Narcotics!!!!!! Flashcards
1
Q
which receptors do narcotics work on?
A
mu
2
Q
what type of pain are narctoics used for?
A
severe or chronic malignant pain
3
Q
what are the three types of opioids?
A
1) full agonist
2) Partial Agonist
3) mixed agonist/antagonist
4
Q
MOA of narcotics
A
bind to opiate receptors in brain and spinal column and inhibit ascending paths
5
Q
what two ways to opiate receptors relieve pain? (two ways)
A
1) increased activation of neurons that inhibit pain transmission
2) increase of endogenous opiods
6
Q
FULL AGONISTS
A
- bind to mu, produce endorphins - pain relief, euphoria
- the larger the dose the larger the effect
7
Q
is there a celling for analgesic effects of full agonists?
A
no
8
Q
What type of pain do you use a full agonist for?
A
moderate to severe acute or chronic pain
9
Q
Morphine
A
- prototype
- extensive first pass
- caution in renal insuficiency pts. bc toxic metabolite
10
Q
Oxycondone
A
- oral only
- Semi-synthetic derivative of MSO4- morphine
- 9.5 times more potent than oral codeine
- 1.5 times more potent than morphine
- extended release available
- tamper deterent available
11
Q
Roxanol
A
concentrated morphine liquid
12
Q
MSIR
A
imediate release morphine
13
Q
MSContin
A
extended release morphine
14
Q
Oxymorphone
A
- metabolite of oxycodone
- IV and PO
- 3x more potent than morphine
15
Q
Hydromorphone
A
- IV. Rectal, PO
- semi-synthetic
- safer choice for renal compromised
- once daily
16
Q
Fentanyl
A
- IV, intrathecal, epidural, transdermal, intranasal and oral transmucosal formulations
- 100 times more powerful than MSO4
17
Q
Fentanyl starting tritration
A
initial titration with a short-acting opioid until they reach steady state ~72 hrs
18
Q
heating pad and fentanyl
A
increased exertion, or high fever could increase release of drug and risk for respiratory depression
19
Q
Methadone
A
- LONG 1/2 life
- Dose-related QT prolongation, torsades & death have been reported
- 1st line in CA
20
Q
1st line treatment of CA includes ___
A
-methadone
21
Q
frequency of dosing for methadone is…
A
- every 8 hrs for pain
- once/day for addiciton
22
Q
Meperidine
A
- only use for less than 48 hours
- 30 hour 1/2 life
23
Q
What adverse effects are cause by meperidine?
A
dysphoria, irritability, tremors, seizure, antimuscaneric effect
24
Q
scary thing about meperidine…
A
If recent use of MAOI, meperidine can cause severe encephalopathy and death
25
What is Codeine converted to?
morphine
26
What is the issue with codeine and rapid metabolizers?
rapidly metabilize codine to morphine which produces a higher level of toxins
27
When is codeine contraindicated?
it is contraindicated in children undergoing tonsilectomy and/or adenoidectomy
28
Is hydrocodone a synthetic or natural opiod?
synthetic
29
what is hydrocodone metabolized into?
hydromorphine
30
what is hydrocodone often combined with?
acetaminophen or ibuprofen
31
zohydro
pure hydrocodone
32
vicodin
hydrocodone + 300 mg acetominiphen
33
Norco
hydrocodone and 326 acetominophin
34
Is Tapentadol a full agonist , partial agonist, or combination?
Full agonist and a NE reuptake inhibitor
35
Absolute contraindication of Tapentadol is what?
DO NOT USE WITH AN MAOI. Wait 14 days
36
Tramadol what type of narcotic and what is the MAOI?
- centrally-acting agonist
-blocks reuptake of norepinephrine and serotonin
binds to a narcotic receptor too but weakly
37
What are the adverse reactions of tramadol?
- lowers seizures threshold
- TCAs SSRI, MAOI, and other opiods and antipsychotics can increase lowered seizure threshold
- nausea and dizziness
38
When is tramadol contraindicated?
