Term
| How can the plant alkaloid opiate affect the brain? |
|
Definition
| opiate receptor in brain is specific w/ high affinity |
|
|
Term
| What are the 3 opioid receptors? |
|
Definition
1) mu (morphine - agonists & antagonists)
2) kappa (dynorphin - partial agonists)
3) delta (enkephalin) |
|
|
Term
| What opioid receptor genes encode the opioid receptors? |
|
Definition
1) MOP for mu
2) KOP for kappa
3) DOP for delta
(4) NOP for nociceptin/orphanin receptor - insensitive to traditional opioid antagonist) |
|
|
Term
| How many mu opioid receptors are there? |
|
Definition
|
|
Term
| How many delta opioid receptors are there? |
|
Definition
|
|
Term
| How many kappa opioid receptors are there? |
|
Definition
|
|
Term
| What is the gold standard of opioids? |
|
Definition
|
|
Term
| What limits morphine's use as an oral agent? |
|
Definition
| though readily absorbed in all routes, in PO route, extensive first pass metabolism decreases bioavailability to ~35% |
|
|
Term
| What form of avilability can morphone still be used orally? |
|
Definition
| long-acting slow release beads (can't chew or drink EtOH - will cause too much release) |
|
|
Term
| What is added to morphine SR beads to decrease risk of abuse? |
|
Definition
| naltrexone (if crushed, antagonist will be released) |
|
|
Term
| How is morphine excreted? |
|
Definition
kidney - polar metabolites
bile - glucuronide conjugates |
|
|
Term
| What metabolite form of morphine mediates the analgestic effect after long term chronic use? |
|
Definition
|
|
Term
SE
morphine use with renal failure |
|
Definition
|
|
Term
| What metabolite of morphine can cause convulsions? |
|
Definition
|
|
Term
| What morphine receptor primarily mediates the CNS effects of morphine? |
|
Definition
|
|
Term
|
Definition
1) CNS
a) pain releif w/o sensory effects or loss of consciousness
b) euphoria, tranquility
2) miosis
3) cough inhibition
4) resp. depression (dose related)
5) increased ICP
6) N/V
7) decreased BP (vasodilation, decreased resistance) => orthostatic hypotension
8) constipation
9) urinary stasis
10) prolongation of labor
11) itching |
|
|
Term
| What type of pain is morphine a better analgestic for? |
|
Definition
|
|
Term
| What paradoxical event can occur with morphine use? |
|
Definition
| hyper algesia, tho mech. unknown |
|
|
Term
| Why is morphine considered multimodal? |
|
Definition
| It's used as a surgical anesthetic (in combination with other drugs) as well |
|
|
Term
| What is the site of action for morphine as a mood enhancer? |
|
Definition
| Locus coeruleus, mesolimbic DA, nucleus accumbens |
|
|
Term
SE
morphine on pain-free individuals |
|
Definition
dysphoria
difficulty thinking
drowsiness
nausea |
|
|
Term
| When can morphine reduce the risk of PSTD? |
|
Definition
| when administered promptly in combat-injured soldiers |
|
|
Term
|
Definition
|
|
Term
| Why does morphine cause miosis? |
|
Definition
|
|
Term
| What mediates the cough reflex? |
|
Definition
|
|
Term
| For whom is the resp. depression of morphine particularly harmful? |
|
Definition
COPD
synergistic with other drugs |
|
|
Term
| Why does morphine cause increased ICP? |
|
Definition
| vasodilation + increased pCO2 |
|
|
Term
| When is N/V common in patients with morphine use? |
|
Definition
| ambulatory patients (not supine) => suggests a vestibular component |
|
|
Term
| When are CV effects NOT seen in a patient with morphine use? |
|
Definition
|
|
Term
| Why is morphine given to patients with pulmonary edema? |
|
Definition
immediate relief from dyspnea
decrease anxiety
vasodilation
decreased peripheral resistance |
|
|
Term
| What heart failure can cause pulmonary edema? |
|
Definition
|
|
Term
| What can cause morphine toxicity? |
|
Definition
1) iatrogenic overuse
2) renal insufficiency
3) accidental OD
4) suicide attempt |
|
|
Term
|
Definition
1) coma
2) resp. depression
3) pinpoint pupils |
|
|
Term
| How was heroin given it's name? |
|
Definition
| it's heroic i.e. fast acting & potent |
|
|
Term
| What is heroin converted to in vivo via deacetlyation? |
|
Definition
|
|
Term
|
Definition
| painkiller with morphine backbone, just more potent & orally active then morphine (tho with same efficacy) |
|
|
Term
|
Definition
1) ER form in cancer patients, etc.
