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Principles of Pharmacology
Principles of Pharmacology
Principles of Pharmacology
Pharmacology:
Part 1
Lecture 8
Definitions
Drug
Biologically Active
Alters cell structure/function
chemically
Exclude
Natural Foods/Water
Psychoactive Drugs
Alters function of nervous system
Consciousness
Arousal
Emotions
Affect
Perceptions
Information Processing
Definitions
Pharmacodynamics
what the drug does to the body
drug action/effect
Pharmacokinetics
what the body does to the drug
metabolism
Definitions
Drug Action
interaction of drug molecule w/
biological tissue
Mechanism of action
specific drug action
morphine binding to opioid receptors
Drug effect
behavioral effects
may know effect but not mechanism
Structure-activity relationship
Several schemes
use depends on goals
Not easy to classify
each drug wide range of properties
Psychophramacology:
Behavioral & Therapeutic
Classification Problems
Alcohol effects
General nervous system depressant
Effects depend on dose
Lo dose --->behavioral excitation
Hi dose ---> behavioral inhibition
What are the effects of alcohol?
It depends!
Another Example
Attention Deficit Hyperactive Disorder
hyperkinesis
Treatment: Ritalin
Classify Ritalin as a sedative?
Generic name: Methylphenidate
a stimulant
No Magic Bullets!
Drug delivered into system
Effects all cells that have receptors
Desired effect
= therapeutic effect
All other effects
= side effects
All drugs have multiple effects
No magic bullets
What are a drug’s effects?
It depends
Many sources of variability
A focus of this course
Deciding to use a drug
weigh benefits vs. risks
there are always risks
Drug Names
At least 3 names
Chemical name
describes molecular structure
Generic name
official legal name
Trade name
brand name
Street name
Example: Amphetamine
dl-amphetamine
generic
Benzedrine
trade
speed, bennies,
street whites, etc.
Drug Equivalence
Important to know when prescribing
Chemical equivalence
identical chemical compounds
Biological equivalence
affect the same systems in same way
Clinical equivalence
same behavioral effect
different molecules affecting different systems
Drug Administration
& Distribution
How To Get From Here To
There?
Drug Here
Target----------------->There
Complex Journey
Routes of Administration
Critical to efficacy
Drug into circulatory system
Crosses membranes
Goes wherever blood takes it
Crosses membranes
Drug effects throughout body
Oral
Per Os (PO)
by mouth
absorption across
membrane in GI
most common
most variable
Oral
Sublingual
under tongue
absorbed across
mucous
membrane
salivary glands
e.g., nitroglycerin
Oral
Chewing
absorbed across
lining of mouth
Injection
Intravenous (IV)
directly into vein
rapid onset of fx
Fastest
Injection
Intramuscular (IM)
Location important
Deltoid - rapid
distribution
Gluteus maximus -
slower
Differnence in blood
supply
Injection
Intrapertoneal (IP)
into peritoneal cavity of abdomen
Can deliver large amounts
Not used in humans much
Danger of infection
Injection
Intrathecal
under sheath of nerve fibers,
spinal cord, or brain
Mostly as local anesthesia
little importance for psychoactive
drugs
Injection
Intracranial (IC)
directly into brain
direct access to cells
intraventricular - into CSF
Effects in brain can differ from
peripheral fx
Inhalation
Smoking
Lungs
gases or vapors
densely lined with
capillaries
large surface area
Fast absorption
Similar to IV
Intranasal
Particles of drug
insufflation = sniffed
Absorption across mucous
membrane of nose
Not in lungs!
Slower absorption
FX not as strong as
inhalation
Other routes
Transdermal patches
absorbed thru skin
slow continuous release
Researching an injection that will also
Suppositories - rectal or vaginal
absorption incomplete & unpredictable
Pellets - Norplant
Microcatheter & pump
The Future: Part 1
Polymer-to-gel
drug + water + biodegradeable polymer
45 C: liquid & injectable
37 C: solidified gel capsule
70% of drug released over 12 days ~
The Future: Part 2
Injections without NEEDLES!?
only some drugs enter via patch
e.g. nicotine, scopolamine
VLF - very low frequency sound
disrupts lipid layer of skin
more room for molecules to enter
insulin, interferon gamma, etc
works in rats & cadavers ~
Choice of route
Consider factors
Concentration in blood
Rapidity of onset
Duration of effects
Magnitude of effects
Amount delivered
Patient characteristics
Blood
Level
Time