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66 Cards in this Set
- Front
- Back
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What opioid receptor inhibits Ach release, increases prolactin release and has euphoria?
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u1 receptor
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What opioid receptor has problems w/ sedation and hallucinations/ disorientations?
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K receptors
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What suppresses noxious thermal stimuli and modulates the mu receptor?
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delta receptors
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Opioid receptors decrease _________________.
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synaptic transmission
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M3G
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Opioid Induced Myoclonus
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What is the role of Dynorphin in the SC Dorsal horn?
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decreases pain threshold so it ENHANCES pain
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Orexin is co-released with ___________________and ______________________.
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Dynorphin and Glutamate
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Morphine Analogs are based on what 3 things?
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Morphine, Thebaine, Codeine
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Modification via Thebaine would give us what?
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Morphine Analogs
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What is the simplification of chemical structures from morphine called?
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Morphine Analogs
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Fentanyl ___________________ is given for chronic malignant pain.
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transdermal patches
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What is a strong opioid agonists with decreased CV effx but increased respiratory center depression?
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Fentanyl
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what are 2 short acting Fentanyl congeners that is given for short painful procedures?
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Alfentanil, Remifentanil
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Tolerance w/Morphine develops except not ______________, ____________________ or __________________________.
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Miosis, constipation, pruritis
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What opioid would cause testerosterone and cortisol in plasma to drop?
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Morphine
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M6G analgesic?
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Morphine
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What is the metabolite of morphine?
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glucornide
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Morphine is used on what type of pain?
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ACUTE PAIN ONLY
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What opioid agonists exhibits CNS excitation and produces normeperidine?
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Meperidine
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post anesthetic shivering?
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Meperidine
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what are the withdrawal symptoms of Opioid Analgesics?
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FLU
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Tramadol can increase mood and decrease pain by blocking _______________________.
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NE and 5HT reuptake
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____________________ : only 10% go thru first pass metabolism to morphine.
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Codeine
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Absence of pain sensation?
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Analgesia
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Absence of ALL sensation?
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Anesthesia
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Why does rubbing a boo boo make it better?
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activates inhibitory local circuit neurons to decrease pain
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What is the MOA of opioids at the presynapse?
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decreases amount of Ca+ entry so less NT are released
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What is the MOA of opioids at the postsynapse?
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increase in K+ efflux so become hyperpolarized
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Opioid receptors activate G proteins----________________ inhibited----------------decrease in cAMP
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adenyl cyclase
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What is the fxn of Meperidine congeners?
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tx diarrhea
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Why do patients die from opioids?
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decreases their sensitization to CO2 and they don't breathe and thus die
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What are the Meperidine congeners that tx diarrhea?
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Diphenoxylate; Loperamide
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Why are antagonists added to opioids?
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to prevent drug abuse. If taken correctly-- get agonist form, if taken incorrectly get antagonist form
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What is the single highest prescribed drug in the USA?
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Hydrocodone
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What is a partial m agonist, used to treat physical dependence and block withdrawal?
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Buprenophine
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What is an narcotic antagonists that can reverse the effect of agonists/antagonists of ANY group>
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Naloxone HCl
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What is a pure antagonists that must be high monitored if administered?
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Naloxone-- give just enough to make them breathe, if any more than they will die
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What drug must you closely closely regulate---Naloxone or Naltrexone?
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Naloxone
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What has no tolerance, is a full mu agonists, and can kill a pt? We give Buprenorphine.
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Methadone
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What are some opioid overdose signs?
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miosis, cyanosis
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Analgesia possibilites suggested by what neuro tract?
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Anterolateral tract
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Why does Morphine cause nausea and vomitting?
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stimulation of CTZ (in area postrema). Involved in motion sickness.
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What are the cardiovascular effects of morphine?
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release of histamine and suppression of central adrenergic tone and suppress reflex vasocontstriciton= VASODILATION= decrease in BP
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Why do pts on Morphine feel urinary urgency?
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tone of detrusor muscle is increased. have urinary retention due to increased muscle tone when sphincter is closed off
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Morphine has what effect on your respiration?
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Bronchocontriction
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Where are most opioids absorbed?
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in GI tract. also undergo a high rate of first pass metabolism. Highly lipophilic opiates absorbed transdermally
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What are 2 Piperidines?
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Alfentanil, Remifentanil
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Most opiates are converted to Glucuronides or N-demethylated via ________________.
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Hepatic Conjugation
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Fentanyl is metabolized by ____________________.
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Cytochrome P450
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What is the Acute Morphine Poisoning Triad?
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Coma, Miosis, Cyanosis (also have asphyxia, pupils dilate, biliary spasms, GI smooth muscle spasm, pulmonary edema, muscle twitches, peripheral vasodilation, hypotension)
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What is the Morphine LD?
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0.2 gm parenterally
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Give 2 examples of Intrabuccal Fentanyl.
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Oralet ---to kids
Actiq ---Cx pts. w/ breakthru pain |
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When does Intrabuccal Fentanyl take effect and for how long?
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within 15-20 minutes and lasts 1-2 hours
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What is used for moderate pain and as an antitussive?
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Codeine
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What is Tramadol MOA?
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NE and 5HT Reuptake Blockade.
weak mu agonist, racemic mixture, BIOAVAILABLE! |
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What are some SE w/Tramadol?
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nausea/vomitting, dizzy, sedation, HA, seizures
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What is a synthetic drug that is similar to codeine?
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Hydrocodene (more potent than codene)
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What is the def. for Tolerance?
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larger doses required for equivalent effect w/repeat administration
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What is the def. of Physical Dependence?
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body adapts to continuous exposure so that the drug is required for NORMAL fxn
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What is a mixed agonists/antagonist that is K agonists/delta partial agonist?
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Pentazocine---shorter duration but faster onset
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What is a mixed opioid receptor that is Mu partial agonist/Mu and Delta antagonist?
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Buprenophine---LONG acting phenanthrene derivative
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What is a moderate receptor agonists that is chemically related to Methadone?
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D-Propoxyphene
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What do high doses of D-propoxyphene cause?
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CNS stimulation, convulsions, respiratory depression, hallucations, confusion, coma
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What is given for Opioid induced constipation?
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methylnaltrexone
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What is a contraindication for Methylnaltrexone?
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mechanical bowel obstruction
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What are 3 warnings to remember w/Methylnaltrexone?
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1. stop if opioids are stopped
2. dizziness 3. additive effx if also used w/SSRIs, lithiu., carbamazepine, or valproic acid |
