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Pharm Exam 2 > Lecture 20 - Gentile - Opioids > Flashcards

Lecture 20 - Gentile - Opioids Flashcards

1
Q

What 4 areas of the brain are activated in acute pain?

A

Insula, Anterior Cingulate, Thalamus, and Basal Ganglia

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2
Q

Which regions are involved in anticipating and perceiving pain?

A

Brain stem and descending pain modulatory system

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3
Q

Chronic pain leads to increasing activation of which brain region?

A

Pre-frontal cortex

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4
Q

Define excitatory neurotransmitters and name 2 of them

A

They are inflammatory chemicals that are released after tissue is damaged

Histamine and Bradykinin

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5
Q

What does Bradykinin do?

A

Stimulates release of prostaglandins and substance P, a potent neurotransmitter that enhances movement of impulses

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6
Q

Most opioids act on the ___

A

Synapse

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7
Q

What cortex identifies the location and intensity of pain?

A

Somatosensory cortex

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8
Q

What cortex determines how an individual interprets the meaning of pain?

A

Associated Cortex

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9
Q

Acute vs Chronic Pain

A

Acute pain is a normal response that can be beneficial (signal damage or warn of harm) and will disappear once the cause is treated

Chronic pain persists and is no longer beneficial

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10
Q

How do you manage pain for acute vs chronic?

A

Acute - reduce the pain by treating the cause

Chronic - can only reduce pain

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11
Q

The most successful way to treat pain is ____

A

Opioids!

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12
Q

What are the 4 types of opioid receptors?

A

Delta, Kappa, Mu, and Nociceptin receptor

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13
Q

Where is the Mu receptor found?

A

Brain, Spinal Cord, and Intestinal Tract

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14
Q

What are the functions of the delta receptor?

A

Analgesia, antidepressant, and physical dependence

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15
Q

Define Analgesia

A

Absence of pain without loss of consciousness

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16
Q

What does physical dependence refer to?

A

Chronic use of drug has produced tolerance

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17
Q

What are the functions of the kappa receptor?

A

Spinal analgesia, sedation, miosis, inhibition of ADH release, dysphoria

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18
Q

What is miosis?

A

Constriction of the pupil to less to 2 mm

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19
Q

What is dysphoria

A

The opposite of euphoria

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20
Q

What are 2 methods to reduce the amount of action potentials generated pre-synaptically?

A

Reduce the amount of neurotransmitter released (inhibit ca entry via ca channels) or hyperpolarize membrane via stimulating k channel and inc k+

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21
Q

How would you shut down neurotransmission post-synaptically

A

K+ channel stimulation

IPSP

22
Q

What opioid receptors are seen pre-synaptically? post-synaptically?

A

pre-synaptically = mu, kappa, and delta

post-synaptically = mu

23
Q

How do opiates work?

A

Inhibit LC neurons via activating K+ channels and inhibiting Na+ dependent inward current (thru inhibition of cAMP via G protein)

24
Q

What is the most important side effect of opioids?

A

Respiratory Depression

KNOW THIS!

25
Q

What are the 3 strong drugs used for pain management?

A

Morphine, Methadone, and Meperidine

26
Q

What are the 2 moderately strong drugs used for pain management?

A

Codeine and Oxycodone

27
Q

What antagonist is used for pain management?

A

Naloxone

28
Q

What are the 2 receptor agonist-antagonists used for pain management?

A

Pentazocine and Buprenorphine

29
Q

Morphine: Indications

A

Pain from MI, sickle cell crisis, surgery, trauma, chronic pain or severe pain

30
Q

Morphine: Side effects

A

Contsipation!

As well as addiction and tolerance

31
Q

Meperidine: MOA

A

Binds kappa receptor, K+ channels, muscarinic receptor, dopamine transporter

32
Q

Meperidine: Indications

A

Moderate/severe pain from biliary spasm or renal colic

33
Q

Meperidine: Side effects

A

*Are mainly from it’s metabolite (norpethidine)

Serotonin syndrome, seizure, dysphoria, temror, respiratory depression

34
Q

Hydrocodone acts at what receptors?

A

Mu receptor (agonist)

Delta receptor (agonist)

35
Q

Hydrocodone: Indications

A

Cough during operations, dry cough from bronchitis

*hydrocodone is an anti-tussive (“anti-cough”)

36
Q

Hydrocodone: Side Effects

A

Constipation

*taken recreationally for mental numbness and euphoria

37
Q

Hydrocodone: OD

A

Pupil widening, loss of consciousness, muscle seizures

38
Q

Describe the mechanism of Euphoria

A

There are 2 presynaptic neurons (one has GABA receptor and other has Mu receptor)

Release of GABA activates negative pathway for dopamine release, but when morphine binds mu receptor there’s inhibited release of GABA so dopamine can be released

*Basically…morphine inhbitits the inhibitor of dopamine secretion (GABA)

39
Q

Codeine: Indications

A

Cough, diarrhea, IBS, narcolepsy

40
Q

Codeine: Side Effects

A

Euphoria, itching, urinary retention, depression, constipation, increased complications in erectile dysfunction

41
Q

Pentazocine binds which receptors?

A

Mu (antagonist)
Delta (agonist)
Kappa (agonist)

42
Q

Pentazocine: Indications

A

Dental extraction

43
Q

Pentazocine: Side Effects

A

Weakly antagonizes the analgesic effects of morphine and meperidine (know)

Hallucinations
Psychomimetic effects
CV effects

44
Q

Naloxone binds which receptors?

A

Mu, delta, and kappa

*is an antagonist for all 3

45
Q

Naloxone: Indications

A

Reverse effects of OD (respiratory depression, sedation, and hypotension)

46
Q

Naloxone cannot be used to counter which drug?

A

Meperidine

47
Q

Naloxone: Side Effects

A

Change in mood
Trembling
Change in heart rhythm
Block the action of pain-lowering endorphins

48
Q

Signs of OD

A

1st = blue lips

Unresponsive to pain stimuli

49
Q

Methadone binds which receptors?

A

Mu - (agonist)
Delta - (agonist)
Glutamate [NMDA] - (antagonist)
Neuronal ACh - (antagonist)

50
Q

What is methadone and why is it used?

A

It is an opioid that lasts longer and is cheaper than morphine

Is used to control intractable cough associated with terminal lung cancer and is also another way to reverse opioid effect

51
Q

Why is methadone used in the treatment of opioid dependance?

A

Methadone binds opioid receptor and stays there much longer… so now the agonist can’t interact with the receptor

52
Q

Remember: Slide 45 of the lecture has a summary table for our reference as well

A

Remember: Slide 45 of the lecture has a summary table for our reference as well

Pharm Exam 2 (7 decks)

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