Basic Pharmacology

What is a drug?
- any chemical agent which
effects any biological process

What is pharmacology ?
- the

study of how drugs

effect biological systems

Introduction

A. Physical Nature of Drugs

Solid drugs -> oral route
aspirin or atropine
Liquid drugs -> oral route, IM, SC
nicotine or ethanol
Gaseous drugs -> inhalation
nitrous oxide, halothane, amylnitrite

Many drugs are weak acids or bases

pH differences in the body may alter the degree of ionization of
drug

What is Pharmacology ?
Pharmacokinetics

Pharmacodynamics

What the body does to drug

What the drug does to body

Pharmacology
Pharmacotherapeutics
The study of the use of drugs

Pharmacocognosy
Identifying crude materials as drugs

Toxicology

Pharmacokinetics
What the body does to
the drug
- Absorption
- Distribution
- Metabolism
(Biotransformation)
Half-life (t1/2)
- Excretion

- the time required for the plasma

concentration of a drug to be

Pharmacodynamics
What the drug does to the
body
- Drug receptors
- Effects of drug
- Responses to drugs
- Toxicity and adverse effects
of drugs

Sources of Drugs
Pharmacocognosy

Animals
Plants
Minerals
Synthetic
Microbes

Many of these old sources are

still in use today
Foxglove

plant

Meadow

flower
Colchicum autumnale

Beef

or pork pancreas

Digitalis

comes from the

foxglove plant and is used in
the treatment of CHF

Colchicine

is the drug of
choice for treatment of gout

Insulin

is used today to treat

diabetes and is derived from
the pancreas of beef or pork or
may be synthetically produced
as well.

Drugs Derived from Plants

Ephedrine

is present in the leaves of a bushy

shrub (species name Ephedra), which, when
burned were used by the ancient Chinese to treat
respiratory ailments. Today, it is a bronchodilator.
Many estrogen hormone replacement therapy
drugs are derived from yams.
The belladonna plant source of atropine, which is
still used to dilate the pupils.

DRUGCLASSIFICATION
- Based on the chemical structure

Basedonthemaineffect(e.g.
analgesics).
Basedonthetherapeuticuse(e.g.
antipsychotic).
Basedonmechanismofaction(e.g.
serotoninagonist).

Drug Nomenclature

micalname*GenericnameTrade
Chemical Name: 2-(4-isobutylphenyl)-propionic acid
Generic Name: ibuprofen
Trade Names: Advil, Aches-N-Pain, Brufen,
Emodin, Haltran, Medipren,
Midol 200, Motrin, Nuprin,
Rufen, Trendar, Wal-Profen
*preclinical nomenclature =

company abbrev-123456 (e.g. WAY-100635, MK-869)

Routes of Administration

Critical to efficacy
Rapidity

of onset
Duration of effects
Magnitude of effects

Systemic administration
Drug

into circulatory system via ...

Enteral routes
Parenteral routes
Drug effects throughout body ~

Routes of Drug
Administration
Enteral
within

Oral (PO), rectal, sublingual

Parenteral
Not

or by way of the GI tract

within the alimentary canal

Inhalation, IM, SC, IP, topical

Central
Into the brain or spinal cord
Intrathecal, ICV

Routes of Drug Administration

common abbreviations
PO = per os = oral
IV = intravenous = into the vein
IM = intramuscular = into the muscle
SC = subcutaneous = between the skin and muscle
IP = intraperitoneal = within the peritoneal cavity
icv = intracerebroventricular =
directly into the ventricle of the brain

Oral

Per Os (PO)

by mouth

absorption

across
membrane in GI
most common
most variable
1st pass metabolism

Cooperation required
Can recall ~

Oral

Sublingual
Absorption:

mucous membrane
salivary glands

e.g.,

nitroglycerin,
buprenorphine

Chewing
absorbed

mouth ~

across lining of

Injection

Intravenous (iv)
directly

into vein
rapid onset of effects

Fastest ~ Intramuscular (im)

Location important
Deltoid

- rapid
Thigh - moderate
Buttocks - slowest
Difference in blood

supply & distance

Routes of Drug Administration and Absorption.

Injecting
(Intravenous):
Puts

drugs directly
into a vein

Put

drugs into
muscles or under
skin

Intravenous (IV)
Intramuscular (IM)
Subcutaneous

15 30 seconds
3 5 minutes
3 5 minutes

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Inc.

Injection

Subcutaneous (sc)
under

skin
slow, steady absorption

Disadvantages
Variable

absorption
limited volume
skin irritations ~

Injection

Intrathecal
under

sheath of nerve fibers,

cord, or brain

spinal

Mostly as local anesthesia

little

importance for most psychoactive drugs

Inhalation
Smoking
Lungs

gases

or vapors
densely lined with capillaries
large surface area

Fast absorption
Similar

to iv ~

Routes of Drug Administration and Absorption.

Inhaling:
Allows

the vaporized
drug to enter the
lungs, the heart and
then the brain in about
7-10 seconds (Most
rapid)

Inhaling: 7 to 10 seconds
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Inc.

(Pictures)
Marijuana inhaling tent used
by the Scythians, c. 500 B.C.
Man in India smokes ganja
(marijuana) in a chillum
pipe.
Copyright, 2004, CNS Productions,
Inc.

Other routes

Transdermal patches
absorbed

by skin
slow continuous release

also liposomes: via injection

Suppositories - rectal or vaginal

absorption

incomplete & unpredictable

Pellets - Norplant
Microcatheter & pump ~

Routes of Drug Administration and

Absorption
Contact or Transdermal
Absorption
Absorption through the
skin is the slowest
method of drug use. It
often takes 12 days
for effects to begin and
the absorption can
continue for about 7
days. Nicotine,
fentanyl, and heart
medications can also
be absorbed this way
Skin creams & ointments
absorbed through skin

Contact or
Transdermal:
1 to 2 days
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Inc.

Toxicity
Toxicity is the ability of a chemical to
damage an organ system, to disrupt a
biochemical process, or to disturb an
enzyme system.

Drug Formulation
Dosage = the amount of drug to be administered
usually based on weight
Example: mg/kg

Concentration = how the drug is formulated

Example: mg/ml

Injection Volume = a liquid measurement

based on weight
Example: ml/kg

Factors Affecting Response to Drugs

Dosage
Route of Administration
IV IH

subling

IM, SC

IP

PO

topical

Rate of Absorption
Rate of Elimination
Physiochemical properties of the drug
age, sex, species, metabolism, etc

Drug-Receptor Interactions

Agonists
activates or enhances
cellular activity.
triggers a series of
biochemical events
alteration in function
second messengers:
biochemicals that
initiate these changes

Antagonists
do not initiate a change
in cellular function.
prevent the binding and
the action of agonists
blockers

Drug-Receptor Interactions
Factors Governing Drug Action

1. Affinity: measure of the tightness that a

drug binds to the receptor

2. Intrinsic activity: measure of the ability of

a drug to generate an effect, producing a
change in cellular activity

Binding of a drug

drug must interact with complementary

surfaces on the receptor.

Antagonist

exhibit affinity for the receptor

do not have intrinsic activity at the receptor
competitive antagonist: binds to the receptor
in a reversible mass-action manner
-agonists given in high concentrations can
displace the antagonist from the receptor
-agonist can then produce its effect