opioids 1 Flashcards

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1
Q

what are opioids?

A
  • narcotic (drug that affects mood/behaviour)
  • produced analgesia (reduction of ability to feel pain) without anaesthesia
  • promotes sense of relaxation and sleep
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2
Q

what does an overdose on opioids lead to?

A
  • coma
  • death
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3
Q

chemically, what 3 groups can opioids be divided into?

A

1/ opiates

2/ semisynthetic narcotics

3/ endogenous peptides

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4
Q

what are opiates?

A
  • opium
  • extract of the opium poppy plant
  • any substances directly derived from opium
  • e.g.: morphine, codeine
  • natural narcotics
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5
Q

what are semi-synthetic narcotics?

A
  • formed by modifying natural compounds
  • chemical process
  • e.g.: heroin
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6
Q

what are endogenous peptides?

A
  • chemically very different
  • these act on the same opioid receptors
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7
Q

identify acute physiological effects of opioids

A
  • analgesia (inability to feel pain)
  • cough supression
  • euphoria
  • relaxation
  • decreased blood pressure
  • reduced sex drive
  • constipation
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8
Q

how does the molecular structure of opiates and related compounds relate to their physiological effects?

A
  • 4 carbohydrate rings
  • methyl amino groups = opioids backbone
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9
Q

what effect does replacing OH group with methyl oxy group have?

A
  • codeine
  • replacing hydroxy (OH) groups with methyl oxy group -> results in compound with different properties
  • compound with methyl oxy group = less analgesic
  • also has less side effects
  • less addictive
  • very potent cough suppressions
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10
Q

what effect does adding acetyl groups to opiates?

A
  • heroin
  • more lipophilic (mixes easier with fatty substances)
  • crosses blood-brain barrier quicker
  • strong high (euphoria)
  • heroin converted into morphine in brain
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11
Q

what effect does replacing methyl group with longer carbohydrate chain?

A
  • compound turns from compound receptor agonist to antagonist
  • blocks opioid receptor
  • used to treat opioid overdose
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12
Q

historically, what has opioids been used to against to treat?

A
  • used against coughing, pain, diarrhoea
  • nowadays, medical use = strictly regulated
  • recreational use = illegal
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13
Q

what are the main cause of overdose deaths?

A

opioids

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14
Q

identify signs of opioid overdose

A
  • respiratory depression
  • pupil constriction (miosis)
  • unresponsive (stupor)
  • hypothermia
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15
Q

how can overdose be treated?

A
  • injected with opioid antagonist
  • naloxone
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16
Q

what is the suggestion that alcohol is more harmful than heroin or crack based on?

A
  • expert assessment of drug harms to others
17
Q

what type of receptors are opioid receptors?

A
  • G-protein couples receptors
  • transmembrane proteins
  • sit in membrane of neurone
  • via g-protein, they are coupled to other effector sites (i.e.: ion channel) or couples to intracellular signalling cascades
18
Q

where can opioid receptors be found?

A
  • CNS
  • peripheral nervous system
  • gastrointestinal tract
19
Q

how are endogenous opioids different to opioids?

A
  • chemically different
  • these are peptides = chain of amino acids
20
Q

why are there different opioid receptors?

A
  • different receptors can exert different effects
  • Kappa opioid receptor when activated = dysphoria rather than euphoria
21
Q

once opioid receptor is activated, what impact does this have on neural activity?

A
  • inhibit neural activity
  • inhibit neurotransmitter release of the neurones carrying the opioid receptor
  • done by neurones expressing opioid receptors
22
Q

identify 3 ways that the opioid receptor may inhibit neural function

A

1/ post-synaptic inhibition of potassium channels (opening of K+ channels)
if potassium channels open -> makes neurone less likely to fire

2/ axoaxonic inhibition
(closing of Ca2+ channels)
opioid receptor sits on axon terminal
closing of calcium channels -> reduce release of neurotransmitter

3/ presynaptic autoreceptors
(reducing transmitter release)
neurones that co-express opioid receptor at synapse with other receptors
opioids act on this -> reduces transmitter release by that axon terminal