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Pharm III Unit I > 7 Opioids and Antagonists > Flashcards

7 Opioids and Antagonists Flashcards

1
Q

Opium is from the _________ plant and contains…

A

Papaver somniferum

10% morphine
0.5% codeine

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2
Q

What are the endogenous opioid peptides?

A

Enkephalins

Beta-endorphin

Dynorphin

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3
Q

Endogenous opioid peptides are ______ in response to pain

A

Released —> decreased responsiveness to pain

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4
Q

Derived from opium

A

Opiate

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5
Q

Having properties similar to drugs derived from opium

A

Opioid

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6
Q

Term that technically means “sleep inducing” but is commonly taken to mean “opioid”

A

Narcotic

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7
Q

Endogenous opioids are found in…

A

Areas of the brain involved in pain and in the reward system

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8
Q

_________ decrease pain transmission in the spinal cord and facilitate dopamine in the reward system, causing euphoria

A

Beta-endorphins

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9
Q

______ decrease pain transmission in the spinal cord

A

Enkephalins

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10
Q

_______ bind to kappa receptors, may produce analgesia, but also dysphoria

A

Dynorphins

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11
Q

What are the three opioid receptors

A

Mu (µ)

Kappa

Delta

(Sigma is not an opioid receptor, it binds to PCP)

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12
Q

Which opioid receptor does most of the things

A

Mu

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13
Q

All opioid receptors are coupled to _______ and decrease ________

A

G-i/o

cAMP

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14
Q

All subtypes of opioid receptors close _____________ on presynaptic nerve terminals

A

Voltage gated Ca2+ channels —> decreases neurotransmitter release and decreases neuronal activity in these pathways

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15
Q

In addition to closing voltage gated Ca2+ channels, µ receptors…

A

Open K+ channels, causing hyperpolarization —> inhibition of nerve transmission

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16
Q

Opioid receptor stimulation decreases the release of NTs by…

A

Inhibiting Ca2+ influx on the presynaptic terminal

Also µ receptors open K+ channels —> hyperpolarization —> harder for neurons to respond to pain signals

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17
Q

Effects of µ receptor stimulation

A

Analgesia
Euphoria
Sedation
Side effects

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18
Q

Effects of kappa receptor stimulation

A

Analgesia in some people, dysphoria in others

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19
Q

Effects of delta receptor stimulation

A

Dysphoria

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20
Q

What are the three ways opioids effect the transmission of pain?

A

Direct action at inflammed and damaged tissue

Inhibition of release of excitatory transmitters in the dorsal horn (spinal anesthesia)

Thalami action

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21
Q

How do opioids modulate pain

A

Periaqueductal gray, may cause release of endogenous opioids as well

Rostral ventral medulla

NE pathway from locus coeruleus to dorsal horn may also decrease pain

Inhibition of neurons may increase the activity of pathways that inhibit pain

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22
Q

What is the relationship between opioids and GABA?

A

GABA normally inhibits descending neuronal pathways that modulate pain

Opioids decrease the release of GABA, allowing the pathways to be activated

This decreases pain transmission in the dorsal horn of the spinal cord

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23
Q

Describe the analgesic effects of opioids

A

Decreases sensation of pain - not numb but they don’t mind it as much

Decreases reaction to pain - relieves SUFFERING from pain

Tolerance develops to the analgesia

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24
Q

What type of pain do opioids not work well for?

A

Nerve pain

Gabapentin is better

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25
Q

What are the sedative effects of opioids?

A

Not used as sleep aids - different quality of sedation (floating, dream-like state)

Disrupts REM

Morphine causes CNS depression in overdose

Codeine, meperidine may cause excitement in overdose

Some species become excited rather than sedated

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26
Q

While morphine causes CNS depression in overdose, _______ and ______ can cause excitation

A

Codeine

Meperidine

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27
Q

What are the different grades of CNS depression you see in opioid overdose?

A

Mental clouding/sedation —> hypnosis or stupor —> coma —> death

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28
Q

What are the effects of opioids on your mood?

A

Can cause a sense of euphoria (floating, pleasure) - researchers trying to dissociate euphoria from analgesia

Some find the experience dysphoric (unpleasant) - kappa and delta receptors are involved in dysphoria

Effect probably depends on receptor distribution in different individuals

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29
Q

Individuals who experience dysphoria while using opioids like have more ________ receptors

A

Kappa and delta

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30
Q

Which opioid causes the worst nausea?

A

Injected morphine

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31
Q

Why do opioids cause emesis?

A

Stimulate chemoreceptor trigger zone (CTZ)

Take with food!

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32
Q

What are the antitussive effects of opioids?

