Opioid Pharmacology

Front 1

Who defines pain as "an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage."

Back 1

International Association of Pain and American Pain Society

Front 2

What are the functions of pain?

Back 2

Detect, localize and limit tissue damage

Front 3

Latin for harm or injury:

Back 3

Noci

Front 4

Free afferent nerve ending:

Back 4

Nociceptor

Front 5

What does the stimulus response process involve?

Back 5

Transduction, transmission, perception and modulation of pain

Front 6

What are the two types of pain?

Back 6

Nociceptive and Neuropathic

Front 7

Somatic/Visceral: Pain from identifiable spot

Back 7

Somatic

Front 8

Somatic/Visceral: Associated with distention of organ capsule

Back 8

Visceral

Front 9

Somatic/Visceral: Associated with obstruction of hollow viscus

Back 9

Visceral

Front 10

Somatic/Visceral: Usually well localized

Back 10

Somatic

Front 11

Somatic/Visceral: Sharp in nature and hurts at the point of stimulus

Back 11

Somatic

Front 12

Somatic/Visceral: Diffuse in nature

Back 12

Visceral

Front 13

Somatic/Visceral: Dull and vague and can be referred

Back 13

Visceral

Front 14

Somatic/Visceral: Superficial or Deep

Back 14

Somatic

Front 15

This type of pain can be described by somatic or visceral?

Back 15

Nociceptive

Front 16

This type of pain can be described by a dysfunction of the CNS allowing for spontaneous excitation

Back 16

Neuropathic

Front 17

An abnormal processing of painful stimuli, can be generated centrally or peripherally, burning, tingling or shocklike and very difficult to treat

Back 17

Neuropathic

Front 18

Thermally noxious stimuli would start at what temperature?

Back 18

43 degrees celcius

Front 19

Transformed into electrical energy.

Back 19

Transduction

Front 20

Signal sent from periphery to CNS.

Back 20

Transmission

Front 21

Descending mechanisms modulate signal transmission in spinal cord.

Back 21

Modulation

Front 22

What do alogens cause? Define alogens.

Back 22

Pain/ Endogenous chemicals or neurotransmitters that generate an action potential

Front 23

Name some alogens

Back 23

Bradykinins, Serotonin, H+, Prostaglandins, Histamine, Substance P

Front 24

Path of transduction,place in order: action potential, pain, sensory nerves to spinal cord, alogens trigger, afferent nerve or nociceptor

Back 24

Pain, alogens trigger, afferent nerve or nociceptor, action potential, sensory nerves to spinal cord

Front 25

Excitatory neurotransmitter presumed to be released by terminals of pain fibers that synapse in the substantia gelatinosa of the spinal cord

Back 25

Substance P

Front 26

T/F Pain transduction is electrosensory.

Back 26

F/ Pain transduction is chemosensory

Front 27

What is released from the phospholipids on the cell membrane b/c of tissue damage?

Back 27

Phospholipase A

Front 28

What does phospholipase A form?

Back 28

Arachidonic Acid

Front 29

Cyclooxygenase (COX) pathway converts arachidonic acid into what?

Back 29

Endoperoxides

Front 30

What do endoperoxides form?

Back 30

Prostacyclin and Prostaglandin E2 (PGE2)

Front 31

This potentiates edema from bradykinin.

Back 31

Prostacyclin

Front 32

This directly stimulates free nerve endings.

Back 32

(PGE2) Prostaglandin E 2

Front 33

What kind of drugs stop the Cyclooxygenase pathway of the Arachidonic Cascade

Back 33

COX 2 inhibitors

Front 34

What are the 2 pathways of the Arachidonic Cascade?

Back 34

Cyclooxygenase and Lipooxygenase pathways

Front 35

The end result of this pathway results in leukotrienes.

Back 35

Lipooxygenase pathway

Front 36

Arachidonic acid > hydroperoxy compounds > leukotrienes (What pathway?)

Back 36

Lipooxygenase pathway

Front 37

Where do we find leukotrienes?

Back 37

Lung

Front 38

What type of nociceptors are found in the walls of the viscera?

Back 38

Interoceptors

Front 39

What type of nociceptors receive stimuli from the skin?

Back 39

Exteroceptors

Front 40

These fibers are unmyelinated and small.

Back 40

C fibers

Front 41

These fibers are myelinated and large.

Back 41

A delta fibers

Front 42

The transmission of pain is sent via sensory afferent pathways to what part of the spinal cord?

Back 42

Dorsal horn

Front 43

If you were to feel a pin prick, what fibers are involved?

Back 43

A delta

Front 44

If you were to stub your toe, what fibers are involved?

Back 44

C fibers

Front 45

Where are A delta and C fibers located?

Back 45

Dorsal root ganglion

Front 46

What other sensations are A delta and C fibers responsible for?

Back 46

Temperature sensation

Front 47

First order neurons aka afferents, enter into the dorsal horn of the posterior spinal cord and have collaterals that can ascend or descend in what?

Back 47

Tract of Lissaer

Front 48

How many rexed laminae are there?

