Term
Three "Step 1" drugs for pain.
In other words, three first rung drugs. |
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Definition
Aspirin
Acetaminophen
NSAIDs |
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Term
| Four drugs on step two of the pain ladder. |
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Definition
Codeine
Tramadol
Hydrocodone
Oxycodone |
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Term
| Three drugs on the top step of the ladder. |
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Definition
Morphine
Hydromorphone
Fentanyl |
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Term
Name 5 high analgesic efficacy drugs.
Which one stands out in terms of receptor effect? |
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Definition
Morphine, Methadone, Meperedine, Fentanly, Buprenorphine.
They are all agonists except Buperenorphine, which is a partial and mixed agonist/antagonist.
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Term
Name three moderate to low analgesic opioids.
Which one stands out in terms of receptor activity? |
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Definition
Hydrocortone, oxycodone, pentazocine.
Pentazocine is a partial and mixed agonist/antagonist. |
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Term
| Name two opioid anatagonists. |
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Definition
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Term
| What is a very common side effect of opiods? |
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Definition
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Term
| Describe how the Mu1 receptors work in terms of function. |
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Definition
Normally GABA is released to inhibit the Pain Inhibitory Neuron so that pain can be felt.
Opioids can bind to the MOR on the GABA-secreting neuron or presynaptically on the axon of the GABA-secreting neuron. Opiods will Inhibit the Inhbitor to allow the Pain Inhibitory Neuron to do its job. |
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Term
| Describe the MOA of opioid receptors. |
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Definition
They are all Gi.
Recall that this means a decrease in cAMP.
This leads to a block of voltage-gated Ca channels presynaptically and opens K channels post-synaptically. |
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Term
| Two major/common adverse effects of opiods besides constipation. |
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Definition
| Nausea and respiratory depression |
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Term
| Morphine causes vascular dialation. What are the three mechanisms for this action? |
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Definition
1. Histamine release
2. Despression of vasomotor centers
3. Hypercapnia |
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Term
| Which hormones increase and which hormones decrease with larger dose of morphine? |
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Definition
Increase: PIH (DA), gNRH, CRH
Decrease: Prolactin, GH
Recall that you will also see Miosis, flushing, sweating, iching, and a depression of the immune system. |
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Term
| Briefly describe the high points of the pharacokinetics of morphine. |
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Definition
| It only has an oral bioavaliability of 25%. There is a very high first pass effect which yields 1 inactive (M3G) and 1 active (M6G) metabolite. |
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Term
| This drug, in comparison to morphine, has a shorter duration of action, does not stimulate histamine much, and has a minimal drop in BP. |
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Definition
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Term
| Fentanyl can be administered many different ways. Some times a high dose can be administered accidentally which can result in a delayed respiratory depression. What causes this? |
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Definition
| Fentanyl is very lipid soluble so it gets temporarily stored and released later. |
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Term
| This opioid is a mu and kappa agonist. It is contraindicated in patients who are on MAO-I's because it can cause CNS excitation resulting in death. |
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Definition
Meperidine.
An intersting fact about this drug is that it has some anti-muscarinic effects so you don't get miosis. |
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Term
| This opioid has an oral bioavalibility over 90% and a much longer halflife than morphine. It also has negligible release of histamine. |
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Definition
Methadone.
This drug is sometimes used to help heroin addicts kick the habit. |
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Term
| This drug is a partial mu-agonist but it binds very strongly so it cannot be antagonized by naloxone. |
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Definition
Buprenorphine.
If you give this drug in a large bolus, it can precipitate withdrawl in patients earlier for a faster recovery from addiction. |
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Term
This opioid is a weak mu-agonist and inhibits reuptake of 5-HT and NE.
Naloxone can reverse the respiratory depression but can only reverse some of the analgesia this drug causes. |
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Definition
Tramadol.
Note that Tramadol lowers the seizure threshold. |
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Term
| What are the three phases of Opioid Withdrawal Syndrome? |
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Definition
Prodromal: restless, irratable, sweating
Acute: anxiety, craving, nausea, vomiting
Protracted: Insomnia, weight and pupil changes |
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Term
| What ion movement system is altered upon the activation of opiod receptors? |
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Definition
| Presynaptic voltage-gated Ca++ channels are closed. |
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Term
| What are the direct and indirect effects which lead to the analgesic effects of opioids? |
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Definition
Direct: inhibition of ascending pathway
Indirect: activation of descending pathway |
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Term
| What is the post-receptor effect triggered by opioid receptor activation? |
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Definition
| Opening of K+ channels on neuronal cell membrane. |
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Term
| Morphine increases non-vascular smooth muscle tone. What two specific locations in the body would this effect that has a clinical impact? |
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Definition
Sphincter of oddi and the internal bladder sphincter both contract when the patient is on morphine.
This can lead to urinary retention of exacerbation of GI issues. |
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Term
| Does morphine decrease tidal volume or decrease the rate of breathing? |
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Definition
Trick question.
Morphine decreases ALL PHASES of respiration because it acts centrally to reduce the brains response to the partial pressure of CO2. |
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Term
| Describe how morphine elicits miosis and how this effect can be blocked. |
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Definition
Morphine stimulates the Edinger-Westphal nucleus which acts on muscarinic receptors thus causing miosis of the eyes.
Atropine blocks muscarinic receptors, thus countering the miosis. |
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Term
What two general types of injuries or pathologies should you not use morphine for?
I know this is a general question so just flip the card. |
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Definition
| Don't use morphine for inflammation or any sort of head injury. |
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Term
| You've just spend 4 years at Evil Medical School to become Dr. Evil. You want to precipitate abstinence syndrome in your patient who is addicted to heroin. How can you accomplish this? |
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Definition
| Naloxone precipitates abstinence syndrome in addicts. This is a rapid onset of withdrawal symptoms with a short duration. |
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Term
| Your patient is a recreational drug user and was just administered an opiate for pain managment. Shortly thereafter the patient began experiencing visual hallucinations. What drug was administered? |
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Definition
| Pentazocine. Recreational drug use can sensitize receptors thus causing dysphoria upon stimulation. |
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Term
| This drug is contraindicated in patients with heart issues because it can increase arterial and pulmonary pressure as well as heart rate. |
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Definition
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Term
| In the pain management of a person addicted to opiates, what subclass of opiates are contraindicated? |
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Definition
| Partial agonists such as Buprenorphine are contraindicated. Recall that this would produce a REDUCED effect which can precipitate withdrawal symptoms. |
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Term
| Opioids stimulate the Chemoreceptor Trigger Zone. Where is this located? |
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Definition
| CTZ is located in the Area Postrema. |
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