Flashcards in Narcotics!!!!!! Deck (73):
which receptors do narcotics work on?
what type of pain are narctoics used for?
severe or chronic malignant pain
what are the three types of opioids?
1) full agonist
2) Partial Agonist
3) mixed agonist/antagonist
MOA of narcotics
bind to opiate receptors in brain and spinal column and inhibit ascending paths
what two ways to opiate receptors relieve pain? (two ways)
1) increased activation of neurons that inhibit pain transmission
2) increase of endogenous opiods
- bind to mu, produce endorphins - pain relief, euphoria
-the larger the dose the larger the effect
is there a celling for analgesic effects of full agonists?
What type of pain do you use a full agonist for?
moderate to severe acute or chronic pain
-extensive first pass
-caution in renal insuficiency pts. bc toxic metabolite
-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
concentrated morphine liquid
imediate release morphine
extended release morphine
-metabolite of oxycodone
-IV and PO
-3x more potent than morphine
-IV. Rectal, PO
-safer choice for renal compromised
-IV, intrathecal, epidural, transdermal, intranasal and oral transmucosal formulations
-100 times more powerful than MSO4
Fentanyl starting tritration
initial titration with a short-acting opioid until they reach steady state ~72 hrs
heating pad and fentanyl
increased exertion, or high fever could increase release of drug and risk for respiratory depression
-LONG 1/2 life
-Dose-related QT prolongation, torsades & death have been reported
-1st line in CA
1st line treatment of CA includes ___
frequency of dosing for methadone is...
-every 8 hrs for pain
-once/day for addiciton
-only use for less than 48 hours
-30 hour 1/2 life
What adverse effects are cause by meperidine?
dysphoria, irritability, tremors, seizure, antimuscaneric effect
scary thing about meperidine...
If recent use of MAOI, meperidine can cause severe encephalopathy and death
What is Codeine converted to?
What is the issue with codeine and rapid metabolizers?
rapidly metabilize codine to morphine which produces a higher level of toxins
When is codeine contraindicated?
it is contraindicated in children undergoing tonsilectomy and/or adenoidectomy
Is hydrocodone a synthetic or natural opiod?
what is hydrocodone metabolized into?
what is hydrocodone often combined with?
acetaminophen or ibuprofen
hydrocodone + 300 mg acetominiphen
hydrocodone and 326 acetominophin
Is Tapentadol a full agonist , partial agonist, or combination?
Full agonist and a NE reuptake inhibitor
Absolute contraindication of Tapentadol is what?
DO NOT USE WITH AN MAOI. Wait 14 days
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
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
When is tramadol contraindicated?
- Hx of seizure, on another med that causes seizures
-increased risk of suicide
What is the MOA of partial agonists?
bind primarily to mu opioid receptors and cause them to produce endorphins
Name 3 partial agonists
Buprenorphine & naloxone (Suboxone)
Buprenorphine ER (Subutex
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
Mixed agonist/ antagonist list
- stimulate and antagonize the narcotic receptor
Butorphanol (Stadol)- only one used
What is morphine and hydromorphine metabolized to?
what can M3G cause?
it is a neurotoxin and can cause seizures
-produces ADRs in patients with Renal failure
What does Meperidine become? wha can it cause?
- It is toxic and cause seizures in patients with renal failure , elderly or on a high dose for a long time
what are the 3 main effects of Narcotic Receptor stimulation?
What narcotic is often used for cough supression?
caused by narcotic
constriction of puols
Nausea and Vomiting
caused by narcotics
List the peripheral effects of narcotics
GI & biliary tract
If a pt. has CVS dz or is hypovolemic what may narcotics cause?
-they will casue blood vessel dilatation and hypotension
What narcotic has anticholinergic effects and what can it cause?
Meperidine can cuase tachycardia
GI effects of Narcotics
-constipation that does not diminish with continued use
-Nillary contraction- pain if gallstones
what are two ways to alive narcotic pt. constipation?
docyate sodium- stool softener
-novanta- specific for pain med pts.
GU side effects
Uterine side effects of narcotics are..
decrease uterine contraction-> prolong labor
Why do narcotics cause pruritis and what can you take as profylaxis?
- profylaxis: diphenhydramine
When does tolerance to narcotics start?
- 2-3 weeks
- the only thing that doesnt decrease with tolerance is miosis, constipation and seizures
change drugs, you change receptor types and therefore get greater affect from the new receptors, receptor upregulation and down regulation
Symptoms of withdrawl
nausea, vomiting, lacrimation, rhinorrhea, mydriasis, piloerection, sweating, diarrhea) & CNS arousal (irritability & dysphoria
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
what happens when benzos/sleeping aids are combined with narcotics?
increased CNS depression
what happens when antipsychotics are combined with narcotics?
what happens when MAOIs are combined with narcotics?
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)
Narcotics and Pulmonary Edema
IV morphine decreases SOB by decreasing anxiety, preload and afterload
no euphoric effect but supresses cough
used for diarrhea
Use of narcotics in anesthesia
-sedate and decrease pain and axiety before enter OR-used more in cardiovascular surgery
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
Used in maintenance programs and can block heroin effects for up to 48 hours
oral, long 1/2 life, lasts for 48 hours
-also given to addicts every other day to prevent ppl in recovery from getting hgih