Back 48

10

Front 49

Where are rexed laminae located?

Back 49

Gray Matter

Front 50

Where is the spinothalamic tract located?

Back 50

White matter

Front 51

Name side effects of neuraxial analgesia?

Back 51

Pruritis, n/v, urinary retention, resp. depression, sedation, CNS excitation, viral reactivation...

Front 52

Pruritis from neuraxial opioids are from cephalad migration of opioid in CSF to where?

Back 52

Trigeminal nucleus

Front 53

How do you treat pruritis from neuraxial opioids?

Back 53

Naloxone or antihistamines

Front 54

Detrusor muscle relaxation, increase in bladder capacity and inhibition of sacral PNS outflow most common in young males is an example of what and is more common in what type of opioid route?

Back 54

Urinary retention and neuraxial route

Front 55

What is the primary treatment of ventilatory depression from neuraxial opioids?

Back 55

Supplemental oxygen

Front 56

Mu1/Mu2: This subtype provides spinal analgesia, ventilatory depression, bradycardia, physical dependence and constipation

Back 56

Mu2

Front 57

Mu1/Mu2: This subtype provides spinal and supraspinal analgesia, euphoria, low abuse potential and miosis

Back 57

Mu1

Front 58

Kappa/Delta: This receptor provides spinal and supraspinal analgesia, modulates mu receptor activity, depression of ventilation and physical dependence

Back 58

Delta

Front 59

Delta receptors respond to what?

Back 59

Enkephalins

Front 60

Kappa/Delta: This receptor provides supraspinal and spinal analgesia, sedation, dysphoria, miosis, less respiratory depression, agonists inhibit neurotransmitter via N calcium channels, Opioid antagonists usually act on these receptors.

Back 60

Kappa

Front 61

What do Kappa receptors respond to?

Back 61

Dynorphins

Front 62

Mu/Kappa/Delta: Are coupled to and increase potassium conductance thus hyperpolarizes cell membrane

Back 62

Mu receptors

Front 63

Mu/Kappa/Delta: Increase potassium conductance thus hyperpolarizes cell membrane.

Back 63

Delta and Mu receptors

Front 64

Mu/Kappa/Delta: Inhibit Calcium thus suppresses the release of neurotransmitter.

Back 64

Kappa

Front 65

Opioids have an excitatory action on the parasympathetic nerve innervating the pupil resulting in pupillary _______

Back 65

Constriction

Front 66

Abolishment of the cortical inhibition________ ______ nucleus is a neurophysiologic effect of opioids.

Back 66

Edinger-Westphal

Front 67

What drugs reduce postop shivering?

Back 67

Meperidine - kappa receptor activation. Tramadol in parturient patients (misprint)??Butorphanol

Front 68

What classification of opioids is most effective in treating pruritis?

Back 68

agonist-antagonist

Front 69

What scenarios do opioids drop BP?

Back 69

Hypovolemic, hypertensive or trauma. (Catecholamine or histamine dependent)

Front 70

Opioid induced bradycardia is due to what?

Back 70

Stimulation of central vagal nucleus and sympathetic blockade

Front 71

What is the one exception to opioid induced bradycardia?

Back 71

Meperidine b/c it is structurally similar to atropine

Front 72

What two opioids cause histamine release?

Back 72

Morphine and meperidine

Front 73

This reaction is at cellular level and not IGE mediated, heroin addicts have this type of reaction.

Back 73

Anaphalactoid

Front 74

This reaction is subjected to the antigen first, then it is IGE mediated.

Back 74

Anaphylaxis

Front 75

Increased rate of metabolism by cytochrome p450 system in liver describes what?

Back 75

Enzyme induction

Front 76

Need to increase dose of opioid to achieve same analgesic effect based on two theories: down regulation of opioid receptors and up regulation of cAMP pathways

Back 76

Tolerance

Front 77

Neuraxial analgesia is specific for what type of pain?

Back 77

Visceral

Front 78

Opioid receptors are present in what part of the spinal cord?

Back 78

Substantia gelatinosa

Front 79

Hydrophilic/Lipophilic: which crosses the dura to get to the spine quicker?

Back 79

Lipophilic

Front 80

Lipophilic/Hydrophilic: Which crosses the dura more slowly? What is a characteristic of the slower movement?

Back 80

Hydrophilic/ it has time to go cephalic

Front 81

Describe the CV side effects of pain: What is released? What happens to HR, CO, CMO2, BP and coagulation?

Back 81

Released: Catecholamines, cortisol, angiotensin II. Increased HR, CO, CMO2, BP and hypercoagulation > DVT

Front 82

Describe the resp side effects of pain: TV, VC, IC, FRC....

Back 82

Decrease TV, VC, IC and FRC, patients are reluctant to cough and deep breathe leads to atelectasis and pneumonia

Front 83

Describe GI/GU side effects of pain.

Back 83

Increase sympathetic activity: decreased gastric emptying, decreased intestinal motility, hypomotility of urethra and bladder.

