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
Morphine: contraindication
Hepatic insufficiency Respiratory insufficiency Head injury
26
Morphine: treatment
Ventilation | Opiate angatonist {Naloxone}
27
Opioids for cough suppressions
Morphine, Codeine, Hydrocodone | {Decrease sensitivity of CNS cough center and mucosal secretion}
28
Bioavailability of Morphine
Low with oral formulation | Duet to 1st pass effect
29
Enzyme converting Codeine to Morphine
O-demethylation (CYP2D6)
30
Hydromorphone
Hydrogenated ketone of morphine More potent than oral morphine Less active metabolites than morphine For severe pain
31
Methadone
No kappa activity (less addiction cycle) Treat opiate withdrawal/ heroin users, and chronic pains Metahadone maintenance
32
Methadone: ADR
Constipation | Biliary spasms
33
Methadone maintenance
Treat opiate withdrawal Develops tolerance Manages opioid craving without IV drug use Reduce effect of opiates with cross tolerance
34
Heroin
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
6-monoacetylmorphine in urine test: drug of abuse?
Heroin
36
Hydrocodone/ Acetaminophen
For moderate to severe pain and Cough
37
Oxycodone
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
Meperidine
Mu-opioid agonist Normeperidine (metabolite)= CNS stimulant, not blocked by Naloxone Doesn't suppress cough MAOI+Meperidine= severe rxn
39
Fentanyl/ Sufenanil, Alfentanil/ Remifentanil
``` Mu-opioid agonist Meperidine analog Much more potent than Morphine For chronic pain Less nausea than Morphine ```
40
Codeine
Less potent analgesic than Morphine Cough syrups Metabolized to Morphine by CYP2D6 (highly polymorphic)
41
Effects of CYP2D6 polymorphism: slow/ high
Slow metabolizers: ineffective analgesic | High metabolizers: overdose {fast conversion to morphine}
42
Propoxyphene
Weak potency mu-agonist For mild to moderate pain Analgesic (used with Acetaminophen or Aspirin) Less dependence potential
43
Pentazocine
Kappa agonist, Weak Mu-antagonist Analgesia, Sedation, Respiratory depression aloxone included in Talwin to prevent drug abuse
44
Buprenorphine
``` Partial Mu agonist, Kappa-antagonist Less effective analgesic than Morphine Sublingal/ IM/ IV routes For treatment of Opioid dependence For Pregnant addicts ```
45
Tramadol
``` 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
Opiate antagonists
``` 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
For overdose patient, which opiate antagonist to give
Naloxone
48
Dextromethorphan
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
Robotripping
By Dextromethorphan in teens {liver damage with Acetaminophen may occur}
50
Alpha 2 adrenergic agonist: MoA
Inhibition of pain by NE with activation of receptors in Dorsal horn of spinal cord For Neutopathic pain and Cancer pain
51
Antidepressants(TCA/ SNRI)
TCA: Amitriptyline SNRI: Venlafaxine, Duloxetine
52
Antidepressants (TCA/ SNRI): MoA
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
Antiepileptics
Gabapentin, Pregabalin (alpha2delta ligands) | Carbamazepine
54
Antiepileptics:MoA
alpha2delta ligands: Reduce activation of N and P/Q Ca2+ channels Carbamazepine: Stabilizes inactive state of Na+v channels For Neutopathic pain
55
Gabapentin
For Post herpetic neuralgia and painful Diabetic neuropathy
56
Pregabalin
For central neuropathic pain, Fibromyalgia, Post herpetic neuralgia, painful Diabetic neuropahty
57
Carbamazepine
For Trigeminal neuralgia (1st line agent)
58
Lidocaine
Topical | Local anesthetic
59
Capsaicin
Topical Chili pepper alkaloid adjunctive TRPV1 antagonist Ion channel expressed on afferent noticeptors
60
Ketamine
NMDA antagonist | Blocks NMDA and Glutamate signaling
61
Baclofen ***
``` Centrally active muscle relaxants For spasticity, Hiccups GABA-B receptor agonist Facilitate spinal inhibition of motor neurons Avoid abrupt withdrawal ```
62
BZ-Diazepam***
Centrally active muscle relaxants For muscle spasms: IV or IM For muscle relaxant: oral as adjunct
63
Carisoprodol**
``` 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
Chlorzoxazone*
``` Not really used now.... Centrally active muscle relaxants For acute muscle spasms and pain Unknown MoA ADR: drowsiness, lightheadness Not for elderly ```
65
Cyclobenzaprine***
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
Metaxalone***
``` Centrally active muscle relaxants For Muscle discomfort Unknown MoA ADR: Jaundice, and other CNS effects (dizziness, headache) Careful with elderly and liver impaired ```
67
Methocarbamol***
``` Centrally active muscle relaxants For muscle spasms and tetanus Unknown MoA Rapid onset Careful with elderly and liver impaired ```
68
Orphenadrine*
Centrally active muscle relaxants | Nah, not really important
69
Tizanadine***
Centrally active muscle relaxants For Tension headaches and low back pains, and muscle spasticity Alpha adrenergic agonist Careful with elderly and liver impaired
70
1st line for Neuropathic pain
Antidepressants/ Ca channel alpha2delta ligands Carbamazepine for Trigeminal neuralgia Opioids if severe intractable pain/ Neuropathic cancer pain
71
2nd line for Neuropathic pain
``` Opioids Other antiepileptics NMDA antagonists Baclofen Adjunct Iidocaine therapy or steroid injection to joint ```
72
1st line for Nociceptive pain
NSAIDs {opioids are in last resort}