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PHTH 561 - Pharm > Pain and opioids, NSAIDS and steroidal anti-inflammatory drugs > Flashcards

Pain and opioids, NSAIDS and steroidal anti-inflammatory drugs Flashcards

1
Q

What is nociception?

A

neural process of encoding noxious stimuli

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2
Q

What is neuralgia?

A

pain in the distribution of nerve(s)

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3
Q

What is allodynia?

A

pain because of a stimuli that doesn’t normally provoke a pain

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4
Q

What is hyperalgesia?

A

more pain from a stimulus that normally provokes pain

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5
Q

What is neuropathic pain?

A

pain because of damage of the neurons or somatosensory nervous system

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6
Q

What are the drugs considered as adjuvants?

A

antidepressants
anticonvulsant
antispasmodic
muscle relaxant
bisphosphate
corticosteroid

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7
Q

What are the drugs considered as weak opioids?

A

codeine
tramadol
low dose morphine

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8
Q

What are the drugs considered as strong opioids?

A

morphine
fentanyl
oxycodone
hydromorphone
buprenorphine

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9
Q

WHO Analgesic Ladder

What is step 1 for mild pain?

A

a non-opioid

+/- adjuvant

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10
Q

WHO Analgesic Ladder

What is step 2 for moderate pain?

A

a weak opioid

+/- non-opioid
+/- adjuvant

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11
Q

WHO Analgesic Ladder

What is step 3 for severe pain?

A

strong opioid

+/- non-opioid
+/- adjuvant

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12
Q

WHO Analgesic Ladder

What is the +/- indicating?

A

That combining an opioid and non-opioid is effective but not combining drugs of the same class

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13
Q

What are the types of drugs used for pain treatment?

It’s a picture sry :(

A
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14
Q

What are the classifications of pain medications?

A
  1. opioid analgesics (HARD ASS DRUGS)
  2. non-opioid analgesics (NSAIDs)
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15
Q

What are the endogenous opioid peptides

A

Endorphins
- derived from POMC

Enkephalins
- derived from proenkephalin

Dynorphine
- derived from prodynorphine

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16
Q

Opioid receptors

What is the primary therapeutic effect of all opioid receptors?

A

spinal and supraspinal analgesia

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17
Q

Opioid receptors

What is the other effects of Mu(μ)?

A

sedation
respiratory depression
constipation
stops neurotransmitter release (ACh and dopamine)
increases hormonal release (prolactin)

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18
Q

Opioid receptors

What is the other effects of Kappa (k)?

A

sedation
constipation
psychotic effects

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19
Q

Opioid receptors

What is the other effects of delta (δ)?

A

increases hormonal release
inhibits neurotransmitter release

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20
Q

What is the effect of a strong agonist on the body?

A

have high affinity (relationship) for certain receptors
- believed to interact primarily with Mu opioid receptors in the CNS

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21
Q

What is the effect of a mild-to-mod agonist on the body?

A

still considered agonist that stimulate opioid receptors
- but do not have as high affinity or efficacy

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22
Q

What drugs are more effective in treating mild-mod pain?

A

codeine and hydrocodone

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23
Q

What is the characteristic of mixed agonist-antagonists?

A

show some agonist and antagonist-like activity at the same time
- drugs have the ability to act differently at specific classes of receptors

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24
Q

What are antagonist?

A

block all receptors that loves the Mu variety

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25
Q

What is the mechanism of the antagonists?

A

they wont produce analgesia but will displace opioid agonist from the receptors = block effects

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26
Q

What is the primary function of antagonist?

A

To treat opioid overdoses and addiction

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27
Q

What is the primary agent used to treat opioid overdose?

A

Naloxone

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28
Q

Morphine - brand name

A

MS contin

29
Q

Methadone - Brand name

A

dolophine

30
Q

Oxycodone - brand name

A

oxycontin

31
Q

Hydromorphone - brand name

A

Dilaudid

32
Q

Fentanyl - brand name

A

duragesic
sublimaze

33
Q

Hydrocodone - brand name

A

Hycodan

34
Q

Buprenorphine - brand name

A

Buprenex

35
Q

Naloxone - brand name

A

Narcan

36
Q

Naltrexone - brand name

A

ReVia
Vivitrol

37
Q

Mechanism of Action of Opioids

What does the opioid drug bind to?

A

the opioid receptors which are Gi/0 protein-couple receptors

38
Q

Mechanism of Action of Opioids

What is the presynaptic effects?

A

They close the voltage-gated Ca2+ channels @ presynaptic nerve terminals
= decrease transmitter release (glutamate and substance-P)

39
Q

Mechanism of Action of Opioids

What is the postsynaptic effects?

A

they open the K+ channels of the postsynaptic neurons and hyperpolarize them
= inhibit postsynaptic neurons

40
Q

What are the CNS effects of opioids?

