Analgesics & NSAIDs

Question 1

ANALGESICS: Opioids

cardinal signs of inflammation (5)

license

morphine, oxycodone, fentanyl, codeine, thedane

Answer 1

• cardinal signs of inflam: pain, redness, swelling, heat, function
• need S2 license
• morphine: gold
• oxycodone: diff color for diff dose
• fentanyl: 75mg continuous transdermal = systemic effect
• codeine: cough
• thedane: poppy heroin; antidote for opioid

Question 2

ANALGESICS: Opioids

purpose (3)

effects (6.3)

Answer 2

PURPOSE
- mod to severe pain (gr. 4-10)
- bind to neuronal receptors
- potential for physical dependence

EFFECTS
- histamine release, OH, respiratory depression, apnea, bradycardia
- suppressed cough reflex
- euphoria
- constipation
- miosis (pupillary constriction)
- nausea, vomit, sedation, drowsy

Question 3

ANALGESICS: Opioids

MOA on brain (3)

MOA on spine (2)

MOA on peripheral nerves (1)

Answer 3

MOA on brain
- stimulate neurons for pain modulation, inhibit pain transmission
- bind to nociceptors

MOA on spine
- inhibit nociceptive to higher levels by: dec pain substance, hyperpolarize post-synaptic neurons

MOA on peripheral nerves
- dec excitability of A-delta & C fibers

Question 4

ANALGESICS: Opioids

Mu - location & effect (4.3)

Kappa - location & effect (3.3)

Delta - location & effect (3.2)

Sigma - location & effect (1.3)

which high/low abuse potential

Answer 4

MU (high)
- supraspinal, periaqueductal gray, hypothalamus, medial thalamic nuclei, limbic system
- supraspinal modulation, euphoria, respiratory depression

KAPPA
- spinal, dorsal horn (substantia gelatinosa), deep layers of cerebral cortex
- spinal modulation, sedation, pressed flexor reflexes

DELTA
- substantia nigra, GP, corpus striatum, limbic
- euphoria, sedation

SIGMA
- hippocampus
- dysphoria, hallucination, cerebrovascular

Question 5

ANALGESICS: Opioids

poppy seeds law

Answer 5

comprehensive drugs act of 2022

Question 6

ANALGESICS: Opioids

abstinence syndrome (15)

Answer 6

• sweating, runny nose, sneeze
• fatigue, weakness, insomnia, uncontrolled yawning, irritability,
• tachycardia
• body aches, gooseflesh, shivering
• stomach cramps, diarrhea, bye appetite

Question 7

ANALGESICS: Non-Opioid

acetaminophen - other name, active what of what, purpose (1.3), indications (3)

Answer 7

• paracetamol
• active metabolite of phenacetin
• anti-pyretic

NOT anti-inflammatory
- no prostaglandin inhibitor
- non-platelet inhibitor
- inhibits cyclooxygenase 3 (COX3)

INDICATIONS
- mild to mod fever
- allergic to aspirin
- fever

Question 8

ANALGESICS: Non-Opioid

pharmacokinetics - peak concentration, half life, metabolism, metabolites (3)

Answer 8

• peak blood concentration: 30-60 mins
• half life: 2-3h
• metabolism: hepatic microsomal enzyme

METABOLITES
- n-acetyl: nephrotoxic (kidney), hepatotoxic (liver)
- acetaminophen sulfate
- glucuronide

Question 9

ANALGESICS: Non-Opioid

adverse effects (8)

Answer 9

• inc hepatic enzyme
• dizzy, excitement, disorientation
• central lobular necrosis, renal tubular necrosis (liver)
• hemolytic anemia, methemoglobinemia

Question 10

NSAIDS:

COX 1 - main = 3 effects

COX 2 = main = 4 effects

Answer 10

COX1 = prostaglandin (homeostatic)
- renal homeostasis
- gastric mucosal production
- platelet

COX 2 = prostaglandin (inflammatory)
- pain
- fever
- inflammation
- little homeostatic effects

Question 11

NSAIDS:

damage = what substance, what acid = 2 pathways, eicosanoids what

thromboxanes - made by, effect (1=1) (2=1)

leukotrines - effect (2), condition

Answer 11

• damage cell membrane = phospholipid
• arachidonic acid = COX (prostaglandin & thromboxanes) & lipoxygenase (leukotrines)
• eicosanodis: initiate inflammation

THROMBOXANES
- synthesized by platelets
- platelet aggregation = clot
- bronchoconstriction & vasoconstriction = asthma

LEUKOTRINES
- bronchoconstriction, mucus production
- allergic rhinitis = inhibit this

Question 12

NSAIDS: Aspirin

what, inhibits what by what

anti-inflammatory (4)

Answer 12

• gold standard for NSAIDs
• inhibits prostaglandin synthesis by inhibiting COX enzyme

ANTI-INFLAMMATORY
- inhibits granulocyte from attaching to damaged cells
- stabilizes lysosome
- inhibits migration of leukocyte & macrocyte to inflammatory site

Question 13

NSAIDS: Aspirin

analgesic - for, how

anti-pyretic - how (1) (1=1=1)

inhibit what & therefore (2)

Answer 13

ANALGESIA
- mild to mod
- peripheral mechanism

ANTI-PYRETIC
- inhibits pyrogen-induced release of prostaglandin
- vasodilate = release heat = cool down

INHIBIT PLATELET AGGREGATION
- stroke & MI mx

Question 14

NSAIDS: Aspirin

absorption - where (2), peak plasma, protein binding

excretion - how, low dose vs. high dose (2)

dosage - kid vs. adult

Answer 14

ABSORPTION
- small intestine, stomach
- peak plasma concentration: 1-2h
- protein binding: 80-90%

EXCRETION
- urine alkalinization
- low dose: first order, t1/2 = 3-5h
- high dose: zero order, t1/2= 15h

DOSAGE
- kids: 50-70mg/kg/day
- adult: 4g/day

Question 15

NSAIDS: Aspirin

adverse effects (3.1.2)

Answer 15

• ulceration: GI mucosa irritation, absorb non-ionized salicylate, inhibit protective mechanism
• allergic reaction
• nephrotoxic, hepatotoxic

Question 16

NSAIDS: Aspirin

ASA intoxication - (3.1.1), mx (3)

Answer 16

salicylism
- tinnitus, dec hearing, vertigo

hyperpnea
- respiratory alkalosis

seizure
- acidosis

MX: alkalinize urine, gastric lavage, ventilatory assist

Question 17

NSAIDS: Aspirin

COX drug

Answer 17

COX2 inhibitor (COXIBS)
- inhibits only bad COX so bye inflammatory