Pharm - Analgesics and Anti-inflammatories

Question 1

Full opioid agonist exemplar

Answer 1

Morphine

Question 2

Morphine metabolism

Answer 2

Absorbed from GI tract, extensively metabolized during first pass
Principle metabolite (90%) is inactive
Morphine-6-glucuronide (~10%) is more active than morphine

Question 3

Morphine indications

Answer 3

severe pain from trauma, MI, cancer

Question 4

Full agonists effectiveness

Answer 4

Fentanyl&raquo_space; morphine > codeine

Question 5

Partial opioid agonist exemplar

Answer 5

Tramadol

Question 6

Tramadol mechanism

Answer 6

partial mu-opioid agonist
inhibits reuptake of 5HT and NE
analgesic effect mediated by M1 metabolite

Question 7

Tramadol drawbacks

Answer 7

M1 metabolite mediated by CYP2D6, which is highly polymorphic
like giving morphine and SNRI in unknown ratio

Question 8

Tramadol side effects

Answer 8

Hypoglycemia, decreased seizure threshold

interacts with antidepressants

Question 9

Opioid antagonists mechanism

Answer 9

Bind to opioid receptors and prevent conformational change needed for activation and agonist activity

Question 10

Opioid antagonists exemplar

Answer 10

Naloxone

Question 11

Naloxone indications

Answer 11

Opioid OD, added to oral opioid agonists to curb using IB

Question 12

Non-specific COX inhibitors exemplars

Answer 12

ASA, ibuprofen

Question 13

ASA mechanism

Answer 13

irreversible inhibition if COX by covalently binding to COX, remaining is competitive inhibitor

Question 14

ASA CI

Answer 14

Children with viral infections d/t Reye syndrome

Question 15

ASA adverse effects

Answer 15

GI irritation/ ulcers/ bleeding
Tinnitus
High doses - hyperventilation, fever, dehydration, metabolic acidosis, impairment of hemostasis
Hypersensitivity reactions uncommon but fatal

Question 16

Ibuprofen adverse effects

Answer 16

GI irritation, nausea, dyspepsia, bleeding
hepatic toxicity
renal toxicity incl acute renal failure if dehydration occurs

Question 17

COX-2 specific inhibitors exemplar

Answer 17

Celecoxib

Question 18

Celecoxib info

Answer 18

potent anti-inflammatory without significant GI toxicity

does not inhibit platelet aggregation

Question 19

Non-specific COX inhibitors w/out anti-inflammatory effect exemplar

Answer 19

acetaminophen

Question 20

Acetaminophen mechanism

Answer 20

Little effect on COX-1 or 2, affinity for COX-3

Question 21

Acetaminophen drawbacks

Answer 21

Toxic intermediate formed, relevant in alcohol use disorder, OD scenario, glutathione depletion –> can lead to hepatic necrosis