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*Pharmacology > Nagelhout Video's- Opioid Agonists/Antagonists > Flashcards

Nagelhout Video's- Opioid Agonists/Antagonists Flashcards

1
Q

What are the 3 endogenous groups of opioids

A

Enkephalins
Endorphins
Dynorphins

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2
Q

What is the oral form of narcan?

A

Naltrexone

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3
Q

Which opioid receptor is responsible for dysphoria?

A

Kappa

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4
Q

Which opioid receptor has an anti-shivering effect?

A

Kappa

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5
Q

What would happen if you gave buprenorphine to someone after giving them morphine?

A

Their pain would get worse (agonist/antagonist or partial agonist)

> alone, this drug will give some analgesia, but if given after a more potent analgesic it will result in increased pain

Buprenorphine (pronounced ‘bew-pre-nor-feen’

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6
Q

what does alkaloid in chemistry mean?

A

naturally occurring, comes from a plant and has pharamacologic effects

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7
Q

phenanthrene alkaloid prototypes (2)

A

Morphine, Codeine

(naturally occuring)`

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8
Q

Semi-synthetic phenanthrene alkaloids (5)

A

HHHO

Heroin
Hydrocodone (Vicodin)
Hydromorphone (Dilaudid)
Oxycodone (Oxycotin)

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9
Q

Phenylpiperidines protype (1)

+4

A

meperidine (Demerol)

(fentanyl, su, al, remi)

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10
Q

If your allergic to a phenanthrene… are you allergic to all phenanthrenes?

A

Yes!

But your not allergic to the phenylipiperidines or the methadones

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11
Q

T/F- all the phenanthrenes cause histamine release

A

True AND Demerol

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12
Q

List the potency of opioids from weakest to strongest:

Remi
Fentanyl
Su
Meperidine
Alfentanil
Morphine
Hydromorphone

A

Meperidine (0.1)
Morphine (1)
Hydromorphone (7)
Alfentanil (10)
Remi (100)
Fentanyl (100)
Sufentanil (1000)

How to remember potency of fentanyl family:

AR Fifteen’S
Al Remi Fent Su

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13
Q

What is remi metabolized by?

A

Nonspecific esterases in the plasma

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14
Q

What’s special about codeine?

A

It’s not an active drug. It’s a prodrug- meaning it becomes active once it’s in the body and it becomes metabolized to it’s active form – morphine and it’s actually morphine that relieves the pain (0.4x less potent then actual morphine)

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15
Q

Why can’t you give codeine to kids?

A

Because if they are fast metabolizers, they will produce higher levels of morphine than expected and it can lead to respiratory depression

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16
Q

What is demerol metabolized to?

What’s the concern?

Who should it be avoided in?

A

Normerperidine

*lowers the seizure threshold! and increases CNS excitability

*HD and old peeps (cant pee out the metabolite)

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17
Q

Any patient on what kind of drug cannot receive demerol?

What drugs fall under this category 5()

A

MAOi’s

Isocarboxizid
Phenelzine
Tranylcypromine

Selegiline
Rasagiline

(seizures, severe cardiac issues)

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18
Q

Why does remifentanil have a low Vd if it’s very lipophilic?

A

Because it’s metabolized in the plasma before it can distribute to other compartments.

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19
Q

What opioid is based on Lean Body weight and why?

3 other drugs based on LBW we use

A

Remifentanil

-because despite it being lipophilic, it behaves like a drug that has a low Vd bc it is rapidly metabolized in the plasma. So the extra fat someone has doesn’t matter.

[vec/roc/cist]

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20
Q

Duration of remifentanil (hours and minutes)

A

0.1 hour
= 6 minutes

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21
Q

One reason you want to front load your opioids

A

Because the most stimulating aspects of surgery are at the beginning –> #1 intubation, #2 skin incision

skin closure is the least stimulating

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22
Q

Opioids shift the CO2 response curve to the right or left

A

Right

(fancy way of saying the cause respiratory depression)

> minute ventilation is lower than expected for a given CO2 level

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23
Q

What’s the purpose of lowering the resp rate at the end of the case?

