Opioids and Opioid Antangonists Flashcards by Anna Logan

What is a natural opioid and give example

Naturally derived from opium

morphine

How well did you know this?

Not at all

Perfectly

What is a synthetic opioid and give example

Manufactured by synthesis

fentanyl

How well did you know this?

Not at all

Perfectly

What is a semisynthetic opioid and give example

Chemical modification of morphine

herioin

How well did you know this?

Not at all

Perfectly

What type of receptors do opioids bind?

G coupled protein receptors

How well did you know this?

Not at all

Perfectly

Where in the body do opioids bind to receptors?

brain and spinal cord

How well did you know this?

Not at all

Perfectly

What are the endogenous opioid ligands?

Enkephalins
Endorpins
Dynorphins

How well did you know this?

Not at all

Perfectly

How do opioids affect neurotransmitter release?

decrease

How well did you know this?

Not at all

Perfectly

in the brain and spinal cord, where are opioid receptors?

Periaqueductal gray matter
amygdala
Corpus striatum
Hypothalamus
Spinal cord (substantia gelatinosa)

How well did you know this?

Not at all

Perfectly

where is the mu1 receptor located?

supraspinal and spinal

How well did you know this?

Not at all

Perfectly

What are the effects of the Mu1 receeptor?

Analgesia--main action
Euphoria
N/V, Pruritis
Low abuse potential
Bradycardia

How well did you know this?

Not at all

Perfectly

What binds to the Mu1 receptor?

Endorphins, morphine and sythetic opioids

How well did you know this?

Not at all

Perfectly

Where is the Mu2 receptor?

spinal

How well did you know this?

Not at all

Perfectly

What are the effects of the Mu2 receptor?

Hypoventilation
analgesia
Euphoria, Sedation
Physical dependence
Constipation

How well did you know this?

Not at all

Perfectly

What binds to MU2 receptor?

Endorphins, morphine and sythetic opioids?

How well did you know this?

Not at all

Perfectly

Where is the kappa receptor?

Supraspinal, spinal

How well did you know this?

Not at all

Perfectly

What are the effects of the kappa receptor?

Analgesia
Respiratory depression
Dysphoria
diuresis

How well did you know this?

Not at all

Perfectly

What binds to the kappa receptor?

Dynorphins
Agonist-antagonist principally
Nalbuphine

How well did you know this?

Not at all

Perfectly

How is the kappa receptor in relation to high intensity pain?

resistant

How well did you know this?

Not at all

Perfectly

Where are the delta opioid receptors?

supraspinal, spinal

How well did you know this?

Not at all

Perfectly

What are the effects of the delta receptor?

Analgesia
Respiratory depression
Physical dependence
Urinary retention

How well did you know this?

Not at all

Perfectly

What binds to delta receptors?

enkaphalins

How well did you know this?

Not at all

Perfectly

Which receptors cause respiratory depression?

Mu2, Kappa, and delta

How well did you know this?

Not at all

Perfectly

Which receptor would give you the feeling “I feel like I am going to die”?

Kappa

How well did you know this?

Not at all

Perfectly

which receptor is associated with constipation?

Mu2

How well did you know this?

Not at all

Perfectly

Which receptors are associated with physical dependence?

Mu2 and Delta | kappa has low abuse potential

what are the 4 classic side effects of neuraxial opioids?

Pruritis N/V Urinary retention Ventilatory depression

Are neuraxial opioid specific or somatic or visceral pain?

visceral

What are the cardiovascular effects of most opioids? | What is the exception?

decrease sympathetic tone and therefore decrease BP, HR. There are minimal effects on the contractility Merperidine is the exception, it has anti muscarinic effects

How do opioids affect RR, Vt, MV, and PaCO2?

Decrease RR, INcrease Vt, but overall decreases MV, and thus increases PaCO2

What effect do opioids have on cough?

supress

What effects do opioids have on MAC?

reduce

What effects do opioids have on cerebral blood flow, metabolic rate and ICP?

Decrease CBF and CMRO2 | ICP increases due to increase PaCO2 from hypoventilation

Which opioid may cause siezures?

Merperidine, from accumulation of normerperidine

What is biliary colic?

Spasm of the sphincter of Oddi Feels similar to angina If not relieved by NTG then it is biliary colic

What can you give to relieve pain associated with biliary colic?

nalaxone

How do you reverse biliary colic?

