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63 Cards in this Set

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Name 3 Endogenous opioid peptides
1. Beta-endorphin
2. Dynorphins
3. Enkephalins
Name the 3 opioid receptors that have been cloned
1. Sigma
2. Kappa
3. Mu *** does 99% of work, most of the opioids bind this
Which receptor does Beta-endorphin, morphine bind to?
Mu (OP-3)
Which receptor does Dynorphin-A bind to?
Kappa
Which receptor does Enkephalins bind to?
Sigma
Name Mu agonists and antagonists
Agonists:
Beta-endorphin
Morphine

Antagonist:
1. Naloxone
Name Kappa agonists and antagonists
Agonist:
1. Dynorphine
2. Pentazocine
Antagonist:
1. Naloxone (need a lot)
Name Delta agonists and antagonists
Agonist:
1. Enkephalins
Antagonist:
1. Naloxone (need a lot)
What are the effects of opioids bound on mu receptors
GI effects; NAUSEA, vomit, constipation, sedation, RESPIRATORY DEPRESSION, MIOSIS - MAY INDICATE MISUSE
What are the effects of opioids bound on Kappa receptors
Kappa receptors involved in visceral pain. Also note that kappa agonists cross BBB hence - DYSPHORIA, DIURESIS - Kappa recept on kindet, hallucinations
What are the effects of opioids bound on delta receptors
Spinal and supra spinal analgesia
Effects of opioids and their metabolites
Convulsions (Demerol)
Respiratory depression
EMETIC EFFECT (40 -50%)
anti-emetic
Antitussive (cough syrup - codeine)
GI effects: Constipation, Decreased motility of entire GI system
This drug has a neurotoxic metabolite secreted by kindeys and accumulates more in kindey failure.
Drug: Demerol
Metabolite - normeperidine. Causes Sz and convulsions ****
This is the most feared side effect of opioids and is rarely seen.
RESPIRATORY DEPRESSION
Primary stimulus for breathing is carbon dioxide, opioids desensitize chemoreceptor to CO2
What is the antidote to respiratory depression seen with opioids
PAIN!!!
How do you know that a patient is going into respiratory depression?
Patient becomes obtunded as a result of CO2 narcosis due to rise in CO2. Are difficult patients to arouse.
What part of our brain anatomy explains why most drugs cause nausea?
The thinnest part of the Blood Brain Barrier is over the chemoreceptor trigger zone (Vomit center), a protective reaction when exposed to noxious stimuli.
True or False:
Opioids works on both limbs of the autonomic system - sympathetic and parasympathetic effects.
TRUE, these effects are independent of each other. The vagolytic effects are via Central Vagal nucleus.
What are the most common side effects of long term opioid receptors?
***KNOW THIS***
CONSTIPATION
No desensitization of mu opioid receptors is gut.
Opioids reverse the order of muscle action, more circular and less longitudinal muscle movement. BOWEL REGIMENTS ARE IMPORTANT!
DEFINE
Opioid Dependence
Get used to the drug and without it you have withdrawal systems. One's system gets used to drug and need to have it.
DEFINE
Tolerance
Over time, may need more of drug for effects,but also have tolerance to side effects.
True of False:
Addiction to drugs is inherent
TRUE,
CHAR. BY 5C'S
CHRONICITY
CRAVING
CONTINUED USE DESPITE HARM
COMPULSIVE USE
CONTROL - IMPAIRED
What's the right dose of an opioid?
*** KNOW THIS ***
No prescribed dose, you titrate to effect. HAVE NO CEILING EFFECT.
Effects of opioids and their metabolites
Convulsions (Demerol)
Respiratory depression
EMETIC EFFECT (40 -50%)
anti-emetic
Antitussive (cough syrup - codeine)
GI effects: Constipation, Decreased motility of entire GI system
This drug has a neurotoxic metabolite secreted by kindeys and accumulates more in kindey failure.
Drug: Demerol
Metabolite - normeperidine. Causes Sz and convulsions ****
This is the most feared side effect of opioids and is rarely seen.
RESPIRATORY DEPRESSION
Primary stimulus for breathing is carbon dioxide, opioids desensitize chemoreceptor to CO2
What is the antidote to respiratory depression seen with opioids
PAIN!!!
How do you know that a patient is going into respiratory depression?
Patient becomes obtunded as a result of CO2 narcosis due to rise in CO2. Are difficult patients to arouse.
What part of our brain anatomy explains why most drugs cause nausea?
The thinnest part of the Blood Brain Barrier is over the chemoreceptor trigger zone (Vomit center), a protective reaction when exposed to noxious stimuli.
