3 - Analgesics

Question 1

what is the classic mechanism by which all NSAIDs work?

Answer 1

act by inhibiting the synthesis of prostaglandins

Question 2

what are the 3 NSAID drugs?

Answer 2

acetaminophen (tylenol - not an NSAID), ibuprofen (advil) and celecoxib (celebrex)

Question 3

what are the indications for acetaminophen?

Answer 3

pain (mild) and fever

Question 4

what is the pharmacology for acetaminophen?

Answer 4

analgesic and antipyretic

Question 5

what is the mechanism of action for acetaminophen?

Answer 5

acts by inhibiting COX and enhancing 5-HT release

also acts centrally at hypothalamus - PG synthetase inhibition

Question 6

in what ways is acetaminophen different from aspirin?

Answer 6

no inflammatory control, no platelet inhibition, central pain relief only, no GI effects and is SAFE in pregnancy

Question 7

what are the common side effects of acetaminophen?

Answer 7

nausea, rash, headache

Question 8

what are the hepatic side effects for acetaminophen?

Answer 8

acute hepatoxicity usually with high doses (>4000mg)

*drug of choice for suicide

Question 9

what are the renal side effects for acetaminophen?

Answer 9

acute renal tubular necrosis and chronic analgesic nephropathy

Question 10

what happens if you take acetaminophen with a combo acetaminophen/antihistamine drug?

Answer 10

there is an additive effect - hepatoxicity

Question 11

what happens if you take acetaminophen with ASA?

Answer 11

there is an additive effect - nephrotoxicity

Question 12

what happens if you take acetaminophen with topical lidocaine?

Answer 12

there is an additive effect - methemoglobinemia

Question 13

what are the indications for ibuprofen?

Answer 13

mild to moderate pain, primary dysmenorrhea and fever

Question 14

what is the mechanism for ibuprofen?

Answer 14

inhibits COX and reduces PG and TXA2 synthesis

Question 15

what are the common side effects for ibuprofen?

Answer 15

headache, fluid retention, ecchymosis, and photosensitivity

Question 16

what are the neuro side effects for ibuprofen?

Answer 16

tinnitus

Question 17

what are the renal side effects for ibuprofen?

Answer 17

acute renal tubular necrosis and chronic analgesic nephropathy

Question 18

what happens if you take ibuprofen with ASA or acetaminophen?

Answer 18

there is an additive effect - hemorrhagic risk

Question 19

what happens if you take ibuprofen with acetaminophen or cyclosporine?

Answer 19

there is an additive effect - nephrotoxicity

Question 20

what are the indications for celecoxib?

Answer 20

arthritis, ankylosing spondylitis, dysmenorrhea and acute pain

Question 21

what is the mechanism of action for celecoxib?

Answer 21

selectively inhibits COX2 only and reduces PG synthesis

Question 22

what are the common side effects for celecoxib?

Answer 22

headaches

Question 23

what are the cardiovascular black box warnings for celecoxib?

Answer 23

stroke, CHF, MI

Question 24

what are the GI black box warnings for celecoxib?

Answer 24

bleeding and ulceration/perforation = although these are minimal

Question 25

what are the GI black box warnings for celecoxib?

Answer 25

bleeding and ulceration/perforation = these are minimal

Question 26

what happens if you take celecoxib with NSAIDs (Ketorolac) or corticosteroids?

Answer 26

hemorrhage

Question 27

what happens if you take celecoxib with azoles?

Answer 27

the metoblism of celecoxib is impaired

Question 28

what is the contraindication/caution with celecoxib?

Answer 28

sulfonamide allergy

Question 29

what type of pain do you use opioids for?

Answer 29

severe or chronic malignant or nonmalignant pain

Question 30

what are the 4 types of opioids?

Answer 30

hydrocodone/acetaminophen (Vicodin), oxycodone (ocycontin), meperidine (demerol), fentanyl (duragesic)

Question 31

what is the indication for hydrocodone/acetaminophen?

Answer 31

moderate - moderately severe pain

Question 32

what is the pharmacology for hydrocodone?

Answer 32

FDA schedule II controlled narcotic analgesic and antitussive

Question 33

what is the mechanism of action for hydrocodone?

Answer 33

acts through G-protein coupled Mu, Kappa, Delta opioid receptors inhibits adenylyl cyclase activity and enhances K+ outflow = this hyperpolarizes nerves affecting neuronal excitability and muscle tone also stimulates prolactin and growth hormone release

Question 34

what are some common side effects for hydrocodone?

Answer 34

lightheadedness, dizziness, sedation, miosis (no tolerance), pruritus and flushing (histamine release - little tolerance) **miosis and itching**

Question 35

what are the CNS side effects for hydrocodone?

Answer 35

drowsiness, mood changes, elevated intracranial pressure - enhanced with head injury

Question 36

what are the cardiovascular side effects for hydrocodone?

Answer 36

bradycardia/tachycardia and orthostatic hypotension

Question 37

what are the respiratory side effects for hydrocodone?

Answer 37

dose-related respiratory depression at brain stem respiratory center (how you die from overdose)

Question 38

what happens if you take hydrocodone/acetaminophen with anticholinergics?

Answer 38

additive effects is seen - constipation and paralytic ileus

Question 39

what happens if you take hydrocodone/acetaminophen with sedating classic antihistaminics?

Answer 39

additive CNS depression

Question 40

what happens if you take hydrocodone/acetaminophen with CAIs?

Answer 40

the acetaminophen impairs renal excretion of CAI - leading to CNS toxicity and metabolic acidosis

Question 41

what is contraindicated/cautioned with hydrocodone/acetaminophen?

Answer 41

mydriatic procedures

Question 42

what is the other analgesic (non NSAID or opioid)?

Answer 42

tramadol (ultram)

Question 43

what is the indication for tramadol?

Answer 43

moderate - moderate severe pain

Question 44

what is the pharmacology for tramadol?

Answer 44

central acting synthetic opioid analgesic

Question 45

what is the mechanism of action for tramadol?

Answer 45

agonist at Mu receptors only and a weak inhibitor of NE/5-HT re-uptake the mu agonist effect is greater with an active metabolite

Question 46

what other drug class mechanism is similar to tramadol?

Answer 46

SNRIs = also inhibit NE and 5-HT re-uptake

Question 47

what are the common side effects for tramadol?

Answer 47

headache, pruritus and flushing

Question 48

what are the respiratory side effects for tramadol?

Answer 48

bronchospasm and respiratory depression

Question 49

what are the CNS side effects for tramadol?

Answer 49

serotonin syndrome, seizures, and suicidal ideation

Question 50

what are the cardiovascular side effects for tramadol?

Answer 50

orthostatic hypotension

Question 51

what happens if you take tramadol with anticholinergics?

Answer 51

additive effect - constipation and paralytic ileus

Question 52

what happens if you take tramadol with sedating classic antihistaminics?

Answer 52

additive effect - CNS depression

Question 53

what happens if you take tramadol with azole antifungals?

Answer 53

the metabolism of tramadol is impaired