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Pharm opioid analgesics
NOVA spring
43
Pharmacology
Graduate
03/02/2011

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Term
example of full agonist of opioids
partial
and
full antagonist
Definition
full agonist: morphine
partial agonist: codeine M-opioid receptor
full antagonist: naloxone works on m-opioids receptor
Term
wht are 3 major receptors families? where are they located?
Definition
μ (mu), κ (kappa), and δ (delta), each has different specificity
Located on membranes of certain cells in the CNS, on nerve terminals in PNS, and on cells of the GI tract and other regions.
Term
MAO of opioids its bunch so read it from the ppt
Definition
Action potentials reaching the dorsal horn can be attenuated at the presynaptic ending by opioids

Opioids also inhibit the postsynaptic neuron, as do certain neuropeptide antagonists acting at tachykinin (NK1) and other neuropeptide receptors

decrease adenylate cyclase, cAMP
2) increase K+ EFFLUX
3) hyperpolarization
4) decrease Ca INFLUX
5) decrease substance p release
Term
opioid well absorption is via __, ____ and __
Definition
subq, IM and ORal
Term
which two opioid meds have less first pass metabolism than other
Definition
codeine and oxycodone
Term
what do you have to watch out when giving high doses
Definition
accumulation.
once given

Highest concentrations localized in tissue
Brain
Liver
Kidneys
Spleen
Lungs
Term
opioids are secreted via ?
Definition
kidney.
Term
1. fentanyl is metabolized by why enzyme?
2. Codeine, oxycodone, and hydrocodone is metabolized by what enzyme?
Definition
1.CYP3A4

2. P450
Term
what is the medication that is given intrathecally which blocks voltage-gated N-type Ca++ channels for chronic pain
Definition
Ziconotide
Term
can effectivenesss of morphine be lost after freq dosing
Definition
yes..To reproduce the original response, a larger dose must be administered
Term
what is withdrawl or abstinence syndrome?
Definition
Physical dependence is defined as a characteristic withdrawal or abstinence syndrome when a drug is stopped or an antagonist is administered
Term
Persistent administration of opioid analgesics would do what to the body
Definition
hyperalgesia.
increase the sensation of pain
Term
Resp depression is due to
Definition
inhibition of brainstem and Most reliable indicator of this depression is a depressed response to a carbon dioxide challenge
Term
SE of opioid is truncal rigidity...how would u tx the this SE
Definition
give opioid antagonist but then the pain will come back
Term
opioids may produce miosis/mydriasis?
Definition
miosis
Term
what is the effect of opioids on CV, and GI?
Definition
most opioids Bradycardia.
GI: constipation. it is also used in tx of severe diarrhea.
Term
opioids produce hypo/hyper tension and how?
Definition
HYPOTENSION
directly: depresses CNS
indirect: histamine release=peripheral vasodilation....this will also cause pruritis
Term
pain is measured by what?
Definition
VAS: visual analog scale
Term
what are some of the use of opioids?
Definition
Analgesia: severe constant pain, cancer pain
Acute pulmo edema due to LHF
given in MI
cough/ diarrhea/ shivering (All opioids reduce shivering, but meperidine has the most pronounced effect
)
Term
why opioids are good in anesthesia?
Definition
Used prior to surgery and anesthesia due to sedative, anxiolytic and analgesic properties
Term
in epidural opioids are given with what else?
Definition
Fentanyl
Term
Fentanyl patch should be reserved for what type of pt?
Definition
Due to risk of respiratory depression FDA recommends the patch be reserved for patients with an oral morphine requirement of at least 60 mg/day for 1 week or more
Term
what opioid is given intranasally?
Definition
Butorphanol
Term
major SE of opioid
Definition
NV, inc ICP, urticaria, resp depression, constipation, urinary retention
Term
what is opioid rotation?
Definition
A patient who is experiencing decreasing effectiveness of one opioid analgesic regimen is "rotated" to a different opioid analgesic (eg, morphine to hydromorphone; hydromorphone to methadone) and typically experiences significantly improved analgesia at a reduced overall equivalent dosage
Term
S & S of stopping the opioids
Definition
abstinence syndrome:::S/sx: rhinorrhea, lacrimation, yawning, chills, gooseflesh (piloerection), hyperventilation, hyperthermia, mydriasis, muscular aches, vomiting, diarrhea, anxiety, and hostility
Term
morphine and heroin withdrawal signs could last up to how much time?
Definition
5 days but some sx may last for months
Methadone withdraw effect could last for 2 weeks
Term
to prevent dependency and withdrawal sx what should clinician do
Definition
frq evaluate if pt really needs the meds.
limit the refills -- no early refills.
start them on diff analgesic when first present
Term
what is the tx for opioid OD?
Definition
Intravenous injection of naloxone dramatically reverses coma due to opioid overdose but not that due to other CNS depressants
Term
what group of meds could have interaction with opioids?
Definition
sedative-hypnotics
antipsychotic tranquilizers
monoamine oxidase inhibitors
Term
3 strong agonist of M receptors
Definition
morphine, hydromorphone and oxymorphone
Term
which drug blocks MNDA receptors and monoaminergic reuptake transporters. + it is an agonist for Mu receptors.

main use of it
Definition
Methadone

useful in cancer pain
Term
methadone should not be give at interval of no more than how many hrs
Definition
8
Term
methadone is metabolized by what two enzymes in liver. what are some of the side effect if liver is dysfunctional.
Definition
CYP3A4 and CYP2B6 --- associated with overdose effects, including respiratory depression or, more rarely, prolonged QT-based cardiac arrhythmias
Term
which one is better in sense of withdrawal signs, tolerance, physical dependence ...between morphine and methadone
Definition
methadone --Withdrawal signs and symptoms occurring after abrupt discontinuance of methadone are milder, although more prolonged, than those of morphine
Term
what drug is used in tx of opioid abuse
Definition
methadone. its withdrawal, tolerance and physical dependece properties make methadone a useful drug for detoxification and for maintenance of the chronic relapsing heroin addict
Term
what are Mu mild to moderate agonists?
Definition
codeine, oxycodone, dihydrocodeine, and hydrocodone. Less efficacious than morphine (they are partial agonists) or have adverse effects that limit the maximum tolerated dose when one attempts to achieve analgesia comparable to that of morphine
Term
two drugs that are used in tx for diarrhea
Definition
Diphenoxylate + atropine (Lomotil)
Atropine is added in a concentration too low to have a significant antidiarrheal effect but is presumed to further reduce the likelihood of abuse
Loperamide (Imodium)
Does not cross blood brain barrier
Usual dose is two tablets to start and then one tablet after each diarrheal stool
Term
if nalbuphine which is a strong kappa receptor agonist and mu receptor antagonist, is given pt suffer resp depression. PA gives pt naloxone but failed to make pt breath--what happened
Definition
when respiratory depression does occur, it may be relatively resistant to naloxone reversal
Term
what is Buprenorphine used for
Definition
Approved for management of opioid dependence
Term
this drug : blocks both serotonin reuptake and inhibits norepinephrine transporter function, it is believed to be only a weak mu receptor agonist.
Definition
Tramadol -- do not give to pt with seizures
Term
antitussive --opioid derivative
Definition
Dextromethorphan
Term
naltrexone
Definition
longer acting narcan
(antagonist...)
treats narcotic AND ETOH addictions
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