Pain Flashcards
Mu1 receptor: site of action, effect, agonists, antagonists
- Site of action
- supraspinal, spinal, and peripheral analgesia
- Effect
- euphoria
- miosis
- bradycardia
- urinary retention
- hypothermia
- agonists
- **all endogenous and synthetic opioid agonists act on these receptors
- endorphins
- morphine
- synthetic opioids
- **all endogenous and synthetic opioid agonists act on these receptors
- antagonists
- naloxone
- naltrexone
- nalmefene
Mu2 receptors: site of effect, effects, agonists, antagonists
- Site of action
- spinal, some supraspinal
- Effect
- hypoventilation
- physical dependence
- constipation
- hypoventilation
- agonists
- **all endogenous and synthetic opioid agonists act on these receptors
- endorphins
- morphine
- synthetic opioids
- **all endogenous and synthetic opioid agonists act on these receptors
- antagonists
- naloxone
- naltrexone
- nalmefene
Kappa receptor: site of effect, effects, agonists, antagonists
- Site of action
- supraspinal, spinal, and min. peripheral analgesia
- Effect
- dysphoria
- sedation
- miosis
- diuresis
- low abuse potential
- agonists
- dynorphins
- opioid agonists/antagonists often have principle actions at the kappa receptor
- antagonists
- naloxone
- naltrexone
- nalmefene
Delta receptor: site of effect, effects, agonists, antagonists
- Site of action
- Mostly peripheral, some supraspinal, and spinal
- Effect
- hypoventilation
- constipation
- urinary retention
- physical dependence
- agonists
- enkephalins
- antagonists
- naloxone
- naltrexone
- nalmefene
Equianalgesic doses for control of chronic pain (chart)
What is the MOA of tylenol? Which patient populations is this a good choice for?
- MOA stated below is not well elucidated
- central anti prostaglandin effect
- antipyretic
- pain redued via blockade of:
- NMDA receptor activation in CNS
- substance P in spinal cord
- lacks peripheral activity - weak anti-inflammatory action (not a true NSAID)
- Good choice in:
- peptic ulcer disease
- pediatric patients
- patients who need well functioning platelets
Can ASA cause ESRD?
- No, ESRD is not induced by chronic ASA (in contrrast to other NSAIDS)
- but can cause prolonged bleeding (up to 15 minutes) in patients with ESRD
Which patient population can experience asthma and anaphylactoid reactions with NSAIDs?
aspirin sensitive population
Overview of common pharmacokinetic and pharmacodynamic effecets of NSAIDs (chart)
Which NSAIDs have have an increased renal risk and why? Which are “renal sparing”?
- can occurs with ALL NSAIDs
- increased risk
- longer half life
- highly potent COX inhibitors
- ketoralac
- indomethacin
- higher dose
- “renal sparing” (lower risk, NOT devoid)
- sulindac, nabumetone
- celecoxib
Adjuvant analgestics - anticonvulsants, Gabapentin (neurontin): What is the MOA and use?
- mechanism not well understood
- used for:
- diabetic neuropathy
- postherpetic neuralgia
Adjuvant analgestics - anticonvulsants, Pregabalin (lyrica): What is the MOA and use?
- gabanergic, analogue of GABA
- analgesic effects may be related to calcium influx inhibition as well as inhibition of the release of excitatory neurotransmitters in spinal and supraspinal pathways via binding to alpha 2 delta 1 subunit of presynaptic VGCC in the CNS
- used for:
- diabetic neuropathy
- post herpetic neuralgia
- fibromyalgia
Adjuvant analgestics - anticonvulsants, carbamazepine (tegretrol): What is the MOA and use?
- NA channel blocker, and GABAnergic
- FDA approved for:
- trigeminal neuralgia
Adjuvant analgestics - anticonvulsants, phenytoin (dilantin), sodium valporoate (depakote), clonazepam (klonopin), and topiramate (topamax): What is the use?
- may relief neuropathic pain
Adjuvant analgestics - Anticonvulsants, Lamitrogen (lamictal): What is the MOA and use?
- gabanergic
- effective for central post stroke pain and HIV associated painful sensory neuropathies
