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Pharmacology > !Neuropharm Opoids > Flashcards

!Neuropharm Opoids Flashcards

1
Q

Opoids

A

Narcotic analgesics and re indicated to reduce pain (chronic pain and palliative, but can be used to wean drug dependent patients

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2
Q

Indications for opoids

A

Pain, weaning, cough, diarrhea

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3
Q

Types of opoids

A

Morphine, fentanyl-general anesthesia , but can also reduce pain without loss of consciousness , but may induce tolerance or dependence

Codeine, heroin, methadone, meperidine, dextromethorphan, and diphenoxylate

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4
Q

MOA opoids

A

Exert their action due to their agonist activity at mu, kappa, and delta receptors

Receptor activity works to decrease synaptic transmission and inhibit release of acetylcholine, NE, 5HT, glutamate, and substance P

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5
Q

Side effects opoids

A

Respiratory depression, addiction, miosis and constipation

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6
Q

Indications for opoids

A

Pain, weaning, cough, diarrhea

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7
Q

Methadone

A

Can be used to wean patients so don’t get withdrawal syndrome

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8
Q

Loperamide and diphenoxylate

A

Treats persistent diarrhea as a common side effect is constopation

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9
Q

MOA opoids

A

Mu kappa and delta receptor agonists

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10
Q

Each receptor has distinct subtypes and different drugs may have mixed properties or partial agonist activity

A

Ok

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11
Q

Opoids and decreased synaptic transmission

A

Opoids work to open k channels and close ca channels, decreasing synaptic transmission. They inhibit release of acetylcholine, NE, 5HT, glutamate and substance p.
PANGS

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12
Q

Side effects opoids

A

Respiratory depression
Addiction
Miosis
Constipation

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13
Q

Opoid and respiratory depression

A

Direct inhibition of the brainstem respiratory center
Becomes less sensitive to carbon dioxide, leading to decreased hypoxia drive, respiratory rate, tidal exchange, and minute volume

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14
Q

Why get addicted to opoid

A

Pleasure produced by opoids, espicially when self administered
Physical dependence, as tolerance may build gradually with repeated use.

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15
Q

Opoids and constipation

A

Decrease GI motility and increases tone, specially anal sphincter

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16
Q

Miosis and opoid

A

Pinpoint pupils
Except in meperidine
Opoids act on mu and k receptors to stimulate the oculomotor nucleus to constrict pupils

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17
Q

Opoid

A

Depressant drug and analgesic that can cause constipation, miosis, nausea and vomiting

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18
Q

Opoid toxicity

A

Lead to cns depression as well as respiratoy depression.

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19
Q

Common causes of opoid toxicity

A

Overdose on morphine or heroin

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20
Q

Naloxone (narcan)

A

Mu opoid receptor antagonist used for reversal of acute life threatening opoid toxicity

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21
Q

Naltrexone

A

Also antidote for opoid toxicity
But it is an opoid receptor antagonist used for dependence treatment rather than in the emergent treatment of opoid overdose

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22
Q

Antidote for opoid toxicity

A

Naloxone

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23
Q

Naxolone

A

Opoid antagonist for reversal
To counteract life threatening depression of the cns and respiratory depression
Injected

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24
Q

Morphine

A

Potent medication used for pain relief . Opoid receptor antagonist

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25
Q

Mechanism of opoid receptor agonist morphine

A

Mu k and delta

With mu being primary target

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26
Q

Indications for morphine

A

Pain , MI

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27
Q

Pain and morphine

A

Chronic and severe pain such as with cancer, pancreatitis or traumatic injuries

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28
Q

How is morphine delivered with chronic pain

A

Patient controlled anesthesia (PCA) pump which allows continuous dosing based not he patients perceived level of pain up to a maximum dose

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29
Q

MI and morphine (also angina and pulmonary edema)

A
  • it decrease the anxiety level and pain experienced by the patient which decreases stress and sympathetic response
  • has vasodilation effects all of which decrease the oxygen demand of the heart.
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30
Q

