Lesson B7 - Pharmacology

Question 1

The amphetamines are a class of central nervous system (CNS) stimulant drugs that enhance the 
activity of

Answer 1

the brain

Question 2

The amphetamines are synthetic organic compounds that are structurally similar to
norepinephrine, epinephrine and

Answer 2

dopamine found in the body

Question 3

Three common amphetamine

compounds are

Answer 3

amphetamine, dextroamphetamine, and methamphetamine.

Question 4

The amphetamines stimulate both the CNS and the

Answer 4

sympathetic nervous system

Question 5

In the CNS, the amphetamines

act primarily by releasing the neurotransmitters, norepinephrine and dopamine, from

Answer 5

nerve terminals.

Question 6

The effects produced by amphetamines depend on the drug dose and the

Answer 6

route of administration.

Question 7

CVS (Cardiovascular System) effects of amphetamine are due to drug-induced displacement
of

Answer 7

norepinephrine from adrenergic nerve terminals, which then acts on postsynaptic α
(vasculature) and β1 (heart) receptors. The effects include:

1. Fight-flight response.
2. Increased blood pressure.
3. Increased heart rate.

Question 8

CNS effects of amphetamine are mediated by the actions of catecholamines in the CNS,
whereby amphetamine primarily increases release (by displacement) and also

Answer 8

inhibits active reuptake of dopamine and norepinephrine in several brain regions

Question 9

The CNS stimulation is dose-dependent, with
low doses primarily affecting the cerebral cortex and high doses affecting the entire
cerebrospinal axis, and can manifest as:

Answer 9

1. Behavioural and psychomotor stimulation (alertness, hyperactivity, insomnia).
2. Anorexia (reduction in appetite).
3. Hyperthermia (increase in body temperature).
4. Respiratory centre stimulation.
5. Neurotransmission in spinal cord.
6. Convulsions, with high doses.

Question 10

The amphetamines act on the following brain areas:

Answer 10

1. Reticular activating system (RAS).
2. The medial forebrain bundle (MFB) is stimulated.
3. Hypothalamus.
4. Limbic system.

Question 11

Therapeutic uses of amphetamine-like drugs:

Answer 11

1. Narcolepsy.
2. Attention-deficit hyperactivity disorder (hyperactive child syndrome)
3. Parkinson’s disease.

Question 12

Tolerance develops

rapidly to the

Answer 12

euphoria and mood elevating effects (widely abused)

Question 13

Cessation of administration of the amphetamines results in mood depression that may be
profound, prolonged sleep, huge appetite, lassitude and

Answer 13

fatigue.

Question 14

Amphetamines usually are self-administered to produce pleasurable effects, including euphoria
and an

Answer 14

abrupt awakening sensation (“rush”)

Question 15

The abuse liability of the amphetamines is considered to be

Answer 15

extremely high

Question 16

Inherent harmfulness of the amphetamine reside in

Answer 16

the long-term toxicities

Question 17

Cocaine is a naturally-occurring alkaloid found in the leaves of

Answer 17

the cocoa bush that is indigenous

to Bolivia, Columbia and Peru.

Question 18

Cocaine is classified pharmacologically as a local

Answer 18

anesthetic and as a CNS stimulant.

Question 19

In terms of law, cocaine is classified as a

Answer 19

narcotic

Question 20

Sigmund Freud studied the CNS effects of cocaine and used it

Answer 20

clinically to withdraw a

colleague from morphine, which then led to dependence on cocaine.

Question 21

Karl Koller introduced cocaine into medicine as a

Answer 21

local anesthetic

Question 22

Currently cocaine is one of the most popular recreational drugs, next to

Answer 22

alcohol, nicotine, caffeine and marijuana.

Question 23

CNS effects are due to generalized CNS stimulation produced by cocaine and are

Answer 23

dose dependent

Question 24

In general, the behavioural effects of cocaine are very similar to those produced by
the

Answer 24

amphetamines

Question 25

Cocaine inhibits the active re-uptake of released

Answer 25

dopamine and norepinephrine into the | presynaptic nerve terminal.

Question 26

The local anesthetic effect of cocaine is due to

Answer 26

its blockade of nerve impulse in sensory nerve | fibres.

Question 27

Cocaine is almost indistinguishable from amphetamine in its acute effects and its pattern of toxicity. The main differences are:

Answer 27

Shorter duration of action for cocaine. ∙ Lower incidence of complications associated with intravenous use as cocaine is usually sniffed or smoked. ∙ Tolerance does not develop as readily to the hallucinatory and behavioural effects of cocaine as compared to the amphetamines.

Question 28

The only legitimate use of cocaine is as a local anesthetic for the

Answer 28

mouth and throat

Question 29

Cocaine is metabolized to an inactive metabolite benzoylecgonine which is excreted in the

Answer 29

urine.

Question 30

Cocaine is a very powerful CNS stimulant that increases

Answer 30

alertness, reduces the need for sleep, | and produces an intense feeling of euphoria. The drug is widely abused

Question 31

Heavy cocaine users may take the drug repeatedly over several hours to days. The attempt is to maintain the euphoric experience. The binge is followed by a

Answer 31

crash, manifested as depression, | lethargy and hunger.

Question 32

crash, manifested as depression, | lethargy and hunger.

Answer 32

drug-induced psychotic | effect.

Question 33

Physical dependence on cocaine has been demonstrated by the appearance of a

Answer 33

withdrawal | syndrome following the cessation of drug use.

Question 34

Psychological dependence on cocaine can occur. The pharmacodynamic characteristics of smoking “crack” (rapid onset and short duration of behavioural effects) are almost “ideal” for the development of

Answer 34

compulsive drug use

Question 35

The abuse liability of cocaine is one of the

Answer 35

highest among all drugs of abuse

Question 36

The inherent harmfulness of the drug is also among the

Answer 36

highest among drugs of abuse

Question 37

Caffeine is the most widely and

Answer 37

regularly used drug in the world

Question 38

The CNS effects of caffeine involve several areas of the brain. In the cerebral cortex, caffeine increases

Answer 38

mental performance and decreases drowsiness and fatigue, motor coordination . In the medulla, the respiratory and vasomotor centres are stimulated, leading to increased respiration and heart rate.

Question 39

The actions of caffeine are exerted by competitively blocking

Answer 39

adenosine receptors in the brain. Adenosine exerts an inhibitory effect on a number of neurons and transmitter systems. When caffeine blocks these adenosine receptors, the neurons are released from the adenosine inhibition and the neuronal activity is increased (stimulation).

Question 40

The abuse liability of caffeine is

Answer 40

low