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www.pharmteacher.com OPIOIDS for PT

Discuss metabolism of codeine and how this relates to efficacy: Codeine is partially converted to morphine by the liver
How does morphine compare to methadone? Similar analgesic potency, but methadone causes less sedation and has a longer duration of action
How does codeine compare to morphine? Codeine is about 1/10 as strong as morphine
How does fentanyl compare to morphine? Fentanyl is more potent than morphine but causes less constipation
What is an Opioid? Natural or synthetic substance that produces morphine-like effects
What is an Opiate? Natural substance derived from the opium poppy plant that produces morphine-like effects
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
List 3 types of endogenous opioids: endorphins, dynorphins, enkephalins
Opioid stimulation reduces the release of these neurotransmitters? norepinephrine, acetylcholine, dopamine, and substance P
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.
Where are opioid receptors located? CNS, peripheral nerve terminals & GI tract
List the physiological response of activation of the Mu (μ) receptors: Analgesia, Respiratory depression, Miosis, Constipation, Sedation, Euphoria
List the physiological response of activation of the Kappa (κ) receptors Analgesia (especial spinal analgesia), Hallucinations, Dysphoria
Which opioid receptors cause dysphoria? Kappa
Which opioid receptors cause respiratory depression? Mu
Which opioid receptors cause constipation? Mu
List common ADRs of opioids: N/V, sedation, constipation, respiratory depression, euphoria, dysphoria, urinary retention, physical dependence, addiction, pseudoallergy, allergy
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
How can opioid-induced N/V be treated? antiemetics
How can opioid-induced constipation be treated? Prevention works best – daily stool softener (docusate) + mild laxative. Acute constipation - treat with stimulant laxatives or enemas
Are true opioid allergies common or rare? True allergy is rare. Pseudoallergy & intolerances are commonly misrecorded as allergies in patient records
Pseudoallergic opioid reactions (itching, flushing) are caused by: histamine release WITHOUT antibody production
What physiological response constitutes a TRUE opioid allergy? True allergic reactions involve antibody production
List the most fatal opioid ADR: Respiratory depression
List the CII opioid agonists: morphine, meperidine, fentanyl, oxycodone; hydromorphone,oxymorphone
List the CIII opioid agonists: codeine/acetaminophen; hydrocodone/acetaminophen
What dosage forms of oxycodone are available? 1) oxycodone immediate release; 2) oxycodone sustained release; 3) oxycodone + acetaminophen immediate release
Which opioids are used as antitussives? codeine & hydrocodone
Describe the onset of action for fentanyl patch: Takes 12 – 24 for complete onset of action and 6 days to reach steady state.
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.
What is the MOA of methadone? Opioid agonist plus an NMDA antagonist & serotonin & norepi reuptake inhibitor making it especially helpful for neuropathic pain
What is the MOA of tramadol? Weak opioid agonist plus a serotonin & norepi reuptake inhibitor making it especially helpful for neuropathic pain
List therapeutic uses of methadone? Chronic pain; neuropathic pain; prevent withdrawal symptoms during addiction treatment
Describe the MOA of the opioid agonists/antagonists: These drugs are agonists at the Kappa receptors but are antagonists at the Mu receptors
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
List the advantages of opioid agonists/antagonists vs. opioid agonists: opioid ag/antag cause less respiratory depression and have a lower addiction potential
List the therapeutic uses of intranasal butorphanol (Stadol®): acute migraine headache
List the therapeutic uses of tramadol: mild/moderate pain; chronic pain; neuropathic pain
List the ADRs of tramadol: similar to opioids plus it increases the risk of seizures
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
How can opioid withdrawal symptoms be avoided? taper the dose over 3 – 5 days
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.
What is addiction? psychological compulsive drug use where continued use reduces quality of life; usually associated with euphoria causing drugs
What is the controlled substance category of tramadol? Not controlled substance
What is tolerance? Neuroadaptation causing diminution of drug effect over time due to chronic exposure. Tolerance is normal and does NOT indicate addiction.
How can opioid tolerance be overcome? Increase the dose. As tolerance develops to opioid benefits, tolerance also develops to ADRs allowing higher doses.
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
What opioid ADR leads to its abuse potential? euphoria and sedation
List the ingredients of Percocet oxycodone + acetaminophen
List the ingredients of Lortab hydrocodone + acetaminophen
List the ingredients of Tylenol #3 codeine + acetaminophen
List the ingredients of Vicodan hydrocodone + acetaminophen
List the ingredients of Percodan oxycodone + aspirin
Which opioids cause the most histamine release? morphine and codeine