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?

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?

25
What is morphine's affinity at each opioid receptor?
Mu & delta - high affinity Kappa - low affinity
26
Why is morphine fast-acting?
Crosses blood-brain barrier quickly
27
What is morphine's major metabolite, and what process is used to create it?
Morphine-6-glucuronide Glucuronidation
28
What is heroin metabolised to, and how?
* Diacetylmorphine via acetylation of morphine * 6-monoacetylmorphine (6-MAM)
29
Heroin is completely illegal. True or false? Give an example
False Legally prescribed as diamorphine
30
What is the white-crystalline form of heroin?
Diacetylmorphine hydrochloride
31
What is 6-MAM's affinity to each opioid receptor?
High affinity at mu
32
What are the effects of 6-MAM?
Similar and greater to/than morphine
33
Is 6-MAM addicting? Explain
Yes Has extremely rapid affect
34
Why is 6-MAM lipid-soluble? Explain the benefit of this
Has acetyl groups Allows the drug to pass through membranes with ease
35
What is the effect of the mu receptor?
Inhibits GABA release which is responsible for dopamine inhibition, results in dopamine high
36
What is the body's response to opioid use?
Reduce natural opioid peptides (endorphins) creating dependence
37
What are the withdrawal symptoms of opioids?
Anxiety Depression Cramps Vomiting Diarrhoea Severe sense of pain not caused by anything
38
What is the effect of codeine? How is this useful in medicine?
Causes respiratory depression, and depressed cough Useful in cough medicine
39
What is the affinity of codeine to each opioid receptor?
Low affinity to all
40
Is codeine analgesic?
No, it is only analgesic when it is converted to morphine
41
How is codeine converted to morphine?
When orally administrated, 10% is O-demethylated and then converted to morphine in the liver by P450 enzymes
42
Why is codeine a drug of abuse? Give some effects
Mixed with alcohol to create lean - Euphoria - Dissociative feeling from parts of body
43
What is methadone's medicinal use?
Treats heroin addiction Reduces physical dependence
44
What is the t1/2 of methadone?
24-48 hours
45
What is the effect of pethidine use?
Analgesic effects at kappa receptor Cause dependence -> drug abuse Less likely to cause addiction
46
What receptor does fentanyl work at?
mu, specifically u
47
How much stronger is fentanyl compared to morphine?
1000x
48
How is fentanyl used medicinally?
Patches Flavoured lollipop - fentanyl citrate
49
What is the use of opioid antagonists?
Treat opioid addiction
50
Name the two opioid antagonists
Naloxane and naltrexone
51
Describe what naloxane does
- acts on mu receptor, competitive inhibition - intravenous administration - produces opioid withdrawal symptoms
52
Describe what naltrexone does
- alcohol addiction treatment - mechanism unknown - just works - more potent than naloxane