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!Narcotic Analgesics Flashcards

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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
Postsynaptic mu receptor activation increases K effluent, which decreases postsynaptoc response to extraordinary NT
Ok
26
Effects of opoids
Analgesic(stimulant) Antidiarrheal(stimulant) Analgesic(dampen) Antitussive(dampen)
27
Morphine good amount
Decrease in pain perception (nociception)
28
Too much morphine
Respiratory depression | Oversee
29
Morphine, methadone, fentanyl MOA
Strong mu receptor agonist and variable affinity delta and k receptors
30
Effects of morphine, methadone and fentanyl
Analgesia, relief of anxiety, sedation, slowed GI transit
31
Clinical applications of morphine , methadone, fentanyl
Severe pain, adjunct in anesthesia (fentanyl, morphine), pulmonary edema (morphine only) maintence in rehabilitation programs (methadone only)
32
Pharmacokinetics morphine , methadone, fentanyl
First pass effect | Duration 1-4 hours(except methadone which is 4-6)
33
Toxicity morphine , methadone, fentanyl
Respiratoy depression, severe constipation, addiction liability, convulsion
34
Hydromorphone, oxymorphone
Like morphine in efficacy, but higher potency
35
Meperdine
Strong agonist with anticholinergic effects
36
Oxycodone
Dose dependent analgesia
37
Sufentanil, alfentanil, remifentanil
Like fentanyl but shorter duration of action
38
Codeine , hydrocodone
Opoid agonists | Less efficacious than morphine can antagonize strong agonists
39
Effects of codeine and hydrocodone
Like strong agonists, and weaker effects
40
Clinical applications codeine, hydrocodone
Mild-moderate pain, cough(codeine)
41
Pharmacokinetics codeine, hydrocodone
Like strong agonists
42
Toxicity codeine hydrocodone
Dependent on genetic variation or metabolism
43
Buprenorphine
Mixed opoid agonist-antagonist | Partial mu agonist and k antagonist
44
Effects buprenorphine
Like strong agonists but can antagonist their effects and also reduces craving for alcohol
45
Clinical application buprenorphine
Moderate pain and some maintence rehabilitation programs
46
Pharmacokinetics buprenorphine
Long duration of action 4-8 h | May precipitate abstinence syndrome
47
Nalbuphine
Mixed opoid agonist antagonist K agonist and mu antagonist
48
Effects of nalbuphine
Like strong agonists but can antagonize their effects also reduces craving for alcohol
49
Clinical application nalbuphine
Moderate pain
50
Nalbuphine pharmacokinetics
Long duration of action 4-8 h may precipitate abstinence syndrome
51
Dextromethrophan
Antitussives | Poorly understood but strong and partial mu agonists are also effective antitussives
52
Action dextromethorphan
Reduces cough reflex+ dextromethorphan, lecopropoxyphene not analgesic
53
Clinical application dextromethorphan
Acute debilitating cough
54
Destromethorphan pharmacokinetics
Duration 30-60 min
55
Toxicity dextromethorphan
Minimal when taken as directed
56
Naloxone
Opoid antagonists Antagonist at mu, delta and kappa
57
Naloxone effects
Rapidly antagonizes all opoid effects
58
Clinical applications naloxone
Opoid overdose
59
Pharmacokinetics naloxone
Duration 1-2 hours (may have to be repeated when treating overdose) and
60
Toxicity naloxone
Precipitates abstinence syndrome in dependent users
61
Tapentadol MOA
Mu agonist strong NET inhibitor
62
Effects tapentadol
Analgesia
63
Clinical use of tapentadol
Moderate pain
64
Pharmacokinetics tapentadol
4-6 hours
65
Toxicity tapentadol
Headache, nausea, and vomiting , possible dependence
66
Tramadol MOA
Mixed effects, weak mu agonist, moderate SERT inhibitor, weak NET inhibitor
67
Effects tramadol
Analgesia
68
Clinical use of tramadol
Moderate pain, adjunct to opoids in chronic syndromes
