Week 5: Amnesics and Hypnotics Flashcards
What are the 5 important Opioid Analgesics and Sedative (Sleep) Hypnotic Prototype Drugs
morphine sulfate
naloxone (Narcan)
nalbuphine (Nubain)
codeine
zolpidem (Ambien)
Narcotics means __
opioids
What is the prototype for the Narcotic class
Morphine
What schedule is morphine
schedule II
___ is the standard by which new analgesics are measured
morphine (it either is weaker or stronger than morphine)
What are the main 3 opioid receptors
Mu (major one)
Delta
Kappa
Opioids are what
naturally occurring substance
What is the main action of morphine (and narcotics)
central action on PAIN PERCEPTION (we want to decrease it)
So it impacts the sensory cortex
Other than act on pain perception what other effects do narcotics like morphine have
Alter attitudes by psychological, sedative, and hypnotic effects
Morphine is a narcotic ____
agonist
What does it mean that morphine is an opioid/narcotic agonist
It interacts with receptors in BRAIN AND OTHER TISSUES - it causes opioid effects to happen
What sort of CNS effects does morphine and opioids/narcotics cause
Analgesia, Drowsiness, Changes in Mood, Mental Clouding - the main reasons we use it
- CONSTRICTED PUPILS
- DECREASES CO2 RESPONSE - BREATHING DECREASE / RESP
- STIMULATES NV - may need to give anti emetic
What other systems and effects can opioids and narcotics and morphine cause besides CNS
- CV - Doesnt impact heart rate but provokes histamine release and can cause hypotension — It dilates resistance vessels and can cause DIZZINESS AND ORTHOSTATIC HYPOTENSION
- GI - decreases motility and biliary tract ==> CONSTIPATION OCCURS
- Smooth Muscle - Increases bladder and sphincter tone leading to URGENCY AND RETENTION; and LARGE DOSES CAUSE BRONCHOCONSTRICTION
- Skin - Dilation leads to FLUSHING, WARM SKIN, AND SOMETIMES ITCHING (histamines)
Why is morphine never given orally usually
morphine has HIGH FIRST PASS when given PO - so we give it IV/Injection usually
ADRs from Morphine (Opioids/Narcotics)
Allergic Rxns
ABUSE POTENTIAL
Orthostatic Hypotension, Itchiness, Warm Skin, Dizziness, Flushing, Constipation, Urinary Retention, Constricted Pupils, NV, Depressed Breahting
Examples of other Narcotics/Opioids
- meperidine (Demerol) - less GI effects but doesnt last as long - additive effects - synthetic opioid - rigors - normoparadeine metabolite causes seizures
- Percocet (Oxycodone and Acetaminophen) & Percodan (Oxycodone and ASA)
- Vicodin and Norco
- Dilaudid (v. potent)
- Fentanyl
naloxone (Narcan)
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
Why is naloxone givne nasally or by IV
because it has a very extensive first pass
naloxone is a pure antagonist, what does that mean
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
If one is addicted to an opioid like morphine and takes naloxone what is an ADR that can occur
if they are addicted the naloxone will cause withdrawl symptoms
What is an example of a narcotic agonist antagonist
Nalbuphine (Nubain)
What does narcotic agonist antagonist mean
it causes a more mild/medium effect as compared to just a narcotic agonist
What route is nalbuphine (Nubain) given
IM, SubQ, or IV
hen might Nalbuphine be given
Sometimes for labor or in cases where they need less powerful opioid effects than a full opioid
ADRs of Nalbuphine (Nubain)
sedation sweatiness clamminess NV dizziness vertigo dry mouth HA respiratory depression
Nalbuphine can be reversed by ___
naloxone
What is a big benefit of choosing Nalbuphine over Morphine sulfate
Nalbuphine has a much lower abuse potential and less severe ARs
What is a prime example of a narcotic analgesic
Codeine
While it is a narcotic analgesic, what other effect does codeine have and is given for
antitussive properties (Coughing)
What is the action of Codeine
it produces a mild to moderate pain relief on its own, but it METABOLIZES INTO MORPHINE to cause relief and also its antitussive properties
Codeine metabolizes into ___
morphine
Why is codeines metabolism so important to recognize
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
hat groups is codeine not recommended in and why?
pediatrics and elderly
this is because it metabolizes into morphine which has depressive CNS effects on breathing for the two groups
What route is codeine usually given in
oral
ADRs of codeine
respiratory depression constipation urinary retention miosis pupilarry constriction constipation
(all similar to morphine but less!!!)
When is comes to tolerance for opioids, what do people never become tolerant/ immune to
pinpoint pupils
resulting constipation
\What is the problem with codeines dosing
needs higher dosing to achieve pain relief but the side effects rise with dosing as it converts to morphine
200 mg PO of codeine converts to ___ mg of morphine
30 mg
Hypnotics (Sedatives)
drugs that help you go to sleep
What is one of the most common hypnotic/sedatives among all ages
diphenhydramine (Benadryl) - it cna be used as an antihistamine but a major ADR is sedation and it is OTC
Benzodiazepines
class of drugs that work as a depressant/sedative
structurally similar to valium
What is the prototype drug for hypnotics that are non BZD (Benzodiazepine)
zolpidem (Ambien)
What is a good sign that a drug is a type of hypnotic
it has a z in the name
ex: zolpidem
zolpidem (Ambien)
New drug that binds to benzo receptors in the brain without being a benzo and causes sedation/hypnotic effects
What is important to know about the absorption and distribution of zolpidem (Ambien)
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
ADRs of zolpidem
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
What is important to know about the dosage and when to take zolpidem (Ambien)
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
zolpidem (Ambien) acts like a ___ but is structurally different
benzodiazepine
What hapened to the OTC dosges of Ambien in 2013
they were cut in half to lessen teh ADRs
zolpidem (Ambien) is used for what sort of treatment timeline
short term treatment not long term use
Ambien CR
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)
zaleplon (Sonata) and eszoplicone (Lunesta) are examples of what
Hypnotics (non-benzo)
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
C. Respiratory System
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
Answer: C. Could lead to accumulation of secretions
- Cannot clear airway due to resp depression and antitussive properties
