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DTII Exam 2 > Egleton: Treatment of Pain > Flashcards

Egleton: Treatment of Pain Flashcards

1
Q

Non-opioid analgesics

A

Aspirin, Acetaminophen, NSAIDs, COX-2 inhibitors

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2
Q

Acetaminophen: major ADR

A

Hepatotoxicity (careful with alcoholics)

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3
Q

NSAIDs: major ADR

A

Gastric ulcers

Inhibit platelet aggregation (more bleeding)

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4
Q

Mu-receptors: key selective endogenous agonists

A

Endomorphin, Enkephalin, Beta-endorphin

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5
Q

Delta-receptors: key selective endogenous agonists

A

Enkephalins

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6
Q

Kappa-receptors: key selective endogenous agonists

A

Dynorphins

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7
Q

Opioid receptors:MoA

A

Activation of inwardly rectifying K+ channels
Inhibition of Ca2+ channels
Inhibition of Adenylyl cyclase (AC) {less cAMP}
{Hyperpolarize the membrane}
{Synaptic remodeling= tolerance/ addiction}

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8
Q

Agonist bias

A

They select which signaling pathways become activated upon binding to the receptor.
{form of tolerance?}

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9
Q

Morphine: use

A

Moderate to severe acute and chronic pain
Treatmetn of acute pulmonary edema
Relief of pain of MI

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10
Q

Hydromorphone: use

A

Severe pain

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11
Q

Methadone: use

A

Analgesia

Controlled withdrawal from opioids

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12
Q

Heroin: use

A

Drug of abuse

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13
Q

Oxycodone: use

A

Moderate to severe pain

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14
Q

Fentanyl: use

A

Surgery and post-surgical analgesics

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15
Q

Codeine: use

A

Analgesic

Antitussive

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16
Q

Propoxyphene

A

Weak analgesic

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17
Q

Buprenophine: use

A

Opioid withdrawal
Detoxification
Maintenance

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18
Q

Naloxone: use

A

Opioid overdose

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19
Q

Naltrexone: use

A

Opioid detoxification

Alcoholism

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20
Q

Morphine: MoA

A

Binds to Mu-receptor
(Less on Kappa-receptor in spinal cord)
Decrease spontaneous activity of gut/ CNS neurons
Prevent substance P release
{Affect respiration/ pain perception/ mood & emotion}

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21
Q

Morphine: effects:

A

CNS: Analgesia without loss of consciousness, Enphoria, Nausea/ Vomiting, Drowsiness/ Itchy nose
Eye: Mitosis (Edinger-Westphal nucleus) {Pathogmonic}
Respiration: Respiration depression (major ADR)
CV: Peripheral vasodilation, Inhibit baroreceptor reflex, Orthostatic hypotension
GI: Constipation {can be used as antidiarrheal!}
Endocrine: decrease plasma LH and Testosterone levels

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22
Q

Pathogmonic sign of Morphine intoxication

A

Mitosis

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23
Q

Morphine: tolerance and dependence

A

No tolerance for miosis, constipation, and respiratory effects
But otherwise, development is characteristic of opioids

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24
Q

Morphine: withdrawal symptoms

A 
Rebound phenomenon
Hyperalgesia {Increased sensitivity to noxious stimuli}
Hyperventilation
Dilation of pupils
Diarrhea
Dysphoria
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25
Q

Morphine: contraindication

A

Hepatic insufficiency
Respiratory insufficiency
Head injury

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26
Q

Morphine: treatment

A

Ventilation

Opiate angatonist {Naloxone}

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27
Q

Opioids for cough suppressions

A

Morphine, Codeine, Hydrocodone

{Decrease sensitivity of CNS cough center and mucosal secretion}

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28
Q

Bioavailability of Morphine

A

Low with oral formulation

Duet to 1st pass effect

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29
Q

Enzyme converting Codeine to Morphine

A

O-demethylation (CYP2D6)

30
Q

Hydromorphone

A

Hydrogenated ketone of morphine
More potent than oral morphine
Less active metabolites than morphine
For severe pain

31
Q

Methadone

A

No kappa activity (less addiction cycle)
Treat opiate withdrawal/ heroin users, and chronic pains
Metahadone maintenance

32
Q

Methadone: ADR

A

Constipation

Biliary spasms

33
Q

Methadone maintenance

A

Treat opiate withdrawal
Develops tolerance
Manages opioid craving without IV drug use
Reduce effect of opiates with cross tolerance

34
Q

Heroin

A

Only used for recreational purpose
Diacetylmorphine> 6-monoacetylmorphine> Morphine
Higher BBB penetration than morphine
Effects by 6-monoacetylmorphine and Morphine
Urine test: 6-monoacetylmorphine specific heroin metabolites

35
Q

6-monoacetylmorphine in urine test: drug of abuse?

A

Heroin

36
Q

Hydrocodone/ Acetaminophen

A

For moderate to severe pain and Cough

37
Q

Oxycodone

A

Manage moderate to severe pain
Used in combination with non-opioid analgesics
{with Ibuprofen, Aspirin, Acetaminophen etc}
Abuse potential with Oxycontin {delayed release formulation}

38
Q

Meperidine

A

Mu-opioid agonist
Normeperidine (metabolite)= CNS stimulant, not blocked by Naloxone
Doesn’t suppress cough
MAOI+Meperidine= severe rxn

39
Q

Fentanyl/ Sufenanil, Alfentanil/ Remifentanil

A 
Mu-opioid agonist
Meperidine analog
Much more potent than Morphine
For chronic pain
Less nausea than Morphine
40
Q

Codeine

A

Less potent analgesic than Morphine
Cough syrups
Metabolized to Morphine by CYP2D6 (highly polymorphic)

