; manipulation to achieve
better body alignment and health.
 Ayurveda – East Indian medicine that involves spiritual and whole-body
well-being, employing change in diet and lifestyle.
 Biofeedback – mental exercise and relaxation to slow heartbeat, lower
blood pressure, and reduce stomach problems.
Common Pharmacy Abbreviations and Terms
Abbreviations are used to express orders, preparation, and administration of
drug therapy.

Most prescribers use abbreviations to write prescriptions and orders.

Knowing prescribing terms and pharmacy abbreviations is essential for

correct and quick interpretation of orders.

Abbreviations and what they mean must be committed to memory in order to

work efficiently in the pharmacy.

Medical Errors
Medication error – an event in which a patient is harmed by a medication in
some way that could have been prevented. The mistake could be made by
the prescriber, the pharmacy, or during administration. A technician’s job is
crucial to ensuring good patient care.

5 R’s:

1. Right Drug
2. Right Strength
3. Right Route
4. Right Time
5. Right Patient
6. Institute For Safe Medication Practices (ISMP) in connection with the
FDA publishes a list of abbreviations trying to be eliminated from use.
7. Abbreviations can easily be misread and misinterpreted for a variety of
reasons. Dangerous abbreviations need to be curbed in their uses.
8.
 9. Dosage Forms and Routes of Administration
10.Drugs must be administered in a way that allows it to reach the
appropriate site of action in a sufficient amount in order to produce a
desired effect.
11.Dosage form – how the drug is delivered.
12.Systemic effect – effects the body as a whole.
13.Local effect – site of action is a specific area or tissue

Systemic Routes of Administration

Routes of administration – how the drug gets into or onto the body.

• Oral

Oral (peroral or PO) – by mouth. The most convenient and cost-effective

means of delivering a medication to a patient.

Oral dosage forms include: tablets, capsules, and liquid forms (syrups).
Tablets can be coated or uncoated; most are swallowed whole, but some can
be chewed (masticated).

Solution – liquids with dissolved substances.

Suspensions – liquids with particulate matter - must be shaken.

Onset of action with most oral dosage forms is around a half an hour after
swallowing.

Orally dissolving tablets (ODTs) – dissolve quickly on the tongue.

Sublingual – dissolve under the tongue.

Buccal – absorbed in the cheek

• Parenteral Routes
Parenteral route – administered by injection; administered elsewhere in the
body than the mouth and alimentary canal.
Intramuscular (IM) – given directly into a muscle.
- Deltoid – upper arm
- Gluteus medius – buttocks

Intravenous (IV) – injections given directly into a vein.

A small catheter is inserted and left in a vein when repeated or continuous
infusion is needed.

Peripheral IV line – inserted into a vein in the arm, wrist, or hand; small
amounts of fluid; time infused is a few days or less.
Central IV line – inserted into one of the larger veins in the upper chest area
near the clavicle (collarbone); inserted surgically; used when large volumes of
fluid must be given; repeated infusions; time is longer than a few days.

Subcutaneous (SQ or SC or Subq) – injections into the fatty tissue under the
dermal layer of the skin about the muscular tissue.
- Abdomen, upper thigh, back of upper arm

Intrathecal (IT) – injections given into the spinal column between

vertebrae; epidural – injections given via a small catheter to deliver a drug
directly into the spinal column over time; both are administered exclusively
by anesthesiologists or anesthetists.

Intradermal (ID) – injections given just underneath the top layer of skin
(epidermis); used for tuberculosis (TB) skin tests (PPD), local anesthesia, and
allergy skin testing
Rectal
Rectal – drugs inserted via the rectum and allowed to melt or dissolve in
place - allows for systemic absorption through the mucosal lining.

Local treatment for hemorrhoids.

Dosage forms include suppositories and enemas.

Transdermal
Transdermal – drug delivery through the skin over time.

Patches can be applied and left in place for a period of time (hours to days).

Implant
Implants – inserted just below the skin to release a drug slowly over time
(months to years).

Long-term treatments, like birth control, work best for this route.

Topical Routes of Administration

Topical – not for the intent of systemic absorption; limited to local
absorption. Not limited to application on the skin. Lungs, eyes, and vagina,
are some ways that are considered topical administrations.

Click on the tabs to read about topical routes of administration:

Dermal – applied topically to the skin; creams, lotions, gels, ointments,

powders, solutions, and pastes.
• For the treatment of local infections, wounds, sunburns, and rashes.
• Systemic absorption is possible if applied to large areas, in large quantities.
Inhalation – delivery of drugs into the lungs, where a patient breathes it in
through the mouth.

