Final Flashcards
These opioid receptors are the most important pharmacologically. When stimulated they produce analgesia, euphoria, respiratory depression, and sedation. With knockout mice who didn’t have the receptor morphine was ineffective.
Mu receptors
These opioid receptors when activated produce analgesia and sedation.
Kappa receptors
These opioid receptors don’t interact with known opioids.
Delta receptors
This class of opioid drugs activate mu and kappa receptors and include morphine, codeine, meperidine, and other morphine like substances.
pure opioid agonists
This class of opioids works depending on the receptor type. They are antagonists at the mu receptor and agonists at the kappa receptor. This class includes pentazocine, nalbuphine, and butorphanol.
agonist-antagonist opioids
This opioid drug is unique because it is a partial agonist at mu receptors and an antagonist at kappa receptors.
Buprenorphine
This class of drugs act as an antagonist at mu and kappa receptors. It includes Naloxone, which is an antidote to overdose.
pure opioid antagonists
This prototype opioid used for moderate to severe pain relief. It’s actions include drowsiness, mental clouding, anxiety reduction, and a sense of well being. It acts through the CNS and the periphery and prolonged use will lead to tolerance and dependence. Adverse effects include respiratory depression, constipation, orthostatic hypotension, urinary retention, cough suppression, biliary colic, emesis, elevated ICP, euphoria/dysphoria, sedation, miosis, neurotoxicity, and with prolonged use hormonal changes and immune system alterations.
Morphine
After using opioids like morphine for a long time this develops to the effects of analgesia, euphoria, sedation, and respiratory depression. It takes increasing doses to get the same response. It also develops for oxycodone, methadone, codein, and heroin.
tolerance
This can develop in regards to morphine and other opioids and raises the abuse potential. This is the reason that opioids have to be slowly withdrawn, and if they aren’t symptoms such as yawning, rhinorrhea, sweating, sneezing, diarrhea, abdominal cramps, muscle pain/spasms, gooseflesh, and kicking.
physical dependence
What do fentanyl, alfentanil, remifentanil, meperidine, methadone, heroin, hydromorphone, oxymorphone, and levorphanolhave in common?
They are all strong opioids.
What do codeine, oxycodone, hydrocodone, and propoxyphene have in common?
They are moderate to strong opioids.
This drug crosses the BBB where it is converted to monoacetylmorphine and morphine. These two substances are responsible for the effects of this drug. It has better lipid solubility than morphine.
heroin
What are the three dosing guidelines for the clinical use of opioids?
assessment of pain - pain status should be evaluated before and 1 hour after opioid use. Dosage determination - opioid doses should be adjusted to accomodate individual variation. Dosing schedule - should be fixed q4 for best results.
This drug is the prototype opioid antagonist that is a structural analog that blocks opioid action. It can be given IM, IV, or subQ. It is used for the reversal of opioid OD, reversal of postoperative opioid effects, and the reversal of neonatal respitratory depression.
Naloxone (Narcan)
This type of headache occurs in a series and last from 15 minutes to 2 hours, and can happen two to three times a day. They are marked by unilateral pain in the inner eye.
cluster headaches
These are the most common type of headache and they tend to take on a headband distribution.
Tension headaches
This type of headache is caused by a neurovascular disorder and involves the inflammation and dilation of intracranial blood vessels.
Migraine headache
The type of migraines where there is an aura present 10-30 minutes before the actual headache where patients report flashes of light, blank areas in the field of vision, or zigzag patterns.
Migraines with aura (classic migraine)
this type of migraine makes up 70% of all migraines and has the same pain with no aura.
Migraines without aura (common migraine)
the following are symptoms for what condition: throbbing head pain, nausea, vomiting, photophobia, phonophobia, hands and feet are cold and sweaty, intolerable to odors, tinnitus, blurred vision, auras, and physical activity intensifies the pain.
Migraines
Name several triggers for migraines.
emotions (stress, anxiety, depression, excitement, frustration), foods (MSG, tyramine, phenylethylamine, yellow food coloring, aspartame), drugs (nitroglycerin, cimetidine, cocaine, alcohol, analgesics, birth control, caffeine), weather (barometric pressure changes, low/high temps), estrogen, carbon monoxide, loud noises, hypoglycemia, sleep issues.
These drugs are a first line drug to abort an ongoing migraine attack and are also known as triptans. They can be taken sub Q, intranasal, and orally and work by constricting intracranial blood vessels and suppressing the release of inflammatory neuropeptides (namely the release of calcitonin gene-related peptide (CGRP) in trigeminal pathways.) Adverse effects are usually mild but include heavy arms and chest pressure, coronary vasospasms, and a teratogenic effect demonstrated in rabbits.
Serotonin 1b/1d agonists (sumatriptan or Imitrex)
This drug is used for migraines and has a similar MOA to triptans but is well tolerated. It can also be used for cluster headaches. Adverse effects include nausea, vomiting, numbness, tingling, tachycardia or bradycardia. OD can cause “ergotism” which is all of the side effects mentioned above plus ischemia, cold extremities, and myalgia.
Ergotamine