Pain Drugs Flashcards

1
Q

List the Non-Opioid Analgesics

A
  1. Aspirin
  2. Acetaminophen
  3. NSAIDs
  4. Cox-2 Inhibitors
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2
Q

What is the MOA of Non-Opioid Analgesics?

A

Target inflammatory components of the pain cascade

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3
Q

What is the use of Non-Opioid Analgesics?

A

Mild to Moderate Pain

-Ex: soft tissue injury, sprain, strain, HA, arthritis

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4
Q

Non-Opioid Analgesics may be beneficial when used synergistically with what types of drugs?

A

Opioids

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5
Q

What is a major side effect of Acetaminophen?

A

Hepatotoxicity/Liver Failure

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6
Q

What is a major side effect of Aspirin and NSAIDs

A
  1. Gastric Ulcers

2. Inhibition of Platelet aggregation

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7
Q

What is a contraindication of Acetaminophen?

A

Alcoholics or Liver Disease Pts

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8
Q

What is a contraindication of NSAIDs

A

Use in patients who are taking Aspirin for CV protection

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9
Q

What are Opioid Receptors?

A

The opioid receptors are G Protein Coupled Receptors lined to Gi/o. There are 3 types: Mu, Delta and Kappa

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10
Q

What happens upon binding of an Opioid Receptor?

A

Activation results in inward rectifying K channels, inhibition of Ca channels, and inhibition of Adenylyl Cyclase

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11
Q

Where are Mu receptors found?

A
  1. CNS (neocortex, Thalamus, Hippocampus/Amygdala, Nucleus Acumbens)
  2. Myenteric Neurons of the Gut
  3. Vas Deferens
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12
Q

What are the physiological effects of Mu Receptor Activation?

A
  1. Supraspinal analgesia
  2. Respiratory Depression
  3. Euphoria/Dependence
  4. Constriction of the Gastric Tract
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13
Q

Where are Delta Receptors found?

A
  1. Olfactory Bulb
  2. Nucleus Acumbens
  3. Caudate and Putamen
  4. Neocortex
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14
Q

What is the physiological effect of Delta Receptor activation?

A
  1. Affects Behavior
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15
Q

Where are Kappa receptors found?

A
  1. Cortex
  2. Nucleus Acumbens
  3. Spinal Cord
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16
Q

What is the physiological effect of Kappa Receptor activation?

A
  1. Spinal Cord Analgesia

2. Sedation

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17
Q

What are the endogenous agonists of Mu receptors?

A
  1. Endomorphin 1 and 2
  2. Enkephalins
  3. B-endorphin
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18
Q

What are the endogenous agonists of Delta receptors?

A
  1. Enkphalins
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19
Q

What are the endogenous agonists of Kappa receptors?

A
  1. Dynorphins
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20
Q

Which drugs are Mu receptor agonists?

A
  1. Morphine
  2. Fentanyl
  3. Methadone
  4. Meperidine
  5. Buprenorphine
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21
Q

Which drugs are Mu Antagonists?

A
  1. Naloxone

2. Naltrexone

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22
Q

Which drugs are Delta Antagonists?

A
  1. Naltrindole
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23
Q

Which drugs are Kappa Agonists?

A
  1. Butorphanol
  2. Pentazocine
  3. Nalbuphrine
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24
Q

What are the strong Opioid Agonists?

A
  1. Morphine
  2. Hydromorphone
  3. Hydrocodone
  4. Methadone
  5. Heroin
  6. Oxycodone
  7. Meperidine
  8. Fentanyl + Analogs
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25
Q

Which drug is used for moderate-severe acute and chronic pain and for treatment of pain from PE and MI?

A

Morphine

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26
Q

Which drug is good for chronic pain and antitussive effects?

A

Hydrocodone

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27
Q

Which drug is good for severe pain? This drug is also a ketone of Morphine, is 7x stronger and has fewer active metabolites.

A

Hydromorphone

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28
Q

Which drug causes analgesia and is good for controlled withdrawal from opioid due to its long T1/2 and slow tolerance rate?

