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Neuro mid term > pharm- opioid analgesics > Flashcards

pharm- opioid analgesics Flashcards

1
Q

what is the critical role of opioids

A

balanced anesthesia and perioperative pain management

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2
Q

what is synergism?

A

combining opioids with other sedatives

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3
Q

what is done to minimize the risk of adverse effects of opioids?

A

dose adjustments

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4
Q

what are considered semisynthetic opioids

A

simple modifications of the morphine molecule

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5
Q

what are more complex, mixed agonist- antagonists opioids

A

nalbuphine and even complete antagonists such as naloxone

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6
Q

what was the first completely synthetic opioid ?

A

meperidine

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7
Q

the mechanism of action of opioids cause an activation of ________, causing inhibitory effects, these inhibitory effects cause _____________, then causing a reduction of ___________

A

G protein

hyperpolatization

neuronal excitability

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8
Q

opioid receptors are linked to G proteins, activation of Gi leads to decreased _____

A

cAMP

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9
Q

what multiple sites are affected by opioids?

A

dorsal horn of the spinal cord, brainstem, forebrain

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10
Q

absorption of opiates via IM, SC routes is rapid and reaches peak plasma levels within ____

A

30 min

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11
Q

Oral absorption of opiates is rapid and has a significant firsta pass ratio with a los ____/_____ ratio

A

oral/ parenternal

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12
Q

opiates rapidly conjugates with ______ in the _____ and ______

A

glucuronide

liver and intestine

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13
Q

what is the active metabolite of morphine

A

morphine-6-glucoronide

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14
Q

does morphine cross placenta?

A

yes

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15
Q

what is the main CNS effect of opioids

A

analgesia - interferes with forebrain mechanisms, inhibits conduction

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16
Q

what side effects to the CNS can opiates have?

A

behavioral effects such as dysphoria followed by euphoria, sedation, drowsiness, and mental clouding, antitussive (direct action on medulla to suppress cough reflex)

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17
Q

what effect do opiates have on hypothalamus?

A

decreases body temp., decreases ACTH, FSH, LH, TSH

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18
Q

what effect do opiates have on respiration?

A

respiratory depression

OD death by resp. failure

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19
Q

what effect do opiates have on GI tract?

A

increase tone and decrease peristalsis (constipation)

20
Q

what effect do opiates have on biliary tract?

A

gall bladder or bile duct spasm due to increased biliary pressure

21
Q

what effect do opiates have on urinary tract?

A

increased muscle tone and decreased urinary output

22
Q

what effect do opiates have on cardiovascular system and brain?

A

orthostatic hypotension as a result of CNS actions, histamine release

cerebral vasodilation increasing CSF pressure

23
Q

what effect to opiates have on immune system?

A

suppression of function of NK cells

24
Q

what is wood thorax?

A

when rapid administration and large doses of fentanyl make ventilation via a bag and mask impossible because of vocal cord rigidity and closure

25
Q

acute toxic symptoms of opiates include a triad of __?

A

coma, pinpoint pupils, respiratory depression

26
Q

how do you treat toxicity of opiates?

A

maintain respiration, opioid antagonists (naloxone)

27
Q

a prodrug: where morphine is the active compound and is metabolized by O-demethylation into morphine by the liver (CYP2D6)

A

codeine

28
Q

a patient with a lack of CYPD26 would not benefit from what opioid?

A

codeine

29
Q

a prototype opioid replaced by fentanyl as the most used intraoperative, with a prolonged latency to peak effect

A

morphine

30
Q

what opioid penetrates the CNS slowly making it less likely to cause respiratory distress?

A

morphine

31
Q

what opiates active metabolite is M6G?

A

morphine

32
Q

what is the most important opioid in modern anesthesia practice?

A

fentanyl

33
Q

what routes can fentanyl be administrated?

A

intravenous , transdermal, transmucosal, transnasal, and transpulmonary

34
Q

fentanyl has a high first pass avoidance this means?

A

larger bioavailability

35
Q

what route administration is best for pain in opioid tolerant cancer patients

A

oral transmucosal (OTFC) + transdermal fentanyl patch

36
Q

what was the first opioid to be administered by continuous infusion?

A

alfentanil

37
Q

short acting opioid with high diffusible fraction, reaches peak effect effect site concentrations quickly

A

alfentanil

38
Q

what opioid has an unpredictable hepatic metabolism with significant interindividual variability of hepatic CYP3A4

A

alfentanil

39
Q

what is the most potent opioid commonly used in anesthesia? 1000 fold less than morphine dose

A

sufentanil

40
Q

opioid with specific clinical goals: very short acting opioid, losing u-receptor agonist activity upon ester hydrolysis. drug that can be titrated up and down as necessary/ used in total intravenous anesthesia

A

remifentanil

41
Q

class of drugs that is a partial agonist and competitive antagonist at the U receptor

A

opioid agonist-antagonist

42
Q

what class of drugs have ceiling effect? what does that mean?

A

opioid agonist-antagonists

analgesics with more limited ventilatory depression (less analgesia)

43
Q

tramadol, buprenorphine, and nalbuphine are

A

opioid agonist- antagonists

read slide on info of those

44
Q

what are pure opioid antagonists

A

complete competitive antagonists of the opioid receptor, used for opioid overdose

45
Q

injectable u antagonist

A

naloxone/naltrexone

46
Q

go over guides for rational use of opiod analgesics

A

:)

Neuro mid term (9 decks)

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