Examples of inhalants: Metered dose inhalers (MDI), dry powder inhalers, and
nebulizers
• Systemic absorption is possible.
• Allows for direct treatment to lung tissues.
• Proper inhalation technique is required for adequate drug delivery and
activity.
Intranasal – drug products sprayed into the nose; available in a liquid dosage
form, delivering the drug to the nasal mucosa.
• Intended for local activity, though some are formulated for systemic
absorption.
• Patients should not forcefully sniff to assist the spray to enter the nose.
• Doing so will cause the drug too far back into the sinuses and down the
throat, missing the intended site of administration.
Intranasal – drug products sprayed into the nose; available in a liquid dosage
form, delivering the drug to the nasal mucosa.
• Intended for local activity, though some are formulated for systemic
absorption.
• Patients should not forcefully sniff to assist the spray to enter the nose.
• Doing so will cause the drug too far back into the sinuses and down the
throat, missing the intended site of administration.
Ophthalmic – drug delivery topically to the eye; eyedrops and eye ointments.
• Limited systemic absorption, but is possible with solutions and ointments.
Otic – delivery of medication into the external ear canal.
• Eardrops are instilled into the ear canal, but the eardrum prevents systemic
absorption.
• Dosage forms include solutions and suspensions.
Vaginal – drug delivery by inserting and applying medication into the vagina.
• Few vaginal products are intended for systemic absorption.
• Dosage forms include creams, gels, solutions, suppositories, ointments, and
tablets.
Atoms and Molecules
Atom – the most basic unit of matter.

Elements – composed of atoms.

Atomic Structure:

Atoms are made up of a nucleus, protons, neutrons, and electrons.

Protons – have a positive electrical charge and determine an element’s

atomic number.

Neutrons – are neutral, and carry no charge (positive or negative).

Electrons – have a negative charge and seek to balance the electrical charge
of an atom.

Ions – atoms or molecules with an electrical charge.

Isotope – same number of protons different number of neutrons; often

radioactive.

Chemical Bonds
Atoms combine by exchanging electrons in the outer shell. Atoms can share
electrons or transfer them completely to another atom.

Covalent bond – sharing electrons; creating a neutrally charge molecule;

strong bond.

Ionic bond – when one element entirely loses electrons and another gains
electrons; remaining connected by electromagnetic attraction; weak bond,
easily broken.

One atom becomes positively charged, the other negative.

Most substances, in the body, are made up of molecules using covalent

bonds.

Molecules and Functional Groups

Molecule – two or more atoms combined via covalent or ionic bonds.

Carbon backbone – chains of carbon atoms strung together or in ring-like

structures.

Functional groups – side portions of a molecule that give it the chemical

properties that allow it to react with others in specific ways.

Molecules react only with those receptors in the body that are shaped
similarly, like a lock and key.

A drug’s activity can be predicted by examining its molecular shape and

functional groups.

Isomers – compounds with the exact same chemical makeup, but arranged
differently in space.

Stereoisomers – isomers of the same molecule that are mirror images of each
other.
 A drug that contains a mixture of stereoisomers can have more drug activity
and/or cause more side effects.

Carbohydrates – common molecule in the body; an essential part of nutrition;

breaking bonds in carbohydrates produces energy; large carbohydrates, like
starches, are used in building cell membranes or stored for energy.

Peptides – composed of amino acids and are the building blocks of protein
molecules.

Proteins are used to build tissues, but can also be used for energy.

Lipids – molecules that form long chains of covalently bonded carbon and
hydrogen atoms; soluble in fat or oil; used to create hormones and other
active biochemical.

Nucleic acids – part of deoxyribonucleic acid (DNA), which forms the genetic
material contained in the cell nucleus.

DNA serves as a road map for the body’s processes and growth cycle.

Acids and Bases

Most drugs are either weak acids or bases; affecting how drug molecules
enter and behave in the body.
pH scale – measuring acidic and basic (alkaline) properties of substances.

 Acids – low pH (below 7).

 Bases – high pH (above 7).

Hydrogen ions – created when an electron orbiting a hydrogen atom is lost,

leaving a lone proton with a positive charge.

Acid molecules donate protons; basic molecules accept protons. Molecules

that have the ability to donate multiple hydrogen ions easily are considered
strong acids; donate few are weak acids. The opposite is true for bases.
When acids and bases come together and exchange protons, remaining
molecules become ionized (positive or negative charge).

Ionization affects drug activity. Ionic molecules cannot easily cross

membranes and enter the bloodstream.
A basic drug in the acidic stomach environment facilitates the exchange of
many protons, creating ionic molecules that are difficult to absorb into the
bloodstream. An acidic drug in the acidic stomach environment, more of the
drug will get absorbed because few molecules will shed protons and most will
remain neutrally charged.
Pharmacodynamics
Drugs work by mimicking, enhancing, or blocking the activity of substances
that are usually already present in the body. Drug molecules interact
with receptors – receives chemical signals – on the surface or inside of
specific cells. Drug receptor theory – based on the lock and key mechanism.