Side effects morphine

A

Nausea and vomiting, CNS depression, biliary colic, constipation, increase intracranial pressure, pupillary constriction, hypotension

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31
Q

Why nausea and vomiting with morphine

A

May stimulate the chemoreceptors trigger zone (CTZ- in the brain. Slow administration decreases the side effect

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32
Q

Morphine and biliary colic

A

May cause spasm of the bile duct and subsequently serious abdominal pain as bile is unable to leave the gall bladder into the duodenum

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33
Q

Morphine and hypotension

A

Vasodilator effects

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34
Q

Tramadol

A

Unique, centrally acting medication that works on multiple neurotransmitters.

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35
Q

Indications for tramadol

A

Chronic pain , analgesic uses (RA, fibromyalgia)

36
Q

Tramadol is a racemic mixture of two tramadol enantiomers

A
  • one works to inhibit serotonin reputable and enhance its release
  • othe inhibits NE reuptake
37
Q

MOA tramadol

A

Weak opoid agonist at mu receptors

Influence NMDA, muscarinic and nicotonic receptors that lead to its analgesic effects

38
Q

Side effects of tramadol

A

Dose independent increased risk of seizure as this drug decreases seizure threshold in patients

39
Q

Indications for tramadol

A

Chronic pain

RA and fibromyalgia

40
Q

MOA tramadol

A

Weak opoid for mu receptors producing analgesic effects

41
Q

Tramadol has synergistic effects with numerous other receptors as it also affects what receptors

A

Nicotonic, muscarinic, NMDA

42
Q

Tramadol inhibits serotonin and NE reuptake

A

Two enantiomers. The modulation of these various receptors and NT in combination that help tramadol exhibit its effects

43
Q

Side effects tramadol

A

Seizure by lowering threshold

44
Q

Codeine

A

Strong opoid

45
Q

How does codeine work

A

Activating mu receptors in the CNS and periphery to produce analgesia

46
Q

Indication for codeine

A

Mild to moderate pain and can also be used as an antitussive

47
Q

Side effects codeine

A

Sedation, constipation, and constriction of the pupils

48
Q

What may codeine be combined with to generate a greater analgesic effect

A

Combined with non opoid analgesics such as acetaminophen and asprin

49
Q

How does codeine work

A

Activating mu opoid receptors int he CNA and periphery, producing pain relief , sedation and respiratoy depression

50
Q

Indications for codeine

A

Mild to moderate pain

Cough

51
Q

Why does codeine suppress cough

A

Acts in medulla to suppress coughing. Though the antitussive effect may be a desired outcome of codeine therapy, lack of coughing can cause secretions to a ccumulate inthe airway.

52
Q

Side effects codeine

A

Sedation, constipation, miosis

53
Q

Cosine and impaired vision

A

Miosis

54
Q

Consideration 1 of codeine

A

Close monitoring with breast feeding-can cause unsaf levels of morphine in breast milk
Babies who become intoxicated may be lethargic , sleepy, disinterested in eating and have difficulty breathing

55
Q

Consideration 2 with codeine

A

Often combined with non opoids

56
Q

Like acetaminophen or aspirins

Have differen MOA so when combined they can relieve pain better than any of the medications alone

A

Ok

57
Q

Meperidine (Demerol)

A

Strong opoid agonist that works by activating my receptors in the central nervous system and periphery to produce analgesia

58
Q

Indication for meperidine (Demerol)

A

Moderate to severe pain

Post anesthesia shivering

59
Q

Side effects meperidine

A

Sedation, constipation, CNS depression, tremors

60
Q

Who should meperidine be used cautiously in

A

Renal failure as metabolites can accumulate int he kidneys causing toxicity

61
Q

What drug should meperidine not be taken with

A

MAO inhibitors, DDRI, tricyclic antidepressants, due to increased risk for serotonin syndrome, coma and death

62
Q

Mechanism of meperidine

A

Opoid receptor antagonist
Activating mu opoid receptor in cns and periphery producing pain relief, sedation, respiratory distress, cough suppression and decreased intestinal peristalsis

