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62 Cards in this Set
- Front
- Back
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What are the principles that should be used with analgesic management of pain?
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Don't use too intense of an analgesic for the pain
Titrate the analgesics to the severity of the pain Use regularly scheduled dosing, not "as needed" Be careful with opioids - people get addicted! |
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What is the hierarchy of analgesics?
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Low potency to high potency:
NSAIDS Low-potency opioids High potency opioids |
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What are examples of some low-potency opioids?
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Codeine
Oxycodone Hydrocodone |
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What are examples of some high potency opioids?
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Morphine
Hydromorphone Methadone Fentanyl Levorphanol |
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What are the therapeutically relevant opioid receptors? Whhich one is he most important?
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Mu
Kappa Mu is the most important therapeutically |
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What is a result of the stimulation of mu opioid receptors?
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Analgesia
Sedation Decreased gut motility Ventilatory depression Euphoria Physical dependance |
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What is a result of the stimulation of kappa opioid receptors?
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Analgesia
Sedation Decrased gut motility |
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What are the different classifications of opioids?
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Pure agonists
Opioid agonist-antagonists Pure opioid antaoniss |
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What is the prototype pure opioid agonist?
What receptors does it activate? |
Morphine sulphate
Both mu and kappa receptors |
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What are examples of opioid agonist-antagonists?
What are their effects at the different receptor subtypes? |
Nalbupine
Activate the kappa receptors Weakly activate or block the mu receptors so that they can't be occupied by stronger agonsts |
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What is the prototype opioid antagonist?
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Naloxone
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What is the prototype partial opioid agonist?
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Pentazocine
Weakly activates mu receptors Activates the kappa recepors |
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Where do opioids have their effects?
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In the brain, but all over the CNS:
Brainstem Spinal cord Primary aferent peripheral nerve terminals |
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Where are some specific places where opioids act to cause their side effects?
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Medullary respiratory control center: respiratory depression
Medullary CTZ: vomiting center GI tract: we don't know how they work there |
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What are the pharmacokinetics of morphine?
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Extensive 1st pass hepatic metabolism!
-Most of the morphine is metabolized the first time around In light of this, give enough to saturate the liver enzymes and then enough to have the desired effect |
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What are the uses of morphine?
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"Gold standard" for severe pain
Allays anxiety about pain Causes venodilation |
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What are the side effects of morphine?
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Euphoria
Ventilatory depression, increased ICP Nausea, emesis Constipation Urinary retention or urgency Gall bladder pain/bile duct spasm Hypotension |
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What is the effect of decreasing respiratory rate on ICP?
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Increases it.
Morphine decreases respiratory rate, and, therefore can increase ICP |
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What is the effect of opioids on the medulla?
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They decrease the normally protective medullary response to increased pCO2
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What is the main cause of death with opioids?
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Ventilatory depression
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What is the definition of tolerance?
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Biologic processes, that, over time, cause decreased drug effectiveness, require increased drug dose to restore level of effect seen before tolerance developed
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What is the definition of dependence?
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Biologic changes in various homeostatic "set points"-->further changes (withdrawal) when drug administration stopped
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What is the definition fo addiction?
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Complex behavioral patterns involveing compulsive seeking and using more of the drug
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What effects of morphine do people not gain tolerance to?
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Miosis: pupils are super dilated
THINK OF THIS WITH SOMEONE COMING IN WITH AN UNKNOWN DRUG OVERDOSE. |
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What effects of morphine do people gain tolerance to?
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Analgesia
Ventilatory depression Euphoria |
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How does the therapeutic index for morphine change as a person is more and more addicted?
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It doesn't.
The LD stays parallel with the ED. |
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With what types of drugs does the therapeutic index change as tolerance develops?
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Alcohol
Barbiturates |
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What is cross-tolerance? How does it relate to opioids?
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If you're tolerant to one opioid, you're tolerant to them all.
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What is he principle of cross dependence? How is this used with therapy?