Glucagon 2mg IV

What are the GI side effects of Opioids?

N/V constipation delayed gastric emptying biliary colic

Whar are the GU side effects of opioids?

Urinary retention due to increase in tone of ureter and vesicle sphincter

Which two opioids cause the most histamine release?

morphine and merperidine

what opioid side effect is associated with the Erdinger-Westphal nucleus?

Miosis--oculomotor nerve

What side effect of opioids is associated with difficulty to bag mask pt?

truncal rigidity

Which two effects of opioids aren't subject to tolerance?

Constipation and miosis

What are the triad of symptoms for an opioid overdose?

Miosis Respiratory depression Coma

What is the onset of morphine?

15-30 min onset with peak effect at 45-90 min

What is the peak effect of morphine?

45-90 min

What is the duration of morphine?

3-4 hours

How is morphine metabolized? What is the metabolite and how does it compare to morphine?

Metabolized via conjugation with glucuronic acid in liver and in kidney. Its metabolite is morphine-6-gucuronide, which is more potent than morphine

What is the dose for intraoperative analgesia of morphine?

.1/-1mg/kg

How does merperidine compare to morphine?

0.1 potency

How can merperidine be delivered?

IV, IM or PO?

How can morphine be delivered?

IV, IM

Wha tis the peak effect and duration time for merperidine?

Peak: 5-7 min Duration: 2-4 hours

How does merperidine behave like atropine/local?

blocks sodium channel | causes tachycardia, dry mouth, mydriasis

How is merperidine metabolized?

90% hepatic metabolism to normeperidine, which is renally eliminated

What is the dose of merperidine for post-op shivering?

12.5-25mg--1 time dose

how does fentanyl compare to morphine?

75-125 times more potent

Waht is the peak ffect and duration of fentanyl?

peak: 3-5 minutes | duration 30-60 min

how can fentanyl be administered?

IV, transdermal, PO, intranasal

Fentanyl is _____ soluble and protein bound

lipid

Where is the first pass uptake of fentanyl?

lungs--up to 75%

HOw does sufentanil compare to fentanyl?

5-10x as potent with greater affinity for opioid receptor

what is the peak and duration of sufentanil?

Peak 3-5 minutes, duration 30-60 minutes

What is the dose for DL of sufentanil?

0.3-1mcg/kg 1-3 minutes before DL

What is the infusion rate for sufentanil?

0.5 mcg/kg followed by 0.5 mcg/kg/hr

How does alfentanyl compare to fentanyl?

1/10-1/5 as potent

What is the duration and peak of alfentanyl?

Peak 1.5-2 minutes | Duration 10-20

HOw does renal failure affect Alfentanyl?

does not alter clearance

What are the uses for alfentanyl?

Because of its rapid on and off of intense analgesia, it is good for retrobulbar block or DL

What is the dose for alfentanyl?

5-10 mcg/kg

How does remifentanyl compare to fentanyl?

similar potency

What is the peak effect and duration of remifentanyl?

peak 1.5-2 minutes | Duration 6-12 minutes

How is remifentanyl metabolized?

plasma and tissue esterases

How can remifentanyl be used?

RBB, continuous drip; quick recovery cases

What is the dose and drip rate for remifantanyl for DL?

0.5-1mcg/kg, then 0.25-0.5 mcg/kg/min

What are the uses of codeine?

antitussive | analgesia for mild to moderate pain

What are the uses for methadone?

long term relief of chronic pain and opioid withdrawl

How does dilaudid compare to morphine?

8x as potent but shorter acting

What type of drugs are Pantozocine, butorphanol and nalbuphine? What are the advantage?

Partial agonist and/or competitive antagonist at opioid receptors Produce analgesia with limited respiratory depression, but do have a ceiling effect

Name two opioid antagonists and routes of administration.

Nalaxone-IV | Naltrexone-po

Which opioid receptors does nalaxone antagonize?

pure Mu antagonist

What is the duration of nalaxone?

30-45 minutes

What is the dose of nalaxone?

1-4mcg/kg | Dilute 400mcg vial in 100 and give 1-2 cc over 2-3 minutes

What are the side effects of nalaxone?

N/V Pain tachycardia Increased SNS activity

Opioids and Opioid Antangonists Flashcards

(83 cards)