Principles of

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

 NT fits receptor site

key & lock
 Change structure of drug...
change its affinity
increase or decrease
may bind to different receptor
 Behavior mediated by synaptic activity
 Drug Classification

 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

 chemical  dl-2 amino-1

phenylpropane

 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

sec min hr hrs

Time