63
Q

Indications for meperidine

A

Moderate to severe pain

Post anesthetic shivering

64
Q

How does meperidine help with post anesthesia shivering

A

Reduce shivering threshold

65
Q

Side effects meperidine

A

Tremors, constipatio, CNS depressant, sedation

66
Q

Considerations with meperidine 1

A

Short term administration-prevent toxicity take less than 48 hrs at a time
Do not excess 600 mg/24 hour

67
Q

Why is meperidine preferred for obstetric use

A

Less likely to depress fetal respiration and uterine contractions, it is often the preferred opoid for obstetric use

68
Q

Meperidine consideration 2

A

Increased risk of serotonin syndrome when taken with MAO inhibitors , SSRI, tricyclic antidepressants

Get excessive activation or serotonin receptors and decreased reuptake of serotonin. As a result there is an increased risk for serotonin syndrome coma and death

69
Q

When taken with consideration 3 for meperidine

A

Does NOT cause miosis

Unlike other opoid medications, no miosis or pupil constriction

70
Q

Consideration 4 meperidine

A

Renal failure increases toxicity risk

Used cautiously in patients with renal failure as metabolites can accumulate in the kidneys causing toxicity

71
Q

Butorphanol

A

Medication indicated to treat migraine headaches and severe pain in patients and is helpful in labor pains

72
Q

MOA butorphanol

A

Mixed actions at the receptor level and acts as a partial agonist at mu and k receptors, while also being a competitive antagonist at mu receptors

73
Q

Bc of butorphanol partial agonist/antagonist activity at mu receptors, it causes __ respiratory depression than full opoid agonist drugs

A

Less

74
Q

Side effect of butorphanol

A

Withdrawal

Usually when patient also being treated with full opoid agonist medication

75
Q

Why get adverse effects with mutorphanol

A

Competitive antagonist activity at mu receptors, competing with the adjunct opoid drug being taken, leading to withdrawal symptoms

76
Q

Indications for butorphanol

A

Migraine
Severe pain
Labor

77
Q

Butorphanol is more effective in women or men

A

Women

78
Q

MOA butorphanol

A

Partial agonist at mu and full agonist at kappa receptors

Less respiratory depression due to drugs partial agonist/antagonist properties at mu opoid receptors

79
Q

Side effect butorphanol

A

Withdrawal
If taking a full opoid agonist concurrently
At mu receptors butorphanol acts as a competitive antagonist and partial agonist

Thus.a patient also taking a fulll opoid agonist medication would experience butorphanol competing for opoid receptors, leading to withdrawal symptoms.

80
Q

How treat withdrawal symptoms of butorphanol

A

Naloxone however overdose isn’t easily reversed

81
Q

Naloxone (narcan)

A

Opoid antagonist that works by blocking opoid receptors int he body, effectively reversing side effects associated with opoid use, such as sedation and respiratory depression

82
Q

Use of naloxone

A

Reverse opoid induced CNS depression and should be administered every 2-3 min until the desired patient response is observed.

83
Q

Side effects naloxone (narcan)

A

Severe nausea, vomiting, excitability, symptoms of opoid withdrawal

84
Q

MOA naloxone

A

Competitive opoid receptor antagonist
It is structurally similar to opoid drugs and works by competing with these medications for opoid receptor sites int he body

Opoid antagonist-blocks the action of opoid , effectively reversing side effects associated with these medications, such as respiratory depression, sedation, coma, and analgesia

85
Q

Indications for naloxone

A

Opoid induced CNS depression

Reverses sedation , respiratory depression, and other CNS effects associated with opoid administration. If given prior to administration of an opoid , naloxone will block opoid receptors and will prevent the opoids drug from taking effect

86
Q

Side effects naloxone

A

Severe nausea and vomiting (if administered too rapidly0
)
Excitable state
Opoid withdrawal symptoms

87
Q

Considerations naloxone

A

Repeated dosing often required

IgE every 2-3 minutes until the desired response is obtained/observed

Pharmacology (52 decks)

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