Week 5: Amnesics and Hypnotics Flashcards

1
Q

What are the 5 important Opioid Analgesics and Sedative (Sleep) Hypnotic Prototype Drugs

A

morphine sulfate

naloxone (Narcan)

nalbuphine (Nubain)

codeine

zolpidem (Ambien)

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2
Q

Narcotics means __

A

opioids

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3
Q

What is the prototype for the Narcotic class

A

Morphine

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4
Q

What schedule is morphine

A

schedule II

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5
Q

___ is the standard by which new analgesics are measured

A

morphine (it either is weaker or stronger than morphine)

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6
Q

What are the main 3 opioid receptors

A

Mu (major one)

Delta

Kappa

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7
Q

Opioids are what

A

naturally occurring substance

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8
Q

What is the main action of morphine (and narcotics)

A

central action on PAIN PERCEPTION (we want to decrease it)

So it impacts the sensory cortex

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9
Q

Other than act on pain perception what other effects do narcotics like morphine have

A

Alter attitudes by psychological, sedative, and hypnotic effects

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10
Q

Morphine is a narcotic ____

A

agonist

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11
Q

What does it mean that morphine is an opioid/narcotic agonist

A

It interacts with receptors in BRAIN AND OTHER TISSUES - it causes opioid effects to happen

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12
Q

What sort of CNS effects does morphine and opioids/narcotics cause

A

Analgesia, Drowsiness, Changes in Mood, Mental Clouding - the main reasons we use it

  1. CONSTRICTED PUPILS
  2. DECREASES CO2 RESPONSE - BREATHING DECREASE / RESP
  3. STIMULATES NV - may need to give anti emetic
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13
Q

What other systems and effects can opioids and narcotics and morphine cause besides CNS

A
  1. CV - Doesnt impact heart rate but provokes histamine release and can cause hypotension — It dilates resistance vessels and can cause DIZZINESS AND ORTHOSTATIC HYPOTENSION
  2. GI - decreases motility and biliary tract ==> CONSTIPATION OCCURS
  3. Smooth Muscle - Increases bladder and sphincter tone leading to URGENCY AND RETENTION; and LARGE DOSES CAUSE BRONCHOCONSTRICTION
  4. Skin - Dilation leads to FLUSHING, WARM SKIN, AND SOMETIMES ITCHING (histamines)
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14
Q

Why is morphine never given orally usually

A

morphine has HIGH FIRST PASS when given PO - so we give it IV/Injection usually

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15
Q

ADRs from Morphine (Opioids/Narcotics)

A

Allergic Rxns

ABUSE POTENTIAL

Orthostatic Hypotension, Itchiness, Warm Skin, Dizziness, Flushing, Constipation, Urinary Retention, Constricted Pupils, NV, Depressed Breahting

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16
Q

Examples of other Narcotics/Opioids

A
  1. meperidine (Demerol) - less GI effects but doesnt last as long - additive effects - synthetic opioid - rigors - normoparadeine metabolite causes seizures
  2. Percocet (Oxycodone and Acetaminophen) & Percodan (Oxycodone and ASA)
  3. Vicodin and Norco
  4. Dilaudid (v. potent)
  5. Fentanyl
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17
Q

naloxone (Narcan)

A

Narcotic Antagonist - blocks and prevents action of opioids and narcotics

gigiven IV or nasally

used to reverse narcotic effects of anesthesia or in case of overdose

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18
Q

Why is naloxone givne nasally or by IV

A

because it has a very extensive first pass

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19
Q

naloxone is a pure antagonist, what does that mean

A

it has no agonist or respiratory depressant effects

it only blocks the opioid receptor and wont cause harm from taking aside from preventing opioids from working

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20
Q

If one is addicted to an opioid like morphine and takes naloxone what is an ADR that can occur

A

if they are addicted the naloxone will cause withdrawl symptoms

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21
Q

What is an example of a narcotic agonist antagonist

A

Nalbuphine (Nubain)

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22
Q

What does narcotic agonist antagonist mean

A

it causes a more mild/medium effect as compared to just a narcotic agonist

23
Q

What route is nalbuphine (Nubain) given

A

IM, SubQ, or IV

24
Q

hen might Nalbuphine be given

A

Sometimes for labor or in cases where they need less powerful opioid effects than a full opioid

25
Q

ADRs of Nalbuphine (Nubain)

A

sedation
sweatiness
clamminess
NV
dizziness
vertigo
dry mouth
HA
respiratory depression

