Pharmacology

Basics
Becky Kaufman Lynn, MD, MBA, IF, NCMP
Evora Women’s Health
Adjunct Associate Professor of OBGYN
St. Louis University
Pharmacology

• Basics of Pharmacology
• Pharmacology of Cannabis
 What is
pharmacology?
• Pharmacology is a branch of
medicine
• Concerned with the study of a
drug or medication action
• A drug is any man-made or
natural molecule which exerts
an effect on the cell, tissue,
organ, or organism
Pharmacology

• Pharmacology includes the design

and development of new drugs to
prevent, treat and cure disease.
An understanding of
basic concepts is
important when
determining how much
drug to give someone
and providing
individualized therapy
Definitions
•Cannabis
•Plant with psychoactive properties
•Cannabinoids
•Exogenous
•Endogenous
 Cannabinoids vs. Endocannabinoids

Natural cannabinoids
Chemical compounds
secreted by the cannabis Synthetic cannabinoids
flower Made in a lab
THC and cannabidiol are 2 of Nabilone, dronabinol
the most commonly used
cannabinoids, but there are
many others

Endocannabinoids
Naturally occurring substances in the body
AEA, 2-AG
 Definitions
•Neurotransmitter- substance released by a nerve cell that
goes to another nerve cell and transmits a signal
•Dopamine
•Serotonin- turkey at Thanksgiving makes you tired

•Hormone: substance in the human body that is involved in

(transmitting information between cells)
•Testosterone
•Estrogen
•Oxytocin
Definitions
Receptor: a protein embedded in the cell
membrane that act in cell signaling by
receiving extracellular molecules.

Enzyme: catalyzes a chemical reaction

 Mini Med
School
•Cells are the basic
building blocks of all
living things
•The human body is
composed of trillions of
cells
•They provide structure
and carry out
specialized functions
Pharmacolog
y
•Pharmacodynamics
•Pharmacokinetics
 Pharmacodynamics
•The study of the effects of drugs on
biological systems
•The study of what drugs do to the
body
•Addresses how drugs interact with
cells, and their receptors and
enzymes
 Receptor
A molecule in a cell
membrane, which
responds specifically
to a particular
substance like a
neurotransmitter,
hormone, antigen, or
other substance.
Receptors
•The most common way
drugs exert their effects.
•Drugs interact with specific
receptor proteins present
on the surface of the cell.
•Once the drug binds with
the receptor, it brings about
biochemical changes or
molecular activity that
cause the clinical effect of
the drug.
 Enzymes

•Proteins that act as

biological catalysts.
• Catalysts accelerate
chemical reactions.
•The molecules upon
which enzymes may
act are called
substrates.
•The enzyme converts
the substrates into
different molecules Ex:worm eats an apple core
known as products.
Agonist vs. Antagonist
Pharmacokinetics
•The study of what
biological systems do to
the drug
•Important to know the
pharmacokinetics to
understand the drugs
effects and side effects
Local vs. Systemic
• Local/Topical- the drug is intended to
act on the site of the body at which it is
administered ex; neosporin
• Systemic- the drug acts on a site that is
away from the area of administration.
• Ex: antidepressants
• In the systemic route, the drug needs to
be absorbed into the bloodstream and
then be transported to the area where it
is intended to act.
• Topical drugs can have a systemic effect
Pharmacokinetics

Absorption Metabolism

Distribution Elimination
 Pharmacokinetics
Absorption: The drug enters the bloodstream from the tissue
in which it is was administered.

Distribution the drug leaves the bloodstream and enters the

body tissues. This is the phase in which most drugs exert their
clinical effects. This includes both intended biological effects
and adverse effects.

Metabolism: The body acts on the drug to metabolize it.

Metabolism may either degrade the drug, making it inactive,
or may convert an inactive drug form into its active form.

Elimination: This is the phase where the drug, either in its

original form, or metabolized form, leaves the body
A drug’s
pharmacokinetics
determines how quickly
it takes effect, how
strong the effect is and,
and how long the effect
lasts
 •How the drug
Absorption gets into the
body
•Swallow it
•Rub it on your
skin
•Put it under your
tongue
•Smoke it
•Breathe it
•Put it in the
rectum or vagina
Absorption
•For systemic drugs, you want them to be absorbed
into the blood stream
•You want to put them where there are a lot of blood
vessels
•Rectum
•Vagina
•Buccal
•GI tract
Routes of
Administration
•Some drugs can be given by more than one route.

•The ideal route of administration depends on:

•Properties of the drug
•whether it is predominantly lipid based or water based
•size of the drug particle

•Desired effects of the drug

• local or systemic
•immediate or delayed onset of action- edible vs. smoking
Bioavailability
• The proportion of a drug that is absorbed into the bloodstream

• Only the bioavailable drug is available for clinical effect, the rest is
excreted (urine, feces) without absorption

• Drugs that are IV are 100% bioavailable

• Oral route has decreased bioavailability

• Example: edibles have low bioavailability due to breakdown by

digestive enzymes and stomach acid and metabolism into other
compounds by the liver
 Factors that affect
bioavailabilty (oral route)
First pass metabolism:
After a drug is absorbed through the stomach or intestine, it
goes directly to the liver and may be metabolized – changed to a
different form

Resistance to digestive enzymes:

Some drugs may not survive degradation by digestive enzymes
which limits their availability

Solubility of the drug:

a drug that is highly lipid soluble may find it difficult to gain
access to the cell surface. At the same time a highly water soluble
drug can’t permeate the phospholipid bilayer.
Distribution Drug leaves the
bloodstream and
enters the
extracellular fluids
and tissues

Cell
Fluid around the cell

Bloodstream
Factors affecting
distribution
•How many blood vessels are
in the tissues
•How “leaky” the blood
vessels are
•Binding of drug to plasma
protein
•Binding of the drug to tissue
protein
•Lipid solubility
Metabolism

•Converts an
active drug
to a form
that is easier
to eliminate
•Or change
the drug into
its active
form
Metabolism
•11-Hydroxy-
Δ9-tetrahydrocannabinol (11-OH-THC),
usually referred to as 11-hydroxy-THC,
is the main active metabolite of THC

•Cannabis
contains tetrahydrocannabinolic
acid (THCA), which is converted
into THC after heating and
then metabolized by the body into
11-hydroxy-THC and then
into 11-nor-9-carboxy-THC
 Cytochrome p450
•Drugs can be inhibitors or inducers
of enzymes.
•An inducing agent can increase the
rate of another drug's metabolism
•Dose may need to be adjusted
•If a medication is taken with an
agent that inhibits its metabolism,
then the drug level can rise and
possibly result in a harmful or
adverse effect.

•Give example of inducers and

inhibitors
Elimination/
excretion
•After metabolism the drug is
eliminated
•Elimination occurs through
the kidney, feces, air, sweat,
saliva and tears
Drug Half Life
• The unit of time in which the plasma drug
concentration decreases by 50%
• Affected by diminished kidney or hepatic
blood flow, diminished kidney or liver
function
• These can increase the half life and
prolong drug action.
Pharmacokinetics in
a graph form
Questions?