Week 10- Opioid Analgesics Flashcards

1
Q

Purpose for opioid analgesics

A

To relieve moderate-to-severe pain

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2
Q

True or false: Opioids are controlled substances in the US because of their potential for abuse

A

True

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3
Q

The term opioid has been instituted to represent all types of ________ analgesic-like agents and _________-like medications, regardless of their origin

A

Narcotic
Morphine

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4
Q

Opioids can be these types of sources

A

Natural
Synthetic
Semisynthetic

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5
Q

Opium contains about ____ biologically active compounds, including morphine and codeine

A

20

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6
Q

The body manufactures and releases these to control pain and inflammation

A

Endogenous opioid peptides

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7
Q

Three distinct families of endogenous opioid peptides

A

Endorphins
Enkephalins
Dynorphins

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8
Q

Endogenous opioid peptides can help regulate…

A

Immune system
GI function
Cardiovascular responses
Physiological systems

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9
Q

True or false: Endogenous opioid peptides are not involved in many aspects of behavior, including response to physical and psychological stress, eating and drinking behaviors, and physiological addiction to exogenous opioids and other drugs

A

False

(it does)

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10
Q

Opioid receptors

A

Mu
Kappa
Delta

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11
Q

Classification of special agents

A

Strong agonists
Mild-to-moderate agonists
Mixed agonist-antagonists
Antagonists

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12
Q

This classification of special agents treat severe pain and have a high affinity with mu receptors

A

Strong agonists

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13
Q

Examples of agonist drugs

A

-Hydromorphone (Hydrostat, Dilaudid)
-Meperidine (Demerol)
-Methadone (Dolophine, Methadose)
-Morphine (MS Contin, Roxanol, Statex, others)
-Tramadol (Ralivia, Ultram)
-Fentanyl

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14
Q

This classification of special agents treat moderate pain

A

Mild-to-moderate agonists

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15
Q

Examples of mild-to-moderate agonists

A

-Codeine
-Hydrocodone (Hycodan)
-Oxycodone (OxyContin, Roxicodone)
-Propoxyphene (Darvon)

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16
Q

This classification of special agents exhibit some agonist and antagonist-like activity at the same time

A

Mixed agonist-antagonists

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17
Q

True or false: Mixed agonist-antagonists leads to less risk of side effects associated with mu receptors

A

True

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18
Q

True or false: Mixed agonist-antagonists produce less psychotropic effects

A

False

(more)

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19
Q

True or false: The maximal analgesic effect of mixed agonist-antagonists is great as strong mu agonists

A

False

(may not)

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20
Q

True or false: Antagonists produce analgesia

A

False

(they do)

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21
Q

This classification of special agents is primarily used to treat opioid overdoses and addiction

A

Antagonists

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22
Q

The primary agent currently used in the US to treat opioid overdose is ______________

A

Naloxone

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23
Q

Metabolic inactivation of these drugs takes place primarily in the __________

A

Liver

24
Q

Some degree of metabolism also occurs in ________, ________, and ________

A

Kidneys
Lungs
CNS

25
Q

Pharmacokinetics of opioids

A

-Oral, IV, IM, rectal, sub-Q, epidural, intranasal
-Transdermal patches
-Iontophoresis

26
Q

Mechanism of actions of opioids

A

Spinal effects
Supraspinal (brain) effects
Peripheral effects

27
Q

Decrease ascending (afferent) pain transmission, combined with their ability to activate descending (efferent) pathways that reduce pain

A

Spinal effects
Supraspinal (brain) effects

28
Q

At peripheral sensory nerve endings, opioids decrease excitability of the neuron and inhibit the neuron from initiating transmission of painful stimuli toward the spinal cord

A

Peripheral effects

29
Q

Inhibitory effect is mediated by opioid receptors that are located on both presynaptic and postsynaptic membranes of pain- mediating synapses

