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Pharmacology > !Narcotic Analgesics > Flashcards

!Narcotic Analgesics Flashcards

1
Q

Analgesia

A

Relief of pain without loss of consciousness

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2
Q

Opium

A

Natural extract from poppy plant used for social and medicinal purpose for thousands of years to produce euphoria, analgesia, sleep and to prevent diarrhea

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3
Q

Opoid drugs

A

Natural+synthetic morphine-like drugs

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4
Q

Narcotic

A

Opoid analgesics

Compounds related to opium and applies to any substance whether endogenous synthetic or semisynthetic drugs that produce morphine like effects that are blocked by antagonists such as naloxone

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5
Q

Antagonist to narcotics

A

Naloxone

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6
Q

Opium effects

A

Euphoria, analgesia and sleep, and to prevent diarrhea

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7
Q

Opiates

A

Drugs derived from opium, and they clued the natural products morphine, codeine, and the wine, and may semisynthetic derivatives such as buprenorphine

Endogenous ones are naturally occurring ligand for opoid receptors

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8
Q

What are opoid analgesics used for

A

Severe pain

Moderate pain

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9
Q

How do opoids such as heroin and morphine work

A

Mimicking naturally occurring substances called endogenous opoid peptides or endorphins

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10
Q

Phenanthrenes

A 
Morphine 
Codeine
Hydrocodone
Hydromorphone
Levophanol
Oxycodone
Oxymorphone
Beprenorphone
Nalbuphine
Butorphanol
Naloxone
Heroin
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11
Q

Benzomorphans

A

Pentazocine
Diphenoxylate
Loperamide

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12
Q

Phenylpiperidines

A

Meperidine
Fentanyl
Sufentanil
Remifentanil

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13
Q

Diphenylheptanes

A

Methadone

Propoxyphene

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14
Q

Natural opium alkaloids

A

Morphine, codeine

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15
Q

Semisynthetic opiates

A

Hydromorphone, oxymorphones

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16
Q

Synthetic opoids

A

Pethidine, tramadol, methadone, fentanyl, alfentanil, remifentanil

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17
Q

Opoid agonist-antagonists

A

Pentazocine

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18
Q

Partial mu receptor agonist

A

Buprenorphine

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19
Q

Mu receptor antagonist

A

Naltrexone

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20
Q

Analgesics

A 
Morphine
Hydromorphinemethadone
Meperidine
Fentanyl
Codeine
Oxycodone
Hydrocodone
Propoxyphene
Dextromethorphan
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21
Q

Mixed receptor agonist antagonists

A

Pentazocine
Nalbuphine
Buprenorphine
Butorphanol

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22
Q

Opoid antagonists

A

Naloxone

Naltrexone

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23
Q

Indications for use of hospital narcotics to relieve pain

A 
MI
Sickle cell crisis
Positive operative procedures
Trauma
Cancer
Kidney stones
Back pain 
Adjunct to general anesthesia
Epidural
Palliative care
Antitussice
Antidiarrheal
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24
Q

MOA

A

Presynaptic mu receptor activation inhibits calcium influx into sensory neurons, which decreases NT release
Postsynaptic mu receptor activation increases K efflux, which decrease postsynaptic response to excitatory Neurotransmission

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25
Q

Postsynaptic mu receptor activation increases K effluent, which decreases postsynaptoc response to extraordinary NT

A

Ok

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26
Q

Effects of opoids

A

Analgesic(stimulant)
Antidiarrheal(stimulant)
Analgesic(dampen)
Antitussive(dampen)

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27
Q

Morphine good amount

A

Decrease in pain perception (nociception)

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28
Q

Too much morphine

A

Respiratory depression

Oversee

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29
Q

Morphine, methadone, fentanyl MOA

A

Strong mu receptor agonist and variable affinity delta and k receptors

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30
Q

Effects of morphine, methadone and fentanyl

A

Analgesia, relief of anxiety, sedation, slowed GI transit

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31
Q

Clinical applications of morphine , methadone, fentanyl

A

Severe pain, adjunct in anesthesia (fentanyl, morphine), pulmonary edema (morphine only) maintence in rehabilitation programs (methadone only)

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32
Q

Pharmacokinetics morphine , methadone, fentanyl

A

First pass effect

Duration 1-4 hours(except methadone which is 4-6)

