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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
What are the contrainidcations of Diclofenac?
pregnant, liver probs, kidney probs, allergy
26
What does Ketorolac do?
NSAID mechanism of action: - block COX1 and COX2 Use: -SHORT TERM pain and inflammation
27
What does Ketorolac ADVERSE EFFECTS?
GI problems
28
What does Ketorolac contrainindications?
pregnant, older, kidney problems, liver probs
29
What does COX1 pathway do in the prostoglandin synthesis?
-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
What does COX2 pathway do in the prostoglandin synthesis?
-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
What are the two selective COX2 inhibitors generic and trade name?
1. celecoxib --> Celebrex 2. meloxicam --> Movera
32
What is the mechanism of action of COX2 inhibitors?
inhibits COX2
33
What is COX2 inhibitors used for?
osteoarthritis rheumatoid arthritis
34
What are the ADVERSE EFFECTS of COX2 inhibitors?
GI probs serious : heart attack and stroke
35
What is the mechanism of action for Acetaminophen?
unknown maybe inhibit prostoglandin in PNS or block COX1/COX2
36
What is the USE of Acetaminophen?
lacks anti-inflammatory action PAIN and FEVER
37
What are the ADVERSE EFFECTS of Acetaminophen?
long term: liver toxicity overdose : liver toxic, coma, internal bleeding
38
What are two drugs generic and trade names for treating migraines?
1. Sumatriptan --> Imitrex 2. Ergotamine, caffeine --> Cafergot
39
What are the 2 natural Opioid Analgesics generic and trade name?
1. Codeine 2. Morphine --> Duramorph
40
What is the mechanism of action for OPIATES in general?
binding to opioid receptors in brain --> affect MU receptors NO upper effective limit --> affects conciousness and breathing at high levels risk of dependency
41
What is the USE of codeine and morphine ?
pain antiperistaltic antitussive --> inhibit cough reflex
42
What are the ADVERSE EFFECTS of codeine and morphine ?
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
What are the contrainidications of morphine?
interacts with medical conditions interacts with things that act on CNS (alcohol, monoamin oxidase inhibitors, meperidine)
44
What are the 2 generic and trade names of Semisynthetic Opioid Anagelsics?
1. Hydrocodone --> Hycodan 2. oxycodone --> Oxycontin
45
What is USE of Hydrocodone
suppresses cough reflex acts as CNS depressant --> to relieve pain
46
What is USE of oxycodone?
pain (post-op and post-partum)
47
What is ADVERSE EFFECTS of oxycodone?
common : euphoria, GI probs serious: slows down breathing, jaundice, toxic to lvier
48
What is MECHANISM of action of oxycodone?
binds to KAPPA and MU receptors in brain
49
What is ADVERSE EFFECTS of hydrocodone?
common: GI probs serious: slows breathing down , serotonin syndrome
50
What is MECHANISM of action of hydrocodone?
agonist to MU receptor
51
What is the ONE synthetic opioid antagonist?
1. Naloxone --> Narcan
52
What are the 4 synthetic opioid agonist/antagonist?
1. buprenorphine --> Buprenex 2. fentanyl --> Sublimaze 3. meperidine --> Demerol 4. pentazocine --> Talwin
53
What does Naloxone do?
for narcotic overdose kicks opioids off the receptors in your brain and bind to the receptors instead
54
Is synthetic tend to be less addictive?
YES --> longer half-life , less withdrawl
55
What is MECHANISM of action for buprenorphine?
high affinity to MU opioid receptor antagonist to KAPPA
56
What is buprenorphine USED for?
PAIN --> moderate to severe cancer stones in urethra heart attack
57
What are the ADVERSE EFFECTS of buprenorphine?
sedation dizzy headache euphoria
58
What does Fentanyl do?
binds to MU receptor used for pain and sedation in op and post-op interacts with stuff that affects CNS (alcohol!)
59
What does Meperidine do?
acts as KAPPA opioid receptor agonist acts on CNS and organs with smooth muscle pre-op --> pain depress cough produce less muscle spasm
60
What does Pentacozine do?
agonist against KAPPA and SIGMA opioid receptors moderate to severe PAIN
61
Overall what does opoids used for?
- pain - antiperistaltic - cough surpressant
62
What receptors does opioids work on?
MU mostly also KAPPA also SIGMA
63
What could the adverse effects be with opioids?
- anything acting on CNS : 1. alcohol 2. CNS depressants 3. monoamine oxidase inhibitors

HSS3106 - Pharmacology (18 decks)

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