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Pharm Exam 3 > Analgesics > Flashcards

Analgesics Flashcards

1
Q

Order of pain transmission

A
  1. Injury occurs (tissue damage, inflammation, infection, etc.(
  2. Release of arachidonic acid OR autocoids (bradykinin, histamine)
  3. (if arachidonic acid) Arachidonic acid creates prostaglandins under the action of COX
  4. Either autocoids OR prostaglandins activate nociceptors
  5. Neurotransmission through spinal cord (synapse with opioid receptors)
  6. Neurotransmission to brain (cerebral cortex –> perception of pain and emotional reaction to pain)
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2
Q

Examples of autocloids

A

histamine and bradykinin

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3
Q

examples of excitatory neurotransmitters released from the pre-synaptic neuron in the gray matter

A

glutamate and substance P

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4
Q

Endogenous opioids

A

endorphins
enkephalins
dynorphins

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5
Q

How do presynaptic opioid receptors inhibit pain neurotransmission?

A

They block voltage dependent calcium channels, which blocks exocytosis of excitatory neurotransmitters

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6
Q

How do postsynaptic opioid receptors block pain neurotransmission?

A

They open potassium channels which hyperpolarize membranes and block the formation of action potentials, essential for transmitting pain sensation

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7
Q

Examples of opioid receptors

A

Mu (u1)
Mu (u2)
delta
kappa

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8
Q

What do u1 receptors induce?

A

analgesia, euphoria and physical dependence

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9
Q

what do u2 receptors induce?

A

sedation, bradycardia, and resp. depression

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10
Q

what do delta receptors induce

A

spinal anesthesia and development of tolerance to opioids

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11
Q

what do kappa receptors induce

A

spinal anesthesia, miosis, and sedation

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12
Q

Non-opioid analgesics

A

NSAIDs:
ibuprofen
naproxen
aspirin
acetaminophen

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13
Q

MOA of NSAIDs

A

COX inhibitors that prevent the production of prostaglandins

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14
Q

Pharmacotoxicology of NSAIDs

A

Gastric irritation, spontaneous hemorrhaging, tinnitus; acetaminophen can cause liver failure in overdoses

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15
Q

MOA of fentanyl

A

full opioid receptor agonist; 100x more potent than morphine and 50x more potent than heroin

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16
Q

What is hydrocodone

A

the most widely prescribed drugs on the market and yet when given for the relief of pain, its dose and potential for addiction can be reduced when given with other medications

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17
Q

MOA of methadone

A

a full opioid receptor agonist that is used in the treatment of opioid addiction because it is a long-acting opioid agonist that reduces the daily cycles of craving and withdrawals.

18
Q

MOA of codeine

A

a moderate to strong opioid receptor agonist that is used as an antitussive medication

19
Q

BOA of buprenorphine

A

A partial opioid receptor agonist that is used in the treatment of moderate to severe opioid use disorder and as an analgesic

20
Q

What is suboxone

A

A combination of buprenorphine and the opioid antagonist naloxone used in the treatment of opioid addiction

21
Q

What is naloxegol?

A

a medication used to treat constipation in pts on long-term opioid therapy; a mu receptor antagonist that does not pass the BBB

22
Q

Examples of opioid receptor antagonists

A

naltrexone (naloxone) and vivitrol

23
Q

what is vivitrol

A

a opioid receptor antagonist that is an injectable formula of naltrexone

24
Q

What is lofexidine

A

an alpha2 adrenergic receptor agonist, a non-opioid, that is used to alleviate the physical symptoms of heroin and other types of opioid withdrawal

25
Q

MOA of gabapentin

A

increases GABA levels in the CNS which inhibits the subunit in the voltage-dependent calcium channel, thus suppressing the release of glutamate

26
Q

Therapeutic use of gabapentin

A

treatment of diabetic peripheral neuropathy, trigeminal neuropathy, fibromyalgia, and “phantom limb pain”

27
Q

What type of anesthetic is procaine?

A

ester-type anesthetic

28
Q

what type of anesthetic is lidocaine?

A

amide-type anesthetic

29
Q

What is the difference between ester-type and amide-type anesthetics?

A

the half life; amide-type anesthetic half life is typically 10 min and ester-type anesthetic is typically 1 minute. Amide anesthetics are metabolized by CYP enzymes and ester anesthetics are metabolized by plasma pseudocholinesterase

30
Q

MOA of lidocaine and procaine

A

both are sodium channel blockers that inhibit formation of action potentials and thus block nerve impulse conduction by nociceptors

31
Q

MOA of propofol

A

enhancing the release of GABA; inhibiting sodium channels, or activating the endocannabinoid system through the CNS

32
Q

What is propofol?

A

General IV anesthetic w/ rapid onset of action, ultra-short duration of action. Used for induction and maintenance of general anesthesia; may induce resp. depression

33
Q

MOA of isoflurane and etomidate

A

activating GABA receptors (inhibitory neurotransmitter)

34
Q

What is isoflurane?

A

a general, inhalation anesthetic w/ global CNS depressant effects. LOC, analgesic, amnesia, suppression of peripheral sensations, and depression of resp. Control centers

35
Q

what is etomidate?

A

a short acting IV anesthetic medication used for the induction of general anesthesia and sedation for short procedures such as reduction of dislocated joints, tracheal intubation, and cardioversion.

36
Q

MOA of ketamine

A

N-methyl-d-aspartate (NMDA) antagonist (subtype of an excitatory receptor for glutamate)

37
Q

Ketamine usages?

A

short-acting IV medication that is used mainly for starting and maintaining anesthesia. Uses include sedation in ICU, analgesia, and treatment of bronchospasms.

38
Q

prophylactic treatment for migraines include…

A

Propranolol (non selective beta antagonist)
amitriptyline (tricyclic antidepressant that elevates serotonin levels)
Divalproex (anti-seizure medication)

39
Q

treatment of ongoing migraine

A

NSAIDs

Ergotamine: alpha 1 adrenergic agonist—cause vasoconstriction

Sumatriptan: selective serotonin receptor agonist

Telcagepant: oral CGRP receptor antagonist

40
Q

MOA of nabilone

A

CB1 and CB2 receptor agonist that has been used in the treatment of chemotherapy-induced nausa/vomiting; treatment of chronic pain (fibromyalgia), and anorexia associated with HIV infections

41
Q

What is the most common endocannabinoid that we produce?

A

Anandamide

42
Q

MOA of Anandamide

A

the primary psychoactive component of cannabis, delta 9 THC, produces its effects through weak partial activation of the endocannabinoid system that contains cannabinoid 1&2 receptors

Pharm Exam 3 (5 decks)

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