Cells have many different receptor molecules (locks) and various substances
(keys) fit exactly into them.
These “keys” are usually produced or processed within the body –
endogenous chemicals – acting as messengers for communication and
regulating physiological processes. When a messenger molecule connects
with a receptor, it triggers a series of reactions within the cell.

Pharmacodynamics – the study of drug receptor theory at the molecular level

and how that interaction translates to drug activity on the entire body.
Mechanism of action – a drugs effect on the body.
Drugs mimic the molecular shape of the body’s endogenous chemicals and
produce either similar effects or block the activity. Drugs in the same
molecular shape are categorized together because they interact with the
same receptors and have similar activity.

Agonist – drugs whose activity stimulate a specific response when binding to

receptors.
Antagonist – drugs that block a response when binding to receptors.
Antagonists block in two ways:

1. directly by inactivating the receptor, blocking its ability to trigger a

response;
2. binding to the receptor in a competitive fashion, keeping agonist
molecules from binding and then triggering a response.

Dose-response Relationship
In order to be effective, a drug must reach the site of action with a large
enough concentration to produce a measurable effect. The safety of a drug
depends on its ability to reach desired concentrations without producing too
many toxic effects. Proper dosing hinges on achieving the desired effect
without producing unwanted effects.

Dose-response curve – graphically shows the relationship between dose and

its effect. The graph shows concentration of drug in the bloodstream over
time. Showing an increased dose results in an increase response.
Ceiling effect – no further increase in dose produces additional response.

Proper dosing aims for the therapeutic range – where the blood
concentrations are in the middle of the curve.

Minimum therapeutic concentration – the lower threshold of the range.

Dosing must achieve this concentration to at least gain any measurable

effect.

Toxic concentration – the upper edge of the range; the incidence of toxic
effects may outweigh any benefit of the drug and thus pose too great a risk.

Efficacy – produce a desired or intended result.

Potency – power to affect body or mind. A drug that achieves the same
response as another drug but at a lower dose is more potent. Timing of
dosing is very important, when desired is a constant concentration in the
therapeutic range.

Steady state – when constant concentration is maintained.

Loading dose – a dose that is large enough to bring blood concentrations up

to the therapeutic range immediately.

Trough – the point at which a drug is at the lowest concentration.

Peak – when the concentration is at its highest.

Pharmacokinetics
Pharmacokinetics – observing and predicting, using a mathematical model, to
study how a drug enters, moves around, and leaves the body.
Pharmacokinetics studies absorption, distribution, and elimination from the
bloodstream.

The four phases of pharmacokinetics are:

1. Absorption
2. Distribution
3. Metabolism
4. Excretion

Absorption
Absorption – the process by which drugs enter the bloodstream. Absorption
affects the onset of drug action as well as the extent of action. Route of
administration affects absorption by enhancing or limiting systemic effect.
Properties of drugs, acidic or basic, and the environment can affect drug
solubility and absorption.

Transport mechanisms that drugs use to cross membranes can also affect
absorption.

Molecules cross membranes through active and passive transport.

Active transport – use energy to bring drug molecules across the membrane.

An example of active transport is the sodium/potassium exchange

pump, which requires ATP for energy. These proteins use energy to pump
potassium into the cell, and sodium out.

Overall absorption can be limited because active transport are limited by

availability of energy sources, can become saturated, or maxed out.
Passive transport – molecules move across on their own.

Passive transport mechanisms, are usually driven by concentration

gradients – drugs absorbed move from areas of high concentration (site of
administration) to areas of low concentration (bloodstream). Higher doses
produce greater absorption.

Diffusion is a passive transport mechanism where many drugs are absorbed

because molecules move along a concentration gradient. Blood flow and
surface area can affect absorption; surface areas that are large, thin, and
have good blood supply, can easily affect systemic absorption.
Distribution
Distribution – the process by which drugs move around in the bloodstream
and reach other tissues of the body.

Volume of distribution (Vd) – how a drug is distributed within the

compartments of the body.

Highly-water soluble drug stays in the bloodstream.

Highly fat- or lipid-soluble, accumulates in fatty tissue and then slowly

released over time back into the bloodstream – two-compartment model

Protein binding – drug molecules can have a high affinity for protein
molecules; binding to proteins, that circulate in the blood.

Blood-brain barrier (BBB) – a layer of cells that affects distribution of drugs to

the central nervous system (CNS).

