PHAR 100: 2.2 Amphetamines & Cocaine
Exam Questions and Answers
Amphetamines and cocaine are: - Answers -two classes of colon CNS stimulant drugs
that have a history of being Misused.
Amphetamines are drugs of widespread misuse and are ____ in Canada: - Answers -
controlled substances
Controlled Substances: - Answers -This means that their use is restricted to certain
medical conditions.
Amphetamines class includes: - Answers -amphetamine, dextroamphetamine,
methamphetamine.
Amphetamine-related compounds include: - Answers -methylphenidate (Ritalin) which is
used to treat ADHD; MDMA (ecstasy): a Derivative of methamphetamine that is often
misused. It fosters the feeling of intimacy and empathy, while improving intellectual
capacities. It is neurotoxic, causing neuronal damage and death. This effect is long
lasting, if not permanent.
Chemistry of amphetamines: - Answers -Amphetamines are synthetic organic
compounds. They are structurally similar to the endogenous neurotransmitters
norepinephrine and dopamine. They can be synthesized readily, resulting in the illicit
manufacturing of these substances, especially methamphetamine. The purity of these
illicit substances is variable, and may contain side products of the chemical reaction,
unreacted chemicals, and cutting or filler agents which can be dangerous.
The mechanism of action of ecstasy is similar to the amphetamines, but: - Answers -it
has a preferential effect on the serotonin-containing neurons, and causes release of
serotonin.
The overall effect of the amphetamines is quite standard. In that they increase excitation
by - Answers -increasing the amount of dopamine or norepinephrine in the synaptic
cleft.
Amphetamines are substrates for - Answers -the dopamine transporter.
Dopamine transporter - Answers -the transporter that clears dopamine out of the
synaptic cleft after neurotransmission.
, Amphetamines compete with dopamine for the dopamine transporter. And the result is
that - Answers -amphetamines end up in the presynaptic nerve.
Once in the nerve, amphetamines block - Answers -the vesicular monoamine
transporter.
The vesicular monoamine transporter is responsible for - Answers -bringing dopamine
into vesicles to be packaged for release when the next nerve impulse arrives.
Since with amphetamines, dopamine is blocked from being packaged into vesicles,
there is a large increase in the concentration of free dopamine in the neuron. This large
concentration of dopamine in the neuron forces the dopamine to - Answers -travel
through the dopamine transporter in the reverse direction. Meaning back out into the
synaptic cleft.
The result of an increase of dopamine in the synaptic cleft is - Answers -an increase in
C N S excitation.
Amphetamines have four main effects within the C N S. These effects include: -
Answers -A decreased threshold for transmitting sensory input to the cerebral cortex,
leading to C N S excitation; A feeling of euphoria and reward; Temperature-regulation
and feeding centre modifications leading to appetite suppression; An increase in
aggressive behaviour and mood swings.
The common amphetamines differ in the magnitude of - Answers -their C N S effects.
What effects do you anticipate will be associated with increased C N S excitation? -
Answers -Increased C N S excitation will lead to increased alertness, a feeling of power,
reduced fatigue, and increased responsiveness. It will also result in increased heart rate
and blood pressure
In addition to C N S effects, amphetamine use has different effects depending on -
Answers -the duration of use and whether it is used concurrently with other drugs.
Short-term effects of amphetamine use in non-C N S tissues may include - Answers -
Chest pain (i.e., angina) or heart attack; Cardiovascular collapse; Increased respiratory
rate
Overdose may result in - Answers -a seizure, high fever, or stroke.
Long-term effects of amphetamine use include: Chronic sleeping problems; Poor
appetite; Anxiety, repetitive behaviour, psychoses, aggressive behaviour; Elevated
blood pressure and abnormal cardiac rhythm - Answers -
Other drugs may be sought concurrently with amphetamines in an attempt to - Answers
-antagonize various toxic effects of the amphetamines.
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