A

Methadone

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29
Q

Oxycodone is used for what?

A

Moderate-Severe pain

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30
Q

Which drug is used for acute analgesia, especially for OB?

A

Meperidine

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31
Q

Which drug is goof for surgery and post-surgery analgesia, and chronic pain for cancer patients (usually as a patch since the duration is short)?

A

Fentanyl + analogs

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32
Q

Which drugs are moderate-low agonists?

A
  1. Codeine

2. Propoxyphene

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33
Q

Which drug is used as an analgesic + antitussive?

A

Codeine

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34
Q

Which drugs are mixed agonists/antagonists (partial agonists)?

A
  1. Buprenorphine
  2. Pentazocine
  3. Butorphanol
  4. Nalbuphine
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35
Q

Which drug is a partial agonist at Mu Receptors?

A

Buprenorphine

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36
Q

Pentazocine, Butorphanol and Nalbuphine are partial agonists at what receptor?

A

Kappa

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37
Q

What drug is used for opioid withdrawal, detoxification and maintenance?

A

Buprenorphine

38
Q

What are the Opioid Antagonists?

A
  1. Naloxone
  2. Naltrexone
  3. Nalmefene
39
Q

Which drug is used for Opioid Overdose?

A

Naloxone

40
Q

Which drug is used for Opioid detoxification and alcoholism?

A

Naltrexone

41
Q

What is the MOA of Morphine?

A

Inhibits neurons in the CNS, GI and Spinal Cord (some Kappa activity in addition to Mu) and prevents release of substance P

42
Q

What are the CNS effects of Morphine?

A
  1. Analgesia
  2. Drowsiness/ Itchy nose
  3. Euphoria and Dysphoria
  4. Nausea and Vomiting
43
Q

What is a sign of Opioid Intoxication?

A

Miosis (excitement at Edinger-Westphal)

44
Q

What is the cause of death in Opioid overdose?

A

Respiratory Depression

45
Q

What are the cardio effects of Morphine?

A
  1. Vasodilation

2. Orthostatic Hypotension

46
Q

What is the GI effect of Morphine?

A
  1. Constipation (decreased motility, tone and secretions)

2. Increased anal sphincter tone and biliary pressure

47
Q

What is the Endocrine effect of Morphine?

A
  1. Decreased LH and Testosterone
  2. Menstrual Irregularities
  3. Male Impotence
48
Q

What effects of opioids are not effected by tolerance?

A
  1. Miosis
  2. Constipation
  3. Respiratory Depression
49
Q

What are withdrawal symptoms of Morphine?

A
  1. Hyperalgesia
  2. Hyperventilation
  3. Dilation of Pupils
  4. Diarrhea
  5. Dysphoria
50
Q

Which drugs potentiate effects of Morphine?

A
  1. Phenothiazines (increase sedative)
  2. MAOIs
  3. TCAs
  4. Amphetamine (increases analgesia)
51
Q

What is the treatment for Opioid Poisoning?

A
  1. Ventillation

2. IV Antagonist (Naloxone)

52
Q

What are the contraindications of opioid use?

A
  1. Liver Issues
  2. Respiratory Insufficiency (obesity, emphysema)
  3. Head injury
53
Q

Which enzyme is important for the breakdown of Morphine into its active metabolites?

A

CYP2D6 (O-demethylation)

54
Q

What metabolite can be detected in the urine of Heroin users?

A

6-monoacetylmorphine

55
Q

Constipation and biliary spasms are a predominant side effect of which drug?

A

Methadone

56
Q

What are the metabolites of Heroin that can cross the BBB (at a higher % than Morphine)?

A

Diacetylmorphine –> 6-monoacetlymorphine (causes effects) and Morphine (causes effects)

57
Q

Lortab and Vicoden, which have a similar effectiveness to Morphine, are combinations of which drugs?

A

Hydrocodone + Acetaminophen

58
Q

What is the delayed release form of Oxycodone?