A

To build up CO2 - opioids shift the CO2 response curve to the right, so it’s going to take a higher CO2 than normal to stimulate them to breathe

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24
Q

If opioids don’t have a direct effect on BP, why do we give it during the case when the BP goes up?

A

Because your treating the sympathetic response to pain and when the pain goes away, the blood pressure drops.

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25
T/F- opioids cause orthostatic hypotension
True for the histamine releasing opioids - histamine vasodilates, blood pools in legs, go to sit up and get dizzy.
26
T/F- giving 100 of fentanyl prior to the doc coming in for induction should not cause a drop in the patient's BP. What will it cause?
True -A drop in HR
27
T/F- opioids have a cough suppressing effect
True! -but can also cause coughing due to reduced sympathetic outflow > parasympathetic dominates - ACH on muscarinic receptors in the lungs - cough
28
What two effects of opioids do you never develop tolerance to?
1. Miosis 2. Constipation
29
Is miosis a parasympathomimentic effect of opioids or a sympathomimetic effect? What fancy word is associated with this?
parasympathomimetic effect (vagal effect) -stimulates CN 3 to cause pupil constriction (PSNS nerves = 3, 7, 9, 10) *Edinger Westfall nuleus
30
Why don't we like patients shivering when they wake up?
Because it increases their O2 demand by 400%, making them more susceptible to hypoxia
31
Pruritis following Intraspinal morphine injection is thought to be mediated by the _____ receptor
mu
32
How does fentanyl cause pruritis if it doesn't release histamine? How can it be treated? Will Benadryl be effective? (4 options)
It's a mu receptor response 1. Narcan (but you don't want to reverse the opioid) 2. 10mg Propofol (antipruritic effects) 3. Zofran(?) 4. Droperidol (?) >>inhibition of serotonin receptors peripherally or intraspinal reduces pruritus *BENADRYL WILL NOT WORK- but might make them sleepy enough not to care)
33
How do narcotics affect biliary pressure?
they increase biliary pressure Bc narcotics have a vagal effect on sphincters in your body and tighten them, including the sphincter of odi
34
Why do some patients have a hard time peeing after surgery?
Because narcotics have a vagal effect on the sphincters in the body (they tighten them up- tighten urinary sphincter, makes it hard to relax) (this doesnt make sense, i thought tightened sphincters was a sympathetic response so you dont shit or pee yourself)
35
What's the number one things you can do if a surgeon needs the sphincter of odi relaxed and is blaming your narcotics for it being contracted? What else can you do? (4 total)
1. Atropine or Glyco >anticholinergic >anti-secretions, sphincter of odi contracts to release bile (secretion), to stop the release of bile (secretion) - can give an anticholinergic and it will relax the sphincter and reduce bile secretion. 2. Nitro (can even slip a tab under their tongue while they are asleep) >smooth muscle relaxant 3. Glucagon 4. Narcan (not a great idea)
36
Which opioid would increase biliary pressure the most and why?: Meperidine Morphine Butorphanol Fentanyl
Fentanyl Morphine Meperidine Butorphanol *correlates with potency
37
What should you do if someone develops chest wall rigidity secondary to high-dose narcotics during induction and you can't ventilate them?
Give Sux and intubate them *Don't have to worry about them being awake bc literature shows the chest wall rigidity only happens when they lose consciousness
38
Remember that patient who developed pulmonary edema after receiving high-dose narcotic by EMS? Why did that happen?
Probably had chest wall rigidity, glottic closure resulting in negative pressure pulmonary edema
39
Mechanism by which chest wall rigidity occurs from high dose narcotics
unknown
40
What is the number 1 culprit of PONV?
Opioids! That's why you should still give Zofran and decadron even if not giving inhalationals