- Hx of seizure, on another med that causes seizures
| - increased risk of suicide
39
What is the MOA of partial agonists?
bind primarily to mu opioid receptors and cause them to produce endorphins
40
Name 3 partial agonists
Buprenorphine (Butrans)
Buprenorphine & naloxone (Suboxone)
Buprenorphine ER (Subutex
41
What happens as the dosage of partial agonists increases?
-When the dosage of a partial agonist is increased, there is only a small increase, if any, in the production of endorphins
42
Mixed agonist/ antagonist list
- stimulate and antagonize the narcotic receptor
- analgesic effect
Butorphanol (Stadol)- only one used
43
What is morphine and hydromorphine metabolized to?
M3G
44
what can M3G cause?
it is a neurotoxin and can cause seizures
| -produces ADRs in patients with Renal failure
45
What does Meperidine become? wha can it cause?
Normerperidine
| - It is toxic and cause seizures in patients with renal failure , elderly or on a high dose for a long time
46
what are the 3 main effects of Narcotic Receptor stimulation?
- Euphoria
- Sedation
- Respiratory depression
47
What narcotic is often used for cough supression?
codeine
48
Miosis
caused by narcotic
| constriction of puols
49
Nausea and Vomiting
caused by narcotics
50
List the peripheral effects of narcotics
```
CVS
GI & biliary tract
GU
Uterus
Pruritus
Miscellaneous
```
51
If a pt. has CVS dz or is hypovolemic what may narcotics cause?
-they will casue blood vessel dilatation and hypotension
52
What narcotic has anticholinergic effects and what can it cause?
Meperidine can cuase tachycardia
53
GI effects of Narcotics
- constipation that does not diminish with continued use
| - Nillary contraction- pain if gallstones
54
what are two ways to alive narcotic pt. constipation?
docyate sodium- stool softener
| -novanta- specific for pain med pts.
55
GU side effects
urinary retention
56
Uterine side effects of narcotics are..
decrease uterine contraction-> prolong labor
57
Why do narcotics cause pruritis and what can you take as profylaxis?
- histamine release
| - profylaxis: diphenhydramine
58
When does tolerance to narcotics start?
- 2-3 weeks
| - the only thing that doesnt decrease with tolerance is miosis, constipation and seizures
59
Opioid rotation
change drugs, you change receptor types and therefore get greater affect from the new receptors, receptor upregulation and down regulation
60
Symptoms of withdrawl
nausea, vomiting, lacrimation, rhinorrhea, mydriasis, piloerection, sweating, diarrhea) & CNS arousal (irritability & dysphoria
61
contraindication to narcotics
1) Head injury- bc increase blood flow to head
2) pregnancy- fdetus becomes dependent
3) impaired respiratory fcn
4) impaired renal fxn
62
what happens when benzos/sleeping aids are combined with narcotics?
increased CNS depression
63
what happens when antipsychotics are combined with narcotics?
increased sedation
64
what happens when MAOIs are combined with narcotics?
HTN
65
Use of narcotics for analgesia
Using narcotics at fixed intervals (scheduled) is more effective for pain relief than on demand use (using just when pain is really bad)
66
Narcotics and Pulmonary Edema
IV morphine decreases SOB by decreasing anxiety, preload and afterload
67
Dextromethorphan
no euphoric effect but supresses cough
68
diphenoxylate
used for diarrhea
69
Use of narcotics in anesthesia
-sedate and decrease pain and axiety before enter OR-used more in cardiovascular surgery
70
Naloxone (Narcan)
Bind to but do not stimulate the narcotic receptor and end up blocking effects of other agonists
-short 1/2 life, reinject every 2 hours
71
Naltrexone (ReVia)
| Nalmefene (Revex)
Used in maintenance programs and can block heroin effects for up to 48 hours
72
Naltrexone (ReVia)
oral, long 1/2 life, lasts for 48 hours
-also given to addicts every other day to prevent ppl in recovery from getting hgih
73
Nalmefene (Revex)
newest long 1/2 life, injectable