A

Oxycontin (high abuse potential)

59
Q

What is the extended release formula of Hydrocodone that has a high OD Potential?

A

Zohydro

60
Q

Phenylpiperdine analgesics include which drugs?

A

Fentanyl + Analogs and Meperidine

61
Q

The excitement at toxic doses of what opioid are not blocked by Naloxone?

A

Meperidine

62
Q

Which combination of drugs can result in a severe reaction of excitation, delirium, hyperpyrexia, convulsions and respiratory depression?

A

Meperidine + MAOIs

63
Q

Fentanyl is an analog of what drug?

A

Meperidine

64
Q

Which drug for chronic pain produces less nausea than Morphine?

A

Fentanyl

65
Q

Which fentanyl derivative is 6000x Morphine, used for surgical anesthesia and may –> respiratory depression and chest wall rigidity?

A

Sufentanil

66
Q

Which fentanyl derivative is short acting?

A

Remifentanil

67
Q

Which drug is ineffective in slow metabolizers but may lead to overdose in rapid metabolizers, and which enzyme is responsible for its breakdown to Morphine?

A

Codein, CYP2D6

68
Q

Which opioid drug is good for its low potential of dependance and weak analgesic effects?

A

Propoxyphene

69
Q

What is the use/effects of Pentazocine?

A

Analgesia, sedation, respiratory depression; used for acute pain

70
Q

What is a risk of Pentazocine?

A

May –> withdrawal in patients who are taking Opioids

71
Q

What is Talwin?

A

A Combination drug including Pentazocine that is good to prevent drug abuse

72
Q

What drug may lead to euphoria in patients taking Pentazocine?

A

Tripelennamine (antihistamine)

73
Q

What drug is good for pregnant addicts?

A

Buprenorphine

74
Q

Which drug, that is not an opioid, bind to the opioid receptor to inhibit NE and 5HT release in the treatment of neuropathic pain?

A

Tramadol

75
Q

Which drug may lead to immediate/violent severe opioid withdrawal symptoms?

A

Naloxone

76
Q

What is Dextromethorphan?

A

A synthetic derivative of morphine that suppresses cough

77
Q

What is the function of Diphenoxylate and Loperamide?

A

Antidiarrheal; acting on mu receptors of the GI nerve plexus

78
Q

What is Clonidine?

A

An Alpha 2 Adrenergic Agonist

79
Q

What is the MOA of Clonidine?

A

–> increased NE which inhibits pain by activating receptors in the Dorsal Horn and Primary Afferents

80
Q

What is the use of Clonidine?

A

Neuropathic or Cancer Pain

81
Q

What antidepressants may be used for pain?

A
  1. TCAs (Amitriptyline)

2. SNRIs (Venlafaxine and Duloxetine)

82
Q

What is the MOA of antidepressants in treating pain?

A

Inhibit the reuptake of NE and 5HT –> promotes NE activation of neurons in the dorsal horn and primary afferents; also may be important in perception of pain

83
Q

What is the use of TCAs and SNRIs?

A

Neuropathic Pain

84
Q

What are the anti-epileptics used for pain?

A
  1. Alpha-2-Delta Ligands (Gabapentin and Pregabalin)

2. Carbamazepine

85
Q

What is the MOA of Gabapentin and Pregabalin?

A

Reduce activation of VG-Ca Channels

86
Q

What is the MOA of Carbamazepine?

A

Stabilizes inactive state of VG-Na Channels

87
Q

What is the use of Carbamazepine?

A

Neuropathic Pain and Trigeminal Neuralgia

88
Q

What is the use of Gabapentin and Pregabalin?

A
  1. Post-Herpetic Neuralgia
  2. Diabetic Neuropathy
  3. Fibromyalgia
89
Q

How does the onset of Pregabalin compare to Gabapentin?

A

It is faster

90
Q

What are Lidocaine and Capsaicin?

A

Topical anesthetics (TRPV1 Antagonist)

91
Q

What is Katamine?

A

An NMDA Antagonist that decreases Glutamate signaling