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123 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What are opioids the drug of choice for?
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Severe or chronic malignant pain
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Are opioids natural or synthetic and what kind of effect do they produce?
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Natural OR synthetic and they produce morphine-like effects.
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What is the term "opiate" reserved for?
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Morphine or Codeine, obtained from the juice of the opium poppy.
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By what are the major effects of the opioids mediated?
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3 major receptor families - mu, kappa and delta.
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By what are the analgesic properties of the opioids primarily mediated?
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MU receptors, but the K receptors in the dorsal horn also contribute.
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With what do the enkephalins interact?
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(More selectively with) the DELTA receptors.
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What are all 3 opioid receptors members of and associated with?
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the G-protein coupled receptor family, & assoc. with ion channels, increasing postsynaptic K+ efflux (hyperpolarization) or reducing presynaptic Ca2+ influx, thus impeding neuronal firing and transmitter release.
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Where is the distribution of the opioid receptors?
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On the peripheral sensory nerve fibers
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What do the opioid receptors in the Brainstem do?
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Mediate respiration, cough and pupillary diameter.
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What does the Medial Thalamus do? (What do the opioid receptors here do?)
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Mediate deep pain that is poorly localized and emotionally influenced.
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What do the opioid receptors in the Spinal Cord do?
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Receptors in the Substantia Gelatinosa are involved w/the receipt and integration of incoming sensory information.
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What do the opioid receptors in the Periphery do?
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Inhibit Ca2+ - dependent release of excitatory, proinflammatory substance, e.g. Substance P, from the nerve endings.
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What is the prototype strong agonist?
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Morphine
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Is Codeine more or less potent than Morphine?
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Less potent
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How do opioids work? What's their MOA?
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they cause hyperpolarization of nerve cells, inhibition of nerve firing, and presynaptic inhibition of transmitter release and decrease the release of substance P.
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DIHI
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What does Morphine appear to inhibit?
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The release of many excitatory transmitters from nerve terminals carrying nociceptive (painful) stimuli.
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Morphine causes Analgesia without what?
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The loss of consciousness
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How do opioids relieve pain?
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Both by raising the pain threshhold at the spinal cord level and (more importantly) by altering the brain's perception of pain.
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Why are opiods said to "alter the affective component of pain?"
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Pts tx-ed w/morphine are still AWARE of pain, but the sensation is not unpleasant.
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What sense does Morphine produce?
Via stimulation of what? |
A powerful sense of contentment (and well-being)
Via stimulation of the VENTRAL TEGMENTUM. |
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With regard to RESPIRATION, what does Morphine do?
How? |
Causes respiratory depression.
By reduction of the sensitivity of respiratory center neurons to CO2. |
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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 properties do Morphine and Codeine have with reference to the cough reflex?
Anything special about these receptors? |
They both have anti-tussive properties. The receptors involved in the anti-tussive action appear to be different from those involved in analgesia.
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What is the pin-point pupil characteristic of?
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Morphine use.
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What does morphine excite?
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The Edinger-Westphal nucleus of the occulomotor nerve.
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Is there tolerance to the excitation of the Edinger-Westphal nucleus of the occulomotor nerve?
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No, there is little tolerance to the effect, and all morphine abusers demonstrate pinpoint pupils.
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Why are the pinpoint pupils important, diagnostically?
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Because many other causes of coma and respiratory depression produce dilation of the pupil.
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How does morphine work with regard to emesis?
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It directly stimulates the chemoreceptor trigger zone in the area postrema that causes vomiting.
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How does Morphine relieve diarrhea? What can it produce?
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By decreasing the motility. It can produce constipation, with little tolerance (developing).
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Does Morphine have any effect on BP or HR?
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No.
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Why is Morphine contraindicated in severe brain injury?
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B/c of the respiratory depression and CO2 retention, cerebral vessels dilate and increase CSF pressure!
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What are the hormonal effects of Morphine?
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It increases ADH, leading to urinary retention. It can also inhibit the bladder voiding reflex...
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What can opioids be used to supplement?
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the sleep-inducing properties of benzos (e.g. flurazepam)
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Which drug is more widely used to suppress the cough reflex?
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Codeine or Dextromethorphan. Codeine has greater anti-tussive action than Morphine.
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How does Morphine work w/ regard to severe pulmonary edema?
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IV Morphine is used to relieve dyspnea caused by pulmonary edema assoc. with LV failure. (poss. d/t its vasodilatory effect)
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How is Morphine administered?
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Usually NOT orally. IM, subq or IV injections produce the most reliable responses.
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When should Morphine NOT be used?
