Opioids & exam review #1

Question 1

drug used for arthritis pain and treat information

Answer 1

Non-opioid analgesics (NSAIDs)
(non steroidal anti-inflammatory drugs)

thins blood

we don’t use in OR

Question 2

drugs used for neuropathic pain

Answer 2

opioids
anticonvulsants
tricyclic antidepressants
serotonin/norepinerphrine reuptake inhibitors

mostly used in OR, opioids is most common one used post op

anticonvulsants is used –> alleviate nerve pain gabapentin

Question 3

severe or chronic nociceptive pain

Answer 3

opioids in select patients

Question 4

opioid drugs

Answer 4

natural
semisynthetic
synthetic

Mechanism of Action:
bind to specific opioid receptors in the CNS to produce effects that mimic endogenous neurotransmitters (endorphins, enkephalins, and dynorphins

place in therapy:
- relieve intense pain
widespread availability has led to abuse of agents with euphoric properties
antagonists that reverse the actions of opioids are also clinically important for use in cases of overdose

Question 5

opioid receptor
will be on test slide 10

Answer 5

mu receptor –>

kappa

delta

all three receptors are members of the g protein

g couple protein recetor

Question 6

Opioid agonist

Answer 6

Morphine:
major analgesic drug contained in crude opium
- prototype strong mu (u) receptor agonist

Question 7

morphine

Answer 7

interacts with opioid receptors on the membranes of certain cells in the CNS & other anatomic structures, such as the gastrointestinal tract and the urinary bladder

Question 8

side effects produced by morphine

Answer 8

respiratory depression
- reduces sensitivity of erspiratory center neurons to carbon dioxide

depression of cough reflux
- morphine and codeine have antitussive properties

miosis
- pinpoint pupil characterisitc of morphine use results from stimulation of mu and kappa receptors
-

Question 9

acions produced by morphine

Answer 9

morphine causes EMESIS
morphine directly stimulates the chemoreceptor trigger zone in the area postrema that causes vomiting

GI tract

produces constipation
might see some fluctuations in bilirubin

cardiovascular
- no major effects
can see hypotension and bradycardia
any opioid if you over do it you will see hypotension and brady cardia

morphine has more of an effect when compared to opioids

Question 10

pharmacokinetics of morphine

Answer 10

first-pass metabolism (goes through the liver for metabolism)

linear pharmacokinetics

Question 11

if a pts renal function is low what can you do in order to prevent increased side effects when giving morphine?

Answer 11

we can extend the intervals when giving the drug so we can give pts body enough time to clear the medication

Question 12

oxycodone

Answer 12

semisynthetic
can be combined with diff medications

first pass metabolism, metabolism in liver by CYP450

excreted by kidneys

Question 13

how would you ween off patient? oral or IV?

Answer 13

always try to switch to oral first, and gradually reduce the dose

Question 14

hydromorphone

Answer 14

low volume of distribution,stays in your intravascular space

Semisynthetic – less allergic reactions

MUCH more POTENT

Oral hydromorphone is approx. 8 to 10 times more potent than morphine

Have to use much smaller doses

Question 15

fentanyl

Answer 15

metabolized through liver CYP450

synthetic opioid

highly lipophilic, crosses blood brain barrier easily (disadvantage?)

given as infusion

Rapid onset and short duration of action, have to give it more frequently will be through infusion

Question 16

There are other opioids (sister drugs and can be used in specific case in OR

Answer 16

for example

fentanyl
sufantanil
alfentanil
remifentanil

Question 17

methadone pharmacokinetics

Answer 17

Use methadone to occupy receptor, it doesn’t cause the high effects, so the patients do not have the cravings

actions mediated by u preceptors

antagonist of NMDA receptor

metabolized by the liver CYP450

very lipophilic, half live ranges from 12-40 hours

stays in system very long –> can accumulate due to long terminal half life (leading to toxicity)

Question 18

meperidine

Answer 18

most commonly used for shivering

crosses blood brain barrier, can cause seizures

short half life, low potency synthetic opioid

Question 19

have to understand potency curve and what it means

Question 20

what are mixed agonist - antagonists?

Answer 20

Answer: Drugs that stimulate one receptor but block another, effects depend on previous exposure to opioids, in opioid naïve patients, mixed agonist–antagonists show agonist activity and are used to relieve pain

In the patient with opioid dependence, the agonist–antagonist drugs may show primarily blocking effects (i.e., produce withdrawal symptoms)

Question 21

buprenorphine

Answer 21

subaxin?

• partial agonist
• acts like morphine in naïve patients (patient who never took meds like that before)
• use it for addiction, similar like methadone. But you wouldn’t have to experience the effect like opioids. It was designed for same purpose as heroin
• block the effect of heroin

Question 22

opioid antagonist

Answer 22

bind with high affinity to opioid receptors

fail to activate the receptor-mediated response

administration of opioid antagonists produces no profound effects in normal individuals

in patients dependent on opioids, antagonists rapidly reverse the effect of agonists, such asmorphineor any full μ agonist, and precipitate the symptoms of opioid withdrawal

Question 23

naloxone

Answer 23

reverses coma and respiratory depression of opioid overdose

nasal or IV

works very rapidly

half life is 30 to 81 minutes

mechanism of action mu, kappa (k), delta

10 fold higher affinity for u (mu) than K (kappa) receptors