2) short-term moderate pain (in conjunction) |
|
|
Term
| What is oxycodone used in conjunction with for short-term moderate pain? |
|
Definition
1) APAP
2) aspirin
3) ibuprofen |
|
|
Term
| What form of oxycodone can be lethal (but leads to a big high)? |
|
Definition
|
|
Term
| What is added to oxycodone to stop attempts at crushing them for abuse? |
|
Definition
| acurox = niacin + inactive ingrediants (causes unpleasant Sx & converts to gel upon attempted extraction) |
|
|
Term
|
Definition
| painkiller of rapid onset & short duration |
|
|
Term
| What causes meperidine toxicity? |
|
Definition
| accumulation of long-lived metabolite (therefore now used only for short-term acute pain) |
|
|
Term
|
Definition
Seizures
Twitches
Delirium
Psych changes |
|
|
Term
| Why does codeine have a high oral/parental ratio? |
|
Definition
| largely protected from first pass metabolism |
|
|
Term
| When does codeine display it/s modest analgestic effects? |
|
Definition
| after demethylation to morphine |
|
|
Term
| Why does codeine not work for some patients? |
|
Definition
| ~10% lack enzyme for conversion to morphine |
|
|
Term
| How is codeine most often seen? |
|
Definition
| in combination formulations (tylenol 3, etc) |
|
|
Term
| How does codeine have antitussive effect (cough suppressant)? |
|
Definition
| distinct receptors (efficacy questioned) |
|
|
Term
| What drug is 80-100x more potent than morphine? |
|
Definition
|
|
Term
| What metabolite is fetanyl converted to? |
|
Definition
| no active metabolite (short duration of action) |
|
|
Term
|
Definition
IV surgical anesthesia (w/ droperidol)
acute post-op pain: patient controlled
Opioid dependent:
a) transdermal patch
b) buccal tablet, buccal film, lozenge on a stick for breakthrough pain |
|
|
Term
|
Definition
| oral partial agonist painkiller w/ low therapeutic index |
|
|
Term
| What is propoxyphen used in combination with? |
|
Definition
1) APAP
2) aspirin/caffeine |
|
|
Term
| What causes toxicity of propoxyphen? |
|
Definition
| accumulation of toxic metabolite |
|
|
Term
|
Definition
cardiotoxicity
convulsion
(no longer used, pulled from market in 2010) |
|
|
Term
| What are the 3 kappa opioid agonisits? |
|
Definition
1) Nalbuphine
2) Butorphanol
3) Pentazocine |
|
|
Term
| Do kappa agonists also bind mu opioid receptors? |
|
Definition
| yes, but they can be weak mu agonists or antagonists |
|
|
Term
|
Definition
less analegsia, resp. depression, tolerance, naloxone reversibility
more adverse behavioral effects |
|
|
Term
| What drug is a codeine derivative? |
|
Definition
|
|
Term
| What opioid receptor does tramadol work at? |
|
Definition
|
|
Term
|
Definition
weak mu agonist
blocks 5-HT & NE uptake |
|
|
Term
| How is tramadol different from most other opioids? |
|
Definition
|
|
Term
| Why is tramadol's use mostly limited to chronic pain? |
|
Definition
|
|
Term
| What combinations of tramadol are available? |
|
Definition
1) ER
2) combination with APAP |
|
|
Term
|
Definition
Hx of seizures or anti-depressants (increase frequency of seizures)
any drug that can contribue to serotonin syndrome |
|
|
Term
|
Definition
|
|
Term
|
Definition
weak mu agonist
NE uptake inhibitor (not 5-HT) |
|
|
Term
|
Definition
| abuse, serotonin syndrome (unclear) |
|
|
Term
|
Definition
|
|
Term
| Why does methadone have a long half life? |
|
Definition
| slow metabolism, highly fat soluble |
|
|
Term
| Is methadone safe for patients with renal failure & chronic pain? |
|
Definition
| yes b/c no active metabolites after hepatic metabolism |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| Why does buprenorphine have a long duration of action & is resistant to naloxone reversal? |
|
Definition
| slow dissociation from receptor |
|
|
Term
|
Definition
|
|
Term
|
Definition
| buprenorphine + naloxone (to prevent abuse) |
|
|
Term
|
Definition
| opioid antagonists (mu>kappa, delta) |
|
|
Term
|
Definition
| ER form for opiate overdose |
|
|
Term
|
Definition
oral prevention of EtOH relapse (poor compliance)
Injectible ER prevention of EtOH use
Obesity (mix with buprenorphine) |
|
|
Term
|
Definition
| burprenorphine + naltrexone |
|
|
Term
|
Definition
| injectible for opioid-induced constipation in pallative care (doesn't cross BBB to block pain) |
|
|
Term
SOA
diphenoxylate (plus atropine) & loperamide |
|
Definition
| merperidine congeners with poor absorption => used to Tx diarrhea |
|
|
Term
|
Definition
| D isomer of methylated levorphanol w/o prototypical opioid effects |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
NMDA receptor antagonist
sigma receptor agonist |
|
|
Term
|
Definition
| new kappa opioid receptor agonist |
|
|
Term
|
Definition
reduce substance p induced itching/scratching
reduce itching in hemodialysis |
|
|
Term
| What are the 3 potential uses of opioids that are under investigation? |
|
Definition
1) antidepressant
2) anti-addiction
3) cardioprotective |
|
|
Term
| Why is APAP use restricted with opioid use? |
|
Definition
| potential for hepatotoxicity & OD |
|
|
Term
One of your patients is on an SNRI, but had complaints of back pain & some shooting pain down her legs. To alleviate this pain, she is given tramadol and told to come back in a month for follow up. She has a seizure 2 days later.
What may have happened?
Would it have been OK if she was on an SSRI instead? |
|
Definition
tramadol blocks uptake of 5-HT & NE, so excess NE => seizure in this patient
no anti-depressant should be given in combination with tramadol. With SSRI, patient is likely to experience serotonin syndrome |
|
|