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33
Q

Toxicity morphine , methadone, fentanyl

A

Respiratoy depression, severe constipation, addiction liability, convulsion

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34
Q

Hydromorphone, oxymorphone

A

Like morphine in efficacy, but higher potency

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35
Q

Meperdine

A

Strong agonist with anticholinergic effects

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36
Q

Oxycodone

A

Dose dependent analgesia

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37
Q

Sufentanil, alfentanil, remifentanil

A

Like fentanyl but shorter duration of action

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38
Q

Codeine , hydrocodone

A

Opoid agonists

Less efficacious than morphine can antagonize strong agonists

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39
Q

Effects of codeine and hydrocodone

A

Like strong agonists, and weaker effects

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40
Q

Clinical applications codeine, hydrocodone

A

Mild-moderate pain, cough(codeine)

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41
Q

Pharmacokinetics codeine, hydrocodone

A

Like strong agonists

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42
Q

Toxicity codeine hydrocodone

A

Dependent on genetic variation or metabolism

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43
Q

Buprenorphine

A

Mixed opoid agonist-antagonist

Partial mu agonist and k antagonist

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44
Q

Effects buprenorphine

A

Like strong agonists but can antagonist their effects and also reduces craving for alcohol

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45
Q

Clinical application buprenorphine

A

Moderate pain and some maintence rehabilitation programs

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46
Q

Pharmacokinetics buprenorphine

A

Long duration of action 4-8 h

May precipitate abstinence syndrome

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47
Q

Nalbuphine

A

Mixed opoid agonist antagonist

K agonist and mu antagonist

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48
Q

Effects of nalbuphine

A

Like strong agonists but can antagonize their effects also reduces craving for alcohol

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49
Q

Clinical application nalbuphine

A

Moderate pain

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50
Q

Nalbuphine pharmacokinetics

A

Long duration of action 4-8 h may precipitate abstinence syndrome

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51
Q

Dextromethrophan

A

Antitussives

Poorly understood but strong and partial mu agonists are also effective antitussives

52
Q

Action dextromethorphan

A

Reduces cough reflex+ dextromethorphan, lecopropoxyphene not analgesic

53
Q

Clinical application dextromethorphan

A

Acute debilitating cough

54
Q

Destromethorphan pharmacokinetics

A

Duration 30-60 min

55
Q

Toxicity dextromethorphan

A

Minimal when taken as directed

56
Q

Naloxone

A

Opoid antagonists

Antagonist at mu, delta and kappa

57
Q

Naloxone effects

A

Rapidly antagonizes all opoid effects

58
Q

Clinical applications naloxone

A

Opoid overdose

59
Q

Pharmacokinetics naloxone

A

Duration 1-2 hours (may have to be repeated when treating overdose) and

60
Q

Toxicity naloxone

A

Precipitates abstinence syndrome in dependent users

61
Q

Tapentadol MOA

A

Mu agonist strong NET inhibitor

62
Q

Effects tapentadol

A

Analgesia

63
Q

Clinical use of tapentadol

A

Moderate pain

64
Q

Pharmacokinetics tapentadol

A

4-6 hours

65
Q

Toxicity tapentadol

A

Headache, nausea, and vomiting , possible dependence

66
Q

Tramadol MOA

A

Mixed effects, weak mu agonist, moderate SERT inhibitor, weak NET inhibitor

67
Q

Effects tramadol

A

Analgesia

68
Q

Clinical use of tramadol

A

Moderate pain, adjunct to opoids in chronic syndromes

69
Q

Pharmacokinetics tramadol

A

4-6 hours

70
Q

Tramadol toxicity

A

Seizures, risk of serotonin syndrome

71
Q

Mu receptor

A

Supraspinal and spinal analgesia, inhibition of respiration, slowed GI transit, modulation of hormone and NT release

