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PED1003-Pharmacology > PED1003/L17 Drugs of Abuse > Flashcards

PED1003/L17 Drugs of Abuse Flashcards

1
Q

Give 3 examples of commonly abused drugs.

A

Nicotine
Opiates
Alcohol
Cannabis
Cocaine
Amphetamines
Ketamine

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2
Q

Why do people continue to abuse drugs? (2)

A

Satisfy cravings (psychological withdrawal)
Avoid unpleasant physical sensations (physical withdrawal)

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3
Q

Describe the reward pathway. (5)

A

DA neurones with cell bodies in VTA project to n. accumbens (ventral striatum)
Activation of neurones releases DA
Acts on inhibitory D2 receptors
Inhibits n. accumbens neurones
Elicits reward pathway

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4
Q

What is the primary target of amphetamines?

A

Plasma membrane transporters

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5
Q

Which amphetamine has affinity for DAT and NAT?

A

d-Amphetamine

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6
Q

Which amphetamine has highest affinity for DAT?

A

Metamphetamine

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7
Q

Which amphetamine has affinity for DAT, NAT and SERT?

A

Ecstasy

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8
Q

What occurs when amphetamines enter the neurone? (5)

A

Amphetamine enters nerve terminal via plasma membrane transporter
Transported into vesicles by VMAT2
Release of stored neurotransmitter into cytosol
Membrane transporter reverses to release NTM into synaptic cleft
Reuptake of released NTM blocked

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9
Q

What symptoms are caused by DA transporters? (3)

A

High impulsivity
Psychosis
Stereotyped behaviours

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10
Q

What symptoms are caused by NA transporters? (2)

A

Locomotor activation
Alertness

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11
Q

What symptoms are caused by the 5-HT transporter? (2)

A

Empathogenic
Anorectic

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12
Q

Explain briefly how amphetamines activate the reward pathway. (2)

A

Increase DA release and increase stimulation of D2 receptors in n. accumbens
DA neurones inhibit n. accumbens neurones

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13
Q

Describe the psychological and physical dependence of amphetamines. (2)

A

Cause psychological dependence (craving)
No physical dependence or withdrawal

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14
Q

What is the mechanism by which cocaine works?

A

Blocks DA transporter

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15
Q

Describe the mechanism of action of cocaine. (3)

A

Binds to DAT plasma membrane transporter
Reuptake of released DA blocked
Level/duration of DA in synaptic cleft increased

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16
Q

Give 3 exogenous opioids.

A

Codeine
Pethidine
Morphine
Diamorphine (heroin)
Fentanyl

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17
Q

Give 3 endogenous opioids.

A

Enkephalins
Dynorphins
B-endorphin

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18
Q

How do opioids act?

A

Through G-protein coupled receptors

19
Q

What do mew receptors in n. accumbens (ventral striatum) mediate?

A

Euphoria

20
Q

What do mew receptors in spinal cord mediate?

A

Analgesia

21
Q

What do mew receptors in the gut mediate?

A

Reduced motility

22
Q

What do mew receptors in the brainstem mediate?

A

Respiratory depression

23
Q

What do the effects of opioids depend on? (2)

A

Relative affinity for mew, delta and kappa receptors
Route of administration into CNS

24
Q

Define tolerance and explain why it occurs.

A

A state in which response to given concentration of drug is reduced
Due to receptor adaptation - down regulation of mew receptors

25
Q

Explain how opioids activate the reward pathway. (3)

A

Activate mew receptors decrease GABA release
DA neurones are desinhibited and fire more AP
INhibit n. accumbens neurones directly

26
Q

How can the effects of opioids be reversed?

A

Mew receptor antagonists
E.g., naloxone

27
Q

What kind of drug is ketamine?

A

NMDA receptor antagonist

28
Q

What are the effects of glutamate mediated by? (2)

A

Excitatory ligand gated ion channel receptors
G-protein linked receptors

29
Q

Describe the structure of the glutamate NMDA receptor.

A

Tetrameric structure
Dimers of GluN1 and GluN2(A-D), GluN3

29
Q

How does ketamine activate the reward pathway?

A

Blocks NMDA receptors
Reduces firing of n. accumbens neurones

30
Q

What kind of drug is nicotine?

A

ACh receptor (nAChR) agonist

31
Q

Give 3 cholinergic systems in the brain.

A

Medial septal n.
Diagonal band of Broca
N. Basalis Meynert
Laterodorsal tegmentum
Pedunculopontine tegmentum

32
Q

What kind of receptor are nicotinic receptors? (2)

A

Ligand-gated ion channel receptors
Pentameric

33
Q

Which nicotinic receptors are responsible for reinforcing effects of nicotine? (3)

A

A4B2
A6B2
Both on DA cell bodies of VTA

34
Q

How does nicotine activate the reward pathway?

A

Activates DA neurones directly and indirectly via Glu inputs

35
Q

Describe the psychological and physical dependence of nicotine. (2)

A

Can cause psychological dependence (cravings)
Does not cause physical dependence

36
Q

What is cannabis converted into in the body?

A

From Delta(9)THC to 11-hydroxyTHC

37
Q

Which receptors does cannabis interact with in the body?

A

G-protein coupled receptors CB1 and CB2

38
Q

What is the endogenous agonist ligand (endocannabinoid) of cannabinoid receptors?

A

Anandamide

39
Q

How do cannanbinoids cause retrogade signalling? (3)

A

Released neurotransmitter activates receptor on postsynaptic neurone
Cannabinoid released and CB1 on presynaptic neurone activated
Neurotransmitter release from presynaptic neurone reduced

40
Q

Name 2 non-rewarding addictive substances.

A

Codeine
Benzodiazepines

41
Q

Give 3 features of benzodiazepines.

A

Sedative
Hypnotic
Anxiolytic
Anticonvulsant
Muscle relaxant

42
Q

Describe the action of the GABA(A) receptor complex and the effect of BDZs. (3)

A

Pentamer chloride channel
Allosteric change opens Cl- channel
BDZs enhance GABA(A) function

PED1003-Pharmacology (27 decks)

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