www.pharmteacher.com OPIOIDS for PT
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| Discuss metabolism of codeine and how this relates to efficacy: | Codeine is partially converted to morphine by the liver
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| How does morphine compare to methadone? | Similar analgesic potency, but methadone causes less sedation and has a longer duration of action
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| How does codeine compare to morphine? | Codeine is about 1/10 as strong as morphine
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| How does fentanyl compare to morphine? | Fentanyl is more potent than morphine but causes less constipation
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| What is an Opioid? | Natural or synthetic substance that produces morphine-like effects
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| What is an Opiate? | Natural substance derived from the opium poppy plant that produces morphine-like effects
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| Explain the MOA of the opioid analgesics: | Opioid agonists: bind & stimulate opioid receptors. They reduce perception of pain, relieve anxiety associated with that pain, and increase pain tolerance
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| List 3 types of endogenous opioids: | endorphins, dynorphins, enkephalins
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| Opioid stimulation reduces the release of these neurotransmitters? | norepinephrine, acetylcholine, dopamine, and substance P
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| List 2 main classes of opioid receptors: | Mu (μ) and Kappa (κ)…The differences in affinity for the various opioid receptors (there are several) makes one opioid slightly different from another.
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| Where are opioid receptors located? | CNS, peripheral nerve terminals & GI tract
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| List the physiological response of activation of the Mu (μ) receptors: | Analgesia, Respiratory depression, Miosis, Constipation, Sedation, Euphoria
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| List the physiological response of activation of the Kappa (κ) receptors | Analgesia (especial spinal analgesia), Hallucinations, Dysphoria
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| Which opioid receptors cause dysphoria? | Kappa
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| Which opioid receptors cause respiratory depression? | Mu
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| Which opioid receptors cause constipation? | Mu
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| List common ADRs of opioids: | N/V, sedation, constipation, respiratory depression, euphoria, dysphoria, urinary retention, physical dependence, addiction, pseudoallergy, allergy
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| Explain the impact of chronic use (and development of tolerance) on the rate of ADRs: | Tolerance develops to most of the opioid side effects except constipation
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| How can opioid-induced N/V be treated? | antiemetics
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| How can opioid-induced constipation be treated? | Prevention works best – daily stool softener (docusate) + mild laxative. Acute constipation - treat with stimulant laxatives or enemas
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| Are true opioid allergies common or rare? | True allergy is rare. Pseudoallergy & intolerances are commonly misrecorded as allergies in patient records
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| Pseudoallergic opioid reactions (itching, flushing) are caused by: | histamine release WITHOUT antibody production
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| What physiological response constitutes a TRUE opioid allergy? | True allergic reactions involve antibody production
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| List the most fatal opioid ADR: | Respiratory depression
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| List the CII opioid agonists: | morphine, meperidine, fentanyl, oxycodone; hydromorphone,oxymorphone
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| List the CIII opioid agonists: | codeine/acetaminophen; hydrocodone/acetaminophen
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| What dosage forms of oxycodone are available? | 1) oxycodone immediate release; 2) oxycodone sustained release; 3) oxycodone + acetaminophen immediate release
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| Which opioids are used as antitussives? | codeine & hydrocodone
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| Describe the onset of action for fentanyl patch: | Takes 12 – 24 for complete onset of action and 6 days to reach steady state.
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| Describe basic administration instructions for fentanyl patch: | Place patch on dry, hairless area of body (chest, upper arms, sides of abdomen). Change patch q72h. Apply the new patch in a different location.
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| What is the MOA of methadone? | Opioid agonist plus an NMDA antagonist & serotonin & norepi reuptake inhibitor making it especially helpful for neuropathic pain
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| What is the MOA of tramadol? | Weak opioid agonist plus a serotonin & norepi reuptake inhibitor making it especially helpful for neuropathic pain
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| List therapeutic uses of methadone? | Chronic pain; neuropathic pain; prevent withdrawal symptoms during addiction treatment
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| Describe the MOA of the opioid agonists/antagonists: | These drugs are agonists at the Kappa receptors but are antagonists at the Mu receptors
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| List the disadvantages of opioid agonists/antagonists vs. opioid agonists: | opioid ag/antag aren’t as effective for pain management and tend to cause more dysphoria/hallucination
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| List the advantages of opioid agonists/antagonists vs. opioid agonists: | opioid ag/antag cause less respiratory depression and have a lower addiction potential
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| List the therapeutic uses of intranasal butorphanol (Stadol®): | acute migraine headache
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| List the therapeutic uses of tramadol: | mild/moderate pain; chronic pain; neuropathic pain
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| List the ADRs of tramadol: | similar to opioids plus it increases the risk of seizures
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| List the drug/drug interactions of tramadol: | similar to opioids plus an increased risk of serotonin syndrome with other sertotonin drugs SSRIs, SNRIs, TCAs, & MAOIs
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| How can opioid withdrawal symptoms be avoided? | taper the dose over 3 – 5 days
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| What is physical dependence? | Neuroadaptation where body becomes dependent upon the drug for normal function. Abstinence results in withdrawal symptoms. This does NOT indicate addiction.
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| What is addiction? | psychological compulsive drug use where continued use reduces quality of life; usually associated with euphoria causing drugs
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| What is the controlled substance category of tramadol? | Not controlled substance
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| What is tolerance? | Neuroadaptation causing diminution of drug effect over time due to chronic exposure. Tolerance is normal and does NOT indicate addiction.
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| How can opioid tolerance be overcome? | Increase the dose. As tolerance develops to opioid benefits, tolerance also develops to ADRs allowing higher doses.
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| List the ADRs of opioid agonist/antagonists: | similar to the opioids but less addiction potential, less respiratory depression, & more psychotomimetic effects, will precipitate opioid withdrawal in physically dependent patients
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| What opioid ADR leads to its abuse potential? | euphoria and sedation
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| List the ingredients of Percocet | oxycodone + acetaminophen
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| List the ingredients of Lortab | hydrocodone + acetaminophen
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| List the ingredients of Tylenol #3 | codeine + acetaminophen
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| List the ingredients of Vicodan | hydrocodone + acetaminophen
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| List the ingredients of Percodan | oxycodone + aspirin
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| Which opioids cause the most histamine release? | morphine and codeine
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