A

Lower doses than those used for analgesia

CODEINE and DEXTROMETHORPHAN most commonly used and very effective for depression of cough reflex

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33
Q

___________ is not an analgesic but works great as an antitussive agent

A

Dextromethorphan

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34
Q

_______ doesn’t suppress cough at all but is a great analgesic

A

Meperidine (Demerol)

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35
Q

What are the effects of opioids on the respiratory system?

A

Respiratory depression more common in overdose but also occurs with therapeutic doses

Decreases response of brain stem to elevated CO2

USEFUL IN PULMONARY EDEMA

Not good in people with pulmonary disease (Ie COPD)

May also cause bronchoconstriction

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36
Q

Effect of opioids on intracranial pressure

A

Increases ICP

Increased CO2 causes vasodilation, increases cerebral blood flow, and increases pressure

Watch out in patients with head trauma

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37
Q

Why would you want to avoid opioids in patients with head trauma?

A

B/c they increase intracranial pressure

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38
Q

All opioids cause miosis except…

A

Meperidine (which actually dilates the pupils

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39
Q

Tell me more about opioids and miosis

A

No tolerance develops (useful when people lie to you about having taken them)

Due to parasympathomimetic - blocked by atropine

Common in overdose but may convert to dilation in comatose patients

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40
Q

Why do you get decreased body temperature when you take opioids?

A

Dysregulation in the hypothalamus

Problematic for those addicts living on the street in winter…

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41
Q

Effects of opioids on the skeletal muscles

A

Supraspinal effect increases tone of the large trunk muscles —> truncal rigidity

May interfere with respiration or with attempts to ventilate patient

Most common with highly lipid soluble drugs like fentanyl

Inject slowly or use neuromuscular blockers to prevent this effect

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42
Q

Truncal rigidity is most common in…

A

Highly lipid soluble drugs like fentanyl

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43
Q

What are the cardiovascular effects of opioids?

A

No direct effect but bradycardia may occur

Decreased BP common

May result from CNS vasomotor depression and/or release of histamine (vasodilators)

Tachycardia may occur with meperidine

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44
Q

What’s the one opioid that causes tachycardia rather than bradycardia?

A

Meperidine

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45
Q

GI effects of opioids

A

Decreased gastric activity both CNS and local inhibition of transmitter release

CONSTIPATION

Decreased gastric motility

Biliary colic, constriction of sphincter of Oddi

Decreased biliary, pancreatic, and intestinal secretions

46
Q

What patient ed is important when starting a patient on opioids?

A

Warn them about constipation and be pro-active in preventing it - maybe give them a stool softener at the same time

47
Q

GU effects of opioids

A

Antidiuretic effect —> decreased urine output

Decreases renal blood flow

Increases sphincter tone —> harder to urinate (worst for those with BPH)

Increases urethral tone —> harder to pass kidney stones

48
Q

Why don’t you give opioids to someone with kidney stones?

A

They increase urethral tone making it harder to pass the stone

49
Q

Effects of opioids on the uterus

A

May prolong labor

50
Q

Endocrine effects of opioids

A

Increases ADH, prolactin, somatotropin

Inhibits luteinizing hormone

51
Q

People will often claim that they are allergic to opioids when they are really just….

A

Reacting to the histamine release that occurs in some people (—> flushing, itching, sweating)

True opioid allergies are very rare

More common when opioids are injected, especially morphine

Generally treated or prevented with antihistamines like Benadryl

52
Q

_____ commonly develops when opioids are used chronically

A

Tolerance

Higher doses will be needed to control pain

Occurs very rapidly - within days

More common with drugs that have lower efficacy

53
Q

How does physical dependence occur with opioids?

A

May result from desensitization of mu receptors or receptor uncoupling

NMDA receptor antagonists may decrease development of tolerance

54
Q

Hyperalgesia with long-term opioid use may be mediated by…

A

Increases in spinal cord dynorphin in that it makes pain transmission more effective

Decreased by NMDA receptor antagonists

55
Q

While tolerance to analgesia, sedation, euphoria, N/V, and respiratory depression do develop with opioids, no tolerance will develop to…

A

Miosis
Constipation
Seizures

56
Q

Urinary retention as a result of opioid use will be worse in…

A

Men with BPH due in part to constriction of urinary sphincter

57
Q

Adverse effects of opioids

A 
N/V (take with food)
Constipation
Urinary retention
Itching/hives
Respiratory depression***
Postural hypotension
Restlessness and hyperactivity 
Dysphoria in some people
58
Q

Tolerance to opioids results from …

A

Receptor desensitization

Down regulation

Uncoupling from G-proteins

(Occurs in thalamus and spinal cord)

59
Q

Patients who develop tolerance to opioids __________ addiction, but patients with addiction ________

A

Do not necessary have addiction

Patients with addiction are also tolerant

The reward pathway is involved in addiction, different from the tolerance areas

60
Q

Why are opioids addictive?