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Suitable doses of a strong abonist can substitute for another that has caused severe dependence, making withdrawal not so bad.
This is what happens when people are in rehab for heroin. |
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In what patients should you be especially cautious about prescribing opioids? WhY?
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Sleep apnea
COPD Ventilatory/respiratory problems could mean that they have more severe effects from the opioids. |
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What is the withdrawal like from heroin? Methadone?
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Heroin/morphine: SUPER INTENSE but relatively brief
Methadone: longer lasting, but more mild |
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Is opioid withdrawal fatal?
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Rarely
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What is the cause of fatalities from alcohol or barbiturate withdrawal?
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Seizures
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What is the potency of fentanyl or sufentanyl vs. morphine?
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It's much stronger: 50-75 times as potent
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What is the administration route for fentanyl and sufentanyl?
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Parenteral
Transdermal Transumcosal |
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What is the use of parenteral fentanyl and sufentanyl?
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General anesthesia induction, maintenance
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What is the use of transdermal fenanyl and sufentanyl?
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Maintenance therapy of severe, chronic pain
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What is the use of transmucosal fentanyl and sufentanyl?
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Preanesthetic medication, conscious sedation
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What is the potency of parenteral methadone compared to MS?
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Equipotent
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What is the oral bioavility of methadone?
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Great (in contrast to morphine)
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What happens to the overall amounts of methadone in the body>
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Tends to accumulate...the enzymes breaking it down get saturated.
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What is the use of methadone?
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Long-term pain control
Detoxification or maintenance therapy for addiction with morphine |
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What are the unique uses of meperidine?
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Cholecystitis: less biliary tract spasming
Shorter half life means less ventilatory depression, etc. |
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What are the problems with meperidine?
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Frequent dosing due to short half-life
You can get accumulations of the drug due to the frequent dosing |
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What are contraindications to a prescription of meperidine?
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DDIs with drugs that increase serotonin availability
SSRIs MAOis Tricyclic antidepressants |
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What makes heroin so potent?
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Lipophilic
Metabolized to active metabolites! |
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What are some of the more moderate opioids?
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Codeine
Hydrocodone Oxycodone |
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What drugs potentiate the effects of the moderate opioids?
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Asprin
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What is a common way that people abuse oxycodone?
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Breaking it up, dissolving and injecting, snorting, etc.
All trying to get higher levels in the drug |
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What are some analgesic adjuncts for severe pain?
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Clondine
Anticonvulsants |
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What is the activity of clondine?
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Stimulation of alpha-2 receptors in the spinal cord-->analgesia
Simulation of alpha-2 in brain: decreased SNS outflow |
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What are some of the anticonvulsants used for severe pain?
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Carbamazepine
Gabapentin Lamotrigine |
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What is the mechanism by which anticonvulsants prevent pain?
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Block sodium channels in sensory neurons carrying pain signals
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What are the indications for the use of pentazocine? What kind of a drug is it?
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Partial opioid agonist: works at kappa receptors, weak agonist of mu recpetors
Moderate pain Can't use it for severe pain because there are severe side effects from high doses of the drug. |
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What are the severe side effects of pentazocine?
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Dysphoria, hallucinations
Hypertension, tachycardia Ventilatory depression |
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What kind of a drug is nalbuphine? What are the uses for it?
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Opioid agonist/antagonist
Few CV effects |
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What kind of a drugs is naloxone? What are the uses for it?
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Opioid antagonist
Diagnosis or treatment of opioid overdose |
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What is the administration of naloxone?
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Injected.
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What are some of the "non-analgesic opioid derivatives?
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Dextromethorphan
Diphenoxylate |
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What is the use of dextromethorpan?
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Antitussive in OTC cough mds
Can't use it for pain because of the side effecs at pain reducing doses |
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What is the activity of dextromethorphan?
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Blockage of NMDA receptors
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What kind of a drug is diphenoxylate? What are uses for the drug?
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Non-analgesic opioid derivative
Oral antidiarrheal |
