Transcript Cocaine and Amphetamines

Chapter 4
The Major Stimulants:
Cocaine and Amphetamines
The History of Cocaine
Derived from coca leaves grown in the
mountainous regions of South America.
Late nineteenth century
cocaine was a common ingredient in
patent medicines
beverages (e.g., pre-1903 formula for Coca-Cola)
The History of Cocaine
Sigmund Freud
promoted cocaine
cure for morphine dependence and
depression
lost enthusiasm as he recognized the
addictive potential of cocaine
Acute Effects of Cocaine
powerful burst of energy
sense of well-being
confidence
elevated sympathetic activity
activates dopamine “reward” pathway
Chronic Effects of Cocaine
Schizophrenic-like symptoms
hallucinations
mood disorders, deep depression
physical deterioration of nasal membranes if
used intranasally.
Medical Uses of Cocaine
The only current medical use of cocaine is
as a local anesthetic.
Produces anesthesia by blocking Na+ ion
channels, thus blocking axon conduction
similar to novocaine, procaine, lidocaine
How Cocaine Works
in the Nervous System
Catecholamine agonist
blocks the reuptake of dopamine (DA) and
norepinephrine (NE)
DA pathways are part of the brain’s reward systems
NE pathways are important for arousal
Activation of reward pathways makes cocaine
particularly subject to abuse
Sympathomimetic (NE) effects can result in heart
attacks
Present-Day Cocaine Abuse
1970s-1980s
cocaine was chic
used by the beautiful, rich and powerful
(and those who aspired to be!)
symbol of status and success
in short term, increased productivity
increased alertness, confidence and energy
also powerful appetite suppressant
thin is beautiful!
1990s
cocaine fell out of favor among rich and powerful
consequences of long-term use became apparent
deaths, public battles with addiction by stars
Present-Day Cocaine Abuse
1980s to present
smokable forms of cocaine
produced faster more intense high
free-base
required treatment of cocaine with ether by the user
very flammable, dangerous to use
crack
treated with baking soda and much safer to make
purchased in ready-to smoke rocks
cheap “hits”
very addictive
affordable to all social strata
a social problem, especially among poor
Figure 4.1
cocaine HCl,
a salt
remove HCl
with ether
treat with
baking soda
Crack cocaine is
A. more dangerous to make than free-base
cocaine.
B. the least addictive form of cocaine
C. usually used by crushing and dissolving for
injection.
D. attractive to users for its relatively cheap “hit.”
E. called “crack” cocaine because of its rectal
route of administration.
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Inc. All rights reserved.
Figure 4.2
Cocaine + Alcohol
One of the most commonly used drug combinations
cocaine is normally metabolized into inactive metabolites,
BUT
In presence of ethanol, much of cocaine is metabolized
to cocaethylene, which is itself psychoactive
acts much like cocaine
longer half-life
more potent re-uptake blocker
also presents greater cardiovascular risk
“crack babies” are most often cocaine + alcohol babies
Treatment for Cocaine Abuse
Pharmacological intervention
Withdrawal symptoms are severe
depression, headaches, irritability,
sleep disturbances
anxiolytics (e.g. Valium) or antidepressants may
be given symptomatically
gamma-vinyl GABA (GVG)
acts on GABA systems, indirectly reduces levels
of dopamine in the nucleus accumbens, an important
structure in reward systems
reduces reinforcing effects of cocaine
Treatment for Cocaine Abuse
Treatment
inpatient programs,
outpatient programs, or a
combination of the two
inpatient followed by outpatient,
which is usually individual or group
counseling
12-step programs
cognitive-behavioral therapy
Effective treatment programs for cocaine addiction include
all but
A.
B.
C.
D.
E.
medically supervised detoxification.
tough love, showing the addict no empathy.
pharmacological treatment.
self-help groups with other addicts.
relearning life management skills without drugs.
Figure 4.3
Percent of patients with four consecutive weeks
of abstinence
Amphetamines
Earliest known use
Chinese medicinal herb
used for thousands of years as a bronchial dilator
1887
ephedrine isolated as the active ingredient
1927
amphetamine (Benzedrine®) was developed as
a synthetic form of ephedrine
1930s
d-amphetamine and methamphetamine
became available worldwide
Acute and Chronic Effects of
Amphetamines
Amphetamines’ effects are similar, but not
identical, to those of cocaine
Stimulate CA release, block reuptake
Acute effects
general arousal
antidepressant
appetite suppressant
keeps people awake for long periods of time.
Figure 4.4
Acute and Chronic Effects of
Amphetamines
Chronic effects may include
paranoia
delusions
hallucinations
violent behaviors
amphetamine psychosis
e.g. bizarre behaviors of the “speed freak”
Table 4.2
Present-Day Patterns of
Methamphetamine Abuse
amphetamine abuse during the 1980s, was largely
overlooked because of preoccupation with cocaine
use/abuse
the emergence of methamphetamine as a drug abuse
problem refocused attention on amphetamines
largely rural
treatment for methamphetamine abuse is similar to
that for cocaine abuse
Medical Uses for Stimulants
Attention Deficit Hyperactivity Disorder
(ADHD)
methylphenidate (Ritalin®)
DA reuptake blocker
atomoxetine (Strattera®)
NE reuptake blocker
d-l amphetamine (3d:1l; Adderall®)
stimulates release
blocks reuptake of CAs
5-HT receptor agonist
Medical Uses for Stimulants
Other medical applications
narcolepsy
nasal congestion (e.g. pseudoephedrine)
Abuse potential:
recreational use
prevent sleep, increase alertness
135 mg
Ampheta-HCl
125 mg
100 mg
RX is Available Only Through Physicians
Replacement for Phentermine / Phendimetrazine / Adipex
Most Powerful PhenTabz Formulation Available
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ANONYMOUS POLL
A = Yes, B = No
Have you ever used Adderall (other than as prescribed)?
Are you familiar with ADDTabz?
Would you try ADDTabz?
Do you know what Ampheta-CDP is?
Being pushed on campuses (including UF’s) as an alternative to
Adderall. Emphasis is as a study aid, not as an alternative
treatment for ADHD.
Ampheta-CDP not listed in any database as a drug.
Unregulated. Not sold as a drug, but as a food supplement.
Effectiveness unclear. No controlled clinical trials, only
testimonials.
(Gentech is a Ft. Myers based
pharmaceutical company.)