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58 Cards in this Set
- Front
- Back
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What Rx classes best treat neurogenic pain?
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1) anticonvulsants (pregabalin)
2) TCAs ( amitriptyline) 3) SNRI's ( duloxetine) |
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What are the three opioid receptors?
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1) MU
2) Kappa 3) Delta |
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What receptor is mainly responsible for the analgesic properties of opioids?
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Mu receptor.
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What two opioids induce their analgesic effects by acting on the Kappa receptor in the dorsal horn?
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butorphanol and nalbuphine.
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What are three mxn proposed for the action of opioids?
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1) Decrease cAMP
2) Block the Ca channel on the presynaptic neuron. 3) Activate the K channel on the post synaptic neuron. |
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Where in the nervous system would you expect to find opioid receptors?
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1) Brainstem
2) Medial Thalamus 3) Spinal chord 4) Hypothalamus 5) Limbic system (amygdala therefore emotion not analgesia) 6) Periphery 7) Immune - cells. |
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What is the MOA of morphine?
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Acts on the kappa receptors in the Lamina I and Lamina II of the dorsal horn to decrease the release of substance P.
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What part of the CNS does morphine have it's euphoric effects on?
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Disinhibition of the ventral tegmentum.
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What effect does morphine have on respiration?
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Blocks the CO2 chemoreceptors and therefore it depresses ventilation rate.
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What is the most common cause of death in acute opioid overdose?
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Respiratory depression.
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What two opioids seem to have an effect on cough depression?
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1) morphine
2) codeine |
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What sign is commonly seen in all opioid abusers?
What is the MXN? |
Pinpoint pupils.
Excitation of the EW nucleus enhances parasympathetic tone to the eye. |
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What is the effect of Morphine on the GIT?
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It can lead to constipation and increase pressure in the biliary tract (contracts GB and biliary sphincter)
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What is the effect of morphine on histamine release?
What symptoms does this cause? |
Morphine causes an increase release in histamine
symptoms: a) urticaria b) sweating c) vasodilation. |
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Why would you use morphine in conjunction with Temazepam?
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Drug wouldn't be able to carry out its sedative properties in the presence of pain.
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How does morphine effect diarrhea?
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It decreases intestinal motility and increases intestinal circular muscle tone.
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Which Rx has a greater antitussive effect morphine or codeine?
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Codeine.
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If a patient has acute pulmonary edema due to Lt heart failure what Rx could you give?
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Morphine, It has a vasodilatory effect.
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What is the worst way to administer morphine? Why?
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Orally because you see poor absorption and extensive first pass metabolism.
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Morphine _______ crosses into the placenta and ________ crosses the BBB.
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Readily
Poorly |
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Which 3 opioids readily pass into the BBB?
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1) Fentanyl
2) Methadone 3) Heroin. |
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Which form of the metabolized morphine is more active 6 or 3?
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6
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What is the effect of morphine on benign hyperplasia?
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Causes urinary retention.
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What 3 drugs are given in the detoxification of morphine?
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1) Methadone
2) Buprenorphine 3) Clonidine |
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What receptors does Meperidine bind to?
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Mu and Kappa
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What differences do you see with Meperidine as oppose to morphine?
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1) Possible increase in CO
2) Pupillary dilation. |
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What is the difference between the uses of Meperidine and morphine?
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Meperidine has no benefit in suppressing cough or diarrhea. It can however, be used in obstetrics.
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What is dangerous about Meperidine use?
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The toxic effects of it's metabolite normeperidine.
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What are the uses of methadone?
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Analgesia and wean opioid abusers of morphine or heroin.
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What is the difference between the route of administration of methadone vs. morphine.
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Methadone can be absorbed well through oral administration.
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How potent is fentanyl with comparison to morphine?
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100 times more potent
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What si the duration of action of fentanyl?
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15 - 30 minutes.
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What is the application of the transmucosal preparation of fentanyl?
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Treatment of extreme pain felt in cancer patients.
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What is the danger of the transdermal patch preparation of fentanyl?
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Causes hypoventilation.
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What type of surgery is fentanyl particularly useful in?
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Cardiac surgery because it has minimal effects on the myocardium.
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What opioid is even more potent than fentanyl?
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Sufentanil
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How much more potent is heroin than morphine? What property is exaggerated?
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Heroin is about 3 times more potent than morphine. It crosses BBB fast so the euphoric property is amplified.
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What is Oxycodone packaged with?
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Acetaminophen. Abuse leads to deaths.
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What is symptom can be relieved by codeine itself rather than it's metobolite morphine?
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Coughing.
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What derivative of methadone is used to treat cough but has weak analgesic properties?
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Propxyphene.
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What are the adverse effects of propoxyphene?
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1) Respiratory depression
2) convulsions 3) hallucinations 4) confusion. |
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What are mixed agonists?
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Drugs that agonize one receptor and block another.
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What is the action of mixed agonist on Naive patients? Patients on opioids?
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a) alleviate pain
b) produce withdrawal symptoms |
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What receptors does Pentazocine act on?
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agonizes kappa and antagonizes mu and delta.
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What Rx has replaced methadone as the drug of choice for morphine detoxification?
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Buprenorphine because it has less effects on
1) respiratory depression 2) hypotension 3) sedation. |
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What receptor does buprenorphine act on?
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Mu receptors.
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What 3 Rx's would you consider as analgesics for patients with respiratory problems?
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1) pentazocine
2) Nalbuphine 3) Butorphanol |
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Aside from binding to Mu, what other synaptic effects does Tramadol have?
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slightly inhibits the re - uptake of 5 -HT and NE
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What drug might increase the serum level of Tramadol?
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cabamazepine
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What Rx might decrease the serum level of Tramadol?
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quinidine.
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What Rx's should not be taken concurrently with Tramadol?
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1) SSRI's (causes seizures)
2) TCA's 3) MAOi's |
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What are the 3 opioid antagonists?
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1) Naloxone
2) Naltrexone 3) Nalmefene |
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What effect do opioid antagonists have on naive patients?
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NONE
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What two characteristics of morphine overdoes can naloxone treat?
How long does it take? |
Respiratory depression and coma.
Takes 30secs |
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What are 2 possible Rxs that you can mix with Naltrexone to give rapid detoxification?
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Clonidine or Buprenorphine
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What is the possible toxicity of Naltrexone?
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Hepatotoxicity.
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Although naltrexone can also be used in chronic alcoholism, what is the Rx of choice?
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BZD's OR clonadine (note this is a selective alpha 2 antagonist).
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What are 3 modes of administration of Nalmefene?
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1) IV
2) Intramuscular 3) Subcutaneous |