Metabolism
 Metabolism – the process in the body by which drugs are converted to other
biochemical compounds, and then excreted through metabolic pathways.

Prodrugs – a compound that on administration and chemical conversion by

metabolic processes becomes an active pharmacological agent.

First-pass effect – the liver metabolizing drugs as they “pass” or travel

through it.

Cytochrome P450 enzyme system – frequently deactivates drugs; liver

enzyme involved in metabolism.

Elimination
Elimination – the process by which drugs leave the body.

• Measured as the rate and extent to which a drug leave the bloodstream

Half-life (t 1/2) – the time it takes half of a drug to be cleared from the blood.

It takes approximately eight half-lives for a drug to be completely eliminated

from the body.

Excretion
Excretion – the process by which drug molecules are removed from the
bloodstream; primarily involving the kidneys.

Excretion can also occur by active or passive mechanisms.

Ionization can affect excretion; ionized drugs cannot easily cross membranes
to exit the bloodstream.

pH of urine can affect ionization and elimination.

Special Populations
Specific characteristics of individuals can affect the pharmacokinetic
properties of the drugs they take.

Influence on pharmacokinetic parameters:

 Females – higher body fat; pregnancy – gastrointestinal motility slows, blood

volume increases, urination increases

 Males – higher metabolism rates

 Cardiovascular disease – blood flow decreases

 Hyperthyroidism – metabolism rate increases in the liver

Age
 The very young and old pose the greatest risks to safe drug therapy.

Pediatric practice – infants and children

 infants being of greatest concern because of body makeup and liver function

 higher body water content, drugs that are highly water-soluble will distribute
well, toxicity is an issue

 good blood circulation

 liver function is not fully mature at birth – affecting absorption, distribution,

and metabolism

Geriatric practice – elderly patients

 Stomach acidity is decreased – higher pH, affecting drugs that need a highly
acidic (low pH) environment for absorption

 Higher body fat content, drugs that are highly fat-soluble may distribute well
and accumulate

 Decreased kidney and liver function, affecting elimination dramatically

 Decreased doses, increased dosing frequency to accommodate altered

absorption, distribution, and elimination

Liver and Kidney Disease

Liver disease – can greatly affect drugs eliminated via metabolism.

 Cirrhosis, hepatitis, and other liver diseases can severely affect liver function.

Kidney function – excretion primarily happens through the kidneys, affecting

elimination.

 Acute and chronic kidney failure make a difference in a drug’s ability to leave
the body.

 Drugs can accumulate and cause toxicity if doses are not adjusted
accordingly.

The key points from this module are:

Pharmacology is the study of how drugs from various sources work inside the
body for their intended purpose.
Pharmaceutics is the study of how drugs are introduced into the body.
Medications are grouped by major drug classes according to their mechanism
of action. Drugs that work in the same way are put into a particular class and
usually given names with a common stem.

Legend or prescription drugs are only available by prescription and are

dispensed from the pharmacy upon receipt of a valid prescription from a
prescriber.
Over-the-counter (OTC) - are medications that can be purchased without a
prescription.
Controlled substances are medications that have been categorized by the
Drug Enforcement Agency (DEA) to have the potential for abuse and
dependence.

A technician's job is crucial to ensuring good patient care. The 5 "R's" of

medication error prevention are:

1. Right Drug
2. Right Strength
3. Right Route
4. Right Time
5. Right Patient

There are many routes of administration including oral, parenteral, rectal,

transdermal, and implant. Topical routes of administration include dermal,
inhalation, intranasal, ophthalmic, otic, and vaginal.

Atoms are the most basic unit of matter and are made up of nucleus, protons,
neutrons, and electrons.

Most drugs are either weak acids or bases (alkaline). The pH scale measures
acidic and basic properties of substances. Acids have a pH level below 7,
while bases have a pH level higher than 7. Acid molecules donate protons;
basic molecules accept protons. When acids and bases come together and
exchange protons, remaining molecules become ionized (positive or negative
charge). Ionization affects drug activity.

Pharmacodynamics – the study of drug receptor theory at the molecular level

and how that interaction translates to drug activity on the entire body.
Pharmacokinetics – observing and predicting, using a mathematical model to
study how a drug enters, moves arounds, and leaves the body. There are four
phases of pharmacokinetics:
1. Absorption – the process by which drugs enter the bloodstream
2. Distribution – the process by which drugs move around in the
bloodstream and reach other tissues of the body.
3. Metabolism – the process in the body by which drugs are converted to
other biochemical compounds, and then excreted through metabolic
pathways.
4. Excretion – the process by which drug molecules are removed from the
bloodstream; primarily involving the bloodstream.
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