A

Opioids increase firing in the reward system, leading to euphoria and reinforcement

Opioid abuse and addiction has become a major problem in the US

61
Q

______ and ______ occur in anyone who uses opioids chronically for any reason

A

Tolerance and physical dependence

Addiction is most common when opioids are used for euphoric effect but an occur with medical use as well

62
Q

Addiction is more likely if _________

A

UNDERprescribed

If the patient develops severe pain, which is relieved by an opioid, this provides reinforcement

Reward pathway activated

If opioids given before the pain gets too severe, it bypasses the reward pathway —> STAY AHEAD OF THE PAIN!

63
Q

Compulsive use of drugs athat are no longer required medically, in spite of adverse consequences

A

Addiction

64
Q

Other signs of addiction

A 
Abandoning responsibilities
Constipation
Depression
Mood swings
Slurred speech
Poor coordination
Needle marks from injection
Infections from injection
65
Q

SSx of withdrawal

A 
Dysphoria, anxiety, insomnia
Anorexia, yawning
Chills, goose bumps
Vomiting, diarrhea
Rhinorrhea, lacrimation
Increased BP, HR, Temp
Muscle aches and twitches
66
Q

Symptoms of withdrawal can be reduced by use of …

A

Clonidine or another opioid (methadone)

Opioid antagonists can precipitate withdrawal if dependent though

67
Q

SSx of opioid overdose

A

CNS depression
Respiratory depression
Pin point pupils (may dilate if severely hypoxic)

Treat by supporting respiration (ABCs)
Use of opioid antagonist naloxone (Narcan)

68
Q

What are the different routes of administration for opioids

A 
Patient controlled analgesia
Transdermal patch
Intranasal spray
Buccal (lollipop)
Sublingual
69
Q

Keys to remember when using opioids to control pain

A

Sedation will be common (can become tolerant)

Stay ahead of the pain - dose around the clock

Combine with non-opioids when possible to maximize effectiveness

Titrate opioid to degree of pain - strong for severe pain, moderate for less severe

Patient controlled analgesia often used post-op

70
Q

How are opioids used in acute pulmonary edema?

A

To relieve dyspnea (mechanism unclear)

71
Q

Which opioids are used for the relief of cough

A

Codeine and dextromethorphan

72
Q

What are the opioids used for treatment of diarrhea?

A

Loperamide (Imodium)

Diphenoxylate/atropine (Lomotil)

73
Q

Opioids + sedative-hypnotics

A

Increased CNS and respiratory depression

74
Q

Opioids + antipsychotics

A

Sedation, maybe respiratory depression

75
Q

Opioids + MAO inhibitors

A

Esp Meperidine/dextromethorphan

May inhibit serotonin reuptake to some degree

BUT - best to avoid ALL opioids with MAOIs

76
Q

Opioids + CYP2D6 inhibitors

A

Inhibit metabolism of codeine, oxycodone, hydrocodone to active compounds

Fluoxetine, paroxetine are the worst for inhibition

77
Q

Contraindications for the use of opioids

A

Use of partial agonist with full agonist - can impair analgesia and cause withdrawal

Patients with head injuries (b/c increase ICP)

Pregnancy (esp at delivery)

Impaired pulmonary function

Impaired hepatic or renal function

Some endocrine diseases

78
Q

Use opioids with caution in patients with …

A 
Severe liver/kidney disease
Pulmonary disease
Biliary tract problems
Seizures (esp meperidine)
Pain of unknown cause (esp abdominal)
Head trauma
Chronic non-terminal pain
Inflammatory bowel disease
Pregnancy/breast feeding
Urinary retention/BPH
79
Q

Morphine stimulates _______ receptors

A

All opioid receptors

Strong agonist

Produces all of the effects of opioids

Useful in severe pain

80
Q

Morphine is more effective when…

A

Injected, due to high first-pass metabolism (~75%) if taken orally

Extended release long-acting oral preparation used in chronic/terminal pain

81
Q

Onset and duration of action for morphine

A

Rapid onset with parenteral admin - max action within one hour

Duration of analgesia is approx 4-6 hours (half-life 2-3 hours, longer in elderly)

82
Q

The standard therapeutic dose of morphine is…

A

10mg SC or IM

This is the dose to which all other analgesic drugs are compared

83
Q

Morphine is metabolized …

A

In the liver by CYP2D6

Conjugated to glucuronide compounds

Morphine-6-glucuronide is very potent analgesic

Morphine-3-glucuronide may cause adverse effects as it accumulates

84
Q

Why don’t you give morphine to pregnant women?