72
Q

Delta receptor

A

Supraspinal and spinal analgesia, modulation of hormones and NT release

73
Q

Kappa receptor

A

Supraspinal and spinal analgesia, psychotomimetic effects, slowed GI transit

74
Q

Endogenous opoid peptide affinity mu receptors

A

Endorphins>enkephalins>dynorphins

75
Q

Delta receptor endogenous opoid peptide affinity

A

Enkephalins>endorphins and dynorphins

76
Q

Kappa receptor

A

Dynorphins» endorphins and enkephalins

77
Q

Morphine receptor

A

Mu and kappa

78
Q

Hydromorphone. Receptor

A

Mu

79
Q

Oxymorphone receptor

A

Mu

80
Q

Methadone receptor

A

Mu

81
Q

Meperidine receptor

A

Mu

82
Q

Fentanyl receptor

A

Mu

83
Q

Sufentanil receptor

A

Mu, delta, kappa

84
Q

Alfentanil receptor

A

Mu

85
Q

Remifentanil receptor

A

Mu

86
Q

Levophanol receptor

A

Mu

87
Q

Levophanol receptor

A

Mu

88
Q

Codeine receptor

A

Activate or inactive mu

89
Q

Hydrocodone receptor

A

Plus or minus mu

90
Q

Oxycodone

A

Mu

91
Q

Pentazocine

A

Plus minus mu

Plus kapp

92
Q

Nelbuphine

A

Negative mu

Plus kappa

93
Q

Nelbuphine

A

Minus mu

Plus kappa

94
Q

Beprenorphine

A

Plus minus mu
Minus delta
Minus kappa

95
Q

Butorphanol

A

Plus minus mu

Plus kappa

96
Q

Alll of them have high efficacy except which

A

Low codeine

Moderate hydrocodone and pentazoicine

97
Q

Methadone

A

Mu opoid full agonist

98
Q

Buprenorphine

A

Partial agonist at mu kappa and delta

99
Q

Naltrexone

A

Partial agonist kappa and antagonist at mu

100
Q

Nalmefene

A

Antagonist nalmefene

Partial agonist kappa

101
Q

Full agonist

A

Methadone

102
Q

Partial agonist

A

Buprenorphine

103
Q

Antagonist

A

Naloxone

104
Q

Adverse effects with acute use

A 
Respiratory depression
Nausea/vomiting
Pruritus
Urticaria
Constipation
Urinary retention 
Delirium
Sedation
Myoclonus
Seizures
105
Q

Adverse effects with chronic use

A 
Hypogonadism 
Immunosuppression 
Increased feeding
Increased growth hormone secretion 
Withdrawal effects
Tolerance dependence
Abuse addiction 
Hyperalgesia
Impairment when driving
106
Q

Methadone addiction

A

Opoid

107
Q

Buprenorphine addiction

A

Opoid

108
Q

Naltrexone addiction

A

Alcohol and opoid

109
Q

Nalmefene addiction

A

Nalmefene

110
Q

Oxycodone side effects central

A

Hallucination, confusion, fainting, dizziness

111
Q

Oxycodone skin advers

A

Hives rash

112
Q

Oxycodone respiratory side effects

A

Difficulty breathing

Slower breathing

113
Q

Face side effects oxycodone

A

Swelling

114
Q

Eyes side effect oxycodone

A

Swelling smaller pupil

115
Q

Throat oxycodone

A

Hoarseness welling difficult swallowing

116
Q

Heart oxycodone

A

Fast or slow heart beat

117
Q

Muscular side effects oxycodone

A

Seizures

118
Q

Contraindications for morphine

A

Acute respiratory depression
Renal failure (from accumulation of the metabolistes morphine-3-glucuronide and morphine-6-glucuronide)
-chemical toxicity
-raised intracranial pressure, including head injury (risk of worsening respiratory depression
-biliary colic
-although it has previously been thought that morphone was contraindicated in acute pancreatitis, a review of the literature shows no evidence for this

119
Q

Mu receptor location

A

Pre and post synaptic on primary afferent neurons and peripheral sensory neurons

120
Q

Endogenous ligand mu

A

B endorphin
Leu enkephlain
Met ankephalin
Dynorphin

121
Q

Clinical effect mu

A 
Supraspinal analgesia
Sedation 
Spinal analgesia
Respiratory depression 
Bradycardia
Hypothermia
Miosis
Euphoria
Pruritus
Nausea and vomiting
Constipation 
Urinary retention
122
Q

Delta receptor

A

Olfactory bulb
Cerebral cortec
Presynaptic on primary afferent neurons , motor integrationa Nd nociceptors areas

123
Q

Endogenous ligand delte

A

Leu enkephalin

Met enkephalins

124
Q

Clinical effect delta

A 
Supraspinal analgesia
Spinal analgesia
Respiratory depression 
Constipation 
Physical dependence
125
Q

Kappa

A

Hypothalamus

Nociceptors areas

126
Q

Endogenous ligand kappa

A

Dynorphin

127
Q

Clinical effect kappa

A 
Supraspinal analgesia
Sedation
Spinal analgesia
Dysphagia
Psychotomimetic effects
Decrease vasopressin and diuretics

Pharmacology (52 decks)

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