Front 84

Describe the effects of pain on the endocrine system: What happens to ACTH, ADH, GH, cortisol, glucagon, insulin and testosterone?

Back 84

Increased ACTH, ADH, GH, cortisol, glucagon. Decreased insulin and testosterone

Front 85

How long could a healthy individual be immunosuppressed after surgery?

Back 85

1-2 weeks

Front 86

What can decrease peripheral and central sensitization?

Back 86

Preemptive analgesia

Front 87

How does analgesia work on ascending pathways? descending pathways?

Back 87

Ascending - inhibits transmissions of pain from the spinal cord. Descending - activates pain control

Front 88

Name pharmacologic interventions utilized to control pain.

Back 88

Antidepressants, anticonvulsants, neuroleptics, corticosteroids, cox inhibitors, opioids

Front 89

What pharmacologic analgesic? Usually lower dose than what it was intended for and action is due to blocking reuptake of serotonin or NE or both.

Back 89

Antidepressants

Front 90

What pharmacologic analgesic: blocks voltage-gated Na channels and is good for neuropathic pain?

Back 90

Anticonvulsants

Front 91

What pharmacologic analgesic: blocks dopaminergic receptors?

Back 91

Neuroleptics

Front 92

What pharmacologic analgesic: inhibits prostaglandin production by blocking phospholipase A2 activation?

Back 92

Corticosteroids

Front 93

What pharmacologic analgesic: works by activation of descending inhibitory pathway in dorsal horn?

Back 93

Alpha 2 adrenergic agonists

Front 94

What pharmacologic analgesic: inhibits prostaglandin synthesis?

Back 94

Cox inhibitors

Front 95

Papaver Somniferum =?
Opos is Greek or what?

Back 95

Opium
juice

Front 96

T/F all opiates are opioids.
T/F all opioids are opiates.

Back 96

T
F

Front 97

Opiate/Opioid/ Narcotic
Drugs that bind to opioid receptors

Back 97

Opioid

Front 98

Opiate/Opioid/Narcotic
Drugs derived from opium

Back 98

Opiate

Front 99

What are the two chemical classes of naturally occuring opiates?

Back 99

Phenanthrene and benzylisoquinoline

Front 100

What is an example of a semisynthetic opioid?

Back 100

Heroin

Front 101

What is your name?
I needed to get 1 card right:)

Back 101

Insert your name here

Front 102

What are the opioid receptors?

Back 102

Mu, Kappa and Delta

Front 103

Opioid receptors are located in the brain, spinal cord and periphery: be more specific.

Back 103

Brain: periaqueductal gray of brainstem, amygdala, corpus striatum, hypothalamus. Spinal cord: Substantia gelatinosa (rexed 2 & 3). Periphery: primary afferent neurons

Front 104

What are the 3 endogenous opioids?

Back 104

enkephalins, endorphins & dynorphins

Front 105

Mu receptors respond to what?

Back 105

Endorphins

Front 106

C fiber pathways: After Tract of Lissauer, first order neurons synape where?

Back 106

Rexed Laminae II or III aka substantia gelatinosa

Front 107

C fiber pathways: Synapse in rexed laminae V, before where?

Back 107

Crossing over and on to the brain

Front 108

First/Second/Third order neurons synapse in dorsal horn.

Back 108

First with second

Front 109

First/Second/Third order neurons cross to contralateral hemisphere and ascend to thalamus.

Back 109

Second

Front 110

First/Second/Third order neurons send axonal projections to reticular formation, nucleus raphe magnus & periaqueductal gray

Back 110

Third

Front 111

First/Second/Third order neurons send axonal projections into sensory cortex

Back 111

Third

Front 112

First/Second/Third order neurons focused in areas of greater sensitivity

Back 112

Third

Front 113

First/Second/Third order neurons found in the thalamus

Back 113

Third

Front 114

Repeated stimulation causes sensitization defines what?

Back 114

Hyperalgesia

Front 115

Primary/Secondary Hyperalgesia: Neurogenic inflammation and Triple response

Back 115

Secondary hyperalgesia

Front 116

Central Modulation can be what?

Back 116

Inhibitory or excitatory

Front 117

Describe the peripheral modulation pathway that puts a patient at risk for DVT.

Back 117

Arachidonic acid > Prostaglandins > Thromboxin > platelet aggregation > clot

Front 118

Prolonged discharge sensitization of second order neurons increasing frequency of discharge and receptor field expansion are examples of what?

Back 118

Central Modulation - spinal facilitation

Front 119

Neuroplasticity - central sensitization to afferent impulses are examples of what?

Back 119

Central Modulation - Spinal Neuroplasticity

Front 120

Endogenous enkephalins, opioids, spinal analgesia that inhibits substance P or block post synaptic response to substance P are examples of what?

Back 120

Central Modulation - Spinal Inhibition

Front 121

Descending neurons from periventricular and periaqueductal gray transmit through nucleus raphe magnus to substancia gelatinosa is an example of what?

Back 121

Central Modulation - Supraspinal Inhibition