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HSS3106 - Pharmacology > Lecture 8- Analgesics > Flashcards

Lecture 8- Analgesics Flashcards

1
Q

What is an ANALGESIC?

A

PAIN KILLERS!

  • alter brain’s interpretation of pain signals
  • stop pain signals from going to the brain
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2
Q

What is an ANTIPYRETIC?

A

reduces FEVER

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3
Q

What is pain?

A

indicator that something is WRONG! (CNS reaction to harmful stimuli)

Acute = short term (stub your pinky toe)

Chronic = long term (arthritis)

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4
Q

What is pain stimuli?

A

results from an inflammatory process –> fluid builds up and puts PRESSURE on an area

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5
Q

What are pain receptors called and what do they do?

A
  • Nociceptors –> mechanical, chemical, thermal, silent, polymodal
  • once activated it sends message to brain cortex
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6
Q

What are the 3 types of pain?

A
  1. Nociceptive
  2. Neuropathic
  3. Nociplastic
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7
Q

What is NOCICEPTIVE pain?

A
  • nerves which sense and respond to parts of the body which suffer from damaged
    -pain is localized, constant, and often with an aching or throbbing pain
    ex: sprains, bone fractures, burns, bumps, bruises, inflammation, obstructions, myofascial pain
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8
Q

What is NEUROPATHIC pain?

A
  • comes directly from the nerves
  • burning, shooting, stabbing, prickling, electric shock-like pain , hypersensitive to touch/movement, hot and cold and pressure
  • ex: post-shingles neuralgia, sciatica, nerve trauma, cancer pain, phantom limb pain, entrapment neuropathy, peripheral neuropathy
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9
Q

What is NOCIPLASTIC pain?

A
  • cannot see anything physically wrong
  • does not respond to most meds
  • can be amplified, widespread, various tissues involved, greater than expected
  • seen in:
    1. fibromyalgia
    2. chronic pelvic pain
    3. tension-type headaches
    4. chronic low back pain
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10
Q

What are 2 neurotransmitters that are considered “natural pain killers” and what do they do?

A
  1. Endorphins
  2. Enkephalins

Job:
- bind with opiate receptors in CNS and inhibit transmission of pain impulses

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11
Q

Do analgesics rely on anesthesia or loss of consciousness?

A

NO!!

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12
Q

What are the 4 non-opioids?

A
  1. acetaminophen
  2. NSAIDS
  3. Salicylates –> Aspirin
  4. Cox-2 inhibitors
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13
Q

What are the 5 NSAIDS generic and trade name?

A
  1. Aspirin –> Bayer
  2. diclofenac –> Cataflam
  3. ibuprofen –> Motrin
  4. ketorolac –> Acular LS
  5. naproxen –> Anaprox, Naprosyn, Naprelan
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14
Q

What do NSAIDS do?

A

relieve PAIN and INFLAMMATION and FEVER

mechanism of action:
- block prostaglandin synthesis (COX PATHWAYS)

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15
Q

What is mechanism of action for Aspirin?

A
  • NSAID

Mechanism of action:
- unknown
-reduce pain and inflammation
-reduce fever
-impedes blood clotting (LOW DOSES) –> inhibit COX1
- pain killer and anticog (HIGH DOSES)

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16
Q

What are the ADVERSE EFFECTS of Aspirin?

A
  • serious: GI hemorrhage at HIGH doses
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17
Q

Should you give kids aspirin if they have a virus?

A

NO!

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18
Q

All NSAIDS except aspirin increase risk of serious adverse cardiovascular events. True or False?

A

True!

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19
Q

What does Ibuprofen do?

A

mechanism of action
- block COX1 and COX2
- pain killer and reduces fever and anti-inflammatory

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20
Q

What are the adverse effects of Ibuprofen?

A

common: GI related probs
Serious: azotemia (issue with nitrogen), hematuria(blood in urine)

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21
Q

What does Naproxen do?

A

mechanism of action:
- block COX1 and COX2
- reduce pain, fever, and inflammation

Use:
- arthritis when its longer lasting

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22
Q

What are the ADVERSE EFFECTS of naproxen?

A

rash, GI tract probs, blood clots

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23
Q

What does Diclofenac do?

A

NSAID

mechanism of action:
- inhibits both COX1 and COX2

USe:
- inflammation, fever, pain
- seen in voltaren! (cream!)
-arthritis

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24
Q

What are the ADVERSE EFFECTS of Diclofenac (fro tablets)?

A

GI problems

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25
Q

What are the contrainidcations of Diclofenac?

A

pregnant, liver probs, kidney probs, allergy

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26
Q

What does Ketorolac do?

A

NSAID

mechanism of action:
- block COX1 and COX2

Use:
-SHORT TERM pain and inflammation

27
Q

What does Ketorolac ADVERSE EFFECTS?

A

GI problems

28
Q

What does Ketorolac contrainindications?

A

pregnant, older, kidney problems, liver probs

29
Q

What does COX1 pathway do in the prostoglandin synthesis?

