Lesson B7 - Pharmacology Flashcards

1
Q
The amphetamines are a class of central nervous system (CNS) stimulant drugs that enhance the 
activity of
A

the brain

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2
Q

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

A

dopamine found in the body

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3
Q

Three common amphetamine

compounds are

A

amphetamine, dextroamphetamine, and methamphetamine.

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4
Q

The amphetamines stimulate both the CNS and the

A

sympathetic nervous system

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5
Q

In the CNS, the amphetamines

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

A

nerve terminals.

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6
Q

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

A

route of administration.

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7
Q

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

A

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.
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8
Q

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

A

inhibits active reuptake of dopamine and norepinephrine in several brain regions

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9
Q

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:

A
  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.
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10
Q

The amphetamines act on the following brain areas:

A
  1. Reticular activating system (RAS).
  2. The medial forebrain bundle (MFB) is stimulated.
  3. Hypothalamus.
  4. Limbic system.
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11
Q

Therapeutic uses of amphetamine-like drugs:

A
  1. Narcolepsy.
  2. Attention-deficit hyperactivity disorder (hyperactive child syndrome)
  3. Parkinson’s disease.
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12
Q

Tolerance develops

rapidly to the

A

euphoria and mood elevating effects (widely abused)

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13
Q

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

A

fatigue.

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14
Q

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

A

abrupt awakening sensation (“rush”)

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15
Q

The abuse liability of the amphetamines is considered to be

A

extremely high

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16
Q

Inherent harmfulness of the amphetamine reside in

A

the long-term toxicities

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17
Q

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

A

the cocoa bush that is indigenous

to Bolivia, Columbia and Peru.

18
Q

Cocaine is classified pharmacologically as a local

A

anesthetic and as a CNS stimulant.

19
Q

In terms of law, cocaine is classified as a

A

narcotic

20
Q

Sigmund Freud studied the CNS effects of cocaine and used it

A

clinically to withdraw a

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

21
Q

Karl Koller introduced cocaine into medicine as a

A

local anesthetic

22
Q

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

A

alcohol, nicotine, caffeine and marijuana.

23
Q

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

A

dose dependent

24
Q

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

A

amphetamines

25
Q

Cocaine inhibits the active re-uptake of released

A

dopamine and norepinephrine into the

presynaptic nerve terminal.

26
Q

The local anesthetic effect of cocaine is due to

A

its blockade of nerve impulse in sensory nerve

fibres.

27
Q

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

A

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.

28
Q

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

A

mouth and throat

29
Q

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

A

urine.

30
Q

Cocaine is a very powerful CNS stimulant that increases

A

alertness, reduces the need for sleep,

and produces an intense feeling of euphoria. The drug is widely abused

31
Q

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

A

crash, manifested as depression,

lethargy and hunger.

32
Q

crash, manifested as depression,

lethargy and hunger.

A

drug-induced psychotic

effect.

33
Q

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

A

withdrawal

syndrome following the cessation of drug use.

34
Q

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

A

compulsive drug use

35
Q

The abuse liability of cocaine is one of the

A

highest among all drugs of abuse

36
Q

The inherent harmfulness of the drug is also among the

A

highest among drugs of abuse

37
Q

Caffeine is the most widely and

A

regularly used drug in the world

38
Q

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

A

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.

39
Q

The actions of caffeine are exerted by competitively blocking

A

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).

40
Q

The abuse liability of caffeine is

A

low