41
Where is the chemoreceptor trigger zone located?
In the area postrema of the brainstem (vomiting center)
42
What are N/V signals from the gut mediated by?
The vagus nerve
43
What kind of receptors are located in the chemoreceptor trigger zone that can be targeted for N/V? (6)
1. Serotonin (5HT-3) 2. Histamine 3. Acetylcholine (muscarinic) [scopalamine] 4. Opioid receptors 5. Benzodiazepine 6. Dopamine
44
T/F- anyone who gets a narcotic is at a high risk for NV
True
45
#1 Risk factor for PONV
Hx of PONV
46
How does Dexamethasone reduce PONV? (5) -- mainly?
mainly be reducing serotonin 1. decreases serotonin in the brain by decreasing the precursor for serotonin (tryptophan) 2. reduces serotonin turnover in the brain 3. reduces release of GI serotinin 4. causes central inhibition of the nucleus tractus solitarus (has outflow pathways to the gut via the vagus nerve) 5. inhibits prostaglandins
47
When would you see the effects of hyperglycemia if giving decadron to a diabetic patient?
6-12 hours postop. *either avoid, or reduce dose
48
Should you give a patient on chronic steroids an antiemetic dose of decadron? Would it work? Why or why not?
Yes, because they their chronic dosing is what they are used to and tolerant of. That's where they live. The extra bolus dose we give them will provide the antiemetic effect.
49
What agent blocks cholinergic impulses from the vestibulocochlear apparatus
Scopolamine
50
What opioid may be more beneficial than Fentanyl for quick minor lump and bump mac cases and why?
Alfentanil, slightly shorter kinetics (lasts 20-40 mins instead of 30-60).
51
Concentration of Narcan How should you draw it up
0.4mg/ml (1 ml vial) -draw up 1ml (0.4mg) -dilute in 0.3cc water *now you have 0.4mg/4mls for a 0.1mg/ml concentration -give in 1ml increments -wait a minute to see if they start breathing, if not, give another cc, repeat as needed
52
Anesthetic considerations for your patient on Vivitrol
vivatrol = extended release naltrexone injection -will have to give more narcotics since it's a competitive antagonist
53
What enzyme converts codeine to morphine in the body?
CYP2D6
54
T/F: serotonin syndrome is usually caused by too much of one serotonertgic agent
False - usually the result of multiple serotonergic drugs
55
What are the serotonergic agents? (11) 4 antidepressant types 3 hard drugs 2 opioids + 2 other drug groups
1. MAOi's 2. SSRIs 3. SNRIs 4. TCAs 5. Meperidine 6. Fentanyl 7. Migraine drugs (triptans) 8.Amphetamines 9. Esctasy 10. Cocaine 11. Antiemetics
56
Drug to treat serotonin syndrome How does it work?
Cyproheptadine (H1 receptor antagonist- antihistamine with anti serotonin and anticholinergic properties)
57
Triad of Serotonin Syndrome
1. NM effects (rigidity) 2. Autonomic effects (cardiac changes, diarrhea, diaphoresis) 3. Mental changes
58
T/F - heroin is the most addictive bc of it's potent analgesic effects
False - bc it's produces the greatest euphoria effects (only 2x stronger than morphine)
59
How do opioid deterrent drugs work ie) Dilaudid pill combined with Narcan
Dilaudid is lipid soluble and gets absorbed into systemic circulation by the GI tract Narcan is water soluble so it does not get absorbed into systemic circulation so it exerts no effects by this route of administration but if you were to try and crush it and snort it or dilute it and inject it, the Narcan would exert it's effects
60
Difference between naltrexone, methadone, and buprenorphine
Naltrexone- blocks brain's opioid receptors Methadone (synthetic) & Buprenorphine (semi-synthetic) are opioid agonists themselves (and prevent opioid withdrawal symptoms & Prevent drug cravings) Methadone must be dispensed in clinics Buprenorphine- can only be prescribed by authorized doctors due to the high risk of getting on the black market and using them to get high

*Pharmacology (25 decks)

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