26
Q

Nalbuphine can be reversed by ___

A

naloxone

27
Q

What is a big benefit of choosing Nalbuphine over Morphine sulfate

A

Nalbuphine has a much lower abuse potential and less severe ARs

28
Q

What is a prime example of a narcotic analgesic

A

Codeine

29
Q

While it is a narcotic analgesic, what other effect does codeine have and is given for

A

antitussive properties (Coughing)

30
Q

What is the action of Codeine

A

it produces a mild to moderate pain relief on its own, but it METABOLIZES INTO MORPHINE to cause relief and also its antitussive properties

31
Q

Codeine metabolizes into ___

A

morphine

32
Q

Why is codeines metabolism so important to recognize

A

since it metabolizes into morphine this means codeine effects will get stronger, and with some people being ultra fast convertors in terms of metabolism this means morphine levels can rise rapidly

33
Q

hat groups is codeine not recommended in and why?

A

pediatrics and elderly

this is because it metabolizes into morphine which has depressive CNS effects on breathing for the two groups

34
Q

What route is codeine usually given in

A

oral

35
Q

ADRs of codeine

A

respiratory depression
constipation
urinary retention
miosis
pupilarry constriction
constipation

(all similar to morphine but less!!!)

36
Q

When is comes to tolerance for opioids, what do people never become tolerant/ immune to

A

pinpoint pupils

resulting constipation

37
Q

\What is the problem with codeines dosing

A

needs higher dosing to achieve pain relief but the side effects rise with dosing as it converts to morphine

38
Q

200 mg PO of codeine converts to ___ mg of morphine

A

30 mg

39
Q

Hypnotics (Sedatives)

A

drugs that help you go to sleep

40
Q

What is one of the most common hypnotic/sedatives among all ages

A

diphenhydramine (Benadryl) - it cna be used as an antihistamine but a major ADR is sedation and it is OTC

41
Q

Benzodiazepines

A

class of drugs that work as a depressant/sedative

structurally similar to valium

42
Q

What is the prototype drug for hypnotics that are non BZD (Benzodiazepine)

A

zolpidem (Ambien)

43
Q

What is a good sign that a drug is a type of hypnotic

A

it has a z in the name

ex: zolpidem

44
Q

zolpidem (Ambien)

A

New drug that binds to benzo receptors in the brain without being a benzo and causes sedation/hypnotic effects

45
Q

What is important to know about the absorption and distribution of zolpidem (Ambien)

A

Absorption - it is rapidly absorbed in the GI tract

Distribution - it has a VERY QUICK PEAK - 1 hour or sooner - but half life can be prolonged in elderly and in liver dysfunction

46
Q

ADRs of zolpidem

A

dizziness

HA

NV

diarrhea

next day drowsiness (only 1-2% but thats still not a lot of people getting up for work at 9 am)

sleep driving and other sleep related behaviors !!!! - sleep walking, sleep eating, other strange things in the middle of the night

47
Q

What is important to know about the dosage and when to take zolpidem (Ambien)

A

you want to take it RIGHT BEFORE BED since it has a RAPID ONSET - do not take it sooner but literally right before even though the effects peak in 1-2 hours the effects come very fast

48
Q

zolpidem (Ambien) acts like a ___ but is structurally different

A

benzodiazepine

49
Q

What hapened to the OTC dosges of Ambien in 2013

A

they were cut in half to lessen teh ADRs

50
Q

zolpidem (Ambien) is used for what sort of treatment timeline

A

short term treatment not long term use

51
Q

Ambien CR

A

form of zolpidem with continuous release that spreads the effects throughout the night so you are not waking up constantly since the peaks are soon (1-2 hours)

52
Q

zaleplon (Sonata) and eszoplicone (Lunesta) are examples of what

A

Hypnotics (non-benzo)

53
Q

The most hazardous adverse effects with the use of morphine occur to the:

A. Integumentary System
B: Cardiovascular System
C. Respiratory System
D. Gastrointestinal System

A

C. Respiratory System

54
Q

Although sometimes used as a cough supressant, Codeine may be a poor choice for someone with a respiratory disorder because it:

A. Causes Bronchoconstriction

B. Causes Bronchodilation

C. Could lead to accumulation of secretions

D. Can lead to drug dependence

A

Answer: C. Could lead to accumulation of secretions

  • Cannot clear airway due to resp depression and antitussive properties