69
Pharmacokinetics tramadol
4-6 hours
70
Tramadol toxicity
Seizures, risk of serotonin syndrome
71
Mu receptor
Supraspinal and spinal analgesia, inhibition of respiration, slowed GI transit, modulation of hormone and NT release
72
Delta receptor
Supraspinal and spinal analgesia, modulation of hormones and NT release
73
Kappa receptor
Supraspinal and spinal analgesia, psychotomimetic effects, slowed GI transit
74
Endogenous opoid peptide affinity mu receptors
Endorphins>enkephalins>dynorphins
75
Delta receptor endogenous opoid peptide affinity
Enkephalins>endorphins and dynorphins
76
Kappa receptor
Dynorphins>> endorphins and enkephalins
77
Morphine receptor
Mu and kappa
78
Hydromorphone. Receptor
Mu
79
Oxymorphone receptor
Mu
80
Methadone receptor
Mu
81
Meperidine receptor
Mu
82
Fentanyl receptor
Mu
83
Sufentanil receptor
Mu, delta, kappa
84
Alfentanil receptor
Mu
85
Remifentanil receptor
Mu
86
Levophanol receptor
Mu
87
Levophanol receptor
Mu
88
Codeine receptor
Activate or inactive mu
89
Hydrocodone receptor
Plus or minus mu
90
Oxycodone
Mu
91
Pentazocine
Plus minus mu | Plus kapp
92
Nelbuphine
Negative mu | Plus kappa
93
Nelbuphine
Minus mu | Plus kappa
94
Beprenorphine
Plus minus mu Minus delta Minus kappa
95
Butorphanol
Plus minus mu | Plus kappa
96
Alll of them have high efficacy except which
Low codeine Moderate hydrocodone and pentazoicine
97
Methadone
Mu opoid full agonist
98
Buprenorphine
Partial agonist at mu kappa and delta
99
Naltrexone
Partial agonist kappa and antagonist at mu
100
Nalmefene
Antagonist nalmefene | Partial agonist kappa
101
Full agonist
Methadone
102
Partial agonist
Buprenorphine
103
Antagonist
Naloxone
104
Adverse effects with acute use
``` Respiratory depression Nausea/vomiting Pruritus Urticaria Constipation Urinary retention Delirium Sedation Myoclonus Seizures ```
105
Adverse effects with chronic use
``` Hypogonadism Immunosuppression Increased feeding Increased growth hormone secretion Withdrawal effects Tolerance dependence Abuse addiction Hyperalgesia Impairment when driving ```
106
Methadone addiction
Opoid
107
Buprenorphine addiction
Opoid
108
Naltrexone addiction
Alcohol and opoid
109
Nalmefene addiction
Nalmefene
110
Oxycodone side effects central
Hallucination, confusion, fainting, dizziness
111
Oxycodone skin advers
Hives rash
112
Oxycodone respiratory side effects
Difficulty breathing | Slower breathing
113
Face side effects oxycodone
Swelling
114
Eyes side effect oxycodone
Swelling smaller pupil
115
Throat oxycodone
Hoarseness welling difficult swallowing
116
Heart oxycodone
Fast or slow heart beat
117
Muscular side effects oxycodone
Seizures
118
Contraindications for morphine
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
Mu receptor location
Pre and post synaptic on primary afferent neurons and peripheral sensory neurons
120
Endogenous ligand mu
B endorphin Leu enkephlain Met ankephalin Dynorphin
121
Clinical effect mu
``` Supraspinal analgesia Sedation Spinal analgesia Respiratory depression Bradycardia Hypothermia Miosis Euphoria Pruritus Nausea and vomiting Constipation Urinary retention ```
122
Delta receptor
Olfactory bulb Cerebral cortec Presynaptic on primary afferent neurons , motor integrationa Nd nociceptors areas
123
Endogenous ligand delte
Leu enkephalin | Met enkephalins
124
Clinical effect delta
``` Supraspinal analgesia Spinal analgesia Respiratory depression Constipation Physical dependence ```
125
Kappa
Hypothalamus | Nociceptors areas
126
Endogenous ligand kappa
Dynorphin
127
Clinical effect kappa
``` Supraspinal analgesia Sedation Spinal analgesia Dysphagia Psychotomimetic effects Decrease vasopressin and diuretics ```

Pharmacology (52 decks)

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