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Flashcards in Narcotics!!!!!! Deck (73):
1

which receptors do narcotics work on?

mu

2

what type of pain are narctoics used for?

severe or chronic malignant pain

3

what are the three types of opioids?

1) full agonist
2) Partial Agonist
3) mixed agonist/antagonist

4

MOA of narcotics

bind to opiate receptors in brain and spinal column and inhibit ascending paths

5

what two ways to opiate receptors relieve pain? (two ways)

1) increased activation of neurons that inhibit pain transmission
2) increase of endogenous opiods

6

FULL AGONISTS

- bind to mu, produce endorphins - pain relief, euphoria
-the larger the dose the larger the effect

7

is there a celling for analgesic effects of full agonists?

no

8

What type of pain do you use a full agonist for?

moderate to severe acute or chronic pain

9

Morphine

-prototype
-extensive first pass
-caution in renal insuficiency pts. bc toxic metabolite

10

Oxycondone

-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

Roxanol

concentrated morphine liquid

12

MSIR

imediate release morphine

13

MSContin

extended release morphine

14

Oxymorphone

-metabolite of oxycodone
-IV and PO
-3x more potent than morphine

15

Hydromorphone

-IV. Rectal, PO
-semi-synthetic
-safer choice for renal compromised
-once daily

16

Fentanyl

-IV, intrathecal, epidural, transdermal, intranasal and oral transmucosal formulations
-100 times more powerful than MSO4

17

Fentanyl starting tritration

initial titration with a short-acting opioid until they reach steady state ~72 hrs

18

heating pad and fentanyl

increased exertion, or high fever could increase release of drug and risk for respiratory depression

19

Methadone

-LONG 1/2 life
-Dose-related QT prolongation, torsades & death have been reported
-1st line in CA

20

1st line treatment of CA includes ___

-methadone

21

frequency of dosing for methadone is...

-every 8 hrs for pain
-once/day for addiciton

22

Meperidine

-only use for less than 48 hours
-30 hour 1/2 life

23

What adverse effects are cause by meperidine?

dysphoria, irritability, tremors, seizure, antimuscaneric effect

24

scary thing about meperidine...

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