41
Q

Effects of CYP2D6 polymorphism: slow/ high

A

Slow metabolizers: ineffective analgesic

High metabolizers: overdose {fast conversion to morphine}

42
Q

Propoxyphene

A

Weak potency mu-agonist
For mild to moderate pain
Analgesic (used with Acetaminophen or Aspirin)
Less dependence potential

43
Q

Pentazocine

A

Kappa agonist, Weak Mu-antagonist
Analgesia, Sedation, Respiratory depression
aloxone included in Talwin to prevent drug abuse

44
Q

Buprenorphine

A 
Partial Mu agonist, Kappa-antagonist
Less effective analgesic than Morphine
Sublingal/ IM/ IV routes
For treatment of Opioid dependence
For Pregnant addicts
45
Q

Tramadol

A 
Not chemically related to opiates
Binds to Opiate receptors
Inhibit NE and 5-HT reuptake
Partial inhibition by Naloxone
ADR: Constipation, Nausea/Vomiting, Dizziness, Drowsiness
Oral
For moderate pain
Analgesics for dogs (addicts may beat pet dog to get it...)
46
Q

Opiate antagonists

A 
Naloxone (1hr), Nalmefene (10hr), Natrexone (24hr)
Highest affinity to Mu-receptor
No analgesic effects
Treat opioid poisoning
Prevent dependence addiction
Induces withdrawal right away
47
Q

For overdose patient, which opiate antagonist to give

A

Naloxone

48
Q

Dextromethorphan

A

Antitussive
Suppress response of cough center (elevate threshold)
No analgesia, Less constipation than Codeine
Not antagonized by Naloxone
Robotripping… (cough syrup abuse in teens)

49
Q

Robotripping

A

By Dextromethorphan in teens {liver damage with Acetaminophen may occur}

50
Q

Alpha 2 adrenergic agonist: MoA

A

Inhibition of pain by NE
with activation of receptors in Dorsal horn of spinal cord
For Neutopathic pain and Cancer pain

51
Q

Antidepressants(TCA/ SNRI)

A

TCA: Amitriptyline
SNRI: Venlafaxine, Duloxetine

52
Q

Antidepressants (TCA/ SNRI): MoA

A

Inhibition of NE and 5HT reuptake
Promote NE activatino of alpha 2 receptors in projection neuron of Dorsal horn and priamry afferents
Alter perception of pain
For Neuropathic pain

53
Q

Antiepileptics

A

Gabapentin, Pregabalin (alpha2delta ligands)

Carbamazepine

54
Q

Antiepileptics:MoA

A

alpha2delta ligands: Reduce activation of N and P/Q Ca2+ channels
Carbamazepine: Stabilizes inactive state of Na+v channels
For Neutopathic pain

55
Q

Gabapentin

A

For Post herpetic neuralgia and painful Diabetic neuropathy

56
Q

Pregabalin

A

For central neuropathic pain, Fibromyalgia, Post herpetic neuralgia, painful Diabetic neuropahty

57
Q

Carbamazepine

A

For Trigeminal neuralgia (1st line agent)

58
Q

Lidocaine

A

Topical

Local anesthetic

59
Q

Capsaicin

A

Topical
Chili pepper alkaloid adjunctive
TRPV1 antagonist
Ion channel expressed on afferent noticeptors

60
Q

Ketamine

A

NMDA antagonist

Blocks NMDA and Glutamate signaling

61
Q

Baclofen ***

A 
Centrally active muscle relaxants
For spasticity, Hiccups 
GABA-B receptor agonist
Facilitate spinal inhibition of motor neurons
Avoid abrupt withdrawal
62
Q

BZ-Diazepam***

A

Centrally active muscle relaxants
For muscle spasms: IV or IM
For muscle relaxant: oral as adjunct

63
Q

Carisoprodol**

A 
Not really used now....
Centrally active muscle relaxants
For acute musculoskeletal pain 
Unknown MoA
ADR: anticholinergic activity, headache, etc
Not for elderly or children under 16
64
Q

Chlorzoxazone*

A 
Not really used now....
Centrally active muscle relaxants
For acute muscle spasms and pain
Unknown  MoA
ADR: drowsiness, lightheadness
Not for elderly
65
Q

Cyclobenzaprine***

A

Centrally active muscle relaxants
For acute muscle spasms and pain and TMJ
Unknown MoA
Large half life of elimination range 8-37hrs (CYP3A4, 1A2, 2D6)
Structurally similar to TCA, same toxicities
Use with care with elderly and liver impaired

66
Q

Metaxalone***

A 
Centrally active muscle relaxants
For Muscle discomfort
Unknown MoA
ADR: Jaundice, and other CNS effects (dizziness, headache)
Careful with elderly and liver impaired
67
Q

Methocarbamol***

A 
Centrally active muscle relaxants
For muscle spasms and tetanus
Unknown MoA
Rapid onset
Careful with elderly and liver impaired
68
Q

Orphenadrine*

A

Centrally active muscle relaxants

Nah, not really important

69
Q

Tizanadine***

A

Centrally active muscle relaxants
For Tension headaches and low back pains, and muscle spasticity
Alpha adrenergic agonist
Careful with elderly and liver impaired

70
Q

1st line for Neuropathic pain

A

Antidepressants/ Ca channel alpha2delta ligands
Carbamazepine for Trigeminal neuralgia
Opioids if severe intractable pain/ Neuropathic cancer pain

71
Q

2nd line for Neuropathic pain

A 
Opioids
Other antiepileptics
NMDA antagonists
Baclofen
Adjunct Iidocaine therapy or steroid injection to joint
72
Q

1st line for Nociceptive pain

A

NSAIDs {opioids are in last resort}

DTII Exam 2 (4 decks)

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