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During labor, for analgesia.
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What is the duration of action of Morphine?
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4-6 hours.
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When is the duration of Morphine longer? Why?
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When it's injected epidurally, b/c its low lipophilicity prevents redistribution.
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What pts are more sensitive to the analgesic effects of morphine, and what does this mean for them?
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Elderly pts! They should be treated with lower doses.
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Who should NOT receive morphine? Why not?
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Neonates, b/c of their low conjugating capacity.
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What are the adverse effects of morphine?
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Severe respiratory depression, which can result in death in acute opioid poisoning.
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What can morphine cause in prostatic hypertrophy?
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Acute urinary retention.
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What does repeated use of morphine produce?
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Tolerance to the respiratory depressant, analgesic, euphoric and sedative effects of morphine.
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With what does tolerance to morphine NOT develop?
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To the pupil-constricting and constipating effects of the drug.
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What kind of dependence readily occurs with morphine?
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Physical and psychological dependence, with morphine and some of the other agonists, as well.
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How is detoxification of heroin- or morphine-dependent individuals accomplished?
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Through oral admin. of methadone or clonidine.
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What do low doses of amphetamine (w/morphine) inexplicably enhance?
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Analgesia
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What is Meperidine?
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A synthetic opioid
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To what receptors does Meperidine bind?
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Mu receptors
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How is Morphine administered?
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Usually NOT orally. IM, subq or IV injections produce the most reliable responses.
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When should Morphine NOT be used?
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During labor, for analgesia.
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What is the duration of action of Morphine?
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4-6 hours.
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When is the duration of Morphine longer? Why?
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When it's injected epidurally, b/c its low lipophilicity prevents redistribution.
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What pts are more sensitive to the analgesic effects of morphine, and what does this mean for them?
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Elderly pts! They should be treated with lower doses.
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Who should NOT receive morphine? Why not?
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Neonates, b/c of their low conjugating capacity.
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What are the adverse effects of morphine?
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Severe respiratory depression, which can result in death in acute opioid poisoning.
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What can morphine cause in prostatic hypertrophy?
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Acute urinary retention.
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What does repeated use of morphine produce?
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Tolerance to the respiratory depressant, analgesic, euphoric and sedative effects of morphine.
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With what does tolerance to morphine NOT develop?
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To the pupil-constricting and constipating effects of the drug.
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What kind of dependence readily occurs with morphine?
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Physical and psychological dependence, with morphine and some of the other agonists, as well.
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How is detoxification of heroin- or morhphine-dependent indiciduals accomplished?
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Through oral admin. of methadone or clonidine.
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What do low doses of amphetamine inexplicably enhance?
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Analgesia
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What is Meperidine?
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A synthetic opioid
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To what receptors does Meperidine bind?
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Mu receptors
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What does Meperidine do to pupils?
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It causes them to dilate (does NOT cause pin-point pupils), b/c of an atropine-like action.
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Where is Meperidine commonly employed?
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In obstetrics.
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When is Meperidine preferred over Morphine and why?
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For analgesia during labor b/c of its shorter action
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What do some pts. experience with Meperidine and why? (adverse effects)
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Dry mouth and blurred vision, due to its antimuscarinic action.
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What is methadone?
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A synthetic, orally effective opioid that is ~ = in potency to morphine, but w/ a somewhat longer duration of action.
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MOA of Methadone? (receptors)
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Its actions are mediated by the Mu receptors.
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Is the analgesic action of Methadone equal, less or more potent to that of morphine?
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Equivalent to that of morphine.
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How/when is methadone used?
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In controlled w/drawal of dependent abuser from heroin and morphine.
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What is the w/drawal syndrome of methadone like? (hint: in terms of length)
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Milder but more protracted than that of other opioids.
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How strong is Fentanyl?
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100-fold the analgesic potency of morphine.
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Is the duration of Fentanyl short or long?
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Short (w/rapid onset).
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When is epidural Fentanyl used?
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During labor.
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When is the transmucosal prep of Fentanyl used?
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In the tx of Ca pts w/breakthrough pain who are tolerant to opioids.
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How should the transdermal patch be used?
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With caution!! Death results from hypoventilation and the patch creates a reservoir of the drug in the skin.
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How are the onset & offset of Fentanyl? (in terms of length)
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The onset is delayed and the offset is prolonged.
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Is Sufentanil more or less potent than Fentanyl?
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MORE potent.
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Does heroin occur naturally?
How is it produced? |
No. It is produced by diacetylation of morphine.
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What allows heroin to cross the BBB?
