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Systemic Pharmacology > 3 - Analgesics > Flashcards

3 - Analgesics Flashcards

1
Q

what is the classic mechanism by which all NSAIDs work?

A

act by inhibiting the synthesis of prostaglandins

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2
Q

what are the 3 NSAID drugs?

A

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

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3
Q

what are the indications for acetaminophen?

A

pain (mild) and fever

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4
Q

what is the pharmacology for acetaminophen?

A

analgesic and antipyretic

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5
Q

what is the mechanism of action for acetaminophen?

A

acts by inhibiting COX and enhancing 5-HT release

also acts centrally at hypothalamus - PG synthetase inhibition

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6
Q

in what ways is acetaminophen different from aspirin?

A

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

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7
Q

what are the common side effects of acetaminophen?

A

nausea, rash, headache

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8
Q

what are the hepatic side effects for acetaminophen?

A

acute hepatoxicity usually with high doses (>4000mg)

*drug of choice for suicide

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9
Q

what are the renal side effects for acetaminophen?

A

acute renal tubular necrosis and chronic analgesic nephropathy

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10
Q

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

A

there is an additive effect - hepatoxicity

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11
Q

what happens if you take acetaminophen with ASA?

A

there is an additive effect - nephrotoxicity

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12
Q

what happens if you take acetaminophen with topical lidocaine?

A

there is an additive effect - methemoglobinemia

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13
Q

what are the indications for ibuprofen?

A

mild to moderate pain, primary dysmenorrhea and fever

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14
Q

what is the mechanism for ibuprofen?

A

inhibits COX and reduces PG and TXA2 synthesis

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15
Q

what are the common side effects for ibuprofen?

A

headache, fluid retention, ecchymosis, and photosensitivity

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16
Q

what are the neuro side effects for ibuprofen?

A

tinnitus

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17
Q

what are the renal side effects for ibuprofen?

A

acute renal tubular necrosis and chronic analgesic nephropathy

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18
Q

what happens if you take ibuprofen with ASA or acetaminophen?

A

there is an additive effect - hemorrhagic risk

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19
Q

what happens if you take ibuprofen with acetaminophen or cyclosporine?

A

there is an additive effect - nephrotoxicity

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20
Q

what are the indications for celecoxib?

A

arthritis, ankylosing spondylitis, dysmenorrhea and acute pain

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21
Q

what is the mechanism of action for celecoxib?

A

selectively inhibits COX2 only and reduces PG synthesis

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22
Q

what are the common side effects for celecoxib?

A

headaches

23
Q

what are the cardiovascular black box warnings for celecoxib?

A

stroke, CHF, MI

24
Q

what are the GI black box warnings for celecoxib?

A

bleeding and ulceration/perforation = although these are minimal

25
Q

what are the GI black box warnings for celecoxib?

A

bleeding and ulceration/perforation = these are minimal

26
Q

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

A

hemorrhage

27
Q

what happens if you take celecoxib with azoles?

A

the metoblism of celecoxib is impaired

28
Q

what is the contraindication/caution with celecoxib?

A

sulfonamide allergy

29
Q

what type of pain do you use opioids for?

A

severe or chronic malignant or nonmalignant pain

30
Q

what are the 4 types of opioids?

A

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

31
Q

what is the indication for hydrocodone/acetaminophen?

A

moderate - moderately severe pain

32
Q

what is the pharmacology for hydrocodone?

A

FDA schedule II controlled narcotic analgesic and antitussive

33
Q

what is the mechanism of action for hydrocodone?

A

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

34
Q

what are some common side effects for hydrocodone?

A

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

35
Q

what are the CNS side effects for hydrocodone?

A

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

36
Q

what are the cardiovascular side effects for hydrocodone?

A

bradycardia/tachycardia and orthostatic hypotension

37
Q

what are the respiratory side effects for hydrocodone?

A

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

38
Q

what happens if you take hydrocodone/acetaminophen with anticholinergics?

A

additive effects is seen - constipation and paralytic ileus

39
Q

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

A

additive CNS depression

40
Q

what happens if you take hydrocodone/acetaminophen with CAIs?

A

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

41
Q

what is contraindicated/cautioned with hydrocodone/acetaminophen?

A

mydriatic procedures

42
Q

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

A

tramadol (ultram)

43
Q

what is the indication for tramadol?

A

moderate - moderate severe pain

44
Q

what is the pharmacology for tramadol?

A

central acting synthetic opioid analgesic

45
Q

what is the mechanism of action for tramadol?

A

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

46
Q

what other drug class mechanism is similar to tramadol?

A

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

47
Q

what are the common side effects for tramadol?

A

headache, pruritus and flushing

48
Q

what are the respiratory side effects for tramadol?

A

bronchospasm and respiratory depression

49
Q

what are the CNS side effects for tramadol?

A

serotonin syndrome, seizures, and suicidal ideation

50
Q

what are the cardiovascular side effects for tramadol?

A

orthostatic hypotension

51
Q

what happens if you take tramadol with anticholinergics?

A

additive effect - constipation and paralytic ileus

52
Q

what happens if you take tramadol with sedating classic antihistaminics?

A

additive effect - CNS depression

53
Q

what happens if you take tramadol with azole antifungals?

A

the metabolism of tramadol is impaired

Systemic Pharmacology (6 decks)

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