A

Spinal effects

30
Q

Opioids bind to specific receptors in the midbrain periaqueductal gray matter (PAG) and remove inhibition (disinhibition) of descending pathways that decrease pain

A

Supraspinal (brain) effects

31
Q

Increased activity of descending pathways travels through the ventromedial ________ (VMM) to reach the __________ horn of the spinal cord

A

Medulla
Dorsal

(supraspinal brain effects)

32
Q

Neurons in descending pathways release _________ and __________ onto dorsal horn synapses and inhibit the ability of these synapses to transmit painful impulses to the brain

A

Serotonin
Norepinephrine

(supraspinal brain effects)

33
Q

SLIDE 16

A
34
Q
A
35
Q

Clinical applications for opioids

A

-Acute moderate-to-severe pain following surgery, trauma, and myocardial infarction
-Chronic pain such as cancer
(non-opioid drugs should be attempted first)
-Should be used only when necessary, because of the potential for serious side effects
-Not effective in treating sharp and intermittent pain
-Anesthetic pre-medication or as an adjunct in general anesthesia
-Cough suppression (short-term use of codeine and codeine-like agents)
-Control of severe diarrhea
-Acute pulmonary edema
-Patient controlled analgesia (PCA)

36
Q

True or false: Orally administered opioids are more effective when given at regularly scheduled intervals rather than when the patient feels the need for them

A

True

37
Q

Problems and adverse effects of opioids

A

-Metal slowing and drowsiness (sedative properties)
-Respiratory depression (slow the breathing rate)
-Orthostatic hypotension
-GI distress

38
Q

This occurs when an individual repeatedly ingests certain substances for mood-altering and pleasurable experiences, such as the heroin

A

Addiction

39
Q

The need to progressively (periodically) increase the dosage of a drug to achieve a therapeutic effect (to provide adequate relief) when the drug is used for prolonged periods

A

Tolerance

40
Q

Mechanisms of tolerance

A

-Receptor down-regulation (removed by endocytosis) and desensitization
-Loss of communication between the opioid receptor and the G protein

41
Q

Tolerance begins after the ________ dose of the narcotic, but the need for increased amounts of the drug usually becomes obvious after ________ weeks of administration

A

First
2-3

42
Q

Tolerance seems to last approximately _____ weeks after the drug is removed

A

1-2

43
Q

The onset of withdrawal symptoms when the drug is abruptly removed

A

Physical dependence

44
Q

Withdrawal symptoms become evident within ______ hours after the last dose of the drug, and peak on day ____ or day ____ after the drug has been stopped; last about ____ days

A

6-10
2
3
5

45
Q

The risk of addiction, tolerance, and dependence is actually very _______ when opioid drugs are used appropriately to treat chronic pain in patients who do not have a history of substance abuse

A

Low

46
Q

True or false: Patients never fail to respond to opioids and never report increased pain sensitivity

A

False

47
Q

True or false: Pain may worsen when opioid drugs are reaching peak effects

A

True

48
Q

True or false: Pain may increase when drug effects are minimal or the dosage is reduced

A

False

(reduce)

49
Q

True or false: Careful baseline pain measurements will be needed to see if pain increases when the opioid drug begins to take effect

A

True

50
Q

Goal of pharmacological treatment of opioid addiction

A

To eventually wean the patient from all opioid drugs (inappropriate or illegal use and abuse of narcotics such as heroin

51
Q

This drug offers several advantages such as milder withdrawal symptoms

A

Methadone

52
Q

This drug is a mixed agonist-antagonist that can be used as an alternative

A

Buprenorphine

53
Q

True or false: Scheduling therapy when drugs reach their peak effects may be advantageous

A

True

54
Q

Constipation especially problematic in SCI patients or other conditions that decrease GI motility

A

GI discomfort

55
Q

Opioids are often administered along with _________ and _________

A

Laxatives
GI stimulants

56
Q

Respiratory response to any rehabilitation exercise may be blunted

A

Respiratory depression