A
  • analgesia
  • euphoria
  • sedation
  • respiratory depression
  • cough suppression
  • miosis
  • truncal rigidity
  • nausea
  • vomitting
  • body temp
  • sleep disturbances
41
Q

Peripheral effects of Opioids

Cardiovascular system effects

A
  • no significants on CVs
  • bradycardia
  • hypotension
  • increased cerebral blood flow
  • increased intracranial pressure

Brady - except Meperidine-tachycardia due to anticholinergic effects

Intracranial pressure - contraindicated in brain injury

42
Q

Peripheral effects of Opioids

Gastrointestinal system effects

A

constipation
- opioids don’t develop the tolerance to constipating effects

43
Q

Peripheral effects of Opioids

Biliary tract effects

A

Biliary colic
- contraction of biliary smooth muscles

44
Q

Peripheral effects of Opioids

Renal effects

A
  • decreased renal function
  • antidiuretic effect
  • urinary retention
45
Q

Peripheral effects of Opioids

Endocrine effects

A
  • decreased testosterone with chronic use
  • decreased libido, energy and mood
  • dysmenorrhea or amenorrhea in women
46
Q

Peripheral effects of Opioids

Pruritis effects

A

Produce flushing and warming of the skin + sweating, urticaria and itching
- increased peripheral histamine release

47
Q

What is the major cause of opioid overdose?

A

Respiratory failure

48
Q

What are the adverse effects with acute use of opioid drug?

A
  • respiratory depression
  • nausea/vomiting
  • pruritus
  • urticaria
  • constipation
  • urinary retention
  • delirium
  • sedation
  • myoclonus
  • seizures
49
Q

What are the adverse effects with chronic use of opioid drug?

A
  • hypoganodism
  • immunosuppresion
  • increased feeding
  • increased growth hormone secretion
  • withdrawal effects
  • tolerance and dependence
  • abuse
  • addiction
  • hyperalgesia
  • impairment of ADLs
50
Q

How is a high degree of tolerance developed in regard to opioids?

What is not developed?

A

develop to the analgesic (no pain), sedating (high af) and respiratory depressants (relaxing) effects of the agonists

it can also be to the antidiuretic, emetic and hypotensive effects

Not to the miotic, convulsant and constipating actions

51
Q

What does COX-1 produce?

A

produces prostaglandins that mediate homeostatic functions
- constitutively expressed

52
Q

What does COX-2 produce?

A

Produces prostaglandins for inflammation, pain and fever
- induced mainly in sites of inflammation by cytokines

53
Q

What is the mechanism of action for NSAIDs?

A

inhibiting COX

54
Q

What is the effects of COX-1 inhibition?

A

peptic ulcers
GI bleeding

55
Q

What is the effects of COX inhibition?

A

Na and water retention
Hypertension
Hemodynamic acute kidney injury

56
Q

What is the effects of COX-2 > COX-1 inhibition?

A

Stroke
MI

57
Q

What are the non-selective NSAIDs for COX1 and COX2?

A

Diclofenac
Ibuprofren
Naproxen

58
Q

What are the COX2-selective NSAIDs?

A

Celecoxib
Rofecoxib

59
Q

What is the mechanism of action of acetaminophen?

A

not fully understood but does inhibit the COX enzyme

a theory:
- it inhibits CNS PG production but has little effect on peripheral cyclooxygenase activity
- analgesia and antipyretic effect probably 2 PG inhibition

60
Q

What are the important side effects of NSAIDs?

A
  • kidney failure
  • liver failure
  • Ulcers
  • prolonged bleeding after injury or surgery
  • cause fluid retention = edema = swelling of ankles
61
Q

What are the therapeutic effects of NSAIDs?

A
  • analgesic
  • anti-inflammatory
  • antipyretic
  • anticoagulant
  • anticancer

All therapeutic effects through inhibition of prostaglandins

62
Q

What is the precursor to steroid synthesis?

A

Cholesterol

63
Q

Glucocorticoids produces what substances?

A

cortisol
corticosterone

64
Q

Mineralocorticoids produces what substance?

A

Aldosterone

65
Q

What is the function of mineralocorticoids?

A

Fluid retention and electrolyte balance

66
Q

Clinical use of corticosteroids

What is the endocrine conditions?

A

used to normalize adrenal cortical hypofunction
- used as a diagnostic tool to evaluate hormal disorders

67
Q

Clinical use of corticosteroids

What is the nonendocrine conditions?

A

different conditions for anti-inflammatory or immunosuppressive effects
- primary nonendocrine conditions will see: RA, myositis, tenosynovitis and collagen diseases

68
Q

What are the adverse effects of corticosteroids?

A
  • adrenocortical suppression
  • peptic ulcers
  • drug-induced cushing syndrome
  • adrenal crisis/shock
  • breakdown of supporting tissues
  • decreases body’s ability to absorb calcium which can lead to osteoporosis and delayed wound healing

PHTH 561 - Pharm (6 decks)

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