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Its greater lipid solubility
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What is the euphoria with heroin like?
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awesome. j/k.
More exaggerated than with morphine |
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Is Codeine a more or less potent analgesic than morphine?
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Much less potent
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At what doses does Codeine show good antitussive activity?
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At doses that do not cause analgesia
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What is the euphoria produced with Codeine like? (as compared with Morphine)
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There is LESS euphoria produced with Codeine than with morphine.
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How is Codeine often used?
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In combo with acetaminophen.
--> Tylenol w/Codeine (APAP) |
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What has Codeine been replaced by in most nonprescription cough preps? Does it have analgesic action?
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Dextromethorphan – no analgesic action!
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What is Oxycodone? How is it active?
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A semisynthetic derivative of morphine.
It is Orally active |
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For what is oxycodone used?
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To tx moderate to severe pain
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What is Propoxyphene? And for what is the dextro isomer used?
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A derivative of methadone.
--> Used as an analgesic to relieve mild to moderate pain. |
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What is the levo isomer of Propoxyphene? Is it an anlagesic? What is its main action?
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NO, it is not an analgesic, but does have ANTITUSSIVE action.
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Is Propoxyphene a stronger or weaker analgesic than codeine?
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Weaker
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How is Propoxyphene often used? In combo with what?
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In combo with aspirin or acetaminophen for an analgesia > that obtained w/either drug alone
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What is the Darvon comound?
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Propoxyphene
ASA Caffeine |
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What is Darvocet?
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Propoxyphene
APAP |
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What can Propoxyphene cause when used with alcohol and sedatives?
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Severe CNS depression and
Death by respiratory depression and Cardiotoxicity |
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How can the respiratory depression and sedation by Propoxyphene be antagonized?
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Naloxone (Narcan)
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What does Naloxone NOT help (which side effect does it not antagonize)?
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The Cardiotoxicity (from using alcohol or sedatives with Propoxyphene)
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What are mixed-agonist-antagonists?
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Drugs that stimulate 1 receptor but block another
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What does the effect of mixed-agonist-antagonists depend on?
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Previous exposure to opioids
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In which individuals do mixed-agonist-antagonists show agonist activity and for what are they used?
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In those who have not recently received opioids
They are used to relieve pain. |
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What do the mixed-agonist-antagonists do in the pt with opioid dependence?
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They primarily blocking effects --> produce w/drawal sx!
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On which receptors does Pentazocine act?
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On the Kappa receptors, and is a weak agonist at Mu and Delta receptors.
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What is Buprenorphine?
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A partial agonist, acting on the Mu receptor.
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What are the major uses of Buprenorphine and why?
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In opiate detoxification, b/c it has a less severe and shorter duration of w/drawal sx compared to methadone
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In contrast to methadone, which is only available at specialized clinics, what is buprenorphine approved for?
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Office-based detox or maintenance
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What are Nalbuphine and Butorphanol, like Pentazocine used for?
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They play a limited role in the tx of chronic pain.
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What is Tramadol?
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A centrally acting analgesic that binds to Mu-receptors
It is used to manage moderate to moderately severe pain |
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What is of particular concern with the use of Tramadol?
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The seizures that can occur!!
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To what do the opioid antagonists bind with high affinity?
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To opioid receptors (gee...) ;)
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Do they have an effect in normal individuals?
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No, no profound effects.
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What do the antagonists rapidly reverse and what sx do they precipitate?
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The effect of agonists and
Precipitate the sx of opiate w/drawal |
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What is Naloxone used to reverse?
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The coma and respiratory depression of opioid overdose
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How does Naloxone work?
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It rapidly displaces all receptor-bound opioid molecules (making it able to reverse the effects of heroin OD)
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What is the time frame in which Naloxone works?
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w/in 30 sec. of IV injection, it reverses the respiratory depression and coma
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What is the duration of action of Naloxone? (general - short or long?)
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relatively short duration
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What does the relatively short duration of action of Naloxone mean? (hint: relapse)
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Pts may lapse back into respiratory depression
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What is the duration of action of Naltrexone?
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It has a longer duration of action than Naloxone – up to 48 hrs.
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How is Naltrexone used? (hint: in combo?) What is it used for?
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In combo with Clonidine – for rapid opioid detox.
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What are the opioid w/drawal sx?
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•Diarrhea
•Rhinorrhea •Vomiting •Chills-piloerection •Lacrimation •Anxiety •Yawning •Hostility •Hyperventilation •Hypothermia |
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What does Meperidine do to pupils? Why?
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It causes them to dilate, b/c of an atropine-like effect.
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