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Year 3 - Drugs of Abuse > 10 - CNS Depressants > Flashcards

10 - CNS Depressants Flashcards

1
Q

What are the effects of CNS depressants?

A
  • slow brain activity
  • calm and soothe -> decrease anxiety, panic attacks & seizures
  • treat insomnia
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2
Q

Name five examples of CNS depressants

A

Alcohol
Cannabis
Benzodiazepines
Opioids
GHB

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3
Q

What do analgesics do?

A

Distort sensory perception, emotion, judgement and thinking

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4
Q

What is the main effect of cannabinoids?

A

Decrease pain

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5
Q

What do hallucinogens do?

A

Cause hallucinations
Change perception & awareness
Cause psychotic-like behaviour

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6
Q

What does THC stand for?

A

Delta tertrahydrocannabinol

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7
Q

What is THC responsible for?

A

Mind altering affects of cannabis
- Euphoria
- Heightened senses
- Relaxation
- Increased libido

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8
Q

Is THC water or lipid soluble?

A

High lipid solubility (allows for passive diffusion across cellular membranes)

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9
Q

What are the side effects of THC?

Physiological & neurological

A

Increased HR
Increased pain tolerance
Induces cell-death
Shrinks neurons
Causes DNA fragmentation in hippocampus

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10
Q

What are endocannabinoids?

A

NT that is naturally produced by body

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11
Q

How do endocannabinoids work on the synaptic level?

A
  • Bind to cannabinoid receptors on neurons producing/facilitating release of GABA
  • Inhibit GABA, preventing GABA from inhibiting dopamine production -> increased dopamine production
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12
Q

How does THC work on the synaptic level?

A
  • Has similar structure to endocannabinoids
  • Competes with endocannabinoids & binds to cannabinoid receptors
  • Inhibits & reduces GABA production -> increase in dopamine
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13
Q

What are the long-term effects of THC on the brain?

A
  • THC binds to various endocannabinoids throughout the brain
  • Results in alteration to brain communication with body -> affects emotions, movement, memory, decision making
  • Frequent use in adolescence rewires brain, can lower IQ and cause addiction
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14
Q

What are the different cannabinoid receptors and where are they located?

A

CB1 - Hippocampus, cerebellum, striatum
CB2 - Peripheral tissues - spleen

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15
Q

Where can THC be detected and for how long?

A

t1/2 in fats - 8 days. detected days-weeks

Urine - infrequent 3-4 days, heavy 10 days, chronic/high fat% up to 30 days

Blood - 2-3 days, heavy up to 2 weeks

Saliva/Oral fluid - 2-24 hours

Hair - up to 90 days

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16
Q

Name the presumptive tests for THC

A
  • DL (Duquenois-Levine) - Violet/black
  • Fast blue B - red/blue
  • Microscopy - identity confirmation for bulk samples
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17
Q

Opioids are CNS depressants and analgesic’s. True or false?

A

True

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18
Q

How many alkaloids are in opium? Give an example

A

20+
Morphine

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19
Q

What is the route of pain?

A

Nocicereseptors respond to potentially damaging stimuli
Nocicereceptors stimulated -> release excitatory NTs -> signals send to thalamus -> pain perception -> somatosensory cortex -> feel pain

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20
Q

What are the different opioid receptors?

A

Mu, delta, kappa

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21
Q

What are the two variations of mu receptor?

A

u1 - analgesia
u2 - respiratory depression & constipation

22
Q

What shape is the structure of opioids?

A

T shaped

23
Q

What are the identifying groups in opioids?

A

Phenolic group
Aromatic ring
Amine group

24
Q

What is the t1/2 of morphine?

A

2-4 hours

25
Q

What is morphine’s affinity at each opioid receptor?

A

Mu & delta - high affinity
Kappa - low affinity

26
Q

Why is morphine fast-acting?

A

Crosses blood-brain barrier quickly

27
Q

What is morphine’s major metabolite, and what process is used to create it?

A

Morphine-6-glucuronide
Glucuronidation

28
Q

What is heroin metabolised to, and how?

A
  • Diacetylmorphine via acetylation of morphine
  • 6-monoacetylmorphine (6-MAM)
29
Q

Heroin is completely illegal. True or false? Give an example

A

False
Legally prescribed as diamorphine

30
Q

What is the white-crystalline form of heroin?

A

Diacetylmorphine hydrochloride

31
Q

What is 6-MAM’s affinity to each opioid receptor?

A

High affinity at mu

32
Q

What are the effects of 6-MAM?

A

Similar and greater to/than morphine

33
Q

Is 6-MAM addicting? Explain

A

Yes
Has extremely rapid affect

34
Q

Why is 6-MAM lipid-soluble? Explain the benefit of this

A

Has acetyl groups
Allows the drug to pass through membranes with ease

35
Q

What is the effect of the mu receptor?

A

Inhibits GABA release which is responsible for dopamine inhibition, results in dopamine high

36
Q

What is the body’s response to opioid use?

A

Reduce natural opioid peptides (endorphins) creating dependence

37
Q

What are the withdrawal symptoms of opioids?

A

Anxiety
Depression
Cramps
Vomiting
Diarrhoea
Severe sense of pain not caused by anything

38
Q

What is the effect of codeine? How is this useful in medicine?

A

Causes respiratory depression, and depressed cough
Useful in cough medicine

39
Q

What is the affinity of codeine to each opioid receptor?

A

Low affinity to all

40
Q

Is codeine analgesic?

A

No, it is only analgesic when it is converted to morphine

41
Q

How is codeine converted to morphine?

A

When orally administrated, 10% is O-demethylated and then converted to morphine in the liver by P450 enzymes

42
Q

Why is codeine a drug of abuse? Give some effects

A

Mixed with alcohol to create lean
- Euphoria
- Dissociative feeling from parts of body

43
Q

What is methadone’s medicinal use?

A

Treats heroin addiction
Reduces physical dependence

44
Q

What is the t1/2 of methadone?

A

24-48 hours

45
Q

What is the effect of pethidine use?

A

Analgesic effects at kappa receptor
Cause dependence -> drug abuse
Less likely to cause addiction

46
Q

What receptor does fentanyl work at?

A

mu, specifically u

47
Q

How much stronger is fentanyl compared to morphine?

A

1000x

48
Q

How is fentanyl used medicinally?

A

Patches
Flavoured lollipop - fentanyl citrate

49
Q

What is the use of opioid antagonists?

A

Treat opioid addiction

50
Q

Name the two opioid antagonists

A

Naloxane and naltrexone

51
Q

Describe what naloxane does

A
  • acts on mu receptor, competitive inhibition
  • intravenous administration
  • produces opioid withdrawal symptoms
52
Q

Describe what naltrexone does

A
  • alcohol addiction treatment
  • mechanism unknown - just works
  • more potent than naloxane

Year 3 - Drugs of Abuse (10 decks)

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