True or False:
Opioids works on both limbs of the autonomic system - sympathetic and parasympathetic effects.
TRUE, these effects are independent of each other. The vagolytic effects are via Central Vagal nucleus.
What are the most common side effects of long term opioid receptors?
***KNOW THIS***
CONSTIPATION
No desensitization of mu opioid receptors is gut.
Opioids reverse the order of muscle action, more circular and less longitudinal muscle movement. BOWEL REGIMENTS ARE IMPORTANT!
DEFINE
Opioid Dependence
Get used to the drug and without it you have withdrawal systems. One's system gets used to drug and need to have it.
DEFINE
Tolerance
Over time, may need more of drug for effects,but also have tolerance to side effects.
True of False:
Addiction to drugs is inherent
TRUE,
CHAR. BY 5C'S
CHRONICITY
CRAVING
CONTINUED USE DESPITE HARM
COMPULSIVE USE
CONTROL - IMPAIRED
What's the right dose of an opioid?
*** KNOW THIS ***
No prescribed dose, you titrate to effect. HAVE NO CEILING EFFECT.
How does PCA [Patient Controlled Anesthesia] work in administration of opioids?
Anytime dosing with PCA, give bolus loading dose and then maintenance doses given at intervals after that to maintain comfort.
List three opioid metabolites that could accumulate and cause side effects.
Normeperidine
Morphine-3-glucuronide (Inactive)
Morphine-6-glucuronide (Active)
Which opioid metabolite is now a separate opioid metabolite in Europe?
Morphine-6-glucuronide
List three naturally occuring opioids
Paregoric
Morphine
Codeine
Heroin is metabolized to?
Morphine
List 5 semi-synthetic opioids
(Substitutions of naturally occuring compounds)
Heroin
Apomorphine
Oxycodone ***
Hydromorphone ***
Oxymorphone
List 6 synthetic opioid drugs (little resemblance to parent compounds)
Meperidine *** (Fav.in abuse)
Fentanyl, sufentanyl *** (Ultrapotent with no active metabolites)
Diphenoxylate - Stop diarrhea
Loperamide - Stop diarrhea
Methadone
Propoxyphene
History of methadone (Dolafone - named after Adolf Hitler)
Manufucture in Germany during world war II. Did not grow opium. Manufactured this drug.
Has an active Dextro-isomer; binds NMDA receptor.
Name three opioid Agonist-Antagonist drugs:
Butophanol
Pentazocine
Nabulphine
What is the MOA of opiod Agonist-Antagonist drugs?
In the presence of other opiod drugs, these drugs act as Mu antagonists and kappa agonists. On their own, the are Mu agonists but have very mild analgesic action.
Drug used in office based treatment of opioid addiction?
Buprenorphine
What is the MOA of Buprenorphine?
A partial agonist with high binding affinity. Binds preferentially than any other drugs being abused, butonly produces a partial effect downstream of binding. No full stimulation G-protein coupled response.
Rapid replacement of drug of abuse without withdrawal due to some effect.
Name one opioid with a ceiling effect.
Buprenorphine
What makes Peripheral Acting Mu-Opioid Receptor antagonists (PAMOR) usefull?
Are selective antagonists, work peripherally eg. gut. Can be used to reduce Constipation, nausea and bowel dysfunction
List 2 PAMOR opiods
Alvimopan
Methylnaltrexone
What is the MOA of Tramadol?
Weak Mu-opioid agonist
Inhibit reuptake of NE and serotonin
Activate alpha adrenegic receptors
What are the indications of tramadol?
Chronic pain
Side effects of tramadol and how are these reduced?
Sedation, Confusion at first.
Start low and go slow.
Name 2 pure opioid receptor antagonists
Naloxene (IV - short acting)
Naltrexone (Oral, long acting)
Do opioids have a ceiling effect?
NO NO NO, Except Buprenophine
What should be considered when changing opioids in patients already on opioids?
Don't give drug concentration on equianalgesic tables. Start at half the dose and titrate up.
Explain incomplete cross-tolerance in administration of opioids.
May restore the efficacy of opioids when rotate from one opioid to another.
Potency vs. Efficacy
Potency - Relative term comparing doses of different agents.
Efficacy - How well does the drug stimulate downstream effects.
Half life of methadone?
15 - 40hrs
What is site syngergy with reference to opioids?
Opioids work at a number of nervous sites in the CNS and these work together to reduce pain.
Average half life of most opioids.
2 - 3hrs
How is buprenorphine administered?
Oral (sublingual)
IM/IV
Name opioid with shortest half life = 30 minutes
Diamorphine