A

-ALWAYS ACTIVE!!!
- good!
- produces thromboxane and prostoglandins (blood clotting and tightening arteries)
- needds help of COX2 for prostacyclin (enzyme that keeps it in check)

30
Q

What does COX2 pathway do in the prostoglandin synthesis?

A

-must be INDUCED
- BAD!
- produces inflammatory prostoglandins
- if it is inhibited too much/only …
create an imbalance in prostacyclin –> increase vasoconstriction –> COX1 goes unchecked–> increase level of stroke and heart attack

31
Q

What are the two selective COX2 inhibitors generic and trade name?

A
  1. celecoxib –> Celebrex
  2. meloxicam –> Movera
32
Q

What is the mechanism of action of COX2 inhibitors?

A

inhibits COX2

33
Q

What is COX2 inhibitors used for?

A

osteoarthritis

rheumatoid arthritis

34
Q

What are the ADVERSE EFFECTS of COX2 inhibitors?

A

GI probs
serious : heart attack and stroke

35
Q

What is the mechanism of action for Acetaminophen?

A

unknown
maybe inhibit prostoglandin in PNS or block COX1/COX2

36
Q

What is the USE of Acetaminophen?

A

lacks anti-inflammatory action

PAIN and FEVER

37
Q

What are the ADVERSE EFFECTS of Acetaminophen?

A

long term: liver toxicity
overdose : liver toxic, coma, internal bleeding

38
Q

What are two drugs generic and trade names for treating migraines?

A
  1. Sumatriptan –> Imitrex
  2. Ergotamine, caffeine –> Cafergot
39
Q

What are the 2 natural Opioid Analgesics generic and trade name?

A
  1. Codeine
  2. Morphine –> Duramorph
40
Q

What is the mechanism of action for OPIATES in general?

A

binding to opioid receptors in brain –> affect MU receptors

NO upper effective limit –> affects conciousness and breathing at high levels

risk of dependency

41
Q

What is the USE of codeine and morphine ?

A

pain

antiperistaltic

antitussive –> inhibit cough reflex

42
Q

What are the ADVERSE EFFECTS of codeine and morphine ?

A

common: postural hypotension (when you get up you feel dizzy), GI probs (we have opioid receptors in our GI tract)
serious: slows down breathing and cortical function

CAN GET ADDDICTED

43
Q

What are the contrainidications of morphine?

A

interacts with medical conditions

interacts with things that act on CNS (alcohol, monoamin oxidase inhibitors, meperidine)

44
Q

What are the 2 generic and trade names of Semisynthetic Opioid Anagelsics?

A
  1. Hydrocodone –> Hycodan
  2. oxycodone –> Oxycontin
45
Q

What is USE of Hydrocodone

A

suppresses cough reflex

acts as CNS depressant –> to relieve pain

46
Q

What is USE of oxycodone?

A

pain (post-op and post-partum)

47
Q

What is ADVERSE EFFECTS of oxycodone?

A

common : euphoria, GI probs
serious: slows down breathing, jaundice, toxic to lvier

48
Q

What is MECHANISM of action of oxycodone?

A

binds to KAPPA and MU receptors in brain

49
Q

What is ADVERSE EFFECTS of hydrocodone?

A

common: GI probs
serious: slows breathing down , serotonin syndrome

50
Q

What is MECHANISM of action of hydrocodone?

A

agonist to MU receptor

51
Q

What is the ONE synthetic opioid antagonist?

A
  1. Naloxone –> Narcan
52
Q

What are the 4 synthetic opioid agonist/antagonist?

A
  1. buprenorphine –> Buprenex
  2. fentanyl –> Sublimaze
  3. meperidine –> Demerol
  4. pentazocine –> Talwin
53
Q

What does Naloxone do?

A

for narcotic overdose

kicks opioids off the receptors in your brain and bind to the receptors instead

54
Q

Is synthetic tend to be less addictive?

A

YES –> longer half-life , less withdrawl

55
Q

What is MECHANISM of action for buprenorphine?

A

high affinity to MU opioid receptor
antagonist to KAPPA

56
Q

What is buprenorphine USED for?

A

PAIN –> moderate to severe
cancer
stones in urethra
heart attack

57
Q

What are the ADVERSE EFFECTS of buprenorphine?

A

sedation
dizzy
headache
euphoria

58
Q

What does Fentanyl do?

A

binds to MU receptor

used for pain and sedation in op and post-op

interacts with stuff that affects CNS (alcohol!)

59
Q

What does Meperidine do?

A

acts as KAPPA opioid receptor agonist

acts on CNS and organs with smooth muscle

pre-op –> pain

depress cough

produce less muscle spasm

60
Q

What does Pentacozine do?

A

agonist against KAPPA and SIGMA opioid receptors

moderate to severe PAIN

61
Q

Overall what does opoids used for?

A
  • pain
  • antiperistaltic
  • cough surpressant
62
Q

What receptors does opioids work on?

A

MU mostly

also KAPPA

also SIGMA

63
Q

What could the adverse effects be with opioids?

A
  • anything acting on CNS :
    1. alcohol
    2. CNS depressants
    3. monoamine oxidase inhibitors

HSS3106 - Pharmacology (18 decks)

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