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Pharm Exam 2
Set 3: Opiates
91
Pharmacology
Graduate
10/22/2011

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Cards

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
3: 1,2,3
Term
How many delta opioid receptors are there?
Definition
2: 1,2
Term
How many kappa opioid receptors are there?
Definition
5: 1a,1b,2a,2b,3
Term
What is the gold standard of opioids?
Definition
morphine
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
morphine-6-glucuronide
Term
SE

morphine use with renal failure
Definition
confusion
Term
What metabolite of morphine can cause convulsions?
Definition
morphione-3-glucuronide
Term
What morphine receptor primarily mediates the CNS effects of morphine?
Definition
mu
Term
Sx

morphine
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
dull continuous
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
SE

morphine in elderly
Definition
confusion/sedation
Term
Why does morphine cause miosis?
Definition
excitation od PS
Term
What mediates the cough reflex?
Definition
medullary cough center
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
supine patient
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
left ventricular
Term
What can cause morphine toxicity?
Definition
1) iatrogenic overuse
2) renal insufficiency
3) accidental OD
4) suicide attempt
Term
Sx

morphine OD
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
morphine
Term
def

oxycodone
Definition
painkiller with morphine backbone, just more potent & orally active then morphine (tho with same efficacy)
Term
SOA

oxycodone
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
snorting or IV use
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
def

meperidine
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
Sx

merperidine toxicity
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
fetanyl
Term
What metabolite is fetanyl converted to?
Definition
no active metabolite (short duration of action)
Term
SOA

fetanyl
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
def

propoxyphen
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
Sx

propoxyphen toxicity
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
Sx

kappa agonists
Definition
less analegsia, resp. depression, tolerance, naloxone reversibility

more adverse behavioral effects
Term
What drug is a codeine derivative?
Definition
tramadol
Term
What opioid receptor does tramadol work at?
Definition
weak mu agonist
Term
MOA

tramadol
Definition
weak mu agonist
blocks 5-HT & NE uptake
Term
How is tramadol different from most other opioids?
Definition
less physical dependence
Term
Why is tramadol's use mostly limited to chronic pain?
Definition
need for slow titration
Term
What combinations of tramadol are available?
Definition
1) ER
2) combination with APAP
Term
CI

tramadol
Definition
Hx of seizures or anti-depressants (increase frequency of seizures)
any drug that can contribue to serotonin syndrome
Term
def

tapentadol
Definition
tramadol-like compound
Term
MOA

tapentadol
Definition
weak mu agonist
NE uptake inhibitor (not 5-HT)
Term
SE

trapentadol
Definition
abuse, serotonin syndrome (unclear)
Term
def

mathadone
Definition
full opioid agonist
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
SOA

methadone
Definition
addict detox/maintenance
Term
def

buprenorphine
Definition
partial mu agonist
Term
Why does buprenorphine have a long duration of action & is resistant to naloxone reversal?
Definition
slow dissociation from receptor
Term
SOA

buprenorphine
Definition
opiate dependence
Term
def

suboxone
Definition
buprenorphine + naloxone (to prevent abuse)
Term
def

naloxone & naltrexone
Definition
opioid antagonists (mu>kappa, delta)
Term
SOA

naloxone
Definition
ER form for opiate overdose
Term
SOA

naltrexone
Definition
oral prevention of EtOH relapse (poor compliance)
Injectible ER prevention of EtOH use
Obesity (mix with buprenorphine)
Term
def

contrave
Definition
burprenorphine + naltrexone
Term
SOA

methylnaltrexone
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
def

dextromethorphan
Definition
D isomer of methylated levorphanol w/o prototypical opioid effects
Term
SOA

dextromethorphan
Definition
antitussive
Term
CI

dextromethorphan
Definition
young children
Term
MOA

dextromethorphan
Definition
NMDA receptor antagonist
sigma receptor agonist
Term
def

nalfurafine
Definition
new kappa opioid receptor agonist
Term
SOA

nalfurafine
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
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