A

Morphine and other opioids readily cross the placental barrier and can affect the fetus resulting in respiratory depression or even drug dependence with chronic use

85
Q

Hydromorphone (Dilaudid) is a ________ analgesic

A

Very strong - more potent than morphine

Very effective for moderate to severe pain

Metabolites don’t accumulate so good if there is renal dysfunction

Less likely to cause histamine release and itching than morphine

86
Q

MOA for Methadone (Dolophine)

A

Long half life and duration of action

Stimulates mu receptors

May also block NMDA receptors and inhibit NE/serotonin reuptake

87
Q

How is Methadone (Dolophine) used?

A

Traditionally used for maintenance treatment of addicts
•Low doses used to prevent withdrawal symptoms
• Withdrawal thought to be milder, but very prolonged

Now commonly used in long-term control of pain

Effective in hard-to-treat types of pain

88
Q

When should Meperidine (Demerol) NOT be used?

A

For more than 48 hours

In high doses

In renal failure (due to accumulation of metabolite, normeperidine)

As a cough suppressant (don’t work)

89
Q

Metabolite of meperidine that causes seizures

A

Normeperidine

90
Q

Meperidine (Demerol) is the one opioid you might use in obstetrics because…

A

Less respiratory depression in baby

91
Q

Meperidine + MAOIs

A

Serotonin syndrome

92
Q

Very lipid soluble and highly potent opioid with a high abuse potential

A

Fentanyl (Sublimaze)

Very commonly used in short surgical procedures, often with midazolam

Popular in longer surgeries b/c of good CV profile

May cause truncal rigidity if given rapidly via IV

93
Q

________ is used for moderate to severe pain, often in combo with acetaminophen

A

Hydrocodone

Generally given orally, well absorbed

Don’t give to patients on SSRIs (esp fluoxetine/paroxetine) b/c they need to be converted by CYP2D6 for effect

Probably shouldn’t give the combo with acetaminophen but whatever

94
Q

Percocet is _____ + ________

A

Oxycodone + acetaminophen

95
Q

Percodan = ______ + ________

A

Oxycodone + aspirin

96
Q

Naloxone or naltrexone are often added to ________ if injected to decrease abuse potential

A

Oxycodone

97
Q

Codeine is _____ if alone, _____ if less than 90mg combined with acetaminophen or aspirin, _______ when less than 2mg/ml in cough suppressants

A

Schedule II

Schedule III

Schedule V

98
Q

Which opioids have CYP2D6 interactions?

A

Codeine, oxycodone, hydrocodone

Less pain relief if 2D6 is inhibited

Codeine may be toxic if 2D6 extensive metabolizers

99
Q

What is Pentazocine/naloxone (TalwinNX)

A

Kappa receptor agonist and mu receptor partial agonists

Moderate pain

May be less sedating than other opioids

May have less resp distress, GI effects

May cause dysphoria

May cause withdrawal

100
Q

What is Buprenorphine?

A

Partial agonists on mu and maybe on kappa

Has ceiling effect - doesn’t cause much euphoria (so low abuse potential)

Now used for maintenance treatment of opioid addiction - decreases craving for drug

Can be injected, sublingual, or intranasal

Combined with naloxone

101
Q

New maintenance drug for opioid addiction

A

Buprenorphine

102
Q

Tramadol + antidepressants

A

Seizures

103
Q

Tramadol should not be combined with these drugs because it may cause serotonin syndrome

A

MAOIs

TCAs

SSRIs

104
Q

MOA for tramadol

A

Weak mu agonist

Inhibits NE/serotonin reuptake, contributing to analgesic effect

Generally mild side effects

105
Q

______ is not an analgesic but works as a cough suppressant

A

Dextromethorphan

106
Q

Dextromethorphan is frequently combined with _________

A

Guafenisen (expectorant)

107
Q

What is robotripping?

A

Dumb ass kids taking too much dextromethorphan

108
Q

How do opioid antagonists work?

A

Pure antagonists bind to opioid receptors and prevent agonists from acting

Mixed agonists/antagonists
• Generally partial agonists
•Alone will cause stimulation of receptor
• Antagonism if other stronger agonists are being used concurrently

May precipitate withdrawal in opioid-dependent individuals

109
Q

Drug of choice for opioid overdose

A

Naloxone (Narcan)

Can reverse respiratory depression, consciousness, awareness of pain, miosis, constipation

Injected or intranasal

Short duration of action (2 hours)

110
Q

How much naloxone should you give a druggy who is ODing?

A

Keep giving it until pupils dilate

Repeated dosing may be required

111
Q

What is Naltrexone (ReVia)

A

Used in treatment of opioid addicts, esp health care professionals

Will precipitate withdrawal

Decreases craving in recovering alcoholics

May cause liver toxicity when used chronically

Pharm III Unit I (9 decks)

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