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6a > Chronic pain pharmaceuticals > Flashcards

Chronic pain pharmaceuticals Flashcards

1
Q

Common chronic pain syndromes

A 
Headache - most common
Back pain - 2nd most common
Post herpetic neuralgia
Pain associated with diabetic neuropathy
Phantom limb pain
Myofascial pain
Posttraumatic neuropathic pain
Central pain
Complex regional pain syndrome (CRPS)
- type I: formerly reflex sympathetic dystrophy (RDS)
- type II: formerly causalgia (burning pain)
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2
Q

Causalgia

A

Syndrome of sustained burning pain, allodynia, and hyperpathia after a traumatic nerve lesion, often combined with vasomotor and sudomotor dysfunction and later trophic changes

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3
Q

1st line agents used in chronic neuropathic pain

A

TCAs

Anticonvulsants - gabapentin, pregabalin, carbamazepine

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4
Q

2nd line agents used in chronic neuropathic pain

A

SSNRIs: venlafaxine

Topical lidocaine

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5
Q

3rd/4th line agents used in chronic neuropathic pain

A 
opioid analgesics
tramadol
SSRIs
other anticonvulsants
IV lidocaine, mexilitine
Topical capsaicin
Cannabinoids
NMDA receptor antagonists: ketamin, dextromethorphan
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6
Q

TCA - secondary amines

A

Nortriptyline

Despiramine

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7
Q

TCA - tertiary amines

A

Amitriptyline

Imipramine

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8
Q

TCA effectiveness

A

avg treated patients have less pain than 74% of patients w/ placebo
most effective in diabetic neuropathy and postherpetic neuralgia
relief of concomitant symptoms: sleep disorder, anxiety disorder, depression

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9
Q

TCA MOA (chronic pain)

A

unclear
serotonin/norepinephrine reuptake inhibition
increased endogenous inhibition by increasing descending pathway transmission

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10
Q

TCA dose/onset

A

analgesic dose is lower than antidepressant dose

analgesic effect almost immediate

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11
Q

TCA side effects

A

Anticholinergic
CVS:
- postural hypotension (due to alpha blockade - increased risk of falls in the elderly, particularly with amitryptiline)
- conduction delay/myocardial depression - typically in OD

2ndary amines are better tolerated than tertiary amines

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12
Q

Calcium channel alpha-2-delta ligands

A

Gabapentin

Pregabalin

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13
Q

Gabapentin

A

GABA analogue

anticonvulsant

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14
Q

Pregabalin

A

Gabapentin analogue

anti-convulsant

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15
Q

Gabapentin effectiveness/indications

A

antiallodynic
no effective on nociceptive threshold
used in chronic neuropathic pain
published evidence but true effectiveness questioned?

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16
Q

Gabapentin MOA

A

does not act via GABA receptors
binds to alpha2delta-1 subunits of presynaptic CaV channels
Reduces release of glut, norepi, substance P, CGRP (excitatory nociceptive NTs

17
Q

Pregabalin effectiveness/indications

A

chronic neuropathic pain

anxiolytic

18
Q

Pregabalin MOA

A

similar to gabapentin
binds to alpha2delta-1 Ca channel subunits with higher affinity
Reduces release of glutamate, norepi, substance P, CGRP
More linear pharmacokinetics than gabapentin

19
Q

Gabapentin dose/onset

A

100-4800 mg/d
reduce in renal failure
oral bioavailability unpredictable

20
Q

Pregabalin dose/onest

A

75-600 mg/d

reduce in renal failure

21
Q

Gabapentin SEs

A

relatively well-tolerated with few SEs:

  • dizziness, somnolence, confusion, ataxia
  • peripheral edema
22
Q

Pregabalin SEs

A

generally well-tolerated with few SEs:

  • dizziness, somnolence, confusion, ataxia
  • peripheral edema
23
Q

Carbamazepine effectiveness (chronic pain)

A

anticonvulsant
drug of first choice for trigeminal neuralgia (tic doloreux)
otherwise limited evidence for analgesic effectiveness

24
Q

Carbamazepine MOA (chronic pain)

A

unclear

maybe? blockade of Na channels

25
Q

Carbamazepine dose/onset (chronic pain)

A

200-1200 mg/d divided in two doses

hepatic enzyme induction

26
Q

Carbamazepine major side effects

A 
Dizziness
Ataxia
Nausea
Hepatitis
Aplastic anemia
Stevens-Johnson syndrome
27
Q

Other anticonvulsants used for chronic pain

A

Lamotrigine, valproic acid, topiramate
Few trials show effectiveness
MOA unclear, Na blockade?
Should be withheld until other interventions have been tried (other than trigeminal neuralgia)

28
Q

Tramadol effectiveness

A

postherpetic neuralgia
diabetic neuropathy
polyneuropathies/post-amputation pain
Extended release formulation approved in Canada

29
Q

Tramadol MOA

A

synthetic opioid
weak mu-agonist activity
inhibits serotonin and norepinephrine reuptake
peripheral local anesthetic properties

30
Q

Tramadol dose

A

100-300 mg once a day

31
Q

Tramadol side effects

A

Relative LACK of:

  • respiratory depression
  • major organ toxicity
  • depression of GI motility
  • reduced seizure threshold
  • relatively low abuse potential
32
Q

Topical capsaicin effectiveness

A

diabetic neuropathy
postherpetic neuralgia
anecdotal evidence for other types of neuropathic pain
Transdermal application

33
Q

Capsaicin MOA

A

prototype agonist at transient receptor potential vanilloid 1 (TRPV1) receptors
depetion of substance P in C-fibers
Nociceptor desensitization

34
Q

Cannabinoid effectiveness

A

Delta-9-tetrahydrocannabinol-cannabidiol
Buccal spray conditionally approved in Canada for neuropathic pain associated with MS
effective in reducing central pain and painful spasms in MS

35
Q

Cannabinoid SEs

A 
lack of long-term followup data
dizziness, fatigue, nausea, mood changes
potential for cognitive impairment
precipitation of psychosis
suicidal ideation
Positive urine drug testing!
36
Q

Drugs NOT indicated in chronic pain

A

hypnotics/sedative-containing preparations

example: FIORINAL, which contains:
- butalbital (barbiturate, associated with high abuse potential)
- caffeine
- ASA

37
Q

Canadian Consensus Guideline: treatment algorithm (2007) for neuropathic pain

A

1) TCA/gabapentin or pregabalin
2) SNRI, topical lidocaine
3) Tramadol, CR opioid analgesic
4) cannabinoids, methadone, lamotrigine, topiramate, valproic acid - add sequentially if partial relief

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